Page last updated: 2024-12-05

diclofenac

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Description

Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation. It is synthesized from the compound 2,6-dichloroaniline through a series of chemical reactions. Diclofenac works by inhibiting the production of prostaglandins, chemicals in the body that cause pain and inflammation. It is effective in treating various conditions, including osteoarthritis, rheumatoid arthritis, and acute pain. Diclofenac is widely studied due to its effectiveness in managing pain and its relatively low cost. Research continues to explore its potential side effects and long-term safety.'

Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID3033
CHEMBL ID139
CHEBI ID47381
SCHEMBL ID2799
MeSH IDM0006284

Synonyms (168)

Synonym
BIDD:GT0380
AB01275502-01
BRD-K08252256-236-05-6
2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid
gtpl2714
2-((2,6-dichlorophenyl)amino)benzeneacetic acid
dichlofenac
2-[2-(2,6-dichloroanilino)phenyl]acetic acid
DIVK1C_000402
KBIO1_000402
DIVK1C_000272
KBIO1_000272
{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
benzeneacetic acid, 2-((2,6-dichlorophenyl)amino)-
einecs 239-348-5
hsdb 7234
prosorb-d
brn 2146636
diclophenac
diclofenacum [inn-latin]
dicrofenac
dichlofenal
diclofenaco [inn-spanish]
SPECTRUM_000930
BSPBIO_002169
OPREA1_011155
BSPBIO_000468
SPECTRUM5_000867
LOPAC0_000441
acetic acid, (o-(2,6-dichloroanilino)phenyl)-
benzeneacetic acid, 2-[(2,6-dichlorophenyl)amino]-
UNM000001216103
PRESTWICK3_000594
BPBIO1_000516
DIF ,
2-[2,6-dichlorophenyl)amino]benzeneacetic acid
diclofenac
15307-86-5
C01690
DB00586
2B17
[2-(2,6-dichloroanilino)phenyl]acetic acid
diclofenac acid
solaraze (tn)
PRESTWICK2_000594
IDI1_000272
diclofenaco
2-[(2,6-dichlorophenyl)amino]benzeneacetic acid
diclofenacum
diclofenamic acid
CHEBI:47381 ,
KBIO2_006546
KBIOGR_002306
KBIO2_007442
KBIO2_001410
KBIO2_004874
KBIOGR_001051
KBIOSS_001410
KBIO2_002306
KBIO3_001389
KBIO2_003978
KBIO3_002786
KBIOSS_002308
SPBIO_002687
PRESTWICK1_000594
SPECTRUM2_000991
SPECTRUM4_000506
NINDS_000402
NINDS_000272
PRESTWICK0_000594
SPECTRUM3_000385
SPBIO_001081
CMAP_000014
IDI1_000402
NCGC00021125-01
chembl139 ,
bdbm13066
2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
HMS2090C10
D3748
2-(2,6-dichloroanilino)phenylacetic acid
las-41007
diclofenac free acid
las41007
AKOS001579542
STK984493
zorvolex (tn)
D07816
diclofenac (usan/inn)
HMS501E04
FT-0666643
NCGC00021125-02
ec 239-348-5
144o8ql0l1 ,
unii-144o8ql0l1
diclofenac [usan:inn:ban]
olfen
zorovolex
zorvolex
diclofenac resinate
isv-205
FT-0624731
aceclofenac impurity a [ep impurity]
diclofenac [orange book]
(o-(2,6-dichloroanilino)phenyl)acetic acid
diclofenac [inn]
diclofenac [vandf]
diclofenac [hsdb]
diclofenac [mart.]
diclofenac [who-dd]
diclofenac [mi]
(2-((2,6-dichlorophenyl)amino)phenyl)acetic acid
diclofenac [usan]
EPITOPE ID:116873
S6073
HY-15036
2-(2-((2,6-dichlorophenyl)amino)phenyl)acetic acid
SCHEMBL2799
KS-1258
[2-(2,6-dichloro-phenylamino)-phenyl]-acetic acid
2-[(2,6-dichlorophenyl)amino]-benzeneacetic acid
2-[2-(2,6-dichlorophenylamino)-phenyl]-acetic acid
2-[(2,6-dichlorophenyl)amino]-phenyl-acetic acid
2-[(2,6-dichlorophenyl)-amino]-benzeneacetic acid
[o-(2,6-dichloro-anilino)-phenyl]-acetic acid
2-[(2,6-dichlorophenyl)-amino]-phenyl-acetic acid
o-(2,6-dichloroanilino)phenylacetic acid
2-[(2,6-dichlorophenyl)amino]phenylacetic acid
2-[2-(2,6-dichlorophenylamino)phenyl]-acetic acid
mfcd00056694
F0722-0745
smr001550371
MLS006011795
[2-(2,6-dichloroanilino)phenyl]acetic acid #
AC-27673
AB01275502_02
DTXSID6022923 ,
SR-01000003041-3
SBI-0051341.P003
2-[2-(2,6-dichlorophenyl)aminophenyl]ethanoic acid
Z57664869
2-(2-(2,6-dichlorophenylamino)phenyl)acetic acid
Q244408
128402-48-2
BCP13860
BCP09087
BRD-K08252256-236-17-1
NCGC00021125-11
HMS3886F09
SY038623
enfenamic acid; n-phenethylanthranilic acid; rh 8
H10425
2-[2-(2,6-dichloroanilino)phenyl]acetic acid.
(2-((2,6-dichlorophenyl)amino-phenyl)acetic acid (hd)
15307-86-5 (free)
2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid (diclofenac)
EN300-119509
diclofenac 1000 microg/ml in acetonitrile
m01ab05
s01bc03
aceclofenac impurity a (ep impurity)
diclofenac (mart.)
dtxcid802923
m02aa15
(2-(2,6-dichloroanilino)phenyl)acetic acid
s17 - pharmaceuticals
57 - pharmaceuticals
am01 - analgesic mixture

Research Excerpts

Overview

Diclofenac (DCF) is a highly consumed non-steroidal anti-inflammatory drug. It is excreted partially metabolized and is poorly removed during wastewater treatment. The drug is considered a prominent contaminant in surface and groundwater worldwide.

ExcerptReferenceRelevance
"Diclofenac (DIC) is a commonly prescribed NSAID that is known to increase the risk of cardiovascular diseases."( Chronic Diclofenac Exposure Increases Mitochondrial Oxidative Stress, Inflammatory Mediators, and Cardiac Dysfunction.
Chiamvimonvat, N; Gomes, AV; Haddad, M; Hammock, BD; Nader, CE; Overton, J; Ren, L; Sirish, P; Thai, PN; Timofeyev, V; Xu, W; Yang, J, 2023
)
2.07
"Diclofenac (DCF) is a highly consumed non-steroidal anti-inflammatory drug that is excreted partially metabolized and is poorly removed during wastewater treatment. "( Nitrosation and nitration of diclofenac and structurally related nonsteroidal anti-inflammatory drugs (NSAIDs) in nitrifying activated sludge.
Cruz-Alcalde, A; Osorio, V; Pérez, S, 2022
)
2.46
"Diclofenac (DCF) is a very common pharmaceutical that, due to its high use and low removal rate, is considered a prominent contaminant in surface and groundwater worldwide. "( Specific glutathione-S-transferases ensure an efficient detoxification of diclofenac in Solanum lycopersicum L. plants.
Azenha, M; Fidalgo, F; Leal, A; Lopes, J; Martins, M; Soares, C; Sousa, B; Teixeira, J, 2021
)
2.29
"Diclofenac is a pharmaceutical active compound frequently detected in wastewater and water bodies, and often reported to be persistent and difficult to biodegrade. "( Diclofenac biotransformation in the enhanced biological phosphorus removal process.
Bronze, MR; Carvalho, G; Freitas, EB; Kolakovic, S; Oehmen, A; Reis, MAM; Salgado, R; Sekulic, MT, 2022
)
3.61
"Diclofenac (DCF) is a common pharmaceutical that widely distributed in natural waters, and has been received an increasing attention because of its potential toxicity. "( Sorption of diclofenac by polystyrene microplastics: Kinetics, isotherms and particle size effects.
Ding, T; Hou, Z; Huang, X; Li, J, 2022
)
2.54
"Diclofenac is an important pharmaceutical present in the water cycle of wastewater treatment and one of the most distributed drugs in aquatic ecosystems. "( Effects of Diclofenac on the Reproductive Health, Respiratory Rate, Cardiac Activity, and Heat Tolerance of Aquatic Animals.
Berezina, NA; Chernova, EN; Malysheva, OA; Sharov, AN, 2022
)
2.55
"Diclofenac is an anti-inflammatory drug and has been frequently detected from the wastewater. "( Diclofenac removal from the wastewater using activated sludge and analysis of multidrug resistant bacteria from the sludge.
Al-Khattaf, FS; Almaary, KS; Elshikh, MS; Hussein, DS; Rasheed El-Naggar, RA, 2022
)
3.61
"Diclofenac is a widely prescribed anti-inflammatory drug having cardiovascular complications as one of the main liabilities that restrict its therapeutic use. "( Ameliorating effect of rutin against diclofenac-induced cardiac injury in rats with underlying function of FABP3, MYL3, and ANP.
Bag, S; Bhardwaj, M; Dhiman, SK; Dogra, A; Gour, A; Kour, D; Kumar, A; Nandi, U; Singh, G, 2023
)
2.63
"Diclofenac sodium is a widely used nonsteroidal anti-inflammatory drug (NSAID) as over-the-counter (OTC) medication for the treatment of inflammatory diseases. "( Six-Step Continuous Flow Synthesis of Diclofenac Sodium via Cascade Etherification/Smiles Rearrangement Strategy: Tackling the Issues of Batch Processing.
Chen, F; Cheng, D; Jiang, M; Li, W; Liu, M; Wan, L; Wang, L, 2022
)
2.44
"Diclofenac (DCF) is a pharmaceutically active contaminant frequently found in aquatic ecosystems. "( Organohalide Respiration with Diclofenac by
Cui, Y; Jin, H; Li, X; Song, Y; Wang, J; Yan, J; Yang, Y; Zhang, Y, 2022
)
2.45
"Diclofenac (DFC) is a pharmacologically active compound frequently detected in various receiving waters. "( Wetland plant-derived biochar enhances the diclofenac treatment performance in vertical subsurface flow constructed wetlands.
Han, J; Qin, N; Wang, H; Wu, B; Xu, D; Xu, R, 2022
)
2.43
"Diclofenac is an emerging surface water contaminant, yet the environmental impact of its degradation products remains elusive. "( Fate, transformation and toxicological implications of environmental diclofenac: Role of mineralogy and solar flux.
Ellepola, N; Patidar, PL; Rubasinghege, G; Viera, T, 2022
)
2.4
"Diclofenac sodium is an anti-inflammatory drug commonly used to cure pain in various treatments. "( Development of zinc ferrite nanoparticles with enhanced photocatalytic performance for remediation of environmentally toxic pharmaceutical waste diclofenac sodium from wastewater.
Bilal, M; Hussain, N; Imran, M; Javaid, A; Jesionowski, T; Latif, S; Liaqat, A, 2023
)
2.55
"Diclofenac sodium is a commonly used drug for the treatment of joint diseases, but simple administration is often affected by drug clearance and rapid metabolism."( Intra-articular delivery of antioxidative polymer-based nanospheres reduces intracellular reactive oxygen species in macrophages and alleviates cartilage damage in a rat model.
Ju, C; Qi, C; Rong, L; Zhang, G, 2023
)
1.63
"Diclofenac (DF) is a non-steroidal anti-inflammatory drug (NSAID) generally prescribed for the treatment of pain. "( Chrysin mitigates diclofenac-induced hepatotoxicity by modulating oxidative stress, apoptosis, autophagy and endoplasmic reticulum stress in rats.
Ayna, A; Caglayan, C; Genç, A; Gür, C; Kandemir, FM; Taysı, S; Varışlı, B, 2023
)
2.69
"Diclofenac is a widely used analgesic, anti-inflammatory, antipyretic drug. "( Kounis Syndrome Associated With the Use of Diclofenac.
Davidovic, G; Folic, MM; Folic, ND; Jankovic, S; Milosavljevic, MN; Pejcic, AV, 2023
)
2.62
"Diclofenac is an emerging pollutant: toxic, persistent, and bioaccumulative, present in several environmental niches in a concentration of parts per million. "( Assessing three industrially produced fungi for the bioremediation of diclofenac.
Balderas-Hernández, VE; Blanco-Orta, MF; García-de la Cruz, RF; González-Ortega, O; Morales-Avila, MM; Paz-Maldonado, LMT; Pedraza-González, DA; Pérez-Martínez, AS, 2023
)
2.59
"Diclofenac (DCF) is a pharmaceutical contaminant of water bodies and therefore, improvement of analytical techniques for its removal and quantitation is one of the current interests of analysts. "( Selective quantification of diclofenac from groundwater and pharmaceutical samples by magnetic molecularly imprinted polymer-based sorbent coupled with the HPLC-PDA detection.
Kaur, V; Mohiuddin, I; Singh, R; Thakur, S, 2023
)
2.65
"Diclofenac sodium (DIC) is a pain reliever and anti-nociceptive medication. "( Natural sporopollenin microcapsules: biological evaluation and application in regulating hepatic toxicity of diclofenac sodium
Dyab, AKF; Meligi, NM, 2023
)
2.57
"Diclofenac (DIC) is a non-steroidal anti-inflammatory drug with a potential nephrotoxic effect."( Podocin, mTOR, and CHOP dysregulation contributes to nephrotoxicity induced of lipopolysaccharide/diclofenac combination in rats: Curcumin and silymarin could afford protective effect.
Alhindi, A; Almalki, H; Badr, A; Hasan, IH; Mostafa, HS, 2023
)
1.85
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) from the group of phenylacetic acid derivatives, which has analgesic, anti-inflammatory and antipyretic properties. "( Spin-Labeled Diclofenac: Synthesis and Interaction with Lipid Membranes.
Atnyukova, AN; Baranov, DS; Dzuba, SA; Kashnik, AS, 2023
)
2.72
"Diclofenac sodium (DS) is an emerging contaminant that is toxic and remains at high concentrations in natural aquatic environments. "( Fabrication of cross-linked chitosan beads grafted by polyethylenimine for efficient adsorption of diclofenac sodium from water.
Huang, F; Ji, C; Liu, Y; Lu, Y; Ouyang, XK; Wang, Z; Yang, LY, 2020
)
2.22
"Diclofenac is a widely used nonsteroidal anti-inflammatory drug. "( Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters.
Huo, X; Liu, K; Ma, X; Meng, Q; Sun, H; Wang, C; Wu, J; Zhu, Y, 2020
)
2.27
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID), whose wide use contributes for its presence in freshwater ecosystems, increasing the probability of causing deleterious changes in aquatic biota."( Acute effects of diclofenac on zebrafish: Indications of oxidative effects and damages at environmentally realistic levels of exposure.
Bio, S; Nunes, B, 2020
)
1.62
"Diclofenac is a NSAID with preferred activity on COX-2 isozymes, but additionally, other targets may be implicated in its analgesic activity."( Spinal Actions of the NSAID Diclofenac on Nociceptive Transmission in Comparison to the K
Rivera-Arconada, I; Vicente-Baz, J, 2020
)
1.57
"Diclofenac (DCF) is a widely used nonsteroidal anti-inflammatory drug, but it comes with a high risk of drug-induced liver injury (DILI). "( Roles of diclofenac and its metabolites in immune activation associated with acute hepatotoxicity in TgCYP3A4/hPXR-humanized mice.
Dai, R; Dai, T; Ding, L; Huang, L; Jiang, W; Xie, S, 2020
)
2.42
"Diclofenac (DIC) is an NSAID and consumption of this drug creates side effects such as liver injury. "( Gallic acid mitigates diclofenac-induced liver toxicity by modulating oxidative stress and suppressing
Esmaeilzadeh, M; Heidarian, E; Moradi, A; Najafi, M; Nouri, A; Roshanmehr, H; Shaghaghi, M, 2020
)
2.32
"Diclofenac is a non-steroidal anti-inflammatory drug widely used by the general population and, although generally contraindicated during pregnancy, it is also used by some pregnant women. "( Prenatal diclofenac exposure delays pubertal development and induces behavioral changes in rats.
Curi, TZ; da Silva, GN; Dos Santos, AC; Grechi, N; Hey, GS; Krebs Ribeiro, DC; Martino-Andrade, AJ; Meldola, H; Passoni, MT; Ramos, ATA; Souza, RIC; Spercoski, KM; Tolouei, SEL, 2020
)
2.42
"Diclofenac sodium (DS) is a widely used nonsteroidal anti-inflammatory drug. "( The effect of diclofenac sodium intoxication on the cardiovascular system in rats.
Dolanbay, T; Gul, HF; Karakurt, E; Makav, M, 2021
)
2.42
"Diclofenac (DIC) is a Nonsteroidal anti-inflammatory drug (NSAID) and consumption of this drug creates side effects such as renal injury. "( Gallic Acid Exerts Nephroprotective, Anti-Oxidative Stress, and Anti-Inflammatory Effects Against Diclofenac-Induced Renal Injury in Malerats.
Abolfathi, M; Heidarian, E; Javadian, M; Khaledi, M; Moradi, A; Nouri, A; Roshanmehr, H, 2021
)
2.28
"Diclofenac sodium (DCF) is a non-steroidal anti-inflammatory drug. "( Optimization of the adsorption of diclofenac by activated carbon and the acidic regeneration of spent activated carbon.
Durna, E; Erkişi, E; Genç, N, 2021
)
2.34
"Diclofenac is a drug commonly used in human and veterinary medicine for the treatment of diseases associated with inflammation and pain. "( Diclofenac-induced cytotoxicity in cultured carp leukocytes.
Nemcova, M; Pikula, J; Seidlova, V; Zukal, J, 2020
)
3.44
"Diclofenac is an effective nonsteroidal anti-inflammatory drug and one of the most prescribed medicines worldwide. "( Effect of diclofenac on semen quality: A review.
Banihani, SA, 2021
)
2.47
"Diclofenac is a worldwide consumed drug included in the watch list of substances to be monitored according to the European Union Water Framework Directive (Directive 2013/39/EU). "( Biological removal processes in aerobic granular sludge exposed to diclofenac.
Bessa, VS; Castro, PML; Moreira, IS; Van Loosdrecht, MCM, 2022
)
2.4
"Diclofenac is a non-steroidal anti-inflammatory drug discovered several decades ago, which has since been used by an estimated one billion patients and has demonstrated an acceptable safety profile. "( Comprehensive review of genotoxicity data for diclofenac.
Elhajouji, A; Erkman, L; Hartmann, A; Maremanda, N; Martus, HJ, 2021
)
2.32
"Diclofenac is an anti-inflammatory drug used as an analgesic. "( Hazardous impact of diclofenac on mammalian system: Mitigation strategy through green remediation approach.
Balasubramanian, M; Brar, SK; Chitra, L; Ganesan, AR; Gu, FL; Meena, RAA; Mohan, K; Palvannan, T; Sathishkumar, P, 2021
)
2.39
"Diclofenac sodium 0.1% is a commonly used NSAID with well-documented clinical efficacy in reducing postoperative inflammation; however, its corneal tolerability and ophthalmic tissue bioavailability require further improvement. "( Design of ophthalmic micelles loaded with diclofenac sodium: effect of chitosan and temperature on the block-copolymer micellization behaviour.
Dodov, MG; Geskovski, N; Gorachinov, F; Goracinova, K; Koummich, SA; Makreski, P; Zoukh, IM, 2022
)
2.43
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) used in livestock farming, with lethal effects on vultures when reaching high concentrations in the carcasses they feed on. "( The veterinary use of diclofenac and vulture conservation in Spain: Updated evidence and socio-ecological implications.
Aymerich, M; Carapeto, R; Casimiro, R; Moreno, I; Moreno-Opo, R; Muñoz, B; Rubio, C, 2021
)
2.38
"Diclofenac 3% gel is a widely used topical treatment with proven efficacy in reducing the burden of actinic keratosis (AK); however, clinical benefit might not fully translate in clinical practice as nonadherence is substantial for prolonged treatment regimens. "( Treatment adherence with diclofenac 3% gel among patients with multiple actinic keratoses: an integrated low-intensity intervention program versus standard-of-care.
Bianchi, L; Calzavara-Pinton, P; Campione, E; Carbone, A; Casari, A; Esposito, M; Fargnoli, MC; Fattori, A; Frascione, P; Pellacani, G; Perino, F; Peris, K; Piccerillo, A; Rossi, MT, 2022
)
2.47
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of growing concern in aquatic environments worldwide; nevertheless, knowledge of its effects on aquatic biota is restricted to a few model species with limited information regarding its mechanisms of impact. "( Acute exposure to an environmentally relevant concentration of diclofenac elicits oxidative stress in the culturally important galaxiid fish Galaxias maculatus.
Brooks, BW; Burket, SR; Gaw, S; Glover, CN; McRae, NK, 2018
)
2.16
"Diclofenac sodium is a widely used nonsteroidal anti-inflammatory drug (NSAID) for relief of inflammatory pain. "( Submucosal Diclofenac for Acute Postoperative Pain in Third Molar Surgery: A Randomized, Controlled Clinical Trial.
Ahmed, B; Bulsara, Y; Dietrich, T; Gorecki, P; Pearson, D; Rainsford, KD; Saund, D; Taneja, P, 2018
)
2.31
"Diclofenac is a non-steroidal anti-inflammatory drug which is used in the treatment of pain and arthritis."( Diclofenac-induced renal toxicity in female Wistar albino rats is protected by the pre-treatment of aqueous leaves extract of Madhuca longifolia through suppression of inflammation, oxidative stress and cytokine formation.
Evan Prince, S; S, JP, 2018
)
2.64
"Diclofenac (DCF) is a widely used non-steroidal anti-inflammatory pharmaceutical which is detected in the environment at concentrations which can pose a threat to living organisms. "( Biodegradation of Diclofenac by the bacterial strain Labrys portucalensis F11.
Bessa, VS; Castro, PML; Mascolo, G; Moreira, IS; Murgolo, S; Piccirillo, C, 2018
)
2.26
"Diclofenac is a widely used analgesic so that exposure during pregnancy may frequently occur. "( Safety of diclofenac use during early pregnancy: A prospective observational cohort study.
Dathe, K; Hultzsch, S; Linsenmeier, V; Meister, R; Meixner, K; Padberg, S; Schaefer, C; Tissen-Diabaté, T, 2018
)
2.33
"Diclofenac is a Non-Steroidal Anti-inflammatory drug which is used as an analgesic. "( Aqueous leaves extract of Madhuca longifolia attenuate diclofenac-induced hepatotoxicity: Impact on oxidative stress, inflammation, and cytokines.
Evan Prince, S; Simon, JP, 2018
)
2.17
"Diclofenac is a non-steroidal antiinflammatory drug. "( Formation of a Toxic Quinoneimine Metabolite from Diclofenac: A Quantum Chemical Study.
Bharatam, PV; Ramesh, M, 2019
)
2.21
"Diclofenac is a preferential cyclooxygenase 2 inhibitor (COX-2) and member of non-steroidal anti-inflammatory drugs (NSAIDs). "( Diclofenac induced apoptosis via altering PI3K/Akt/MAPK signaling axis in HCT 116 more efficiently compared to SW480 colon cancer cells.
Arisan, ED; Bozdağ, G; Çoker-Gürkan, A; Coşkun, D; Ergül, Z; Obakan-Yerlikaya, P; Palavan-Ünsal, N; Rencüzoğulları, Ö, 2018
)
3.37
"As diclofenac is an over-the-counter drug, its use among patients cannot be monitored by health teams in follow-up sessions."( In vitro evaluation of the interchangeability of different brands of diclofenac sodium tablets available in the Colombian market
Baena, Y; Matiz, GE; Pérez, DA; Trujillo, M, 2018
)
1.23
"Diclofenac is a potent NSAID of clinical choice, which is widely used for containing inflammation. "( Molecular docking of anti-inflammatory drug diclofenac with metabolic targets: Potential applications in cancer therapeutics.
Goel, Y; Pandey, SK; Singh, SM; Singh, VK; Temre, MK; Yadav, S, 2019
)
2.22
"Diclofenac (DIC) is a new type of contaminant that has been widely detected in the water environment, posing threats to the ecological environment and human health. "( Removal of diclofenac by three-dimensional electro-Fenton-persulfate (3D electro-Fenton-PS).
Chen, H; Feng, Y; Li, X; Long, Y; Suo, N; Wang, Z; Yu, Y, 2019
)
2.35
"Diclofenac (DFC) is a common anti-inflammatory drug, and has attracted the significant attention due to its massive use around the world and its environmental impact. "( Evaluation of diclofenac biodegradation by the ascomycete fungus Penicillium oxalicum at flask and bench bioreactor scales.
Aranda, E; Camacho-Morales, RL; González-López, J; Olicón-Hernández, DR; Pozo, C, 2019
)
2.32
"diclofenac is a commonly used drug in the emergency department, we urge emergency physicians to be aware of the existence of this potentially fatal diclofenac-related adverse drug effect."( Acute ST-Segment Elevation Myocardial Infarction Following Intramuscular Diclofenac: A Case of Kounis Syndrome.
AlAli, A; Raja, R; Rajah, F; Rajh, F, 2019
)
1.47
"Diclofenac (DIC) is a phenyl acetic acid derivative which is well known for its analgesic and anti-inflammatory. "( Hepatoprotective effects of silymarin against diclofenac-induced liver toxicity in male rats based on biochemical parameters and histological study.
Heidarian, E; Nouri, A, 2021
)
2.32
"Diclofenac is a commercial non-steroidal anti-inflammatory drug commonly present as a pollutant in naturally occurring water sources and wastewaters. "( Magnetic nanotechnology for diclofenac remediation: molecular basis of drug adsorption and neurobehavioral toxicology as a preliminary study for safe application.
Agotegaray, MA; Ferreira, ML; Gumilar, F; Lassalle, VL, 2021
)
2.36
"Diclofenac potassium is a non-steroidal anti-inflammatory drug that is used to treat pain."( Diclofenac-induced thrombotic thrombocytopenic purpura with concomitant complement dysregulation: a case report and review of the literature.
Ali, A; Gaddam, M; Khaja, M; Lara, JP; Malik, S; Santana, Y, 2019
)
2.68
"Diclofenac (DF) is a widely used non-steroidal anti-inflammatory drug for the treatment of rheumatic disorders, but is often associated with liver injury. "( Urinary proteomic profiling reveals diclofenac-induced renal injury and hepatic regeneration in mice.
Laarakkers, CM; Masereeuw, R; Pertijs, JC; Russel, FG; van Swelm, RP; Verweij, V, 2013
)
2.11
"Diclofenac is an established analgesic, and new formulations using the potassium or epolamine salts, which can be dissolved in water, have been developed for rapid absorption, which may be beneficial in acute migraine."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2013
)
2.55
"Diclofenac is an effective and well-tolerated nonsteroidal anti-inflammatory drug (NSAID) frequently used in the treatment of acute pain. "( Efficacy and safety of low dose subcutaneous diclofenac in the management of acute pain: a randomized double-blind trial.
Dietrich, T; Gugliotta, B; Leeson, R; Petersen, B, 2014
)
2.1
"Diclofenac sodium is a 2-arylacetic acid, nonsteroidal anti-inflammatory drug. "( Anaphylaxis after intramuscular injection of diclofenac sodium.
Afacan, MA; Ayranci, M; Colak, S; Erdogan, MO; Gunes, H; Kandis, H; Saritas, A, 2014
)
2.1
"Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. "( Comparison of skin permeability for three diclofenac topical formulations: an in vitro study.
Derendorf, H; Folzer, E; Gonzalez, D; Singh, R, 2014
)
2.11
"Diclofenac (DCF) is a common anti-inflammatory pharmaceutical that is often detected in waste wasters, effluents and surface waters. "( Fate of diclofenac in municipal wastewater treatment plant - a review.
Sillanpää, M; Vieno, N, 2014
)
2.28
"Diclofenac sodium is a nonsteroidal anti-inflammatory drug and is effective in the management of pain following periodontal surgery. "( Comparative evaluation of transdermal diclofenac patch with oral diclofenac as an analgesic modality following root coverage procedures.
Khaleelahmed, S; Prabhuji, ML; Tejaswi, DV,
)
1.85
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and anti-pyretic properties. "( Evaluation of developmental toxicity and teratogenicity of diclofenac using Xenopus embryos.
Chae, JP; Hwang, YS; Kim, SH; Lee, HS; Min, BH; Park, MJ; Park, MS, 2015
)
2.1
"Diclofenac (DCF) is a widely used anti-inflammatory drug found in various water bodies, posing threats to human health. "( Degradation of diclofenac by ultrasonic irradiation: kinetic studies and degradation pathways.
Luo, X; Nie, E; Wang, D; Yang, M; Yang, X; Zheng, Z, 2014
)
2.2
"Diclofenac is a nonsteroidal anti-inflammatory drug. "( Structural basis for the 4'-hydroxylation of diclofenac by a microbial cytochrome P450 monooxygenase.
Arakawa, T; Fushinobu, S; Ikeda, H; Liu, L; Shoun, H; Wakagi, T; Xu, LH, 2015
)
2.12
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, antinociceptive, and antipyretic activities. "( Evaluation of antinociceptive activity of nanoliposome-encapsulated and free-form diclofenac in rats and mice.
Chiong, HS; Goh, JZ; Hakim, MN; Tang, SN; Yong, YK; Zuraini, A, 2015
)
2.09
"Diclofenac (DCF) is a nonsteroidal anti-inflammatory drug commonly prescribed to reduce pain in acute and chronic inflammatory diseases. "( Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac.
Csanaky, IL; Goedken, MJ; Manautou, JE; Scialis, RJ, 2015
)
2.07
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class with anti-inflammatory, analgesic, and antipyretic properties. "( Advances in NSAID development: evolution of diclofenac products using pharmaceutical technology.
Altman, R; Bosch, B; Brune, K; Patrignani, P; Young, C, 2015
)
2.12
"Diclofenac is a nonsteroidal anti-inflammatory drug, available as a potassium salt (immediate release) or sodium salt (enteric coated to suppress dissolution in the stomach). "( Single dose oral diclofenac for acute postoperative pain in adults.
Derry, S; Moore, RA; Wiffen, PJ, 2015
)
2.2
"Diclofenac (DCLF) is a widely used non-steroidal anti-inflammatory drug that is associated with idiosyncratic, drug-induced liver injury (IDILI) in humans. "( Calcium Contributes to the Cytotoxic Interaction Between Diclofenac and Cytokines.
Breier, AB; Ganey, PE; Maiuri, AR; Roth, RA; Turkus, JD, 2016
)
2.12
"Diclofenac is a widely prescribed NSAID, which by itself and its reactive metabolites (Phase-I and Phase-II) may be involved in serious idiosyncratic hepatotoxicity. "( Mitochondrial toxicity of diclofenac and its metabolites via inhibition of oxidative phosphorylation (ATP synthesis) in rat liver mitochondria: Possible role in drug induced liver injury (DILI).
Hansen, SH; Skonberg, C; Syed, M, 2016
)
2.18
"Diclofenac sodium is a commonly used anti-inflammatory drug."( COMPARISON OF ANTI-INFLAMMATORY ACTIVITY OF NIGELLA SATIVA AND DICLOFENAC SODIUM IN ALBINO RATS.
Bashir, MU; Qureshi, HJ; Saleem, T,
)
1.09
"Diclofenac is a non-steroidal anti-inflammatory drug and its use can be associated with severe adverse reactions, notably myocardial infarction, stroke and drug-induced liver injury (DILI). "( Immunogenomics reveal molecular circuits of diclofenac induced liver injury in mice.
Borlak, J; Choi, MS; Lee, EH; Oh, JH; Park, SM; Selvaraj, S; Spanel, R; Yoon, S, 2016
)
2.14
"Diclofenac is a non-steroidal antinflammatory drug (NSAID) that finds indication in the treatment of debilitating pathologies characterized by chronic pain sustained by inflammation, such as in rheumatic disease (rheumatoid arthritis or osteoarthritis) or periarthritis, bursitis, tendonitis, myositis and sciatica. "( Spinal antinflammatory action of Diclofenac.
Sandri, A, 2016
)
2.16
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID), which may cause serious intestinal adverse reactions (enteropathy). "( Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity.
Chen, Y; Li, Y; Ling, ZL; Liu, L; Liu, XD; Shu, N; Sun, BB; Tang, XG; Wang, F; Xia, LZ; Xie, QS; Xu, P; Zhang, M; Zhao, KJ; Zhong, ZY, 2016
)
2.13
"Diclofenac is a widely prescribed NSAID that causes severe idiosyncratic drug induced liver injury (IDILI) in a small part of the patient population. "( Simulation of interindividual differences in inactivation of reactive para-benzoquinone imine metabolites of diclofenac by glutathione S-transferases in human liver cytosol.
Commandeur, JN; den Braver, MW; Venkataraman, H; Vermeulen, NP; Zhang, Y, 2016
)
2.09
"Diclofenac (DCF) is a prevalent anti-inflammatory drug used throughout the world. "( Diclofenac and its transformation products: Environmental occurrence and toxicity - A review.
Brar, SK; Das, RK; Lonappan, L; Surampalli, RY; Verma, M, 2016
)
3.32
"Diclofenac (DICLO) is a non-selective NSAID that has been linked to serious side effects including gastric ulcers and renal injury."( Examination of the pharmacodynamics and pharmacokinetics of a diclofenac poly(lactic-co-glycolic) acid nanoparticle formulation in the rat.
Denham, JW; Hanley, GA; Harirforoosh, S; Murrell, DE; Panus, PC; West, KO, 2016
)
1.4
"Diclofenac is a widely used anti-inflammatory drug that is persistent in the environment along with the 4'- and 5-hydroxy metabolites."( The self-sufficient P450 RhF expressed in a whole cell system selectively catalyses the 5-hydroxylation of diclofenac.
Flitsch, SL; Hauer, B; Hayes, MA; Hussain, SA; Klenk, JM; Kulig, JK; Nebel, BA; Porter, JL; Richter, SM; Tavanti, M; Turner, NJ, 2017
)
1.39
"Diclofenac (DCF) is a non-steroidal analgesic and antiphlogistic. "( Diclofenac can exhibit estrogenic modes of action in male Xenopus laevis, and affects the hypothalamus-pituitary-gonad axis and mating vocalizations.
Efosa, NJ; Hoffmann, F; Kleiner, W; Kloas, W, 2017
)
3.34
"Diclofenac sodium (DS) is a non-steroidal anti-inflammatory drug with antipyretic and analgesic effects. "( The use of diclofenac sodium in urological practice: A structural and neurochemical based review.
Atilla, MK; Kaplan, AA; Ulubay, M; Yurt, KK, 2018
)
2.31
"Diclofenac is a member of the class of drugs termed non-steroidal anti-inflammatory drugs (NSAIDs) which belong to the most frequently detected pharmaceuticals in the water-cycle in Europe."( Selective trace analysis of diclofenac in surface and wastewater samples using solid-phase extraction with a new molecularly imprinted polymer.
Knopp, D; Niessner, R; Schüssler, W; Sengl, M; Sun, Z, 2008
)
1.36
"Diclofenac sodium is a nonsteroidal anti-inflammatory drug widely used in painful and inflammatory diseases. "( Different crystal morphologies arising from different preparation methods of a same polymorphic form may result in different properties of the final materials: the case of diclofenac sodium trihydrate.
Antoniella, E; Bartolomei, M; Bertocchi, P; Gaudiano, MC; Manna, L; Rodomonte, A, 2008
)
1.98
"Diclofenac (DCLF) is a nonsteroidal anti-inflammatory drug that is associated with idiosyncratic adverse drug reactions in humans. "( Gene expression profiles in livers from diclofenac-treated rats reveal intestinal bacteria-dependent and -independent pathways associated with liver injury.
Blomme, EA; Deng, X; Ganey, PE; Liguori, MJ; Roth, RA; Sparkenbaugh, EM; Waring, JF, 2008
)
2.06
"Diclofenac is an important analgesic and anti-inflammatory drug, widely used for treatment of postoperative pain, rheumatoid arthritis, and chronic pain associated with cancer. "( Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone.
Beijnen, JH; Lagas, JS; Schinkel, AH; van de Wetering, K; van der Kruijssen, CM, 2009
)
2.16
"Diclofenac is a commonly used non-steroidal anti-inflammatory drug (NSAID) for symptom control in osteoarthritis (OA) of the knee and soft tissue injuries. "( Topical diclofenac: clinical effectiveness and current uses in osteoarthritis of the knee and soft tissue injuries.
Banning, M, 2008
)
2.22
"Diclofenac is a useful and safe addition to postoperative analgesia for adult tonsillectomy. "( Comparative study of posttonsillectomy hemorrhage with the use of diclofenac versus dihydrocodeine for postoperative analgesia and review of the literature.
Hussain, SS; Lee, MS; McKean, SA, 2008
)
2.03
"Diclofenac is a nonsteroidal anti-inflammatory drug which is available as prescription (RX) and over-the-counter (OTC) medication for the systemic and topical treatment of painful and inflammatory conditions such as arthritis and back pain. "( Preferential uptake of the non steroid anti-inflammatory drug diclofenac into inflamed tissues after a single oral dose in rats.
Hasler-Nguyen, N; Schweitzer, A; Zijlstra, J, 2009
)
2.04
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID), available as a potassium salt (immediate-release) or sodium salt (delayed-release). "( Single dose oral diclofenac for acute postoperative pain in adults.
Derry, P; Derry, S; McQuay, HJ; Moore, RA, 2009
)
2.14
"Oral diclofenac is an effective single-dose treatment for moderate to severe postoperative pain. "( Single dose oral diclofenac for acute postoperative pain in adults.
Derry, P; Derry, S; McQuay, HJ; Moore, RA, 2009
)
1.21
"Diclofenac is a widely used anti-inflammatory non-steroidal drug that escapes conventional urban wastewater treatment trains because of its resistance to biodegradation. "( Degradation of diclofenac during sonolysis, ozonation and their simultaneous application.
Belgiorno, V; Kassinos, D; Naddeo, V; Ricco, D, 2009
)
2.15
"Diclofenac (DF) is a widely used non-steroid anti-inflammatory drug, associated with a range of side effects. "( Photodegradation mechanism of the common non-steroid anti-inflammatory drug diclofenac and its carbazole photoproduct.
Eriksson, LA; Musa, KA, 2009
)
2.03
"Diclofenac is a non-steroidal anti-inflammatory drug that is prescribed for treatment of rheumatic diseases and as an analgesic. "( Diclofenac inhibits proliferation but not NGF-induced differentiation of PC12 cells.
Badinloo, M; Meimandi, MS; Rajabalian, S, 2009
)
3.24
"Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in the treatment of ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. "( Preparation, characterization and dissolution studies of fast release diclofenac sodium tablets from PVP solid dispersions.
Barrera, MG; Bassani, G; Bolmaro, RE; Lamas, MC; Lambri, OA; Leonardi, D; Salomon, CJ,
)
1.81
"Diclofenac sodium is a non-steroidal anti-inflammatory drug of choice to treat arthritis because of its potential anti-inflammatory and analgesic activity. "( Development of iron/ethylcellulose (core/shell) nanoparticles loaded with diclofenac sodium for arthritis treatment.
Arias, JL; Delgado, AV; López-Viota, J; López-Viota, M, 2009
)
2.03
"Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug widely used in humans and animals. "( Effect of different penetration enhancers on diclofenac permeation across horse skin.
Andreeta, A; Ferrante, M; Landoni, MF, 2010
)
2.06
"Diclofenac is a poorly water soluble drug and also causes gastrointestinal toxicity."( Development and physicochemical evaluation of pharmacosomes of diclofenac.
Rawat, MS; Semalty, A; Semalty, M; Singh, D, 2009
)
1.31
"Diclofenac is an effective analgesic for perioperative acute pain in children. "( Diclofenac for acute pain in children.
Pritchard, D; Savage, I; Standing, JF; Waddington, M, 2009
)
3.24
"Diclofenac is a nonsteroidal antiinflammatory drug with potent analgesic and anti-inflammatory properties. "( Bioequivalence study of low-dose diclofenac potassium tablet formulations.
Fotopoulos, G; Gold, MS; Hinz, B; Hug, AM, 2009
)
2.08
"Diclofenac sodium is a non-steroidal anti-inflammatory drug that inhibits filamentation in Candida albicans. "( The role of diclofenac sodium in the dimorphic transition in Candida albicans.
Dominguez, A; Ghalehnoo, ZR; Najimi, M; Rashki, A,
)
1.95
"Diclofenac is an important analgesic and anti-inflammatory drug that is widely used for the treatment of postoperative pain, rheumatoid arthritis, and chronic pain associated with cancer. "( Hepatic clearance of reactive glucuronide metabolites of diclofenac in the mouse is dependent on multiple ATP-binding cassette efflux transporters.
Beijnen, JH; Lagas, JS; Schinkel, AH; Sparidans, RW; Wagenaar, E, 2010
)
2.05
"Diclofenac is a proven, commonly prescribed nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. "( Diclofenac: an update on its mechanism of action and safety profile.
Gan, TJ, 2010
)
3.25
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) used in patients who suffer from painful autoimmune diseases such as rheumatoid arthritis."( Immunomodulatory effects of diclofenac in leukocytes through the targeting of Kv1.3 voltage-dependent potassium channels.
Bielańska, J; Comes, N; David, M; Felipe, A; González, T; Parra, D; Soler, C; Valenzuela, C; Villalonga, N, 2010
)
1.38
"Diclofenac (DF) is an anti-inflammatory drug found in aqueous environments as a pollutant due to its widespread use. "( Ultrasound assisted photocatalytic degradation of diclofenac in an aqueous environment.
Anandan, S; Ashokkumar, M; Grieser, F; Kumar, PS; Madhavan, J; Zhou, M, 2010
)
2.06
"Diclofenac is a widely used drug that can cause serious hepatotoxicity, which has been linked to metabolism by cytochrome P450s (P450). "( Metabolism related toxicity of diclofenac in yeast as model system.
Dragovic, S; Tjong, TF; van Leeuwen, JS; Vermeulen, NP; Vos, JC; Vredenburg, G, 2011
)
2.1
"Diclofenac is an effective, opiate-sparing analgesic for acute pain in children, which is commonly used in pediatric surgical units. "( Diclofenac pharmacokinetic meta-analysis and dose recommendations for surgical pain in children aged 1-12 years.
Korpela, R; Olkkola, KT; Standing, JF; Tibboel, D, 2011
)
3.25
"Diclofenac sodium is a non-steroidal anti-inflammatory drug (NSAID), and is frequently used in everyday oral medications, topical ointments, gel agents and eye drops."( Allergic contact dermatitis due to diclofenac sodium in eye drops.
Asato, Y; Hagiwara, K; Miyazato, H; Taira, K; Uezato, H; Yamaguchi, S; Yamamoto, Y, 2011
)
1.37
"Diclofenac is a nonsteroidal anti-inflammatory drug frequently found in the aquatic environment. "( Diclofenac in fish: blood plasma levels similar to human therapeutic levels affect global hepatic gene expression.
Asker, N; Cuklev, F; Fick, J; Förlin, L; Kristiansson, E; Larsson, DG, 2011
)
3.25
"Diclofenac is a widely used analgesic drug that can cause serious adverse drug reactions. "( Involvement of the pleiotropic drug resistance response, protein kinase C signaling, and altered zinc homeostasis in resistance of Saccharomyces cerevisiae to diclofenac.
van Leeuwen, JS; Vermeulen, NP; Vos, JC, 2011
)
2.01
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) which has been shown to increase the susceptibility of various bacteria to antimicrobials and demonstrated to have broad antimicrobial activity. "( Alterations in the transcriptome and antibiotic susceptibility of Staphylococcus aureus grown in the presence of diclofenac.
Cantore-Matyi, SA; Dupre, JM; Elasri, MO; Gustafson, JE; Helal, NS; Horan, S; Kumar-Singh, A; Nagarajan, V; Riordan, JT; Song, Y; Wilkinson, BJ; Zaman, S, 2011
)
2.02
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) commonly prescribed for pain relief in osteoarthritis (OA). "( A comparison of the therapeutic efficacy of diclofenac in osteoarthritis: a systematic review of randomised controlled trials.
Pavelka, K, 2012
)
2.08
"Diclofenac is a frequently prescribed drug for rheumatic diseases and muscle pain. "( Simulation of the oxidative metabolism of diclofenac by electrochemistry/(liquid chromatography/)mass spectrometry.
Brauckmann, C; Faber, H; Karst, U; Melles, D; Wehe, CA; Wentker, K, 2012
)
2.09
"Diclofenac is an established analgesic, and new formulations using the potassium or epolamine salts, which can be dissolved in water, have been developed for rapid absorption, which may be beneficial in acute migraine."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2012
)
2.54
"Diclofenac (DCF) is a widely used nonsteroidal anti-inflammatory drug that is regularly detected in surface waters. "( Diclofenac: New data on chronic toxicity and bioconcentration in fish.
Burri, R; Hartmann, A; Memmert, U; Peither, A; Schmidt, T; Sumpter, JP; Weber, K, 2013
)
3.28
"Diclofenac suppository is an economical alternative to intravenous ketorolac."( Prospective randomized trial of pre-emptive analgesics following ambulatory inguinal hernia repair: intravenous ketorolac versus diclofenac suppository.
Goh, LC; Lau, H; Lee, F; Patil, NG; Wong, C, 2002
)
1.24
"Diclofenac is a nonsteroidal anti-inflammatory drug bearing a carboxylic acid functional group. "( The metabolism of diclofenac--enzymology and toxicology perspectives.
Tang, W, 2003
)
2.1
"Diclofenac is a non-steroidal anti-inflammatory drug that is widely used clinically but side effects associated with the administration of the drug have been reported. "( Diclofenac induces apoptosis in hepatocytes by alteration of mitochondrial function and generation of ROS.
Castell, JV; Donato, T; Gómez-Lechón, MJ; Jover, R; O'Connor, E; Ponsoda, X, 2003
)
3.2
"Diclofenac sodium is a non-steroidal anti-inflammatory agent commonly used to provide analgesia post-surgery. "( A prospective, randomised trial of preoperative rectal diclofenac: are we closing the gate after the horse has gone?
Lowe, D; Lyons, JB; Moriarty, J; Niazi, A; Sheehan, SJ,
)
1.82
"Diclofenac is a benzene-acetic acid derivative that acts, like other NSAIDs, by inhibiting cyclo-oxygenase isoforms that mediate the body's production of the prostaglandins implicated in pain and inflammation. "( Single dose oral diclofenac for postoperative pain.
Barden, J; Edwards, J; McQuay, HJ; Moore, RA, 2004
)
2.11
"Oral diclofenac is an effective single-dose treatment for moderate to severe postoperative pain. "( Single dose oral diclofenac for postoperative pain.
Barden, J; Edwards, J; McQuay, HJ; Moore, RA, 2004
)
1.18
"Diclofenac is a nonsteroidal anti-inflammatory drug that causes rare but serious hepatotoxicity, the mechanism of which is unclear. "( Hepatic adducts, circulating antibodies, and cytokine polymorphisms in patients with diclofenac hepatotoxicity.
Aithal, GP; Alexander, G; Caldwell, J; Daly, AK; Day, CP; Kenna, JG; Leathart, JB; Ramsay, L; Sonchit, N, 2004
)
1.99
"Diclofenac sodium is a non-steroidal anti-inflammatory drug commonly used to attenuate painful inflammatory reactions in surgery. "( Effect of diclofenac sodium on the healing process of end-to-end anastomosis in carotid arteries of rabbits. Histopathological and biomechanical studies.
Bonetti Yoshida, W; Crocci, AJ; Freire Cerqueira, N; Hussni, CA; Mattar, L; Rodrigues, AC; Sequeira, JL; Swain Müller, S, 2003
)
2.16
"Diclofenac (DCF) is a widely used nonsteroidal anti-inflammatory drug implicated as a cause of immune hemolytic anemia. "( Diclofenac-induced antibodies against red blood cells are heterogeneous and recognize different epitopes.
Bein, G; Kroll, H; Röder, L; Sachs, UJ; Santoso, S; Smart, E, 2004
)
3.21
"Diclofenac is a non-steroidal anti-inflammatory drug of the phenylacetic class. "( [Intramuscular application of diclofenac--case report and critical consideration of a therapeutic measure].
Bertram, C; Grass, H; Rothschild, MA; Schuff, A,
)
1.86
"Diclofenac is a non-steroidal anti-inflammatory drug used for a variety of painful and inflammatory conditions. "( Diclofenac systemic exposure is not increased when topical diclofenac is applied to ultraviolet-induced erythema.
Kienzler, JL; Knops, A; Magnette, JL; Ménart, C; Nollevaux, F; Sallin, D, 2004
)
3.21
"Diclofenac is a widely prescribed anti-inflammatory agent that has a similar diphenyl motif in its structure."( An inactivation stabilizer of the Na+ channel acts as an opportunistic pore blocker modulated by external Na+.
Kuo, CC; Yang, YC, 2005
)
1.05
"Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in painful and inflammatory diseases. "( Physico-chemical characterisation and intrinsic dissolution studies of a new hydrate form of diclofenac sodium: comparison with anhydrous form.
Antoniella, E; Bartolomei, M; Bertocchi, P; Rodomonte, A, 2006
)
2
"Diclofenac is a widely used nonsteroidal anti-inflammatory drug that has been associated with rare but serious hepatotoxicity. "( Critical role of free cytosolic calcium, but not uncoupling, in mitochondrial permeability transition and cell death induced by diclofenac oxidative metabolites in immortalized human hepatocytes.
Boelsterli, UA; Gupta, R; Lim, MS; Lim, PL, 2006
)
1.98
"Diclofenac is a widely used nonsteroidal anti-inflammatory drug and is among the most common drugs causing idiosyncratic hepatotoxicity in several recent series with up to 20% mortality in jaundiced subjects. "( Genetic susceptibility to diclofenac-induced hepatotoxicity: contribution of UGT2B7, CYP2C8, and ABCC2 genotypes.
Aithal, GP; Daly, AK; Dang, TS; Day, CP; Leathart, JB; Swainsbury, RA, 2007
)
2.08
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that has been detected widely in surface waters in North America and Europe. "( Structural and functional responses of river biofilm communities to the nonsteroidal anti-inflammatory diclofenac.
Korber, DR; Lawrence, JR; Neu, TR; Swerhone, GD; Topp, E; Wassenaar, LI, 2007
)
2
"Diclofenac 3% gel is an effective treatment for actinic keratoses (AKs) and is reported to be generally well tolerated with only mild local reactions. "( Genetically determined susceptibility to COX-2 inhibitors: a report of exaggerated responders to diclofenac 3% gel in the treatment of actinic keratoses.
Forschner, T; Patel, MJ; Ulrich, C, 2007
)
2
"Diclofenac is a non-steroidal anti-inflammatory drug, which tends to be relatively persistent in the environment. "( Transformation of diclofenac by the indigenous microflora of river sediments and identification of a major intermediate.
Claussnitzer, U; Garten, C; Gröning, J; Held, C; Kaschabek, SR; Schlömann, M, 2007
)
2.12
"Diclofenac is a nonsteroidal anti-inflammatory drug and has been shown to have anti-inflammatory, analgesic, and antipyretic activity."( Treatment with H2S-releasing diclofenac protects mice against acute pancreatitis-associated lung injury.
Bhatia, M; Moore, PK; Sidhapuriwala, JN; Sparatore, A, 2008
)
1.36
"Diclofenac is a nonsteroidal anti-inflammatory drug that nonselectively inhibits constitutive and inducible isoenzymes of cyclooxygenase. "( [Prenatal tolerability evaluation of diclofenac].
Burdan, F; Kiś, J; Przybylski, P, 2007
)
2.06
"Diclofenac sodium is a non-steroidal anti-inflammatory drug (NSAID). "( Bioavailability of diclofenac sodium after pretreatment with diosmin in healthy volunteers.
Krishna, DR; Rajnarayana, K; Venkatesham, A, 2007
)
2.11
"Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in painful and inflammatory diseases. "( Hydrate modifications of the non-steroidal anti-inflammatory drug diclofenac sodium: Solid-state characterisation of a trihydrate form.
Antoniella, E; Bartolomei, M; Bertocchi, P; Minelli, G; Rodomonte, A, 2007
)
2.02
"Diclofenac (DCF) is a widely used non-steroidal anti-inflammatory drug, which also act as a mitochondrial toxin. "( Modulation of dopaminergic neurotransmission in rat striatum upon in vitro and in vivo diclofenac treatment.
Baranyi, M; Fekete, A; Kittel, A; Milusheva, E; Sperlágh, B; Vizi, ES; Zelles, T, 2008
)
2.01
"Diclofenac sodium proved to be a very potent antipyretic agent with serious side effects."( Antipyretic therapy with diclofenac sodium. Observations on effect and serious side effects in critically ill patients.
Alexander, JP; Stoutenbeek, CP; Zandstra, DF, 1983
)
1.29
"Diclofenac is a nonsteroidal antiinflammatory drug (NSAID) that is widely used systemically and topically. "( Topical diclofenac following excimer laser: effect on corneal sensitivity and wound healing in rabbits.
Aquavella, JV; Bassage, S; del Cerro, M; Loya, N; Park, SB; Vyas, S,
)
2.01
"Diclofenac is a nonsteroidal anti-inflammatory drug approved in the United States in 1988 for the treatment of patients with osteoarthritis, rheumatoid arthritis, or ankylosing spondylitis. "( Diclofenac-associated hepatotoxicity: analysis of 180 cases reported to the Food and Drug Administration as adverse reactions.
Banks, AT; Harter, JG; Ishak, KG; Zimmerman, HJ, 1995
)
3.18
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that has been commercially available for many years and its pharmacokinetics are well documented."( Pharmacokinetics of diclofenac and misoprostol when administered alone or as a combination product.
Karim, A, 1993
)
1.33
"Diclofenac is a nonsteroidal anti-inflammatory agent that is reported to cause serious hepatic injury in some patients. "( Metabolic activation and immunochemical localization of liver protein adducts of the nonsteroidal anti-inflammatory drug diclofenac.
Amouzedeh, HR; Hargus, SJ; McCoy, SC; Myers, TG; Pohl, LR; Pumford, NR,
)
1.78
"Diclofenac is an effective and safe analgesic and antiinflammatory drug."( [Diclofenac vs nimesulide in arthrosis. Plasma levels and clinical efficacy].
Amaro, G; Estevez, F; Giusti, M; Havranek, H; Lasalvia, L, 1993
)
1.92
"Diclofenac sodium is a non-steroidal anti-inflammatory widely used drug both in the treatment of the rheumatic diseases and as analgesic. "( [Tissue necrosis: a side effect of sodium diclofenac: report of cases and discussion of the physiopathology].
Alonso, N; Borrelli Júnior, M; Branco, PD; Giovannetti, M; Ikejiri, CI; Machado, MA,
)
1.84
"Diclofenac is a frequently prescribed nonsteroidal antiinflammatory drug (NSAID). "( Diclofenac induced hepatitis. 3 cases with features of autoimmune chronic active hepatitis.
Barr, RJ; Clarke, D; Scully, LJ, 1993
)
3.17
"Diclofenac is a well established nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of a variety of painful inflammatory conditions. "( Diclofenac/misoprostol. A review of its pharmacology and therapeutic efficacy in painful inflammatory conditions.
Davis, R; Goa, KL; Yarker, YE, 1995
)
3.18
"Diclofenac is a nonsteroidal anti-inflammatory drug that has been implicated in several cases of severe hepatotoxicity. "( Covalent modification of rat liver dipeptidyl peptidase IV (CD26) by the nonsteroidal anti-inflammatory drug diclofenac.
George, JW; Hargus, SJ; Martin, BM; Pohl, LR, 1995
)
1.95
"Diclofenac is a non-steroidal anti-inflammatory drug available in an ophthalmic preparation. "( The effectiveness of topical diclofenac in relieving discomfort following traumatic corneal abrasions.
Andrews, RM; Dayan, M; Fitt, AW; Griffiths, PG; Jayamanne, DG; Mitchell, KW, 1997
)
2.03
"Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class. "( Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls.
Anderson, KE; Davies, NM, 1997
)
2.03
"Diclofenac is an anti-inflammatory analgesic which is widely used in the therapy of inflammatory joint pain. "( [Diclofenac-associated acute cholestatis hepatitis].
Hackstein, H; Mohl, W; Püschel, W; Stallmach, A; Zeitz, M, 1998
)
2.65
"Diclofenac sodium is an ideal candidate for incorporation in a controlled release device to diminish its adverse effects after oral administration. "( Formulation optimization of controlled release diclofenac sodium microspheres using factorial design.
Amin, AF; Gohel, MC, 1998
)
2
"Diclofenac (1) is a photosensitizing nonsteroidal antiinflammatory drug. "( Phototoxicity associated with diclofenac: a photophysical, photochemical, and photobiological study on the drug and its photoproducts.
Bosca, F; Encinas, S; Miranda, MA, 1998
)
2.03
"Diclofenac is a cyclo-oxygenase inhibitor and thus carries the pharmacodynamic properties of other nonsteroidal anti-inflammatory drugs with inhibition of prostaglandin synthesis, resulting in vasoconstriction of the ductus arteriosus."( Contraction of the fetal ductus arteriosus induced by diclofenac. Case report.
Elchalal, U; Nadjari, M; Nir, A; Rein, AJ,
)
1.1
"Diclofenac-potassium is a potent NSAID available as a fast-acting oral tablet, which has been shown to be safe and effective in several other acute pain indications."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
1.24
"Diclofenac potassium is an effective analgesic in the range of aspirin (650 mg) at the 25-mg dose and superior in efficacy and longer lasting than aspirin at the 50- and 100-mg doses."( Onset and duration of analgesia of diclofenac potassium in the treatment of postepisiotomy pain.
DeCastro, A; Olson, NZ; Sunshine, A; Zighelboim, I,
)
1.13
"Diclofenac sodium is a nonsteroidal anti-inflammatory drug with analgesic, antipyretic, and anti-inflammatory activity. "( Percutaneous transport of diclofenac sodium from mixtures of fatty alcohol (or fatty acid) and propylene glycol through the rabbit abdominal skin.
Guu, YB; Wang, DP; Wang, MT; Wong, CY, 1999
)
2.05
"Diclofenac sodium (DS), is a potent drug in the NSAID group having non-steroidal, anti-inflammatory properties, and is widely used in the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis."( In vitro and in vivo evaluation of diclofenac sodium loaded albumin microspheres.
Caliş, S; Ercan, MT; Hincal, AA; Kaş, HS; Peksoy, I; Tunçay, M,
)
1.13
"Diclofenac is a commonly used non-steroidal anti-inflammatory drug in women of reproductive age. "( A study on placental transfer of diclofenac in first trimester of human pregnancy.
Lau, TK; Siu, SS; Yeung, JH, 2000
)
2.03
"Diclofenac seemed to be a COX-2 inhibitor because its IC50 values were similar to the IC50 values of NS-398."( Inhibition of COX in ocular tissues: an in vitro model to identify selective COX-2 inhibitors.
Bellot, JL; Castillo, M; García-Cabanes, C; Orts, A; Palmero, M, 2001
)
1.03
"Diclofenac (DCLF) is a nonsteroidal anti-inflammatory drug that is widely used for the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and acute muscle pain conditions. "( Diclofenac induced in vivo nephrotoxicity may involve oxidative stress-mediated massive genomic DNA fragmentation and apoptotic cell death.
Gross, SM; Hickey, EJ; Raje, RR; Ray, SD; Reid, VE, 2001
)
3.2
"Diclofenac is a non-steroidal anti-inflammatory drug, commonly used by reproductive age women for the treatment of a variety of conditions. "( A study of diclofenac-induced teratogenicity during organogenesis using a whole rat embryo culture model.
Chan, LY; Chiu, PY; Lau, TK; Siu, SS, 2001
)
2.14
"Diclofenac is a potent inhibitor of prostaglandin synthesis, as well as an established antipyretic and analgesic agent. "( Determination of diclofenac in rat bile and its interaction with cyclosporin A using on-line microdialysis coupled to liquid chromatography.
Liu, SC; Tsai, TH, 2002
)
2.1
"Diclofenac is a potent anti-inflammatory and analgesic compound with good antipyretic and uricosuric properties. "( The pharmacology of diclofenac sodium (Voltarol).
Maier, R; Menassé, R; Pericin, C; Riesterer, L; Ruegg, M; Ziel, R, 1979
)
2.03
"Diclofenac is a non steroïdal anti-inflammatory drug. "( [Myoclonus during a treatment with diclofenac (author's transl)].
Alcalay, M; Bontoux, D; Reboux, JF; Thomas, P,
)
1.85
"Diclofenac sodium is a widely used enteric-coated nonsteroidal anti-inflammatory drug. "( 'Diaphragmlike' stricture and ulcer of the colon during diclofenac treatment.
Becich, MJ; Evans, BA; Martin, SP; Trellis, DR; Whitcomb, DC, 1992
)
1.97
"Diclofenac sodium is a potent nonsteroidal anti-inflammatory drug with analgesic activity. "( Ocular diclofenac. A review of its pharmacology and clinical use in cataract surgery, and potential in other inflammatory ocular conditions.
Chrisp, P; Goa, KL,
)
2.03
"Diclofenac is a useful adjunct in the management of postthoracotomy pain."( Nonsteroidal antiinflammatory drugs for postthoracotomy pain. A prospective controlled trial after lateral thoracotomy.
Conacher, I; Hilton, C; Morritt, G; Rhodes, M, 1992
)
1
"Diclofenac sodium is a widely used drug with interesting absorption and disposition features when administered to laboratory animals. "( Pharmacokinetics and bioavailability of diclofenac in the rat.
Aristorena, JC; Garcia-Carbonell, MC; Peris-Ribera, JE; Pla-Delfina, JM; Torres-Molina, F, 1991
)
1.99
"Diclofenac sodium is a valid alternative, which shows similar analgesic efficacy."( Comparative study of the efficacy of dipyrone, diclofenac sodium and pethidine in acute renal colic. Collaborative Group of the Spanish Society of Clinical Pharmacology.
, 1991
)
1.26
"Diclofenac is a widely used non-steroidal anti-inflammatory drug, being the most commonly prescribed of its kind in the world. "( Diclofenac associated hepatitis.
Chapman, RW; Iveson, TJ; Kelly, PM; McGee, JO; Ryley, NG; Trowell, JM, 1990
)
3.16
"Diclofenac sodium is a nonsteroidal antiinflammatory drug (NSAID) that has been used in 120 countries since its introduction in Japan in 1974. "( Review of diclofenac and evaluation of its place in therapy as a nonsteroidal antiinflammatory agent.
Alissandratos, J; Arkin, CR; Carter, CA; Mickle, TR; Petty, DE; Skoutakis, VA; Smith, VH, 1988
)
2.12
"Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) advocated for use in painful and inflammatory rheumatic and certain non-rheumatic conditions. "( Diclofenac sodium. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Sorkin, EM; Todd, PA, 1988
)
3.16
"Diclofenac sodium is a nonsteroidal, anti-inflammatory drug that has been studied in the United States for the treatment of rheumatoid arthritis in 681 patients, 468 of whom were enrolled in five multicenter, double-blind parallel controlled investigations. "( Efficacy and safety of diclofenac sodium in rheumatoid arthritis. Experience in the United States.
Caldwell, JR, 1986
)
2.02
"Diclofenac is an alternative to opiates in the management of postoperative pain."( Diclofenac and oxycodone in treatment of postoperative pain: a double-blind trial.
Nuutinen, LS; Pentikäinen, IT; Wuolijoki, E, 1986
)
2.44
"Diclofenac seems to be a promising drug for the maintenance of mydriasis during eye surgery."( Prevention of surgically induced miosis by diclofenac eye drops.
Bellucci, R; Bonomi, L; De Franco, I; Massa, F; Perfetti, S, 1987
)
1.26
"Diclofenac is an anti-inflammatory drug possessing the original property of acting as a negative chemokinetic agent, for migration of both stimulated and unstimulated PMN."( Diclofenac sodium, a negative chemokinetic factor for neutrophil locomotion.
Giroud, JP; Gougerot-Pocidalo, MA; Hakim, J; Perianin, A, 1985
)
2.43

Effects

Diclofenac sodium has a significant effect on decreasing the pain associated with swallowing postoperatively and on the general condition of the patient. It has a unique proposed mechanism of action in AK that may involve COX-2 inhibition, inhibition of angiogenesis, and induction of apoptosis.

Diclofenac sodium has shown its radioprotective potential by scavenging radiation induced free radicals which are depicted by its ability in restoring the fraction of supercoiled form of plasmid DNA back to normal. Diclfenac instillation has been used widely in cataract surgery to prevent postoperative inflammation.

ExcerptReferenceRelevance
"Diclofenac sodium has a short half-life (about 1.5 hours), requiring repeated administration, and as a result, serious complications, such as GI bleeding, peptic ulcer, and kidney and liver dysfunction, are generated. "( Fabrication and
Chiu, IH; Lin, IL; Liu, JY; Minhas, MU; Suhail, M; Tsai, MJ; Ullah, H; Wu, PC, 2023
)
2.35
"Diclofenac has an impact on the levels of MMP-2, MMP-3 and MMP-13, which are needed for normal healing process, and it can also lead to disruption of tendon healing."( The effect of diclofenac on matrix metalloproteinase levels in the rotator cuff.
Avci, A; Cabuk, FK; Cabuk, H; Durmaz, H; Ertem, F; Muhittin Şener, I, 2014
)
2.21
"Diclofenac sodium 3% gel has a unique proposed mechanism of action in AK that may involve COX-2 inhibition, inhibition of angiogenesis, and induction of apoptosis. "( Diclofenac sodium 3% gel for the management of actinic keratosis: 10+ years of cumulative evidence of efficacy and safety.
Martin, GM; Stockfleth, E, 2012
)
3.26
"Diclofenac sodium has a significant effect on decreasing the pain associated with swallowing postoperatively and on the general condition of the patient. "( Comparative study of diclofenac sodium and paracetamol for treatment of pain after adenotonsillectomy in children.
Husban, AM; Nawasreh, OO; Tawalbeh, MI, 2001
)
2.07
"Diclofenac has an antinociceptive activity that, in addition to cyclooxygenase inhibition, can be modulated by additive and supraadditive interactions with adrenergic drugs."( An isobolographic analysis of the adrenergic modulation of diclofenac antinociception.
Miranda, HF; Pinardi, G; Sierralta, F, 2001
)
1.28
"Diclofenac has the highest risk, while naproxen has the lowest risk of developing these complications."( Comparative analysis of the use of non-steroidal anti-inflammatory drugs in Montenegro, Finland and Croatia in the period 2010-2019.
Mugoša, S; Šahman-Zaimović, M, 2022
)
1.44
"Diclofenac has increased cardiovascular risks, but its risk profile compared with other COX-2 inhibitors remains unknown."( Cardiovascular Risks of Diclofenac Versus Other Older COX-2 Inhibitors (Meloxicam and Etodolac) and Newer COX-2 Inhibitors (Celecoxib and Etoricoxib): A Series of Nationwide Emulated Trials.
Pedersen, L; Schmidt, M; Sørensen, HT, 2022
)
2.47
"Diclofenac sodium has a short half-life (about 1.5 hours), requiring repeated administration, and as a result, serious complications, such as GI bleeding, peptic ulcer, and kidney and liver dysfunction, are generated. "( Fabrication and
Chiu, IH; Lin, IL; Liu, JY; Minhas, MU; Suhail, M; Tsai, MJ; Ullah, H; Wu, PC, 2023
)
2.35
"Diclofenac sodium salt has been assumed as low molecular weight probe to detect the different binding behaviour of polymeric materials; mucin from bovine submaxillary glands was selected as the model protein for differentiating their mucoadhesion."( Binding and mucoadhesion of sulfurated derivatives of quaternary ammonium-chitosans and their nanoaggregates: An NMR investigation.
Balzano, F; Cesari, A; Fabiano, A; Piras, AM; Uccello-Barretta, G; Zambito, Y, 2020
)
1.28
"Diclofenac has been responsible for the deaths of millions of vultures on the Asian subcontinent. "( Does the renal portal valve exist in a raptor species? A study aimed at further evaluating the mechanism of toxicity of diclofenac in vultures.
Duncan, N; Groenewald, HB; Havenga, L; Naidoo, V; Wolter, K, 2020
)
2.21
"Diclofenac (DCF) has been recognized as an emerging contaminant in aquatic environments. "( Regulation of pregnane-X-receptor and microRNAs on detoxification-related genes expressions in Mugilogobius abei under the exposure to diclofenac.
Ku, P; Li, K; Nie, X; Ou, R; Wang, C, 2018
)
2.13
"Diclofenac and EMLA have been used to minimize these adverse effects; however, conflicting results have been reported regarding which has better outcomes."( Comparison of EMLA and Diclofenac on Reduction of Pain and Phlebitis Caused by Peripheral IV Catheter: A Randomized-Controlled Trial Study.
Babaieasl, F; Kheradmand, M; Saeidzadeh, S; Yarandi, HN,
)
1.16
"Oral diclofenac has been associated with DILI more frequently than other NSAIDs and requires periodic monitoring of liver transaminases and judicious consideration of clinical signs and symptoms of hepatotoxicity."( Elevated Transaminases with Topical Diclofenac: A Case Report.
Daniels, AM; Gibbs, LM; Herndon, CM,
)
0.86
"The diclofenac sodium has the following pharmacokinetic characteristics in swine: rapid absorption and elimination; high peak concentration; and bioavailability."( Pharmacokinetics of diclofenac sodium injection in swine.
Bu, SJ; Huang, C; Huang, LX; Li, YJ; Li, YY; Yang, HF, 2019
)
1.32
"Diclofenac residues have been found in surface water, and thus could present a potential risk to aquatic species. "( The effects of diclofenac on early life stages of common carp (Cyprinus carpio).
Blahova, J; Chromcova, L; Plhalova, L; Praskova, E; Prokes, M; Stepanova, S; Svobodova, Z, 2013
)
2.19
"Diclofenac sodium has shown its radioprotective potential by scavenging radiation induced free radicals which are depicted by its ability in restoring the fraction of supercoiled form of plasmid DNA back to normal."( Radioprotective role of clinical drug diclofenac sodium.
Adhikari, JS; Alok, A; Chaudhury, NK, 2013
)
1.38
"Diclofenac instillation has been used widely in cataract surgery to prevent postoperative inflammation. "( Albumin-binding of diclofenac and the effect of a site II inhibitor in the aqueous humor of cataract patients with the instillation of diclofenac.
Arimori, K; Ogata, K; Osaki, T; Ozaki, M; Setoguchi, N; Takamura, N; Tokunaga, J, 2014
)
2.17
"Diclofenac has hitherto been considered by many dermatologists as a safe alternative in NSAID-induced pseudoporphyria."( Diclofenac-induced pseudoporphyria; an under-recognized condition?
Callan, M; Staughton, RC; Turnbull, N, 2014
)
2.57
"The diclofenac ligand has been found to act as bidentate chelating agent."( Synthesis, spectroscopic and thermal studies of Mg(II), Ca(II), Sr(II) and Ba(II) diclofenac sodium complexes as anti-inflammatory drug and their protective effects on renal functions impairment and oxidative stress.
El-Megharbel, SM; Hamza, RZ; Refat, MS, 2015
)
1.12
"Diclofenac has an impact on the levels of MMP-2, MMP-3 and MMP-13, which are needed for normal healing process, and it can also lead to disruption of tendon healing."( The effect of diclofenac on matrix metalloproteinase levels in the rotator cuff.
Avci, A; Cabuk, FK; Cabuk, H; Durmaz, H; Ertem, F; Muhittin Şener, I, 2014
)
2.21
"Diclofenac has been shown to activate aryl hydrocarbon receptor (AHR), which induces transcription in the metabolic enzyme cytochrome P450 1a (cyp1a)."( Hypoxia and the pharmaceutical diclofenac influence the circadian responses of three-spined stickleback.
Götting, M; Kanerva, M; Lubiana, P; McCairns, RJ; Nikinmaa, M; Prokkola, JM, 2015
)
1.42
"Diclofenac (DCF) has been detected in significant amounts in municipal treated wastewater effluent. "( Short and long-term exposure to diclofenac alter oxidative stress status in common carp Cyprinus carpio.
Dublán-García, O; Galar-Martínez, M; Gómez-Oliván, LM; Islas-Flores, H; López-Martínez, LX; Morachis-Valdes, G; Saucedo-Vence, K, 2015
)
2.14
"Diclofenac sodium has limited efficacy and should probably not be used in acute pain."( Single dose oral diclofenac for acute postoperative pain in adults.
Derry, S; Moore, RA; Wiffen, PJ, 2015
)
1.48
"Diclofenac has been used mainly topically, and recent focus has been on intravitreal delivery."( Efficacy of systemic diclofenac sodium on intravitreal concentration.
Abrishami, M; Hoseini, H; Jadidi, K; Naderi, M; Panahi, Y, 2018
)
1.52
"Diclofenac (DCF) has been treated in water with ozone in the presence of various activated carbons. "( Diclofenac removal from water with ozone and activated carbon.
Alvarez, P; Beltrán, FJ; Oropesa, A; Pocostales, P, 2009
)
3.24
"Diclofenac has been of environmental concern due to the potential harmful effects on non-target organisms at environmentally relevant concentrations. "( Enzymatic and microbial transformation assays for the evaluation of the environmental fate of diclofenac and its metabolites.
Chang, HR; Kim, K; Kwon, JH; Lee, E; Lee, HJ; Yoon, SH, 2012
)
2.04
"Diclofenac sodium 3% gel has also demonstrated efficacy for clearing AK lesions in immunosuppressed populations."( Diclofenac sodium 3% gel for the management of actinic keratosis: 10+ years of cumulative evidence of efficacy and safety.
Martin, GM; Stockfleth, E, 2012
)
2.54
"Diclofenac sodium 3% gel has a unique proposed mechanism of action in AK that may involve COX-2 inhibition, inhibition of angiogenesis, and induction of apoptosis. "( Diclofenac sodium 3% gel for the management of actinic keratosis: 10+ years of cumulative evidence of efficacy and safety.
Martin, GM; Stockfleth, E, 2012
)
3.26
"Diclofenac has frequently been implicated as the cause of immune hemolytic anemias and less frequently of immune thrombocytopenia. "( Diclofenac-induced antibodies against RBCs and platelets: two case reports and a concise review.
Ahrens, N; Aslan, T; Hoffmann, T; Kiesewetter, H; Meyer, O; Salama, A, 2003
)
3.2
"Diclofenac has been used for the evaluation of CYP2C9 activity in vitro as well as in vivo with varying results. "( Reproducibility over time of the urinary diclofenac/4'-OH diclofenac ratio among different CYP2C9 genotypes.
Berecz, R; Cáceres, MC; Conzález, I; Dorado, P; Llerena, A,
)
1.84
"Diclofenac has been demonstrated to be an effective migraine treatment in several placebo-controlled studies. "( Efficacy of diclofenac sodium softgel 100 mg with or without caffeine 100 mg in migraine without aura: a randomized, double-blind, crossover study.
Goldstein, J; Kolodner, K; Lipton, RB; Lyon, JA; Peroutka, SJ; Swarbrick, J, 2004
)
2.15
"Diclofenac-K has been recently launched at low oral doses in different countries for over-the-counter use. "( Bioavailability of diclofenac potassium at low doses.
Brune, K; Chevts, J; Hinz, B; Rau, T; Renner, B; Schmidt, A; Szelenyi, I; Werner, U; Wuttke, H, 2005
)
2.1
"Diclofenac has been implicated in many cases of life-threatening immune hemolytic anemia (IHA). "( Misdiagnosis in patients with diclofenac-induced hemolysis: new cases and a concise review.
Ahrens, N; Genth, R; Kiesewetter, H; Salama, A, 2006
)
2.07
"Diclofenac sodium has been demonstrated to be effective in preventing proliferation of lens epithelial cells both in vitro and in animal studies. "( Effect of diclofenac on prevention of posterior capsule opacification in human eyes.
Bozkurt, E; Ermis, S; Inan, UU; Oztürk, F; Yaman, S, 2006
)
2.18
"diclofenac injection has rarely been reported in the published work."( Nicolau syndrome aggravated by cold application after i.m. diclofenac.
Ada, S; Cağlar, B; Güleç, AT; Senel, E, 2008
)
1.31
"Diclofenac has the added advantage, in our institution, of being 60% less expensive than ketorolac."( A comparative study of ketorolac and diclofenac on post-laparoscopic cholecystectomy pain.
Fredman, B; Jedeikin, R; Olsfanger, D, 1995
)
1.29
"Diclofenac/misoprostol has demonstrated to be an alternative with a better cost/effectiveness ratio, and therefore more efficient than diclofenac alone or the concomitant use of diclofenac either with omeprazol or ranitidine. "( [Economic evaluation of the use of diclofenac/misoprostol in the treatment of osteoarticular diseases].
Soto Alvarez, J, 2000
)
2.03
"Diclofenac sodium has a significant effect on decreasing the pain associated with swallowing postoperatively and on the general condition of the patient. "( Comparative study of diclofenac sodium and paracetamol for treatment of pain after adenotonsillectomy in children.
Husban, AM; Nawasreh, OO; Tawalbeh, MI, 2001
)
2.07
"Diclofenac has an antinociceptive activity that, in addition to cyclooxygenase inhibition, can be modulated by additive and supraadditive interactions with adrenergic drugs."( An isobolographic analysis of the adrenergic modulation of diclofenac antinociception.
Miranda, HF; Pinardi, G; Sierralta, F, 2001
)
1.28
"Diclofenac (Voltarol) has no effect on carbohydrate metabolism, insulin levels or tolbutamide metabolism, nor does it enhance the effect of tolbutamide, biguanide or glibenclamide. "( Diclofenac sodium (Voltarol): drug interactions and special studies.
Fowler, PD, 1979
)
3.15

Actions

Diclofenac (DCF) can cause adverse reactions such as gastrointestinal, renal and cardiovascular disorders. topical administration may be an attractive alternative to the management of local pain in order to avoid these side effects. Diclfenac could cause gastrointestinal complications, neurotoxicity, cardiotoxicity, hepatotoxicity, nephrotoxicity, hematot toxicity, genotoxicity and teratogenicity.

ExcerptReferenceRelevance
"Diclofenac (DCF) can cause several adverse effects in the environment and it should be removed from industrial pharmaceutical wastewaters. "( Photo-Fenton process applied for the treatment of industrial wastewaters containing diclofenac: optimization with low iron ions concentrations and without pH control.
Almeida, J; Carvalho, JF; Miele, RG; Moraes, JEF; Oliveira, IHM; Parise, BF, 2023
)
2.58
"Diclofenac could cause gastrointestinal complications, neurotoxicity, cardiotoxicity, hepatotoxicity, nephrotoxicity, hematotoxicity, genotoxicity, teratogenicity, bone fractures, and skin allergy in mammals even at a low concentration."( Hazardous impact of diclofenac on mammalian system: Mitigation strategy through green remediation approach.
Balasubramanian, M; Brar, SK; Chitra, L; Ganesan, AR; Gu, FL; Meena, RAA; Mohan, K; Palvannan, T; Sathishkumar, P, 2021
)
1.67
"Diclofenac (DCF) can cause adverse reactions such as gastrointestinal, renal and cardiovascular disorders; therefore, topical administration may be an attractive alternative to the management of local pain in order to avoid these side effects. "( Photo(geno)toxicity changes associated with hydroxylation of the aromatic chromophores during diclofenac metabolism.
Andreu, I; Consuelo Jiménez, M; Garcia-Lainez, G; Limones-Herrero, D; Martínez-Reig, AM; Miranda, MA, 2018
)
2.14
"Diclofenac (DIC) can cause nephrotoxicity in humans. "( Ameliorative effects of N-acetyl cysteine on diclofenac-induced renal injury in male rats based on serum biochemical parameters, oxidative biomarkers, and histopathological study.
Heidarian, E; Nouri, A, 2019
)
2.22
"Diclofenac can cause damage to the function of mucous membrane barricade of small intestine. "( [Effect of non-steroidal anti-inflammatory drugs on small intestinal barrier function in rats].
Chen, FM; Lü, B; Meng, LN; Si, JM; Wu, WF; Yu, LM; Zhang, S, 2009
)
1.8
"S-diclofenac derivatives inhibit osteoclast formation and activity, suppress breast cancer cell support for osteoclastogenesis and prevent osteolysis. "( Hydrogen sulphide-releasing diclofenac derivatives inhibit breast cancer-induced osteoclastogenesis in vitro and prevent osteolysis ex vivo.
Del Soldato, P; Frantzias, J; Idris, AI; Logan, JG; Mollat, P; Ralston, SH; Sparatore, A, 2012
)
1.39
"Diclofenac does not cause a significant change in cerebral blood flow velocity in patients with supratentorial tumours."( Effect of diclofenac on cerebral blood flow velocity in patients with supratentorial tumours.
Dinsmore, J; Jones, SJ, 2002
)
2.16
"Diclofenac caused the increase in intestinal permeability, enteric bacterial count, enteric protein and albumin loss and bacterial translocation. "( [Effect of glutamine on the non-steroidal anti-inflammatory drug-induced bacterial translocation].
Ann, JY; Chang, SK; Do, JH; Han, SP; Jeon, WK; Kim, HJ; Kim, JG; Kim, JW; Kim, SJ, 2004
)
1.77
"Diclofenac intake was lower in the Viscoseal group from Day 3 to Day 28 with a proven superiority (LB-CI > 0.5) in favour of Viscoseal on Days 3 (MW-S: P = 0.0093), 4 (MW-S: P= 0.0075), and 7 (MW-S: P = 0.0195) indicating that the product had an NSAID-sparing effect."( Effects of Viscoseal, a synovial fluid substitute, on recovery after arthroscopic partial meniscectomy and joint lavage.
Mathies, B, 2006
)
1.06
"Diclofenac caused the increase in gut damage, enteric bacterial numbers and BT. "( Combined effects of bovine colostrum and glutamine in diclofenac-induced bacterial translocation in rat.
Jeon, WK; Kim, EJ; Kim, JW, 2005
)
2.02
"Diclofenac can cause gastric mucosal lesions, including ulcers, more easily than other NSAIDs. "( Up-to-date information on gastric mucosal lesions from long-term NSAID therapy in orthopedic outpatients: a study using logistic regression analysis.
Fukui, H; Takakura, Y; Yajima, H; Yamao, J, 2007
)
1.78
"Diclofenac inhibits the increase in both pulmonary arterial pressure and EVLW during reperfusion and reventilation of LLL. "( Effect of cyclooxygenase inhibition in a canine model of unilateral pulmonary occlusion and reperfusion.
Albrecht, DM; Krieter, H; Segiet, W; Stieber, C; van Ackern, K, 1995
)
1.73
"Diclofenac did not inhibit corneal haze formation significantly."( Effect of anti-inflammatory agents on corneal wound-healing process after surface excimer laser keratectomy.
Amano, S; Kaji, Y; Obata, H; Ohashi, T; Oshika, T; Sakai, H; Shirasawa, E; Tsuru, T; Yamashita, H, 2000
)
1.03
"Diclofenac and metamizol inhibit prostaglandin synthesis, thus attenuate the peripheral nociceptive sensitization caused by the surgical trauma."( Diclofenac and metamizol in postoperative analgesia in plastic surgery.
Büyükkocak, U; Cinel, I; Oral, U; Saray, A; Tellioglu, AT, 2001
)
2.47

Treatment

Diclofenac treatment caused kidney and liver function test abnormalities, reduced hematocrit and hemoglobin levels but increased WBC and platelet counts. The dicl ofenac-treated group had a significantly lower opioid consumption in the first 24 hours postoperatively than their untreated counterparts.

ExcerptReferenceRelevance
"Diclofenac treatment induced an overall delay in developmental landmarks of puberty onset in male and female offspring, which reached statistical significance for PPS at the lowest diclofenac dose."( Prenatal diclofenac exposure delays pubertal development and induces behavioral changes in rats.
Curi, TZ; da Silva, GN; Dos Santos, AC; Grechi, N; Hey, GS; Krebs Ribeiro, DC; Martino-Andrade, AJ; Meldola, H; Passoni, MT; Ramos, ATA; Souza, RIC; Spercoski, KM; Tolouei, SEL, 2020
)
1.7
"The diclofenac-treated group had a significantly lower opioid consumption in the first 24 hours postoperatively than did their untreated counterparts (39.8 vs."( The Addition of Diclofenac to a Multimodal Pain Control Regimen Decreases Postoperative Pain and Opioid Consumption.
De Souza, R; Delanois, RE; Etcheson, JI; George, NE; Gurk-Turner, C; Gwam, CU; Nace, J; Smith, SS, 2017
)
1.28
"Diclofenac sodium treatment significantly ("( Assessment of dose-dependent reproductive toxicity of diclofenac sodium in male rats.
Purohit, A; Ram, H; Vyas, A, 2019
)
1.48
"Diclofenac treatment caused kidney and liver function test abnormalities, reduced hematocrit and hemoglobin levels but increased WBC and platelet counts."( Diclofenac induced gastrointestinal and renal toxicity is alleviated by thymoquinone treatment.
Akkaya, B; Aslan, M; Aycan, İÖ; Coşkunfırat, N; Elpek, Ö; Kaya, S; Kıraç, E; Tuzcu, H, 2018
)
2.64
"Diclofenac treatment exerted a teratogenic effect on Xenopus embryos with a teratogenic index (TI) value of 2.64 TI; if this value is higher than 1.2, the cut-off value indicative of toxicity."( Evaluation of developmental toxicity and teratogenicity of diclofenac using Xenopus embryos.
Chae, JP; Hwang, YS; Kim, SH; Lee, HS; Min, BH; Park, MJ; Park, MS, 2015
)
1.38
"Diclofenac treatment was most effective at inhibiting pupil miosis when the hardness of the nucleus was grade 3, P=0.009."( Effect of topical nonsteroidal anti-inflammatory drugs and nuclear hardness on maintenance of mydriasis during phacoemulsification surgery.
Liu, C; Liu, L; Liu, Y; Wu, M; Ye, S; Zhang, W, 2014
)
1.12
"Diclofenac pretreatment eliminated these respiratory effects of IL-1β."( Cyclooxygenase pathway in modulation of the ventilatory response to hypercapnia by interleukin-1β in rats.
Aleksandrov, VG; Aleksandrova, NP; Danilova, GA, 2015
)
1.14
"Diclofenac-treated cats had a significantly lower glomerular filtration rate than did control-treated cats after the second but not after the first treatment period, presumably associated with iatrogenic hypovolemia."( Systemic absorption and adverse ocular and systemic effects after topical ophthalmic administration of 0.1% diclofenac to healthy cats.
Allen, DG; Hsu, KK; Johnson, RJ; KuKanich, BK; Nykamp, SG; Pinard, CL, 2015
)
1.35
"Diclofenac treatment produced dose-related reversal of CRANE at 0.03-1.0 mg/kg with a plateau effect observed at higher doses (up to 30 mg/kg)."( Complete Freund's adjuvant-induced reduction of exploratory activity in a novel environment as an objective nociceptive endpoint for sub-acute inflammatory pain model in rats.
Bannon, AW; Joshi, SK; Zhu, CZ, 2015
)
1.14
"Diclofenac treatment of mice at 30 mg/kg for 3 days caused significant serum ALT and AST elevations, hepatomegaly and degenerative changes including hepatic glycogen depletion, hydropic swelling, cholesterolosis and eosinophilic hepatocytes with one animal presenting subsegmental infarction due to portal vein thrombosis."( Immunogenomics reveal molecular circuits of diclofenac induced liver injury in mice.
Borlak, J; Choi, MS; Lee, EH; Oh, JH; Park, SM; Selvaraj, S; Spanel, R; Yoon, S, 2016
)
1.42
"Diclofenac treatment was associated with increased activity of caspases 3, 7, and 8 and induction of p53 transcriptional target genes."( Modulation of p73 isoforms expression induces anti-proliferative and pro-apoptotic activity in mantle cell lymphoma independent of p53 status.
Chaturvedi, NK; Dave, BJ; Hassan, HM; Joshi, SS; Singh, RK; Varney, ML; Weisenburger, DD, 2016
)
1.16
"S-diclofenac treatment also resulted in stabilization of p53 coupled with the induction of downstream proteins such as p21, p53AIP1 and Bax."( Effect of S-diclofenac, a novel hydrogen sulfide releasing derivative inhibit rat vascular smooth muscle cell proliferation.
Baskar, R; Del Soldato, P; Moore, PK; Sparatore, A, 2008
)
1.28
"Diclofenac treatment resulted in a significant reduction in COX-2 expression and its activity."( Modulation of inflammatory changes in early stages of colon cancer through activation of PPARgamma by diclofenac.
Kaur, J; Sanyal, SN, 2010
)
1.3
"Diclofenac treatment ameliorated the elevated delta psi M and its associated events to exert its chemopreventive action against early stages of colon cancer."( Intrinsic mitochondrial membrane potential change and associated events mediate apoptosis in chemopreventive effect of diclofenac in colon cancer.
Kaur, J; Sanyal, SN, 2010
)
1.29
"Diclofenac treatment was discontinued and occasional use of acetaminophen for the back pain was recommended."( Hemoptysis under diclofenac and antiplatelet doses of aspirin.
Yiannakopoulou, EC, 2011
)
1.43
"Diclofenac sodium-treated birds showed severe clinical signs of toxicity with high mortality, a significant increase (P < 0.01) in serum concentrations of creatinine, uric acid, alanine aminotransferase, and aspartate aminotransferase, and these changes correlated well with gross and microscopic examination findings of kidney and liver."( An initial safety assessment of hepatotoxic and nephrotoxic potential of intramuscular ketoprofen at single repetitive dose level in broiler chickens.
Jayakumar, K; Manafi, M; Mohan, K; Narayanaswamy, HD; Pavithra, BH, 2012
)
1.1
"Diclofenac treatment could result in an increased proportion of patients with anastomotic leakage after colorectal surgery. "( Postoperative use of non-steroidal anti-inflammatory drugs in patients with anastomotic leakage requiring reoperation after colorectal resection: cohort study based on prospective data.
Gögenur, I; Klein, M; Rosenberg, J, 2012
)
1.82
"Diclofenac treatment caused a significant delay in new bone formation in association with an impairment of blood clot remission/organization."( Histometric study of socket healing after tooth extraction in rats treated with diclofenac.
Brentegani, LG; Lamano Carvalho, TL; Sala, MA; Yugoshi, LI, 2002
)
1.26
"Diclofenac treatment significantly diminished hematocrit, hemoglobin, and corpuscular volume and increased the number of platelets."( Gastrointestinal tolerability of metamizol, acetaminophen, and diclofenac in subchronic treatment in rats.
Alarcón de la Lastra, C; Martín, MJ; Motilva, V; Ortiz, P; Sánchez, S, 2002
)
1.28
"Diclofenac treatments (1 mg/kg bid) selectively decreased the accumulation of neutrophils and ED1(+) macrophages by 59% and 35%, respectively, in the paratenon, where blood vessels are numerous, but did not reduce the accumulation of neutrophils and ED1(+) macrophages in the core of the tendon."( Nonsteroidal anti-inflammatory drug reduces neutrophil and macrophage accumulation but does not improve tendon regeneration.
Côté, CH; Frenette, J; Marsolais, D, 2003
)
1.04
"Diclofenac-treated patients exhibited a marked fall in intraocular pressure (p<0.01), whereas in placebo-treated patients, this diminution was less noticeable (p<0.05)."( The influence of diclofenac ophthalmic solution on the intraocular pressure-lowering effect of topical 0.5% timolol and 0.005% latanoprost in primary open-angle glaucoma patients.
Antinozzi, PP; Caccavale, A; Costagliola, C; Cotticelli, L; Parmeggiani, F; Sebastiani, A, 2005
)
1.39
"In diclofenac-treated eyes, mean changes in visual acuity letter score from baseline in the diclofenac and placebo groups were +1.8 letters and -1.0 at week 1 (P=0.505 between groups). "( Effect of adjunctive diclofenac with verteporfin therapy to treat choroidal neovascularization due to age-related macular degeneration: phase II study.
Beer, PM; Boyer, DS; Joffe, L; Koester, JM; Marx, JL; Weisberger, A; Yoser, SL,
)
1.07
"Diclofenac-treated MDCKII cells on the other hand showed extensive propidium iodide staining, suggestive of cell death by necrosis."( Nephrotoxic cell death by diclofenac and meloxicam.
Halliwell, B; Ng, LE; Wong, KP, 2008
)
1.37
"The diclofenac sodium treatment (total of 58 periods) reduced the pain significantly in comparison with placebo (57 periods), as evaluated by subjective rating (P less than 0.001) and by a 6-point scale of pain intensity (P less than 0.05)."( Treatment of primary dysmenorrhea with diclofenac sodium.
Pulkkinen, MO; Riihiluoma, P; Wuolijoki, E, 1981
)
1.01
"The diclofenac-treated patients rarely experienced the early peak in pain, had less pain overall until 72 hours postoperatively, and experienced significantly less photophobia and burning/stinging."( Topical diclofenac in the treatment of ocular pain after excimer photorefractive keratectomy.
Carpel, E; DeMarchi, J; Doughman, D; Frantz, JM; Lane, SS; Lindstrom, R; Ostrov, C; Parker, P; Sher, NA; Talley, A,
)
1.05
"Diclofenac treatment was discontinued in two patients, due to a duodenal ulcer or severe erosive gastritis."( Non-steroidal anti-inflammatory drug-induced gastropathy: a comparative endoscopic and histopathological evaluation of the effects of tenoxicam and diclofenac.
al-Habdan, I; al-Nahdi, M; al-Quorain, AA; Marwah, S; Satti, MB,
)
1.05
"Diclofenac-treated patients experienced significantly less photophobia, burning/stinging, and ocular pain and took significantly fewer oral narcotic analgesics over the first 24 hours postoperatively than placebo-treated patients."( Efficacy and safety of topical diclofenac in reducing ocular pain after excimer photorefractive keratectomy.
Cherry, PM; Fsadni, MG; Raj, PS; Tutton, MK, 1996
)
2.02
"Diclofenac treatment can lead to overestimation in ureteral stone disease, by delaying renal excretion bilaterally, but predominantly on the side of calculus."( Diclofenac treatment prolongs renal transit time in acute ureteral obstruction: a renographic study.
Jacobsson, H; Kinn, AC; Larsson, SA; Nelson, E, 2000
)
3.19
"Thus diclofenac pretreatment partially prevented the insult-induced increase in total and regional neuronal c-fos-LI."( The effect of diclofenac on the expression of spinal cord c-fos-like immunoreactivity after ischemia-reperfusion-induced acute hyperalgesia in the rat tail.
Cousins, MJ; Lin, Y; Mather, LE; Power, I, 2000
)
1.12
"The diclofenac-treated group showed a statistically significant decrease in corneal sensitivity (p < 0.001) at the measurement carried out 15 min after instillation of the last drop and lasting up to the end of the study, when the corneal anaesthesia was similar to that induced by the topical anaesthetic treatment."( The effects of the topical administration of non-steroidal anti-inflammatory drugs on corneal epithelium and corneal sensitivity in normal subjects.
Aragona, P; Ferreri, G; Laganà, E; Spinella, R; Tripodi, G, 2000
)
0.79
"Diclofenac treatment resulted in the formation of drug adducts in enterocytes. "( Drug enterocyte adducts: possible causal factor for diclofenac enteropathy in rats.
Aronson, JF; Atchison, CR; Balakumaran, A; Daiker, DH; Hargus, SJ; Hoffmann, WE; Pohl, LR; Shipp, BK; Treinen-Moslen, M; West, AB, 2000
)
2
"Diclofenac-treated patients experienced statistically significant elevations in mean hepatic transaminases and serum creatinine and reductions in haemoglobin concentration when compared to placebo, events not observed with celecoxib."( Celecoxib versus diclofenac in the management of osteoarthritis of the knee.
Borenstein, D; Geis, GS; Lefkowith, JB; McKenna, F; Wallemark, C; Wendt, H, 2001
)
1.37
"One diclofenac-treated patient had a significant increase in alanine aminotransferase at the final evaluation."( Comparison of etodolac and diclofenac in osteoarthritis of the knee.
Grisanti, AM; Samara, AM; Vaz, AA,
)
0.91
"The diclofenac treatment had no influence on hematological and coagulation profiles, nor on muscle and liver enzymes in comparison with placebo."( Prophylactic diclofenac infusions in major orthopedic surgery: effects on analgesia and acute phase proteins.
Camu, F; Claeys, MA; Maes, V, 1992
)
1.13
"Diclofenac pretreatment prevented PGI2 synthesis and significantly reduced fluid extravasation."( Bradykinin-induced oedema formation proceeds from B2 receptor stimulation and is potentiated by concomitantly released prostaglandins.
Afflerbach, F; Berghöfer, A; Llach Puig Neppl, J; Neppl, H; Neuhof, H, 1991
)
1
"Diclofenac acid pretreatment and daily injections prevented lung collagen accumulation after intratracheal bleomycin."( The effect of diclofenac acid (Voltaren) on bleomycin-induced pulmonary fibrosis in hamsters.
Chandler, DB; Young, K, 1989
)
1.36
"Treatment with diclofenac sodium vs hydrocodone/APAP did not statistically impact pain scores at PODs 1, 2, 3, or 5."( Are nonsteroidal anti-inflammatory drugs effective enough for postoperative pain control after functional endoscopic sinus surgery and septoplasty? A randomized, controlled study.
Citardi, MJ; Jiang, ZY; Luong, AU; Radabaugh, P; Saini, AT; Schmale, I; Starr, NC; Talmadge, J; Yao, WC, 2022
)
1.06
"Pretreatment with diclofenac for four weeks improved the clearance rate in one study (24.9%), administration of retinoids had a significant effect in one of two studies (16.25%), while salicylic acid and urea did not lead to improved PDT efficacy."( Improving the efficacy of photodynamic therapy for actinic keratosis: A comprehensive review of pharmacological pretreatment strategies.
Andersen, F; Bjerring, P; Haedersdal, M; Lerche, CM; Pihl, C, 2023
)
1.23
"Treatment with diclofenac only on the right side of the body resulted in clearing of 55% of all treated lesions, which increased to 60% three months after finishing therapy."( Using photodynamic therapy to estimate effectiveness of innovative combined diclofenac and tazaroten therapy of disseminated actinic keratosis.
Jurczyszyn, K; Lipinski, A; Nockowski, P; Osiecka, BJ; Sieja, A; Ziółkowski, P, 2015
)
0.99
"sBCC treated with diclofenac showed a significant decrease in Ki-67 (P < .001) and Bcl-2 (P = .001), and after combination therapy for Ki-67 (P = .012). "( The effect of topical diclofenac 3% and calcitriol 3 μg/g on superficial basal cell carcinoma (sBCC) and nodular basal cell carcinoma (nBCC): A phase II, randomized controlled trial.
Brinkhuizen, T; Frencken, KJ; Hoff, ML; Kelleners-Smeets, NW; Mosterd, K; Nelemans, PJ; Rennspiess, D; van der Horst, MP; van Steensel, MA; Winnepenninckx, VJ; Zur Hausen, A, 2016
)
1.08
"The treatment with diclofenac sodium, in the PTZ induced kindling model, decreased severity of seizures and interleukin-6 and TNF-α levels in the hippocampus of animals treated with doses of 5 and 10mg/kg."( Effect of diclofenac sodium on seizures and inflammatory profile induced by kindling seizure model.
Coitinho, AS; Glassmann, D; Gomez, R; Marafon, P; Pereira, P; Vieira, V, 2016
)
1.16
"The treatment with diclofenac caused significantly lower sodium plasma concentrations whereas the concentration of potassium was increased."( Interaction of diclofenac and ketoprofen with cardioactive drugs in rats.
Jakovljevic, V; Milijasević, B; Popovic, M; Rasković, A; Sabo, A; Tomić, Z; Vasovic, V,
)
0.8
"Treatment with diclofenac sodium and bromfenac sodium ophthalmic solution prevented progression of anterior capsule contraction and PCO."( Efficacy of ophthalmic nonsteroidal antiinflammatory drugs in suppressing anterior capsule contraction and secondary posterior capsule opacification.
Aose, M; Gotoh, N; Matsui, E; Matsushima, H; Mukai, K; Nagata, M; Satoshi, W; Senoo, T; Wataru, T, 2009
)
0.69
"Treatment with diclofenac sodium during a relatively long period of reversible unilateral ureteric obstruction, similar to its use in the management of ureteric colic, appears to ameliorate the alterations in the hemodynamic glomerular functions at least 2 weeks following the reversal of obstruction."( The effect of diclofenac sodium on renal function in reversible unilateral ureteric obstruction.
Hammad, FT; Lubbad, L, 2011
)
1.07
"Treatment with diclofenac in HA is effective and well tolerated during a treatment period of 3 months as well as 6 months. "( Open label randomized study comparing 3 months vs. 6 months treatment of actinic keratoses with 3% diclofenac in 2.5% hyaluronic acid gel: a trial of the German Dermatologic Cooperative Oncology Group.
Dirschka, T; Eigentler, TK; Garbe, C; Held, L; Leiter, U; Nashan, D; Pflugfelder, A; Stockfleth, E; Weide, B; Welter, AK, 2012
)
0.95
"Treatment with diclofenac sodium extending past the acute inflammatory phase was no more effective than short and timely treatment in this model of skeletal muscle damage."( Influence of nonsteroidal anti-inflammatory drug treatment duration and time of onset on recovery from exercise-induced muscle damage in rats.
Côté, CH; Frémont, P; Lapointe, BM, 2003
)
0.67
"Treatment with diclofenac resulted in nuclear condensation (a morphological change due to apoptosis of NSCs) 24hr after the treatment and activated caspase-3 after 6 hr, indicating that diclofenac may cause apoptosis of neuronal cells via activation of the caspase cascade."( Diclofenac inhibits proliferation and differentiation of neural stem cells.
Kamisaki, Y; Kori, M; Kudo, C; Matsuzaki, K; Nakajima, A; Niwa, H; Shibuya, A; Wada, K; Yamai, K, 2003
)
2.1
"Rats treated with diclofenac did not exhibit reductions in rate of responding or total reinforcers obtained."( The non-steroidal anti-inflammatory drug diclofenac sodium attenuates lipopolysaccharide-induced alterations to reward behavior and corticosterone release.
Asnis, GM; De La Garza, R; Fabrizio, KR; Radoi, GE; Vlad, T, 2004
)
0.91
"Treatment with diclofenac or 5-Fu resulted in elevated COX-2 mRNA expression both in HepG2 and Hep3B cells."( [Diclofenac suppresses hepatoma cell proliferation and promotes cyclooxygenase-2 mRNA expression].
Chen, NN; Wu, SG, 2006
)
1.58
"Pretreatment with diclofenac Na significantly attenuated the IOP lowering effect of tafluprost in WT mice but not in EP3KO mice."( The IOP-lowering effects and mechanism of action of tafluprost in prostanoid receptor-deficient mice.
Aihara, M; Araie, M; Narumiya, S; Ota, T; Saeki, T, 2007
)
0.66
"Pretreatment with diclofenac or ibuprofen blocked pain behaviour (SBL) after activation of excitatory amino acid receptors of the NMDA type, but not pain behaviour after activation of AMPA or substance P (SP) receptors."( Central antinociceptive effects of non-steroidal anti-inflammatory drugs and paracetamol. Experimental studies in the rat.
Björkman, R, 1995
)
0.61
"Pretreatment with diclofenac alone or in combination with methylprednisolone did not result in a notable increase in the incidence of complications as compared to placebo."( Effect of preoperative single doses of diclofenac and methylprednisolone on wound healing.
Hyrkäs, T, 1994
)
0.88
"Posttreatment with diclofenac was more effective than posttreatment with indomethacin."( Mechanism of diclofenac analgesia: direct blockade of inflammatory sensitization.
Ferreira, SH; Tonussi, CR, 1994
)
0.98
"Both treatment with diclofenac before surgery and delayed treatment were superior to placebo concerning pain scores within 6 h after onset of anaesthesia (P < 0.0065 and P < 0.0005, respectively)."( Diclofenac for pain relief after arthroscopy: a comparison of early and delayed treatment.
Björkman, R; Brodd, B; Sandin, R; Stam, H; Sternlo, JE, 1993
)
2.04
"Pretreatment of diclofenac inhibited LPS-induced expression of E-selectin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) in HUVEC, determined by flow cytometry and a cellular enzyme-linked immunosorbent assay (cell-ELISA)."( Diclofenac inhibits endothelial cell adhesion molecule expression induced with lipopolysaccharide.
Sakai, A, 1996
)
2.07
"pretreatment with diclofenac (100-500 micrograms/animal), a cyclooxygenase inhibitor other than indomethacin."( Brain prostaglandins mediate the bombesin-induced increase in plasma levels of catecholamines.
Okuma, Y; Osumi, Y; Yokotani, K, 1996
)
0.62
"Treatment with diclofenac sodium tended to normalize this activity but there was no significant histological improvement."( Modulation of murine osteoarthritis.
Bitensky, L; Chambers, MG; Chayen, J, 1996
)
0.63
"Treatment with diclofenac sodium, 0.1%, revealed a significantly more rapid improvement of the clinical symptoms as compared with sodium chloride, 5%."( Diclofenac sodium, 0.1% (Voltaren Ophtha), versus sodium chloride, 5%, in the treatment of filamentary keratitis.
Appel, I; Avisar, R; Robinson, A; Weinberger, D; Yassur, Y, 2000
)
2.09
"PMNs treated with diclofenac alone or fMLP alone."( Stimulation of human polymorphonuclear leukocytes potentiates the uptake of diclofenac and the inhibition of chemotaxis.
Giroud, JP; Hakim, J; Perianin, A, 1990
)
0.83
"Pretreatment with diclofenac 0.1% eye drops effectively inhibited paracentesis-induced miosis; the postoperative pupil narrowing amounted to only 9% of the original diameter in both untreated and atropine-treated eyes."( Prevention of surgically induced miosis by diclofenac eye drops.
Bellucci, R; Bonomi, L; De Franco, I; Massa, F; Perfetti, S, 1987
)
0.86

Toxicity

The new diclofenac+thiocolchicoside FDC formulation may allow treating effectively acute LBP while reducing the number of injections and hence the risk of local adverse reactions.

ExcerptReferenceRelevance
" The five most commonly reported adverse events were abdominal pain by 23."( Overall safety of Arthrotec.
Geis, GS, 1992
)
0.28
" Under conditions of vitamin A deficiency formation of acetanilide toxic metabolites was increased as a result of which excretion of mercapturic acids with urine was elevated but excess of vitamin A and its hyperdose inhibited these reactions."( [Biotransformation and toxicity of xenobiotics in various routes of administration of vitamin A into the rat body].
Bogdanov, NG; Gutsol, VI; Pentiuk, AA,
)
0.13
"Peptic gastroduodenal lesions due to nonsteroidal antiinflammatory drugs (NSAID) are well known, but not the adverse effects of these preparations in the lower GI tract."( [Side effects of non-steroidal antirheumatic agents in the lower gastrointestinal tract].
Güller, R, 1987
)
0.27
" Five (26%) fentiazac-treated patients and four (21%) diclofenac sodium-treated patients reported adverse effects, mostly gastro-intestinal."( The efficacy and safety of fentiazac and diclofenac sodium in peri-arthritis of the shoulder: a multi-centre, double-blind comparison.
Kolarz, G; Mayrhofer, F; Scherak, O; Thumb, N,
)
0.65
" Documentation is derived from clinical trials, post-marketing surveillance, special studies, and spontaneous reports of adverse drug reactions from foreign countries."( Worldwide safety experience with diclofenac.
Catalano, MA, 1986
)
0.55
" This relatively little known side effect of these drugs on the lower intestinal tract is apparently not rare."( [Side effects of non-steroidal antirheumatic agents on the lower intestinal tract].
Filippini, L; Ritschard, T, 1986
)
0.27
" Adverse experiences were infrequent and generally mild or transient."( Worldwide clinical safety experience with diclofenac.
Willkens, RF, 1985
)
0.53
" In both groups, the most frequently reported adverse events were gastrointestinal in nature, with abdominal pain reported most frequently (in 22."( Review of the safety of diclofenac/misoprostol.
Gagnier, P, 1993
)
0.59
" Of 273 elderly patients treated with at least 600 mg daily, only 12% withdrew because of adverse events, a rate similar to that in the younger age-group."( Safety profile of etodolac in the elderly population.
Bacon, PA, 1994
)
0.29
" Local adverse events were minimum for both groups."( Single blind study to evaluate the efficacy and safety of naproxen gel compared with diclophenac emulgel in the treatment of soft tissue injuries.
Butrón, F; Galicia, A; Martinez-Zurita, F; Zamora, G, 1994
)
0.29
" Safety was measured in 3 ways: (1) physician global rating scale, (2) number of patients with adverse events, and (3) dropouts due to adverse events."( A study to determine the efficacy and safety of tenoxicam versus piroxicam, diclofenac and indomethacin in patients with osteoarthritis: a meta-analysis.
Bersinic, S; Cuddy, LJ; Riedemann, PJ; Torrance, GW; Tugwell, PX, 1993
)
0.52
" However, the combination of diclofenac and pirarubicin was more toxic than pirarubicin alone and induced centrolobular necrosis and sclerosing cholangitis."( Oral diclofenac combined with intra-portal pirarubicin: increased efficacy on liver VX2 tumour and hepatotoxicity in rabbits.
Ardouin, P; Bognel, C; Donatini, B; Munck, JN; Ramirez, L; Rougier, P, 1994
)
1.09
" The fact that is a potent analgesic spread its use to almost all fields in medicine, increasing the reports of adverse effects associated with it."( [Tissue necrosis: a side effect of sodium diclofenac: report of cases and discussion of the physiopathology].
Alonso, N; Borrelli Júnior, M; Branco, PD; Giovannetti, M; Ikejiri, CI; Machado, MA,
)
0.4
" We suggest that the immune complex mechanism could have induced these adverse reactions."( Serious adverse effects induced by simultaneous administration of two nonsteroidal anti-inflammatory drugs.
Awaya, N; Handa, M; Matsuyama, M; Ogino, M; Okada, H; Saruta, T; Suzuki, H; Toya, S, 1993
)
0.29
" The incidence of > or = 1 adverse event considered by the investigator to be related or probably related to therapy was similar in all groups."( Safety experience with nabumetone versus diclofenac, naproxen, ibuprofen, and piroxicam in osteoarthritis and rheumatoid arthritis.
DeLapp, RE; Eversmeyer, W; Jensen, CP; Poland, M, 1993
)
0.55
" On the contrary, verapamil even accentuates the toxic effects of diclofenac."( Failure of calcium antagonistic agents to prevent hepatotoxicity induced by diclofenac.
Estler, CJ; Lepper, H; Schmitz, G, 1995
)
0.76
"Topical diclofenac significantly reduced the ocular pain and discomfort immediately after excimer PRK without any clinically significant complications or adverse effects."( Efficacy and safety of topical diclofenac in reducing ocular pain after excimer photorefractive keratectomy.
Cherry, PM; Fsadni, MG; Raj, PS; Tutton, MK, 1996
)
1.01
" Forty-two adverse events possibly or probably related to treatment were observed in the aceclofenac group and 37 in the tenoxicam group."( Aceclofenac is as safe and effective as tenoxicam in the treatment of ankylosing spondylitis: a 3 month multicenter comparative trial. Spanish Study Group on Aceclofenac in Ankylosing Spondylitis.
de Buergo, M; Montull Fruitós, E; Rico Lenza, H; Villa Alcázar, LF, 1996
)
0.29
" Adverse events in both groups were minor, predominantly gastro-intestinal, and fewer patients tended to experience gastro-intestinal events on aceclofenac (13%) than on diclofenac (17%)."( A multi-centre, double-blind comparative study of the efficacy and safety of aceclofenac and diclofenac in the treatment of rheumatoid arthritis.
Ferrer, F; Marcolongo, R; Parnham, MJ; Pasero, G; Serni, U, 1995
)
0.71
"We sought to identify differences in the description of adverse drug experiences in reports of randomized clinical trials (RCTs) from the United States and Japan, using diclofenac and simvastatin as test drugs."( Japanese and American reports of randomized trials: differences in the reporting of adverse effects.
Hayashi, K; Walker, AM, 1996
)
0.49
" The overall pattern of adverse events and laboratory abnormalities in the study population were similar to those reported in patients with RA treated with other nonsteroidal antiinflammatory agents and concomitant cyclosporine."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
1.74
" There were no adverse reactions in either group."( [Comparative, randomized, parallel clinical study of the effectiveness and safety of aceclofenac vs. paracetamol in the treatment of viral pharyngoamygdalitis].
Conti, M, 1997
)
0.3
" Adverse events incidence and severity were assessed."( [Efficacy and safety of nabumetone in the treatment of knee osteoarthritis: a comparative clinical trial versus aceclofenac. Study Group of Nabumetone for Osteoarthritis of the Knee].
Gijón Baños, J, 1997
)
0.3
" 15 nabumetone-treated and 23 aceclofenac-treated patients withdrew from the study due to moderate to severe adverse events."( [Efficacy and safety of nabumetone in the treatment of knee osteoarthritis: a comparative clinical trial versus aceclofenac. Study Group of Nabumetone for Osteoarthritis of the Knee].
Gijón Baños, J, 1997
)
0.3
" Ultimately it is the balance between bioactivation, detoxification, and defense mechanisms that determines whether a compound will or will not elicit a toxic effect."( The use of cultured hepatocytes to investigate the mechanisms of drug hepatotoxicity.
Bort, R; Castell, JV; Gómez-Lechón, MJ; Ponsoda, X, 1997
)
0.3
"A report is presented of five aged patients with hemorrhagic colon ulcer, which was strongly suspected to be a side effect of non steroidal anti-inflammatory drugs (NSAID)."( [Hemorrhagic colon ulcer as a side effect of non-steroidal anti-inflammatory drugs in five aged patients].
Kusakabe, N; Matsui, I; Matsui, Y; Matsumura, Y; Morimoto, S; Ogihara, T; Takahashi, E, 1997
)
0.3
" Adverse events were similar between groups (P = ."( The efficacy and safety of diclofenac 0.1% versus prednisolone acetate 1% following trabeculectomy with adjunctive mitomycin-C.
Cate, EA; Dubiner, HB; Kent, AR; Mundorf, TK; Stewart, JA; Stewart, WC; Whitaker, R, 1998
)
0.6
" Evaluation of the profile of adverse events was the main aim of the trial, together with assessment of efficacy."( Gastrointestinal tolerability of meloxicam compared to diclofenac in osteoarthritis patients. International MELISSA Study Group. Meloxicam Large-scale International Study Safety Assessment.
Alegre, C; Baumelou, E; Bégaud, B; Dequeker, J; Hawkey, C; Isomäki, H; Kahan, A; Littlejohn, G; Mau, J; Papazoglou, S; Steinbrück, K, 1998
)
0.55
"Diclofenac, a 2-arylacetic acid, nonsteroidal anti-inflammatory drug, has been reported to cause adverse hepatic effects in certain individuals."( Diclofenac toxicity to hepatocytes: a role for drug metabolism in cell toxicity.
Bort, R; Castell, JV; Gómez-Lechón, MJ; Jover, R; Ponsoda, X, 1999
)
3.19
" We identified epidemiologic studies, published from January 1970 to December 1995, that investigated the association of serious adverse effects with aspirin, diclofenac, acetaminophen, and dipyrone to determine and compare the excess mortality associated with short-term drug use."( Comparative safety evaluation of non-narcotic analgesics.
Andrade, SE; Martinez, C; Walker, AM, 1998
)
0.5
" Adverse symptoms were acceptable with both drugs."( A double-blind evaluation of the analgesic efficacy and toxicity of oral ketorolac and diclofenac in cancer pain. The TD/10 recordati Protocol Study Group.
Camaggi, CM; Pannuti, F; Robustelli della Cuna, G; Strocchi, E; Ventaffrida, V,
)
0.35
" Types of adverse events were similar for all treatment groups, with GI adverse events predominating."( Comparison of the upper gastrointestinal safety of Arthrotec 75 and nabumetone in osteoarthritis patients at high risk for developing nonsteroidal anti-inflammatory drug-induced gastrointestinal ulcers.
Agrawal, NM; Ball, J; Bocanegra, TS; Caldwell, J; Dhadda, S; Hancock, L; Hurley, S; Kivitz, AJ; Weaver, AL, 1999
)
0.3
"5%) dropped out in the nimesulide group (two early recovery, one lack of effect, one adverse event), compared with 13 (21."( Comparative efficacy and safety of nimesulide and diclofenac in patients with acute shoulder, and a meta-analysis of controlled studies with nimesulide.
Wober, W, 1999
)
0.56
" This is due to the lower incidence of gastrointestinal adverse events with nimesulide, and the absence of serious gastrointestinal complications leading to hospitalization, which more than offset the higher acquisition cost of nimesulide."( Economic comparison of nimesulide and diclofenac, and the incidence of adverse events in the treatment of rheumatic disease in Greece.
Liaropoulos, L, 1999
)
0.57
" However, while effective, it has low oral bioavailability and some problematic adverse effects."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.52
" Diclofenac-potassium seemed to be as well tolerated as placebo, with fewer adverse events reported than after sumatriptan treatment and with more patients assessing the overall tolerability of diclofenac-potassium better than that of sumatriptan."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
1.43
" Side effect incidence and patient and investigator opinions were also recorded."( Tolerability and safety of 0.1% diclofenac plus 0.3% tobramycin fixed-dose ophthalmic solution: a randomized, comparative, controlled study in healthy volunteers.
Andreu, D; Costa, J; Martínez, M; Notivol, R; Salvá, P, 1999
)
0.59
"To determine whether the use of diclofenac ophthalmic solution is a safe and effective analgesic in the treatment of traumatic corneal abrasions in the emergency department."( Safety and efficacy of diclofenac ophthalmic solution in the treatment of corneal abrasions.
Allegra, JR; Eskin, B; Nashed, AH; Szucs, PA, 2000
)
0.9
" The outcome measurements were improvement in NPIS score 2 hours after treatment, use of oxycodone-acetaminophen, and occurrence of any adverse effects."( Safety and efficacy of diclofenac ophthalmic solution in the treatment of corneal abrasions.
Allegra, JR; Eskin, B; Nashed, AH; Szucs, PA, 2000
)
0.62
"Diclofenac ophthalmic solution appears to be a safe and effective analgesic in the treatment of traumatic corneal abrasions in the ED."( Safety and efficacy of diclofenac ophthalmic solution in the treatment of corneal abrasions.
Allegra, JR; Eskin, B; Nashed, AH; Szucs, PA, 2000
)
2.06
"Tramadol, a weak opioid mu-receptor agonist, may have a favourable potency and side effect profile for intravenous patient-controlled analgesia (PCA)."( Efficacy and side effects of tramadol versus oxycodone for patient-controlled analgesia after maxillofacial surgery.
Rosenberg, PH; Silvasti, M; Svartling, N; Tarkkila, P; Tuominen, M, 1999
)
0.3
"Ophthalmologic adverse effects of bisphosphonate therapy are infrequent and of unclear pathogenesis."( Uveitis, an under-recognized adverse effect of pamidronate. Case report and literature review.
Acquaviva, PC; Bernard, P; Dahan, L; Daumen-Legré, V; Lafforgue, P; Pham, T; Rey, J, 2000
)
0.31
"Conventional nonsteroidal anti-inflammatory drugs (NSAIDs) are associated with a spectrum of toxic effects, notably gastrointestinal (GI) effects, because of inhibition of cyclooxygenase (COX)-1."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000
)
0.31
"To determine whether celecoxib, a COX-2-specific inhibitor, is associated with a lower incidence of significant upper GI toxic effects and other adverse effects compared with conventional NSAIDs."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000
)
0.31
"Incidence of prospectively defined symptomatic upper GI ulcers and ulcer complications (bleeding, perforation, and obstruction) and other adverse effects during the 6-month treatment period."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000
)
0.31
"In this study, celecoxib, at dosages greater than those indicated clinically, was associated with a lower incidence of symptomatic ulcers and ulcer complications combined, as well as other clinically important toxic effects, compared with NSAIDs at standard dosages."( Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.
Agrawal, NM; Burr, AM; Eisen, G; Faich, G; Geis, GS; Goldstein, JL; Kent, JD; Lefkowith, JB; Makuch, R; Pincus, T; Silverstein, FE; Simon, LS; Stenson, WF; Verburg, KM; Whelton, A; Zhao, WW, 2000
)
0.31
" Safety was assessed by evaluation of adverse events, vital signs, and laboratory data."( Safety and efficacy of meloxicam in the treatment of osteoarthritis: a 12-week, double-blind, multiple-dose, placebo-controlled trial. The Meloxicam Osteoarthritis Investigators.
Caldwell, J; Dalgin, P; Fleischmann, R; Hall, D; Roszko, P; Yocum, D, 2000
)
0.31
"The incidence of all adverse events was lower at each dosage of meloxicam than for diclofenac but greater than for placebo."( Safety and efficacy of meloxicam in the treatment of osteoarthritis: a 12-week, double-blind, multiple-dose, placebo-controlled trial. The Meloxicam Osteoarthritis Investigators.
Caldwell, J; Dalgin, P; Fleischmann, R; Hall, D; Roszko, P; Yocum, D, 2000
)
0.53
"Meloxicam is a safe and effective medication for the symptomatic treatment of OA."( Safety and efficacy of meloxicam in the treatment of osteoarthritis: a 12-week, double-blind, multiple-dose, placebo-controlled trial. The Meloxicam Osteoarthritis Investigators.
Caldwell, J; Dalgin, P; Fleischmann, R; Hall, D; Roszko, P; Yocum, D, 2000
)
0.31
" Gastrointestinal safety was assessed by the incidence of gastrointestinal symptoms and adverse events."( Treatment of elderly patients with nabumetone or diclofenac: gastrointestinal safety profile.
DeLapp, R; Kaine, J; Morgan , GJ; Palmer, R, 2001
)
0.57
" However, differences between the groups were apparent in the frequency of adverse gastrointestinal events."( Treatment of elderly patients with nabumetone or diclofenac: gastrointestinal safety profile.
DeLapp, R; Kaine, J; Morgan , GJ; Palmer, R, 2001
)
0.57
" Some xenobiotics are electrophilic, and others are biotransformed by the liver into highly reactive metabolites that are usually more toxic than the parent compound."( The use of cultured hepatocytes to investigate the metabolism of drugs and mechanisms of drug hepatotoxicity.
Bort, R; Castell, JV; Gómez-Lechón, MJ; Ponsoda, X,
)
0.13
" Toxic doses of DCLF can cause nephrotoxicity in humans and experimental animals."( Diclofenac induced in vivo nephrotoxicity may involve oxidative stress-mediated massive genomic DNA fragmentation and apoptotic cell death.
Gross, SM; Hickey, EJ; Raje, RR; Ray, SD; Reid, VE, 2001
)
1.75
"In order to detect adverse drug reactions, large observational drug safety studies are necessary as randomized clinical trials rarely have enough power."( The multiple propensity score for analysis of dose-response relationships in drug safety studies.
Donnan, PT; MacDonald, TM; Steinke, D; Wang, J,
)
0.13
" Probabilities of noncompliance, lack of efficacy and incidence of adverse events were obtained from comparative randomised double-blind clinical trials."( Iatrogenic cost factors incorporating mild and moderate adverse events in the economic comparison of aceclofenac and other NSAIDs.
Badia, X; Brosa, M; Martínez, E; Peris, F, 2001
)
0.31
"Total costs to the healthcare provider, including NSAID treatment costs (drug acquisition costs and physician visits for prescription) and iatrogenic costs (substitution treatment costs for patients not achieving clinical efficacy and costs of medical visits, treatment, diagnostic tests and hospital stays associated with adverse events) and the iatrogenic cost factor (ICF) were used as the primary outcome measures."( Iatrogenic cost factors incorporating mild and moderate adverse events in the economic comparison of aceclofenac and other NSAIDs.
Badia, X; Brosa, M; Martínez, E; Peris, F, 2001
)
0.31
"Ketorolac is approved for the relief of postoperative pain but concerns have been raised over a possible risk of serious adverse effects and death."( Ketorolac, diclofenac, and ketoprofen are equally safe for pain relief after major surgery.
Abdalla, M; Bianchi, PG; Bonnet, F; Camu, F; Ebrahim, S; Escolar, G; Forrest, JB; Greer, IA; Heitlinger, E; Jage, J; Kehlet, H; Langman, MJ; Pocock, S; Samama, MM; Velo, G, 2002
)
0.7
"38%) had a serious adverse outcome, with 19 deaths (0."( Ketorolac, diclofenac, and ketoprofen are equally safe for pain relief after major surgery.
Abdalla, M; Bianchi, PG; Bonnet, F; Camu, F; Ebrahim, S; Escolar, G; Forrest, JB; Greer, IA; Heitlinger, E; Jage, J; Kehlet, H; Langman, MJ; Pocock, S; Samama, MM; Velo, G, 2002
)
0.7
"We conclude that ketorolac is as safe as ketoprofen and diclofenac for the treatment of pain after major surgery."( Ketorolac, diclofenac, and ketoprofen are equally safe for pain relief after major surgery.
Abdalla, M; Bianchi, PG; Bonnet, F; Camu, F; Ebrahim, S; Escolar, G; Forrest, JB; Greer, IA; Heitlinger, E; Jage, J; Kehlet, H; Langman, MJ; Pocock, S; Samama, MM; Velo, G, 2002
)
0.95
" These results suggested that poloxamer gel with sodium chloride could be a more effective and safe rectal delivery system of diclofenac sodium."( Effect of sodium chloride on the release, absorption and safety of diclofenac sodium delivered by poloxamer gel.
Choi, HG; Kim, CK; Kim, HM; Oh, YK; Park, YJ; Rhee, JD; Yong, CS, 2003
)
0.76
" In order to evaluate sublethal toxic effects of diclofenac in fish, rainbow trout (Oncorhynchus mykiss) exposed to diclofenac concentrations ranging from 1 microg/L to 500 microg/L over a 28 day period were investigated by histopathological methods."( Toxic effects of the non-steroidal anti-inflammatory drug diclofenac. Part I: histopathological alterations and bioaccumulation in rainbow trout.
Ferling, H; Mallow, U; Negele, RD; Schwaiger, J; Wintermayr, H, 2004
)
0.82
" No serious adverse events were observed in this study."( Analgesic safety and efficacy of diclofenac sodium softgels on postoperative third molar extraction pain.
Bon, C; Lyon, JA; Peroutka, SJ; Phillips, CL; Shugars, D; Swarbrick, J; Zuniga, JR, 2004
)
0.6
" The softgel provided a very rapid onset of analgesic activity, a prolonged analgesic duration, and an acceptable side-effect profile in the postoperative third molar surgery pain model."( Analgesic safety and efficacy of diclofenac sodium softgels on postoperative third molar extraction pain.
Bon, C; Lyon, JA; Peroutka, SJ; Phillips, CL; Shugars, D; Swarbrick, J; Zuniga, JR, 2004
)
0.6
"Retrospective analysis of adverse event databases."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
"Reports of adverse events submitted to the FDAs Spontaneous Reporting System and the Adverse Event Reporting System from January 1969-December 2000 for these drugs were analyzed according to the number of adverse events reported for each drug per year from the time the drug was approved until December 2000."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
" Various other factors affected spontaneous reporting of adverse events, as peaks in the number of reports were seen numerous times for each drug after the initial 5-year marketing period."( Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration.
Hartnell, NR; Wilson, JP, 2004
)
0.32
" However, user ability to discover the most common side effect to the drug seemed not to be affected."( Awareness and frequency of potential side effects on nonsteroidal anti-inflammatory drugs among the Jordanian patient population.
Abdel-Hafiz, SM; Al-Safi, SA; Albsoul-Younes, AM; Jabateh, SK, 2004
)
0.32
" Clinical efficacy variables (visual analog scale, Lesquesne index and global satisfaction score) and adverse events were monitored at baseline and 2nd and 4th weeks of treatment."( A four-week, randomized, double-blind trial of the efficacy and safety of SKI306X: a herbal anti-arthritic agent versus diclofenac in osteoarthritis of the knee.
Ahn, JH; Chang, DY; Cho, YB; Han, CK; Jung, KO; Jung, YK; Kim, DH; Kim, JM; Kwak, WJ; Lee, CS; Lee, MC; Lung, YB; Park, BJ; Park, YS; Roh, KJ; Seo, JG; Seong, SC; Shin, YU, 2004
)
0.53
" Reported treatment-emergent adverse effects were infrequent, generally mild and none were considered to be related to the trial medication."( The efficacy and safety of low-dose diclofenac sodium 0.1% gel for the symptomatic relief of pain and erythema associated with superficial natural sunburn.
Alekxandrova, I; Amal, S; Césarini, JP; Khemis, A; Kienzler, JL; Magnette, J; Savaluny, E; Trabelsi, M,
)
0.41
" Efficacy assessments included overall joint pain intensity and Western Ontario and McMaster Universities Osteoarthritis Index subscales; tolerability was evaluated by adverse event and physician reporting."( Efficacy and safety of four doses of lumiracoxib versus diclofenac in patients with knee or hip primary osteoarthritis: a phase II, four-week, multicenter, randomized, double-blind, placebo-controlled trial.
Beier, J; Geusens, P; Gitton, X; Hasler, P; Moore, A; Patel, SK; Poór, G; Schnitzer, TJ; Senftleber, I; Sloan, VS, 2004
)
0.57
" Frequencies of adverse events were also recorded."( Gastroduodenal safety and tolerability of lumiracoxib compared with Ibuprofen and celecoxib in patients with osteoarthritis.
Cousin, M; Fiedorowicz-Fabrycy, IF; Gitton, X; Hawkey, CC; Hoexter, G; Nasonov, EL; Pikhlak, EG; Svoboda, P, 2004
)
0.32
" A greater number of patients in the ibuprofen group discontinued treatment due to an adverse event compared with both lumiracoxib groups and the celecoxib group."( Gastroduodenal safety and tolerability of lumiracoxib compared with Ibuprofen and celecoxib in patients with osteoarthritis.
Cousin, M; Fiedorowicz-Fabrycy, IF; Gitton, X; Hawkey, CC; Hoexter, G; Nasonov, EL; Pikhlak, EG; Svoboda, P, 2004
)
0.32
"5% of participants reported adverse events and 6 participants (1."( Safety and usage pattern of low-dose diclofenac when used as an over-the-counter medication: results of an observational cohort study in a community-based pharmacy setting.
Hasford, J; Hoye, K; Moore, N, 2004
)
0.6
"Overall, this study showed that low-dose diclofenac-K is efficacious, safe and commonly used in accordance with the directions for use when used as an OTC medication."( Safety and usage pattern of low-dose diclofenac when used as an over-the-counter medication: results of an observational cohort study in a community-based pharmacy setting.
Hasford, J; Hoye, K; Moore, N, 2004
)
0.86
" A topical NSAID formulation may provide symptom relief with fewer adverse effects."( Efficacy and safety of a topical diclofenac solution (pennsaid) in the treatment of primary osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled clinical trial.
Roth, SH; Shainhouse, JZ, 2004
)
0.6
" We assessed safety by evaluation of adverse events, vital signs, and irritation at the application site."( Efficacy and safety of a topical diclofenac solution (pennsaid) in the treatment of primary osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled clinical trial.
Roth, SH; Shainhouse, JZ, 2004
)
0.6
" There was no significant difference between groups in NSAID-related gastrointestinal tract complaints or in dropouts due to study-related adverse effects."( Efficacy and safety of a topical diclofenac solution (pennsaid) in the treatment of primary osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled clinical trial.
Roth, SH; Shainhouse, JZ, 2004
)
0.6
"Topical diclofenac is effective in the treatment of the symptoms of primary OA of the knee, with only minor local irritation and no significant systemic adverse events."( Efficacy and safety of a topical diclofenac solution (pennsaid) in the treatment of primary osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled clinical trial.
Roth, SH; Shainhouse, JZ, 2004
)
1.04
" Now, rare adverse reactions to several commonly prescribed medications contribute to the total burden of drug-induced liver injury."( Diclofenac-induced liver injury: a paradigm of idiosyncratic drug toxicity.
Aithal, GP, 2004
)
1.77
" Prespecified gastrointestinal adverse events were more frequent with naproxen than with either lumiracoxib dose or placebo."( Efficacy, safety and tolerability of lumiracoxib in patients with rheumatoid arthritis.
Alten, R; Geusens, P; Kralidis, G; Krammer, G; Richardson, P; Rovensky, J; Sloan, VS, 2004
)
0.32
" Results support the good safety profile of both formulations when dosed three times daily for 4 weeks in absence of concomitant use of drugs potentially toxic for cornea."( Comparison of the efficacy and safety of two formulations of diclofenac sodium 0.1% eyedrops in controlling postoperative inflammation after cataract surgery.
Arnoux, YV; Bodaghi, B; Colin, J; Jaulerry, SD; Le Hoang, P; Weber, ME,
)
0.37
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Measurements also included physical examination and adverse events."( The efficacy and safety of aceclofenac versus placebo and naproxen in women with primary dysmenorrhoea.
Fortea, J; Lamarca, R; Letzel, H; Mégard, Y; Raber, A, 2006
)
0.33
" An NSAID with high efficacy, high GI tolerability and devoid of adverse cardiovascular effects is therefore a profile preferred by physicians."( Efficacy and safety of aceclofenac in the treatment of osteoarthritis: a randomized double-blind comparative clinical trial versus diclofenac - an Indian experience.
Chandanwale, AS; Jain, UK; Kapoor, S; Oak, J; Pareek, A, 2006
)
0.54
" Tolerability assessment was based on adverse events."( Efficacy and safety of aceclofenac in the treatment of osteoarthritis: a randomized double-blind comparative clinical trial versus diclofenac - an Indian experience.
Chandanwale, AS; Jain, UK; Kapoor, S; Oak, J; Pareek, A, 2006
)
0.54
" Adverse events were documented when reported by the patients themselves, and when study personnel asked about specific events."( Comparison of the analgesic efficacy and safety of nepafenac ophthalmic suspension compared with diclofenac ophthalmic solution for ocular pain and photophobia after excimer laser surgery: a phase II, randomized, double-masked trial.
Colin, J; Paquette, B, 2006
)
0.55
" Adverse events were infrequent, and no serious adverse events occurred."( Comparison of the analgesic efficacy and safety of nepafenac ophthalmic suspension compared with diclofenac ophthalmic solution for ocular pain and photophobia after excimer laser surgery: a phase II, randomized, double-masked trial.
Colin, J; Paquette, B, 2006
)
0.55
" The incidences of related adverse events were 35."( Evaluation of efficacy and safety of diacerein in knee osteoarthritis in Chinese patients.
Huang, F; Li, J; Li, ZG; Liang, DF; Ma, L; Su, Y; Tang, FL; Wu, DH; Xu, H; Zhang, FC; Zhang, JL; Zheng, WJ; Zhou, HQ; Zhou, YX, 2006
)
0.33
" It is generally well tolerated and has no severe adverse effect."( Evaluation of efficacy and safety of diacerein in knee osteoarthritis in Chinese patients.
Huang, F; Li, J; Li, ZG; Liang, DF; Ma, L; Su, Y; Tang, FL; Wu, DH; Xu, H; Zhang, FC; Zhang, JL; Zheng, WJ; Zhou, HQ; Zhou, YX, 2006
)
0.33
"Idiosyncratic adverse drug reactions (IADRs) represent an important human health problem, yet animal models for preclinical prediction of these reactions are lacking."( Modest inflammation enhances diclofenac hepatotoxicity in rats: role of neutrophils and bacterial translocation.
Blomme, EA; Deng, X; Ganey, PE; Liguori, MJ; Luyendyk, JP; Maddox, JF; Roth, RA; Stachlewitz, RF; Waring, JF, 2006
)
0.63
" Phototransformation of diclofenac was reported from laboratory assays as well as in natural water systems, raising the question of possible adverse effects of the phototransformation products of diclofenac to aquatic organisms."( Phytotoxicity assessment of diclofenac and its phototransformation products.
Adler, N; Altenburger, R; Bartels, P; Schmitt-Jansen, M, 2007
)
0.94
" The primary endpoint was the cumulative rate of discontinuations due to clinical and laboratory GI adverse experiences (AE)."( Gastrointestinal side effects of etoricoxib in patients with osteoarthritis: results of the Etoricoxib versus Diclofenac Sodium Gastrointestinal Tolerability and Effectiveness (EDGE) trial.
Baraf, HS; Bird, S; Brzezicki, J; Curtis, SP; Fuentealba, C; Greenwald, M; Kaur, A; O'Brien, K; Polis, A; Soffer, B, 2007
)
0.55
" The incidence of adverse events in patients taking single or multiple doses of diclofenac potassium is similar to that of ibuprofen and placebo."( Diclofenac potassium 12.5mg tablets for mild to moderate pain and fever: a review of its pharmacology, clinical efficacy and safety.
Moore, N, 2007
)
2.01
"In a number of adverse drug reactions leading to hepatotoxicity drug metabolism is thought to be involved by generation of reactive metabolites from nontoxic drugs."( Development of an in vitro assay for the investigation of metabolism-induced drug hepatotoxicity.
Badolo, L; Dalgaard, L; Dubois, J; Hansen, SH; Otto, M, 2008
)
0.35
"Cyclo-oxygenase (COX)-2 selective inhibitors (coxibs) were designed to reduce the incidence of gastrointestinal (GI) adverse events (AEs) which occur with non-selective NSAIDs (ns-NSAIDs)."( Global gastrointestinal safety profile of etoricoxib and lumiracoxib.
Hunt, RH; Yuan, Y, 2007
)
0.34
" The adverse event (AE) incidence was similar for HPbetaCD diclofenac sodium and PG-BA diclofenac sodium, except that in the current trial and in integrated safety results from the present and prior studies, phlebitis was more common with PG-BA diclofenac sodium."( Dyloject, a novel injectable diclofenac formulation, offers greater safety and efficacy than voltarol for postoperative dental pain.
Carr, DB; Ernst, CC; Gawarecki, DG; Hamilton, DA; Harrison, S; Leeson, RM; Mermelstein, FH; Moshman, M,
)
0.67
" Pooled data on thrombophlebitis from the present investigation and our prior studies of the novel formulation indicate this adverse effect is less frequent and less severe with HPbetaCD diclofenac sodium than with PG-BA diclofenac sodium."( Dyloject, a novel injectable diclofenac formulation, offers greater safety and efficacy than voltarol for postoperative dental pain.
Carr, DB; Ernst, CC; Gawarecki, DG; Hamilton, DA; Harrison, S; Leeson, RM; Mermelstein, FH; Moshman, M,
)
0.61
"To see the toxic effects of NSAID on kidney tissue of albino rats."( Adverse effects of diclofenac sodium on renal parenchyma of adult albino rats.
Perveen, S; Qureshi, GS; Yasmeen, T, 2007
)
0.67
"Tubeless PCNL is safe and effective even after supracostal access and is associated with less postoperative pain and a shorter hospital stay."( Tubeless percutaneous nephrolithotomy: safe even in supracostal access.
Demirci, D; Erşekerci, E; Huri, E; Karacagil, M; Sofikerim, M, 2007
)
0.34
" We demonstrate that both DF and meloxicam are toxic to renal tubular epithelial (RTE) cells following 12 h of exposure, due to an increase in production of reactive oxygen species (ROS), which could be temporarily ameliorated by pre-incubation with uric acid (UA)."( Diclofenac toxicity in Gyps vulture is associated with decreased uric acid excretion and not renal portal vasoconstriction.
Naidoo, V; Swan, GE, 2009
)
1.8
" Rofecoxib was withdrawn worldwide due to an associated increased risk of CV events and lumiracoxib has been withdrawn from Australia, Canada, Europe and a few other countries following reports of suspected adverse liver reactions."( A 6-week, multicentre, randomised, double-blind, double-dummy, active-controlled, clinical safety study of lumiracoxib and rofecoxib in osteoarthritis patients.
Krammer, G; Stricker, K; Yu, S, 2008
)
0.35
" The primary safety measures were the incidence of predefined GI adverse events (AEs) and peripheral oedema."( A 6-week, multicentre, randomised, double-blind, double-dummy, active-controlled, clinical safety study of lumiracoxib and rofecoxib in osteoarthritis patients.
Krammer, G; Stricker, K; Yu, S, 2008
)
0.35
" General safety and tolerability were evaluated by adverse event (AE) reporting and physical examinations and laboratory tests at each visit."( Long-term efficacy and safety of lumiracoxib 100 mg: an open-label extension of a 13-week randomized controlled trial in patients with primary osteoarthritis of the knee.
Beaulieu, A; Paster, Z; Rebuli, R; Sheldon, EA; Yu, S,
)
0.13
" Another pharmaceutical that is regularly associated with adverse effects on the liver, sometimes leading to acute liver failure, is the widely used non-steroidal anti-inflammatory drug (NSAID) diclofenac."( Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes.
Kling, M; Lauer, B; Mueller, SO; Tuschl, G, 2009
)
0.83
" subcapitata varied during the oxidation, probably due to the formation of some intermediate products more toxic than DCF."( Degradation of diclofenac by TiO(2) photocatalysis: UV absorbance kinetics and process evaluation through a set of toxicity bioassays.
Belgiorno, V; Guida, M; Kassinos, D; Meric, S; Rizzo, L; Russo, F, 2009
)
0.71
"To compare the adverse event (AE)-related discontinuation rate with celecoxib vs."( A randomized, multicentre, double-blind, parallel-group study to assess the adverse event-related discontinuation rate with celecoxib and diclofenac in elderly patients with osteoarthritis.
Dahlberg, LE; Holme, I; Høye, K; Ringertz, B,
)
0.33
" The commonest adverse event associated with TDiclo was dry skin (18."( Efficacy and safety of topical diclofenac containing dimethyl sulfoxide (DMSO) compared with those of topical placebo, DMSO vehicle and oral diclofenac for knee osteoarthritis.
Bookman, AAM; Grierson, LM; Naseer, Z; Shainhouse, ZJ; Simon, LS, 2009
)
0.64
" Incidence and severity of adverse events were comparable for the three treatments; overall tolerability was rated as very good/good by 93% of the patients."( Efficacy and safety of lornoxicam compared with placebo and diclofenac in acute sciatica/lumbo-sciatica: an analysis from a randomised, double-blind, multicentre, parallel-group study.
Geertsen, MS; Herrmann, WA, 2009
)
0.6
") occurring after the start of rabeprazole treatment were handled as adverse events."( Efficacy and safety of rabeprazole in non-steroidal anti-inflammatory drug-induced ulcer in Japan.
Mizokami, Y, 2009
)
0.35
" A control group was treated by mineral water (0+0) mg/kg and a second group was treated with only a toxic dose of 100 mg/kg of PARA (100+0)."( [Protective effect of diclofenac towards the oxidative stress induced by paracetamol toxicity in rats].
Aouacheri, W; Djafer, R; Lefranc, G; Saka, S,
)
0.45
" Moreover, erythrocyte sedimentation rate (ESR), blood C-reactive protein (CRP), blood and urinary routine tests, liver and kidney function examination, and the adverse reaction that occurred during the treatment period were observed."( Clinical efficacy and safety of Gubitong Recipe () in treating osteoarthritis of knee joint.
Jin, DE; Tao, QW; Xu, Y; Yan, XP, 2009
)
0.35
" No evident adverse reaction occurred during the treatment period."( Clinical efficacy and safety of Gubitong Recipe () in treating osteoarthritis of knee joint.
Jin, DE; Tao, QW; Xu, Y; Yan, XP, 2009
)
0.35
"GBT is an effective and safe recipe for the treatment of osteoarthritis of knee joint, which could alleviate the joint pain, stiffness, and dysfunction."( Clinical efficacy and safety of Gubitong Recipe () in treating osteoarthritis of knee joint.
Jin, DE; Tao, QW; Xu, Y; Yan, XP, 2009
)
0.35
" Safety assessment included adverse events, skin irritation scores of the treated knee(s), ocular examinations, and routine laboratory tests."( A long-term, open-label study to confirm the safety of topical diclofenac solution containing dimethyl sulfoxide in the treatment of the osteoarthritic knee.
Grierson, LM; Naseer, Z; Shainhouse, JZ,
)
0.37
" Patients were assessed for safety variables that included adverse events, local skin reactions, laboratory results, dosage of immunosuppressive medication and indication of graft rejection."( Results of a randomized, placebo-controlled safety and efficacy study of topical diclofenac 3% gel in organ transplant patients with multiple actinic keratoses.
Johannsen, A; Röwert-Huber, J; Sterry, W; Stockfleth, E; Ulrich, C; Ulrich, M,
)
0.36
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
"NSAIDs used for the treatment of osteoarthritis (OA) have dose-related risks for gastrointestinal, cardiovascular and renal adverse events (AEs), particularly in elderly patients."( Safety and efficacy of topical diclofenac sodium gel for knee osteoarthritis in elderly and younger patients: pooled data from three randomized, double-blind, parallel-group, placebo-controlled, multicentre trials.
Altman, RD; Baraf, HS; Barthel, HR; Gloth, FM; Gold, MS, 2011
)
0.66
"To evaluate the risk of adverse events (AEs) associated with topical diclofenac for the treatment of acute and chronic musculoskeletal conditions."( Safety profile of topical diclofenac: a meta-analysis of blinded, randomized, controlled trials in musculoskeletal conditions.
Fotopoulos, G; Maibach, H; Taylor, RS, 2011
)
0.9
"Nephrotic syndrome, with or without concomitant tubulointerstitial nephritis, is a rare renal adverse effect of NSAIDs."( Safe administration of celecoxib to a patient with repeated episodes of nephrotic syndrome induced by NSAIDs.
Knotek, M; Ljubanovic, D; Mihovilovic, K, 2011
)
0.37
" Both the study medications were well tolerated with no incidence of serious adverse event (SAE)."( Efficacy and safety of aceclofenac-cr and aceclofenac in the treatment of knee osteoarthritis: a 6-week, comparative, randomized, multicentric, double-blind study.
Chandurkar, N; Dalal, B; Gupta, A; Jesalpura, B; Mehrotra, A; Mukherjee, A; Pareek, A; Sirsikar, A, 2011
)
0.37
" Aceclofenac-CR was found to be similar in terms of efficacy as conventional aceclofenac in knee OA patients with fewer adverse events."( Efficacy and safety of aceclofenac-cr and aceclofenac in the treatment of knee osteoarthritis: a 6-week, comparative, randomized, multicentric, double-blind study.
Chandurkar, N; Dalal, B; Gupta, A; Jesalpura, B; Mehrotra, A; Mukherjee, A; Pareek, A; Sirsikar, A, 2011
)
0.37
"Already considered a drug that can reverse the toxic side effects of NSAIDs, BPC 157 (10 μg/kg, 10 ng/kg) was strongly effective throughout the entire experiment when given (i) intraperitoneally immediately after diclofenac or (ii) per-orally in drinking water (0."( Pentadecapeptide BPC 157 and its effects on a NSAID toxicity model: diclofenac-induced gastrointestinal, liver, and encephalopathy lesions.
Blagaic, AB; Brcic, L; Coric, M; Djakovic, Z; Djuzel, V; Drmic, D; Dzidic, S; Filipovic, M; Franjic, S; Gjurasin, M; Ilic, S; Klicek, R; Kolenc, D; Radic, B; Romic, Z; Seiwerth, S; Sever, M; Sikiric, P; Stambolija, V; Stupnisek, M; Zarkovic, K; Zoricic, I, 2011
)
0.79
" Fifteen patients experienced a total of 19 adverse events (AEs), 17 of which were mild to moderate, and 2 of which were severe."( Effectiveness and safety of diclofenac epolamine topical patch 1.3% for the treatment of acute pain due to back strain: an open-label, uncontrolled study.
Gimbel, J; Jacobs, D; Paterson, C; Pixton, G, 2011
)
0.66
" Overall, DCF was the most cytotoxic drug for zebra mussel cells, followed by GEM, CBZ, while ATL has not a noteworthy toxic potential."( Cytotoxicity assessment of four pharmaceutical compounds on the zebra mussel (Dreissena polymorpha) haemocytes, gill and digestive gland primary cell cultures.
Binelli, A; Parolini, M; Provini, A; Quinn, B, 2011
)
0.37
" We estimated 95% confidence interval, Q and 12 criteria, Mantel-Haenszel and DerSimonian-Laird statistics and relative risk of adverse reactions."( [Diclofenac sodium in osteoarthritis. Is there risk of hepatotoxicity? A systematic review].
Koniaeva, EI; Matveev, AV, 2010
)
1.27
" Both the study medications were well tolerated with no incidence of serious adverse events."( Zaltoprofen, a noninferior alternative to diclofenac for the treatment of primary knee osteoarthritis -- a comparative evaluation of efficacy and safety in a 4-week, multicentric, randomized, double-blind, double-dummy trial.
Ambade, RE; Chandurkar, NB; Gupta, AK; Jesalpura, BH; Pareek, A; Sirsikar, AD; Swamy, AP, 2011
)
0.63
" Safety was evaluated through adverse event (AE) reporting, physical examination, and laboratory investigations."( An open-label, long-term safety and tolerability trial of diclofenac sodium 1% gel in patients with knee osteoarthritis.
Alwine, LK; Gold, MS; Peniston, JH, 2011
)
0.61
" However, serious gastrointestinal and cardiovascular systemic adverse events (AEs) are associated with oral NSAIDs and can be treatment limiting."( Diclofenac sodium topical solution 1.5% w/w with dimethyl sulfoxide compared with placebo for the treatment of osteoarthritis: pooled safety results.
Fuller, P; Roth, SH, 2011
)
1.81
" However, this group of drugs is associated with serious adverse drug reactions."( Differential involvement of mitochondrial dysfunction, cytochrome P450 activity, and active transport in the toxicity of structurally related NSAIDs.
Unlü, B; van Leeuwen, JS; Vermeulen, NP; Vos, JC, 2012
)
0.38
" The need for rescue medication and the presence of adverse effects were considered as secondary outcome of the study."( Intramuscular drotaverine and diclofenac in acute renal colic: a comparative study of analgesic efficacy and safety.
Akantappa Bandakkanavar, TK; Arora, P; Dash, A; Maiti, R, 2012
)
0.67
" This work provides an insight into non-covalent interactions between emerging contaminants and biomolecule, and is helpful for clarifying the toxic mechanism of such emerging contaminants."( Interactions of acidic pharmaceuticals with human serum albumin: insights into the molecular toxicity of emerging pollutants.
Chen, J; Gao, H; Qian, Y; Zhang, Y; Zhou, X, 2012
)
0.38
" The WOMAC scale was applied at 4 weeks and adverse events were recorded."( Safety and efficacy of methylprednisolone infiltration in anserine syndrome treatment.
Esquivel-Valerio, JA; Galarza-Delgado, DÁ; Garza-Elizondo, MA; Negrete-López, R; Vega-Morales, D,
)
0.13
" The incidence of adverse events did not show any differences either."( Safety and efficacy of methylprednisolone infiltration in anserine syndrome treatment.
Esquivel-Valerio, JA; Galarza-Delgado, DÁ; Garza-Elizondo, MA; Negrete-López, R; Vega-Morales, D,
)
0.13
" However, treatment with NSAIDs may be accompanied by adverse effects such as gastrointestinal damage and platelet dysfunction."( Toxicity of non-steroidal anti-inflammatory drugs: a review of melatonin and diclofenac sodium association.
Altunkaynak, ME; Aygün, D; Kaplan, S; Odaci, E; Onger, ME, 2012
)
0.61
" More importantly, curcumin treatment was found to be safe and did not relate with any adverse events."( A randomized, pilot study to assess the efficacy and safety of curcumin in patients with active rheumatoid arthritis.
Chandran, B; Goel, A, 2012
)
0.38
"The most common adverse events involved the skin or subcutaneous tissue, primarily at the application site."( Pooled safety analysis of diclofenac sodium topical solution 1.5% (w/w) in the treatment of osteoarthritis in patients aged 75 years or older.
Fuller, P; Roth, SH, 2012
)
0.68
" Incidence of moderate-to-severe abdominal symptoms and discontinuation of treatment due to GI adverse events (AEs) were lower in the celecoxib group."( Efficacy and safety of celecoxib versus diclofenac and omeprazole in elderly arthritis patients: a subgroup analysis of the CONDOR trial.
Essex, MN; Kellner, HL; Li, C, 2012
)
0.65
" Safety concerns associated with nonsteroidal anti-inflammatory drugs (NSAIDs) have prompted the development of new formulations that minimize adverse events (AEs) and maintain efficacy."( A phase 2 study evaluating the efficacy and safety of a novel, proprietary, nano-formulated, lower dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012
)
0.59
" This leads us to a conclusion that DCF has, with high probability, no adverse effect on both fish species up to 320 µg/L."( Diclofenac: New data on chronic toxicity and bioconcentration in fish.
Burri, R; Hartmann, A; Memmert, U; Peither, A; Schmidt, T; Sumpter, JP; Weber, K, 2013
)
1.83
" The incidence of treatment-related adverse events was similar across groups."( Analgesic efficacy and safety of a novel injectable formulation of diclofenac compared with intravenous ketorolac and placebo after orthopedic surgery: a multicenter, randomized, double-blinded, multiple-dose trial.
Carr, DB; Daniels, S; Hamilton, DA; Lang, E; Melson, T, 2013
)
0.63
"HPβCD diclofenac is safe and efficacious for acute moderate and severe pain after orthopedic surgery and significantly spares morphine use."( Analgesic efficacy and safety of a novel injectable formulation of diclofenac compared with intravenous ketorolac and placebo after orthopedic surgery: a multicenter, randomized, double-blinded, multiple-dose trial.
Carr, DB; Daniels, S; Hamilton, DA; Lang, E; Melson, T, 2013
)
1.11
" Tizanidine-induced adverse effects were examined in 100 patients treated with coadministration of tizanidine and 8 CYP1A2 inhibitors."( [Clinical survey of tizanidine-induced adverse effects--impact of concomitant drugs providing cytochrome P450 1A2 modification--].
Homma, M; Kohda, Y; Matsumoto, S; Momo, K; Sasaki, T, 2013
)
0.39
" Their adverse effects on the upper gastrointestinal (GI) tract are well documented and well known among clinicians and often mitigated against by coprescribing proton pump inhibitors."( Lower gastrointestinal adverse effects of NSAIDS: an extreme example of a common problem.
Conway, C; Elton, C; Mandegaran, R, 2013
)
0.39
"To study the adverse effects of Celecoxib and compare them with those of other non-steroidal anti-inflammatory drugs (NSAIDs) in an Asian Indian cohort."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013
)
0.39
" All the recorded adverse events were noted and compared between the Celecoxib and non-selective NSAID users."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013
)
0.39
" Multiple NSAID users had higher adverse events (6."( How safe is Celecoxib for Asian-Indian patients with rheumatic diseases?
Chandra, C; Chandy, SJ; Danda, D; Iliyas, MM; Mathew, AJ, 2013
)
0.39
"Non-steroidal anti-inflammatory drugs (NSAIDs) are an effective and common treatment for chronic pain disorders, but long-term use is associated with risk of potentially life-threatening gastrointestinal adverse events (AEs)."( Safety and efficacy of long-term esomeprazole 20 mg in Japanese patients with a history of peptic ulcer receiving daily non-steroidal anti-inflammatory drugs.
Kinoshita, Y; Miwa, H; Sugano, K; Takeuchi, T, 2013
)
0.39
"Decisions to use or avoid nonsteroidal anti-inflammatory drugs (NSAIDs) for postsurgical pain are often influenced by concerns about bleeding and renal adverse effects."( Safety of a novel parenteral formulation of diclofenac after major orthopedic or abdominal/pelvic surgery in a population including anticoagulated, elderly or renally insufficient patients: an open-label, multiday, repeated dose clinical trial.
Carr, DB; Chelly, JE; Lacouture, PG; Melson, TI; Paadre, S; Singla, SK, 2013
)
0.65
" Adverse events (AEs) were recorded throughout the study."( Safety of a novel parenteral formulation of diclofenac after major orthopedic or abdominal/pelvic surgery in a population including anticoagulated, elderly or renally insufficient patients: an open-label, multiday, repeated dose clinical trial.
Carr, DB; Chelly, JE; Lacouture, PG; Melson, TI; Paadre, S; Singla, SK, 2013
)
0.65
" The GI tolerability was evaluated based on the incidence and severity of predefined GI adverse events (AEs), number of gastroprotective agents (GPAs) consumed by patients, and discontinuation from the study due to GI AEs."( Comparison of gastrointestinal safety and tolerability of aceclofenac with diclofenac: a multicenter, randomized, double-blind study in patients with knee osteoarthritis.
Chandurkar, N; Pareek, A, 2013
)
0.62
" The incidence of adverse events of abnormal peripheral sensation was lower than in previous tanezumab trials."( Efficacy and safety of tanezumab added on to diclofenac sustained release in patients with knee or hip osteoarthritis: a double-blind, placebo-controlled, parallel-group, multicentre phase III randomised clinical trial.
Balanescu, AR; Brown, MT; Davignon, I; Feist, E; Smith, MD; West, CR; Wolfram, G, 2014
)
0.66
" Although no new safety signals were observed, the higher incidence of adverse events in the tanezumab+diclofenac group suggests that combination therapy is unfavourable."( Efficacy and safety of tanezumab added on to diclofenac sustained release in patients with knee or hip osteoarthritis: a double-blind, placebo-controlled, parallel-group, multicentre phase III randomised clinical trial.
Balanescu, AR; Brown, MT; Davignon, I; Feist, E; Smith, MD; West, CR; Wolfram, G, 2014
)
0.88
" Diclofenac spray was well tolerated, with a low overall rate of adverse events."( A randomized, double-blind, placebo-controlled multicentre study to evaluate the efficacy and safety of diclofenac 4% spray gel in the treatment of acute uncomplicated ankle sprain.
Giannetti, B; Menke, G; Novellini, R; Predel, HG; Seigfried, B, 2013
)
1.51
" Adverse events (AEs) were recorded throughout the study."( Efficacy and safety of diclofenac diethylamine 1.16% gel in acute neck pain: a randomized, double-blind, placebo-controlled study.
Burnett, I; Giannetti, B; Hug, AM; Pabst, H; Predel, HG; Schaefer, A, 2013
)
0.7
"Use of nonsteroidal anti-inflammatory drugs (NSAIDs) is primarily limited by renal and gastrointestinal adverse effects."( Effects of rebamipide on nephrotoxicity associated with selected NSAIDs in rats.
Bullins, KW; Denham, JW; Hanley, AV; Hanley, GA; Harirforoosh, S; Panus, PC; Wood, RC; Wyatt, JE, 2013
)
0.39
" The formation of more toxic mid-byproducts during the ClO2 disinfection process poses a potential risk to consumers."( Oxidation of diclofenac by aqueous chlorine dioxide: identification of major disinfection byproducts and toxicity evaluation.
Liu, G; Liu, H; Wang, Y; Xie, Y, 2014
)
0.77
"Tricyclic antidepressants, not influencing the P450 3A4 activity, are safe in combination with drugs of other groups used in the treatment of comorbid patients."( [Preclinical investigation of pharmaceuticals impact against cytochrome P450 activity and prognosis of substrate affinity as means for providing substrate therapy safety].
Baĭchorov, IKh; Fomin, EV; Shikh, EV; Sizova, ZhM, 2013
)
0.39
" We investigated the membrane transport of diclofenac and its toxic effects on gene expression and the development of zebrafish embryos."( Developmental toxicity of diclofenac and elucidation of gene regulation in zebrafish (Danio rerio).
Chen, JB; Gao, HP; Gao, HW; Li, CQ; Zhang, Y; Zhang, YL; Zhou, XF, 2014
)
0.97
" Results of HET-CAM and ICE tests suggest that sulphacetamide is moderately toxic in the presence of light/UV-A and very slightly irritant without irradiation."( Photochemical toxicity of drugs intended for ocular use.
Kaithwas, G; Kishor, K; Sahu, RK; Saraf, SA; Singh, B, 2014
)
0.4
" Here, we analyzed the developmental toxic effects of diclofenac using Xenopus embryos according to the Frog Embryo Teratogenesis Assay-Xenopus (FETAX) protocol."( Evaluation of developmental toxicity and teratogenicity of diclofenac using Xenopus embryos.
Chae, JP; Hwang, YS; Kim, SH; Lee, HS; Min, BH; Park, MJ; Park, MS, 2015
)
0.91
" Firstly, PCIS were incubated with 0-200 μM diclofenac (DCF), one of the most intensively studied NSAIDs, to investigate whether they could correctly reflect the toxic mechanisms."( Precision cut intestinal slices are an appropriate ex vivo model to study NSAID-induced intestinal toxicity in rats.
de Graaf, IA; Groothuis, GM; Niu, X; van der Bij, HA, 2014
)
0.66
"NSAIDs, such as diclofenac, are the most commonly used medications to treat osteoarthritis (OA), but they are associated with dose-related adverse events (AEs)."( Efficacy and safety of low-dose submicron diclofenac for the treatment of osteoarthritis pain: a 12 week, phase 3 study.
Gibofsky, A; Hochberg, MC; Jaros, MJ; Young, CL, 2014
)
1.01
" When the possibility of poor compliance and the potential adverse effects of misoprostol are considered, rebamipide appears to be a clinically effective and safe alternative."( Preventive efficacy and safety of rebamipide in nonsteroidal anti-inflammatory drug-induced mucosal toxicity.
Cho, CS; Kang, YM; Kim, JH; Kim, SK; Lee, DH; Lee, SK; Lee, ST; Lee, YC; Park, SH; Park, W; Park, YW; Rew, JS; Yoo, WH, 2014
)
0.4
" These toxicity tests suggest that the formation of enhanced toxic intermediates during the Fe(VI) disinfection process may pose potential health risk to consumers."( Oxidation of diclofenac by potassium ferrate (VI): reaction kinetics and toxicity evaluation.
Gao, S; Liu, G; Liu, H; Wang, Y; Xie, Y, 2015
)
0.79
" Results suggest that the photolysis by-products of diclofenac were more toxic than those from the other compounds tested, showing an increase in GST and CAT levels, which are also supported by higher MDA levels."( Ecotoxicity of ketoprofen, diclofenac, atenolol and their photolysis byproducts in zebrafish (Danio rerio).
Carvalho, G; Diniz, MS; Noronha, JP; Oehmen, A; Pereira, VJ; Reis, MA; Salgado, R, 2015
)
0.96
" Simvastatin was the most toxic tested compound for zebrafish embryo, followed by diclofenac."( Toxicity screening of diclofenac, propranolol, sertraline and simvastatin using Danio rerio and Paracentrotus lividus embryo bioassays.
Martins, R; Ribeiro, S; Santos, MM; Torres, T, 2015
)
0.96
" We conclude that diclofenac is toxic to non-target soil invertebrates, although its mode of action is different from the mammalian toxicity."( Ecotoxicogenomic assessment of diclofenac toxicity in soil.
Chen, G; den Braver, MW; Roelofs, D; van Gestel, CA; van Straalen, NM, 2015
)
1.04
" One of the main DCF metabolites is a reactive diclofenac acyl glucuronide (DCF-AG) that covalently binds to biologic targets and may contribute to adverse drug reactions arising from DCF use."( Multidrug Resistance-Associated Protein 3 Plays an Important Role in Protection against Acute Toxicity of Diclofenac.
Csanaky, IL; Goedken, MJ; Manautou, JE; Scialis, RJ, 2015
)
0.89
"Diclofenac is used for the treatment of osteoarthritis (OA); however, like other nonsteroidal anti-inflammatory drugs (NSAIDs) it can be associated with serious dose-related adverse events (AEs)."( Low-dose SoluMatrix diclofenac in the treatment of osteoarthritis: A 1-year, open-label, Phase III safety study.
Altman, RD; Cryer, B; Gibofsky, A; Hochberg, MC; Hopkins, WE; Imasogie, O; Kivitz, A; Markenson, JA; Nezzer, J; Strand, V; Young, CL, 2015
)
2.18
"Similar to other NSAIDs, diclofenac is associated with serious dose-related cardiovascular, gastrointestinal, and renal adverse events."( Low-dose SoluMatrix diclofenac : a review of safety across two Phase III studies in patients with acute and osteoarthritis pain.
Altman, R; Daniels, S; Gibofsky, A; Imasogie, O; Young, C, 2015
)
1.04
" Few serious gastrointestinal, cardiovascular, renal, or hepatic adverse events commonly associated with NSAID use were reported in these studies."( Low-dose SoluMatrix diclofenac : a review of safety across two Phase III studies in patients with acute and osteoarthritis pain.
Altman, R; Daniels, S; Gibofsky, A; Imasogie, O; Young, C, 2015
)
0.74
"5-mg group reported adverse events that were considered by the investigator to be related to the study drug."( Safety and pharmacokinetics of single and multiple intravenous bolus doses of diclofenac sodium compared with oral diclofenac potassium 50 mg: A randomized, parallel-group, single-center study in healthy subjects.
Allenby, K; Gautam, A; McDowell, J; Munjal, S; Okumu, F, 2016
)
0.66
" All adverse events were recorded for safety assessment."( Efficacy and safety of etoricoxib compared with NSAIDs in acute gout: a systematic review and a meta-analysis.
Liu, P; Ma, JL; Wang, J; Zhang, S; Zhang, W; Zhang, Y, 2016
)
0.43
" Treatment-emergent adverse events (TEAEs), skin irritation, and vital signs were assessed and collected throughout the study."( Efficacy and safety of diclofenac sodium 2% topical solution for osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled, 4 week study.
Holt, RJ; Kent, JD; Wadsworth, LT, 2016
)
0.74
" No serious adverse events were reported."( Efficacy and safety of diclofenac sodium 2% topical solution for osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled, 4 week study.
Holt, RJ; Kent, JD; Wadsworth, LT, 2016
)
0.74
" It has been shown to be a safe and effective for treatment of AK on both skin and mucosal lip."( Topical treatment of actinic keratosis with 3.0% diclofenac in 2.5% hyaluronan gel: review of the literature about the cumulative evidence of its efficacy and safety.
Cozzani, E; Javor, S; Parodi, A, 2016
)
0.69
"We have previously reported that mice lacking the efflux transporter Mrp3 had significant intestinal injury after toxic diclofenac (DCF) challenge, and proposed that diclofenac acyl glucuronide (DCF-AG), as a substrate of Mrp3, played a part in mediating injury."( Elucidation of the Mechanisms through Which the Reactive Metabolite Diclofenac Acyl Glucuronide Can Mediate Toxicity.
Manautou, JE; Scialis, RJ, 2016
)
0.88
" Finally, the new formulation of progesterone was shown to be safe and not inferior to other products already on the market, with the exception of progesterone administered vaginally."( Efficacy and Safety Profile of Diclofenac/Cyclodextrin and Progesterone/Cyclodextrin Formulations: A Review of the Literature Data.
Bonagura, AC; Cenami, R; Cimmaruta, D; Fiorentino, S; Fossati, T; Rossi, F; Scavone, C; Torella, M, 2016
)
0.72
" Acute adverse events in the morphine group occurred in 19 (3%) participants."( Delivering safe and effective analgesia for management of renal colic in the emergency department: a double-blind, multigroup, randomised controlled trial.
Afzal, MS; Al Hilli, SA; Al Rumaihi, K; Anjum, S; Cameron, PA; Mitra, B; Morley, K; Pathan, SA; Shukla, D; Straney, LD; Thomas, SH, 2016
)
0.43
"Interindividual variability in drug metabolism is an important cause of adverse drug reactions and variability in drug efficiency."( How polymorphisms of the cytochrome P450 genes affect ibuprofen and diclofenac metabolism and toxicity.
Bilić, I; Božina, N; Dimovski, A; Domjanović, IK; Krasniqi, V, 2016
)
0.67
" The aim of this study was to evaluate the toxic effects of three typical NSAIDs, diclofenac (DFC), acetaminophen (APAP) and ibuprofen (IBP), toward the water flea Daphnia magna."( Toxicity Thresholds for Diclofenac, Acetaminophen and Ibuprofen in the Water Flea Daphnia magna.
Du, J; Mei, CF; Xu, MY; Ying, GG, 2016
)
0.97
" Any observed adverse effects were also scrutinized."( Efficacy and short-term safety of topical Dwarf Elder (Sambucus ebulus L.) versus diclofenac for knee osteoarthritis: A randomized, double-blind, active-controlled trial.
Emtiazy, M; Hashempur, MH; Jabbari, M; Kamalinejad, M; Razavi, SZ; Shahraki, HR, 2016
)
0.66
" In addition, no serious adverse effect was reported."( Efficacy and short-term safety of topical Dwarf Elder (Sambucus ebulus L.) versus diclofenac for knee osteoarthritis: A randomized, double-blind, active-controlled trial.
Emtiazy, M; Hashempur, MH; Jabbari, M; Kamalinejad, M; Razavi, SZ; Shahraki, HR, 2016
)
0.66
" Data are limited regarding CV risks associated with short-term nonsteroidal anti-inflammatory drug use, including injectable formulations, although it has been suggested that even a single dose may increase CV adverse event (AE) risk."( Cardiovascular safety of hydroxypropyl-β-cyclodextrin-diclofenac in the management of acute postsurgical pain: a pooled analysis of 2 randomized, double-blind, placebo- and active comparator-controlled phase III clinical trials.
Carr, DB; Daniels, SE; Gan, TJ; Lacouture, PG; Min, LH; Reyes, CR; Singla, N, 2016
)
0.68
"Oral ketamine appears to be a safe and effective option in improving depressive symptoms of patients with chronic pain with mild-to-moderate depression."( Efficacy and safety of oral ketamine versus diclofenac to alleviate mild to moderate depression in chronic pain patients: A double-blind, randomized, controlled trial.
Afarideh, M; Agah, E; Akhondzadeh, S; Arbabi, M; Ghajar, A; Jafarinia, M; Noorbala, AA; Saravi, MA; Tafakhori, A, 2016
)
0.7
"Nonsteroidal anti-inflammatory drugs (NSAIDs), which are globally prescribed, exhibit mainly anti-inflammatory and analgesic effects but also can cause adverse effects including gastrointestinal erosions, ulceration, bleeding, and perforation."( (1)H-Nuclear magnetic resonance-based metabolic profiling of nonsteroidal anti-inflammatory drug-induced adverse effects in rats.
Choi, KH; Chung, MW; Lee, HJ; Park, JH; Um, SY, 2016
)
0.43
" At typical detected environmental concentrations, the drug does not exhibit toxic effects towards living organisms, albeit chronic exposure may lead to severe effects."( Diclofenac and its transformation products: Environmental occurrence and toxicity - A review.
Brar, SK; Das, RK; Lonappan, L; Surampalli, RY; Verma, M, 2016
)
1.88
" The benefit-risk profile of mefenamic acid should now be re-evaluated in light of effective and less toxic alternatives."( Central nervous system toxicity of mefenamic acid overdose compared with other NSAIDs: an analysis of cases reported to the United Kingdom National Poisons Information Service.
Cooper, G; Crichton, S; Eddleston, M; Kamour, A; Lupton, DJ; Thomas, SH; Thompson, JP; Vale, JA, 2017
)
0.46
" Concerning duration, while the identification of a safe temporal window is less defined, some studies reported an absence or a very low risk when the exposure is shorter than 30 days."( Safety and efficacy of low doses of diclofenac on acute pain in the emergency setting.
Capaldi, L; Di Leo, M; Franceschi, F; Gabrielli, M; Gilardi, E; Merra, G; Migneco, A; Ojetti, V; Petruzziello, C; Santarelli, L; Saviano, L, 2016
)
0.71
" Renal safety was assessed by examining treatment-emergent adverse events (AEs) and postoperative blood urea nitrogen (BUN) and serum creatinine shifts."( A Pooled Analysis Evaluating Renal Safety in Placebo- and Active Comparator-Controlled Phase III Trials of Multiple-Dose Injectable HPβCD-Diclofenac in Subjects with Acute Postoperative Pain.
Carr, DB; Daniels, SE; Gan, TJ; Hamilton, DA; Johnson, O; Lacouture, PG; Min, LH; Reyes, CR; Singla, N, 2016
)
0.64
" In the present study, we investigated the toxic effects of DCF on the physiological parameters (e."( Toxic effects of diclofenac on life history parameters and the expression of detoxification-related genes in Daphnia magna.
Bao, S; Liu, Y; Nie, X; Pan, B; Wang, C; Wang, L, 2017
)
0.79
" However, toxicity in natural ecosystems is not usually the result of exposure to a single substance but to a mixture of toxic agents, yet only a few studies have evaluated the toxicity of mixtures."( Cyto-genotoxicity and oxidative stress in common carp (Cyprinus carpio) exposed to a mixture of ibuprofen and diclofenac.
Dublán-García, O; Galar-Martínez, M; Islas-Flores, H; Manuel Gómez-Oliván, L; Michelle Sánchez-Ocampo, E; Ortíz-Reynoso, M; SanJuan-Reyes, N, 2017
)
0.67
" Patients with aceclofenac CR showed significant increases in heartburn and indigestion and adverse gastrointestinal effects, compared to aceclofenac."( Efficacy and Safety of Different Aceclofenac Treatments for Chronic Lower Back Pain: Prospective, Randomized, Single Center, Open-Label Clinical Trials.
Jung, WC; Kang, YM; Kim, HS; Kim, JH; Lee, BH; Lee, HM; Moon, SH; Suk, KS; Yang, JH, 2017
)
0.46
" Aceclofenac CR slightly increased gastrointestinal adverse effects, such as heartburn and indigestion."( Efficacy and Safety of Different Aceclofenac Treatments for Chronic Lower Back Pain: Prospective, Randomized, Single Center, Open-Label Clinical Trials.
Jung, WC; Kang, YM; Kim, HS; Kim, JH; Lee, BH; Lee, HM; Moon, SH; Suk, KS; Yang, JH, 2017
)
0.46
" RESULTS No foal developed any adverse effects attributed to diclofenac application, and no significant differences in values of evaluated variables were identified between treatment groups."( Randomized, controlled clinical trial of safety and plasma concentrations of diclofenac in healthy neonatal foals after repeated topical application of 1% diclofenac sodium cream.
Barnett, SE; Hines, MT; Knych, HK; Seino, KK; Sellon, DC, 2017
)
0.93
"Diclofenac (DCF) adverse reactions involve diverse mechanisms in different models."( N-acetylcysteine potentiates diclofenac toxicity in Saccharomyces cerevisiae: stronger potentiation in ABC transporter mutant strains.
Abdel-Razzak, Z; Al-Attrache, H; Chamieh, H; Hamzé, M; Morel, I; Taha, S, 2018
)
2.21
" None of the patients developed any adverse effects when using the transdermal patch, whereas 3 patients reported gastric irritation and a mild burning sensation when taking oral diclofenac."( Analgesic efficacy and safety of transdermal and oral diclofenac in postoperative pain management following dental implant placement.
Arya, K; Gowda, T; Kumar, T; Mehta, DS; Raja Rajeswari, S,
)
0.57
" Nephrotoxicity is a life-threatening side-effect of nonsteroidal anti-inflammatory drugs (NSAIDs)."( Curcumin ameliorates diclofenac sodium-induced nephrotoxicity in male albino rats.
Ahmed, AY; El-Raouf, OMA; Gad, AM, 2017
)
0.77
" No difference in adverse events was observed between the two groups."( Efficacy and safety of adalimumab by intra-articular injection for moderate to severe knee osteoarthritis: An open-label randomized controlled trial.
Wang, J, 2018
)
0.48
" Main outcomes included pain relief measured using visual analogue scale at 2, 4 and 12 weeks and patient global assessment (PGA) at 4 and 12 weeks for efficacy, all-cause withdrawals, and adverse events."( Efficacy and safety of diclofenac in osteoarthritis: Results of a network meta-analysis of unpublished legacy studies.
Andrew Moore, R; Chaves, RL; Guyot, P; Iqbal, A; Nixon, RM; Pandhi, S, 2017
)
0.77
" Vultures exposed to carprofen as residues in the kidney tissue or pure drug equivalents showed no toxic signs."( The use of toxicokinetics and exposure studies to show that carprofen in cattle tissue could lead to secondary toxicity and death in wild vultures.
Chipangura, J; Duncan, N; Galligan, TH; Green, RE; Naidoo, V; Taggart, MA; Wolter, K, 2018
)
0.48
"Kidney has a vital role in renal clearance, maintenance of blood pressure, elimination of toxic products and formation of prostaglandins."( Diclofenac-induced renal toxicity in female Wistar albino rats is protected by the pre-treatment of aqueous leaves extract of Madhuca longifolia through suppression of inflammation, oxidative stress and cytokine formation.
Evan Prince, S; S, JP, 2018
)
1.92
" Based on the results, tolpersione injection and per os formulations can be considered an effective and safe drugs in the combined therapy for patients with acute nonspecific back pain."( [Results of a randomized double blind parallel study on the efficacy and safety of tolpersione in patients with acute nonspecific low back pain].
Brylev, LV; Chefranova, ZY; Guekht, AB; Kukushkin, ML; Laskov, VB; Makarov, NS; Pizova, NV; Sholomov, II; Sokov, EL,
)
0.13
" Both the test and the reference treatment were well tolerated in terms of adverse effects, laboratory parameters and vital signs."( Efficacy and safety of a fixed combination of intramuscular diclofenac 75 mg + thiocolchicoside 4 mg in the treatment of acute low back pain: a phase III, randomized, double blind, controlled trial.
Albamonte, E; Caggiano, G; Costantino, C; Giossi, A; Mancuso, M; Rigamonti, A; Sproviero, E; Tornari, P, 2018
)
0.72
"The new diclofenac+thiocolchicoside FDC formulation may allow treating effectively acute LBP while reducing the number of injections and hence the risk of local adverse reactions, and improving the patient's compliance."( Efficacy and safety of a fixed combination of intramuscular diclofenac 75 mg + thiocolchicoside 4 mg in the treatment of acute low back pain: a phase III, randomized, double blind, controlled trial.
Albamonte, E; Caggiano, G; Costantino, C; Giossi, A; Mancuso, M; Rigamonti, A; Sproviero, E; Tornari, P, 2018
)
1.16
"To ascertain if etoricoxib increases the risk of gastrointestinal adverse events (GAEs) compared with placebo, diclofenac, and naproxen in the treatment of patients with osteoarthritis (OA) or rheumatoid arthritis (RA)."( Gastrointestinal safety of etoricoxib in osteoarthritis and rheumatoid arthritis: A meta-analysis.
Feng, X; Mei, H; Tian, M; Zhang, W, 2018
)
0.69
"Diclofenac (DCF) can cause adverse reactions such as gastrointestinal, renal and cardiovascular disorders; therefore, topical administration may be an attractive alternative to the management of local pain in order to avoid these side effects."( Photo(geno)toxicity changes associated with hydroxylation of the aromatic chromophores during diclofenac metabolism.
Andreu, I; Consuelo Jiménez, M; Garcia-Lainez, G; Limones-Herrero, D; Martínez-Reig, AM; Miranda, MA, 2018
)
2.14
" parietina showed similar toxic effects, expressed as ergosterol content."( Toxicity of Diclofenac in the Fern Azolla filiculoides and the Lichen Xanthoria parietina.
Bačkor, M; Bačkorová, M; Loppi, S; Paoli, L; Vannini, A; Vichi, M, 2018
)
0.86
" It is also particularly associated with its adverse effects on avian fauna and linked to environmental issues."( Assessment of dose-dependent reproductive toxicity of diclofenac sodium in male rats.
Purohit, A; Ram, H; Vyas, A, 2019
)
0.76
" Overall incidence of treatment-emergent adverse events (TEAEs) was similar in the three groups (p = 0."( Safety of Injectable HPβCD-Diclofenac in Older Patients with Acute Moderate-to-Severe Postoperative Pain: A Pooled Analysis of Three Phase III Trials.
Chelly, JE; Lacouture, PG; Reyes, CRD, 2018
)
0.78
" Reports of gastrointestinal adverse effects with traditional NSAIDs and cardiovascular adverse effects associated with selective cyclooxygenase-2 (COX-2) inhibitors have prompted the hunt for a better NSAID with no or minimal adverse effects."( Comparison of Clinical Effectiveness and Safety of Newer Nonsteroidal Anti-inflammatory Drugs in Patients of Osteoarthritis of Knee Joint: A Randomized, Prospective, Open-label Parallel-group Study.
Garg, Y; Gore, R; Kumar, A; Singh, J; Sohal, HS,
)
0.13
" Gastrointestinal symptoms like nausea and stomatitis, skin rashes, alopecia, central nervous system symptoms like headache and confusion, hepatotoxicity and myelosuppression are some of the adverse effects."( Severe bone marrow suppression due to methotrexate toxicity following aceclofenac-induced acute kidney injury.
Biju, IK; Manappallil, RG; Peringat, J; Prasan, D, 2018
)
0.48
" Both meloxicam and diclofenac exerted toxic effects on the hepatic cells."( The use of liver slices from the Cape vulture (Gyps coprotheres) to better understand the role of liver toxicity of non-steroidal anti-inflammatory drugs (NSAIDs) in vultures.
Adawaren, EO; Bekker, L; Duncan, N; Mukandiwa, L; Naidoo, V; Njoya, EM, 2018
)
0.8
" In addition, the rate of adverse reaction of research group was also lower than that of control group, P<0."( Clinical therapeutic effect and safety of celecoxib in treating knee osteoarthritis.
Bi, J; Yu, C; Yu, X; Yu, Z; Zhao, L, 2018
)
0.48
" Thus, the aim of this study was to analyze the toxic effects of pharmaceuticals in non-standard endpoints on two macrophyte species, Lemna minor and Lemna gibba."( Evaluation of pharmaceutical toxic effects of non-standard endpoints on the macrophyte species Lemna minor and Lemna gibba.
Alkimin, GD; Barata, C; Daniel, D; Frankenbach, S; Nunes, B; Serôdio, J; Soares, AMVM, 2019
)
0.51
" Even though ozonation has proven to be very efficient in reducing pharmaceutical parent compound concentrations in wastewater effluents, much remains unclear regarding potentially toxic ozonation by-product (OBP) formation."( Embryotoxicity of ozonated diclofenac, carbamazepine, and oxazepam in zebrafish (Danio rerio).
Ahrens, L; Carlsson, G; Golovko, O; Norrgren, L; Örn, S; Pohl, J; Weiss, J, 2019
)
0.81
" Further studies utilizing other specific tests, such as corneal lineage are required before safe and efficient ophthalmologic use."( Toxicity of therapeutic contact lenses based on bacterial cellulose with coatings to provide transparency.
Cavicchioli, M; Coelho, F; do Vale Braido, GV; Franchi, LP; Lima Ribeiro, SJ; Mendes, LS; Messaddeq, Y; O Capote, TS; Scarel-Caminaga, RM; Specian, SS, 2019
)
0.51
" Adverse effects were significantly less in the curcumin group (13% versus 38% in the diclofenac group; P <0."( Safety and efficacy of curcumin versus diclofenac in knee osteoarthritis: a randomized open-label parallel-arm study.
Gade, P; Karad, S; Khanwelkar, C; Shep, D, 2019
)
1.01
" While measured to have a moderate effect on pain in osteoarthritis, NSAIDs have been associated with wide-ranging adverse events affecting the gastrointestinal, cardiovascular, and renal systems."( Safety of Oral Non-Selective Non-Steroidal Anti-Inflammatory Drugs in Osteoarthritis: What Does the Literature Say?
Al-Daghri, N; Bruyère, O; Chapurlat, R; Cooper, C; Herrero-Beaumont, G; Rannou, F; Reginster, JY; Roth, R; Uebelhart, D, 2019
)
0.51
" Randomized, double-blind, placebo-controlled, parallel-group trials that assessed adverse events (AEs) with topical NSAIDs in patients with OA were eligible for inclusion."( Safety of Topical Non-steroidal Anti-Inflammatory Drugs in Osteoarthritis: Outcomes of a Systematic Review and Meta-Analysis.
Beaudart, C; Bruyère, O; Charles, A; Cooper, C; Geerinck, A; Honvo, G; Leclercq, V; Rabenda, V; Reginster, JY; Thomas, T; Veronese, N, 2019
)
0.51
"Topical NSAIDs may be considered safe in the management of OA, especially with regard to low gastrointestinal toxicity."( Safety of Topical Non-steroidal Anti-Inflammatory Drugs in Osteoarthritis: Outcomes of a Systematic Review and Meta-Analysis.
Beaudart, C; Bruyère, O; Charles, A; Cooper, C; Geerinck, A; Honvo, G; Leclercq, V; Rabenda, V; Reginster, JY; Thomas, T; Veronese, N, 2019
)
0.51
" Long term usage and over-dosage of diclofenac is associated with adverse effects like drug-induced liver injury, gastrointestinal and renal toxicity."( Protective effect of the ethanolic and methanolic leaf extracts of Madhuca longifolia against diclofenac-induced toxicity in female Wistar albino rats.
Katturaja, R; Namachivayam, A; Nithyanandham, S; Parthasarathy, M; Prince, SE; Simon, JP, 2019
)
1.01
" However, adverse effects in the kidney limit its clinical application."( Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters.
Huo, X; Liu, K; Ma, X; Meng, Q; Sun, H; Wang, C; Wu, J; Zhu, Y, 2020
)
0.83
" Cilastatin can be potentially used in the clinic as a therapeutic agent to alleviate the adverse renal reaction to diclofenac."( Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters.
Huo, X; Liu, K; Ma, X; Meng, Q; Sun, H; Wang, C; Wu, J; Zhu, Y, 2020
)
1.04
" At a low concentration of toxic substances, a hormetic stimulating effect occurs, while an inhibitory effect occurs at higher concentrations."( Elimination of the hormesis phenomenon by the use of synthetic sea water in a toxicity test towards Aliivibrio fischeri.
Drzymała, J; Kalka, J, 2020
)
0.56
" Safety after treatment was evaluated by recording adverse events and laboratory investigations."( Efficacy and safety of combination of curcuminoid complex and diclofenac versus diclofenac in knee osteoarthritis: A randomized trial.
Gade, P; Karad, S; Khanwelkar, C; Shep, D, 2020
)
0.8
" Adverse effects were significantly less in curcuminoid complex plus diclofenac group (13% vs 38% in diclofenac group; P < ."( Efficacy and safety of combination of curcuminoid complex and diclofenac versus diclofenac in knee osteoarthritis: A randomized trial.
Gade, P; Karad, S; Khanwelkar, C; Shep, D, 2020
)
1.03
"The safety of diclofenac (DIC) use in clinical practice has been questioned because of adverse cardiovascular effects."( Calcitriol Reduces Adverse Effects of Diclofenac on Mitochondrial Function in Isolated Rat Heart Mitochondria.
Atashbar, S; Azizian, S; Khezri, S; Kurdpour, P; Salimi, A; Shaikhgermchi, Z, 2020
)
1.19
" Minor adverse effects appeared to be related to the higher doses of tramadol."( Efficacy and Safety of Two Fixed-Dose Combinations of Tramadol Hydrochloride and Diclofenac Sodium in Postoperative Dental Pain.
Alvarado, F; Desjardins, P; Gil, M; González, M; Guajardo, R, 2020
)
0.78
"The adverse effect of diclofenac administration on the male reproductive organ in both humans and rats has been reported."( Selenium attenuates diclofenac-induced testicular and epididymal toxicity in rats.
Aliyu-Banjo, NO; Odunola, OA; Owumi, SE, 2020
)
1.2
" Adverse events were defined as irritation, gastrointestinal upset/bleed, rectal bleed, and hematemesis."( Determination of efficacy and toxicity of diclofenac microemulsion formulation for musculoskeletal pain: an observational study.
Banh, HL; Cave, A, 2020
)
0.82
" No adverse effects were reported."( Determination of efficacy and toxicity of diclofenac microemulsion formulation for musculoskeletal pain: an observational study.
Banh, HL; Cave, A, 2020
)
0.82
" It is reported that DCF has adverse effects on aquatic organisms."( Ozonation of diclofenac in the aqueous solution: Mechanism, kinetics and ecotoxicity assessment.
An, Z; Bo, X; Han, D; He, M; Li, M; Mei, Q; Qiu, Z; Sun, J; Wang, X; Wei, B; Wei, F; Xie, J, 2020
)
0.93
" Adverse events of therapy were mild."( [Assessment of the safety, tolerability and effectiveness of first Russian generic aceclofenac in patients with undifferentiated peripheral inflammatory arthritis].
Akhverdyan, YR; Papichev, EV; Polyakova, YV; Sivordova, LE; Zavodovsky, BV, 2020
)
0.56
" The aim of this study was to evaluate the renal anatomy and related vasculature of the Cape griffon vulture (Gyps coprotheres) (CGV), a species sensitive to the toxic effects of diclofenac, using gross anatomy, histology and vascular casting."( Does the renal portal valve exist in a raptor species? A study aimed at further evaluating the mechanism of toxicity of diclofenac in vultures.
Duncan, N; Groenewald, HB; Havenga, L; Naidoo, V; Wolter, K, 2020
)
0.96
" Safety evaluations were performed after the initial dose and at the end of study on day 90; adverse events were monitored throughout the study."( An Open-Label Study Evaluating the Pharmacokinetics and Safety of Diclofenac Potassium for Oral Solution for the Acute Treatment of MWA or MWoA in Pediatric Participants.
Amend, DL; Ferger, SM; Hogan, RM; McVige, JW; Shanahan, CM, 2020
)
0.8
" The most frequently reported treatment emergent adverse events were arthralgia and motion sickness, each of which occurred in 2 (8%) of the participants."( An Open-Label Study Evaluating the Pharmacokinetics and Safety of Diclofenac Potassium for Oral Solution for the Acute Treatment of MWA or MWoA in Pediatric Participants.
Amend, DL; Ferger, SM; Hogan, RM; McVige, JW; Shanahan, CM, 2020
)
0.8
"Diclofenac (DCF), a persistent pharmaceutical micropollutant which occurs in the ecosystems causing adverse effects on aquatic as well as terrestrial organisms."( Ecotoxicological assessment of micropollutant Diclofenac biosorption on magnetic sawdust: Phyto, Microbial and Fish toxicity studies.
Narayanasamy, S; Shahnaz, T; Sivaprakasam, S; Suganya, E; Vishnu Priyan, V, 2021
)
2.32
"The proliferation and possible adverse effects of emerging contaminants such as pharmaceutical and personal care products (PPCPs) in waters and the environment is a cause for increasing concern."( Bacterial ecotoxicity and shifts in bacterial communities associated with the removal of ibuprofen, diclofenac and triclosan in biopurification systems.
Aguilar-Romero, I; Romero, E; van Dillewijn, P; Wittich, RM, 2020
)
0.77
"At present, information about clinical efficacy and adverse events of controlled release (CR) form of pelubiprofen, a prodrug of 2-arylopropionic acid with relatively selective effects on cyclooxygenase-2 activity, remains scarce."( Efficacy and safety of short-term use of a pelubiprofen CR and aceclofenac in patients with symptomatic knee osteoarthritis: A double-blinded, randomized, multicenter, active drug comparative, parallel-group, phase IV, non-inferiority clinical trial.
Chang, MJ; Han, SB; Kang, SB; Kim, KI; Kim, MK; Kim, SH; Lee, HJ; Lee, S; Moon, YW; Park, HG; Shin, JY; Yoo, JD, 2020
)
0.56
" For safety analysis, adverse events, clinical laboratory tests, vital signs, and physical examinations were assessed and conducted at each follow-up visit."( Efficacy and safety of short-term use of a pelubiprofen CR and aceclofenac in patients with symptomatic knee osteoarthritis: A double-blinded, randomized, multicenter, active drug comparative, parallel-group, phase IV, non-inferiority clinical trial.
Chang, MJ; Han, SB; Kang, SB; Kim, KI; Kim, MK; Kim, SH; Lee, HJ; Lee, S; Moon, YW; Park, HG; Shin, JY; Yoo, JD, 2020
)
0.56
"Pelubiprofen CR 90 mg is as effective as aceclofenac 200 mg with reduced adverse events for the treatment of symptomatic knee osteoarthritis."( Efficacy and safety of short-term use of a pelubiprofen CR and aceclofenac in patients with symptomatic knee osteoarthritis: A double-blinded, randomized, multicenter, active drug comparative, parallel-group, phase IV, non-inferiority clinical trial.
Chang, MJ; Han, SB; Kang, SB; Kim, KI; Kim, MK; Kim, SH; Lee, HJ; Lee, S; Moon, YW; Park, HG; Shin, JY; Yoo, JD, 2020
)
0.56
" In this study, the adverse effects of four pharmaceuticals, 17α-ethynylestradiol (synthetic estrogen), methotrexate (anticancer drug), diclofenac (nonsteroidal anti-inflammatory drug) and fluoxetine (antidepressant), and their binary mixtures at mg/L concentrations were assessed using the 7-day Lemna minor test, with both apical and biochemical markers evaluated."( Combined toxicity of therapeutic pharmaceuticals to duckweed, Lemna minor.
Kumar, A; Markovic, M; Neale, PA; Nidumolu, B, 2021
)
0.82
" Stimulated inflammatory conditions seemed to reduce toxic effects."( Inflammation reduces osteoblast cytotoxicity induced by diclofenac: An in vitro study.
Aguirre, J; Bonvini, JM; Borgeat, A; Camponovo, C; Rupnik, B; Saporito, A, 2021
)
0.87
" However, studies evaluating the toxic effect of mixtures of these contaminants are scarce."( Geno-cytotoxicity and congenital malformations produced by relevant environmental concentrations of aluminum, diclofenac and their mixture on Cyprinus carpio. An interactions study.
Cano-Viveros, S; Galar-Martínez, M; García-Medina, S; Gasca-Pérez, E; Gómez-Oliván, LM; Islas-Flores, H; Quiroga-Santos, EH; Ruíz-Lara, K, 2021
)
0.83
" To simulate variable environmental conditions, the aim of our study was to examine adverse effects of diclofenac under different temperatures of cell incubation (18, 21, 24, 27 and 30 °C)."( Diclofenac-induced cytotoxicity in cultured carp leukocytes.
Nemcova, M; Pikula, J; Seidlova, V; Zukal, J, 2020
)
2.22
" Safety was evaluated by adverse event monitoring."( Efficacy and Safety of Diclofenac-Hyaluronate Conjugate (Diclofenac Etalhyaluronate) for Knee Osteoarthritis: A Randomized Phase III Trial in Japan.
Kano, K; Nishida, Y; Nobuoka, Y; Seo, T, 2021
)
0.93
" Biodegradation of DCF by this bacterial consortium generates relatively safe final by-products."( Removal of diclofenac by a local bacterial consortium: UHPLC-ESI-MS/MS analysis of metabolites and ecotoxicity assessment.
Aissaoui, S; Fagnani, E; Ouled-Haddar, H; Pérez, S; Sifour, M, 2021
)
1.01
"Diclofenac, one of the most commonly used non-steroidal anti-inflammatory drugs, leads to severe adverse effects on the kidneys."( Phosphodiesterase (1, 3 & 5) inhibitors attenuate diclofenac-induced acute kidney toxicity in rats.
Abdel-Razek, NS; Salem, HA; Wadie, W, 2021
)
2.32
" Observation indicators included: the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC), Hospital for Special Surgery Knee Score (HSS), liver and kidney function, adverse reactions, and so on."( Efficacy and safety of Biqi capsule in the treatment of knee osteoarthritis: A protocol of a randomized controlled trial.
Huang, H; Jia, M; Tian, K; Wang, W; Zhou, Y, 2021
)
0.62
" As the carboxylic acid moiety present in common NSAIDs is responsible for some of their adverse effects, but is not required for their anti-inflammatory activity, we sought to mask this group through direct coupling to glucosamine, which is thought to prevent cartilage degradation."( Molecular docking-guided synthesis of NSAID-glucosamine bioconjugates and their evaluation as COX-1/COX-2 inhibitors with potentially reduced gastric toxicity.
Hall, CD; Jones Lipinski, RA; Katritzky, AR; Morisseau, C; Sebastiano, CS; Smith, BC; Thillier, Y, 2021
)
0.62
" The overall adverse event profile of the groups was similar, and no difference was found in skin reaction rates between the 2 groups."( Comparison of the Efficacy and Safety of Ketoprofen Plaster and Diclofenac Plaster for Osteoarthritis-Related Knee Pain: A Multicenter, Randomized, Active-Controlled, Open-Label, Parallel-Group, Phase III Clinical Trial.
Cha, JE; Ershova, O; Hyun, BJ; Kastanayan, A; Krechikova, D; Nikulenkova, N; Polyakova, S; Shvarts, Y; Vinogradova, I; Yakushin, S, 2021
)
0.86
"Cisplatin (CDDP) is a well-known anticancer agent, and CDDP-induced nephrotoxicity (CIN) is one of the most serious adverse effects."( Diclofenac potentiates the antitumor effect of cisplatin in a xenograft mouse model transplanted with cisplatin-resistant cells without enhancing cisplatin-induced nephrotoxicity.
Furugen, A; Kobayashi, M; Narumi, K; Okamoto, K; Saito, Y; Ueda, H, 2021
)
2.06
" Fourteen adverse events (none serious) in nine patients (8."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022
)
1
"The FLECTOR topical system safely and effectively provided pain relief for minor soft tissue injuries in the pediatric population, with minimal systemic nonsteroidal anti-inflammatory drug exposure and low potential risk of local or systemic adverse events."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022
)
1
" This study shows that FDETS can safely and effectively provide pain relief for soft tissue injuries in children, with minimal systemic NSAID exposure and a low potential risk of either local or systemic adverse events."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022
)
1
" Subsequently, a number of other NSAIDs have been identified as toxic to vultures, while one, meloxicam, is safe at concentrations likely to be encountered by vultures in the wild."( Experimental safety testing shows that the NSAID tolfenamic acid is not toxic to Gyps vultures in India at concentrations likely to be encountered in cattle carcasses.
Chandramohan, S; Chutia, K; Galligan, TH; Green, RE; Gupta, R; Kesavan, M; Mahendran, K; Mallord, JW; Mathesh, K; Pawde, A; Prakash, NV; Prakash, VM; Ravichandran, P; Saikia, D; Sharma, AK; Shringarpure, R; Timung, A, 2022
)
0.72
" Adverse events (AEs) were evaluated as the safety outcome."( Efficacy and safety of S-flurbiprofen plaster in knee osteoarthritis patients: A 2-week randomized controlled Phase III clinical trial compared to diclofenac gel.
Fuady, A; Matsumoto, H; Tomatsu, K; Yasuda, S, 2022
)
0.92
"Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently used medications for pain, even though they increase the risk for adverse cardiovascular events."( Reduced risk of NSAID-Induced adverse events with concomitant use of misoprostol (MICRO study).
Cheung, AK; Munger, MA; Nelson, SD; Sauer, BC; Teng, CC, 2022
)
0.72
"Compared with NSAID use alone, the concomitant use of NSAID plus misoprostol is associated with a reduced risk of NSAID-induced cardiovascular, cerebrovascular, and renal adverse events."( Reduced risk of NSAID-Induced adverse events with concomitant use of misoprostol (MICRO study).
Cheung, AK; Munger, MA; Nelson, SD; Sauer, BC; Teng, CC, 2022
)
0.72
"Despite the extensive therapeutic uses of diclofenac, it may cause several adverse effects, including hepatorenal injury."( Resveratrol mitigates diclofenac-induced hepatorenal toxicity in rats via modulation of miR-144/Nrf2/GSH axis.
Abdelmonem, M; Ahmed, KA; Elbaz, EM, 2022
)
1.3
" Adverse drug reactions may be renal, gastrointestinal, hematological, or immunologic."( Efficacy and Safety of NSAIDs in Infants: A Comprehensive Review of the Literature of the Past 20 Years.
Gorenflo, M; Saur, P; van den Anker, JN; van Dyk, M; Welzel, T; Ziesenitz, VC, 2022
)
0.72
" This study provides novel mechanistic insights into the toxic effects of anti-inflammatory drugs on aquatic crustaceans."( Acute toxic effects of diclofenac exposure on freshwater crayfish (Procambarus clarkii): Insights from hepatopancreatic pathology, molecular regulation and intestinal microbiota.
Li, M; Li, Z; Ren, N; Sun, K; Zhang, Y, 2022
)
1.03
" Therefore, we aimed to evaluate the overall incidence and patterns of adverse events (AEs), the effectiveness of aceclofenac CR, and the differences in incidence rates of the AEs based on each patient's baseline charateristics."( Safety and effectiveness of 4-week therapy with aceclofenac controlled release once a day.
Abd El-Aty, AM; Bang, JS; Chung, YH; Jeong, JC; Jeong, JH; Jung, TW; Park, SY; Park, T, 2022
)
0.72
" DF toxic effects could be the consequences of mitochondrial dysfunction and free radical effects."( Hepatoprotective Effect of Coenzyme Q10 in Rats with Diclofenac Toxicity.
Abed Al-Kareem, Z; Ali Zghair, M; Aziz, ND, 2022
)
0.97
" The implementation of practical guidelines and training programs for health care workers to appropriately prescribe, dispense, and administer PRN medicines are necessary, and should at least include providing clarification for their indication, dose and frequency, as well as any cautionary instructions to ensure safe and effective use of such medicines."( Surviving surgery; succumbing to pharmacotherapy: A case report underscoring the importance of PRN order clarification for patient safety.
Farasatinasab, M; Karimian, Z; Nassiri, S; Tahermanesh, K, 2023
)
0.91
"we conclude from these results that Artemisia may have a role in reducing the toxic effect of diclofenac on kidney and liver by decreasing the liver enzymes and kidney criteria in the blood."( Hepatorenal protective activity of Artemisia against diclofenac toxicity in male rats.
Kadhim, SH; Mosa, AU; Ubaid, MM, 2022
)
1.19
" No serious adverse events (SAEs) were registered, and the most commonly detected adverse events were skin reactions at the application site."( Efficacy and safety of Diclofenac sodium plaster in patients with acute pain of the limbs: a randomized, placebo and active-controlled, double-blind, parallel-group trial.
Barbaro, B; Giordan, N; Gruber, G; Pabst, H; Picciotto, R, 2023
)
1.22
" Significant limitations of DIC treatment stem from its adverse effects."( Natural sporopollenin microcapsules: biological evaluation and application in regulating hepatic toxicity of diclofenac sodium
Dyab, AKF; Meligi, NM, 2023
)
1.12
" Drug-related adverse events were mild-to-moderate and resolved by the treatment end."( Safety and Efficacy of Oral Nalbuphine on Postoperative Pain in Hemorrhoidectomy Patients: A Randomized, Double-blind, Placebo-controlled, Pivotal Trial.
Chen, WS; Hsiao, KH; Hu, OY; Jao, SW; Jiang, JK; Lee, CC; Lee, TY; Lin, CC; Lin, HC; Lin, TC; Wu, CC, 2023
)
0.91
" The in silico prediction suggested that the formed transformation products maintained the persistence, bioaccumulation potential, and multi-endpoint toxic effects such as genotoxicity, developmental toxicity, and acute/chronic toxicity on different aquatic species."( Photodegradation of typical pharmaceuticals changes toxicity to algae in estuarine water: A metabolomic insight.
Chi, L; Feng, M; Li, B; Lin, J; Yuan, Q, 2024
)
1.44

Pharmacokinetics

The aim was to characterize the dissolution profile of a poorly soluble drug, diclofenac, from a commercially available multiple-unit enteric coated dosage form, Diclo-Puren® capsules. The pharmacokinetic (PK) properties of DPSGC are investigated and compared with a commercially Available oral dic lofenAC potassium tablet in patients after unilateral first metatarsal bunionectomy.

ExcerptReferenceRelevance
" The relative bioavailability from the test formulation (a solution gel) in terms of Cmax and AUC, calculated from the amount of drug reaching the systemic circulation, was found to be twice the amount after application of reference product (an emulsion gel)."( Comparative pharmacokinetics and bioavailability study of percutaneous absorption of diclofenac from two topical formulations containing drug as a solution gel or as an emulsion gel.
Seth, BL, 1992
)
0.51
" Also tmax was shorter for Dr (1."( [Comparative bioavailability and pharmacokinetics of Dolotren retard and Dolotren].
Honorato, J; Lucero, ML; Montes, B; Suárez, J; Valiente, R,
)
0.13
" Vt and total plasma clearance were higher than in adults but the elimination half-life was similar."( Pharmacokinetics of intravenous diclofenac sodium in children.
Korpela, R; Olkkola, KT, 1990
)
0.56
" Diurnal profiles were recorded on the 1st and 4th days, from which pharmacokinetic parameters were calculated: particular attention was given to cumulation."( The pharmacokinetics of a new sustained-release form of diclofenac sodium in humans.
Mascher, H, 1989
)
0.52
" The method is applied for the determination of the pharmacokinetic parameters of diclofenac after administration of two formulations (enteric-coated tablet and slow-release tablet), to a healthy male volunteer."( A rapid and sensitive high-performance liquid chromatographic method for the determination of diclofenac sodium in serum and its use in pharmacokinetic studies.
Abdel-Hameed, ME; el-Sayed, YM; Najib, NM; Suleiman, MS, 1988
)
0.72
"05) the area under the curve in tissue-cage fluid of ceftriaxone and cefotiam-treated animals, and the terminal half-life of ceftriaxone in their sera (3."( Enhancement of the therapeutic effect of cephalosporins in experimental endocarditis by altering their pharmacokinetics with diclofenac.
Brion, N; Carbon, C; Joly, V; Pangon, B; Vallois, JM, 1988
)
0.48
" We thus found no clinical manifestations of the pharmacokinetic interaction."( A study to determine the clinical relevance of the pharmacokinetic interaction between aspirin and diclofenac.
Bird, HA; Hill, J; Leatham, P; Wright, V, 1986
)
0.49
"Only recently have the pharmacokinetic characteristics of nonsteroidal anti-inflammatory drugs (NSAIDs) been recognized as decisive factors in understanding the effects and side effects of these drugs."( Clinical relevance of nonsteroidal anti-inflammatory drug pharmacokinetics.
Brune, K, 1987
)
0.27
" Plasma levels of diclofenac were measured and pharmacokinetic parameters were calculated."( Pharmacokinetics of diclofenac sodium after intramuscular administration in combination with triamcinolone acetate.
Barth, J; Derendorf, H; Grüner, A; Möllmann, H; Mullersman, G, 1986
)
0.93
"Even the most widely used non-steroidal anti-inflammatory drugs (NSAID's) show considerable variations in their pharmacokinetic behaviour in volunteers and moreso in patients."( Pharmacokinetic factors as causes of variability in response to non-steroidal anti-inflammatory drugs.
Brune, K, 1985
)
0.27
" A single oral dose of enteric-coated diclofenac sodium was given to 10 patients with active rheumatoid disease, adopting the same procedures used for a group of 10 healthy volunteers in whom pharmacokinetic data was already available."( The pharmacokinetics of diclofenac sodium in patients with active rheumatoid disease.
Crook, PR; Fowler, PD; Jack, DB; Kendall, MJ; Willis, JV, 1982
)
0.84
" The dispersible formulation showed a relative extent of bioavailability between 78% and 99% (90% CI) for the AUC0-infinity, being the 90% CI for the Cmax 63%-129%."( Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks.
Carcas, AJ; Frias, J; Guerra, P; Lucero, ML; Macía, MA; Valiente, R, 1995
)
0.53
" This method has been applied to evaluate the pharmacokinetic parameters of the drugs, using a noncompartmental model, after the oral administration of 5 mg/kg nitrofenac to rats."( Plasma concentrations and pharmacokinetic parameters of nitrofenac using a simple and sensitive HPLC method.
Adami, A; Benoni, G; Cuzzolin, L; Del Soldato, P; Grigolini, L; Terzi, M, 1995
)
0.29
" In experiment 1, single injections were administered IV to 1 cow and IV and IM to 1 heifer (7 days apart), and pharmacokinetic variables were calculated."( High-performance liquid chromatography method for determination of flunixin in bovine plasma and pharmacokinetics after single and repeated doses of the drug.
Johansson, IM; Odensvik, K, 1995
)
0.29
" The pharmacokinetic properties of Ortopak were similar to those of Voltaren-retard, which were close to those of diclophenac-sodium in the blood plasma within the therapeutic range."( [The pharmacokinetics of the new Russian prolonged-action form of diclofenac sodium--Ortopek--in a single oral dose].
Ignat'ev, VG; Kemenova, VA; Kurapov, AP; Rubtsova, TM; Starodubtsev, AK,
)
0.37
" The paper deals with local tolerability and pharmacokinetic (percutaneous absorption) studies carried out both on animals and on volunteers."( Local tolerability and pharmacokinetic profile of a new transdermal delivery system, diclofenac hydroxyethylpyrrolidine plaster.
Assandri, A; Canali, S; Giachetti, C, 1993
)
0.51
" Thirty min after the first administration on the first day (single) and 30 min after the last administration in the morning of the 8th day (repeated premedication), pharmacokinetic examinations with retarded theophylline capsules (250 mg) or enteric coated tablets of diclofenac (50 mg) were performed."( Potential pharmacokinetic interactions of nocloprost clathrate with retarded theophylline and enteric coated diclofenac after single and repeated premedication in healthy volunteers.
Amon, I; Franke, G; Scheuch, E; Siegmund, W; Stolz, E; Zschiesche, M, 1993
)
0.68
" The mean pharmacokinetic characteristics of cyclosporine were unchanged during coadministration with diclofenac."( Pharmacokinetics of cyclosporine and multiple-dose diclofenac during coadministration.
Hitzenberger, G; Johnston, A; Koelle, EU; Kovarik, JM; Merdjan, H; Mueller, EA, 1993
)
0.75
"The pharmacokinetic properties of a new gastroprotective pharmaceutical formulation of diclofenac (CAS 15307-79-6) were investigated in twelve healthy volunteers."( Pharmacokinetic studies in healthy volunteers on a new gastroprotective pharmaceutic form of diclofenac.
Carabelli, A; Contos, S; De Bernardi di Valserra, M; Feletti, F; Germogli, R; Maggi, L; Tripodi, AS, 1993
)
0.73
" isradipine to assess a possible pharmacokinetic interaction."( Effects of diclofenac on isradipine pharmacokinetics and platelet aggregation in volunteers.
Blom, M; Grass, P; Kovarik, JM; Kutz, K; Meyer, EC; Ott, S; Snyman, JR; Sommers, DK; van Wyk, M, 1993
)
0.68
" These suppositories were evaluated with respect to their pharmacokinetic behaviour in 12 healthy, male human volunteers."( Comparative pharmacokinetic evaluation of compressed suppositories of diclofenac sodium in humans.
Diwan, PV; Fadnavis, NW; Ramakrishna, S, 1996
)
0.53
" To derive a model relating drug targeting index (DTI) to the pharmacokinetic parameters of the target and systemic sites, and to compare predictions with observations."( Regional drug delivery II: relationship between drug targeting index and pharmacokinetic parameters for three non-steroidal anti-inflammatory drugs using the rat air pouch model of inflammation.
Brennan, BS; Gifford, LA; Houston, JB; Martin, SW; McLachlan, A; Rowland, M; Stevens, AJ, 1995
)
0.29
" Lack of pharmacokinetic interaction was handled as an equivalence problem."( Lack of pharmacokinetic interaction between pantoprazole and diclofenac.
Bliesath, H; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.54
" Referring to the pharmacokinetic parameters Cmax and tmax typical differences between oral and rectal formulations were observed."( Pharmacokinetics and drug input characteristics for a diclofenac-codeine phosphate combination following oral and rectal administration.
Hanses, A; Meiss, F; Mutschler, E; Spahn-Langguth, H, 1996
)
0.54
" Lack of pharmacokinetic interaction was handled as an equivalence problem."( Lack of pharmacokinetic interaction between pantoprazole and diclofenac.
Bliesath, H; Huber, R; Koch, HJ; Mascher, H; Steinijans, VW; Wurst, W, 1996
)
0.54
" Pharmacokinetic profiles of diclofenac were obtained at the end of each treatment period."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
2.03
" Diclofenac half-life was not altered."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
2.65
" Due to the pharmacokinetic interaction that increases diclofenac systemic exposure, it would be prudent to start combination therapy with diclofenac doses at the lower end of the therapeutic dose range."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
1.98
" The Cmax obtained with Voltaren was significantly higher than that obtained with Inflaban (1,161 +/- 102 and 799 +/- 83, respectively)."( Bioavailability and pharmacokinetic properties of 2 sustained-release formulations of diclofenac sodium, Voltaren vs inflaban: effect of food on inflaban bioavailability.
Deleq, S; Hasan, M; Najib, N; Sallam, E; Shubair, M; Zmeili, S, 1996
)
0.52
"The pharmacokinetic analysis of an oral sustained-release preparation of diclofenac sodium has been investigated using multi-segment absorption models in which it has been assumed that the gastrointestinal tract can be divided into several segments in each of which the drug has its own lag-time and absorption rate constants."( Pharmacokinetic analysis of the absorption characteristics of diclofenac sodium in man by use of a multi-segment absorption model.
Mahmood, I, 1996
)
0.77
" Pharmacokinetic analyses were carried out using a computer program."( Pharmacokinetics and hepatotoxicity of diclofenac using an isolated perfused rat liver.
Domínguez, AR; González-Martin, G; Guevara, A, 1997
)
0.57
" Moreover, the effect lasted longer than expected from pharmacokinetic data."( Pharmacokinetic-pharmacodynamic modeling of the antinociceptive effect of diclofenac in the rat.
Castañeda-Hernández, G; Flores-Murrieta, FJ; Granados-Soto, V; Lopez-Muñoz, FJ; Torres-López, JE, 1997
)
0.53
" The aim of the present study was to evaluate the comparative efficacy of intramuscularly injected nimesulide with that of diclofenac and to elucidate the pharmacokinetic profile of this formulation."( Comparative analgesic activity of nimesulide and diclofenac by intramuscular route: correlation with pharmacokinetic profile of nimesulide.
Gupta, SK; Mathur, P; Sengupta, S; Velpandian, T, 1998
)
0.76
" The analgesic activity of nimesulide was subsequently correlated with its pharmacokinetic profile."( Analgesic efficacy and pharmacokinetics of topical nimesulide gel in healthy human volunteers: double-blind comparison with piroxicam, diclofenac and placebo.
Gupta, SK; Kabir, SR; Sengupta, S; Velpandian, T, 1998
)
0.5
" Peak analgesic effect was observed at 120 min post-treatment, which correlated with the pharmacokinetic profile of the drug in gel formulation."( Analgesic efficacy and pharmacokinetics of topical nimesulide gel in healthy human volunteers: double-blind comparison with piroxicam, diclofenac and placebo.
Gupta, SK; Kabir, SR; Sengupta, S; Velpandian, T, 1998
)
0.5
"The superior analgesic activity of nimesulide (as gel formulation), correlating with its pharmacokinetic profile, indicates that the topical route of administration may be a safe and effective alternative to the presently used oral and rectal routes."( Analgesic efficacy and pharmacokinetics of topical nimesulide gel in healthy human volunteers: double-blind comparison with piroxicam, diclofenac and placebo.
Gupta, SK; Kabir, SR; Sengupta, S; Velpandian, T, 1998
)
0.5
" The present study was designed to evaluate the anti-inflammatory activity of a new parenteral formulation of nimesulide and to correlate it with the pharmacokinetic profile."( Anti-inflammatory activity and pharmacokinetic profile of a new parenteral formulation of nimesulide.
Bhardwaj, RK; Gupta, SK; Sengupta, S; Tyagi, P; Velpandian, T, 1999
)
0.3
" The pharmacokinetic parameters calculated from the blood levels of the drug reveal a profile typical of a sustained-release formulation, with the ability to maintain adequate plasma levels for 24 hr (i."( Pharmacokinetic profile of a new matrix-type transdermal delivery system: diclofenac diethyl ammonium patch.
Devi, K; Paranjothy, KL, 1999
)
0.53
" A pharmacokinetic model was then developed to relate the tissue retention half lives for diclofenac, diazepam, water, lignocaine and salicylate to their fraction unbound in the tissues, their fraction unbound in the perfusate and the perfusate flow rate."( A physiological pharmacokinetic model for solute disposition in tissues below a topical below a topical application site.
Cross, SE; Roberts, MS, 1999
)
0.52
"Concomitant administration of diclofenac reduced the partial clearance of quinidine by N-oxidation by 27%, while no effect was found for other pharmacokinetic parameters of quinidine."( Effect of diclofenac, disulfiram, itraconazole, grapefruit juice and erythromycin on the pharmacokinetics of quinidine.
Brosen, K; Damkier, P; Hansen, LL, 1999
)
0.99
"This paper reports the results of a pharmacokinetic study involving 24 healthy volunteers and designed to characterise the rate and extent of diclofenac absorption after the administration of a single dose of diclofenac (CAS 15307-86-5) potassium salt 50 mg in sachet (Voltfast) and tablet (Cataflam) formulations."( Pharmacokinetics of diclofenac after oral administration of its potassium salt in sachet and tablet formulations.
Abbondati, G; Ceppi Monti, N; Crivelli, F; Dal Bo, L; Ismaili, S; Marzo, A; Tettamanti, RA; Uhr, MR; Verga, F, 2000
)
0.83
" The mean area under the serum concentration-time curve extrapolated to infinity, oral clearance, half-life, maximal concentration, and time to peak concentration for diclofenac and its metabolites were determined and compared using analysis of variance."( Pharmacokinetics of diclofenac sodium in chronic active hepatitis and alcoholic cirrhosis.
Bauer, LA; Carithers, R; Chan, K; Horn, JR; Lau, H; Lill, JS; O'Sullivan, T; Strandness, DE; Thakker, K, 2000
)
0.83
"Population pharmacokinetics of a fast release diclofenac were assessed with special focus on pharmacodynamic implications."( Population pharmacokinetics of fast release oral diclofenac in healthy volunteers: relation to pharmacodynamics in an experimental pain model.
Brune, K; Drover, D; Geisslinger, G; Kettenmann, B; Kobal, G; Lötsch, J; Renner, B, 2000
)
0.82
"Earlier drug absorption and lower pharmacokinetic variability of the fast-release formulation are likely to be preserved in a population."( Population pharmacokinetics of fast release oral diclofenac in healthy volunteers: relation to pharmacodynamics in an experimental pain model.
Brune, K; Drover, D; Geisslinger, G; Kettenmann, B; Kobal, G; Lötsch, J; Renner, B, 2000
)
0.56
"5 mgkg(-1)) pharmacokinetic parameters compared with administering AZT alone."( Zidovudine, diclofenac and ketoprofen pharmacokinetic interactions in rats.
Radwan, MA, 2000
)
0.69
" The aim of this study was to further investigate these pharmacokinetic DMXAA-drug interactions in the rat model."( A difference between the rat and mouse in the pharmacokinetic interaction of 5,6-dimethylxanthenone-4-acetic acid with thalidomide.
Ching, LM; Kestell, P; Paxton, JW; Tingle, MD; Zhou, S, 2001
)
0.31
" The cause of the species difference in the pharmacokinetic response to thalidomide by DMXAA is unknown, and indicates difficulties in predicting the outcome of such a combination in patients."( A difference between the rat and mouse in the pharmacokinetic interaction of 5,6-dimethylxanthenone-4-acetic acid with thalidomide.
Ching, LM; Kestell, P; Paxton, JW; Tingle, MD; Zhou, S, 2001
)
0.31
" The study was also extended to determine the pharmacokinetic profile of a newer formulation of meloxicam gel after topical application on depilated skin of rats."( Comparison of analgesic and anti-inflammatory activity of meloxicam gel with diclofenac and piroxicam gels in animal models: pharmacokinetic parameters after topical application.
Bansal, P; Bhardwaj, RK; Gupta, SK; Jaiswal, J; Velpandian, T,
)
0.36
"These data indicate that concomitant administration of diclofenac with nateglinide does not significantly alter the pharmacokinetic profile of either drug."( A 3-way crossover study to evaluate the pharmacokinetic interaction between nateglinide and diclofenac in healthy volunteers.
Anderson, DM; Buraglio, M; Crick, N; Shelley, S, 2002
)
0.78
" With an increase in injected dose, total body clearance was decreased while the distribution volume at steady state (V(dss)) was reduced and plasma half-life was prolonged."( Dose-dependent pharmacokinetics and disposition of bisphosphonic prodrug of diclofenac based on osteotropic drug delivery system (ODDS).
Fujisaki, J; Hata, T; Hirabayashi, H; Kimura, S; Sawamoto, T; Tokunaga, Y, 2002
)
0.54
" Analysis of variance was performed to determine whether lumiracoxib alone differed from lumiracoxib plus omeprazole or from lumiracoxib plus Al/Mg antacid for overall exposure (area under the concentration-time curve from zero to infinity [AUC( infinity )]) and peak concentration (C(max)), with treatment sequence, subject, period and treatment as factors."( Lack of effect of omeprazole or of an aluminium hydroxide/magnesium hydroxide antacid on the pharmacokinetics of lumiracoxib.
Langholff, W; Milosavljev, S; Rordorf, C; Scott, G; Shenouda, M; Vinluan Reynolds, C, 2004
)
0.32
" The pharmacodynamic study was carried out to evaluate the effect of Trikatu on the anti-inflammatory activity of diclofenac sodium using carragenin-induced rat paw edema model."( Pharmacokinetic and pharmacodynamic studies on interaction of "Trikatu" with diclofenac sodium.
D'Mello, PM; Lala, LG; Naik, SR, 2004
)
0.76
" The steady-state pharmacokinetics of lumiracoxib were evaluated in plasma and synovial fluid by both a population pharmacokinetic model and noncompartmental analysis."( Pharmacokinetics of lumiracoxib in plasma and synovial fluid.
Huff, JP; Kalbag, J; Looby, M; Milosavljev, S; Reynolds, C; Rordorf, C; Ruff, DA; Scott, G; Weaver, M, 2004
)
0.32
"Lumiracoxib was rapidly absorbed (peak plasma concentration at 2 hours) and the terminal elimination half-life in plasma was short (6 hours)."( Pharmacokinetics of lumiracoxib in plasma and synovial fluid.
Huff, JP; Kalbag, J; Looby, M; Milosavljev, S; Reynolds, C; Rordorf, C; Ruff, DA; Scott, G; Weaver, M, 2004
)
0.32
" This pharmacokinetic profile renders diclofenac suppository a suitable formulation for short duration surgery."( Diclofenac and metabolite pharmacokinetics in children.
Anderson, BJ; Jacqz-Aigrain, E; Rømsing, J; Tibboel, D; van der Marel, CD, 2004
)
2.04
" An analysis of variance was used to detect differences in PK parameters (AUC, Cmax and Tmax) between the treatment groups."( No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor.
Kalbag, J; Lasseter, K; Milosavljev, S; Oberstein, S; Rordorf, C; Yeh, CM, 2004
)
0.32
" Pharmacokinetic parameters were calculated with compartmental and non-compartmental analysis."( No effect of short term ranitidine intake on diclofenac pharmacokinetics.
Farcau, D; Leucuţa, A; Nanulescu, M; Vlase, L, 2004
)
0.58
"To investigate the pharmacodynamic behaviour of the selective cyclooxygenase-2 inhibitor, lumiracoxib, in the rat air pouch."( Pharmacodynamic behaviour of the selective cyclooxygenase-2 inhibitor lumiracoxib in the lipopolysaccharide-stimulated rat air pouch model.
Cramer, JA; Esser, RE; Georgieva, A; Maniara, W; Miserendino-Molteni, R; Porter, W; Ramos, L; Sharr, M; Zhang, X; Zhuang, S, 2005
)
0.33
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
"The present study aims to investigate the pharmacokinetic interaction between non-steroidal anti-inflammatory drugs and tetracycline in rats."( Pharmacokinetic interaction of tetracycline with non-steroidal anti-inflammatory drugs via organic anion transporters in rats.
Han, HK; Oh, YH, 2006
)
0.33
" It was observed that the simultaneous administration of diclofenac sodium and 300 mg kg(-1) of CME decreased significantly the values of Cmax (7."( Gastroprotection and effect of the simultaneous administration of Cuachalalate (Amphipterygium adstringens) on the pharmacokinetics and anti-inflammatory activity of diclofenac in rats.
Arrieta, J; Castañeda-Hernández, G; Cruz-Antonio, L; Navarrete, A; Oliva, I; Sánchez-Mendoza, ME, 2005
)
0.77
" Diclofenac pharmacokinetic parameters were determined by noncompartmental analysis."( Pharmacokinetics of diclofenac in sheep following intravenous and intramuscular administration.
Al-Hadiya, BM; Alkharfy, KM; Altaher, AY; Khan, RM, 2006
)
1.57
" Cmax of diclofenac sodium in aqueous humor instilled with liposome and eye-drop solution were (0."( [Preparation of diclofenac sodium liposomes and its ocular pharmacokinetics].
Huang, LJ; Liang, RC; Liu, K; Sun, KX; Wang, AP, 2006
)
1.1
" The method was successfully applied for pharmacokinetic study of aceclofenac in rats."( High-performance liquid chromatography and pharmacokinetics of aceclofenac in rats.
Musmade, P; Srinivasan, KK; Subramanian, G, 2007
)
0.34
" administration of diclofenac was best described by a two compartment open pharmacokinetic model."( Pharmacokinetics of diclofenac and its interaction with enrofloxacin in sheep.
Ahmad, AH; Kumar, A; Malik, JK; Rahal, A, 2008
)
1
" The present observations suggest that reduction of the pharmacokinetic parameters may lead to drug accumulation in the regenerating-damaged liver with an attendant possible increase in toxic effects."( Pharmacokinetics of diclofenac in rats intoxicated with CCL4, and in the regenerating liver.
Castañeda-Hernández, G; Favari, L; Muriel, P; Reyes-Gordillo, K, 2007
)
0.66
" Voriconazole did not affect significantly the elimination half-life or time to maximum concentration of diclofenac."( Effect of voriconazole on the pharmacokinetics of diclofenac.
Hynninen, VV; Laine, K; Leino, K; Lundgren, S; Neuvonen, PJ; Olkkola, KT; Rane, A; Valtonen, M, 2007
)
0.81
"Enterohepatic recirculation (EHC) is a common pharmacokinetic phenomenon that has been poorly modelled in animals."( Population pharmacokinetic modelling of the enterohepatic recirculation of diclofenac and rofecoxib in rats.
Chain, A; Danhof, M; Della Pasqua, O; Huntjens, DR; Metcalf, A; Spalding, DJ; Strougo, A; Summerfield, S, 2008
)
0.58
"Our findings show the relevance of exploring EHC in a quantitative manner to accurately interpret pharmacodynamic findings in vivo, in particular when scaling across species."( Population pharmacokinetic modelling of the enterohepatic recirculation of diclofenac and rofecoxib in rats.
Chain, A; Danhof, M; Della Pasqua, O; Huntjens, DR; Metcalf, A; Spalding, DJ; Strougo, A; Summerfield, S, 2008
)
0.58
"48 microg/ml and a prolonged elimination half-life (T1/2beta: 47."( Pharmacokinetics and tissue residues of an oxytetracycline/diclofenac combination in cattle.
Errecalde, JO; Marchetti, L; Mariño Hernández, E; Mestorino, N, 2007
)
0.58
" The proposed method was successfully applied to the preliminarily study of potential pharmacokinetic interaction between Mor and diclofenac."( Sensitive HPLC-fluorescence detection of morphine labeled with DIB-Cl in rat brain and blood microdialysates and its application to the preliminarily study of the pharmacokinetic interaction between morphine and diclofenac.
Kuroda, N; Nakashima, K; Ogata, Y; Wada, M; Yamada, H; Yokota, C, 2008
)
0.74
" The plasma protein-binding activities, rather than metabolic clearance, in both types of rats would be a determining factor in the pharmacokinetic behaviour differences between control and AA rats."( Prediction of metabolic clearance of diclofenac in adjuvant-induced arthritis rats using a substrate depletion assay.
Fujii, A; Iwaki, M; Kawase, A; Komura, H; Uno, S, 2008
)
0.62
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Several pharmacokinetic (PK) parameters, including C(max), T(max), t(1/2), AUC(0-t), AUC(0-infinity), and k(e), were determined from the plasma concentrations of the 2 aceclofenac formulations."( Bioequivalence and pharmacokinetic evaluation of two branded formulations of aceclofenac 100 mg: a single-dose, randomized, open-label, two-period crossover comparison in healthy Korean adult volunteers.
Kang, JS; Lee, MH; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2008
)
0.35
" The purpose of this work was to examine in the rat if such interaction involves pharmacokinetic mechanisms or is solely limited to the pharmacodynamic level."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.61
" To evaluate the possibility of a pharmacokinetic interaction, the oral bioavailability of diclofenac (18 mg/kg) was studied in presence and the absence of glibenclamide (10 mg/kg)."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.83
" Notwithstanding, the interaction does no appear to involve pharmacokinetic mechanisms, as oral glibenclamide failed to produce any significant alteration in oral diclofenac bioavailability."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.81
" This interaction, however, appears due solely to a pharmacodynamic mechanisms as diclofenac pharmacokinetics are not altered."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.84
"To develop a population pharmacokinetic model for a new diclofenac suspension (50 mg 5 ml(-1)) in adult volunteers and paediatric patients, and recommend a dose for acute pain in children."( Population pharmacokinetics of oral diclofenac for acute pain in children.
Howard, RF; Johnson, A; Savage, I; Standing, JF; Wong, IC, 2008
)
0.87
" Population pharmacokinetic modelling was undertaken with NONMEM."( Population pharmacokinetics of oral diclofenac for acute pain in children.
Howard, RF; Johnson, A; Savage, I; Standing, JF; Wong, IC, 2008
)
0.62
" The transplacental pharmacokinetic model was fitted to the time profiles of the drug concentrations in the effluent and placenta to obtain transplacental pharmacokinetic parameters."( Transplacental pharmacokinetics of diclofenac in perfused human placenta.
Fujii, T; Hori, S; Nagata, H; Nakano, H; Ohtani, H; Satoh, S; Sawada, Y; Shintaku, K; Taketani, Y; Tsujimoto, M; Tsukimori, K, 2009
)
0.63
" The objective of this study was to determine pharmacokinetic parameters and to compare the bioavailability of the new formulation of injection diclofenac sodium (75 mg/ml), given as an intradeltoid injection, with the reference formulation (75 mg/3 ml) given intragluteally."( Pharmacokinetic profile of a new formulation of injection diclofenac designed for intradeltoid use.
Jaiswal, V; Nivsarkar, M; Ojha, A; Padh, H; Patel, S; Shep, D, 2009
)
0.8
" The objective of this study was to evaluate the pharmacokinetic properties of ciprofloxacin tablets with concurrent administration of diclofenac tablets in healthy adult human volunteers."( Pharmacokinetic interaction of ciprofloxacin with diclofenac: a single-dose, two-period crossover study in healthy adult volunteers.
Iqbal, Z; Khan, A; Khan, GS; Khan, JA; Naz, A, 2009
)
0.81
" The pharmacokinetic parameters were calculated using a noncompartmental model and a two-compartment model."( Pharmacokinetic interaction of ciprofloxacin with diclofenac: a single-dose, two-period crossover study in healthy adult volunteers.
Iqbal, Z; Khan, A; Khan, GS; Khan, JA; Naz, A, 2009
)
0.61
" AUC(0-infinity), Cmax, Tmax and other disposition kinetics were obtained with non-compartmental procedure."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and dehydrated rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2009
)
0.6
" Pharmacokinetic models were developed for both the dosage forms, and simulations were performed for different doses."( Influence of dosage form on the intravitreal pharmacokinetics of diclofenac.
Durairaj, C; Edelhauser, HF; Kim, SJ; Kompella, UB; Shah, JC, 2009
)
0.59
"By choosing a less soluble form of a drug such as diclofenac acid, vitreous elimination half-life can be prolonged up to 24 days, potentially resulting in therapeutic levels in the posterior segment tissues for a few months."( Influence of dosage form on the intravitreal pharmacokinetics of diclofenac.
Durairaj, C; Edelhauser, HF; Kim, SJ; Kompella, UB; Shah, JC, 2009
)
0.84
" In this study, the pharmacokinetic (PK) properties of DPSGC are investigated and compared with a commercially available oral diclofenac potassium tablet in patients after primary unilateral first metatarsal bunionectomy."( A pharmacokinetic analysis of diclofenac potassium soft-gelatin capsule in patients after bunionectomy.
Boesing, SE; Bon, C; Kowalski, M; Moore, KA; Stoker, DG,
)
0.63
"A novel, rapid and selective ultra performance liquid chromatography mass spectrometric method had been developed for the pharmacokinetic study of diclofenac sodium (DS) after single intravenous injection of DS aqueous injection and DS lipid microsphere (LM) injection in rats."( A new rapid ultra-performance liquid chromatography method for the pharmacokinetic and bioavailability study of diclofenac sodium aqueous injection and lipid microsphere injection in rats.
Cui, Y; Guan, TT; Lin, X; Tang, X; Zhang, Y, 2010
)
0.77
"The aim of this study was to characterize the effects of food intake on the pharmacokinetic (PK) profile of oral DPSGC at doses of 25 and 50 mg."( Effects of food intake on the pharmacokinetics of diclofenac potassium soft gelatin capsules: a single-dose, randomized, two-way crossover study.
Moore, KA; Scallion, R, 2009
)
0.61
" Therefore, in view of the vast clinical uses and interactions of NSAIDs with commonly used therapeutic agents, the interaction of the NSAID diclofenac and glibenclamide was investigated about pharmacokinetic profile and antinociceptive effect in rats."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.88
" In pharmacokinetic interaction study, no significant (P>0."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.68
" Likewise, the validated assay had sufficient accuracy and precision for pharmacokinetic determination of diclofenac in the rat."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.89
"To compare the pharmacokinetic profiles of diclofenac potassium liquid-filled soft gelatin capsules (DPSGC) using patented ProSorb dispersion technology with an immediate-release, diclofenac potassium 50-mg comparator tablet in two open-label, single-dose, randomized, crossover relative bioavailability studies in healthy volunteers."( Pharmacokinetic comparison of an oral diclofenac potassium liquid-filled soft gelatin capsule with a diclofenac potassium tablet.
Lissy, M; Moore, K; Scallion, R; Stiff, DD, 2010
)
0.89
" A pharmacokinetic meta-analysis has been undertaken with the aim of recommending a dose for children aged 1-12 years."( Diclofenac pharmacokinetic meta-analysis and dose recommendations for surgical pain in children aged 1-12 years.
Korpela, R; Olkkola, KT; Standing, JF; Tibboel, D, 2011
)
1.81
"Studies containing diclofenac pharmacokinetic data were identified during a Cochrane systematic review, and authors were asked to provide raw data."( Diclofenac pharmacokinetic meta-analysis and dose recommendations for surgical pain in children aged 1-12 years.
Korpela, R; Olkkola, KT; Standing, JF; Tibboel, D, 2011
)
2.14
"As a consequence of a continuous demand for increased throughput of pharmacokinetic (PK) studies, industries have introduced strategies to reduce the number of samples such as cassette analysis (pooling of samples after the in-life phase)."( High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC-MS/MS.
Betnér, I; Briem, S; Bueters, T; Dahlström, J; Kvalvågnaes, K, 2011
)
0.37
" Also, this assay was applied to determine the pharmacokinetic parameters of diclofenac in healthy Turkish volunteers who had been given 50 mg diclofenac."( HPLC method for determination of diclofenac in human plasma and its application to a pharmacokinetic study in Turkey.
Asci, A; Palabiyik, SS; Yilmaz, B, 2011
)
0.88
" Oral and topical diclofenac had no pharmacokinetic effects on furosemide."( Randomized, open-label, 5-way crossover study to evaluate the pharmacokinetic/pharmacodynamic interaction between furosemide and the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen in healthy volunteers.
Jacobs, D; McGuinness, N; Paterson, CA; Rasmussen, S; Youngberg, SP, 2011
)
0.9
" Furosemide also affected plasma and urine pharmacokinetic profiles."( Randomized, open-label, 5-way crossover study to evaluate the pharmacokinetic/pharmacodynamic interaction between furosemide and the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen in healthy volunteers.
Jacobs, D; McGuinness, N; Paterson, CA; Rasmussen, S; Youngberg, SP, 2011
)
0.56
" In the case of diclofenak treatment without vitamins Cmax corresponds to 1137."( [The influence of vitamin B group on monooxygenase activity of cytochrome P450 3A4: pharmacokinetics and electro analysis of catalytic properties].
Archakov, AI; Bylko, TV; Kukes, VG; Makhova, AA; Ramenskaia, GV; Shikh, EV; Shumiantseva, VV; Sizova, OS; Usanov, SA,
)
0.13
"The present study was designed as an open label, multiple-dose, randomized, parallel trial to evaluate the pharmacodynamic drug-drug interaction of lisinopril and concomitantly administered diclofenac sodium in non-diabetic and diabetic, mild to moderate hypertensive, osteoarthritic patients."( Potential pharmacodynamic drug-drug interaction between concomitantly administered lisinopril and diclofenac sodium: a call for appropriate management in hypertensive osteoarthritic patients.
Chudasama, H; Goswami, SK; Jain, S; Santani, D, 2011
)
0.78
" The applicability of this method for pharmacokinetic studies has been established after successful application during a 12-subject bioavailabity study."( A high performance liquid chromatography-tandem mass spectrometric method for the determination of mefenamic acid in human plasma: application to pharmacokinetic study.
Bhavsar, R; Dhaneshwar, S; Mahadik, M, 2012
)
0.38
" This phase 1 clinical trial characterizes the pharmacokinetic (PK) profile of an investigational, proprietary, nano-formulated, lower-dose oral diclofenac (nano-formulated diclofenac) compared with oral diclofenac in healthy subjects."( The pharmacokinetic parameters of a single dose of a novel nano-formulated, lower-dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012
)
0.8
" The maximum measured plasma concentration (Cmax), time to maximum measured concentration (Tmax), terminal elimination half-life (T1/2), and area under the concentration time curve (AUC), along with safety and tolerability, were assessed."( The pharmacokinetic parameters of a single dose of a novel nano-formulated, lower-dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012
)
0.6
"Mean (± standard deviation) Tmax for nano-formulated diclofenac 18 (0."( The pharmacokinetic parameters of a single dose of a novel nano-formulated, lower-dose oral diclofenac.
Daniels, S; Gibofsky, A; Manvelian, G, 2012
)
0.85
"2 mg kg(-1) of diclofenac sodium either intravenously or orally, diclofenac concentration was measured in whole blood samples and pharmacokinetic parameters were estimated."( Contrasting effects of cord injury on intravenous and oral pharmacokinetics of diclofenac: a drug with intermediate hepatic extraction.
Arauz, J; Castañeda-Hernández, G; Cruz-Antonio, L; Franco-Bourland, RE; Guízar-Sahagún, G, 2012
)
0.96
"Acute SCI induces significant pharmacokinetic changes for diclofenac, a marker drug with intermediate hepatic extraction."( Contrasting effects of cord injury on intravenous and oral pharmacokinetics of diclofenac: a drug with intermediate hepatic extraction.
Arauz, J; Castañeda-Hernández, G; Cruz-Antonio, L; Franco-Bourland, RE; Guízar-Sahagún, G, 2012
)
0.85
" Plasma phenytoin levels were assayed by HPLC and pharmacokinetic parameters were calculated."( Effect of aceclofenac on pharmacokinetic of phenytoin.
Attrey, SD; Bansal, YS; Joshi, R; Medhi, B; Pandhi, P; Prakash, A; Singh, D, 2012
)
0.38
"The present study was undertaken to compare the bioavailability and pharmacokinetic parameters of diclofenac sodium and diclofenac potassium in normal and experimentally induced diabetic state in 24 rabbits using a validated reversed phase HPLC method with a washout period of one week."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and alloxan-diabetic rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2012
)
0.84
" The development of NSAIDs having safer therapeutic profile depends on the better understanding of their mechanisms, physicochemical and pharmacokinetic properties."( Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach.
Kumar, M; Sinha, VR; Thareja, S, 2012
)
0.38
"One single-dose, randomized, three-way, crossover relative bioavailability study and one linearity single escalating dose, randomized, three-way cross-over pharmacokinetic study were conducted at two different clinical sites."( Pharmacokinetics of a new diclofenac sodium formulation developed for subcutaneous and intramuscular administration.
Ducharme, MP; Gugliotta, B; Müller, M; Oraha, AZ; Rusca, A; Zeitlinger, M, 2012
)
0.68
" with respect to Cmax and AUC."( Pharmacokinetics of a new diclofenac sodium formulation developed for subcutaneous and intramuscular administration.
Ducharme, MP; Gugliotta, B; Müller, M; Oraha, AZ; Rusca, A; Zeitlinger, M, 2012
)
0.68
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"Similar pharmacokinetic behavior of diclofenac was found both in normal and FCA-induced arthritic rats."( Pharmacokinetic-pharmacodynamic modeling of diclofenac in normal and Freund's complete adjuvant-induced arthritic rats.
Guo, HF; Li, P; Liu, L; Liu, XD; Zhang, J, 2012
)
0.92
"Arthritis induced by FCA does not alter the pharmacokinetic behaviors of diclofenac in rats, but the pharmacodynamics of diclofenac is slightly affected."( Pharmacokinetic-pharmacodynamic modeling of diclofenac in normal and Freund's complete adjuvant-induced arthritic rats.
Guo, HF; Li, P; Liu, L; Liu, XD; Zhang, J, 2012
)
0.87
" Our pharmacokinetic studies of 7e demonstrated this prodrug is a potential candidate for a slower and sustained release form of rhein."( Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies.
Cai, J; Chao, M; Chen, J; Duan, Y; Ji, M; Yu, J, 2012
)
0.38
" Preliminary pharmacokinetic studies have shown in vivo bioconversion of prodrug to diclofenac."( Pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effect.
Barbieri, KP; Bosquesi, PL; Campos, ML; Chelucci, RC; Chin, CM; de Castro Souto, PC; Matsubara, MH; Moreira, V; Peccinini, RG; Santos, JL; Teixeira, C, 2012
)
0.83
" The vesicles were characterized for physicochemical properties, ex vivo permeation using human skin and pharmacokinetic parameters and anti-inflammatory activity in rats."( Ceramide-2 nanovesicles for effective transdermal delivery: development, characterization and pharmacokinetic evaluation.
Bhandari, A; Gaur, PK; Kumar, Y; Mishra, S; Purohit, S, 2014
)
0.4
"To investigate the herb-drug pharmacokinetic interaction of artificial calculus bovis (ACB) with diclofenac sodium (DS) and chlorpheniramine maleate (CPM) in rats."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.84
" The proposed method was successfully applied to compare the herb-drug pharmacokinetic interaction of ACB with DS and CPM in rats following intragastric administration."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.62
" There was no apparent pharmacokinetic interaction between DS and CPM."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.62
"This study indicated that co-administration of ACB with DS and CPM can result in an apparent herb-drug pharmacokinetic interaction in rats."( Herb-drug pharmacokinetic interaction of artificial calculus bovis with diclofenac sodium and chlorpheniramine maleate in rats.
Huang, Y; Lv, M; Peng, C; Tian, J; Tian, Y; Zhang, Z, 2013
)
0.62
" Study 2: Cmax for diclofenac was 2904 and 6031 ng/ml after the first IV dose of 18."( Single-dose and multiple-dose pharmacokinetics and dose proportionality of intravenous and intramuscular HPβCD-diclofenac (Dyloject) compared with other diclofenac formulations.
Carr, DB; Hamilton, DA; Lacouture, PG; Mermelstein, F; Ramaiya, A; Wright, C, 2013
)
0.93
"  Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h."( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics.
Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014
)
0.61
" The aim of this work was to compare the pharmacokinetic profiles of diclofenac from DICCIC (7."( Pharmacokinetic profile of a new diclofenac prodrug without gastroulcerogenic effect.
Baldan-Cimatti, HM; Candido, CD; Davanco, MG; de Campos, ML; Dos Santos, JL; Nogueira, MA; Padilha, EC; Peccinini, RG, 2012
)
0.89
" Although eperisone hydrochloride and aceclofenac are frequently coadministered, no published studies have reported on the pharmacokinetic interactions between these 2 drugs."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.39
"The aim of this study was to investigate any pharmacokinetic interactions between eperisone hydrochloride and aceclofenac in healthy Korean men."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.39
" Pharmacokinetic analyses were conducted using noncompartmental methods."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.39
"No clinically significant pharmacokinetic differences exist between 150 mg eperisone hydrochloride and 200 mg aceclofenac when administrated as a monotherapy or in combination."( Pharmacokinetic interactions between eperisone hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men.
Bae, KS; Choi, HY; Kim, MJ; Kim, SE; Kim, YH; Lim, HS; Noh, YH; Park, KM, 2013
)
0.39
" Pharmacokinetic parameters of moxifloxacin were determined in rats following oral administration to rats in the presence and absence of diclofenac."( Effect of diclofenac on the pharmacokinetics of moxifloxacin in rats.
Chen, L; Guo, S; Wu, LX; Xu, M; Zhang, JH, 2014
)
1.01
" In this study, we investigated the pharmacokinetic drug interactions of rebamipide with two selected NSAIDs, celecoxib or diclofenac."( Pharmacokinetic interactions between rebamipide and selected nonsteroidal anti-inflammatory drugs in rats.
Cooper, DL; Harirforoosh, S; Wood, RC; Wyatt, JE, 2014
)
0.61
" The Cmax was comparable after SC administration in the quadriceps or abdomen, and ~ 17% higher in the gluteus."( Pharmacokinetics of a new subcutaneous diclofenac formulation administered to three body sites: quadriceps, gluteus, and abdomen.
Cardì, F; Drago, F; Gugliotta, B; Piazza, C; Salomone, S; Vitale, DC, 2014
)
0.67
"The objective of this research was to characterize the dissolution profile of a poorly soluble drug, diclofenac, from a commercially available multiple-unit enteric coated dosage form, Diclo-Puren® capsules, and to develop a predictive model for its oral pharmacokinetic profile."( Predicting the oral pharmacokinetic profiles of multiple-unit (pellet) dosage forms using a modeling and simulation approach coupled with biorelevant dissolution testing: case example diclofenac sodium.
Blume, H; Dressman, JB; Kambayashi, A, 2014
)
0.81
"This study compared the pharmacokinetic properties and safety profile of low-dose (18- and 35-mg) diclofenac capsules manufactured using SoluMatrix Fine Particle Technology (Trademark of iCeutica Inc."( Pharmacokinetic properties and tolerability of low-dose SoluMatrix diclofenac.
Desjardins, PJ; Olugemo, K; Solorio, D; Young, CL, 2015
)
0.87
" Pharmacokinetic parameters (T(max), C(max), AUC(0-t), AUC(0-∞)) were calculated from the concentrations of diclofenac in the plasma."( Pharmacokinetic properties and tolerability of low-dose SoluMatrix diclofenac.
Desjardins, PJ; Olugemo, K; Solorio, D; Young, CL, 2015
)
0.87
"The pharmacokinetic properties of low-dose SoluMatrix diclofenac capsules in the healthy volunteers in this study suggest rapid diclofenac absorption as measured by T(max)."( Pharmacokinetic properties and tolerability of low-dose SoluMatrix diclofenac.
Desjardins, PJ; Olugemo, K; Solorio, D; Young, CL, 2015
)
0.9
" Blood samples for pharmacokinetic analysis were taken for up to 12 hours post-dose and analyzed for diclofenac concentrations."( Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.
Bujanover, S; Chen, C; Kareht, S; Rapoport, AM, 2015
)
0.91
"When taken under fed conditions, the oral solution resulted in an approximately 80% faster median tmax (0."( Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.
Bujanover, S; Chen, C; Kareht, S; Rapoport, AM, 2015
)
0.7
"When taken under fed conditions, the oral solution resulted in a similar median tmax (0."( Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.
Bujanover, S; Chen, C; Kareht, S; Rapoport, AM, 2015
)
0.7
"Diclofenac potassium oral solution and tablet formulations produced statistically significantly different Cmax and tmax but similar AUC under fed and fasting conditions."( Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.
Bujanover, S; Chen, C; Kareht, S; Rapoport, AM, 2015
)
2.14
"In a randomized, parallel-group, single-center study in 42 healthy adults, the safety and pharmacokinetic parameters of an intravenous formulation of 18."( Safety and pharmacokinetics of single and multiple intravenous bolus doses of diclofenac sodium compared with oral diclofenac potassium 50 mg: A randomized, parallel-group, single-center study in healthy subjects.
Allenby, K; Gautam, A; McDowell, J; Munjal, S; Okumu, F, 2016
)
0.66
"The pharmacokinetic study of a diclofenac sodium capsule filled with enteric-coated pellets (abbreviated as CAPSULE) in healthy Chinese subjects was evaluated using liquid chromatography-electrospray ionization-tandem mass spectrometry with simple sample preparation."( Pharmacokinetic Study of a Diclofenac Sodium Capsule Filled with Enteric-coated Pellets in Healthy Chinese Volunteers by Liquid Chromatography-electrospray Ionization-tandem Mass Spectrometry.
Deng, M; Liu, H; Liu, M; Ma, JY; Tong, Y; Yang, M; Zhang, Y; Zhao, H, 2016
)
1.02
"Non-compartmental pharmacokinetic analysis of diclofenac sodium (DIC) and papaverine hydrochloride (PAP) after oral administration of composed tablets to rabbits was developed."( PHARMACOKINETICS OF DICLOFENAC SODIUM AND PAPAVERINE HYDROCHLORIDE AFTER ORAL ADMINISTRATION OF TABLETS TO RABBITS.
Jawień, W; Kasperek, R; Poleszak, E; Zimmer, Ł,
)
0.71
" In the pyridine series, compound 7a was found to be a highly potent and selective EP4 antagonist, with suitable rat and dog pharmacokinetic profiles."( Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.
Blanco, MJ; Chambers, M; Chandrasekhar, S; Fisher, MJ; Harvey, A; Lin, C; Mudra, D; Oskins, J; Vetman, T; Wang, XS; Warshawsky, AM; Yu, XP, 2016
)
0.43
" Comparing pharmacokinetic data with MRI data it was observed that maximal blood levels occurred before the solvent and the dispersion agent were removed from the muscle tissue."( Simultaneous magnetic resonance imaging and pharmacokinetic analysis of intramuscular depots.
Evert, K; Hadlich, S; Kühn, JP; Oswald, S; Probst, M; Scheuch, E; Seidlitz, A; Siegmund, W; Weitschies, W, 2016
)
0.43
" The concentration-time and drug release curves were drawn, and T max (min), C max (μg·mL(-1)), AUC0→∞ , and MRT were compared using a pharmacokinetic systems program."( Preparation and In Vivo Pharmacokinetics of the Tongshu Suppository.
Dong, L; Liu, G; Liu, S; Lu, K; Zheng, Y, 2016
)
0.43
"This study was conducted with the aim to determine the pharmacokinetic and bioequivalence of diclofenac potassium 50 mg test (F4) tablet formulation with reference product (Caflam)."( Pharmacokinetic and bioequivalence studies of immediate release diclofenac potassium tablets (50mg) in healthy volunteers.
Ali, H; Bushra, R; Hanif, M; Khursheed, R; Naz, A; Shoaib, MH; Zafar, F, 2016
)
0.89
"Coadministration of diclofenac and sunitinib, tyrosine kinase inhibitor, led to sex-divergent pharmacokinetic drug-drug interaction outcomes."( Diclofenac sex-divergent drug-drug interaction with Sunitinib: pharmacokinetics and tissue distribution in male and female mice.
Chee, EL; Chee, YL; Chew, CC; Fernández, C; Koo, TW; Liew, MH; Mariño, EL; Modamio, P; Ng, S; Segarra, I, 2017
)
2.22
"The knowledge of pharmacokinetic and pharmacodynamic properties of antiepileptic drugs is helpful in optimizing drug therapy for epilepsy."( Evaluation of Brain Pharmacokinetic and Neuropharmacodynamic Attributes of an Antiepileptic Drug, Lacosamide, in Hepatic and Renal Impairment: Preclinical Evidence.
Kumar, B; Medhi, B; Modi, M; Saikia, B, 2017
)
0.46
"The accuracy of physiologically based pharmacokinetic (PBPK) model prediction in children, especially those younger than 2 years old, has not been systematically evaluated."( Predictive Performance of Physiologically Based Pharmacokinetic (PBPK) Modeling of Drugs Extensively Metabolized by Major Cytochrome P450s in Children.
Al-Huniti, N; Bui, KH; Cheung, SYA; Johnson, TN; Li, J; Xu, H; Zhou, D; Zhou, W, 2018
)
0.48
" The prostate tissue penetration and related pharmacokinetic parameters were evaluated by non-compartmental analysis."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018
)
0.48
" A two-factor analysis of variance (ANOVA) with replication indicated an overall statistically significant difference in the pharmacokinetic parameters for celecoxib, diclofenac, ibuprofen, and naproxen."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018
)
0.68
" The pharmacokinetic data indicated that celecoxib has the highest penetration and retention in rat prostate tissues."( Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.
Radhakrishnan, J; Radhakrishnan, R; Yellepeddi, VK, 2018
)
0.48
" This work describes the optimization of the pharmacokinetic properties of a previously published family of triazine lead compounds."( Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
Augustyns, K; Baán, A; Caljon, G; Kiekens, F; Maes, L; Matheeussen, A; Salado, IG; Van der Veken, P; Verdeyen, T, 2018
)
0.48
"To develop a simple HPLC-DAD method for simultaneous determination of febuxostat (FEB) and diclofenac (DIC) in biological samples to assess pharmacokinetic outcomes of their coadministration."( A novel HPLC-DAD method for simultaneous determination of febuxostat and diclofenac in biological samples: pharmacokinetic outcomes.
Amin, OA; El-Kimary, EI; El-Yazbi, AF; El-Yazbi, FA; Elkhatib, MA; Khamis, EF; Younis, SE, 2019
)
0.97
" The pharmacokinetic parameters were calculated by non-compartmental analysis with DAS2."( Pharmacokinetics of diclofenac sodium injection in swine.
Bu, SJ; Huang, C; Huang, LX; Li, YJ; Li, YY; Yang, HF, 2019
)
0.84
" In the quest for a suitable combination with improved therapeutic efficacy and better tolerability, pharmacodynamic and pharmacokinetic interaction studies were performed for diclofenac with or without IS01957 in mice model."( Effect of IS01957, a para-coumaric acid derivative on pharmacokinetic modulation of diclofenac through oral route for augmented efficacy.
Abdullah, ST; Bhatt, S; Dogra, A; Gour, A; Koul, S; Malik, TA; Nandi, U; Rath, SK; Sangwan, PL; Sharma, A; Singh, G, 2019
)
0.93
" Values for total clearance of compounds from plasma should be one of the most important pharmacokinetic parameters for predictions."( Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data.
Ito, S; Iwamoto, K; Kamimura, H; Mizunaga, M; Nakayama, K; Negoro, T; Nishiwaki, M; Nomura, Y; Suemizu, H; Yamazaki, H; Yoneda, N, 2020
)
0.56
" Diclofenac had a half-life of 66."( An Open-Label Study Evaluating the Pharmacokinetics and Safety of Diclofenac Potassium for Oral Solution for the Acute Treatment of MWA or MWoA in Pediatric Participants.
Amend, DL; Ferger, SM; Hogan, RM; McVige, JW; Shanahan, CM, 2020
)
1.71
"Diclofenac potassium for OS exhibited a favorable pharmacokinetic and safety profile in 12- to 17-year-old patients with a diagnosis of episodic MWA or MWoA."( An Open-Label Study Evaluating the Pharmacokinetics and Safety of Diclofenac Potassium for Oral Solution for the Acute Treatment of MWA or MWoA in Pediatric Participants.
Amend, DL; Ferger, SM; Hogan, RM; McVige, JW; Shanahan, CM, 2020
)
2.24
"The aim of the study was to determine the various pharmacokinetic parameters of the newly developed cost-effective aceclofenac 100 mg tablet formulation (F-15) and to establish the bioequivalence against the marketed brand (ACEMED)."( Pharmacokinetics and bioequivalence assessment of optimized directly compressible Aceclofenac (100 mg) tablet formulation in healthy human subjects.
Ali, H; Bushra, R; Ghayas, S; Shoaib, MH, 2020
)
0.56
" Quantitative methods and modeling, such as physiologically-based pharmacokinetic (PBPK) modeling, can support alternative BE approaches with reduced or no human testing."( Physiologically-based pharmacokinetic modeling to support bioequivalence and approval of generic products: A case for diclofenac sodium topical gel, 1.
Babiskin, A; Tsakalozou, E; Zhao, L, 2021
)
0.83
" The aim of the present research was to investigate whether and how morin affect the pharmacokinetic profile of diclofenac sodium."( Effect and underlying mechanism of morin on the pharmacokinetics of diclofenac sodium in rats.
Dai, Y; Huang, D; Shao, S; Wei, Z; Xia, Y; Zhang, J, 2021
)
1.07
" The aim of this study was to evaluate the pharmacokinetic interaction between tegoprazan and commonly used NSAIDS, namely, naproxen, aceclofenac, and celecoxib."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022
)
0.72
" Pharmacokinetic blood samples were collected up to 24 hours after the last dose."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022
)
0.72
"Seventeen subjects from cohort 1, sixteen subjects from cohort 2, and thirteen subjects from cohort 3 were included in the pharmacokinetic analysis."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022
)
0.72
"Changes in the maximum aceclofenac or celecoxib concentrations were detected after concurrent administration with tegoprazan, which were considered mainly due to the pharmacodynamic effect of tegoprazan."( Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects.
Kang, M; Kim, B; Kim, MG; Moon, SJ; Shin, N, 2022
)
0.72
" The proteomics-informed physiologically-based pharmacokinetic (PBPK) model explains the reported higher exposure of diclofenac in women consistent with ~ 3-fold lower expression of UGT2B17."( Intestinal Metabolism of Diclofenac by Polymorphic UGT2B17 Correlates with its Highly Variable Pharmacokinetics and Safety across Populations.
Ahire, D; Heyward, S; Prasad, B, 2023
)
1.42
" Following the successful application of this improved technique to plasma samples, the pharmacokinetic characteristics of each selected drug were evaluated using (UPLC) with UV detection at 210 nm."( Green UPLC method for estimation of ciprofloxacin, diclofenac sodium, and ibuprofen with application to pharmacokinetic study of human samples.
Ahmed-Anwar, AA; Farghali, AA; Hassouna, MEM; Mahmoud, R; Mohamed, MA, 2023
)
1.16

Compound-Compound Interactions

Diclofenac prescriptions increased the risk for hospitalisation due to peptic ulcer significantly. In vitro enzyme kinetic data were used to predict the in vivo clearance and drug-drug interaction potential of four well known CYP2C9 substrates (tolbutamide, fluvastatin, ibuprofen)

ExcerptReferenceRelevance
"Seventy-five mg diclofenac sodium were given intramuscularly to 15 subjects alone and in combination with 40 mg triamcinolone acetate."( Pharmacokinetics of diclofenac sodium after intramuscular administration in combination with triamcinolone acetate.
Barth, J; Derendorf, H; Grüner, A; Möllmann, H; Mullersman, G, 1986
)
0.94
"Angiostasis and vascular regression in chronic granulomatous inflammation was assessed in mice induced with diclofenac in combination with hyaluronan."( Angiostasis and vascular regression in chronic granulomatous inflammation induced by diclofenac in combination with hyaluronan in mice.
Alam, CA; Seed, MP; Willoughby, DA, 1995
)
0.73
"To determine the mode of protective effects of misoprostol against the chronic gastrointestinal ulceration from the NSAID, diclofenac, studies were undertaken in domestic pigs, a model of human gastrointestinal ulceration, to determine (1) the effects of repeated daily dosing for 10 days of diclofenac 5 mg/kg/day twice a day (as Voltaren tablets) on the gastrointestinal morphology, 59fe-red blood loss, mucosal myeloperoxidase (MPO) activity (as an indicator of leukocyte infiltration), and mucosal leukotrienes (LTS); and (2) the mucosal protective effects of 10-40 micrograms/kg/day misoprostol twice a day (as Cytotec tablets) given with diclofenac 5 mg/kg/day twice a day compared with diclofenac 5 mg/kg/day alone and aspirin 150 mg/kg/twice a day (USP tablets) as a standard."( Chronic effects of misoprostol in combination with the NSAID, diclofenac, on gastrointestinal tract of pigs. Relation to diarrheagenic activity, leukocyte infiltration, and mucosal leukotrienes.
Perkins, WE; Rainsford, KD; Stetsko, PI, 1995
)
0.74
" The results of this study indicated that there was minimal drug-drug interaction between diclofenac and ranitidine."( Application of dual radiotelemetric technique in studying drug-drug interaction between diclofenac sodium and ranitidine HCl in volunteers.
Alioth, C; Blum, RA; Chan, KK; D'Andrea, DT; Kochak, GM; Schentag, JJ; Teng, L; Ziehmer, BA, 1993
)
0.73
"Twenty patients with severe, treatment refractory RA were sequentially treated with stable doses of diclofenac (100-200 mg/day) for one month followed by diclofenac combined with cyclosporine (3 mg/kg/day) for one month."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
1.95
"Diclofenac can be safely combined with cyclosporine in the management of RA when appropriate clinical monitoring and dose titrations are performed."( Diclofenac combined with cyclosporine in treatment refractory rheumatoid arthritis: longitudinal safety assessment and evidence of a pharmacokinetic/dynamic interaction.
Alten, R; Genth-Stolzenburg, S; Guerret, M; Kovarik, JM; Kurki, P; Markert, E; Mueller, E; Zeidler, H, 1996
)
3.18
" During endotoxin shock, this drug combination efficiently counteracts pulmonary hypertension and improves cardiac performance and splenic and renal blood flow."( The endothelin receptor antagonist, bosentan, in combination with the cyclooxygenase inhibitor, diclofenac, counteracts pulmonary hypertension in porcine endotoxin shock.
Hemsén, A; Lundberg, JM; Rudehill, A; Wanecek, M; Weitzberg, E, 1997
)
0.52
" We evaluated the quality of analgesia and the incidence of side effects with smaller doses of intrathecal morphine combined with intramuscular (i."( Small doses of intrathecal morphine combined with systemic diclofenac for postoperative pain control after cesarean delivery.
Amaro, AR; Cappelli, EL; Cardoso, MM; Carvalho, JC; Prado, AA, 1998
)
0.54
"The effects of half-sized secretory leukocyte protease inhibitor or diclofenac sodium administered alone or in combination with the benzoxazinorifamycin KRM-1648 on the therapeutic efficacy of KRM-1648 against Mycobacterium avium complex (MAC) in mice were studied."( Therapeutic effects of benzoxazinorifamycin KRM-1648 administered alone or in combination with a half-sized secretory leukocyte protease inhibitor or the nonsteroidal anti-inflammatory drug diclofenac sodium against Mycobacterium avium complex infection i
Kawahara, S; Kawauchi, H; Sano, C; Sato, K; Shimizu, T; Tomioka, H, 1999
)
0.73
"The effects of diclofenac sodium(DFNa) combined with dionine in cases with fibrin exudation membrane on intraocular lens (IOL) were studied."( [Effects of diclofenac sodium combined with dionine in cases with fibrinous membrane after intraocular lens implantation].
Jia, SB; Tang, LS, 2001
)
1.04
"Thirty-two eyes, derived from sixteen adult pure bred New Zealand rabbits, were divided at random into two groups after extracapsular lens extraction with posterior chamber IOL implantation: (1) rabbits received DFNa eyedrops combined with dionine eyedrops; (2) rabbits received Pred forte eyedrops."( [Effects of diclofenac sodium combined with dionine in cases with fibrinous membrane after intraocular lens implantation].
Jia, SB; Tang, LS, 2001
)
0.69
"DFNa combined with dionine is effective in treating fibrin exudation membrane after extracapsular lens extraction and IOL implantation, and it is more effective than the pred forte."( [Effects of diclofenac sodium combined with dionine in cases with fibrinous membrane after intraocular lens implantation].
Jia, SB; Tang, LS, 2001
)
0.69
" The plasma pharmacokinetics of melagatran, diclofenac, diazepam, N-desmethyl-diazepam and nifedipine were determined when administered alone and in combination with ximelagatran."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.58
"No inhibition, or only minor inhibition, of CYP enzymes by ximelagatran, the intermediates or melagatran was shown in the in vitro studies, suggesting that ximelagatran would not cause CYP-mediated drug-drug interactions in vivo."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.32
" Together, the in vitro and in vivo studies indicate that metabolic drug-drug interactions involving the major human CYP enzymes should not be expected with ximelagatran."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.32
"To investigate the effects of diclofenac alone or when combined with alpha-tocopherol on the oxidative activity of polymorphonuclear leukocytes (PMNs) in healthy and osteoarthritic (OA) patients."( Effect of diclofenac alone or in combination with alpha-tocopherol on the oxidative activity of polymorphonuclear leukocytes in healthy and osteoarthritic individuals.
Al-Arfaj, AS; Al-Dalaan, AN; Al-Humayyd, MS; Al-Tuwaijri, AS; Alballa, SR; Mustafa, AA, 2004
)
1.01
" In osteoarthritic patients, diclofenac alone and when combined with alpha-tocopherol showed no significant change in CL response of whole blood."( Effect of diclofenac alone or in combination with alpha-tocopherol on the oxidative activity of polymorphonuclear leukocytes in healthy and osteoarthritic individuals.
Al-Arfaj, AS; Al-Dalaan, AN; Al-Humayyd, MS; Al-Tuwaijri, AS; Alballa, SR; Mustafa, AA, 2004
)
1.02
"The effect of diclofenac alone or in combination with alpha-tocopherol did not produce a consistent effect on the CL response of whole blood or isolated PMNs of healthy or osteoarthritic patients."( Effect of diclofenac alone or in combination with alpha-tocopherol on the oxidative activity of polymorphonuclear leukocytes in healthy and osteoarthritic individuals.
Al-Arfaj, AS; Al-Dalaan, AN; Al-Humayyd, MS; Al-Tuwaijri, AS; Alballa, SR; Mustafa, AA, 2004
)
1.09
" In the present study, in vitro enzyme kinetic data were used to predict the in vivo clearance and drug-drug interaction potential of four well known CYP2C9 substrates (tolbutamide, fluvastatin, ibuprofen and diclofenac) that are frequently used as benchmark substances in screening programs."( An evaluation of the in vitro metabolism data for predicting the clearance and drug-drug interaction potential of CYP2C9 substrates.
Andersson, TB; Bredberg, E; Ericsson, H; Sjöberg, H, 2004
)
0.51
"A technique using a fully automated on-line solid phase extraction (SPE) system (Symbiosis, Spark Holland) combined with liquid chromatography (LC)-mass spectrometry (MS/MS) has been investigated for fast bioanalytical method development, method validation and sample analysis using both conventional C18 and monolithic columns."( Development and application of a new on-line SPE system combined with LC-MS/MS detection for high throughput direct analysis of pharmaceutical compounds in plasma.
Alnouti, Y; Bi, H; Gusev, AI; Kavetskaia, O; Srinivasan, K; Waddell, D, 2005
)
0.33
" The present prospective, placebo-controlled and double-blind study aimed to evaluate the analgesic efficacy of diclofenac, a non-steroid anti-inflammatory drug (NSAID), in combination with paracetamol and opioids."( Analgesic efficacy of diclofenac in combination with morphine and paracetamol after mastectomy and immediate breast reconstruction.
Legeby, M; Olofsson, C; Sandelin, K; Wickman, M, 2005
)
0.85
"To evaluate the preemptive effects of diclofenac sodium, in combination with remifentanil and ketamine."( The preemptive use of diclofenac sodium in combination with ketamine and remifentanil does not enhance postoperative analgesia after laparoscopic gynecological procedures.
Aypar, U; Canbay, O; Celebi, N; Coskun, F; Karakas, O; Peker, L, 2006
)
0.92
" We found that six of the eight potent inhibitors identified in this screen (IC50 <10 microM against at least one CYP isozyme) correlated with significant drug-drug interactions in the clinic."( Drug-drug interactions of anti-infective drugs: utility of fluorescence cyp inhibition assays in drug discovery.
Fridén, M; Nandi, VN; Vanaja, K, 2006
)
0.33
"By developing a high-performance liquid chromatography (HPLC) method, we estimated the blood concentrations of diclofenac in human volunteers administered with the transdermal patches prepared with povidone-ethylcellulose and oral diclofenac tablets."( HPLC detection of plasma concentrations of diclofenac in human volunteers administered with povidone-ethylcellulose-based experimental transdermal matrix-type patches.
Das, S; Dey, S; Mahapatra, S; Mukherjee, B; Roy, G, 2006
)
0.81
"5% hyaluronic acid in combination with sunscreens."( 3% diclofenac in 2.5% hyaluronic acid (Solaraze) does not induce photosensitivity or phototoxicity alone or in combination with sunscreens.
Duteil, L; Ortonne, JP; Queille-Roussel, C,
)
0.75
" The aim of this study was to ascertain whether DCL used in combination with the first-line antitubercular antibiotic streptomycin (STM) synergistically augments its efficacy in vitro as well as in a murine tuberculosis infection model."( Activity of diclofenac used alone and in combination with streptomycin against Mycobacterium tuberculosis in mice.
Dastidar, SG; Dutta, NK; Mazumdar, K; Park, JH, 2007
)
0.72
"Inhibition of cytochrome P450 (CYP) is a principal mechanism for metabolism-based drug-drug interactions (DDIs)."( Development of an in vitro drug-drug interaction assay to simultaneously monitor five cytochrome P450 isoforms and performance assessment using drug library compounds.
Burdette, D; Dunklee, MB; Fahmi, O; Heinle, L; Hyland, R; Lee, C; Miller, H; Smith, D; Thurston, A; Zientek, M,
)
0.13
"5 mg combined with either aceclofenac 100 mg or placebo."( Almotriptan and its combination with aceclofenac for migraine attacks: a study of efficacy and the influence of auto-evaluated brush allodynia.
De Klippel, N; Giurgea, S; Herroelen, L; Jacquy, J; Louis, P; Monseu, G; Schoenen, J; Vandenheede, M, 2008
)
0.35
"A method for quantitative analysis of diclofenac sodium powder on the basis of near-infrared (NIR) spectroscopy is investigated by using of orthogonal projection to latent structures (O-PLS) combined with artificial neural network (ANN)."( Quantitative analysis of diclofenac sodium powder via near-infrared spectroscopy combined with artificial neural network.
Dou, Y; Liang, L; Liu, G; Ren, Y; Wang, B; Zhang, H, 2009
)
0.93
" CYP2C9*3 has been reported to reduce the metabolism of diclofenac and alter the extent of drug-drug interactions (DDIs)."( Effects of CYP2C9*3 and CYP2C9*13 on Diclofenac Metabolism and Inhibition-based Drug-Drug Interactions.
Chen, C; Huang, H; Liu, D; Ma, P; Wei, D; Yang, J; Zhu, J; Zi, J, 2010
)
0.88
"To observe the curative effect of Chinese drugs-paste separated moxibustion combined with electroacupuncture (EA) for knee osteoarthritis (KOA)."( [Clinical observation on the therapeutic effect of drugs-paste separated moxibustion combined with electroacupunture for knee osteoarthritis patients of cold-damp type].
Chen, RL; Ji, L; Miao, FR; Zhu, Y, 2010
)
0.36
" Chinese drugs-paste separated moxibustion was applied to Shenque (CV 8) for 9 moxa-cones, combined with EA (4 Hz/20 Hz, 1-2 mA) of Liangqiu (ST 34), Heding (EX-LE 2), Neixiyan (EX-LE 4), etc."( [Clinical observation on the therapeutic effect of drugs-paste separated moxibustion combined with electroacupunture for knee osteoarthritis patients of cold-damp type].
Chen, RL; Ji, L; Miao, FR; Zhu, Y, 2010
)
0.36
"Chinese drugs-paste-separated moxibustion combined with EA is effective in the treatment of KOA of cold-damp type."( [Clinical observation on the therapeutic effect of drugs-paste separated moxibustion combined with electroacupunture for knee osteoarthritis patients of cold-damp type].
Chen, RL; Ji, L; Miao, FR; Zhu, Y, 2010
)
0.36
"The present study was designed as an open label, multiple-dose, randomized, parallel trial to evaluate the pharmacodynamic drug-drug interaction of lisinopril and concomitantly administered diclofenac sodium in non-diabetic and diabetic, mild to moderate hypertensive, osteoarthritic patients."( Potential pharmacodynamic drug-drug interaction between concomitantly administered lisinopril and diclofenac sodium: a call for appropriate management in hypertensive osteoarthritic patients.
Chudasama, H; Goswami, SK; Jain, S; Santani, D, 2011
)
0.78
"Cryopreserved human hepatocytes suspended in human plasma (HHSHP) have previously provided accurate CYP3A drug-drug interaction (DDI) predictions from a single IC(50) that captures both reversible and time-dependent inhibition."( Predictions of cytochrome P450-mediated drug-drug interactions using cryopreserved human hepatocytes: comparison of plasma and protein-free media incubation conditions.
Hall, SD; Harrelson, JP; Mao, J; Mohutsky, MA; Wrighton, SA, 2012
)
0.38
"Inhibition of cytochrome P450-mediated drug metabolism by a concomitantly administered second drug is one of the major causes of drug-drug interactions in humans."( Drug-drug interactions and cooperative effects detected in electrochemically driven human cytochrome P450 3A4.
Di Nardo, G; Ferrero, S; Gilardi, G; Sadeghi, SJ, 2012
)
0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" The underlying mechanism for TL-118-treatment success was associated with hepatic perfusion attenuation resulting from reduced nitric-oxide (NO) serum levels as elucidated by using hemodynamic response imaging (HRI, a functional MRI combined with hypercapnia and hyperoxia)."( Improved efficacy of a novel anti-angiogenic drug combination (TL-118) against colorectal-cancer liver metastases; MRI monitoring in mice.
Abramovitch, R; Corchia, N; Edrei, Y; Gross, E, 2012
)
0.38
" TL-118, a novel drug combination has been recently developed to inhibit tumor angiogenesis."( TL-118 and gemcitabine drug combination display therapeutic efficacy in a MYCN amplified orthotopic neuroblastoma murine model--evaluation by MRI.
Abramovitch, R; Corchia, N; Dery, E; Fried, I; Gross, E; Komar-Stossel, C; Meir, K, 2014
)
0.4
"A simple solid phase microextraction method based on molecularly imprinted polymer sorbent in the hollow fiber (MIP-HF-SPME) combined with fiber optic-linear array spectrophotometer has been applied for the extraction and determination of diclofenac in environmental and biological samples."( Solid phase microextraction of diclofenac using molecularly imprinted polymer sorbent in hollow fiber combined with fiber optic-linear array spectrophotometry.
Dadfarnia, S; Khodadoust, S; Pebdani, AA; Shabani, AM, 2015
)
0.89
"A fast and low-cost sample preparation method of graphene based dispersive solid-phase extraction combined with gas chromatography-mass spectrometric (GC-MS) analysis, was developed."( Graphene oxide-based dispersive solid-phase extraction combined with in situ derivatization and gas chromatography-mass spectrometry for the determination of acidic pharmaceuticals in water.
Lee, HK; Li, SF; Naing, NN, 2015
)
0.42
"The aims of this study were to prepare fine intra-articular-administrated chitosan thermosensitive hydrogels combined with alginate microspheres and to investigate the possibility of those hydrogels as a drug delivery system for promoting the anti-inflammation effect."( Intra-articular Administration of Chitosan Thermosensitive In Situ Hydrogels Combined With Diclofenac Sodium-Loaded Alginate Microspheres.
Li, W; Luan, K; Qi, X; Qin, J; Qin, X; Song, L; Wu, Z; Yang, R, 2016
)
0.65
" The results indicated uniform trend to an increase in the number of clathrincoated vesicles under conditions of hormone treatment combined with prostaglandin synthesis blockade in animals with different neurohypophyseal status."( Electron Microscopic Study of the Inner Medulla in Rat Kidneys under Conditions of Vasopressin Treatment Combined with Prostaglandin Synthesis Blockade.
Babina, AV; Lavrinenko, VA, 2016
)
0.43
"Coadministration of diclofenac and sunitinib, tyrosine kinase inhibitor, led to sex-divergent pharmacokinetic drug-drug interaction outcomes."( Diclofenac sex-divergent drug-drug interaction with Sunitinib: pharmacokinetics and tissue distribution in male and female mice.
Chee, EL; Chee, YL; Chew, CC; Fernández, C; Koo, TW; Liew, MH; Mariño, EL; Modamio, P; Ng, S; Segarra, I, 2017
)
2.22
"Levocetirizine dihydrochloride is known to interact with some anti-inflammatory drugs."( In vitro drug interaction of levocetirizine and diclofenac: Theoretical and spectroscopic studies.
Abdel Gaber, SA; Abo Dena, AS, 2017
)
0.71
" This study was designed to find out whether there is an augmentation of the therapeutic effectiveness of the antiinflammatory drugs like diclofenac sodium (NSAID), prednisolone (steroid) and atorvastatin (statin) when used in combination with ascorbic acid (antioxidant)."( Evaluation of the Anti-Inflammatory Activities of Diclofenac Sodium, Prednisolone and Atorvastatin in Combination with Ascorbic Acid.
Ahmed, T; Ahsan, CR; Al Shoyaib, A; Archie, SR; Chowdhury, FA; Faruk, A, 2020
)
1.01
" The inhibitions of such responses were measured after administering a drug alone and in combination with ascorbic acid."( Evaluation of the Anti-Inflammatory Activities of Diclofenac Sodium, Prednisolone and Atorvastatin in Combination with Ascorbic Acid.
Ahmed, T; Ahsan, CR; Al Shoyaib, A; Archie, SR; Chowdhury, FA; Faruk, A, 2020
)
0.81
"Concomitant treatment with drugs that inhibit drug metabolising enzymes and/or transporters, such as commonly prescribed statins and nonsteroidal anti-inflammatory drugs (NSAIDs), has been associated with prolonged drug exposure and increased risk of adverse drug reactions (ADRs) due to drug-drug interactions."( Drug-drug-gene interactions as mediators of adverse drug reactions to diclofenac and statins: a case report and literature review.
Borić Bilušić, A; Božina, N; Božina, T; Domjanović, IK; Fistrek Prlić, M; Ganoci, L; Gvozdanović, K; Križ, T; Laganović, M; Simičević, L, 2021
)
0.86
"In this work, the novel hollow mesoporous coagulant was prepared by chitosan-polydopamine coating and permanganate loading into silica nanoparticles for investigating the simultaneous enrichment and degradation of diclofenac sodium (DCFS) combined with ultraviolet irradiation."( Permanganate release from silica-based hollow mesoporous coagulant combined with UV for spatiotemporal enrichment and degradation of diclofenac sodium.
An, Y; Hu, X; Khan, S; Qu, J; Sun, Q; Zhang, Z; Zheng, H, 2021
)
1.01
"To investigate the effects of different nonsteroidal anti-inflammatory drugs combined with platelet-rich plasma on inflammatory factor levels in patients with osteoarthritis."( Effects of Different Nonsteroidal Anti-Inflammatory Drugs Combined with Platelet-Rich Plasma on Inflammatory Factor Levels in Patients with Osteoarthritis.
Cheng, Y; Huang, Y; Jiang, W; Zhang, Y, 2022
)
0.72

Bioavailability

Sodium diclofenac (Na-DFC) and celecoxib (CLXB) are common nonsteroidal anti-inflammatory (NSAID) drugs which suffer from poor bioavailability and severe side effects when consumed orally. Their transdermal delivery might present important advices.

ExcerptReferenceRelevance
" Two independent studies have shown that aspirin markedly reduces the bioavailability of diclofenac, as measured by "area under the curve"."( Diclofenac sodium (Voltarol): drug interactions and special studies.
Fowler, PD, 1979
)
1.92
" The superiority of the regulated-dogs over the intact dogs was confirmed in comparative bioavailability studies by using two classes of commercial preparations."( Bioavailability study of commercial sustained-release preparations of diclofenac sodium in gastrointestinal physiology regulated-dogs.
Kawata, M; Mizuta, H; Nagamatsu, Y; Ogawa, K; Sagara, K; Yamada, I, 1992
)
0.52
" Pharmacokinetic and bioavailability studies of the combination product taken separately and together reveal a high between- and within-subject variability in plasma diclofenac levels, especially when the enteric-coated tablets were given after food; reliable values for peak plasma diclofenac concentration could not be ascertained."( Biopharmaceutical profile of diclofenac-misoprostol combination tablet, Arthrotec.
Karim, A; Smith, M, 1992
)
0.77
"The effect of food on the bioavailability of diclofenac from a 150 mg diclofenac hydrogel bead (HGB) capsule was evaluated in 12 healthy male subjects in a fed and fasted state."( Effect of food and relative bioavailability following single doses of diclofenac 150 mg hydrogel bead (HGB) capsules in healthy humans.
Castellana, J; Kochak, GM; Mangat, S; Thakker, KM; Wagner, W, 1992
)
0.78
" The relative bioavailability from the test formulation (a solution gel) in terms of Cmax and AUC, calculated from the amount of drug reaching the systemic circulation, was found to be twice the amount after application of reference product (an emulsion gel)."( Comparative pharmacokinetics and bioavailability study of percutaneous absorption of diclofenac from two topical formulations containing drug as a solution gel or as an emulsion gel.
Seth, BL, 1992
)
0.51
" For this purpose the bioavailability of both formulations, orally administered in single and multiple doses, was determined."( [Comparative bioavailability and pharmacokinetics of Dolotren retard and Dolotren].
Honorato, J; Lucero, ML; Montes, B; Suárez, J; Valiente, R,
)
0.13
" The bioavailability was determined according to the time (tmax) of the concentration maximum in plasma (Cmax) and the area under the curve (AUC)."( The influence of food on the absorption of diclofenac as a pure substance.
Feller, K; Gramatte, T; Hrdlcka, P; Richter, K; Terhaag, B, 1991
)
0.54
" The mean relative bioavailability was 116% for diclofenac plus sucralfate compared to diclofenac alone, and 100% for piroxicam plus sucralfate compared to piroxicam alone."( Study on the interaction between sucralfate and diclofenac/piroxicam in healthy volunteers.
Ungethüm, W, 1991
)
0.79
" After oral dosing, an early peak was also observed, but it was lower than that obtained after intraduodenal dosing: 71% diclofenac bioavailability was found in bile duct-cannulated rats intraduodenally dosed, whereas in normal animals dosed by mouth a bioavailability of 79% was obtained."( Pharmacokinetics and bioavailability of diclofenac in the rat.
Aristorena, JC; Garcia-Carbonell, MC; Peris-Ribera, JE; Pla-Delfina, JM; Torres-Molina, F, 1991
)
0.76
" The extent of bioavailability of ibuprofen was not increased by magnesium hydroxide."( The effect of magnesium hydroxide on the oral absorption of ibuprofen, ketoprofen and diclofenac.
Neuvonen, PJ, 1991
)
0.5
"A comparative bioavailability study and in vitro characterization were conducted on two commercial products of diclofenac sodium (Voltaren "A" and Inflaban "B") in the form of enteric-coated tablets (25 and 50 mg)."( Comparative bioavailability of two tablet formulations of diclofenac sodium in normal subjects.
Alawneh, Y; Hasan, MM; Najib, NM; Rawashdeh, NM; Sallam, EN; Shubair, MS, 1991
)
0.74
"A radiotelemetric technique with the Heidelberg capsule (HC) was used to improve the quality of data generated in a bioavailability study involving an enteric-coated (EC) formulation."( Application of radiotelemetric technique in evaluating diclofenac sodium absorption after oral administration of various dosage forms in healthy volunteers.
Chan, KK; John, VA; Mojaverian, P; Ziehmer, BA, 1990
)
0.53
"Diclofenac 100 mg suppository is well absorbed from the gastrointestinal tract of six human volunteers."( Pharmacokinetics of rectal diclofenac and its hydroxy metabolites in man.
Guelen, PJ; Janssen, TJ; Landsdorp, D; Vree, TB, 1990
)
2.02
"The bioavailability of an in vitro sustained-release formulation of diclofenac sodium was compared with a conventional product in six healthy male volunteers."( A study on the relative bioavailability of a sustained-release formulation of diclofenac sodium.
Abdulahameed, M; el-Sayed, Y; Hasan, M; Najib, N; Suleiman, MS, 1989
)
0.74
"A bioavailability study and an in vitro characterization were conducted on two brands of diclofenac sodium enteric-coated tablets marketed in Jordan."( Comparative bioavailability and in vitro characterization of two brands of diclofenac sodium enteric-coated tablets.
Abdulhameed, M; el-Sayed, Y; Hasan, M; Muti, H; Najib, N; Suleiman, MS, 1988
)
0.73
" The applicability of the assays to study the bioavailability of two formulations in a multiple-dosage trial is described."( Detection and quantification of non-steroidal anti-inflammatory agents by gas chromatography/mass spectrometry: diclofenac.
Aubets, J; Camí, J; de la Torre, R; Mestres, M; Segura, J; Ugena, B, 1988
)
0.49
"The bioavailability of diclofenac (D) was assessed in 12 healthy volunteers treated orally with single doses of 100 mg (retard formulation) and subsequently retreated with the same dose of (D) plus sulglicotide (S) 200 mg."( Lack of effect of a single-dose of sulglicotide on the bioavailability of diclofenac.
Bertè, F; Cenedese, A; Cornelli, U; De Bernardi di Valserra, M; Feletti, F; Nazzari, M, 1988
)
0.82
"The pharmacokinetics and relative bioavailability of diclofenac sodium from a new sustained-release formulation (Effekton-100) and from a standard sustained-release formulation (Voltaren-Retard) were compared in 11 healthy adult male volunteers."( Comparative pharmacokinetic analysis of a novel sustained-release dosage form of diclofenac sodium in healthy subjects.
Ben-David, J; Hussein, Z; Raz, I; Samara, E, 1988
)
0.75
" The bioavailability of these two preparations of diclofenac sodium did not differ significantly as judged by absorption lag time, peak plasma concentration, time to peak plasma concentrations or area under the plasma concentration-time curve."( Comparative bioavailability of two enteric-coated tablet preparations of diclofenac sodium.
Paton, DM, 1987
)
0.76
" An evaluation of the response-related pharmacokinetics of the three most widely used NSAIDs, diclofenac, indomethacin, and piroxicam, shows some obvious reasons for these differences: The onset of absorption and the bioavailability of diclofenac can vary considerably, and relevant inter-patient differences are found in the terminal plasma half-life of indomethacin and piroxicam."( Clinical relevance of nonsteroidal anti-inflammatory drug pharmacokinetics.
Brune, K, 1987
)
0.49
" An evaluation of the response-related pharmacokinetic parameters of the three presently most widely used NSAID's, namely diclofenac, indomethacin and piroxicam shows some obvious reasons: While the onset of absorption and the bioavailability of diclofenac varies considerably, we find relevant differences in the terminal plasma half-life of indomethacin and particularly piroxicam."( Pharmacokinetic factors as causes of variability in response to non-steroidal anti-inflammatory drugs.
Brune, K, 1985
)
0.48
"Five different preparations of diclofenac-suppositories (A, B, C, D, E) are investigated for in vitro liberation (modified paddle method) and for in vivo bioavailability in man (8-12 subjects) in a crossover design."( [In vitro and in vivo studies of diclofenac suppositories in humans].
le Petit, G; Richter, K; Rogner, M; Terhaag, B, 1985
)
0.84
"We carried out a comparative study of the bioavailability of a typical, enteric-coated diclofenac with regard to a new dispersible formulation whose faster dissolution results in an earlier onset of its analgesic effect."( Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks.
Carcas, AJ; Frias, J; Guerra, P; Lucero, ML; Macía, MA; Valiente, R, 1995
)
0.76
" The absorption rate from the intestinal tract into the portal system was determined using the portal-venous difference in plasma concentrations of diclofenac, considering 40% partitioning of diclofenac into erythrocytes."( Evaluation of intestinal absorption into the portal system in enterohepatic circulation by measuring the difference in portal-venous blood concentrations of diclofenac.
Fukuyama, T; Nakagawa, T; Tabata, K; Yamaoka, K, 1995
)
0.69
" Pharmacokinetic studies of the fixed combination have found that no drug-drug interaction occurs between misoprostol and diclofenac after either single or multiple doses, and the bioavailability of misoprostol and diclofenac are comparable with that of misoprostol and diclofenac given alone."( Efficacy and gastroduodenal safety of a fixed combination of diclofenac and misoprostol in the treatment of arthritis.
McKenna, F, 1995
)
0.74
" This results in an increase in the rate of absorption of the active compound and, consequently, in an earlier onset of analgesic action."( Piroxicam-beta-cyclodextrin in the treatment of acute pain of rheumatic disease.
Franchimont, P; Reginster, JY, 1993
)
0.29
"The relative bioavailability of four monolithic enteric coated (MEC) diclofenac products was compared in 16 healthy volunteers."( The bioavailability of diclofenac from enteric coated products in healthy volunteers with normal and artificially decreased gastric acidity.
Barends, DM; Meulenbelt, J; Olling, M; Rauws, AG; Salomons, P; Van Gelderen, ME, 1994
)
0.83
" The in-vivo data suggest a reduction of diclofenac bioavailability when colestipol or cholestyramine is administered concomitantly."( The effects of cholestyramine and colestipol on the absorption of diclofenac in man.
al-Balla, SR; al-Meshal, MA; el-Sayed, YM; Gouda, MW, 1994
)
0.79
"Relative bioavailability of enteric-coated diclofenac (CAS 15307-86-5) was investigated after a single-dose administration of a multiple-unit formulation (Diclo-Puren 50, test) in comparison to a single-unit formulation (reference)."( [The bioavailability of enteric coated diclofenac formulations. 2. Bioavailability following single administration of a multiple-unit formulation in comparison to a single-unit formulation under fasting and non-fasting conditions].
Babej-Dölle, RM; Blume, H; Scheidel, B; Stanislaus, F; Walter, K, 1994
)
0.82
" The absolute bioavailability after oral administration of 50 mL buffer, 50 mL water, and 200 mL water solutions were 107, 97, and 109%, respectively, compared to approximately 50% in man."( Pharmacokinetics and metabolism of diclofenac sodium in Yucatan miniature pigs.
Chan, KK; Das, H; Oberle, RL; Sawchuk, RJ; Wong, SL, 1994
)
0.57
"The bioavailability of two suspension formulations of potassium diclofenac (Flogan, Merck and Cataflam, Ciba-Geigy) were compared in eighteen healthy male volunteers who received a single dose of 7 ml of each suspension (equivalent to 105 mg of potassium diclofenac) in an open randomized two period crossover design, with a fourteen-day washout period between doses."( Comparative bioavailability of two suspension formulations of potassium diclofenac in healthy male volunteers.
de Nucci, G; Fernandes, AG; Franco, LM; Mendes, GB; Moreno, RA; Muscara, MN, 1994
)
0.76
"A single dose comparative bioavailability study and an in vitro evaluation were conducted on two sustained-release formulations of diclofenac sodium (Voltaren "V" and Diclogesic "D")."( A comparative bioavailability study on two sustained-release formulations of diclofenac sodium following a single dose administration.
Hasan, MM; Muti, H; Najib, NM, 1993
)
0.72
" As far as diclofenac is concerned, single premedication increased significantly the rate of absorption and total body clearance but lowered the AUC of the NSAID."( Potential pharmacokinetic interactions of nocloprost clathrate with retarded theophylline and enteric coated diclofenac after single and repeated premedication in healthy volunteers.
Amon, I; Franke, G; Scheuch, E; Siegmund, W; Stolz, E; Zschiesche, M, 1993
)
0.89
"Bioavailability Study of Enteric Coated Diclofenac Formulations/1st Communication: Bioavailability study following single-dose administration of a multiple-unit formulation compared with a single-unit formulation Relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after single-dose administration of an enteric coated multiple-unit formulation (Diclo-Puren 50, test) in comparison to a single-unit dosage form (reference)."( [Biological availability of gastric juice-resistant coated diclofenac preparations. 1. Bioavailability study following a single administration of a multiple-unit formulation in comparison with a single-unit formulation].
Babej-Dölle, RM; Blume, H; Scheidel, B; von Nieciecki, A; Walter, K, 1993
)
0.8
" The new diclofenac-sucralfate association shows a different rate of absorption (namely an early and greater peak plasma concentration of diclofenac) and a similar extent of absorption (AUC(0-infinity) being not statistically different) as compared to the reference enteric-coated tablets of 50 mg diclofenac."( Pharmacokinetic studies in healthy volunteers on a new gastroprotective pharmaceutic form of diclofenac.
Carabelli, A; Contos, S; De Bernardi di Valserra, M; Feletti, F; Germogli, R; Maggi, L; Tripodi, AS, 1993
)
0.92
" The relative rectal bioavailability was 107."( Comparative pharmacokinetic evaluation of compressed suppositories of diclofenac sodium in humans.
Diwan, PV; Fadnavis, NW; Ramakrishna, S, 1996
)
0.53
" The results obtained show a similar extent of diclofenac and codeine bioavailability for both administration routes, but the rate of drug input was lower for the suppositories."( Pharmacokinetics and drug input characteristics for a diclofenac-codeine phosphate combination following oral and rectal administration.
Hanses, A; Meiss, F; Mutschler, E; Spahn-Langguth, H, 1996
)
0.8
"The bioavailability of a single dose of a potassium diclofenac (KDIC) suspension (Flogan, Merck, 7ml, 105 mg) was studied in 13 healthy male volunteers in the fasting state (placebo phase, PLA), after gastric acid secretion blockade (subacute pretreatment with omeprazole, OME phase) and after food intake (FOOD phase)."( Influence of gastric acid secretion blockade and food intake on the bioavailability of a potassium diclofenac suspension in healthy male volunteers.
De Nucci, G; Dias, HB; Moreno, H; Moreno, RA; Muscara, MN; Poli, A; Ribeiro, W, 1996
)
0.76
"In this study, in vitro characterization, bioavailability and pharmacokinetics of 2 different sustained-release diclofenac sodium dosage forms were compared, Voltaren (100 mg tablets), manufactured by Ciba-Geigy and Inflaban (100 mg enteric-coated tablets), manufactured by the Arab Pharmaceutical Manufacturing Company."( Bioavailability and pharmacokinetic properties of 2 sustained-release formulations of diclofenac sodium, Voltaren vs inflaban: effect of food on inflaban bioavailability.
Deleq, S; Hasan, M; Najib, N; Sallam, E; Shubair, M; Zmeili, S, 1996
)
0.73
"The pharmacokinetic analysis of an oral sustained-release preparation of diclofenac sodium has been investigated using multi-segment absorption models in which it has been assumed that the gastrointestinal tract can be divided into several segments in each of which the drug has its own lag-time and absorption rate constants."( Pharmacokinetic analysis of the absorption characteristics of diclofenac sodium in man by use of a multi-segment absorption model.
Mahmood, I, 1996
)
0.77
" The relative bioavailability of the two formulations were 59."( Comparative study of in-vitro release and bioavailability of sustained release diclofenac sodium from certain hydrophilic polymers and commercial tablets in beagle dogs.
al-Dardiri, MA; al-Helw, AR; Hosny, EA, 1997
)
0.52
" The relative bioavailability in the human was about 86%."( [Preparation of diclofenac sodium controlled release pellets and multiple-dose evaluation in healthy volunteers].
Long, XY; Lu, RB; Xu, SP; Zeng, XW, 1996
)
0.64
" Although the 2 products are not equivalent regarding the secondary parameter Tmax, still the data indicate that they could be considered bioequivalent regarding rate of absorption (Cmax), extent of absorption (Cmax and AUC), and elimination (t1/2)."( Comparative bioavailability of two capsule formulations of mefenamic acid.
Jalal, IM; Najib, NM; Rawashdeh, NM, 1997
)
0.3
" For in vivo bioavailability studies rabbits were used as animal models."( In vivo and in vitro diclofenac sodium evaluation after rectal application of soft gelatine capsules enabling application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) for controlled release.
Müller-Goymann, CC; Schneeweis, A, 1997
)
0.62
" The in vivo bioavailability studies show bioequivalence in terms of AUC for both formulations (capsules and Voltaren suppositories)."( In vivo and in vitro diclofenac sodium evaluation after rectal application of soft gelatine capsules enabling application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) for controlled release.
Müller-Goymann, CC; Schneeweis, A, 1997
)
0.62
"58 micrograms h/ml resulting in a relative bioavailability of 145."( Effect of coating of aluminum carboxymethylcellulose beads on the release and bioavailability of diclofenac sodium.
Hosny, EA, 1998
)
0.52
" The in vivo absorption for the sustained-release formulation is slow first order and follows a flip-flop model since disposition rate constants are greater than absorption rate constants."( Determination of the population pharmacokinetic parameters of sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium by simultaneous data fitting using NONMEM.
Amidon, GL; Hassan, MM; Idkaidek, NM; Najib, NM; Smith, DE, 1998
)
0.5
"This study determines comparative bioavailability of diclofenac sodium lotion compared to an aqueous solution after topical application to viable human skin in vitro."( In vitro cutaneous disposition of a topical diclofenac lotion in human skin: effect of a multi-dose regimen.
Hewitt, PG; Maibach, HI; Poblete, N; Shainhouse, JZ; Wester, RC, 1998
)
0.81
" There was no significant change in the bioavailability of theses NSAIDs during omeprazole therapy in this study."( Lack of drug-drug interaction between three different non-steroidal anti-inflammatory drugs and omeprazole.
Andersson, T; Bredberg, E; Lagerström, PO; Naesdal, J; Wilson, I, 1998
)
0.3
" Sequential time blood and urine samples were taken to determine pharmacokinetics, bioavailability and metabolism."( In vivo bioavailability and metabolism of topical diclofenac lotion in human volunteers.
Hewitt, PG; Hui, X; Maibach, HI; Poblete, N; Shainhouse, JZ; Wester, RC, 1998
)
0.55
"8), and bioavailability in beagle dogs relative to the commercial enteric-coated tablets Voltaren."( Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads.
el-Mahrouk, GM; Gouda, MW; Hosny, EA, 1998
)
0.55
" However, while effective, it has low oral bioavailability and some problematic adverse effects."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.52
" The rate of absorption with the sachets proved to be very fast, reaching peak values at 10 min in seven subjects and at 15 min in the remaining subjects: mean time was 13."( Pharmacokinetics of diclofenac after oral administration of its potassium salt in sachet and tablet formulations.
Abbondati, G; Ceppi Monti, N; Crivelli, F; Dal Bo, L; Ismaili, S; Marzo, A; Tettamanti, RA; Uhr, MR; Verga, F, 2000
)
0.63
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"Spinal cord injury (SCI) has been proposed to reduce drug bioavailability after intramuscular administration owing to an impairment in blood flow to paralyzed limbs."( Bioavailability of diclofenac after intramuscular administration to rats with experimental spinal cord injury.
García-López, P; Salas, R, 1999
)
0.63
" All S-NO-diclofenac derivatives acted as orally bioavailable prodrugs, producing significant levels of diclofenac in plasma within 15 min after oral administration to mice."( Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
Bandarage, UK; Chen, L; Fang, X; Garvey, DS; Glavin, A; Janero, DR; Letts, LG; Mercer, GJ; Saha, JK; Schroeder, JD; Shumway, MJ; Tam, SW, 2000
)
1.02
"The bioavailability of a newly developed effervescent tablet containing 50 mg diclofenac Na (DIC-effervesc) was investigated and compared with an enteric-coated dragée (DIC-enteric)."( Bioavailability of a new effervescent tablet of diclofenac.
Barkworth, M; Hoffmann, A; Terhaag, B; Vens-Cappell, B, 2000
)
0.79
" The bioavailability was compared as ratios of the geometric means of AUC0-infinity and Cmax."( Bioavailability of a new effervescent tablet of diclofenac.
Barkworth, M; Hoffmann, A; Terhaag, B; Vens-Cappell, B, 2000
)
0.56
"The relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after a single administration of a multiple-unit formulation containing 75 mg diclofenac sodium in enteric-coated pellets (A) in comparison to an enteric-coated tablet with 50 mg diclofenac sodium (B), a capsule containing 140 mg diclofenac resinate (C) and a dispersible tablet containing 46."( [Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation of enteric-coated pellets].
von Nieciecki, A; Walter, K, 2001
)
0.89
" Results of the bioavailability studies indicated that formulation 4 with drug:HPMC:NaCMC equal to 1:2:1 was similar to the marketed product Dicloran SR and showed better bioavailability than Voveran SR."( Formulation and evaluation of diclofenac sodium using hydrophilic matrices.
Jayasagar, G; Rao, YM; Veni, JK, 2001
)
0.6
" In rectal-resected rabbits, its bioavailability after rectal administration was significantly lower than that in normal rabbits, and furthermore that after intracolostomal administration was significantly lower than that in rectal-resected rabbits."( Pharmacokinetics of dicrofenac after its intrarectal and intracolostomal administration to rabbits with rectal resection or colostoma construction.
Fujimoto, S; Matsuda, T; Nagasawa, K; Nakanishi, H; Ohnishi, N; Takara, K; Yokoyama, T, 2001
)
0.31
" The last salification form has shown a prompter absorption rate and a faster onset of analgesic activity than the acid form and sodium salt."( Increased absorption rate of diclofenac from fast acting formulations containing its potassium salt.
Conti, M; Reiner, A; Reiner, G; Reiner, V, 2001
)
0.6
"The effects of food, antibiotics, diclofenac sodium (DS) and methotrexate (MTX) on oral bioavailability (BA) of MTX were examined in rats."( Variability of oral bioavailability for low dose methotrexate in rats.
Akahori, M; Kuroda, T; Namba, K; Torimaru, T; Yamamoto, S,
)
0.41
" The present study investigated the influence of tropical climate conditions (class IV: 40 degrees C, 75% relative humidity) on the drug content, in vitro dissolution and oral bioavailability of different formulations of two essential drugs marketed in Tanzania: diclofenac sodium and ciprofloxacin tablets."( Drug formulations intended for the global market should be tested for stability under tropical climatic conditions.
Bortel, LV; Remon, JP; Risha, PG; Vergote, G; Vervaet, C, 2003
)
0.5
" Oral bioavailability was also not influenced by tropical conditions."( Drug formulations intended for the global market should be tested for stability under tropical climatic conditions.
Bortel, LV; Remon, JP; Risha, PG; Vergote, G; Vervaet, C, 2003
)
0.32
" We performed a bioavailability randomized, cross-over study to compare the plasma profiles of diclofenamic acid after repeated epicutaneous administration of the new topical formulation with those of the marketed DHEP formulation without lecithin."( Effect of lecithin on epicutaneous absorption of diclofenac epolamine.
Conte, A; Mautone, G; Petrini, M; Ronca, G, 2002
)
0.57
" Pharmacokinetic and bioavailability study in eight human subjects were performed by HPLC method."( [Studies on diclofenac sodium pulsatile release pellets].
Dang, DS; Guo, T; Song, HT; Sui, Y; Sun, XH; Zheng, CL, 2003
)
0.7
"8 h, and the bioavailability was (91 +/- 12)%."( [Studies on diclofenac sodium pulsatile release pellets].
Dang, DS; Guo, T; Song, HT; Sui, Y; Sun, XH; Zheng, CL, 2003
)
0.7
"Pharmacokinetic studies were carried out to assess bioavailability of diclofenac preparations."( A comparison of gastrointestinal permeability induced by diclofenac-phospholipid complex with diclofenac acid and its sodium salt.
Jamali, F; Khazaeinia, T,
)
0.61
" In vivo evaluation was performed on six healthy human volunteers and various pharmacokinetic parameters (c(max), t(max), AUC(0-24), MRT) and relative bioavailability were calculated."( Development and biopharmaceutical evaluation of osmotic pump tablets for controlled delivery of diclofenac sodium.
Mishra, B; Rani, M; Sankar, C; Surana, R, 2003
)
0.54
"Lumiracoxib was well absorbed and demonstrated similar potency to naproxen as a COX-2 inhibitor (77% and 66% inhibition, respectively, vs."( Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2 selective inhibitor: An integrated study.
Atherton, C; Bebb, J; Bonner, J; Branson, J; Brough, J; Burdsall, J; Cunliffe, R; Hawkey, CJ; Jones, J; McKaig, B; Rordorf, C; Scott, G; Stevenson, D, 2004
)
0.32
""Trikatu"-an Ayurvedic formulation comprising of a 1:1:1 ratio of dried fruits of Piper nigrum, Piper longum and dried rhizomes of Zingiber officinale is widely used to enhance the bioavailability of drugs, like vasicine, indomethacin, etc."( Pharmacokinetic and pharmacodynamic studies on interaction of "Trikatu" with diclofenac sodium.
D'Mello, PM; Lala, LG; Naik, SR, 2004
)
0.55
" The rate of absorption of lumiracoxib was not significantly altered by hepatic impairment based on Cmax and Tmax."( No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor.
Kalbag, J; Lasseter, K; Milosavljev, S; Oberstein, S; Rordorf, C; Yeh, CM, 2004
)
0.32
" Oxaprozin has a high oral bioavailability (95%), with peak plasma concentrations at 3 to 5 hours after dosing."( Oxaprozin: kinetic and dynamic profile in the treatment of pain.
Kean, WF, 2004
)
0.32
" Through in vitro drug release kinetics, using regression coefficient analysis and Peppas equation, different pharmacokinetic parameters and relative bioavailability were determined."( Formulation and biopharmaceutical evaluation of osmotic matrix tablets of diclofenac sodium.
Mishra, B; Rani, M; Sankar, C; Surana, R,
)
0.36
" Drug bioavailability of a selected diclofenac sodium buccoadhesive product was then compared with that of Voltarin 100 SR tablet."( Formulation and evaluation of diclofenac sodium buccoadhesive discs.
Basalious, EB; El-Samaligy, MS; Yahia, SA, 2004
)
0.89
" The aim of this study was to determine the bioavailability of low-dose diclofenac-K."( Bioavailability of diclofenac potassium at low doses.
Brune, K; Chevts, J; Hinz, B; Rau, T; Renner, B; Schmidt, A; Szelenyi, I; Werner, U; Wuttke, H, 2005
)
0.89
" The absolute bioavailability of diclofenac-K after oral administration did not differ significantly in the 12."( Bioavailability of diclofenac potassium at low doses.
Brune, K; Chevts, J; Hinz, B; Rau, T; Renner, B; Schmidt, A; Szelenyi, I; Werner, U; Wuttke, H, 2005
)
0.94
"Our data indicate that diclofenac-K is rapidly and well absorbed at low dose, and are consistent with a rapid onset of action of the drug."( Bioavailability of diclofenac potassium at low doses.
Brune, K; Chevts, J; Hinz, B; Rau, T; Renner, B; Schmidt, A; Szelenyi, I; Werner, U; Wuttke, H, 2005
)
0.97
"The bioavailability of a generic diclofenac sodium sustained release tablet preparation (Zolterol, SR) was compared with the innovator product, Voltaren, SR."( Comparative bioavailability study of a generic sustained release diclofenac sodium tablet.
Choy, WP; Ling, SS; Magosso, E; Ng, BH; Ur-Rahman, N; Wong, JW; Yuen, KH, 2004
)
0.84
" Various pharmacokinetic parameters (ie, C(max), T(max), area under the curve [AUC(0-24)], and mean residence time) and relative bioavailability were compared."( Comparative in vitro and in vivo evaluation of matrix, osmotic matrix, and osmotic pump tablets for controlled delivery of diclofenac sodium.
Mishra, B; Rani, M, 2004
)
0.53
" The beads were evaluated for their bioavailability in six beagle dogs relative to the commercial enteric-coated Voltaren tablets."( Evaluation of crosslinked chitosan hydrogel beads as a carrier for prolonged delivery of diclofenac sodium: in vitro and in vivo studies.
Alsarra, IA, 2004
)
0.55
" In the comparative bioavailability study, we found that the developed spheroids were able to sustain the drug release over 8 hr and could improve the extent of absorption and bioavailability of the drug."( Development of controlled release spheroids using natural polysaccharide as release modifier.
Dhobe, RR; Gowthamarajan, K; Kulkarni, GT; Suresh, B; Yohanan, F,
)
0.13
"Two different transdermal diclofenac (CAS 15307-86-5) formulations (Olfen Patch 140 mg diclofenac sodium as test preparation and 180 mg diclofenac epolamine plaster, equivalent to 140 mg diclofenac sodium, as reference preparation) were investigated in 24 healthy male and female volunteers in order to compare the transdermal bioavailability between both treatments following topical multiple dose administration."( Determination of the transdermal bioavailability of a newly developed diclofenac sodium patch in comparison with a reference preparation.
Arnold, P; Cambon, N; Frentzel, A; Gschwend, MH; Martin, W; Scheiwe, W; Verdun, MO, 2005
)
0.86
"The study was designed to evaluate the relative bioavailability of diclofenac in plasma, subcutaneous adipose and skeletal muscle tissue after repeated topical administration using MIKA Diclofenac Spray Gel (4%), a novel formulation, and after oral dosing using VOLTAREN 50 mg enteric coated tablets."( Favourable dermal penetration of diclofenac after administration to the skin using a novel spray gel formulation.
Brunner, M; Dehghanyar, P; Martin, W; Menke, G; Müller, M; Seigfried, B, 2005
)
0.85
"The relative bioavailability of diclofenac in subcutaneous adipose and skeletal muscle tissue was substantially higher after topical compared with oral dosing (324% and 209%, respectively) whereas relative plasma bioavailability was 50-fold lower."( Favourable dermal penetration of diclofenac after administration to the skin using a novel spray gel formulation.
Brunner, M; Dehghanyar, P; Martin, W; Menke, G; Müller, M; Seigfried, B, 2005
)
0.89
" Lumiracoxib has good oral bioavailability (74%)."( Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor.
Choi, L; Mangold, JB; Marshall, P; Rordorf, CM, 2005
)
0.33
"The aim of this study was to evaluate the effect of sodium diclofenac on the bioavailability of amoxicillin."( Effect of sodium diclofenac on the bioavailability of amoxicillin.
Ambrosano, GM; Cogo, K; de Cássia Bergamaschi, C; Del Fiol, Fde S; Franco, GC; Groppo, FC; Montan, MF; Motta, RH; Rosalen, PL, 2006
)
0.92
" The absolute bioavailability of IM DCLF appears to be approximately 100%."( Pharmacokinetics of diclofenac in sheep following intravenous and intramuscular administration.
Al-Hadiya, BM; Alkharfy, KM; Altaher, AY; Khan, RM, 2006
)
0.66
"In this study, we investigated the bioavailability of iontophoretically delivered diclofenac with the methylnicotinate (MN) test."( Determination of the in vivo bioavailability of iontophoretically delivered diclofenac using a methyl nicotinate skin inflammation assay.
Barel, AO; Clarys, P; Clijsen, R; Lambrecht, R, 2006
)
0.79
" Bioavailability was assessed by quantification of an MN-induced erythema under the different conditions."( Determination of the in vivo bioavailability of iontophoretically delivered diclofenac using a methyl nicotinate skin inflammation assay.
Barel, AO; Clarys, P; Clijsen, R; Lambrecht, R, 2006
)
0.56
"The procedure used enabled us to evaluate the bioavailability of a non-steroidal anti-inflammatory drug in the skin."( Determination of the in vivo bioavailability of iontophoretically delivered diclofenac using a methyl nicotinate skin inflammation assay.
Barel, AO; Clarys, P; Clijsen, R; Lambrecht, R, 2006
)
0.56
" This drug, therefore affects the bioavailability of two major respiratory complex I substrates which would normally contribute substantially to supplying the reducing equivalents for mitochondrial electron transport for generation of ATP in the renal cell."( Action of diclofenac on kidney mitochondria and cells.
Halliwell, B; Ng, LE; Vincent, AS; Wong, KP, 2006
)
0.74
" These physicochemical results indicate that solid molecular dispersions based on PHEMA hydrogels can effectively enhance the dissolution and therefore should be potentially useful in improving the oral bioavailability of poorly water-soluble drugs."( Solid molecular dispersions of poorly water-soluble drugs in poly(2-hydroxyethyl methacrylate) hydrogels.
Lee, PI; Zahedi, P, 2007
)
0.34
" The oral bioavailability in rats was determined for selected diclofenac derivatives."( Aminocarbonyloxymethyl ester prodrugs of flufenamic acid and diclofenac: suppressing the rearrangement pathway in aqueous media.
Iley, J; Järvinen, T; Mendes, E; Moreira, R; Mota-Filipe, H; Rautio, J; Ribeiro, L; Silva, N, 2007
)
0.82
" The ocular bioavailability of liposome in aqueous humor was 211% compared with that of eyedrop."( [Preparation of diclofenac sodium liposomes and its ocular pharmacokinetics].
Huang, LJ; Liang, RC; Liu, K; Sun, KX; Wang, AP, 2006
)
0.68
"The objective of present study was to improve the solubility, dissolution rate, micromeritic properties and bioavailability of aceclofenac (NSAID) by formulating its spherical agglomerates."( Improved bioavailability of aceclofenac from spherical agglomerates: development, in vitro and preclinical studies.
Muatlik, S; Pandey, S; Ranjith, AK; Reddy, MS; Usha, AN, 2007
)
0.34
" Co-administration of enrofloxacin did not affect Vd(area) and MRT but absorption rate constant (K(a)), beta, t1/2Ka, t1/2beta, AUC, AUMC, Cl(B) and bioavailability (F) were significantly increased."( Pharmacokinetics of diclofenac and its interaction with enrofloxacin in sheep.
Ahmad, AH; Kumar, A; Malik, JK; Rahal, A, 2008
)
0.67
" The results show that liver damage and regeneration increases the bioavailability by decreasing elimination."( Pharmacokinetics of diclofenac in rats intoxicated with CCL4, and in the regenerating liver.
Castañeda-Hernández, G; Favari, L; Muriel, P; Reyes-Gordillo, K, 2007
)
0.66
"In this study the significant effect of chitosan on improving the dissolution rate and bioavailability of aceclofenac has been demonstrated by simple solvent change method."( Enhancement of dissolution rate and bioavailability of aceclofenac: a chitosan-based solvent change approach.
Anju, P; Manoj, K; Mutalik, S; Usha, AN, 2008
)
0.35
" Following oral administration, the less lipophilic celecoxib has a lower bioavailability (20-40%) than the other two coxibs (74-100%)."( Clinical use and pharmacological properties of selective COX-2 inhibitors.
Klotz, U; Shi, S, 2008
)
0.35
" Etoricoxib is partly metabolised by the cytochrome P450 isoenzyme CYP 3A4 and increases the bioavailability of ethinylestradiol."( Etoricoxib: new drug. Avoid using cox-2 inhibitors for pain.
, 2007
)
0.34
"This study was conducted to compare the bioavailability of 2 branded formulations of aceclofenac 100 mg (test and reference) marketed in Korea."( Bioequivalence and pharmacokinetic evaluation of two branded formulations of aceclofenac 100 mg: a single-dose, randomized, open-label, two-period crossover comparison in healthy Korean adult volunteers.
Kang, JS; Lee, MH; Park, JH; Park, YS; Rhim, SY; Shaw, LM, 2008
)
0.35
" To evaluate the possibility of a pharmacokinetic interaction, the oral bioavailability of diclofenac (18 mg/kg) was studied in presence and the absence of glibenclamide (10 mg/kg)."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.83
"6 h, oral bioavailability of 37% and 90%) with anti-inflammatory activity (ED 50 = 37 micromol/kg, mouse) and efficacy in pain models (thermal hyperalgesia, ED 50 = 72 micromol/kg, rat)."( Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Adair, RM; Altenbach, RJ; Bettencourt, BM; Brioni, JD; Cowart, MD; Drizin, I; Esbenshade, TA; Fix-Stenzel, SR; Honore, P; Hsieh, GC; Liu, H; Marsh, KC; McPherson, MJ; Milicic, I; Miller, TR; Sullivan, JP; Wetter, JM; Wishart, N; Witte, DG, 2008
)
0.35
"Most of the floating systems have an inherent drawback of high variability in the GI transit time, invariably affecting the bioavailability of drug."( Hollow microspheres of diclofenac sodium - a gastroretentive controlled delivery system.
Abraham, S; Bv, B; Furtado, S; R, D; S, B; V, M, 2008
)
0.66
" The bioavailability in terms of systemic exposure from the patch compared with oral intake (75 mg/day) is in the order of 1%."( Diclofenac epolamine (Flector) patch: evidence for topical activity.
Petersen, B; Rovati, S, 2009
)
1.8
" The objective of this study was to determine pharmacokinetic parameters and to compare the bioavailability of the new formulation of injection diclofenac sodium (75 mg/ml), given as an intradeltoid injection, with the reference formulation (75 mg/3 ml) given intragluteally."( Pharmacokinetic profile of a new formulation of injection diclofenac designed for intradeltoid use.
Jaiswal, V; Nivsarkar, M; Ojha, A; Padh, H; Patel, S; Shep, D, 2009
)
0.8
"Two different salts of diclofenac, diclofenac sodium and diclofenac potassium, in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and dehydrated rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2009
)
0.91
"In an open-label, single-dose, three-way crossover, relative bioavailability study, 24 healthy volunteers were randomized to receive each of the 25-mg DPSGC formulations (development processes A and B) and the 1-mL (25-mg) liquid diclofenac formulation (similar to the fill liquid used in the DPSGC products) during three inpatient visits."( Single-dose pharmacokinetic study of rapidly dispersing diclofenac potassium formulations in healthy volunteers.
Kowalski, MM; Lissy, M; Moore, KA; Stiff, DD, 2009
)
0.78
"The results support our hypothesis that CD improves bioavailability of drugs to the synovial joints."( "ChilDrive": a technique of combining regional cutaneous hypothermia with iontophoresis for the delivery of drugs to synovial fluid.
Murthy, SN; Sammeta, SM, 2009
)
0.35
"Pharmacosomes are amphiphilic lipid vesicular systems that have shown their potential in improving the bioavailability of poorly water soluble as well as poorly lipophilic drugs."( Development and physicochemical evaluation of pharmacosomes of diclofenac.
Rawat, MS; Semalty, A; Semalty, M; Singh, D, 2009
)
0.59
"Systemic bioavailability and pharmacodynamics of topical diclofenac sodium gel 1% were compared with those of oral diclofenac sodium 50-mg tablets."( Systemic bioavailability of topical diclofenac sodium gel 1% versus oral diclofenac sodium in healthy volunteers.
Gold, M; Kienzler, JL; Nollevaux, F, 2010
)
0.88
"In this open-label, randomized, single-dose (2 distinct doses), 2-way crossover bioavailability study, healthy adult volunteers were randomly assigned to receive a single dose of DPSGC 25 or 50 mg after an overnight fast (fasted condition) or high-fat breakfast (fed condition) (period 1)."( Effects of food intake on the pharmacokinetics of diclofenac potassium soft gelatin capsules: a single-dose, randomized, two-way crossover study.
Moore, KA; Scallion, R, 2009
)
0.61
" The bioavailability of DFS in microspheres was about 61% that of Voltaren, for the parameters AUC and Cmax, and they are therefore not bioequivalent to Voltaren in relation to the extent of absorption."( Comparative in vitro and in vivo evaluations of oral sustained-release formulations of diclofenac sodium in beagle dogs.
Lemos-Senna, E; Mazon-Cardoso, T; Medeiros, DC; Poli, A, 2009
)
0.58
" A first-order model, including lag time and decreased relative bioavailability as a function of the dose, described the absorption process."( Pharmacokinetic-pharmacodynamic modelling of the analgesic effects of lumiracoxib, a selective inhibitor of cyclooxygenase-2, in rats.
Castañeda-Hernández, G; Ortiz, MI; Salazar-Morales, UE; Trocóniz, IF; Vásquez-Bahena, DA, 2010
)
0.36
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms."( Colloids as a sink for certain pharmaceuticals in the aquatic environment.
Maskaoui, K; Zhou, JL, 2010
)
0.36
" Besides, this antagonism was not produced by diminution in the bioavailability of diclofenac."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.91
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"To compare the pharmacokinetic profiles of diclofenac potassium liquid-filled soft gelatin capsules (DPSGC) using patented ProSorb dispersion technology with an immediate-release, diclofenac potassium 50-mg comparator tablet in two open-label, single-dose, randomized, crossover relative bioavailability studies in healthy volunteers."( Pharmacokinetic comparison of an oral diclofenac potassium liquid-filled soft gelatin capsule with a diclofenac potassium tablet.
Lissy, M; Moore, K; Scallion, R; Stiff, DD, 2010
)
0.89
" Thus, dissolution profiles suggested that combination of kappa-carrageenan and sodium starch glycolate resulted into fast-disintegrating, immediate-release pellets, overcoming the bioavailability problem of the poorly soluble drug, aceclofenac, and enteric coating of these pellets avoids the exposure of aceclofenac to ulcer-prone areas of the gastrointestinal tract."( Development and characterization of enteric-coated immediate-release pellets of aceclofenac by extrusion/spheronization technique using kappa-carrageenan as a pelletizing agent.
Awari, JG; Kilor, VA; Sapkal, NP; Shewale, BD, 2010
)
0.36
" Oral bioavailability of P2026 was estimated from plasma concentration of diclofenac and nitrate/nitrite (NOx)."( Oral bioavailability, efficacy and gastric tolerability of P2026, a novel nitric oxide-releasing diclofenac in rat.
Desai, DC; Deshattiwar, JJ; Deshmukh, NJ; Dhiman, M; Gaikwad, PP; Karwa, M; Mali, SV; Nemmani, KV; Pamidiboina, V; Pathan, AR; Satyam, A; Sharma, SD; Thanga Mariappan, T, 2010
)
0.81
"An attempt has been made in the present study to formulate soluble ocular inserts of aceclofenac to facilitate the bioavailability of the drug into the eye, as no eye drop solution could be formulated."( Glycerogelatin-based ocular inserts of aceclofenac: physicochemical, drug release studies and efficacy against prostaglandin E₂-induced ocular inflammation.
Gilhotra, RM; Mathurm, M, 2011
)
0.37
" However, no published data is available regarding the combined pharmacokinetics and bioavailability of this particular fixed dose combination."( Bioequivalence study of a fixed dose combination tablet containing rabeprazole and diclofenac sodium in healthy Indian subjects.
Chakrabarty, US; Chatterjee, B; Das, A; Mukherjee, J; Pal, TK; Roy, B; Sahoo, B; Sengupta, P, 2010
)
0.59
" Although the relative bioavailability of colonic administration of diclofenac, metformin and cevimeline compared to oral administration was similar regardless of the drug doses in the colon, colonic absorption of diltiazem varied according to the doses."( The relationship between the drug concentration profiles in plasma and the drug doses in the colon.
Hosoi, Y; Kanamaru, T; Konno, T; Nakagami, H; Tajiri, S; Yada, S; Yoshida, K, 2010
)
0.6
" These results suggest that this novel ocular drug delivery system appears to offer promise as a means to improving the bioavailability of drugs after ophthalmic applications."( Zn-Al-NO(3)-layered double hydroxides with intercalated diclofenac for ocular delivery.
Cao, F; Liao, Z; Ping, Q; Wang, Y, 2011
)
0.62
" Bioavailability study of different coated pellets revealed that the drug concentration in plasma of beagle dogs was too low to be detected and, implied that the drug was nearly not released from the preparations before reaching colon due to the appearance of lag time in the dissolution process."( Preparation and in vitro-in vivo evaluation of double layer coated and matrix sustained release pellet formulations of diclofenac potassium.
Fu, J; He, H; Li, G; Meng, J; Tang, X; Wang, X; Weng, Y; Xu, L, 2011
)
0.58
" The objective of this study was to compare the bioavailability of test formulation with the reference formulation given intramuscularly in healthy volunteers."( Comparative bioavailability study of a new formulation of injection of 75 mg diclofenac sodium in 1 ml with the conventional injection of 75 mg diclofenac sodium given in 3 ml volume.
Jaiswal, V; Nivsarkar, M; Ojha, A; Padh, H; Patel, S; Shep, D, 2011
)
0.6
" However, it was accepted as safe for ophthalmic use and could increase diclofenac sodium bioavailability in aqueous humor significantly."( Optimization and evaluation of thermoresponsive diclofenac sodium ophthalmic in situ gels.
Asasutjarit, R; Fuongfuchat, A; Thanasanchokpibull, S; Veeranondha, S, 2011
)
0.86
" When PK parameters were grouped as low-medium-high, clearance, volume of distribution, half life and bioavailability were similar between discrete and cassette analysis for 90%, 86%, 95% and 90% of the total number of compounds tested, respectively."( High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC-MS/MS.
Betnér, I; Briem, S; Bueters, T; Dahlström, J; Kvalvågnaes, K, 2011
)
0.37
"Spray-dried emulsion (SDE) was prepared and characterized to improve the intestinal absorption and oral bioavailability of ZLR-8, a nitric oxide-releasing derivative of diclofenac, currently under preclinical development."( Spray-dried oil-in-water emulsion to improve the intestinal absorption and oral bioavailability of ZLR-8, a nitric oxide-releasing derivative of diclofenac.
Gao, Y; Zhang, J; Zhang, Y; Zheng, Z, 2011
)
0.76
" Accurate and precise RP-HPLC methods for the detection of ZLR-8 and its metabolite diclofenac were constructed to perform the bioavailability study."( Spray-dried oil-in-water emulsion to improve the intestinal absorption and oral bioavailability of ZLR-8, a nitric oxide-releasing derivative of diclofenac.
Gao, Y; Zhang, J; Zhang, Y; Zheng, Z, 2011
)
0.79
" SDE significantly enhanced the intestinal absorption rate of ZLR-8 in duodenum and jejunum but had indistinctive effect on permeability."( Spray-dried oil-in-water emulsion to improve the intestinal absorption and oral bioavailability of ZLR-8, a nitric oxide-releasing derivative of diclofenac.
Gao, Y; Zhang, J; Zhang, Y; Zheng, Z, 2011
)
0.57
"The aim of this study was to evaluate the relative bioavailability of a new controlled-release formulation of aceclofenac (200 mg od; Clanza CR®) in comparison with immediate-release aceclofenac (100 mg twice daily [bid], Airtal®) and to assess the effect of food on the pharmacokinetics of the new controlled-release aceclofenac formulation."( Pharmacokinetics of a new once-daily controlled-release formulation of aceclofenac in Korean healthy subjects compared with immediate-release aceclofenac and the effect of food: a randomized, open-label, three-period, crossover, single-centre study.
Bae, SK; Kim, SH; Lee, HJ; Lee, HW; Lee, SH; Lim, MS; Seong, SJ; Shin, SY; Yoon, YR, 2012
)
0.38
" Additionally, the bioavailability of controlled-release aceclofenac was not affected by high-fat foods."( Pharmacokinetics of a new once-daily controlled-release formulation of aceclofenac in Korean healthy subjects compared with immediate-release aceclofenac and the effect of food: a randomized, open-label, three-period, crossover, single-centre study.
Bae, SK; Kim, SH; Lee, HJ; Lee, HW; Lee, SH; Lim, MS; Seong, SJ; Shin, SY; Yoon, YR, 2012
)
0.38
"The aim of this study was the comparison of in vitro dissolution and in vivo bioavailability of two different brands of diclofenac sodium (CAS 15307-86-5) enteric coated tablets in healthy male Iranian volunteers in a single-dose, randomized, open-label, single blind study, which was conducted according to a crossover design in healthy volunteers."( Comparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations.
Basmenji, S; Valizadeh, H; Zakeri-Milani, P, 2011
)
0.81
"Diclofenac bioavailability after intravenous administration was increased in injured rats compared with controls due to a reduced clearance."( Contrasting effects of cord injury on intravenous and oral pharmacokinetics of diclofenac: a drug with intermediate hepatic extraction.
Arauz, J; Castañeda-Hernández, G; Cruz-Antonio, L; Franco-Bourland, RE; Guízar-Sahagún, G, 2012
)
2.05
"The present study was undertaken to compare the bioavailability and pharmacokinetic parameters of diclofenac sodium and diclofenac potassium in normal and experimentally induced diabetic state in 24 rabbits using a validated reversed phase HPLC method with a washout period of one week."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and alloxan-diabetic rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2012
)
0.84
" The bioavailability of two controlled release tablet formulations was studied and compared to that of commercial tablets, and rabbit stomachs were also histologically examined 24 h after administration of the various tablets."( Stability, bioavailability, and ulcerative activity of diclofenac sodium-mastic controlled release tablets.
Abd El-Gawad, AH; Guda, TK; Nouh, AT, 2010
)
0.61
" MTH is more effective to counteract gastric stasis associated with migraine, and it enhances the rate of absorption of non-steroidal anti-inflammatory drugs (NSAIDs)."( Formulation and evaluation of bilayer tablets of metoclopramide hydrochloride and diclofenac sodium.
Amrutkar, JR; Gattani, SG; Khabiya, SS; Kushare, SS,
)
0.36
" However, few studies have assessed the bioavailability of pharmaceuticals to fish in natural waters."( Bioavailability of pharmaceuticals in waters close to wastewater treatment plants: use of fish bile for exposure assessment.
Brozinski, JM; Kronberg, L; Lahti, M; Oikari, A; Segner, H, 2012
)
0.38
" It could be concluded that polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability."( Effect of polacrilin potassium as disintegrant on bioavailability of diclofenac potassium in tablets : a technical note.
Bele, MH; Derle, DV, 2012
)
0.61
"To assess the relative bioavailability of diclofenac sodium hydroxypropyl β-cyclodextrin (HPβCD) administered via the subcutaneous (s."( Pharmacokinetics of a new diclofenac sodium formulation developed for subcutaneous and intramuscular administration.
Ducharme, MP; Gugliotta, B; Müller, M; Oraha, AZ; Rusca, A; Zeitlinger, M, 2012
)
0.94
"One single-dose, randomized, three-way, crossover relative bioavailability study and one linearity single escalating dose, randomized, three-way cross-over pharmacokinetic study were conducted at two different clinical sites."( Pharmacokinetics of a new diclofenac sodium formulation developed for subcutaneous and intramuscular administration.
Ducharme, MP; Gugliotta, B; Müller, M; Oraha, AZ; Rusca, A; Zeitlinger, M, 2012
)
0.68
"To compare the bioavailability of diclofenac-K 2 × 12."( Diclofenac potassium 12.5 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative, bioavailability study versus diclofenac potassium 12.5 mg tablets.
Gold, M; Kienzler, JL, 2012
)
2.1
" The new formulation is expected to have a faster rate of absorption and comparable overall bioavailability compared with the tablet formulations."( Diclofenac potassium 25 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative bioavailability study vs. diclofenac potassium 2 x 12.5 mg tablets.
Armogida, M; Gold, M, 2012
)
1.82
"To compare the systemic bioavailability of diclofenac from the new 25 mg liquid capsule vs."( Diclofenac potassium 25 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative bioavailability study vs. diclofenac potassium 2 x 12.5 mg tablets.
Armogida, M; Gold, M, 2012
)
2.08
"In this randomized, open-label, crossover, comparative bioavailability study, 42 healthy subjects (mean age 23."( Diclofenac potassium 25 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative bioavailability study vs. diclofenac potassium 2 x 12.5 mg tablets.
Armogida, M; Gold, M, 2012
)
1.82
" However, the rate of absorption of diclofenac was much faster from the liquid capsule than from the tablets, with a much greater early exposure to diclofenac."( Diclofenac potassium 25 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative bioavailability study vs. diclofenac potassium 2 x 12.5 mg tablets.
Armogida, M; Gold, M, 2012
)
2.1
"Due to the multi-factorial physiological implications of bariatric surgery, attempts to explain trends in oral bioavailability following bariatric surgery using singular attributes of drugs or simplified categorisations such as the biopharmaceutics classification system have been unsuccessful."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"The trends in oral bioavailability pre to post surgery were found to be dependent on a combination of drug parameters, including solubility, permeability and gastrointestinal metabolism as well as the surgical procedure carried out."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
" These results suggest a great potential of our micelle formulations as a novel ocular drug delivery system to improve the bioavailability of the drugs."( Diclofenac/biodegradable polymer micelles for ocular applications.
Chen, H; Li, J; Li, X; Sun, S; Weng, Y; Zhang, Z, 2012
)
1.82
" The calculated relative bioavailability of the aceclofenac DIA patch was 18."( Formulation and biopharmaceutical evaluation of a transdermal patch containing aceclofenac.
Chi, SC; Nguyen, T; Park, ES; Rhee, YS, 2013
)
0.39
" In vivo pharmacokinetic study indicated that the developed nano-composite hydrogel could significantly increase the bioavailability of diclofenac and maintain the concentration of diclofenac in aqueous humor above MEC at least 24h after administration as compared with that of the commercial diclofenac sodium eye drops, which might be able to reduce the frequency of administration for patients."( Development and evaluation of fast forming nano-composite hydrogel for ocular delivery of diclofenac.
Chen, H; Li, X; Zhang, Z, 2013
)
0.81
"Study 1: Bioavailability in terms of AUC after IV administration was equivalent for HPβCD-diclofenac compared with Voltarol and after IM administration of HPβCD-diclofenac and Voltarol."( Single-dose and multiple-dose pharmacokinetics and dose proportionality of intravenous and intramuscular HPβCD-diclofenac (Dyloject) compared with other diclofenac formulations.
Carr, DB; Hamilton, DA; Lacouture, PG; Mermelstein, F; Ramaiya, A; Wright, C, 2013
)
0.82
"  Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h."( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics.
Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014
)
0.61
" The absorption rate of fluorescein isothiocyanate (FITC)-labeled lysozyme in the proximal intestine was higher than that for a marker of non-specific absorption, FD-10, and was suppressed by colchicine (endocytosis inhibitor)."( Intestinal absorption of lysozyme, an egg-white allergen, in rats: kinetics and effect of NSAIDs.
Hamura, K; Matsuo, H; Yokooji, T, 2013
)
0.39
"There is a need for information on the bioavailability in pediatric patients of drugs from manipulated dosage forms when applied in combination with food and/or co-medication under realistic daily practice circumstances."( In vitro gastrointestinal model (TIM) with predictive power, even for infants and children?
Anneveld, B; de Koning, BA; de Wildt, SN; Hanff, LM; Havenaar, R; Lelieveld, JP; Minekus, M; Mooij, MG, 2013
)
0.39
"Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations."( Pharmacodynamics of diclofenac from novel Eudragit entrapped microspheres.
Adedokun, MO; Attama, AA; Kenechukwu, FC; Momoh, MA; Odo, CE, 2014
)
0.95
" A comparative bioavailability study using a selected CPOP formulation (T) versus the innovator product (R) revealed that CPOP tablet maintained a less fluctuated DS plasma concentration for up to 24 h with a detected mean Cmax of 836."( Controlled porosity osmotic pump system for the delivery of diclofenac sodium: in-vitro and in-vivo evaluation.
El-Ashmawy, AA; Emara, LH; Mursi, NM; Raslan, HM; Taha, NF, 2014
)
0.64
"To assess the relative bioavailability of a new subcutaneous (SC) diclofenac hydroxypropyl b-cyclodextrin (HPbCD) formulation administered to three body sites: quadriceps, gluteus, and abdomen."( Pharmacokinetics of a new subcutaneous diclofenac formulation administered to three body sites: quadriceps, gluteus, and abdomen.
Cardì, F; Drago, F; Gugliotta, B; Piazza, C; Salomone, S; Vitale, DC, 2014
)
0.91
"This was a pilot, single-dose, randomized, three-way crossover relative bioavailability study."( Pharmacokinetics of a new subcutaneous diclofenac formulation administered to three body sites: quadriceps, gluteus, and abdomen.
Cardì, F; Drago, F; Gugliotta, B; Piazza, C; Salomone, S; Vitale, DC, 2014
)
0.67
"The relative bioavailability of SC diclofenac HPbCD was comparable when administered to the quadriceps, gluteus, and abdomen."( Pharmacokinetics of a new subcutaneous diclofenac formulation administered to three body sites: quadriceps, gluteus, and abdomen.
Cardì, F; Drago, F; Gugliotta, B; Piazza, C; Salomone, S; Vitale, DC, 2014
)
0.95
" A significant enhancement of 189% and 164% in oral bioavailability (AUC0-8) was observed for optimized aceclofenac loaded mesoporous formulation (MS11/72) and nonporous silica (NP), respectively, when compared to plain aceclofenac in male Wistar rats."( Impact of surface area of silica particles on dissolution rate and oral bioavailability of poorly water soluble drugs: a case study with aceclofenac.
Kumar, D; Sailaja Chirravuri, SV; Shastri, NR, 2014
)
0.4
" In this study, to investigate its absolute bioavailability and metabolism in rats, aceclofenac was dissolved in a sterile aqueous solution containing urea (20 %) and trisodium citrate (10 %), and administered via oral (20 mg/kg) and intravenous (10 mg/kg) routes."( Absolute bioavailability and metabolism of aceclofenac in rats.
Jeong, TC; Kang, W; Kim, E; Kwon, KI; Noh, K; Shin, BS; Yun, HY, 2015
)
0.42
"Sodium diclofenac (Na-DFC) and celecoxib (CLXB) are common nonsteroidal anti-inflammatory (NSAID) drugs which suffer from poor bioavailability and severe side effects when consumed orally, and their transdermal delivery might present important advantages."( HIV-TAT enhances the transdermal delivery of NSAID drugs from liquid crystalline mesophases.
Aserin, A; Cohen-Avrahami, M; Garti, N; Ottaviani, MF; Shames, AI, 2014
)
0.86
"Anti-POR siRNA can be used to significantly reduce hepatic metabolism by various CYPs as well as greatly increase the bioavailability of high clearance compounds following an oral dose, thus enabling it to be used as a tool to increase drug exposure in vivo."( siRNA-mediated knockdown of P450 oxidoreductase in rats: a tool to reduce metabolism by CYPs and increase exposure of high clearance compounds.
Brown, D; Burke, RS; Carr, BA; Deshmukh, SV; DiMuzio, J; DiPietro, MA; Eisenhandler, R; Fauty, SE; Gibson, C; Gindy, ME; Hamilton, KA; Hochman, JH; Knemeyer, I; Koeplinger, KA; Kwon, HW; Lifsted, TQ; Menzel, K; Patel, M; Prueksaritanont, T; Pudvah, N; Rearden, P; Rudd, DJ; Seitzer, J; Somasuntharam, I; Strapps, WR; Thompson, CD, 2014
)
0.4
" Elastic vesicles (EVs) of curcumin were prepared to improve its cutaneous bioavailability and to use it for topical anti-inflammatory effect."( Development and evaluation of curcumin-loaded elastic vesicles as an effective topical anti-inflammatory formulation.
Agrawal, R; Kaur, IP; Sandhu, SK; Sharma, I, 2015
)
0.42
" To determine the possibility of a pharmacokinetic interaction, the oral bioavailability of diclofenac (10 mg/kg) was studied in presence and the absence of curcumin (31 mg/kg)."( Synergistic effect of the interaction between curcumin and diclofenac on the formalin test in rats.
Castañeda-Hernández, G; Chávez Piña, AE; De Paz-Campos, MA; Ortiz, MI; Zazueta-Beltrán, L, 2014
)
0.87
" Increase in the bioavailability of both diclofenac and carbamazepine following multiple GFJ ingestion was revealed."( Evidence of reduced oral bioavailability of paracetamol in rats following multiple ingestion of grapefruit juice.
Alhussainy, TM; Arafat, TA; Idkaidek, NM; Ismail, OA; Qinna, NA, 2016
)
0.7
" It was concluded that the batch which was prepared by using combination of crosspovidone and sodium starch glycolate as a super disintegrant shows excellent disintegration time, enhance dissolution rate, taste masking and hence lead to improve efficacy and bioavailability of drug."( Novel approach of aceclofenac fast dissolving tablet.
Ali, N; Dave, V; Sharma, S; Vishwakarma, P; Yadav, S, 2015
)
0.42
"Enhanced oral bioavailability of aceclofenac has been achieved using chitosan cocrystals of aceclofenac and its entrapment into alginate matrix a super saturated drug delivery system (SDDS)."( Chitosan cocrystals embedded alginate beads for enhancing the solubility and bioavailability of aceclofenac.
Ganesh, M; Hemalatha, P; Jang, HT; Jeon, UJ; Peng, MM; Saravanakumar, A; Ubaidulla, U, 2015
)
0.42
" The in vivo ophthalmic drug absorption study performed on rabbits indicated that DC-TMCNs could improve ophthalmic bioavailability of DC."( Development and Evaluation of Diclofenac Sodium Loaded-N-Trimethyl Chitosan Nanoparticles for Ophthalmic Use.
Asasutjarit, R; Fuongfuchat, A; Kewsuwan, P; Ritthidej, GC; Theerachayanan, T; Veeranodha, S, 2015
)
0.71
" To estimate the bioavailability of DF in the skin, MN responses at different times following initial DF application (1."( In vivo determination of the diclofenac skin reservoir: comparison between passive, occlusive, and iontophoretic application.
Baeyens, JP; Barel, AO; Clarys, P; Clijsen, R, 2015
)
0.71
" Additionally, in vivo bioavailability has been investigated on beagle dogs."( Formulation and in vivo evaluation of diclofenac sodium sustained release matrix tablet: effect of compression force.
Al-Enazi, FK; Barakat, NS; Elbagory, IM; Harisa, GI; Shazly, GA; Taha, EI, 2015
)
0.69
" In vivo pharmacokinetics studies showed enhanced pre-corneal retention and penetration of the DIC/MPEG-PCL-CS nanosuspension, which resulted in a higher concentration of DIC (Cmax) in the aqueous humor and better bioavailability compared with commercial DIC eye drops (P < 0."( Chitosan grafted methoxy poly(ethylene glycol)-poly(ε-caprolactone) nanosuspension for ocular delivery of hydrophobic diclofenac.
Chen, H; Li, X; Liang, R; Luo, Z; Shi, S; Yu, J; Zhang, Z, 2015
)
0.63
" The ability of the nanocrystals to improve dermal drug bioavailability was investigated in vitro using Franz diffusion vertical cells and newborn pig skin, in comparison with diclofenac acid coarse suspensions and a commercial topical formulation containing diclofenac sodium."( Novel nanosized formulations of two diclofenac acid polymorphs to improve topical bioavailability.
Ennas, G; Fadda, AM; Lai, F; Marongiu, F; Muzzalupo, R; Pireddu, R; Sinico, C, 2015
)
0.88
"Effective clinical utilisation of non-steroidal anti-inflammatory drugs, such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration."( Development of reconstitutable suspensions containing diclofenac sodium-loaded microspheres for pediatric delivery.
Bozkır, A; Canefe, K; Devrim, B; Oz, UC, 2015
)
0.89
" In vivo experiments on rats have shown that HPβCD has no statistically significant effect on absorption or bioavailability of DF-Na in spite of the observed improvement of its in vitro dissolution by HPβCD."( Potential interaction between zinc ions and a cyclodextrin-based diclofenac formulation.
Abdel Jalil, M; El-Sabawi, D; Hamdan, II, 2016
)
0.67
" Thanks to these properties, the bioavailability of the ophthalmic preparations can be increased, especially with the application of CLNaHA."( Comparative study of nanosized cross-linked sodium-, linear sodium- and zinc-hyaluronate as potential ocular mucoadhesive drug delivery systems.
Berkó, S; Bonferoni, MC; Budai-Szűcs, M; Caramella, C; Csányi, E; Facskó, A; Horvát, G; Maroda, M; Mori, M; Sandri, G; Soós, J; Szabó-Révész, P, 2015
)
0.42
" Pharmacokinetic analysis showed that oral administration of a tablet composed of DIC and PAP do not change the pharmacokinetic parameters such as MRT, MAT, Cl and bioavailability of the active substances compared with single administration of DIC and PAP after single dose."( PHARMACOKINETICS OF DICLOFENAC SODIUM AND PAPAVERINE HYDROCHLORIDE AFTER ORAL ADMINISTRATION OF TABLETS TO RABBITS.
Jawień, W; Kasperek, R; Poleszak, E; Zimmer, Ł,
)
0.45
" Moreover, results of studies investigating the characteristics of progesterone and cyclodextrins showed that the new formulation (progesterone/HPβCD 25 mg solution) has the same bioavailability as other products containing progesterone."( Efficacy and Safety Profile of Diclofenac/Cyclodextrin and Progesterone/Cyclodextrin Formulations: A Review of the Literature Data.
Bonagura, AC; Cenami, R; Cimmaruta, D; Fiorentino, S; Fossati, T; Rossi, F; Scavone, C; Torella, M, 2016
)
0.72
" Finally, the use of cyclodextrins led to significant increases in solubility and bioavailability of drugs, such as diclofenac and progesterone, and improvement in the efficacy and safety of these drugs."( Efficacy and Safety Profile of Diclofenac/Cyclodextrin and Progesterone/Cyclodextrin Formulations: A Review of the Literature Data.
Bonagura, AC; Cenami, R; Cimmaruta, D; Fiorentino, S; Fossati, T; Rossi, F; Scavone, C; Torella, M, 2016
)
0.93
" The ability of nanocrystals to improve dermal drug bioavailability was investigated ex vivo by using Franz diffusion vertical cells and mouse skin, in comparison with both diclofenac acid coarse suspensions and a commercial formulation."( Diclofenac acid nanocrystals as an effective strategy to reduce in vivo skin inflammation by improving dermal drug bioavailability.
Caddeo, C; Ennas, G; Fadda, AM; Lai, F; Marongiu, F; Pireddu, R; Scano, A; Sinico, C; Valenti, D, 2016
)
2.07
"The oral bioavailability of diclofenac potassium 50 mg administered as a soft gelatin capsule (softgel capsule), powder for oral solution (oral solution), and tablet was evaluated in a randomized, open-label, 3-period, 6-sequence crossover study in healthy adults."( Relative bioavailability of diclofenac potassium from softgel capsule versus powder for oral solution and immediate-release tablet formulation.
Bende, G; Bhad, P; Biswal, S; Chen, Y; Salunke, A; Sunkara, G; Wagner, R; Winter, S, 2016
)
1.02
" Compared with the Aceclofenac suppository, the relative bioavailability of the Tongshu suppository was 104."( Preparation and In Vivo Pharmacokinetics of the Tongshu Suppository.
Dong, L; Liu, G; Liu, S; Lu, K; Zheng, Y, 2016
)
0.43
" It was found that there is a significant increase in the bioavailability of diclofenac sodium from AHD2 formulation which was evident from the high AUC and MRT values compared with the pure drug."( Araucaria Gum: Novel Natural Polymer for Controlled Drug Delivery. Development, In Vitro and In Vivo Evaluation of Araucaria Gum Based Matrix Tablets for Controlled Release.
Lohithasu, D; Naga Durga, DH; Ramana Murthy Kolapalli, V, 2017
)
0.68
" With 8-10 times, greater bioavailability of drug-loaded LPHNPs than free MTX and ACL was obtained."( Functionalized Lipid-Polymer Hybrid Nanoparticles Mediated Codelivery of Methotrexate and Aceclofenac: A Synergistic Effect in Breast Cancer with Improved Pharmacokinetics Attributes.
Garg, NK; Jain, A; Jain, S; Katare, OP; Sharma, G; Singh, B; Tyagi, RK, 2017
)
0.46
"During the last decades, the study of the in vitro dissolution of pharmaceuticals has been strongly encouraged by the FDA in order to determine its relationship with the in vivo bioavailability of a drug."( Modeling and comparison of release profiles: Effect of the dissolution method.
Cascone, S, 2017
)
0.46
"Assessment of the bioavailability of topically applied drugs designed to act within or beneath the skin is a challenging objective."( Topical bioavailability of diclofenac from locally-acting, dermatological formulations.
Bunge, AL; Chiu, WS; Cordery, SF; Delgado-Charro, MB; Guy, RH; Pensado, A; Shehab, MZ, 2017
)
0.75
" Although post-operative prescription of anti-inflammatory drugs is used to manage the inflammation, the need for local drug delivery systems has been rising because of low bioavailability and fast clearance of drugs."( Surgical suture releasing macrophage-targeted drug-loaded nanoparticles for an enhanced anti-inflammatory effect.
Choy, YB; Heo, CY; Huh, BK; Kim, BH; Kim, H; Park, JH; Yoo, YC, 2017
)
0.46
"This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation-ultrasonication approach."( Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies.
Hussain, Z; Ibrahim, K; Khan, MA; Khan, S; Rahim, H; Sadiq, A; Shah, SMH; Shahat, AA; Ullah, R, 2017
)
0.46
" These compounds were found to be orally bioavailable and highly effective."( Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
Eswaran, S; Narayanan, S; Shivarudraiah, P; Shruthi, TG; Subramanian, S, 2019
)
0.51
"The data was consistent with the concept that heparin increased the clinical activity of the DHEP plus medicated plaster versus the reference DHEP medicated plaster through improved bioavailability due to enhanced movement of diclofenac from the plaster."( Rationale and evidence for the incorporation of heparin into the diclofenac epolamine medicated plaster.
Jones, C; Nencioni, A; Rainsford, KD; Roberts, MS, 2019
)
0.94
" We demonstrated promising results in the safety of employing BC lenses functionalized with a drug delivery system permitting the bioavailability of ophthalmic drugs."( Toxicity of therapeutic contact lenses based on bacterial cellulose with coatings to provide transparency.
Cavicchioli, M; Coelho, F; do Vale Braido, GV; Franchi, LP; Lima Ribeiro, SJ; Mendes, LS; Messaddeq, Y; O Capote, TS; Scarel-Caminaga, RM; Specian, SS, 2019
)
0.51
"Rb1 micelle formulations have great potential as a novel ocular drug delivery system to improve the bioavailability of drugs such as diclofenac."( Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery.
Lan, J; Li, M; Li, X; Lu, X; Wang, H; Wu, X; Xin, M; Zhang, F; Zhuang, Z, 2019
)
0.72
"The transdermal transit of diclofenac from the hydrogel demonstrated a faster onset and a greater absorption rate than either emulsion gel formulation, suggesting that the hydrogel formulation may have a faster onset of action in underlying tissues vs."( Hydrogel increases diclofenac skin permeation and absorption.
Haltner-Ukomadu, E; Hussein, K; Richter, A; Sacha, M, 2019
)
1.14
" On the other hand, IS01957 has been designed under the purview of anti-inflammatory drug and bioavailability enhancer."( Effect of IS01957, a para-coumaric acid derivative on pharmacokinetic modulation of diclofenac through oral route for augmented efficacy.
Abdullah, ST; Bhatt, S; Dogra, A; Gour, A; Koul, S; Malik, TA; Nandi, U; Rath, SK; Sangwan, PL; Sharma, A; Singh, G, 2019
)
0.74
" In vivo pharmacokinetics studies showed the bioavailability of DS was better after oral administration of DS-loaded SA/CMCS-ZnO hydrogel beads."( In vitro and in vivo release of diclofenac sodium-loaded sodium alginate/carboxymethyl chitosan-ZnO hydrogel beads.
Cao, W; Chen, S; Fan, YY; Gong, X; Jia, J; Li, W; Lian, X; Niu, B; Wang, H; Yan, J, 2019
)
0.8
" Altogether these data indicate that differences beyond ±10% between rheological parameters of test and reference formulation might not translate into meaningful release nor bioavailability divergence."( Relationship between rheological properties, in vitro release and in vivo equivalency of topical formulations of diclofenac.
Hernández, MJ; Hidalgo, I; Merino, V; Merino-Sanjuán, M; Nácher, A; Peris, D; Pleguezuelos-Villa, M; Sallan, M; Soler, L, 2019
)
0.72
"The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs."( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020
)
0.56
"The objective of this work was to design a diclofenac epolamine (DE) flash tablets (FTs) intended to dissolve in the mouth saliva, thereby improving the DE bioavailability and reducing its first-pass liver metabolism."( Fabrication, optimization, and in vitro/in vivo evaluation of diclofenac epolamine flash tablet.
El Sisi, AM; El-Nabarawi, MA; Elshafeey, AH; Mahmoud, DM, 2020
)
1.06
" Microemulsion delivery formulations are thermodynamically stable, have superior bioavailability and better penetration of lipophilic and hydrophilic drug into the dermis."( Determination of efficacy and toxicity of diclofenac microemulsion formulation for musculoskeletal pain: an observational study.
Banh, HL; Cave, A, 2020
)
0.82
"Persistence and environmental implication of pharmaceuticals in agricultural soil is determined depending on adsorption, bioavailability and toxicity."( Adsorption, Bioavailability and Microbial Toxicity of Diclofenac in Agricultural Soil.
Lhamo, P; Mahanty, B; Prakathi, J, 2020
)
0.81
"Self-emulsifying drug delivery systems (SEDDS) were formulated to increase the solubility and ultimately the oral bioavailability of ACF."( Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System.
Asim, MH; Ijaz, M; Jianxian, C; Murtaza, G; Saleem, K; Ur-Rehman, M, 2020
)
0.56
"Results obtained indicate that iontophoretic mediated transport of deformable liposomes could improve the regional bioavailability of diclofenac sodium to the synovial joints, an efficient mode for treating MSD in the elderly."( Iontophoretic Mediated Intraarticular Delivery of Deformable Liposomes of Diclofenac Sodium.
Murthy, SN; S, S; Shivakumar, HN; Vanaja, K, 2021
)
1.06
" The prepared tablets were tested for average weight, hardness, friability, disintegration, dissolution and in vivo bioavailability in rabbits."( Formulation of Aceclofenac Tablets Using Nanosuspension as Granulating Agent: An Attempt to Enhance Dissolution Rate and Oral Bioavailability.
Amin, F; Bari, A; Farooq, U; Mahmood, HM; Rahim, H; Sadiq, A; Ullah Jan, N; Ullah, R, 2020
)
0.56
" The in vivo bioavailability (in rabbits model) of aceclofenac nanosuspension-based tablets (ACN-1, ACN-2) proved an improved absorption as in comparison to the marketed formulation."( Formulation of Aceclofenac Tablets Using Nanosuspension as Granulating Agent: An Attempt to Enhance Dissolution Rate and Oral Bioavailability.
Amin, F; Bari, A; Farooq, U; Mahmood, HM; Rahim, H; Sadiq, A; Ullah Jan, N; Ullah, R, 2020
)
0.56
"This boosted in vitro and in vivo bioavailability may be attributed to reduced particle size of aceclofenac nanoformulations used in tablets."( Formulation of Aceclofenac Tablets Using Nanosuspension as Granulating Agent: An Attempt to Enhance Dissolution Rate and Oral Bioavailability.
Amin, F; Bari, A; Farooq, U; Mahmood, HM; Rahim, H; Sadiq, A; Ullah Jan, N; Ullah, R, 2020
)
0.56
" Hence, the improvement in solubility and bioavailability of ACF is very crucial for successful product development."( Novel Aceclofenac-l-Cystine and Aceclofenac-Urea Cocrystals with Enhanced Oral Bioavailability.
Gupta, A; Kumar, S; Mishra, CK; Singh, S, 2021
)
0.62
"The specific objective of this research work was the measurement of bioavailability and other pharmacokinetic parameters of ACF cocrystals prepared by the mechanochemical grinding method."( Novel Aceclofenac-l-Cystine and Aceclofenac-Urea Cocrystals with Enhanced Oral Bioavailability.
Gupta, A; Kumar, S; Mishra, CK; Singh, S, 2021
)
0.62
"Cocrystals of ACF with l-cystine and urea were prepared by neat grinding (NG) method and in-vivo oral bioavailability of prepared cocrystals was measured in Wistar rats."( Novel Aceclofenac-l-Cystine and Aceclofenac-Urea Cocrystals with Enhanced Oral Bioavailability.
Gupta, A; Kumar, S; Mishra, CK; Singh, S, 2021
)
0.62
"Percent relative bioavailability of ACF-l-CYS NG and ACF-UREA NG cocrystals in Wistar rats was found to be 242."( Novel Aceclofenac-l-Cystine and Aceclofenac-Urea Cocrystals with Enhanced Oral Bioavailability.
Gupta, A; Kumar, S; Mishra, CK; Singh, S, 2021
)
0.62
"The present study indicates that the enhanced aqueous solubility of the prepared cocrystals leads to enhanced oral bioavailability of ACF."( Novel Aceclofenac-l-Cystine and Aceclofenac-Urea Cocrystals with Enhanced Oral Bioavailability.
Gupta, A; Kumar, S; Mishra, CK; Singh, S, 2021
)
0.62
"Improved bioavailability of Aceclofenac (ACE) may be achieved through proniosomes, which are considered as one of the most effective drug delivery systems and are expected to represent a valuable approach for the development of better oral dosage form as compared to the existing product."( Effect of Different Carriers on In Vitro and In Vivo Drug Release Behavior of Aceclofenac Proniosomes.
Chatterjee, B; Saleh, MSM; Sammour, RMF; Shahiwala, A; Taher, M, 2021
)
0.62
" Moreover, the relative oral bioavailability of proniosomes with maltodextrin and glucose as carriers compared to the pure drug was 183% and 112%, respectively."( Effect of Different Carriers on In Vitro and In Vivo Drug Release Behavior of Aceclofenac Proniosomes.
Chatterjee, B; Saleh, MSM; Sammour, RMF; Shahiwala, A; Taher, M, 2021
)
0.62
" Our pharmacogenomic findings supported the suspicion that ADRs, most notably the multi-organ toxicity experienced by our patient, may be owed to drug-drug-gene interactions and increased bioavailability of the prescribed drugs due to slower detoxification capacity and decreased hepatic and renal elimination."( Drug-drug-gene interactions as mediators of adverse drug reactions to diclofenac and statins: a case report and literature review.
Borić Bilušić, A; Božina, N; Božina, T; Domjanović, IK; Fistrek Prlić, M; Ganoci, L; Gvozdanović, K; Križ, T; Laganović, M; Simičević, L, 2021
)
0.86
"1% is a commonly used NSAID with well-documented clinical efficacy in reducing postoperative inflammation; however, its corneal tolerability and ophthalmic tissue bioavailability require further improvement."( Design of ophthalmic micelles loaded with diclofenac sodium: effect of chitosan and temperature on the block-copolymer micellization behaviour.
Dodov, MG; Geskovski, N; Gorachinov, F; Goracinova, K; Koummich, SA; Makreski, P; Zoukh, IM, 2022
)
0.99
"Skin sampling by tape stripping measures the local bioavailability of topical drug products in the stratum corneum (SC)."( Investigator Impact on Reproducibility of Drug Bioavailability in Stratum Corneum Sampling by Tape Stripping.
Bunge, AL; Hassan, HE; Shukla, S; Stinchcomb, AL, 2022
)
0.72
" Therefore, a drug's binding to SA is especially important for its bioavailability and it is a key problem in the drug design process."( Structural Investigation of Diclofenac Binding to Ovine, Caprine, and Leporine Serum Albumins.
Bujacz, A; Talaj, JA; Zielinski, K, 2023
)
1.2
" The bioavailability and inhibitory activity of UADs against UA-glucuronidation were evaluated using differentiated Caco-2 cell monolayers."( Urolithin A conjugation with NSAIDs inhibits its glucuronidation and maintains improvement of Caco-2 monolayers' barrier function.
Granica, S; Korczak, M; Piwowarski, JP; Popowski, D; Roszkowski, P; Skowrońska, W; Żołdak, KM, 2023
)
0.91

Dosage Studied

An innovative simple, fast, precise and accurate ultra-high performance liquid chromatography (UPLC) method was developed. In common with other fixed combination products, dosage flexibility is somewhat compromised with diclofenac/misoprostol.

ExcerptRelevanceReference
" Clofezone was given at a daily dosage of 1200 mg during the first week and 600 mg during the second week; the corresponding dosages of diclofenac were 150 mg and 75 mg."( Comparison of clofezone and diclofenac in the treatment of out-patients suffering from activated (painful) osteoarthrosis.
Brackertz, D,
)
0.63
"In a double-blind, crossover study conducted in ten hospitalised patients suffering from active rheumatoid arthritis, the anti-inflammatory effect of diclofenac sodium (Voltaren) in a daily dosage of 125 mg was compared with that of placebo under strictly standardised conditions."( A study of the anti-inflammatory effect of Voltaren in patients with rheumatoid arthritis.
Bijlsma, A; ten Pas, JG, 1978
)
0.46
"A report is given on a long-term controlled trial in which diclofenac sodium (Voltaren) was compared with indomethacin in 36 patients with rheumatoid arthritis, both drugs being administered in a dosage of 75-125 mg daily."( The long-term efficacy and tolerability of Voltaren (diclofenac sodium) and indomethacin in rheumatoid arthritis.
Bijlsma, A, 1978
)
0.75
" Clinical parameters showed that the best degree of improvement was obtained with the diclofenac 50 mg twice-daily dosage regime."( Comparative clinical trials with diclofenac sodium (Voltarol) and naproxen in rheumatic conditions: investigation of possible changes in diclofenac dose and dose interval.
Bach, GL, 1979
)
0.76
" Dosage was one tablet (25 mg diclofenac) three times daily during the first week."( Diclofenac (Voltarol) in rheumatoid arthritis: a report of a double-blind trial.
Boardman, PL; Doreen, MS; Fowler, PD; Poole, PH, 1979
)
1.99
", with subsequent dosage adjustments according to response."( An open assessment of the efficacy and tolerability of diclofenac sodium (Voltarol) in patients with rheumatic disease and a comparative study of diclofenac sodium (Voltarol) with indomethacin in patients with osteoarthritis and rheumatoid arthritis.
Cash, HC; McMahon, MF, 1979
)
0.51
" The degree of gastric or intestinal irritation seen with dosing of other drugs was as follows; indomethacin greater than diclofenac Na greater than ibuprofen greater than aspirin greater than phenylbutazone or indomethacin greater than CH-800 = diclofenac Na greater than ibuprofen greater than phenylbutazone, respectively."( [Irritative activity of a new anti-inflammatory agent 4-(p-chorophenyl)-2-phenyl-5-thiazoleacetic acid (CH-800) on the gastrointestinal tract in rats (author's transl)].
Ohtsuki, H; Okabe, S; Tabata, K, 1979
)
0.47
" The daily maintenance dosage from the fourth week of treatment onwards was 75 mg diclofenac and 500 mg naproxen."( [Long-term comparative study: diclofenac (voltaren) and naproxen (proxen) in arthritis].
Placheta, P; Siegmeth, W, 1978
)
0.77
" The employment of a special diet favourably influenced the course of the disease and enabled the dosage of antirheumatic drugs to be reduced, thereby reducing the frequency of side-effects of the drugs."( On the medicinal efficacy of dietetic therapy in patients with rheumatoid arthritis.
Denissov, LN; Samsonov, MA; Sharafetdinov, Kh, 1992
)
0.28
" However, these results do not favor vidarabine dosage supplementation in this indication because the duration of PE is less than 8 per cent of a daily administration period."( Diclofenac, paracetamol, and vidarabine removal during plasma exchange in polyarteritis nodosa patients.
Fauvelle, F; Guillevin, L; Leon, A; Nicolas, P; Perret, G; Petitjean, O; Tod, M,
)
1.57
" The present study was undertaken to assess the pharmacokinetics of the drug after iv and gastrointestinal dosing to rats."( Pharmacokinetics and bioavailability of diclofenac in the rat.
Aristorena, JC; Garcia-Carbonell, MC; Peris-Ribera, JE; Pla-Delfina, JM; Torres-Molina, F, 1991
)
0.55
" The four NSAID diclofenac, acemetacin, ibuprofen, and mefenamic acid administered to healthy volunteers at the recommended dosage led to significant suppression of thromboxane synthesis; this effect was more pronounced with acemetacin and ibuprofen than with diclofenac."( [Inhibition of thrombocyte function by non-steroidal anti-rheumatic agents: a comparative study between diclofenac, acemetacin, mefenamic acid and ibuprofen].
Raineri-Gerber, I; von Felten, A, 1991
)
0.84
" The coculture of indomethacin with interleukin-2 (IL-2) augmented LAK cell activity in an indomethacin dose-response manner, and diminished PGE2 content in the corresponding culture supernatant in a reverse dose-response manner."( Prostaglandin E2 from macrophages of murine splenocyte cultures inhibits the generation of lymphokine-activated killer cell activity.
Chu, TM; Lin, TH; Nakajima, I; Ohnishi, H, 1991
)
0.28
"Repeat oral dosing of nabumetone for 1 month maintains anti-inflammatory efficacy in a carrageenan model of paw oedema yet does not cause gastrointestinal damage."( Anti-inflammatory efficacy and gastrointestinal irritancy: comparative 1 month repeat oral dose studies in the rat with nabumetone, ibuprofen and diclofenac.
Blower, PR; Gentry, C; Melarange, R; O'Connell, C, 1991
)
0.48
" The dose-response curve of SNP was shifted to the right, and the relaxation to verapamil was slightly reduced."( Endothelium-derived relaxing factor influences renal vascular resistance.
Förstermann, U; Frölich, JC; Radermacher, J, 1990
)
0.28
" But considering that the application of NSAIDs is frequently associated with side effects, a reduction of dosage would be to the patient's benefit."( [Reduced diclofenac administration by B vitamins: results of a randomized double-blind study with reduced daily doses of diclofenac (75 mg diclofenac versus 75 mg diclofenac plus B vitamins) in acute lumbar vertebral syndromes].
Koehler, CO; Kuhlwein, A; Meyer, HJ, 1990
)
0.7
" Further, changes in plasma levels of the drug from other dosage forms were related to changes in pH environment as determined by the HC."( Application of radiotelemetric technique in evaluating diclofenac sodium absorption after oral administration of various dosage forms in healthy volunteers.
Chan, KK; John, VA; Mojaverian, P; Ziehmer, BA, 1990
)
0.53
"A phamacokinetic study in man has been made of a new dosage form of diclofenac hydroxyethylpyrrolidine (DIEP); soluble salt packed in sachets was compared with diclofenac sodium as enteric coated tablets."( Comparative bioavailability of diclofenac hydroxyethylpyrrolidine vs diclofenac sodium in man.
Lualdi, P; Maggi, CA; Mautone, G, 1990
)
0.8
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of diclofenac sodium are reviewed."( Diclofenac sodium.
Small, RE, 1989
)
1.94
" Gastroscopy was performed at base-line after the dosing period of 14 days and again after a follow-up period of 14 days without any treatment."( [Gastroduodenal tolerance of tenoxicam versus diclofenac-Na: an endoscopy double-blind controlled study in healthy probands].
Dammann, HG; Marinis, E; Müller, P; Simon, B,
)
0.39
" Gastric tolerance was assessed by endoscopy, which was performed at base-line, after the 14 day dosing period and after a 14 day follow-up period without treatment."( Comparison of the gastroduodenal tolerance of tenoxicam and diclofenac Na. A double-blind, endoscopically controlled study in healthy volunteers.
Dammann, HG; Leucht, U; Müller, P; Simon, B, 1989
)
0.52
" To ensure the human therapeutic dose, each drug was given twice a day per os in 3 different dosage regimes."( Impact of NSAIDS on murine antigen induced arthritis. I. Investigation of antiinflammatory and chondroprotective effects.
de Vries, BJ; van den Berg, WB, 1989
)
0.28
" Animals given dexamethasone were divided into three groups and the drug was administered at a constant dosage of 2 mg/kg: (a) 2 days, 1 day, and 3 h intraperitoneally before (chronic pretreatment), (b) 3 h intraperitoneally before (acute pretreatment), and (c) 5 min intravenously and 6 h and 1 day intraperitoneally after (chronic posttreatment) induction of ischemia."( Chronic dexamethasone pretreatment aggravates ischemic neuronal necrosis.
Koide, T; Siesjö, BK; Wieloch, TW, 1986
)
0.27
"ml-1 for A and B, respectively) or to the lag time between dosing and the appearance of the drug in serum (1."( Comparative bioavailability and in vitro characterization of two brands of diclofenac sodium enteric-coated tablets.
Abdulhameed, M; el-Sayed, Y; Hasan, M; Muti, H; Najib, N; Suleiman, MS, 1988
)
0.51
" Conveniently, dosage adjustments are not required in the elderly or in those patients with renal or hepatic impairment."( Diclofenac sodium. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Sorkin, EM; Todd, PA, 1988
)
1.72
"Plasma and knee joint synovial fluid (SF) concentration of diclofenac sodium and its hydroxylated metabolites were measured after chronic dosing with the 100 mg polymer matrix formulation."( Plasma and synovial fluid concentrations of diclofenac sodium and its hydroxylated metabolites during once-daily administration of a 100 mg slow-release formulation.
Dawes, PT; Fowler, PD; John, VA; Shotton, PA, 1986
)
0.78
" We conclude that the proposed dosage (in the selected patient population) constitutes effective antipyretic treatment devoid of major side effects."( Antipyretic therapy in ICU patients: evaluation of low dose diclofenac sodium.
Basilico, E; Grossi, E; Pesenti, A; Riboni, A, 1986
)
0.51
" The study indicates that visual analogue scales may also be useful in assessment of swelling and that Voltaren in a fixed dosage offers a promising alternative against postoperative pain and swelling."( Voltaren as an analgesic after surgical removal of a lower wisdom tooth.
Henrikson, PA; Thilander, H; Wåhlander, LA, 1985
)
0.27
" Another advantage of piroxicam is its low effective dosage level achieved by a single daily dose."( [Treatment of rheumatoid arthritis. Open parallel study with the non-steroidal antirheumatics piroxicam and diclofenac].
Rohde, J; Schwegler, F; Standel, W, 1980
)
0.47
" For this the dosage of diclofenac was reduced to 100 mg/d."( Diclofenac and piroxicam in a double-blind trial results and methodological problems. Working Party of the Society for Rheumatology of the GDR for the Testing of Anti-rheumatic Drugs.
Friedländer, R; Häntzschel, H; Hüge, W; Keitel, W; Keysser, M; Seidel, W; Tanner, E; Wächter, G; Weber, J; Wille, R, 1984
)
2.02
" To define the relationship between OT sensitivity and uterine PG production, we measured uterine sensitivity to OT by a quantitative dose-response procedure in rats on Days 19, 20, 21 and 22 of pregnancy and monitored uterine and placental tissue concentrations of PGF2 alpha and PGE2."( Uterine and placental prostaglandins and their modulation of oxytocin sensitivity and contractility in the parturient uterus.
Chan, WY, 1983
)
0.27
" Diclofenac was detected in synovial fluid 2 h after dosing but at a lower level than in plasma."( Plasma and synovial fluid concentrations of diclofenac sodium and its major hydroxylated metabolites during long-term treatment of rheumatoid arthritis.
Crook, PR; Fowler, PD; John, VA; Shadforth, MF, 1983
)
1.44
" For diclofenac, indometacin and piroxicam proposals for a more rational procedure of their dose-response relationship determination are discussed."( [Transsynovial kinetics and correlation of dosage and effect of non-steroidal anti-rheumatic agents].
Fenner, H, 1982
)
0.78
" In a comparison of two non-steroidal anti-inflammatory agents in this condition we attempted to overcome the difficulties by using a run-in period during which the dosage of one of the trial drugs was adjusted to suit the individual patient."( The run-in period in trial design: a comparison of two non-steroidal anti-inflammatory agents in psoriatic arthropathy.
Bird, HA; Fowler, PD; Leatham, PA; Wright, V, 1982
)
0.26
" After intravenous dosing both plasma levels and areas under curves were significantly reduced although none of the rate constants was affected."( A study of the effect of aspirin on the pharmacokinetics of oral and intravenous diclofenac sodium.
Jack, DB; Kendall, MJ; Willis, JV, 1980
)
0.49
" Six subjects then took part in a study involving single and repeated dosing under fasting and non-fasting conditions."( The influence of food on the absorption of diclofenac after single and multiple oral doses.
Jack, DB; Kendall, MJ; Willis, JV, 1981
)
0.53
" Statistical analysis of the excretion of diclofenac and its metabolites showed that, during chronic administration, absorption was not significantly influenced by dosing before or after food."( The influence of food on the absorption of diclofenac as determined by the urinary excretion of the unchanged drug and its major metabolites during chronic administration.
Jack, DB; John, VA; Kendall, MJ; Willis, JV, 1981
)
0.79
" An overestimation of rare side-effects of drugs should not block the application of certain medicaments, however, they should be given only in such a high dosage as it is necessary."( [Hematotoxic lesions caused by non-steroidal antirheumatic agents].
Hüge, W; Stobbe, H, 1980
)
0.26
" On therapeutic dosing of mice daily with HYAL EX-0001 from day 7 after induction of the granulomatous tissue, the granulomatous tissue development was dramatically reduced from 111."( Angiostasis and vascular regression in chronic granulomatous inflammation induced by diclofenac in combination with hyaluronan in mice.
Alam, CA; Seed, MP; Willoughby, DA, 1995
)
0.52
" Intestinal permeability was measured in rats given diclofenac either by sc bolus or iv infusion and dose-response data compared."( Concentration-response relationships for three nonsteroidal anti-inflammatory drugs in the rat intestine.
Ford, J; Houston, JB, 1995
)
0.54
"To determine the mode of protective effects of misoprostol against the chronic gastrointestinal ulceration from the NSAID, diclofenac, studies were undertaken in domestic pigs, a model of human gastrointestinal ulceration, to determine (1) the effects of repeated daily dosing for 10 days of diclofenac 5 mg/kg/day twice a day (as Voltaren tablets) on the gastrointestinal morphology, 59fe-red blood loss, mucosal myeloperoxidase (MPO) activity (as an indicator of leukocyte infiltration), and mucosal leukotrienes (LTS); and (2) the mucosal protective effects of 10-40 micrograms/kg/day misoprostol twice a day (as Cytotec tablets) given with diclofenac 5 mg/kg/day twice a day compared with diclofenac 5 mg/kg/day alone and aspirin 150 mg/kg/twice a day (USP tablets) as a standard."( Chronic effects of misoprostol in combination with the NSAID, diclofenac, on gastrointestinal tract of pigs. Relation to diarrheagenic activity, leukocyte infiltration, and mucosal leukotrienes.
Perkins, WE; Rainsford, KD; Stetsko, PI, 1995
)
0.74
"We have treated 10 patients suffering from kala-azar in Brazil with Amphocil (amphotericin B cholesterol dispersion) at a dose of 2 mg/kg/d for 5 d, following an earlier study in which this dosage for 7 d was found to cure all of 9 patients, with no relapse during 12 months."( Treatment of kala-azar in Brazil with Amphocil (amphotericin B cholesterol dispersion) for 5 days.
Brito, EF; Dember, J; Dietze, R; Fagundes, SM; Feitosa, TF; Fonschiffrey, G; Ksionski, G; Milan, EP; Suassuna, FA,
)
0.13
" Patients were then randomised to receive a diclofenac 50mg/misoprostol 200 micrograms fixed combination tablet (n = 331) or diclofenac 50mg (n = 339) for 8 weeks at the same dosage frequency as in the open-label phase."( Efficacy of diclofenac/misoprostol vs diclofenac in the treatment of ankylosing spondylitis.
McKenna, F, 1993
)
0.93
"The pharmacokinetics of a new diclofenac/misoprostol combination dosage form have been investigated."( Pharmacokinetics of diclofenac and misoprostol when administered alone or as a combination product.
Karim, A, 1993
)
0.9
" and rectal dosage of 50 mg diclofenac sodium and was found to be highly suitable for routine analyses."( A new rapid and sensitive high-performance liquid chromatographic assay for diclofenac in human plasma.
Hanses, A; Mutschler, E; Spahn-Langguth, H, 1995
)
0.81
"In the dosage used, diclofenac was as effective an anti-inflammatory agent for uncomplicated post-cataract inflammation as prednisolone."( A comparison of topical diclofenac with prednisolone for postcataract inflammation.
Brennan, KM; Roberts, CW, 1995
)
0.92
" Analgesic and antiinflammatory activity and good tolerance of three dosage forms (tablets, suppositories, ampoules) of diclonate P were established on a statistically significant basis."( [Diclonate P in rheumatoid arthritis].
Alekberova, ZS; Balabanova, RM; Chichasova, NV; Ivanova, MM; Nasonov, EL; Tsvetkova, ES, 1994
)
0.29
" The administered dosage was 10 mg every 6 h for ketorolac and 50 mg every 8 h for diclofenac sodium."( Ketorolac versus diclofenac sodium in cancer pain.
Corli, O; De Conno, F; Gallucci, M; Piva, L; Speranza, R; Tamburini, M; Toscani, F; Ventafridda, V, 1994
)
0.85
"The aim of this study was the assessment of blood and synovial levels of diclofenac after repeated epicutaneous dosing with DHEP plasters in patients with joint effusion."( Pharmacokinetics of diclofenac hydroxyethylpyrrolidine (DHEP) plasters in patients with monolateral knee joint effusion.
Gallacchi, G; Marcolongo, R, 1993
)
0.84
" The significance of the results is discussed with reference to the dosage and timing of analgesia and to nursing practice."( Pain relief after major gynaecological surgery.
Cashman, JN; Hennessy, D; Lovett, PE; Stanton, SL,
)
0.13
"Nitric oxide synthase(NOS) inhibitor,N omega-nitro-L-arginine methyl ester (L-NAME, 10-300 mg/kg) and L-NG-monomethyl-arginine (L-NMMA, 30-300 mg/kg) suppressed the swellings of adjuvant-injected paw of rats (25-54%) at day 2 and 8 when dosed intraperitoneally and orally for 4 days from day -1 to day 2 after adjuvant."( Nitric oxide and superoxide radical are involved in both initiation and development of adjuvant arthritis in rats.
Oyanagui, Y, 1994
)
0.29
" The importance of systemically mediated damage was further determined by gastrotoxicity dose-response curves and pyloric ligation experiments in which indomethacin was administered either orally or parenterally, or into stomach or duodenum with the pylorus occluded."( Gastric mucosal damage induced by nonsalicylate nonsteroidal antiinflammatory drugs in rats is mediated systemically.
Giraud, AS; Skeljo, MV; Yeomans, ND, 1993
)
0.29
" The two products were not found to be statistically different with respect to the lag time between dosing and appearance of the drug in the serum (0."( A comparative bioavailability study on two sustained-release formulations of diclofenac sodium following a single dose administration.
Hasan, MM; Muti, H; Najib, NM, 1993
)
0.51
"Pursuant to anecdotal case reports of a possible drug-drug interaction between cyclosporine and diclofenac, an open, two-period crossover study in 24 healthy male volunteers was undertaken in which a single oral dose of 300 mg cyclosporine was administered alone and on day 8 of multiple oral dosing of 50 mg diclofenac every 8 hours."( Pharmacokinetics of cyclosporine and multiple-dose diclofenac during coadministration.
Hitzenberger, G; Johnston, A; Koelle, EU; Kovarik, JM; Merdjan, H; Mueller, EA, 1993
)
0.76
" Serial blood samples were obtained for up to 12 hr after dosing and drug levels were determined by validated HPLC methods."( Application of dual radiotelemetric technique in studying drug-drug interaction between diclofenac sodium and ranitidine HCl in volunteers.
Alioth, C; Blum, RA; Chan, KK; D'Andrea, DT; Kochak, GM; Schentag, JJ; Teng, L; Ziehmer, BA, 1993
)
0.51
"Bioavailability Study of Enteric Coated Diclofenac Formulations/1st Communication: Bioavailability study following single-dose administration of a multiple-unit formulation compared with a single-unit formulation Relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after single-dose administration of an enteric coated multiple-unit formulation (Diclo-Puren 50, test) in comparison to a single-unit dosage form (reference)."( [Biological availability of gastric juice-resistant coated diclofenac preparations. 1. Bioavailability study following a single administration of a multiple-unit formulation in comparison with a single-unit formulation].
Babej-Dölle, RM; Blume, H; Scheidel, B; von Nieciecki, A; Walter, K, 1993
)
0.8
"Diclofenac/misoprostol at twice daily dosing is associated with significantly fewer gastroduodenal ulcers than either piroxicam or naproxen."( Double-blind comparison of efficacy and gastroduodenal safety of diclofenac/misoprostol, piroxicam, and naproxen in the treatment of osteoarthritis.
Bruyn, GA; Geis, GS; Melo Gomes, JA; Roth, SH; Woods, EM; Zeeh, J, 1993
)
1.97
" Dosage increases were permitted after a 2-week trial period."( Efficacy of nabumetone versus diclofenac, naproxen, ibuprofen, and piroxicam in osteoarthritis and rheumatoid arthritis.
DeLapp, RE; Lister, BJ; Poland, M, 1993
)
0.57
" Other significant factors contributing to an increase in SGOT concentrations were duration of therapy and, perhaps, daily dosage (mg/lb)."( Differential effects of diclofenac and aspirin on serum glutamic oxaloacetic transaminase elevations in patients with rheumatoid arthritis and osteoarthritis.
Anderson, W; Furst, DE, 1993
)
0.59
" It was also demonstrable after subcutaneous dosing or when injury was measured by a change in mucosal potential difference."( Gastric mucosal adaptation to diclofenac injury.
Cook, GA; Elliott, SL; Giraud, AS; Skeljo, MV; Yeomans, ND, 1996
)
0.58
" In common with other fixed combination products, dosage flexibility is somewhat compromised with diclofenac/misoprostol."( Diclofenac/misoprostol. A review of its pharmacology and therapeutic efficacy in painful inflammatory conditions.
Davis, R; Goa, KL; Yarker, YE, 1995
)
1.95
" The remaining patients (group A, n = 10) were given diclofenac in a dosage of 150 mg per day for three days then 75 mg per day for three days."( Corticosteroid therapy for the treatment of acute attacks of crystal-induced arthritis: an effective alternative to nonsteroidal antiinflammatory drugs.
Gabay, C; Vischer, TL; Werlen, D, 1996
)
0.54
"Adaptation is the name given to the progressive decrease in gastric mucosal damage following repeated dosing with damaging agents."( Adaptation of the gastric epithelium to injury is maintained in vitro and is associated with increased TGF-alpha expression.
Doljanin, K; Giraud, AS; Skeljo, MV; Yeomans, ND, 1996
)
0.29
" This seems to be caused by a slow release from the dosage form or dissolution of the drugs, which is confirmed by a longer MITtot compared to the MRTsys in most of the volunteers."( Pharmacokinetics and drug input characteristics for a diclofenac-codeine phosphate combination following oral and rectal administration.
Hanses, A; Meiss, F; Mutschler, E; Spahn-Langguth, H, 1996
)
0.54
", was given during the second week of each dosage regimen after three endoscopic biopsies had been taken from each of the duodenum, antrum and corpus."( Effects of misoprostol on healing and prevention of biopsy-induced gastroduodenal lesions occurring during the administration of diclofenac to volunteers.
Armstrong, D; Blum, AL; Dorta, G; Margalith, D; Nicolet, M; Saraga, E; Vouillamoz, D, 1996
)
0.5
") diclofenac followed by oral dosing in patients with acute lumbago."( The efficacy and tolerability of an 8-day administration of intravenous and oral meloxicam: a comparison with intramuscular and oral diclofenac in patients with acute lumbago. German Meloxicam Ampoule Study Group.
Colberg, K; Degner, FL; Hettich, M; Sigmund, R, 1996
)
1.22
" Injectable microspheres and in situ gel-forming implant systems of PLG (50:50) copolymer may therefore be considered as prospective implantable controlled-release dosage forms to deliver drugs in long-term therapy of chronic ailments."( Biodegradable injectable implant systems for long term drug delivery using poly (lactic-co-glycolic) acid copolymers.
Chandrashekar, G; Udupa, N, 1996
)
0.29
" A significant analgesic effect was obtained within two weeks of treatment with 150mg diclofenac daily; this improvement was maintained on reduction of the dosage to 75-100mg over the next ten weeks."( Comparative efficacy and tolerability of two diclofenac formulations in the treatment of painful osteoarthritis.
Bakshi, R, 1996
)
0.78
"In this study, in vitro characterization, bioavailability and pharmacokinetics of 2 different sustained-release diclofenac sodium dosage forms were compared, Voltaren (100 mg tablets), manufactured by Ciba-Geigy and Inflaban (100 mg enteric-coated tablets), manufactured by the Arab Pharmaceutical Manufacturing Company."( Bioavailability and pharmacokinetic properties of 2 sustained-release formulations of diclofenac sodium, Voltaren vs inflaban: effect of food on inflaban bioavailability.
Deleq, S; Hasan, M; Najib, N; Sallam, E; Shubair, M; Zmeili, S, 1996
)
0.73
"Taking into account the limited improvement noted over rest and cast immobilization and the number of associated adverse events, it is difficult to recommend the use of diclofenac in the treatment of lateral epicondylitis at the dosage used in this study."( Efficacy of diclofenac in lateral epicondylitis of the elbow also treated with immobilization. The University of Montreal Orthopaedic Research Group.
Guibert, R; Labelle, H,
)
0.7
"A new oral dosage form of diclofenac sodium, enabling the single administration of the daily dose of 150 mg, has been tested for treatment of 20 patients suffering from osteoarthritis of the spine."( Effective treatment of osteoarthritis with a 150 mg prolonged-release of diclofenac sodium.
Andreotti, L; Arcangeli, P; Palazzini, E,
)
0.66
" After achieving adequate analgesia with regular dosing of oral methadone (T1), patient-controlled analgesia with methadone was administered for 3 days (T2)."( Opioid-sparing effect of diclofenac in cancer pain.
Barresi, L; Caligara, M; Dardanoni, G; Mercadante, S; Sapio, M; Serretta, R, 1997
)
0.6
" IB showed a dose-response relationship which appeared to plateau at doses of 50 and 100 mg/kg."( Effects of the combined oral administration of NSAIDs and dextromethorphan on behavioral symptoms indicative of arthritic pain in rats.
Caruso, FS; Frenk, H; Lu, J; Mao, J; Mayer, DJ; Price, DD, 1996
)
0.29
" The dose-response curves were first obtained for each drug alone."( Isobolographic analysis of interactions between intravenous morphine, propacetamol, and diclofenac in carrageenin-injected rats.
Benoist, JM; Fletcher, D; Gautron, M; Guilbaud, G, 1997
)
0.52
" Dosage adjustments for the elderly, children or for patients with various disease states (such as hepatic disease or rheumatoid arthritis) may not be required."( Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls.
Anderson, KE; Davies, NM, 1997
)
0.59
"Some adaptation occurred in over 90% of subjects after 4 weeks dosing with an NSAID, but adaptation was less frequent in older subjects and in smokers."( The influence of age, gender, Helicobacter pylori and smoking on gastric mucosal adaptation to non-steroidal anti-inflammatory drugs.
Campbell, F; Lipscomb, GR; Rees, WD, 1997
)
0.3
"To assess the possible therapeutic effect of 40 mg sublingual piroxicam (fast-dissolving dosage form, FDDF) compared with intramuscular 75 mg diclofenac, as a reference drug, on acute renal colic in a randomized, double-blind controlled clinical trial."( Piroxicam fast-dissolving dosage form vs diclofenac sodium in the treatment of acute renal colic: a double-blind controlled trial.
Echarte, JL; Gelabert, A; Iglesias, ML; Mínguez, S; Nogués, X; Pedro-Botet, J; Supervía, A, 1998
)
0.77
"Cross-linked high amylose starches have been developed as excipients for the formulation of controlled-release solid dosage forms for the oral delivery of drugs."( Cross-linked high amylose starch for controlled release of drugs: recent advances.
Cartilier, L; Chouinard, F; Dumoulin, Y; Lenaerts, V; Marchessault, R; Mateescu, MA; Mebsout, F; Moussa, I; Szabo, P, 1998
)
0.3
"Diclofenac, naproxen, and piroxicam can be administered together with omeprazole 20 mg daily without need for dosage alteration."( Lack of drug-drug interaction between three different non-steroidal anti-inflammatory drugs and omeprazole.
Andersson, T; Bredberg, E; Lagerström, PO; Naesdal, J; Wilson, I, 1998
)
1.74
" The rare but severe complications preclude further use of the intramuscular dosage in view of the availability of oral alternatives."( [Erythema and fever after diclofenac i.m].
Schaad, HJ; Zürcher, RM, 1998
)
0.6
" This suggests a continuous delivery of [14C]-diclofenac sodium from the lotion into and through skin which only ceased when the dosing site was washed."( In vivo bioavailability and metabolism of topical diclofenac lotion in human volunteers.
Hewitt, PG; Hui, X; Maibach, HI; Poblete, N; Shainhouse, JZ; Wester, RC, 1998
)
0.81
" Both formulations are, therefore, in compliance with the USP requirements for release from enteric-coated dosage forms."( Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads.
el-Mahrouk, GM; Gouda, MW; Hosny, EA, 1998
)
0.55
"05) DS:(EC + CS) solid dispersion was prepared and developed into a capsule dosage from, using lactose as diluent."( Development of diclofenac sodium controlled release solid dispersion powders and capsules by freeze drying technique using ethylcellulose and chitosan as carriers.
Dangprasirt, P; Pongwai, S, 1998
)
0.65
" Following a dosage increase to 150 microg/day, she suffered from an acute attack of pseudogout."( Pseudogout attack associated with chronic thyroiditis and Sjögren's syndrome.
Arai, S; Hama, Y; Kondo, T; Mineshita, M; Warabi, H; Yasuda, H, 1999
)
0.3
" The usual oral dosage of aceclofenac is 100 mg twice daily in adults."( [Pharma-clinics. The drug of the month. Aceclofenac (Biofenac)].
Scheen, AJ, 1999
)
0.3
" Dose-response relationships show that higher doses of ibuprofen may be particularly effective."( Postoperative analgesia and vomiting, with special reference to day-case surgery: a systematic review.
McQuay, HJ; Moore, RA, 1998
)
0.3
"Multiple unit dosage forms for oral delivery of bioactive agents offer many advantages over single unit products (e."( In vitro release modulation from crosslinked pellets for site-specific drug delivery to the gastrointestinal tract. I. Comparison of pH-responsive drug release and associated kinetics.
Fassihi, R; Pillay, V, 1999
)
0.3
"98 per patient depending on the dosage of diclofenac used."( Economic evaluation of nimesulide versus diclofenac in the treatment of osteoarthritis in Greece.
Diamantopoulos, E; Ifandi, G; Ignatiades, T; Katostaras, F; Liaropoulos, L; Spinthouri, M, 1998
)
0.83
" Blood samples were taken before and up to 6 h after dosing and the plasma obtained from it was tested for its ability to inhibit prostanoid formation in IL-1beta-treated A549 cells (COX-2 system) and human washed platelets (COX-1 system)."( Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs.
Giuliano, F; Warner, TD, 1999
)
0.3
" Secondary analyses showed that diclofenac-potassium provided significant pain relief from 60 min after dosing and for all remaining endpoints in the 8-h observation period."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.8
"5 mg rofecoxib, 25 mg rofecoxib, 400 mg ibuprofen, or placebo and the mean +/- SE change in oral temperature at 4 hours after dosing was -0."( Cyclooxygenase-2 inhibition by rofecoxib reverses naturally occurring fever in humans.
Adcock, S; Bachmann, KA; Chan, CC; Cohen, RA; Davidson, MH; Dobratz, D; Gertz, BJ; Grasing, K; Hedges, J; Jones, TM; McBride, KJ; Moritz, C; Mukhopadhyay, S; Schwartz, JI, 1999
)
0.3
"The use of natural polymers for design of dosage form has received considerable attention recently, especially from the safety point of view."( Aging phenomena of chitosan and chitosan-diclofenac sodium system detected by low-frequency dielectric spectroscopy.
Bak, GW; Bodek, KH, 1999
)
0.57
" dosing to rats, telmisartan 1-O-acylglucuronide was rapidly cleared from plasma with a clearance of 180 ml/min/kg, compared with 15."( Disposition and chemical stability of telmisartan 1-O-acylglucuronide.
Beschke, K; Ebner, T; Heinzel, G; Prox, A; Wachsmuth, H, 1999
)
0.3
"Postoperative renal dysfunction in rats is induced by ketorolac dosed concurrently with gentamicin."( Renal dysfunction associated with the perioperative use of diclofenac.
Cousins, MJ; Eckstein, RP; Jordan, V; Kim, H; Lin, Y; Mather, LE; Power, I; Xu, M, 1999
)
0.55
" This produced a dosage form with a high intraparticulate porosity in the dry state."( Tablet and capsule hydrophilic matrices based on heterodisperse polysaccharides having porosity-independent in vitro release profiles.
Kelly, ML; Staniforth, JN; Tobyn, MJ, 2000
)
0.31
" Timed plasma concentrations of diclofenac during a 12-h-period after dosing were measured by means of HPLC with UV detection at 275 nm and a quantification limit of 10 ng/ml; the method was fully validated for pharmacokinetic purposes."( Pharmacokinetics of diclofenac after oral administration of its potassium salt in sachet and tablet formulations.
Abbondati, G; Ceppi Monti, N; Crivelli, F; Dal Bo, L; Ismaili, S; Marzo, A; Tettamanti, RA; Uhr, MR; Verga, F, 2000
)
0.91
" Nevertheless, many commercially available pharmaceutical dosage forms have no protective coat to avoid the inactivation in the gastric juices."( Analysis of diclofenac sodium and derivatives.
Ballesteros, MP; Frutos, P; Palomo, ME, 1999
)
0.68
" Applicability of the proposed methods was examined by analysing dosage forms of the investigated drugs."( Spectrophotometric and spectrofluorimetric determination of etodolac and aceclofenac.
El Kousy, NM, 1999
)
0.3
" In this present study, it was aimed to prepare microsphere formulations of DS using a natural biodegradable polymer as a carrier for intraarticular administration to extend the duration period of the dosage form in the knee joint."( In vitro and in vivo evaluation of diclofenac sodium loaded albumin microspheres.
Caliş, S; Ercan, MT; Hincal, AA; Kaş, HS; Peksoy, I; Tunçay, M,
)
0.41
" In contrast, the small intestines in old rats of both genders given the 50 mg/kg dosage had >30% fewer ulcers and a fourfold decrease in area of ulceration compared to young rats."( Aging enhances susceptibility of diclofenac-treated rats to gastric ulceration, while attenuating enteropathy.
Atchison, CR; Balakumaran, A; Hoffmann, WE; Treinen-Moslen, M; West, AB, 2000
)
0.59
" Systematic studies on SCI-induced alterations are thus required to provide information leading to a rational dosing regimen design for SCI patients."( Bioavailability of diclofenac after intramuscular administration to rats with experimental spinal cord injury.
García-López, P; Salas, R, 1999
)
0.63
"The incidence of all adverse events was lower at each dosage of meloxicam than for diclofenac but greater than for placebo."( Safety and efficacy of meloxicam in the treatment of osteoarthritis: a 12-week, double-blind, multiple-dose, placebo-controlled trial. The Meloxicam Osteoarthritis Investigators.
Caldwell, J; Dalgin, P; Fleischmann, R; Hall, D; Roszko, P; Yocum, D, 2000
)
0.53
"Rofecoxib is effective in treating OA with once-daily dosing for 6 weeks and 1 year."( Rofecoxib, a new cyclooxygenase 2 inhibitor, shows sustained efficacy, comparable with other nonsteroidal anti-inflammatory drugs: a 6-week and a 1-year trial in patients with osteoarthritis. Osteoarthritis Studies Group.
Bolognese, J; Daniels, B; DeTora, L; Fisher, C; Saag, K; Samara, A; Sperling, R; van der Heijde, D,
)
0.13
"8 mg), CPK activity was shown to depend on both the type of dosage form and, in the case of nanocapsules, on the chemical nature of the central oily core."( Poly(rac-lactide) nanocapsules containing diclofenac: protection against muscular damage in rats.
Barratt, G; Devissaguet, JP; Fessi, H; Guterres, SS; Puisieux, F, 2000
)
0.57
"A known impurity is formed in the production of a parenteral dosage form of diclofenac sodium if terminally sterilized by autoclave."( Diclofenac sodium injection sterilized by autoclave and the occurrence of cyclic reaction producing a small amount of impurity.
Akhteruzzaman, M; Alam, AH; Das, SC; Deb, AK; Islam, M; Khan, AH; Roy, J, 2001
)
1.98
" Dose-response curves were obtained for the antinociceptive effect of diclofenac, phenylephrine, clonidine, desipramine, prazosin, and yohimbine administered both systemically and intrathecally, and ED(50)s were calculated."( An isobolographic analysis of the adrenergic modulation of diclofenac antinociception.
Miranda, HF; Pinardi, G; Sierralta, F, 2001
)
0.79
" We proposed a multiple propensity score, which is an extension of the propensity score, to reduce the bias in a dose-response analysis in a drug safety study."( The multiple propensity score for analysis of dose-response relationships in drug safety studies.
Donnan, PT; MacDonald, TM; Steinke, D; Wang, J,
)
0.13
" There has been endoscopically validated usefulness of employing enterosoluble and injectable dosage forms during the first days of NAID-therapy."( [Comparative efficacy of diclobrou for prophylaxis of NSAID-associated gastropathies in patients with osteoarthritis].
Bohomaz, VM; Dubovenko, ZO; Khomchenkova, NI; Kushyk, MF; Puzanova, OH; Svintsits'kyĭ, AS,
)
0.13
" Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable and convenient rectal dosage form for diclofenac sodium."( Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium.
Choi, HG; Choi, JS; Kim, CK; Kim, KM; Lim, SJ; Oh, PS; Quan, QZ; Rhee, JD; Yong, CS, 2001
)
0.71
" The 2 h plasma concentration ratios from studies 1 and 2 were combined and a pooled analysis performed to compare ratios within each study (to determine the change in ratio when MDZ was dosed with and without chlorzoxazone) and between studies (to determine the consistency of the ratios when MDZ was given either as part of the two six drug cocktails or when given alone and as part of the five drug cocktail)."( An interaction between the cytochrome P450 probe substrates chlorzoxazone (CYP2E1) and midazolam (CYP3A).
Dickins, M; Gibson, A; Palmer, JL; Pleasance, S; Scott, RJ, 2001
)
0.31
"In this investigation, modified-release dosage forms of diltiazem HCl (DT) and diclofenac sodium (DS) were prepared."( A novel approach for the preparation of highly loaded polymeric controlled release dosage forms of diltiazem HCl and diclofenac sodium.
Ibrahim, HG; Kakish, HF; Najib, NM; Tashtoush, B, 2002
)
0.75
" These results show that diclofenac lotion and lipogel maybe more suitable formulations than the conventional topical dosage form."( In-vitro release of diclofenac diethylammonium from lipid-based formulations.
Parnianpour, M; Parsaee, S; Sarbolouki, MN, 2002
)
0.94
" In contrast to standard doses of 2 nonsteroidal antiinflammatory drugs (NSAIDs), a supratherapeutic valdecoxib dosage does not impair platelet function (COX-1)."( Valdecoxib does not impair platelet function.
Kent, JD; Leese, PT; Recker, DP; Talwalker, S, 2002
)
0.31
"These results show that an accelerated dosing schedule of sulphasalazine has identical effects to diclofenac in reducing symptoms, indicating it is a rapidly effective DMARD."( Treating rheumatoid arthritis early with disease modifying drugs reduces joint damage: a randomised double blind trial of sulphasalazine vs diclofenac sodium.
Choy, EH; Erhardt, C; Henderson, E; Kingsley, GH; Macfarlane, D; Panayi, GS; Papasavvas, G; Plant, MJ; Scott, DL; Williams, P; Wojtulewski, J; Young, A,
)
0.55
" This study evaluated the effect of diclofenac sodium, administered at clinical dosage and duration, on bone union."( Effect of diclofenac sodium on union of tibial fractures in rats.
Akman, S; Aksoy, B; Bilgiç, B; Gögüs, A; Seckin, F; Sener, N,
)
0.81
" The twice a day dosage of lornoxicam revealed to be appropriate."( [Analgesic dose range finding of lornoxicam compared to diclofenac. Crossover double blind study in rheumatoid arthritis].
Di Munno, O; Pasero, GP,
)
0.38
" Therefore, to optimize the osteotropic delivery of diclofenac via a bisphosphonic prodrug, the dosage regimen should be such that plasma concentration of DIC-BP is maintained at a level lower than that required for precipitate formation of complexes, similar to the usage of other bisphosphonates."( Dose-dependent pharmacokinetics and disposition of bisphosphonic prodrug of diclofenac based on osteotropic drug delivery system (ODDS).
Fujisaki, J; Hata, T; Hirabayashi, H; Kimura, S; Sawamoto, T; Tokunaga, Y, 2002
)
0.79
"The demographic features, hernia types, anaesthetic time, dosage of anaesthetic medication and operative details of the two groups were comparable."( Prospective randomized trial of pre-emptive analgesics following ambulatory inguinal hernia repair: intravenous ketorolac versus diclofenac suppository.
Goh, LC; Lau, H; Lee, F; Patil, NG; Wong, C, 2002
)
0.52
" Compared to conventional tablets, release of the model drug from these HPMC matrix tablets was prolonged; as a result, an oral release dosage form to avoid the gastrointestinal adverse effects was achieved."( In-vitro studies of diclofenac sodium controlled-release from biopolymeric hydrophilic matrices.
Bravo, SA; Lamas, MC; Salamón, CJ,
)
0.45
"For diclofenac, area under the concentration-time curve over the dosage interval (AUC(tau)) was larger in young subjects (3."( Influence of age and cytochrome P450 2C9 genotype on the steady-state disposition of diclofenac and celecoxib.
Brenner, SS; Dilger, K; Herrlinger, C; Hofmann, U; Klotz, U; Marx, C; Mürdter, TE, 2003
)
1.1
" This would indicate that both drugs need no dosage reduction in the elderly (at least up to 75 years) and that, besides CYP2C9, additional CYP species contribute to the elimination of both agents."( Influence of age and cytochrome P450 2C9 genotype on the steady-state disposition of diclofenac and celecoxib.
Brenner, SS; Dilger, K; Herrlinger, C; Hofmann, U; Klotz, U; Marx, C; Mürdter, TE, 2003
)
0.54
" Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable, convenient and effective rectal dosage form for diclofenac sodium."( Physicochemical characterization and in vivo evaluation of thermosensitive diclofenac liquid suppository.
Choi, HG; Choi, YK; Kim, CK; Kim, YI; Park, BJ; Quan, QZ; Rhee, JD; Yong, CS, 2003
)
0.74
" Dosing and duration varied, but in all 3 cases diclofenac was used at least 4 times a day for at least 3 days after LASIK."( Histopathology of corneal melting associated with diclofenac use after refractive surgery.
Hsu, JK; Johnston, WT; McDonnell, PJ; Pangalinan, R; Rao, N; Read, RW; Smith, RE, 2003
)
0.83
" A flexible dosing regimen is proposed, starting with an initial dose of 2 tablets (2 x 12."( A multicenter, randomized, double-blind, double-dummy, placebo- and active-controlled, parallel-group comparison of diclofenac-K and ibuprofen for the treatment of adults with influenza-like symptoms.
Frank, WO; Gold, MS; Grebe, W; Ionescu, E; Liu, JM, 2003
)
0.53
" The flexible dosing regimens comprised 2 tablets of diclofenac-K (12."( A multicenter, randomized, double-blind, double-dummy, placebo- and active-controlled, parallel-group comparison of diclofenac-K and ibuprofen for the treatment of adults with influenza-like symptoms.
Frank, WO; Gold, MS; Grebe, W; Ionescu, E; Liu, JM, 2003
)
0.78
"5 mg taken in a flexible dosing regimen was more effective than placebo in relieving influenza-like symptoms, with comparable tolerability Efficacy and tolerability of diclofenac-K were similar to those of ibuprofen 200 mg."( A multicenter, randomized, double-blind, double-dummy, placebo- and active-controlled, parallel-group comparison of diclofenac-K and ibuprofen for the treatment of adults with influenza-like symptoms.
Frank, WO; Gold, MS; Grebe, W; Ionescu, E; Liu, JM, 2003
)
0.72
" Our results suggested that a rectal poloxamer gel system with sodium chloride and poloxamers was a more physically stable, convenient, and effective rectal dosage form for diclofenac sodium."( Physicochemical characterization of diclofenac sodium-loaded poloxamer gel as a rectal delivery system with fast absorption.
Baek, SH; Chang, HW; Choi, HG; Jahng, Y; Jeong, TC; Kim, CK; Lee, SH; Rhee, JD; Sah, H; Son, JK; Yong, CS, 2003
)
0.79
"Although fitting orders to renal function avoids overdosage and therefore iatrogenic risk, dosage adjustment is rarely made."( Assessing residents' prescribing behavior in renal impairment.
Brücker, G; Deray, G; Launay-Vacher, V; Levu, S; Ravaud, P; Salomon, L, 2003
)
0.32
" Although no adjustment to renal function was required, 28% of the residents decreased the dosage of amlodipine and ordered an underdose."( Assessing residents' prescribing behavior in renal impairment.
Brücker, G; Deray, G; Launay-Vacher, V; Levu, S; Ravaud, P; Salomon, L, 2003
)
0.32
"Considering the iatrogenic risk related to the lack of dosage adjustment, attention should be drawn to increasing residents' awareness of dosage adjustment in renal impairment and to providing them with better information on patients' renal function."( Assessing residents' prescribing behavior in renal impairment.
Brücker, G; Deray, G; Launay-Vacher, V; Levu, S; Ravaud, P; Salomon, L, 2003
)
0.32
" The mean dosage and the total amount of Pethidine at 24 hours were significantly lower in G2 compared with G1."( Postoperative pain relief after laparoscopic cholecystectomy: a randomised prospective double-blind clinical trial.
Goroshina, J; Lepner, U; Samarütel, J, 2003
)
0.32
" Therapeutic use of diclofenac is associated with rare but sometimes fatal hepatotoxicity characterized by delayed onset of symptoms and lack of a clear dose-response relationship."( The metabolism of diclofenac--enzymology and toxicology perspectives.
Tang, W, 2003
)
0.98
" Topical diclofenac was more effective than oral diclofenac 1 hour after dosing and produced higher tissue concentrations (46."( Peripheral and central antihyperalgesic effects of diclofenac in a model of human inflammatory pain.
Burian, M; Geisslinger, G; Seegel, M; Tegeder, I, 2003
)
0.99
": Sixty-five healthy male subjects were randomized to receive 8 days' dosing with lumiracoxib 200 mg twice daily (b."( Gastroduodenal tolerability of lumiracoxib vs placebo and naproxen: a pilot endoscopic study in healthy male subjects.
Branson, J; Ford, M; Kellett, N; Mair, S; Milosavljev, S; Rordorf, C; Scott, G, 2003
)
0.32
" The primary efficacy outcome for the flexible multiple dosing regimen was the End of Study global efficacy assessment."( Relief of acute low back pain with diclofenac-K 12.5 mg tablets: a flexible dose, ibuprofen 200 mg and placebo-controlled clinical trial.
Dreiser, RL; Gold, M; Ionescu, E; Liu, JH; Marty, M, 2003
)
0.6
" The flexible multiple dosing regimens of diclofenac-K and ibuprofen were both significantly superior to placebo on the End of Study global efficacy assessment, time to rescue medication over the entire study period, the End of Day global efficacy assessment on Days 1-2, pain intensity difference on the VAS at Visit 3 and the Eifel algofunctional index at Visit 3 (also at Visit 2 in diclofenac-K 12."( Relief of acute low back pain with diclofenac-K 12.5 mg tablets: a flexible dose, ibuprofen 200 mg and placebo-controlled clinical trial.
Dreiser, RL; Gold, M; Ionescu, E; Liu, JH; Marty, M, 2003
)
0.86
"The flexible multiple dosing regimen of diclofenac-K 12."( Relief of acute low back pain with diclofenac-K 12.5 mg tablets: a flexible dose, ibuprofen 200 mg and placebo-controlled clinical trial.
Dreiser, RL; Gold, M; Ionescu, E; Liu, JH; Marty, M, 2003
)
0.86
"5 mg) vs paracetamol (500 mg) and placebo given in a flexible dosage regimen to treat pain resulting from extraction of impacted third molar teeth."( Analgesic efficacy of low-dose diclofenac versus paracetamol and placebo in postoperative dental pain.
Gold, MS; Ionescu, E; Kubitzek, F; Liu, JM; Ziegler, G, 2003
)
0.6
"To determine whether a topical ophthalmic diclofenac sodium formulation containing a proprietary polymeric drug delivery system (ISV-205), when dosed concomitantly with 1% prednisolone acetate, is effective in blocking the intraocular pressure (IOP) response in humans."( Prevention of corticosteroid-induced intraocular pressure elevation using ISV-205.
Stewart, WC, 2003
)
0.58
" We also determined the role of cytochrome P450 2C9 (CYP2C9) polymorphism on coumarin dosage and INR in NSAID users."( Potential interaction between acenocoumarol and diclofenac, naproxen and ibuprofen and role of CYP2C9 genotype.
Brouwers, JR; de Jong-van den Berg, LT; de Vries-Bots, AM; Piersma-Wichers, M; Plat, AW; Slomp, J; van Dijk, AA; van Dijk, KN, 2004
)
0.58
" Adult male Sprague-Dawley rats were dosed orally (equivalent to 15 mg/kg diclofenac sodium) as the acid or its sodium salt as well as diclofenac-DPPC complex."( A comparison of gastrointestinal permeability induced by diclofenac-phospholipid complex with diclofenac acid and its sodium salt.
Jamali, F; Khazaeinia, T,
)
0.61
" Differences observed in blood pressure response between COX inhibitors may not be related in their sensitivity but rather their dosing frequency."( Effects of COX inhibition on blood pressure and kidney function in ACE inhibitor-treated blacks and hispanics.
Alausa, T; Bakris, GL; Folker, A; Hung, E; Izhar, M, 2004
)
0.32
" Thromboxane B(2) (TxB(2)) inhibition was measured prior to lumiracoxib dosing and 2 hours afterwards."( Lumiracoxib: pharmacokinetic and pharmacodynamic profile when coadministered with fluconazole in healthy subjects.
Laurent, A; Milosavljev, S; Rordorf, C; Scott, G; Yeh, CM; Yih, L, 2004
)
0.32
" At the start and end of each dosing period, COX-2 selectivity was assessed by ex vivo serum thromboxane B(2) (COX-1) and lipopolysaccharide stimulated prostaglandin (PG) E(2) (COX-2), mucosal injury by endoscopy, and small and large bowel permeability by 0- to 5-hour and 5- to 24-hour (51)Cr-EDTA absorption."( Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2 selective inhibitor: An integrated study.
Atherton, C; Bebb, J; Bonner, J; Branson, J; Brough, J; Burdsall, J; Cunliffe, R; Hawkey, CJ; Jones, J; McKaig, B; Rordorf, C; Scott, G; Stevenson, D, 2004
)
0.32
" Lumiracoxib can, therefore, be administered concurrently with either of these agents without need for lumiracoxib dosage alteration."( Lack of effect of omeprazole or of an aluminium hydroxide/magnesium hydroxide antacid on the pharmacokinetics of lumiracoxib.
Langholff, W; Milosavljev, S; Rordorf, C; Scott, G; Shenouda, M; Vinluan Reynolds, C, 2004
)
0.32
" Drug release decreased with the increase of amount of drug and it is dependent of dosage form."( Evaluation of xanthan and highly substituted galactomannan from M. scabrella as a sustained release matrix.
Andreazza, IF; Bresolin, TM; Ganter, JL; Ughini, F, 2004
)
0.32
" Postoperatively the propacetamol dosage was repeated twice and diclofenac once on the ward."( Propacetamol and diclofenac alone and in combination for analgesia after elective tonsillectomy.
Hiller, A; Savolainen, S; Silvanto, M; Tarkkila, P, 2004
)
0.9
"This study compared the analgesic dose-response relationship and tolerability of 3 doses of ProSorb diclofenac K and placebo in the treatment of pain after dental impaction surgery."( Dose-ranging analgesic study of Prosorb diclofenac potassium in postsurgical dental pain.
Adamson, D; Christensen, S; Hersh, EV; Kiersch, TA; Levin, LM; Lyon, JA; Noveck, R; Watson, G, 2004
)
0.81
"The clinical variables examined included intensity of pain as measured by a visual analogue scale; pain, stiffness, and physical function subscales of the Western Ontario and McMaster Universities (WOMAC) osteoarthritis index; dosage of diclofenac taken during treatment; and the profile of quality of life in the chronically ill (PQLC) instrument, evaluated before and after the treatment programme."( Acupuncture as a complementary therapy to the pharmacological treatment of osteoarthritis of the knee: randomised controlled trial.
Aguilar, I; Borge, MA; Gaspar, O; Jurado, R; León, JM; Méndez, C; Panadero, MD; Perea-Milla, E; Sánchez-Rodríguez, F; Vas, J; Vega, E, 2004
)
0.51
"Forty healthy volunteers instilled Dicloabak in the randomised eye and thiomersal-preserved diclofenac in the other eye, according to a strictly identical dosing regimen, for 28 days."( [Ocular tolerance of a new formulation of nonpreserved diclofenac].
Chiambaretta, F; Creuzot-Garcher, C; Dubray, C; Pilon, F; Pouliquen, P; Rebika, H; Rigal, D, 2004
)
0.79
" First, dose-response relationships of each of diclofenac, piroxicam and alpha-tocopherol were evaluated using bone marrow lymphocytes counts and monoamines levels in plasma, brain and spleen."( Effects of diclofenac, piroxicam and alpha-tocopherol on monoaminelymphopoietic interfacing in mice.
Hamed, MR; Hasan, WA; Hassanein, NM, 2004
)
0.97
" Because thoracic epidural analgesia is easily administered and the dosage of the drugs used effectively controlled, it is a practical method for perioperative pain control for UAE."( [Thoracic epidural analgesia is effective in perioperative pain relief for uterine artery embolization].
Katayama, M; Kitazono, M; Nagao, T; Ohshima, K; Ohwada, T; Shimizu, H, 2005
)
0.33
"Overview of three dose-response studies demonstrating the efficacy of lumiracoxib, a novel COX-2 selective inhibitor, for chronic pain associated with osteoarthritis (0A), or rheumatoid arthritis (RA) and acute pain following dental extraction."( Lumiracoxib in the treatment of osteoarthritis, rheumatoid arthritis and acute postoperative dental pain: results of three dose-response studies.
Gitton, X; Jayawardene, S; Schnitzer, TJ; Sloan, VS, 2005
)
0.33
" Comparison of release rate-time plots of dissolution data of marketed product with the newly developed dosage form indicated the ability of the later to sustain more diclofenac sodium release."( Evaluation of crosslinked chitosan hydrogel beads as a carrier for prolonged delivery of diclofenac sodium: in vitro and in vivo studies.
Alsarra, IA, 2004
)
0.74
" Clinical studies support a once-daily dosing regimen, despite its relatively short plasma elimination half-life (3 - 6 h)."( Clinical pharmacology of lumiracoxib, a second-generation cyclooxygenase 2 selective inhibitor.
Bannwarth, B; Berenbaum, F, 2005
)
0.33
"The degradation products of diclofenac in aqueous dosage form in accelerated storage conditions were characterized by electrospray ionization-ion trap mass spectrometry (ESI-MS)."( Identification of degradation products of diclofenac by electrospray ion trap mass spectrometry.
Bouchon, B; Galmier, MJ; Lartigue, C; Madelmont, JC; Mercier, F; Pilotaz, F, 2005
)
0.89
" Thus, the poloxamer-based solid suppository with P 124 and P 188 was a mucoadhesive, safe and effective rectal dosage form for diclofenac sodium."( Physicochemical characterization and in vivo evaluation of poloxamer-based solid suppository containing diclofenac sodium in rats.
Choi, HG; Kim, CK; Kim, DD; Kim, JO; Kim, YI; Lee, KC; Oh, YK; Park, YJ; Rhee, JD; Yong, CS; Yoo, BK, 2005
)
0.75
" A cell culture model of the gastric epithelial cell surface would prove useful for biopharmaceutical screening of new chemical entities and dosage forms."( A collagen IV matrix is required for guinea pig gastric epithelial cell monolayers to provide an optimal model of the stomach surface for biopharmaceutical screening.
Coombes, AG; Hanson, PJ; Kavvada, KM; Moore, VA; Murray, JG, 2005
)
0.33
" Thus, the clear aceclofenac-loaded soft capsule with ethanolamine was a more effective oral dosage form with fast absorption for poorly water-soluble aceclofenac."( Trials of clear aceclofenac-loaded soft capsules with accelerated oral absorption in human subjects.
Choi, HG; Gil, YS; Kim, CK; Kim, JO; Lee, KH; Oh, YK; Park, SM; Park, YJ; Rhee, JD; Woo, JS; Yong, CS; Yoo, BK; Yu, CH, 2005
)
0.33
" Least square means (95% CI) of all observations during the first 6 h after dosing showed that diclofenac caused a reduction in GFR from 71 (64-78) to 59 (52-66) ml/min."( Cyclooxygenase inhibition causes marked impairment of renal function in elderly subjects treated with diuretics and ACE-inhibitors.
Björkman, S; Höglund, P; Juhlin, T, 2005
)
0.55
"The study was designed to evaluate the relative bioavailability of diclofenac in plasma, subcutaneous adipose and skeletal muscle tissue after repeated topical administration using MIKA Diclofenac Spray Gel (4%), a novel formulation, and after oral dosing using VOLTAREN 50 mg enteric coated tablets."( Favourable dermal penetration of diclofenac after administration to the skin using a novel spray gel formulation.
Brunner, M; Dehghanyar, P; Martin, W; Menke, G; Müller, M; Seigfried, B, 2005
)
0.85
"The relative bioavailability of diclofenac in subcutaneous adipose and skeletal muscle tissue was substantially higher after topical compared with oral dosing (324% and 209%, respectively) whereas relative plasma bioavailability was 50-fold lower."( Favourable dermal penetration of diclofenac after administration to the skin using a novel spray gel formulation.
Brunner, M; Dehghanyar, P; Martin, W; Menke, G; Müller, M; Seigfried, B, 2005
)
0.89
" Storage under uncontrolled environmental conditions or contact with water vapour during manufacturing process could thus influence the performance of the final dosage form."( Physico-chemical characterisation and intrinsic dissolution studies of a new hydrate form of diclofenac sodium: comparison with anhydrous form.
Antoniella, E; Bartolomei, M; Bertocchi, P; Rodomonte, A, 2006
)
0.55
" The method was applied to serum collected at 3h after rats were treated with an experimentally useful dosage range of 3, 10 and 50mg/kg diclofenac."( Efficient high performance liquid chromatograph/ultraviolet method for determination of diclofenac and 4'-hydroxydiclofenac in rat serum.
Kanz, MF; Kaphalia, BS; Kaphalia, L; Kumar, S; Treinen-Moslen, M, 2006
)
0.76
" Results support the good safety profile of both formulations when dosed three times daily for 4 weeks in absence of concomitant use of drugs potentially toxic for cornea."( Comparison of the efficacy and safety of two formulations of diclofenac sodium 0.1% eyedrops in controlling postoperative inflammation after cataract surgery.
Arnoux, YV; Bodaghi, B; Colin, J; Jaulerry, SD; Le Hoang, P; Weber, ME,
)
0.37
" In a diary, patients recorded compliance to dosing and use of rescue medication and assessed daily pain on movement, spontaneous pain, and pain relief."( Efficacy of topical diclofenac diethylamine gel in osteoarthritis of the knee.
Albrecht, HH; Elkik, F; Gold, MS; Liu, JM; Niethard, FU; Solomon, GS; Unkauf, M, 2005
)
0.65
" Twice-daily dosage of aceclofenac 100 mg and etoricoxib 60 mg were recommended for the double blind study."( Comparative efficacy of aceclofenac and etoricoxib in post extraction pain control: randomized control trial.
Chalini, S; Raman, U,
)
0.13
" In patients with rheumatoid arthritis, peak lumiracoxib synovial fluid concentrations occur 3-4 hours later than in plasma and exceed plasma concentrations from 5 hours after dosing to the end of the 24-hour dosing interval."( Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor.
Choi, L; Mangold, JB; Marshall, P; Rordorf, CM, 2005
)
0.33
"02 hr) produces a null difference as the net effect on bioavailability, particularly when the drug is to be used in multiple dosage regimen."( Pharmacokinetics of diclofenac sodium in normal man.
Ahmed, T; Hasan, F; Hasan, SM; Talib, N, 2005
)
0.65
" An increased risk was observed for diclofenac and rofecoxib, the latter one with a clear dose-response trend."( Non-steroidal antiinflammatory drugs and the risk of acute myocardial infarction.
García Rodríguez, LA; Hernández-Díaz, S; Varas-Lorenzo, C, 2006
)
0.61
" The results detailed within this paper indicate that agar is a viable filler for extended release hot melt produced dosage forms."( The use of agar as a novel filler for monolithic matrices produced using hot melt extrusion.
Devine, DM; Geever, LM; Higginbotham, CL; Kennedy, JE; Lyons, JG; O'Sullivan, P, 2006
)
0.33
" Optimal calibration range was fixed (1-way ANOVA) and then the method was applied to dosage form analysis."( Rapid colorimetric assay of diclofenac sodium tablets using 4-carboxyl-2,6-dinitrobenzene diazonium ion (CDNBD).
Adegoke, OA; Idowu, OS; Oderinu, BA; Olaniyi, AA, 2006
)
0.63
" The injectable dosage form of Diclofenac was introduced into the Iran drug market in 1993."( Injectable diclofenac: a painful shot into Iran's health system.
Cheraghali, AM, 2006
)
1.01
"A total of 223 patients satisfying the American College of Rheumatology criteria for knee OA were chosen for this 17-week, randomized, double-dummy, diclofenac sodium-controlled trial, with diacerein dosage of 100 mg/d and diclofenac sodium of 75mg/d."( Evaluation of efficacy and safety of diacerein in knee osteoarthritis in Chinese patients.
Huang, F; Li, J; Li, ZG; Liang, DF; Ma, L; Su, Y; Tang, FL; Wu, DH; Xu, H; Zhang, FC; Zhang, JL; Zheng, WJ; Zhou, HQ; Zhou, YX, 2006
)
0.53
" Owing to sticky and waxy nature of GMO, preparation of oral solid dosage form utilizing GMO is still a challenge for pharmaceutical researchers."( Spray dried glyceryl monooleate-magnesium trisilicate dry powder as cubic phase precursor.
Biradar, SV; Paradkar, AR; Shah, MH, 2006
)
0.33
" Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release."( Development of hollow/porous calcium pectinate beads for floating-pulsatile drug delivery.
Badve, SS; Korde, A; Pawar, AP; Sher, P, 2007
)
0.34
" The results suggest an optimal relationship between the amount of CCS and the thickness of the coating film, which provides appropriate dissolution rate of diclofenac sodium from the dosage forms."( The influence of formulation on the dissolution profile of diclofenac sodium tablets.
De Castro, WV; Derendorf, H; Mertens-Talcott, SU; Moreira-Campos, LM; Nunan, EA; Oliveira, MA; Pianetti, GA; Pires, MA; Vianna-Soares, CD, 2006
)
0.77
" The in vitro and in vivo studies showed that M could be a new, alternative dosage form for effective therapy."( Transdermal delivery of diclofenac sodium through rat skin from various formulations.
Ertan, G; Güneri, T; Kantarci, G; Sarigüllü Ozgüney, I; Sözer, S; Yeşim Karasulu, H, 2006
)
0.64
" Well documented safety and efficacy, a rapid onset of action and a flexible daily dosing regimen are essential in this context."( Diclofenac potassium 12.5mg tablets for mild to moderate pain and fever: a review of its pharmacology, clinical efficacy and safety.
Moore, N, 2007
)
1.78
" When lumiracoxib is coadministered with warfarin or aspirin, no dosage adjustment is required."( Lumiracoxib.
Barkin, R; Buvanendran, A, 2007
)
0.34
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
"75% with 5 doses each side, total dosage 40 mL (300 mg), via parasternal intercostal injection or saline before insertion of the sternal wires and closure of the sternal wound."( Parasternal intercostal block with ropivacaine for pain management after cardiac surgery: a double-blind, randomized, controlled trial.
Almeida, AA; Barr, AM; Tutungi, E, 2007
)
0.34
" This work stresses the importance of assessing the correct crystalline form also in API of well-established use to guarantee quality, safety and efficacy of the final dosage form."( Hydrate modifications of the non-steroidal anti-inflammatory drug diclofenac sodium: Solid-state characterisation of a trihydrate form.
Antoniella, E; Bartolomei, M; Bertocchi, P; Minelli, G; Rodomonte, A, 2007
)
0.58
" Pain intensity was measured using the categorical scale and the primary efficacy variable was the summed pain intensity difference over 8 hours after dosing (SPID-8)."( Lumiracoxib 400 mg compared with celecoxib 400 mg and placebo for treating pain following dental surgery: a randomized, controlled trial.
Davis, N; Fricke, J; Krammer, G; Yu, V, 2008
)
0.35
"Coated pellets controlling drug release are a very popular dosage form which is widely used in medical practice."( [Effect of thermal curing of the ethyl cellulose film on the rapidity of release of diclofenac sodium from pellets].
Cepáková, L; Gryczová, E; Prokopová, A; Rabisková, M; Tomásek, V, 2007
)
0.56
" These types of topical dosage forms could give sustained delivery of drug onto the skin, could tolerate the incorporation of an enhancer, a humectant and an occlusive phase, so they are interesting promises to improve skin absorption of nonsteroidal anti-inflammatory drugs and to prevent side effects associated."( Release study of diclofenac from new carbomer gels.
Bregni, C; Carlucci, A; Chiappetta, D; Faiden, N; García, R; Pasquali, R, 2008
)
0.69
" The in vitro drug release study revealed that HPMC K100CR at a concentration of 40% of the dosage form weight was able to control the simultaneous release of both DS and CS for 9 hours."( Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate.
Avachat, A; Kotwal, V, 2007
)
0.58
" Blood samples were collected at pre-defined time points after dosing to determine plasma concentrations over time."( Population pharmacokinetic modelling of the enterohepatic recirculation of diclofenac and rofecoxib in rats.
Chain, A; Danhof, M; Della Pasqua, O; Huntjens, DR; Metcalf, A; Spalding, DJ; Strougo, A; Summerfield, S, 2008
)
0.58
"The US Food and Drug Administration's (FDA's) guidance for industry on dissolution testing of immediate-release solid oral dosage forms describes that drug dissolution may be the rate limiting step for drug absorption in the case of low solubility/high permeability drugs (BCS class II drugs)."( Mathematical evaluation of similarity factor using various weighing approaches on aceclofenac marketed formulations by model-independent method.
Chotai, NP; Desai, JU; Gandhi, TR; Nagda, CD; Soni, TG, 2008
)
0.35
" Analytical parameter (DeltappmO(2)) and toxicological index (respiratory inhibition, delta%) measured after 1h of exposure were utilized for dose-response relationship study."( A new respirometric endpoint-based biosensor to assess the relative toxicity of chemicals on immobilized human cells.
Campanella, L; Dragone, R; Frazzoli, C; Grappelli, C, 2009
)
0.35
"The prediction of the in vivo drug release characteristics of modified release oral dosage forms by in vitro dissolution tests is a prerequisite for successful product development."( Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses.
Garbacz, G; Giessmann, T; Mönnikes, H; Nagel, S; Siegmund, W; Wedemeyer, RS; Weitschies, W; Wilson, CG, 2008
)
0.61
"Literature data are reviewed regarding the scientific advisability of allowing a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing either diclofenac potassium and diclofenac sodium."( Biowaiver monographs for immediate release solid oral dosage forms: diclofenac sodium and diclofenac potassium.
Amidon, GL; Barends, DM; Binjesoh, V; Chuasuwan, B; Dressman, JB; Junginger, HE; Midha, KK; Polli, JE; Shah, VP; Stavchansky, S; Zhang, H, 2009
)
0.77
"The aim of this study was to develop an enteric-coated multiunit dosage form containing aceclofenac, a nonsteroidal anti-inflammatory drug."( Multiparticulate drug delivery system of aceclofenac: development and in vitro studies.
Arumugam, K; Averineni, RK; Meka, SR; Nayak, U; Nayanabhirama, U; Shavi, GV; Sureshwar, P, 2009
)
0.35
" The proposed procedure can be a fast and convenient alternative to the standard pharmacopoeial methods of diclofenac sodium quantification in solid dosage forms."( Quantitative determination of diclofenac sodium in solid dosage forms by FT-Raman spectroscopy.
Mazurek, S; Szostak, R, 2008
)
0.85
" Hundred and forty-four male Sprague Dawley rats were dosed with 3, 5 and 10 mg kg(-1) diclofenac and ibuprofen in saline via intraperitoneal injection for 15 days."( Morphological alteration in mitochondria following diclofenac and ibuprofen administration.
Fakurazi, S; Ithnin, H; Moorthy, M, 2008
)
0.82
"Two different salts of diclofenac, diclofenac sodium and diclofenac potassium, in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and dehydrated rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2009
)
0.91
" Efficient removal of background ions permitted the detection of drug-related ions in in vivo samples (plasma, bile, urine and feces) obtained from rats orally dosed with (14)C-loratadine with minimal interference."( A retention-time-shift-tolerant background subtraction and noise reduction algorithm (BgS-NoRA) for extraction of drug metabolites in liquid chromatography/mass spectrometry data from biological matrices.
Alton, K; Chowdhury, S; Ding, W; Ghosal, A; Tong, W; Zhu, P, 2009
)
0.35
"In vitro biorelevant dissolution tests enabling the prediction of in vivo performance of an oral modified-release (MR) dosage form were developed in this study."( Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form.
De Maio, V; Dressman, JB; Jantratid, E; Mattavelli, V; Ronda, E; Vertzoni, M, 2009
)
0.57
" Pharmacokinetic models were developed for both the dosage forms, and simulations were performed for different doses."( Influence of dosage form on the intravitreal pharmacokinetics of diclofenac.
Durairaj, C; Edelhauser, HF; Kim, SJ; Kompella, UB; Shah, JC, 2009
)
0.59
" More research on optimum dosing and safety in asthmatic children is required."( Diclofenac for acute pain in children.
Pritchard, D; Savage, I; Standing, JF; Waddington, M, 2009
)
1.8
" The dosage of study treatment was 8-24 mg/day LNX, 100-150 mg/day diclofenac or placebo."( Efficacy and safety of lornoxicam compared with placebo and diclofenac in acute sciatica/lumbo-sciatica: an analysis from a randomised, double-blind, multicentre, parallel-group study.
Geertsen, MS; Herrmann, WA, 2009
)
0.83
" The observed susceptibility of the tested dosage forms toward biorelevant stress bears in our interpretation the risk to cause unwanted fluctuations in drug plasma concentration profiles."( Investigation of dissolution behavior of diclofenac sodium extended release formulations under standard and biorelevant test conditions.
Garbacz, G; Weitschies, W, 2010
)
0.63
" Additional measures included NPRS scores at predefined times over 48 hours, the summed pain intensity difference over 48 hours (SPID48), the time-weighted sum of pain relief scores over the first 8 hours, the mean dosing interval (the time from dosing to the time rescue medication or the next dose of study medication was administered, whichever was less), the proportion of patients requiring rescue medication, and the onset of perceptible and meaningful pain relief (2-stopwatch method)."( Diclofenac potassium liquid-filled soft gelatin capsules in the management of patients with postbunionectomy pain: a Phase III, multicenter, randomized, double-blind, placebo-controlled study conducted over 5 days.
Boesing, SE; Diamond, E; Duckor, S; Gottlieb, I; Raymond, G; Riff, DS; Soulier, S, 2009
)
1.8
"001), and overall mean dosing interval (331."( Diclofenac potassium liquid-filled soft gelatin capsules in the management of patients with postbunionectomy pain: a Phase III, multicenter, randomized, double-blind, placebo-controlled study conducted over 5 days.
Boesing, SE; Diamond, E; Duckor, S; Gottlieb, I; Raymond, G; Riff, DS; Soulier, S, 2009
)
1.8
"Sodium diclofenac (SD) release from dosage forms has been studied under different conditions."( Dissolution parameters for sodium diclofenac-containing hypromellose matrix tablet.
Bresolin, TM; da Silva, C; Mourão, SC; Porta, V; Serra, CH, 2010
)
1.09
" Besides, diclofenac sodium could be given as supplementary dugs with the dosage used recorded if necessary."( Clinical efficacy and safety of Gubitong Recipe () in treating osteoarthritis of knee joint.
Jin, DE; Tao, QW; Xu, Y; Yan, XP, 2009
)
0.76
" ESR and CRP levels remained unchanged in all patients, and the proportion and mean dosage of diclofenac sodium used were similar in the two groups."( Clinical efficacy and safety of Gubitong Recipe () in treating osteoarthritis of knee joint.
Jin, DE; Tao, QW; Xu, Y; Yan, XP, 2009
)
0.57
" The dose-response surface of irgasan and diclofenac indicated a concentration addition."( Measuring and modeling of binary mixture effects of pharmaceuticals and nickel on cell viability/cytotoxicity in the human hepatoma derived cell line HepG2.
Bauer, M; Herbarth, O; Rudzok, S; Schlink, U, 2010
)
0.62
"The aim of the present study was to develop stable parenteral submicron lipid emulsions (SLEs) for sustained delivery of diclofenac acid, used to treat arthritic conditions, to minimize dosing frequency."( Preparation, characterization, and in vivo pharmacodynamic evaluation of parenteral diclofenac submicron lipid emulsions.
Kishan, V; Prabhakar, K; Varshika, E,
)
0.56
" Patients were assessed for safety variables that included adverse events, local skin reactions, laboratory results, dosage of immunosuppressive medication and indication of graft rejection."( Results of a randomized, placebo-controlled safety and efficacy study of topical diclofenac 3% gel in organ transplant patients with multiple actinic keratoses.
Johannsen, A; Röwert-Huber, J; Sterry, W; Stockfleth, E; Ulrich, C; Ulrich, M,
)
0.36
" The combination of diclofenac sodium and metamizole sodium is acceptable, although, at a lower dosage of metamizole, the duration of analgesia is shortened."( Evidence-based intravenous pain treatment with analgesic infusion regimens.
Cihal, P; Kamyar, MR; Lemmens-Gruber, R; Nemec, K; Timin, E, 2010
)
0.68
" Related to the salicin content of the willow bark extract, a higher dosage of ASA was needed."( In vitro anti-proliferative effects of the willow bark extract STW 33-I.
Bonaterra, GA; Kelber, O; Kinscherf, R; Metz, J; Weiser, D, 2010
)
0.36
" Importance of aceclofenac as a new generational NSAID has inspired the development of topical dosage forms."( Evaluation of extemporaneously manufactured topical gels containing aceclofenac on inflammation and hyperalgesia in rats.
Dua, K; Pabreja, K; Padi, SS, 2010
)
0.36
" These preparations may offer a number of therapeutic advantages over immediate release dosage forms in drug delivery."( Utilization of hydrophilic swellable polymers as carriers for sustained drug delivery from matrices and three layer tablet systems.
Efentakis, M; Naseef, H; Vlachou, M, 2010
)
0.36
" Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form."( Influence of oleic acid on the rheology and in vitro release of lumiracoxib from poloxamer gels.
de Sousa, VP; Moreira, TS; Pierre, MB, 2010
)
0.36
"After the dosing of an extended-release (ER) formulation, compounds may exist in solutions at various concentrations in the colon because the drugs are released at various speeds from the ER dosage form."( The relationship between the drug concentration profiles in plasma and the drug doses in the colon.
Hosoi, Y; Kanamaru, T; Konno, T; Nakagami, H; Tajiri, S; Yada, S; Yoshida, K, 2010
)
0.36
"Matrix type, monolithic, dosage forms suitable for controlled release that exhibit pH-dependent behavior are considerably less common than similarly behaving multiparticulated, enterically coated dosage forms, although simpler and less expensive to make."( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures.
Drefko, W; Moroni, A; Thone, G, 2011
)
0.37
"Evaluate the properties of alginates and alginate-containing systems to produce pH-sensitive, monolithic, controlled release dosage forms that perform acceptably and determine their limits of application in regard with stability, pH and Ca(++) sensitivity, and appropriated rate of release."( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures.
Drefko, W; Moroni, A; Thone, G, 2011
)
0.37
") with other gel-forming gums such as propylene glycol alginate (PGA), xanthan, or hydroxypropyl methylcellulose have been evaluated for applicability in the manufacture of controlled release dosage forms with three drugs of different solubility and ionic character."( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures.
Drefko, W; Moroni, A; Thone, G, 2011
)
0.37
" with a number of other gums have been demonstrated suitable to manufacture pH-sensitive, matrix-type solid dosage forms with release-controlling properties for up to 12 hours."( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures.
Drefko, W; Moroni, A; Thone, G, 2011
)
0.37
"The prediction of the in vivo drug release characteristics of modified release (MR) oral dosage forms by in vitro dissolution tests is a prerequisite for successful product development."( A biorelevant dissolution stress test device - background and experiences.
Garbacz, G; Klein, S; Weitschies, W, 2010
)
0.36
"To improve the predictive power of dissolution testing, the authors recently developed a new dissolution test apparatus that simulates physical conditions of the gastrointestinal (GI) passage of MR dosage forms."( A biorelevant dissolution stress test device - background and experiences.
Garbacz, G; Klein, S; Weitschies, W, 2010
)
0.36
" Results of these experiments thus indicated that a high sensitivity of dosage forms to GI-specific physical conditions has to be regarded as a major cause of irregularities in the drug release profiles, which may result in fluctuations of the individual drug plasma concentration profiles, as, for example, caused by dose dumping."( A biorelevant dissolution stress test device - background and experiences.
Garbacz, G; Klein, S; Weitschies, W, 2010
)
0.36
" Oswestry Disability Index (ODI), Patients' Satisfaction Score (PSS), and dosage and cost of the drugs used for pain management were recorded at baseline, 30 and 60 days after treatment."( Efficacy of diclofenac sodium in pain relief after conventional radiofrequency denervation for chronic facet joint pain: a double-blind randomized controlled trial.
Huang, X; Liu, X; Ma, K; Wang, W; Wang, Y; Wu, T; Yiqun, M, 2011
)
0.75
" RPTEC/TERT1 cells were cultured with either the dosing vehicle (DMSO) or with exposure to one of six compounds (nifedipine, potassium bromate, monuron, D-mannitol, ochratoxin A and sodium diclofenac), several of which are known to cause renal effects."( Metabolic response to low-level toxicant exposure in a novel renal tubule epithelial cell system.
Athersuch, TJ; Cavill, R; Ebbels, TM; Ellis, JK; Jennings, P; Keun, HC; McMorrow, T; Radford, R; Ryan, MP; Slattery, C, 2011
)
0.56
" These studies propose for the first time a molecular basis for the observed often-unexpected, concentration-dependant changes in HPMC solution properties when co-formulated with different NSAIDs, and underline the importance of characterising such fundamental interactions that have the potential to influence drug release in solid HPMC-based dosage forms."( Solution interactions of diclofenac sodium and meclofenamic acid sodium with hydroxypropyl methylcellulose (HPMC).
Griffiths, PC; Melia, CD; Pygall, SR; Timmins, P; Wolf, B, 2011
)
0.67
" Importance of aceclofenac as a NSAID has inspired development of topical dosage forms."( Aceclofenac topical dosage forms: in vitro and in vivo characterization.
Dua, K; Pabreja, K; Ramana, MV, 2010
)
0.36
" Hence, such formulations of previously well established molecules provide a new direction towards developing better and convenient dosing alternatives."( Comparative bioavailability study of a new formulation of injection of 75 mg diclofenac sodium in 1 ml with the conventional injection of 75 mg diclofenac sodium given in 3 ml volume.
Jaiswal, V; Nivsarkar, M; Ojha, A; Padh, H; Patel, S; Shep, D, 2011
)
0.6
" Recently, a Cochrane review concluded the major knowledge gap in diclofenac use is dosing information."( Diclofenac pharmacokinetic meta-analysis and dose recommendations for surgical pain in children aged 1-12 years.
Korpela, R; Olkkola, KT; Standing, JF; Tibboel, D, 2011
)
2.05
" A group of male and female rats was treated with one of these compounds for 15 days, after which a single dosage of scopolamine was administered."( Comparative protective action of curcumin, memantine and diclofenac against scopolamine-induced memory dysfunction.
Ali, EH; Arafa, NM, 2011
)
0.61
" The influence of excipients and of a size of the solid dosage forms on the amount of the released substances at the intervals of time using the different rates of flow of the dissolution medium was investigated."( Simultaneous release of diclofenac sodium and papaverine hydrochloride from tablets and pellets using the flow-through cell apparatus described by dimensionless equations.
Kasperek, R,
)
0.44
" The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized."( The influence of dissolution conditions on the drug ADME phenomena.
Cascone, S; De Santis, F; Lamberti, G; Titomanlio, G, 2011
)
0.37
" Equal volumes of three plasma samples corresponding to each time point of three discretely dosed rats with different compounds were pooled (cassette analysis)."( High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC-MS/MS.
Betnér, I; Briem, S; Bueters, T; Dahlström, J; Kvalvågnaes, K, 2011
)
0.37
" An ibuprofen dosage of 1,600 mg/day did not induce LUF syndrome either at continuous periovulatory or discontinuous exposure."( Luteinized unruptured follicle syndrome increased by inactive disease and selective cyclooxygenase 2 inhibitors in women with inflammatory arthropathies.
Micu, MC; Micu, R; Ostensen, M, 2011
)
0.37
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Collagen and U46619 caused in vivo thrombus formation with the former, but not latter, sensitive to oral dosing with aspirin."( Thrombosis is reduced by inhibition of COX-1, but unaffected by inhibition of COX-2, in an acute model of platelet activation in the mouse.
Armstrong, PC; Emerson, M; Kirkby, NS; Mitchell, JA; Warner, TD; Zain, ZN, 2011
)
0.37
" Toxicity studies with Diclofenac, Paracetamol and Verapamil in both cell lines show dose-response characteristics and EC(50) values similar to hHeps."( Comparative analysis of phase I and II enzyme activities in 5 hepatic cell lines identifies Huh-7 and HCC-T cells with the highest potential to study drug metabolism.
Dooley, S; Ehnert, S; Hao, L; Lin, J; Liu, L; Mühl-Benninghaus, R; Neumann, J; Nussler, AK; Nussler, N; Schyschka, L; Stöckle, U, 2012
)
0.69
"Conventional dosage form is nowadays mostly replaced by sustained release formulation in order to increase drug efficacy and patient compliance."( Preparation and in-vitro in-vivo evaluation of sustained release matrix diclofenac sodium tablets using PVP-K90 and natural gums.
Iqbal, Z; Khan, A; Khan, JA; Khan, R; Nasir, F; Rashid, A, 2011
)
0.6
"The obtained results revealed that the presence of Acryl-EZE in the matrix tablets is effective in protecting the dosage forms from release in acid environments such as gastric fluid."( Development of gastro intestinal sustained release tablet formulation containing acryl-EZE and pH-dependent swelling HPMC K 15 M.
Chaumeil, JC; Daoud, K; Lamoudi, L, 2012
)
0.38
"Pharmaceutical pellets are spherical or nearly spherical multi-unit dosage forms designed to optimize pharmacokinetics and pharmacodynamics features of drug release."( Analysis of pharmaceutical pellets: an approach using near-infrared chemical imaging.
Breitkreitz, MC; Calefe, L; da Fonseca, P; de Souza, AM; Moffa, M; Poppi, RJ; Sabin, GP, 2011
)
0.37
", South Korea, for once-daily (od) dosing provides biphasic aceclofenac release consisting of immediate release of 85 mg followed by sustained release of 115 mg."( Pharmacokinetics of a new once-daily controlled-release formulation of aceclofenac in Korean healthy subjects compared with immediate-release aceclofenac and the effect of food: a randomized, open-label, three-period, crossover, single-centre study.
Bae, SK; Kim, SH; Lee, HJ; Lee, HW; Lee, SH; Lim, MS; Seong, SJ; Shin, SY; Yoon, YR, 2012
)
0.38
" No dose-response for diclofenac exposure was found."( Non-steroidal anti-inflammatory drugs and the risk of Clostridium difficile-associated disease.
Brassard, P; Delaney, JA; Dial, S; Suissa, D, 2012
)
0.69
" First, we established the dosing condition for liver injury in normal mice."( Involvement of immune-related factors in diclofenac-induced acute liver injury in mice.
Fukami, T; Higuchi, S; Nakajima, M; Tsuneyama, K; Yano, A; Yokoi, T, 2012
)
0.64
"Our aim was to prepare and determine the pharmacokinetics of injectable lipid nanoemulsions of diclofenac acid for treating arthritic conditions by reducing the frequency of dosing and pain at site of injection."( Formulation and pharmacokinetics of diclofenac lipid nanoemulsions for parenteral application.
Kandadi, P; Ramreddy, S; Veerabrahma, K,
)
0.62
"There were insufficient data to evaluate other doses of oral diclofenac, or to compare different formulations or different dosing regimens; only one study compared oral diclofenac with an active comparator (oral sumatriptan 100 mg)."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2012
)
2.06
" The results obtained in this study suggest that 84 days of continuous oral treatment of three different dosages of Polycan led to lesser degrees of articular stiffness and histological cartilage damage compared with OA controls 91 days after OA inducement, suggesting that the optimal Polycan dosage to treat OA is 42."( Efficacy test of Polycan, a beta-glucan originated from Aureobasidium pullulans SM-2001, on anterior cruciate ligament transection and partial medial meniscectomy-induced-osteoarthritis rats.
Cho, HR; Kim, JW; Ku, SK, 2012
)
0.38
" The variation in bioavailability and disposition of diclofenac sodium and diclofenac potassium in diabetic state will require adjustment of the dosage regimen prescribed for diabetics in clinical setting."( Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and alloxan-diabetic rabbits.
Ahmad, M; Iqbal, M; Murtaza, G, 2012
)
0.88
"The key physicochemical properties of functional excipients should be identified, and the influence of their variability on the properties of the final dosage form should be evaluated during the development phase."( Characterization of physicochemical properties of hydroxypropyl methylcellulose (HPMC) type 2208 and their influence on prolonged drug release from matrix tablets.
Baumgartner, S; Devjak Novak, S; Šporar, E; Vrečer, F, 2012
)
0.38
" It is the first described method by azo dye derivatization for the analysis of aceclofenac in bulk samples and dosage forms."( Sensitive spectrophotometric determination of aceclofenac following azo dye formation with 4-carboxyl-2,6-dinitrobenzene diazonium ion.
Adegoke, OA; Aderibigbe, SA; Idowu, OS; Olaleye, SO,
)
0.13
"In the absence of clinical studies, the ability to project the direction and the magnitude of changes in bioavailability of drug therapy, using evidence-based mechanistic pharmacokinetic in silico models would be of significant value in guiding prescribers to make the necessary adjustments to dosage regimens for an increasing population of patients who are undergoing bariatric surgery."( A mechanistic pharmacokinetic model to assess modified oral drug bioavailability post bariatric surgery in morbidly obese patients: interplay between CYP3A gut wall metabolism, permeability and dissolution.
Ammori, BJ; Ashcroft, DM; Darwich, AS; Jamei, M; Pade, D; Rostami-Hodjegan, A, 2012
)
0.38
"A reproducible, rapid and sensitive method has been developed for the assay of chlorzoxazone (CHL), paracetamol (PCM) and aceclofenac (ACE) in their combined solid dosage forms using packed-column supercritical fluid chromatography (SFC)."( Development and validation of packed column supercritical fluid chromatographic technique for quantification of chlorzoxazone, paracetamol and aceclofenac in their individual and combined dosage forms.
Desai, PP; Mehta, PJ; Patel, NR; Sherikar, OD, 2012
)
0.38
"05), respectively, but this effect did not show a dose-response relationship (P>0."( [Diclofenac inhibits Kv1.3 and Kir2.1 expressions in human macrophages and affects the membrane potential and foam cell formation].
Lei, X; Lin, X; Wang, D; Yuan, Z; Zhang, W, 2012
)
1.29
" Therapeutic products containing diclofenac sodium salt in doses of 100 mg and 75 mg with a qualitatively and quantitatively diversified share of excipients and a variable dosage form of the drug (solid capsules, tablets with modified release) were subjected to technological and pharmaceutical analysis."( [Technological and pharmacotherapeutic properties of selected drugs with modified release of diclofenac sodium].
Kołodziejczyk, MK; Kołodziejska, J; Zgoda, MM, 2012
)
0.88
"Market therapeutic products with diclofenac sodium in doses of 75 mg and 100 mg, technological analysis of the drug dosage form was conducted, disintegration time of solid oral dosage forms of the drug with diclofenac sodium salt was examined and research on pharmaceutical availability of diclofenac sodium salt from tested therapeutic products was conducted using the acid phase and the buffer phase according to the FP standards for delayed release enteral dosage forms."( [Technological and pharmacotherapeutic properties of selected drugs with modified release of diclofenac sodium].
Kołodziejczyk, MK; Kołodziejska, J; Zgoda, MM, 2012
)
0.88
" All therapeutic products bear features of a dosage form of modified release of diclofenac sodium salt, frequently of a delayed release formula in the duodenum or the small intestine with regard to the limitation of typical undesirable effects after taking NSAIDs."( [Technological and pharmacotherapeutic properties of selected drugs with modified release of diclofenac sodium].
Kołodziejczyk, MK; Kołodziejska, J; Zgoda, MM, 2012
)
0.83
"Tested therapeutic products with diclofenac sodium salt are differentiated by the type of a dosage form."( [Technological and pharmacotherapeutic properties of selected drugs with modified release of diclofenac sodium].
Kołodziejczyk, MK; Kołodziejska, J; Zgoda, MM, 2012
)
0.88
"A novel injectable formulation of diclofenac, Dyloject, utilizes hydroxypropyl-β-cyclodextrin (HPβCD) as a solubilizing agent, allowing dosing as a small-volume intravenous bolus for postoperative pain."( Analgesic efficacy and safety of a novel injectable formulation of diclofenac compared with intravenous ketorolac and placebo after orthopedic surgery: a multicenter, randomized, double-blinded, multiple-dose trial.
Carr, DB; Daniels, S; Hamilton, DA; Lang, E; Melson, T, 2013
)
0.91
"The aim of this work was to develop by means of co-extrusion a multilayered dosage form characterized by a dual release profile of the same drug."( Co-extrusion as manufacturing technique for multilayer mini-matrices with dual drug release.
Dierickx, L; Remon, JP; Vervaet, C, 2013
)
0.39
"There were insufficient data to evaluate other doses of oral diclofenac, or to compare different formulations or different dosing regimens; only one study compared oral diclofenac with an active comparator (oral sumatriptan 100 mg)."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2013
)
2.07
" Marketed formulations for parenteral administration usually contain 75 mg/3 mL of diclofenac sodium, which provide limited dosing flexibility, and are usually given intramuscularly."( Efficacy and safety of low dose subcutaneous diclofenac in the management of acute pain: a randomized double-blind trial.
Dietrich, T; Gugliotta, B; Leeson, R; Petersen, B, 2014
)
0.89
"There is a need for information on the bioavailability in pediatric patients of drugs from manipulated dosage forms when applied in combination with food and/or co-medication under realistic daily practice circumstances."( In vitro gastrointestinal model (TIM) with predictive power, even for infants and children?
Anneveld, B; de Koning, BA; de Wildt, SN; Hanff, LM; Havenaar, R; Lelieveld, JP; Minekus, M; Mooij, MG, 2013
)
0.39
"In the past decades, the vertical diffusion cell has emerged as a useful device for testing drug release of topical dosage forms."( Influence of different test parameters on in vitro drug release from topical diclofenac formulations in a vertical diffusion cell setup.
Klein, S, 2013
)
0.62
" The FSM represents a fully computer-controlled dynamic flow-through system, in which dosage forms are hosted in so-called gastric vessels."( Development of a bio-relevant dissolution test device simulating mechanical aspects present in the fed stomach.
Garbacz, G; Görke, K; Koziolek, M; Neumann, M; Weitschies, W, 2014
)
0.4
"Individual pharmacokinetics after administration of enteric coated tablets are often highly variable and this has been ascribed to the interaction of the dosage form with the physiology of the gastrointestinal tract."( Understanding the in vivo performance of enteric coated tablets using an in vitro-in silico-in vivo approach: case example diclofenac.
Blume, H; Dressman, J; Kambayashi, A, 2013
)
0.6
" Diclofenac submicron particle capsules have been developed using SoluMatrix technology to provide analgesia at lower doses than available solid oral dosing forms."( Lower-dose diclofenac submicron particle capsules provide early and sustained acute patient pain relief in a phase 3 study.
Argoff, C; Daniels, S; Gibofsky, A; Jensen, S; Silberstein, S; Young, CL, 2013
)
1.69
" Approximately 20 mg of diclofenac was applied daily to a 10 × 15 cm dosing site centered over the patella of the right knee."( Biodistribution of diclofenac following repeated topical applications of two diclofenac sodium formulations to minipigs.
Barrett, T; Devarakonda, K; Giuliani, M; Wible, JH, 2014
)
1.04
" The effects of calcination temperature, initial pH, catalyst and oxone dosage on the degradation efficiency were investigated."( CoFe2O4 magnetic nanoparticles as a highly active heterogeneous catalyst of oxone for the degradation of diclofenac in water.
Deng, J; Gao, N; Hu, X; Shao, Y; Tan, C; Zhou, S, 2013
)
0.6
" Despite the many available forms of NSAIDs, including injectable as well as topical, oral dosing is the most common route, usually the one route consistently associated with chronic use and thus the one that carries the most risk."( Nonsteroidal anti-inflammatory drugs and their risk: a story still in development.
Simon, LS, 2013
)
0.39
" We administered body-weight adjusted full dose of low-molecular weight heparin (enoxaparin) in a therapeutic dosage for 10 days."( Penile Mondor's syndrome after endovenous treatment of the great saphenous vein with 1470 nm diode laser.
Knittel, M; Schwarz, T; Zeller, T; Zerweck, C, 2015
)
0.42
" A microemulsion-based technology has various advantages over other technically complex dosage forms."( Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with zolmitriptan and diclofenac: formulation and in vitro-in vivo characterization.
Christie, M; Dubey, R; Martini, LG, 2014
)
0.62
" It was also found that the hydrated form of diclofenac sodium arises during the preparation of the dosage form the using technology of impregnating the solid carrier by non-aqueous solvents, which resulted in reducing of the drug release rate from prepared tablets up to twice."( [Monitoring of formation of diclofenac sodium salt hydrates and their influence on the drug dissolution from prepared tablets].
Doležel, P; Králová, M; Muselík, J; Vetchý, D, 2013
)
0.94
" Individual dose-response curves of the antinociceptive effect of these compounds were built to calculate the ED50, as well as the pharmacological interaction, by using isobolographic analysis."( Isobolographic analysis of the antinociceptive interaction between ursolic acid and diclofenac or tramadol in mice.
Cortés, A; Déciga-Campos, M; Díaz-Reval, I; González-Trujano, ME; Pellicer, F, 2014
)
0.63
"The objective of this research was to characterize the dissolution profile of a poorly soluble drug, diclofenac, from a commercially available multiple-unit enteric coated dosage form, Diclo-Puren® capsules, and to develop a predictive model for its oral pharmacokinetic profile."( Predicting the oral pharmacokinetic profiles of multiple-unit (pellet) dosage forms using a modeling and simulation approach coupled with biorelevant dissolution testing: case example diclofenac sodium.
Blume, H; Dressman, JB; Kambayashi, A, 2014
)
0.81
" These matrix tablets might be helpful to minimize dosing frequency and reduction of various side effects during prolong period of treatment."( In vitro aceclofenac release from IPN matrix tablets composed of chitosan-tamarind seed polysaccharide.
Basu, SK; Jana, S; Sen, KK, 2014
)
0.4
" Formulation design, development and in-vitro evaluation used in this study may serve as rational approach for manufacturing taste-masked orodispersible dosage forms."( Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations.
Breitkreutz, J; Gerber, F; Guhmann, M; Pöllinger, N; Preis, M; Weitschies, W, 2015
)
0.67
" Increasing carbon dosage and contact time enhanced the removal of micropollutants."( Adsorption characteristics of selected hydrophilic and hydrophobic micropollutants in water using activated carbon.
Choi, DJ; Her, N; Kim, SK; Nam, SW; Zoh, KD, 2014
)
0.4
"Diclofenac dosing in children for analgesia is currently extrapolated from adult data."( Postoperative analgesia using diclofenac and acetaminophen in children.
Anderson, BJ; Hannam, JA; Holford, NH; Mahadevan, M, 2014
)
2.13
" These preliminary studies could be useful in formulation development of DS especially in terms of liquid dosage forms and injectable formulations."( Solution thermodynamics and solubilization behavior of diclofenac sodium in binary mixture of Transcutol-HP and water.
Haq, N; Shakeel, F; Shazly, GA, 2014
)
0.65
"To our knowledge, this is the first study to quantify and aggregate the continuous relationship between the risk of GI or CV events and the dosage of an NSAID."( Relationship between diclofenac dose and risk of gastrointestinal and cardiovascular events: meta-regression based on two systematic literature reviews.
Miles, L; Mladsi, DM; Odom, DM; Ronquest, N; Saag, KG; Sherif, BN; Wang, J, 2014
)
0.72
"The sole objective of this work was to design successful dosage oral forms of diclofenac sodium (DiNa)-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS)."( Formulation in vitro and in vivo evaluation of SRMS-based heterolipid-templated homolipid delivery system for diclofenac sodium.
Attama, AA; Kunle, OO; Mumuni, M, 2016
)
0.87
" bi-hourly) was not observed to affect the removal efficiency of the cited conventional water quality parameters, significantly lower removal efficiencies were found for tonalide and bisphenol A for the VF wetland that received bi-hourly dosing (VS2p) (higher volume per pulse), probably due to the more reducing conditions observed in that system."( Emerging organic contaminants in vertical subsurface flow constructed wetlands: influence of media size, loading frequency and use of active aeration.
Avila, C; Bayona, JM; García, J; Headley, T; Kassa, K; Mueller, RA; Nivala, J; Olsson, L, 2014
)
0.4
" The reference dose of Diclofenac used in all randomized controlled trials is 150 mg/die; this controlled release dosage allows to decrease the number of daily administrations, ensuring a better patient compliance, especially if elderly and/or in polytherapy."( [Diclofenac: update on tolerableness and spinal anti-inflammatory action].
Sandri, A, 2014
)
1.62
" tablets, suppository, gel-formulations) with different indications, dosage recommendations and contraindications may easily lead to confusion, thus accounting for inadequate use on the one hand or withholding of an effective analgesic."( [Diclofenac up2date - Part 1: Pharmacology and comparison with other drugs].
Bolbrinker, J; Bushuven, S; Heise, D, 2014
)
1.31
" The dosage is 50 mg of powdered diclofenac potassium dissolved in 1 to 2 ounces (30 to 60 mL) of water prior to administration, with dosing time in relation to food intake not specified - this was the case for the pivotal efficacy and safety trials in subjects with acute migraine attacks in which the primary endpoints were achieved."( Differential pharmacokinetics of diclofenac potassium for oral solution vs immediate-release tablets from a randomized trial: effect of fed and fasting conditions.
Bujanover, S; Chen, C; Kareht, S; Rapoport, AM, 2015
)
0.98
" tablets, suppository, gel-formulations) with different indications, dosage recommendations and contraindications may easily lead to confusion, thus accounting for inadequate use on the one hand or withholding of an effective analgesic."( [Diclofenac up2date - Part 2: The use in specific groups of patients].
Bolbrinker, J; Bushuven, S; Heise, D, 2014
)
1.31
" Effects of orally dosed standard analgesics on CRANE were examined 48 h following bilateral CFA injection."( Complete Freund's adjuvant-induced reduction of exploratory activity in a novel environment as an objective nociceptive endpoint for sub-acute inflammatory pain model in rats.
Bannon, AW; Joshi, SK; Zhu, CZ, 2015
)
0.42
"Among their beneficial effects, non-steroidal anti-inflammatory drugs may also exert several side effects which depend on the dosage and the type of these medications."( [Cardiovascular side effects of non-steroidal anti-inflammatory drugs in the light of recent recommendations. Diclofenac is not more dangerous].
Horváth, VJ; Koós, CG; Lakatos, P; Putz, Z; Szabó, G; Tabák, GÁ, 2015
)
0.63
" Both DCF and SMX were removed from solution (adsorbed to GO), up to 35% and 12%, respectively, within 6h, and an increase in GO dosage enhanced the removal of DCF."( Adsorption characteristics of diclofenac and sulfamethoxazole to graphene oxide in aqueous solution.
Boateng, LK; Flora, JR; Her, N; Jung, C; Li, H; Nam, SW; Yoon, Y; Yu, M; Zoh, KD, 2015
)
0.71
"This Phase III multicenter, open-label study assessed the safety of SoluMatrix diclofenac in patients with OA dosed up to 52 weeks (ClinicalTrials."( Low-dose SoluMatrix diclofenac in the treatment of osteoarthritis: A 1-year, open-label, Phase III safety study.
Altman, RD; Cryer, B; Gibofsky, A; Hochberg, MC; Hopkins, WE; Imasogie, O; Kivitz, A; Markenson, JA; Nezzer, J; Strand, V; Young, CL, 2015
)
0.97
" Delayed- and extended-release forms of diclofenac sodium were initially developed with the goal of improving the safety profile of diclofenac and providing convenient, once-daily dosing for the treatment of patients with chronic pain."( Advances in NSAID development: evolution of diclofenac products using pharmaceutical technology.
Altman, R; Bosch, B; Brune, K; Patrignani, P; Young, C, 2015
)
0.95
"The safety results from the Phase III studies indicate that all dosing regimens of low-dose SoluMatrix diclofenac up to 12 weeks are generally well tolerated."( Low-dose SoluMatrix diclofenac : a review of safety across two Phase III studies in patients with acute and osteoarthritis pain.
Altman, R; Daniels, S; Gibofsky, A; Imasogie, O; Young, C, 2015
)
0.96
"5% topical solutions as well as lower systemic exposure compared to oral dosing (approximately 93% less)."( Bioequivalence of diclofenac sodium 2% and 1.5% topical solutions relative to oral diclofenac sodium in healthy volunteers.
Holt, RJ; Kent, JD; Taiwo, T, 2015
)
0.75
" In the first pair, patients of the main group (n = 31) received APTPA (a combination of 500 mg of glucosamine hydrochloride and 500 mg of chondroitin sulfate) in dosage 1 tablet twice a day during 1 month and then 1 tablet during 2 months plus melaxen (3 mg of melatonin 30-40 min before sleep), patients of the control group (n = 29) received only APTPA."( [A role of melatonin in the treatment of low back pain].
Danilov, AB; Kurganova, YM, 2015
)
0.42
"Rats were given either vehicle or rebamipide (30 mg/kg) orally twice daily for two days, then on the third day respective groups were dosed with either vehicle, celecoxib (40 mg/kg), or diclofenac (10 mg/kg) in addition to a respective dose of vehicle or rebamipide."( Celecoxib or diclofenac hepatic status in the presence or absence of rebamipide.
Denham, JW; Harirforoosh, S; Murrell, DE; Panus, PC; Rahmasari, Y, 2015
)
0.98
" In a cross-over study, 12 healthy male volunteers were given 50 mg CAPSULE and diclofenac sodium enteric-coated tablet (abbreviated as TABLET, used as a control dosage form) at fasting."( Pharmacokinetic Study of a Diclofenac Sodium Capsule Filled with Enteric-coated Pellets in Healthy Chinese Volunteers by Liquid Chromatography-electrospray Ionization-tandem Mass Spectrometry.
Deng, M; Liu, H; Liu, M; Ma, JY; Tong, Y; Yang, M; Zhang, Y; Zhao, H, 2016
)
0.96
" The presence of a low dosage of Cl(-)(0-10 mM) promoted the degradation of DCF, whereas high Cl(-) addition (>10 mM) inhibited DCF degradation."( Oxidative degradation of diclofenac by thermally activated persulfate: implication for ISCO.
Chen, J; Huang, T; Liu, H; Qian, Y, 2016
)
0.74
" COX selectivity was determined from dose-response curves by calculating a ratio (COX-2/COX-1) of IC50 values."( In vitro pharmacological evaluation of multitarget agents for thromboxane prostanoid receptor antagonism and COX-2 inhibition.
Bertinaria, M; Buccellati, C; Capra, V; Carnevali, S; Cena, C; Fruttero, R; Garella, D; Hoxha, M; Rolando, B; Rovati, GE; Sala, A, 2016
)
0.43
" The blood samples were collected after DIC dosing and analyzed by HPLC."( Effect of Resveratrol Treatment on the Pharmacokinetics of Diclofenac in Healthy Human Volunteers.
Bedada, SK; Neerati, P; Yellu, NR, 2016
)
0.68
" The performed microarray studies informed on > 600 differential expressed genes of which 35, 37 and 50 coded for inflammation, 51, 44 and 61 for immune and 116, 129 and 169 for stress response, respectively after single and repeated dosing for 3 and 14 days."( Immunogenomics reveal molecular circuits of diclofenac induced liver injury in mice.
Borlak, J; Choi, MS; Lee, EH; Oh, JH; Park, SM; Selvaraj, S; Spanel, R; Yoon, S, 2016
)
0.7
"Oral delivery of drugs is the most common method, but due to the inability of drugs to restrain and localize in the gastro-intestinal tract, oral administration of drugs in conventional dosage forms have short-term limitations."( Effect of Calcium Chloride on Release Behavior of Babul (Acacia nilotica) gum Microbeads.
Malviya, R; Sharma, PK,
)
0.13
"SoluMatrix diclofenac at two dosage strengths demonstrated an opioid-sparing effect postoperatively in this phase 3 study."( SoluMatrix® Diclofenac: Sustained Opioid-Sparing Effects in a Phase 3 Study in Patients with Postoperative Pain.
Argoff, C; Gudin, J; McCarberg, B; Nalamachu, S; Young, C, 2016
)
1.2
" Both 27 and 48 demonstrated robust activity in the acute rat monoiodoacetate-induced osteoarthritis model of pain, and subchronic dosing of 48 showed a shift to a lower EC50 over 7 days."( Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Daanen, JF; DeGoey, DA; El-Kouhen, OF; Fricano, MM; Frost, JM; Ghoreishi-Haack, N; Gum, RJ; Hsieh, GC; Kort, ME; Lundgaard, GL; Matulenko, MA; Neelands, T; Pai, M; Shi, L; Zhan, C; Zhang, XF, 2016
)
0.43
" The influence of pH, concentration of hydrogen peroxide, FeZ wt% within the composite, and photocatalyst dosage on DCF removal and conversion efficiency by solar/TiO2-FeZ/H2O2 process was investigated."( Solar-driven photocatalytic treatment of diclofenac using immobilized TiO2-based zeolite composites.
Bozic, AL; Dionysiou, DD; Fanetti, M; Kete, M; Kovacic, M; Kusic, H; Salaeh, S; Stangar, UL; Suligoj, A, 2016
)
0.7
"This study is a 6-week, randomized, double-blind, controlled, parallel-group trial with two intervention arms (ketamine, fixed daily dosage of 150mg vs."( Efficacy and safety of oral ketamine versus diclofenac to alleviate mild to moderate depression in chronic pain patients: A double-blind, randomized, controlled trial.
Afarideh, M; Agah, E; Akhondzadeh, S; Arbabi, M; Ghajar, A; Jafarinia, M; Noorbala, AA; Saravi, MA; Tafakhori, A, 2016
)
0.7
"To examine consumers' proposed behaviors regarding dosage and storage as a measure of a medicine label's usability and consumers' functional health literacy."( User testing as a method for identifying how consumers say they would act on information related to over-the-counter medicines.
Aslani, P; Raynor, DK; Tong, V,
)
0.13
"Appropriate dosing for constant back pain was reported by 29 consumers."( User testing as a method for identifying how consumers say they would act on information related to over-the-counter medicines.
Aslani, P; Raynor, DK; Tong, V,
)
0.13
"Consumers may act inappropriately on OTC label information about dosage and/or storage, which could potentially adversely impact medication use."( User testing as a method for identifying how consumers say they would act on information related to over-the-counter medicines.
Aslani, P; Raynor, DK; Tong, V,
)
0.13
" Rectal diclofenac (100 mg) has been shown to reduce the incidence of pancreatitis; however, this dosage form is unavailable in several countries."( No Benefit of Oral Diclofenac on Post-Endoscopic Retrograde Cholangiopancreatography Pancreatitis.
Doi, S; Hayashi, T; Hisai, H; Ishiwatari, H; Iwashita, T; Kato, J; Kawakami, H; Kawakubo, K; Matsusaki, S; Ono, M; Sakamoto, N; Sonoda, T; Urata, T; Yasuda, I, 2016
)
1.2
"An innovative simple, fast, precise and accurate ultra-high performance liquid chromatography (UPLC) method was developed for the determination of diclofenac (Dic) along with its impurities including the new dimer impurity in various pharmaceutical dosage forms."( A novel stability-indicating UPLC method development and validation for the determination of seven impurities in various diclofenac pharmaceutical dosage forms.
Azougagh, M; Bakhous, K; Benaji, B; Elkarbane, M; Iben Moussad, S; Issmaili, S; Skalli, A, 2016
)
0.84
" The present findings may contribute to more efficient and reliable PAT solutions in the manufacturing of prolonged release dosage forms."( Applicability of near-infrared spectroscopy in the monitoring of film coating and curing process of the prolonged release coated pellets.
Hudovornik, G; Korasa, K; Vrečer, F, 2016
)
0.43
" Worldwide health authorities, including the European Medicines Agency, Health Canada, and the US Food and Drug Administration, have advised that NSAIDs be prescribed at the lowest effective dosage and for the shortest duration."( Cost-effectiveness of Low-dose Submicron Diclofenac Compared With Generic Diclofenac.
Miles, L; Mladsi, D; Odom, D; Ronquest, N; Saag, K, 2016
)
0.7
"Our results suggest that over the duration and dosage examined, DICLO-NP may reduce renal necrosis without influencing other side effects or drug characteristics."( Examination of the pharmacodynamics and pharmacokinetics of a diclofenac poly(lactic-co-glycolic) acid nanoparticle formulation in the rat.
Denham, JW; Hanley, GA; Harirforoosh, S; Murrell, DE; Panus, PC; West, KO, 2016
)
0.67
" The granules possessed a satisfactory dosage uniformity, a flowability suitable for an oral dosage form manufacturing, along with a sustained drug release up to 9h, driven by both ion exchange and transport kinetics."( Surface modified zeolite-based granulates for the sustained release of diclofenac sodium.
Biondi, M; Catalanotti, L; de Gennaro, B; De Rosa, G; Iaffaioli, RV; Mayol, L; Quagliariello, V; Serri, C, 2017
)
0.69
"The objective of the present investigation was to assess of Araucaria gum (AHG) obtained from bark exudates of the Araucaria heterophylla (family: Araucariaceae) for the design of oral controlled release forms, in particular tablet dosage forms by using matrix systems."( Araucaria Gum: Novel Natural Polymer for Controlled Drug Delivery. Development, In Vitro and In Vivo Evaluation of Araucaria Gum Based Matrix Tablets for Controlled Release.
Lohithasu, D; Naga Durga, DH; Ramana Murthy Kolapalli, V, 2017
)
0.46
"The above results clearly indicated that AHG gum can be used for the development of oral controlled release dosage forms by using matrix systems."( Araucaria Gum: Novel Natural Polymer for Controlled Drug Delivery. Development, In Vitro and In Vivo Evaluation of Araucaria Gum Based Matrix Tablets for Controlled Release.
Lohithasu, D; Naga Durga, DH; Ramana Murthy Kolapalli, V, 2017
)
0.46
"Nausea at the time of dosing does not diminish the effectiveness of diclofenac potassium for oral solution."( Post Hoc Subanalysis of Two Randomized, Controlled Phase 3 Trials Evaluating Diclofenac Potassium for Oral Solution: Impact of Migraine-Associated Nausea and Prior Triptan Use on Efficacy.
Diener, HC; Lipton, RB; Schmidt, P, 2017
)
0.92
" Histological analysis revealed a significant increase in the proportion of renal hematopoietic tissue (renal hematopoietic hyperplasia) after 28days at the lowest concentration and at all higher concentrations, following a clear dose-response pattern."( Diclofenac affects kidney histology in the three-spined stickleback (Gasterosteus aculeatus) at low μg/L concentrations.
Asker, N; Ekman, E; Fick, J; Larsson, DGJ; Näslund, J; Norrgren, L, 2017
)
1.9
"This research aims to evaluate the role of tamsulosin in the medical expulsion therapy for distal ureteral stones, including her effects in stone expulsion time, expulsion rates, stone size, pain episodes and analgesic dosage usage."( The Role of the Tamsulosin in the Medical Expulsion Therapy for Distal Ureteral Stones.
Hyseni, N; Nuraj, P, 2017
)
0.46
"61 h from healthy birds dosed intravenously at 5 mg/kg."( The use of toxicokinetics and exposure studies to show that carprofen in cattle tissue could lead to secondary toxicity and death in wild vultures.
Chipangura, J; Duncan, N; Galligan, TH; Green, RE; Naidoo, V; Taggart, MA; Wolter, K, 2018
)
0.48
" Dose-response curves were then obtained and analyzed after the co-administration of geraniin with morphine or diclofenac in fixed ratio (1:1) combinations based on specific fractions (1/2, 1/4, and 1/8) of their respective ED50 values for the formalin test."( An isobolographic analysis of the anti-nociceptive effect of geraniin in combination with morphine or diclofenac.
Abotsi, WKM; Agyare, C; Ameyaw, EO; Biney, RP; Boakye-Gyasi, E; Kasanga, EA; Woode, E, 2018
)
0.91
" TSQM scores for global satisfaction (P < 0·001) and effectiveness (P = 0·002) were higher with IngMeb, as was dosing instruction adherence (≥ 90% vs."( Phase IV head-to-head randomized controlled trial comparing ingenol mebutate 0·015% gel with diclofenac sodium 3% gel for the treatment of actinic keratosis on the face or scalp.
Harwood, CA; Larsson, T; Serra-Guillén, C; Skov, T; Stockfleth, E; Østerdal, ML, 2018
)
0.7
" The proposed method was validated according to the ICH guidelines and was successfully applied to the analysis of these drugs in their tablet dosage forms with high accuracy."( Simultaneous Determination of Tizanidine, Nimesulide, Aceclofenac and Paracetamol in Tablets and Biological Fluids Using Micellar Liquid Chromatography.
Belal, F; Derayea, S; Hammad, MA; Omar, MA; Saleh, SF; Zayed, S, 2018
)
0.48
" Dose-response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid-induced writhing test in mice."( Assessment of the antinociceptive and ulcerogenic activity of the tapentadol-diclofenac combination in rodents.
Alonso-Castro, ÁJ; Granados-Soto, V; Isiordia-Espinoza, MA; Sánchez-Enriquez, S; Zapata-Morales, JR, 2018
)
0.96
" In this study, the permeability of human skin was compared using two synthetic membranes: cellulose acetate and Strat-M® membrane and lipophilic and hydrophilic compounds either as saturated or formulated solutions as well as marketed dosage forms."( Membrane properties for permeability testing: Skin versus synthetic membranes.
Dorrani, M; Goodyear, B; Haq, A; Joshi, V; Michniak-Kohn, B, 2018
)
0.48
" Additionally, diclosomes were incorporated into gel dosage forms and their performance in terms of permeation enhancement were evaluated."( Innovative topical formulations from diclofenac sodium used as surfadrug: The birth of Diclosomes.
Mazzotta, E; Muzzalupo, R; Tavano, L, 2018
)
0.75
" The simulated gastric/intestinal fluid of DDASS was improved in this study to realize the influence of dynamic pH change on the complete oral dosage form."( In Vitro-In Vivo Predictive Dissolution-Permeation-Absorption Dynamics of Highly Permeable Drug Extended-Release Tablets via Drug Dissolution/Absorption Simulating System and pH Alteration.
Feng, G; Gu, H; He, X; Li, ZQ; Nyagblordzro, M; Tian, S; Wu, ZG, 2018
)
0.48
" Dosage, maximum daily dose, and contraindications information was found and understood by most (≥9/10 per group), except the Voltaren dosage which was misunderstood by 4/20."( Comparative User Testing of Australian and UK Over-the-Counter Labels and Leaflets for Diclofenac.
Aslani, P; Raynor, DK; Tong, V, 2018
)
0.7
" The recommended dosing regimens have generally ranged from 3 to 5 injections."( Efficacy of a Single Intra-Articular Injection of 2% Sodium Hyaluronate Plus 0.5% Mannitol in Patients with Symptomatic Osteoarthritis of the Knee: A Preliminary Report.
Lamsam, C; Lertwanich, P, 2016
)
0.43
" Kuntze have good potential to improve drug entrapment efficiency of the CA beads, and the DS-loaded GS-CA beads can be used as multiunit dosage forms for sustaining drug release in simulated GI condition."( Modification of alginate beads using gelatinized and ungelatinized arrowroot (Tacca leontopetaloides L. Kuntze) starch for drug delivery.
Khlibsuwan, R; Pongjanyakul, T; Tansena, W, 2018
)
0.48
" In the source water system, the integrated AC-NF process with coagulation pretreatment (the alum dosage of 60 mg/L) achieved satisfactory performance (the removal efficiencies of three target compounds reached > 95%)."( Performance evaluation of integrated adsorption-nanofiltration system for emerging compounds removal: Exemplified by caffeine, diclofenac and octylphenol.
Chiang, PC; Dang, Z; Gong, B; Huang, CP; Huang, Z; Pan, SY; Wu, P, 2019
)
0.72
" The experiment shows absorption of DS increased by increasing IL dosage in modifying Mt."( Preparation of ionic liquids/montmorillonite composites and its application for diclofenac sodium removal.
Gao, L; Tang, N; Wang, Q; Wu, L, 2019
)
0.74
"This study investigated gastrointestinal drug concentrations of the weakly acidic drug diclofenac when dosed to healthy volunteers after intake of the FDA standard meal."( Gastric and Duodenal Diclofenac Concentrations in Healthy Volunteers after Intake of the FDA Standard Meal: In Vivo Observations and in Vitro Explorations.
Augustijns, P; Brouwers, J; Rubbens, J; Tack, J, 2019
)
1.06
"Human liver slice function was stressed by daily dosing of acetaminophen (APAP) or diclofenac (DCF) to investigate injury and repair."( Progression of Repair and Injury in Human Liver Slices.
Fisher, RL; Ulyanov, AV; Vickers, AEM, 2018
)
0.71
" The developed clay/polymer hybrids can act as potential candidates for the design of modified dosage forms of anionic drugs."( Chitosan/beidellite nanocomposite as diclofenac carrier.
Cheikh, D; García-Villén, F; Majdoub, H; Viseras, C; Zayani, MB, 2019
)
0.79
" The most significant benefit of this dosage format will only be realised once more pharmaceutical products become available."( Characterisation and optimisation of diclofenac sodium orodispersible thin film formulation.
Dunn, C; Ford, S; Halbert, G; Khadra, I; Mullen, A; Obeid, MA; Watts, S, 2019
)
0.79
" Some recent studies have also contributed to its prospective case in oral drug delivery and dosage forms albeit with limited commercial viability."( Clay nanotubes as a novel multifunctional excipient for the development of directly compressible diclofenac potassium tablets in a SeDeM driven QbD environment.
Ahmed, FR; Ahmed, K; Ali, T; Geckeler, KE; Qazi, F; Shoaib, MH; Siddiqui, F; Yousuf, RI, 2019
)
0.73
" Adult Wistar rats treated with CPZ (3 mg/kg/day, IP) were orally dosed with diclofenac and L-dopa/carbidopa for 21 days."( Neuroprotective effect of diclofenac on chlorpromazine induced catalepsy in rats.
Khan, SS; Mirza, T; Naeem, S; Najam, R; Sikandar, B, 2019
)
1.04
"5-15 mg/kg), the effective dosage range of diclofenac was identified (> 5 mg/kg/day)."( Dose-dependency of the cardiovascular risks of non-steroidal anti-inflammatory drugs.
Ahmed, SA; Al-Lawati, H; Jamali, F, 2019
)
0.78
" Through the definition of IVRT analytical target profile, a risk assessment analysis was carried out, in which the critical analytical attributes (in vitro release rate, cumulative amount released at an initial/final point and dose depletion) and critical method variables (medium, membrane and dosage regimen) were identified."( aQbD as a platform for IVRT method development - A regulatory oriented approach.
Cardoso, C; Miranda, M; Pais, AACC; Vitorino, C, 2019
)
0.51
" Acidic to neutral pH conditions were more favorable for DCF adsorption, while increasing initial DCF concentration and adsorbent dosage resulted in higher DCF removal efficiencies for the three oxides."( Optimization, isotherm, and kinetic studies of diclofenac removal from aqueous solutions by Fe-Mn binary oxide adsorbents.
de Luna, MDG; Ensano, BMB; Ong, DC; Pingul-Ong, SMB; Rivera, KKP, 2019
)
0.77
"This research aims at formulation of controlled release dosage form containing curcumin microspheres and diclofenac diethylamine and then incorporating it into gel formulation for treatment of inflammation associated with rheumatoid arthritis."( Controlled Release Gel Encompassing Curcumin Microspheres and Diclofenac Diethylamine for Feat Against Arthritis Inflammation.
Dabre, S; Singh, P, 2020
)
1.01
"1- fold higher ex vivo corneal permeation than their respective conventional aqueous solution dosage forms."( Optimization of the Interaction between Diclofenac and Ibuprofen with Benzalkonium Chloride to Prepare Ocular Nanosuspension.
Ahuja, M; Kumar, T; Tak, D, 2019
)
0.78
"The optimized nanosuspension formulations of diclofenac and ibuprofen were found to be physically stable and microbiologically safe with greater corneal penetration than the conventional solution dosage forms."( Optimization of the Interaction between Diclofenac and Ibuprofen with Benzalkonium Chloride to Prepare Ocular Nanosuspension.
Ahuja, M; Kumar, T; Tak, D, 2019
)
1.04
"Hormesis is an ecotoxicological phenomenon referred to as the biphasic dose-response effect."( Elimination of the hormesis phenomenon by the use of synthetic sea water in a toxicity test towards Aliivibrio fischeri.
Drzymała, J; Kalka, J, 2020
)
0.56
" A clinical dosage (4 mg/mL) of dexamethasone (Dex) showed toxic effects on chondrocytes, and the long-time treatment by lower doses (4-400 μg/mL) induced hypertrophic changes in the chondrocytes."( Primary Human Chondrocytes Affected by Cigarette Smoke-Therapeutic Challenges.
Arnscheidt, C; Aspera-Werz, RH; Chen, T; Ehnert, S; Nussler, AK; Tendulkar, G; Zhu, S, 2020
)
0.56
"To evaluate currently approved analgesics, that is, opioids, nonsteroidal anti-inflammatory drugs (NSAIDs), anticonvulsants, and serotonin and norepinephrine reuptake inhibitors (SNRIs) used as analgesics, for 1) differences in pharmacokinetic parameters under fed vs fasting conditions and 2) factors involved in dosage recommendations in relation to food."( Effects of Food on Bioavailability of Analgesics; Resulting Dosage and Administration Recommendations.
Hertz, SH; Lee, DJ; Naraharisetti, SB; Sahajwalla, C; Srour, S; Xu, Y, 2020
)
0.56
" Based on 79 analgesic products reviewed, food effect dosage recommendations depend on whether an analgesic will be dosed on a regular interval around-the-clock vs on an as-needed basis, the shape of concentration-time profile, steady-state concentrations, the type of meals used in the pharmacokinetic study, and drug administration with regard to food in clinical trials."( Effects of Food on Bioavailability of Analgesics; Resulting Dosage and Administration Recommendations.
Hertz, SH; Lee, DJ; Naraharisetti, SB; Sahajwalla, C; Srour, S; Xu, Y, 2020
)
0.56
" 80% DCF was removed at mild condition (pH 6-7) within 60 s, and its removal rate could be enhanced with the increase in Fe(II) dosage and PAA concentration."( Degradation of diclofenac by Fe(II)-activated peracetic acid.
Fu, Y; Liu, Y; Shi, H; Wang, S; Wang, Z, 2021
)
0.97
" The objective of this study was to develop a tunable extruded 3D printing platform based on thermo-sensitive gelatin pastes to meet the needs of achieving different drug release characteristics with flexible dosing and design."( A tunable extruded 3D printing platform using thermo-sensitive pastes.
Ivone, R; Lin, X; Shen, J; Wang, X; Xie, L; Yang, G; Yang, Y, 2020
)
0.56
" Notably, slow addition of any of the four therapeutics to cultured macrophages, mimicking the slowly increasing plasma concentration reported for standard oral dosage in patients, yielded no detectable change in pseudopod morphology."( Rapid exposure of macrophages to drugs resolves four classes of effects on the leading edge sensory pseudopod: Non-perturbing, adaptive, disruptive, and activating.
Buckles, TC; Djukovic, D; Falke, JJ; Ziemba, BP, 2020
)
0.56
" Thus, the developed method can be used for the combined dosage form analysis and its chemical stability studies."( Synchronous UPLC Resolution of Aceclofenac and Diacerin in Their Powdered Forms and Matrix Formulation: Stability Study.
Abd El-Rahman, MK; Ahmed, DA; Lotfy, HM; Weshahy, SA, 2020
)
0.56
" Spurred by topical advancement in polymer chemistry and drug delivery, hydrogels that release a drug in temporal, spatial and dosage controlled fashion have been trendy."( Inflammation targeted chitosan-based hydrogel for controlled release of diclofenac sodium.
Butt, MTZ; Butt, OM; Gull, N; Islam, A; Jabeen, S; Khan, A; Khan, RU; Khan, SM; Khan, SU; Shah, A, 2020
)
0.79
"To evaluate the pharmacokinetics, safety, and tolerability of a single 50-mg oral dose of diclofenac potassium for oral solution (OS) in a pediatric cohort with a diagnosis of episodic migraine; the 3-month safety trial following an outpatient dosing period was also evaluated."( An Open-Label Study Evaluating the Pharmacokinetics and Safety of Diclofenac Potassium for Oral Solution for the Acute Treatment of MWA or MWoA in Pediatric Participants.
Amend, DL; Ferger, SM; Hogan, RM; McVige, JW; Shanahan, CM, 2020
)
1.02
"12 % at pH 6, biosorbent dosage 25 mg for 50 mg/L of DCF."( Ecotoxicological assessment of micropollutant Diclofenac biosorption on magnetic sawdust: Phyto, Microbial and Fish toxicity studies.
Narayanasamy, S; Shahnaz, T; Sivaprakasam, S; Suganya, E; Vishnu Priyan, V, 2021
)
0.88
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" Also, dosage and frequency of the received Diclofenac and adverse effects of the intervention were recorded."( Effects of Aromatherapy with Lavender (Lavandula angustifolia MILL) on Post-Dural Puncture Headache: A Randomized Placebo-Controlled Trial.
Asayesh, H; Bahadori, H; Hosseini Amiri, M; Nasiri, M; Rajaee, M; Yousefi Khosroabadi, Z, 2022
)
0.98
" The second phase was similar to the first, except each treatment was administered at a dosage of 1 drop/eye, twice daily for 5 days and CS was measured before treatment initiation and at 15 minutes and 24 and 48 hours after the last dose."( Effects of topical instillation of 0.1% diclofenac sodium, 0.5% ketorolac tromethamine, and 0.03% flurbiprofen sodium on corneal sensitivity in ophthalmologically normal cats.
Meekins, JM; Rankin, AJ; Roberts, JK; Roush, JK, 2021
)
0.89
"Improved bioavailability of Aceclofenac (ACE) may be achieved through proniosomes, which are considered as one of the most effective drug delivery systems and are expected to represent a valuable approach for the development of better oral dosage form as compared to the existing product."( Effect of Different Carriers on In Vitro and In Vivo Drug Release Behavior of Aceclofenac Proniosomes.
Chatterjee, B; Saleh, MSM; Sammour, RMF; Shahiwala, A; Taher, M, 2021
)
0.62
" Specifically, we demonstrated that treatment with diclofenac (DCF), an NSAID commonly used to treat inflammation associated with acute infection and other conditions, globally suppressed cytokine secretion when dosed in isolation."( Synergistic Action of Diclofenac with Endotoxin-Mediated Inflammation Exacerbates Intestinal Injury
Carrier, RL; Chen, WLK; Griffith, LG; Lauffenburger, DA; Miyazaki, H; Suter, E; Velazquez, J, 2021
)
1.19
"An emulsion is a biphasic dosage form comprising of dispersed phase containing droplets that are uniformly distributed into a surrounding liquid which forms the continuous phase."( Solid-in-Oil-in-Water Emulsion: An Innovative Paradigm to Improve Drug Stability and Biological Activity.
Kamath, S; Kg, H; Kulyadi, GP; Sawant, A, 2021
)
0.62
" himalayensis by oral gavage, with 15 control birds dosed with benzyl alcohol (the carrier solution for tolfenamic acid)."( Experimental safety testing shows that the NSAID tolfenamic acid is not toxic to Gyps vultures in India at concentrations likely to be encountered in cattle carcasses.
Chandramohan, S; Chutia, K; Galligan, TH; Green, RE; Gupta, R; Kesavan, M; Mahendran, K; Mallord, JW; Mathesh, K; Pawde, A; Prakash, NV; Prakash, VM; Ravichandran, P; Saikia, D; Sharma, AK; Shringarpure, R; Timung, A, 2022
)
0.72
" It is demonstrated that the combination of Diclofenac concentration prediction via NIR spectroscopy and mass prediction via 3D MRT allow to estimate the dosage of each individual tablet."( Towards real-time release of pharmaceutical tablets: 100% in-line control via near-infrared spatially resolved spectroscopy and 3D microwave resonance technology.
Brouckaert, D; Chauchard, F; Dollinger, M; Krumme, M; Pellegatti, L; Roggo, Y; Vandenbroucke, F, 2022
)
0.98
" Here, we describe the tissue distribution analysis of diclofenac from a dosed whole-body mouse thin tissue section using a dropletProbe mass spectrometry system."( Development and Application of DropletProbe Mass Spectrometry for Examining Biodistribution of Therapeutics.
Cancilla, MT; Chen, B; Kertesz, V; Vavrek, M, 2022
)
0.97
" Therefore, this study aimed to investigate a foamable microemulsion as an alternative topical and transdermal dosage form for diclofenac sodium (DS)."( In Vitro Evaluation of a Foamable Microemulsion Towards an Improved Topical Delivery of Diclofenac Sodium.
Azarmi, S; Bou-Chacra, NA; Hajjar, B; Löbenberg, R; Park, C; Silva, DA; Zuo, J, 2022
)
1.15
" The blood samples were taken before dosing and at 4th, 8th, 24th and 72nd hour post-dosing for measurement of cardiac markers such as H-FABP, cTn-I, CK-MB."( The effect of tilmicosin and diclofenac sodium combination on cardiac biomarkers in sheep.
Atik, O; Corum, O; Durna Corum, D; Ider, M; Ok, M; Uney, K; Yildiz, R, 2023
)
1.2
" In this survey, the prescribed dosage was reduced or discontinued in 150 and 56 patients, respectively, receiving celecoxib and diclofenac prescribed alone, as recorded in a Japanese database of adverse drug events."( Plasma and Hepatic Exposures of Celecoxib and Diclofenac Prescribed Alone in Patients with Cytochrome P450 2C9*3 Modeled after Virtual Oral Administrations and Likely Associated with Adverse Drug Events Reported in a Japanese Database.
Adachi, K; Murayama, N; Nakano, H; Ohyama, K; Saito, Y; Sato, T; Shimizu, M; Tanaka, Y; Yamazaki, H, 2023
)
1.37
" Furthermore, the influence of the following parameters of the vertical flow constructed wetlands on wastewater toxicity was investigated: the dosing system, the presence of pharmaceuticals and the plants Miscanthus giganteus."( Effects of diclofenac, sulfamethoxazole, and wastewater from constructed wetlands on Eisenia fetida: impacts on mortality, fertility, and oxidative stress.
Drzymała, J; Kalka, J, 2023
)
1.3
" The cumulative dosage of diclofenac in the PHN131 group was only around half of that in the placebo group ( P <0."( Safety and Efficacy of Oral Nalbuphine on Postoperative Pain in Hemorrhoidectomy Patients: A Randomized, Double-blind, Placebo-controlled, Pivotal Trial.
Chen, WS; Hsiao, KH; Hu, OY; Jao, SW; Jiang, JK; Lee, CC; Lee, TY; Lin, CC; Lin, HC; Lin, TC; Wu, CC, 2023
)
1.21
" High performance liquid chromatography coupled with atmospheric pressure chemical ionization-ion trap mass spectrometry (HPLC-APCI-MS) analyses of the degradation products of diclofenac in aqueous dosage revealed the presence of at least seven products while HR Orbitrap MS analysis showed that the enzymatic treatment produced high molecular weight metabolites through a radical oligomerization mechanism of diclofenac."( Removal and degradation of sodium diclofenac via radical-based mechanisms using S. sclerotiorum laccase.
Coman, C; Hădade, N; Moț, AC; Pesek, S; Silaghi-Dumitrescu, R, 2023
)
1.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitorA compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
drug allergenAny drug which causes the onset of an allergic reaction.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
monocarboxylic acidAn oxoacid containing a single carboxy group.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
amino acidA carboxylic acid containing one or more amino groups.
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

PathwayProteinsCompounds
Diclofenac Action Pathway2967
Diclofenac metabolic pathway56

Protein Targets (44)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC50 (µMol)1.90000.00101.94459.6000AID1199060
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC50 (µMol)0.00300.00051.41288.2000AID347221
Bile salt export pumpHomo sapiens (human)IC50 (µMol)54.48500.11007.190310.0000AID1443986; AID1449628
Dihydrofolate reductaseHomo sapiens (human)Ki160.00000.00000.37564.9000AID1660990
Cytochrome c oxidase subunit 2Homo sapiens (human)IC50 (µMol)10.05000.02000.84933.0000AID1717039
Carbonic anhydrase 1Homo sapiens (human)IC50 (µMol)100.00000.00582.14107.9000AID1796989; AID50345
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)100.00000.00021.10608.3000AID1796989; AID47749
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki19.31000.01501.24876.9200AID407366; AID407369
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)3.40110.00032.177410.0000AID1061773; AID1141098; AID1142444; AID1164201; AID1164203; AID1196112; AID1226814; AID1301936; AID1426399; AID1461593; AID1542241; AID1608176; AID1650563; AID1717038; AID1810791; AID325048
Cytochrome P450 3A4Homo sapiens (human)Ki1,640.00000.00011.41629.9000AID589146
Interleukin-8Homo sapiens (human)IC50 (µMol)0.00800.00800.04360.0900AID426392
Calcium/calmodulin-dependent protein kinase type II subunit alphaRattus norvegicus (Norway rat)Ki5.10000.02201.47405.1000AID1909902
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Fatty acid-binding protein, intestinalHomo sapiens (human)Ki86.30000.30005.48149.4000AID1801103
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC50 (µMol)100.00000.00101.191310.0000AID1199061
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50 (µMol)131.00000.10002.50004.9000AID1802994
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50 (µMol)131.00004.90004.90004.9000AID1802994
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50 (µMol)131.00000.30003.25807.3000AID1802994
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Ki52.00008.50008.50008.5000AID624642
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50 (µMol)131.00004.72004.81004.9000AID1802994
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)1.55720.00021.557410.0000AID1301936; AID1423032; AID161484; AID1650563; AID312490; AID313126; AID340309; AID348028; AID390753; AID403703; AID625243; AID664063
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.00132.22068.3000AID179746
C-X-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)5.00600.00102.022710.0000AID426476; AID426477
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.00321.79008.3000AID179746
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.00321.54318.3000AID179746
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)3.27510.00010.995010.0000AID1061774; AID1142445; AID1164203; AID1226815; AID1301937; AID1423035; AID1426401; AID1461599; AID1608177; AID162494; AID1650564; AID1810792; AID254798; AID254882; AID313125; AID325050; AID325055; AID347222; AID403704; AID546254; AID625244; AID664066
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.00291.786810.0000AID179746
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50 (µMol)131.00004.90004.90004.9000AID1802994
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.50000.00321.54318.3000AID179746
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Prostaglandin G/H synthase 2Ovis aries (sheep)IC50 (µMol)5.01500.00101.453910.0000AID1141097; AID1196113; AID1542242; AID664056
Prostaglandin G/H synthase 2Mus musculus (house mouse)IC50 (µMol)0.05020.00050.40086.2000AID313120; AID325049; AID325055; AID775744; AID775745
Carbonic anhydrase 9Homo sapiens (human)IC50 (µMol)100.00000.00030.63029.3900AID1796990; AID48294
Solute carrier family 22 member 6Homo sapiens (human)IC50 (µMol)4.00000.27004.53069.9000AID681160
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.00291.823210.0000AID179746
Carbonic anhydrase 4Bos taurus (cattle)IC50 (µMol)100.00000.02100.20600.6200AID1796989; AID48114
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)500.00000.01002.765610.0000AID721754
P2Y purinoceptor 12Rattus norvegicus (Norway rat)IC50 (µMol)0.02000.02000.34000.9600AID1061774
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC50 (µMol)109.69860.00033.166210.0000AID1549771; AID1549781
TransthyretinHomo sapiens (human)Kd0.53000.00301.348210.0000AID1239060; AID1705462
AlbuminHomo sapiens (human)Kd2.45470.08933.31358.0000AID327170
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km16.00005.00006.830010.0000AID624637
TransthyretinHomo sapiens (human)Kd10.22000.06000.17170.3800AID216266; AID99661
TransthyretinHomo sapiens (human)Kd23.69001.10002.82676.1800AID216267; AID99662
Cytochrome P450 2C9 Homo sapiens (human)Km1.70000.19002.43005.4000AID1209240
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km12.00007.34007.34007.3400AID624632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (245)

Processvia Protein(s)Taxonomy
retinoid metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
farnesol catabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
cellular detoxification of aldehydeAldo-keto reductase family 1 member B10Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A9Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1 Bos taurus (cattle)
cellular oxidant detoxificationProstaglandin G/H synthase 1 Bos taurus (cattle)
monoatomic ion transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cell surface receptor signaling pathwayTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to coldTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to xenobiotic stimulusTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic cyclic compoundTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
thermoceptionTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein homotetramerizationTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to hydrogen peroxideTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
tetrahydrobiopterin biosynthetic processDihydrofolate reductaseHomo sapiens (human)
one-carbon metabolic processDihydrofolate reductaseHomo sapiens (human)
negative regulation of translationDihydrofolate reductaseHomo sapiens (human)
axon regenerationDihydrofolate reductaseHomo sapiens (human)
response to methotrexateDihydrofolate reductaseHomo sapiens (human)
dihydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate biosynthetic processDihydrofolate reductaseHomo sapiens (human)
folic acid metabolic processDihydrofolate reductaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityDihydrofolate reductaseHomo sapiens (human)
regulation of removal of superoxide radicalsDihydrofolate reductaseHomo sapiens (human)
response to hypoxiaCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial electron transport, cytochrome c to oxygenCytochrome c oxidase subunit 2Homo sapiens (human)
lactationCytochrome c oxidase subunit 2Homo sapiens (human)
cellular respirationCytochrome c oxidase subunit 2Homo sapiens (human)
proton transmembrane transportCytochrome c oxidase subunit 2Homo sapiens (human)
ATP synthesis coupled electron transportCytochrome c oxidase subunit 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
signal transductionTransthyretinHomo sapiens (human)
purine nucleobase metabolic processTransthyretinHomo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
positive regulation of gene expressionInterleukin-8Homo sapiens (human)
negative regulation of gene expressionInterleukin-8Homo sapiens (human)
positive regulation of cellular biosynthetic processInterleukin-8Homo sapiens (human)
negative regulation of cell adhesion molecule productionInterleukin-8Homo sapiens (human)
angiogenesisInterleukin-8Homo sapiens (human)
response to molecule of bacterial originInterleukin-8Homo sapiens (human)
chemotaxisInterleukin-8Homo sapiens (human)
inflammatory responseInterleukin-8Homo sapiens (human)
signal transductionInterleukin-8Homo sapiens (human)
G protein-coupled receptor signaling pathwayInterleukin-8Homo sapiens (human)
negative regulation of cell population proliferationInterleukin-8Homo sapiens (human)
calcium-mediated signalingInterleukin-8Homo sapiens (human)
regulation of cell adhesionInterleukin-8Homo sapiens (human)
neutrophil chemotaxisInterleukin-8Homo sapiens (human)
receptor internalizationInterleukin-8Homo sapiens (human)
response to endoplasmic reticulum stressInterleukin-8Homo sapiens (human)
intracellular signal transductionInterleukin-8Homo sapiens (human)
neutrophil activationInterleukin-8Homo sapiens (human)
cellular response to fibroblast growth factor stimulusInterleukin-8Homo sapiens (human)
regulation of single stranded viral RNA replication via double stranded DNA intermediateInterleukin-8Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayInterleukin-8Homo sapiens (human)
positive regulation of angiogenesisInterleukin-8Homo sapiens (human)
embryonic digestive tract developmentInterleukin-8Homo sapiens (human)
induction of positive chemotaxisInterleukin-8Homo sapiens (human)
cellular response to lipopolysaccharideInterleukin-8Homo sapiens (human)
cellular response to interleukin-1Interleukin-8Homo sapiens (human)
cellular response to tumor necrosis factorInterleukin-8Homo sapiens (human)
positive regulation of neutrophil chemotaxisInterleukin-8Homo sapiens (human)
regulation of entry of bacterium into host cellInterleukin-8Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideInterleukin-8Homo sapiens (human)
chemokine-mediated signaling pathwayInterleukin-8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
fatty acid metabolic processFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid transportFatty acid-binding protein, intestinalHomo sapiens (human)
intestinal lipid absorptionFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid transportFatty acid-binding protein, intestinalHomo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
epithelial cell maturationAldo-keto reductase family 1 member B1Homo sapiens (human)
renal water homeostasisAldo-keto reductase family 1 member B1Homo sapiens (human)
carbohydrate metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
C21-steroid hormone biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
regulation of urine volumeAldo-keto reductase family 1 member B1Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member B1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
fructose biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
cellular hyperosmotic salinity responseAldo-keto reductase family 1 member B1Homo sapiens (human)
metanephric collecting duct developmentAldo-keto reductase family 1 member B1Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1-6Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1-6Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
receptor internalizationC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 1Homo sapiens (human)
immune responseC-X-C chemokine receptor type 1Homo sapiens (human)
neutrophil chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
bile acid secretionUDP-glucuronosyltransferase 1A3Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
monoatomic anion transportSolute carrier family 22 member 6Homo sapiens (human)
response to organic cyclic compoundSolute carrier family 22 member 6Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 6Homo sapiens (human)
organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transportSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 6Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 6Homo sapiens (human)
renal tubular secretionSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
coumarin metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A7Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A10Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (122)

Processvia Protein(s)Taxonomy
retinal dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B10Homo sapiens (human)
alcohol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
geranylgeranyl reductase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1 Bos taurus (cattle)
heme bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
metal ion bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellularly gated calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
temperature-gated cation channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
mRNA regulatory element binding translation repressor activityDihydrofolate reductaseHomo sapiens (human)
mRNA bindingDihydrofolate reductaseHomo sapiens (human)
dihydrofolate reductase activityDihydrofolate reductaseHomo sapiens (human)
folic acid bindingDihydrofolate reductaseHomo sapiens (human)
NADPH bindingDihydrofolate reductaseHomo sapiens (human)
sequence-specific mRNA bindingDihydrofolate reductaseHomo sapiens (human)
NADP bindingDihydrofolate reductaseHomo sapiens (human)
cytochrome-c oxidase activityCytochrome c oxidase subunit 2Homo sapiens (human)
cytochrome-c oxidase activityCytochrome c oxidase subunit 2Homo sapiens (human)
copper ion bindingCytochrome c oxidase subunit 2Homo sapiens (human)
protein bindingCytochrome c oxidase subunit 2Homo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
hormone activityTransthyretinHomo sapiens (human)
protein bindingTransthyretinHomo sapiens (human)
identical protein bindingTransthyretinHomo sapiens (human)
thyroid hormone bindingTransthyretinHomo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
interleukin-8 receptor bindingInterleukin-8Homo sapiens (human)
protein bindingInterleukin-8Homo sapiens (human)
chemokine activityInterleukin-8Homo sapiens (human)
heparin bindingInterleukin-8Homo sapiens (human)
CXCR chemokine receptor bindingInterleukin-8Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid transmembrane transporter activityFatty acid-binding protein, intestinalHomo sapiens (human)
fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
protein bindingFatty acid-binding protein, intestinalHomo sapiens (human)
long-chain fatty acid bindingFatty acid-binding protein, intestinalHomo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B1Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glyceraldehyde oxidoreductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
interleukin-8 receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8 bindingC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
UDP-glycosyltransferase activityUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
protein bindingSolute carrier family 22 member 6Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
chloride ion bindingSolute carrier family 22 member 6Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Bos taurus (cattle)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein kinase C bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein kinase C bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (53)

Processvia Protein(s)Taxonomy
extracellular regionAldo-keto reductase family 1 member B10Homo sapiens (human)
lysosomeAldo-keto reductase family 1 member B10Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B10Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B10Homo sapiens (human)
mitochondrionAldo-keto reductase family 1 member B10Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1 Bos taurus (cattle)
plasma membraneTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
stereocilium bundleTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolDihydrofolate reductaseHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
mitochondrionCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial inner membraneCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial respiratory chain complex IVCytochrome c oxidase subunit 2Homo sapiens (human)
membraneCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial membraneCytochrome c oxidase subunit 2Homo sapiens (human)
respiratory chain complex IVCytochrome c oxidase subunit 2Homo sapiens (human)
mitochondrial matrixCytochrome c oxidase subunit 2Homo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular regionTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
azurophil granule lumenTransthyretinHomo sapiens (human)
extracellular exosomeTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular regionInterleukin-8Homo sapiens (human)
extracellular spaceInterleukin-8Homo sapiens (human)
cytosolCalcium/calmodulin-dependent protein kinase type II subunit alphaRattus norvegicus (Norway rat)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
microvillusFatty acid-binding protein, intestinalHomo sapiens (human)
apical cortexFatty acid-binding protein, intestinalHomo sapiens (human)
cytosolFatty acid-binding protein, intestinalHomo sapiens (human)
nucleusFatty acid-binding protein, intestinalHomo sapiens (human)
extracellular spaceAldo-keto reductase family 1 member B1Homo sapiens (human)
nucleoplasmAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1-6Homo sapiens (human)
intracellular membrane-bounded organelleUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
secretory granule membraneC-X-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B10 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
caveolaSolute carrier family 22 member 6Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 6Homo sapiens (human)
protein-containing complexSolute carrier family 22 member 6Homo sapiens (human)
side of membraneCarbonic anhydrase 4Bos taurus (cattle)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A10Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A10Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (943)

Assay IDTitleYearJournalArticle
AID1584741Drug metabolism in rat liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1348379Drug metabolism in human liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 15 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1220257Ratio of drug level in blood to plasma in human2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID194100Antiinflammatory effect measured as % inhibition in carrageenan induced paw edema test in rat.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
AID1736742Metabolic stability in human liver microsomes assessed as parent compound remaining in presence of NADPH after 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID1584734Drug metabolism in mouse liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID681225TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, Diclofenac: 5 uM) in Xenopus laevis oocytes2001Molecular pharmacology, May, Volume: 59, Issue:5
Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney.
AID1663587Intrinsic clearance in mouse liver microsomes2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Synthesis, in vitro ADME profiling and in vivo pharmacological evaluation of novel glycogen phosphorylase inhibitors.
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1209238Drug metabolism in assessed as human CYP2C9-mediated intrinsic clearance per mg protein2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1394639Drug metabolism in human liver S9 fraction assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured immediately in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID327169Apparent permeability across parallel artificial membrane2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin.
AID1220238Intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID263719Inhibition of beta amyloid protein 42 in SH-SY5Y cell lines overexpressing SPA4CT at 100 uM2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
AID1409437Metabolic stability in human liver microsomes assessed as compound remaining at 2 uL after 60 mins in absence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1209592Dissociation constant, pKa of the basic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1422276Intrinsic clearance in human liver microsomes at 1 uM by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID313126Inhibition of COX12007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1529185Protein binding in human serum albumin after 4.5 hrs by LC-MS based rapid equilibrium dialysis method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1457812Intrinsic clearance in mouse liver microsomes assessed per mg of protein2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1548578Half life in human liver microsomes in presence of NADPH regenerating system by LC-MS/MS analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID1593391Stability in human liver microsomes assessed as parent compound remaining measured after 60 mins2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1887668Metabolic stability in human liver microsomes assessed as half life at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID28928Intrinsic permeability of the compound2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID1220255Apparent permeability by PAMPA method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1301946Analgesic activity in Swiss albino mouse assessed as reduction in formalin-induced paw flinches in neurogenic phase at 5 mg/kg, ip dosed 30 mins before formalin injection measured up to 5 mins2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID664484Aqueous solubility of the compound in phosphate based buffer at pH 7.42012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
AID1422312Clearance in dog hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID284303Analgesic activity in Wistar Albino mouse at 10 mg/kg, po after 3 hrs by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1403476Anti-inflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to control2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1756362Metabolic stability in rat hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1461592Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 2 hrs by plethysmometry method (Rvb = 0%)2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1571694Intrinsic clearance in human liver microsomes assessed per mg protein in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1584744Drug metabolism in rat liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID313123Inhibition of mouse COX2 Y355F mutant2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1524890Intrinsic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID1207638Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1239061Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
AID664055Reversible binding to ram seminal vesicle COX1 at 300 uM at 600 MHz and 37 degC by saturation transfer difference 1[H]NMR spectroscopy2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Binding of ibuprofen, ketorolac, and diclofenac to COX-1 and COX-2 studied by saturation transfer difference NMR.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1141098Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID166747Variation of intraocular pressure in day one at a dose of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1394641Drug metabolism in human liver S9 fraction assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 30 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1718809Intrinsic clearance in CD-1 mouse liver microsomes at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID1846852Anti-inflammatory activity against formalin-induced foot paw edema in Wistar rat assessed as oedema inhibition at 10 mg/kg,po measured after 6 hrs by plethysmometric analysis relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1692511Half life in rat liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1692509Half life in mouse liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1501500Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced protein extravasation in thoracic cavity at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1413500Intrinsic clearance in human liver microsomes at 10 mM preincubated for 10 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1196112Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID1584737Drug metabolism in mouse liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1211796Intrinsic clearance in cryopreserved human HepaRG cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID325069Inhibition of mouse COX2 V349A mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1736739Metabolic stability in human liver microsomes assessed as half life incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID1743192Analgesic activity in rat assessed as prolongation of latency period at 10 mg/kg, ip measured after 1 hr by hot-plate test relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1564371Microsomal stability in mouse liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 30 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1529184Protein binding in immobilized human serum albumin by HPLC analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1211282Fraction metabolized glucuronidation in human liver microsomes in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1334723Anti-inflammatory activity against carrageenan-induced paw edema in albino rat assessed as paw thickness at 60 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured at 1 hr post carrageenan challenge (Rvb = 0.394 +/- 0.220 mm)
AID1717039Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID166754Variation of intraocular pressure in fourth day at a dose of 30 mg/kg at a dose by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID540235Phospholipidosis-negative literature compound
AID216265Inhibition of wild type TTR fibril formation at OD4002002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID373867Hepatic clearance in human hepatocytes in absence of fetal calf serum2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
First-principle, structure-based prediction of hepatic metabolic clearance values in human.
AID1196114Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX22015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID1474711Analgesic activity in Dunkin Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced thermal hyperalgesia at 10 mg/kg, po qd administered 1 hr prior to LPS stimulation measured after 4.5 hrs by plantar test relative to control2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1348375Drug metabolism in mouse liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 60 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1529186Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID325048Inhibition of ovine COX1 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1211793Lipophilicity, log P of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1223486Intrinsic clearance in human hepatocytes from chimeric mouse with humanized liver assessed per 10'6 cells at 10 uM after 0.25 to 2 hrs by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1209259Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by optimal design approach2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1394647Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 60 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1698011Fraction unbound in human plasma
AID1514463Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 120 mins by LC-MS/MS analysis (Rvb = 100%)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1736740Metabolic stability in human liver microsomes assessed as intrinsic clearance incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID624653Inhibition of codeine glucuronidation by human UGT enzymes from liver homogenate2005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1752935Intrinsic clearance in human liver microsomes measured upto 40 mins by LC-MS/MS analysis
AID1348374Drug metabolism in mouse liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 60 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1571699Intrinsic clearance in liver by measuring in intrinsic clearance in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID284310Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 10 mg/kg after 2 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1128733Inhibition of human recombinant COX-2 assessed as PGF2-alpha formation using arachidonic acid as substrate at 20 uM by enzyme immunoassay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID348028Inhibition of COX1 assessed as inhibition of arachidonic acid conversion to prostaglandin-E2 release2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Toward optimization of the second aryl substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.
AID1584738Drug metabolism in mouse liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID184052Inhibitory activity was measured on carrageenan-induced paw edema at a dose of 25 mg/Kg at 4 hours after intraperitoneal administration in rats1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Molecular design, synthesis, and antiinflammatory activity of a series of beta-aminoxypropionic acids.
AID1211278Clearance in iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1355800Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in absence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID254798Inhibitory concentration against COX-2; (valus obtained by Kato et al.)2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.
AID1584746Drug metabolism in dog liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID407366Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1514445Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 15 mins in presence of G-6-P, G-6-PDH, MgCl2 and NADP+ by LC-MS/MS analysis (Rvb = 100%)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1846821Inhibition of 2VCX (unknown origin) by Egg-albumin method2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1211218Ratio of unbound intrinsic glucuronidation clearance in human liver microsomes in presence of 1% bovine serum albumin to unbound intrinsic glucuronidation clearance in human liver microsomes in absence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID471922Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1196113Inhibition of ovine COX2 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay2015European journal of medicinal chemistry, Mar-06, Volume: 92Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: anti-inflammatory and analgesic activities.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID48114Inhibitory activity against bovine carbonic anhydrase IV was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID675290Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 2 hrs post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID1501489Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced pleural accumulation in total leucocytes at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by May-Grunwald-Giemsa staining-based Neuba2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID177360Antiinflammatory activity was evaluated in an adjuvant arthritis (subchronic inflammation) test after administering compound orally in rats.1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1272696Ulcerogenicity in albino Wistar rat assessed as ulcer index at 100 mg/kg, po after 20 hrs2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.
AID493624Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 1 hr (Rvb = 1.925 +/- 0.1011 ml)2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1880228Permeability of compound in PBS buffer at pH 7.4 at 500 mM incubated for 18 hrs by UV plate reader based PAMPA assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1824587Metabolic stability in Sprague-Dawley rat liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID681782TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Diclofenac: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, May, Volume: 55, Issue:5
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.
AID403703Inhibition of human COX1 expressed in sf9 cells2005Journal of natural products, Oct, Volume: 68, Issue:10
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
AID1211237Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID493628Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 24 hrs (Rvb = 1.39 +/- 0.053 ml)2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1584749Drug metabolism in dog liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1584752Drug metabolism in human liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1501491Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced pleural accumulation in neutrophils cells at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by May-Grunwald-Giemsa staining-based Neub2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID681153TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Chemical research in toxicology, Dec, Volume: 14, Issue:12
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1422310Clearance in human hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID1271594Binding affinity to bovine serum albumin assessed as association constant to higher affinity site at pH 6.4 to 8.4 by equilibrium dialysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID1375706Antiarthritic activity in CFA-induced Sprague-Dawley rat rheumatoid arthritis model assessed as decrease in difference between weight burden on contralateral and ipsilateral paw at 6.2 mg/kg, po measured up to 75 mins by incapacitance test2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis.
AID1461594Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 4 hrs by plethysmometry method (Rvb = 0%)2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1703908Permeability of the compound by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1301937Inhibition of human recombinant COX2 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID1296908Decrease of pain in monoiodoacetate-induced acute osteoarthritis rat model assessed as increase in grip force deficit of hind limbs at 30 mg/kg, po relative to control2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID664054Reversible binding to sheep placenta COX2 at 300 uM at 600 MHz and 37 degC by saturation transfer difference 1[H]NMR spectroscopy2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Binding of ibuprofen, ketorolac, and diclofenac to COX-1 and COX-2 studied by saturation transfer difference NMR.
AID1422271Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 30 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1461597Gastrointestinal toxicity in adjuvant-induced Wistar rat arthritis model assessed as ulcer index treated for 7 days measured on day 21 post arthritis induction2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1501472Drug metabolism assessed as UGT2B15 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID624632Drug glucuronidation reaction catalyzed by human recombinant UGT1A32005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID471924Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1499675Inhibition of recombinant human COX2 at 20 uM using arachidonic acid as substrate by ELISA2017European journal of medicinal chemistry, Sep-29, Volume: 138Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity.
AID493629Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 1 hr2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1164201Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1211297Drug recovery in plasma (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1142447Antiinflammatory activity in po dosed albino rat assessed as inhibition of carrageenan-induced paw edema administered 1 hr prior challenge measured 2 hrs post challenge2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1517057Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 1 hr before carrageenan stimulation and measured after 3 hrs relative to control
AID1779259Metabolic stability in human liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID243230Binding affinity towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID1887669Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID1564372Microsomal stability in mouse liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 60 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1220256Total clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1449546Clearance in human liver microsomes at 1 uM by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1571698Intrinsic clearance in rat liver microsomes assessed per mg protein in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1743187Antiinflammatory activity in rat model of carrageenan-induced paw edema assessed as inhibition of hind paw swelling at 10 mg/kg, ip measured after 1 hr relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID178754Inhibitory activity in the adjuvant induced arthritis model of chronic inflammation in rat1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.
AID1422307Half life in Sprague-Dawley rat hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID78389Compound is evaluated for the inhibition of [125I]T3 uptake by H4 rat hepatoma cells at 0.1 mM1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Thyroid hormone uptake by hepatocytes: structure-activity relationships of phenylanthranilic acids with inhibitory activity.
AID755104Inhibition of UGT in human liver microsomes using 4-methylumbelliferone as substrate after 10 mins by fluorescence analysis2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Semisynthesis, cytotoxicity, antiviral activity, and drug interaction liability of 7-O-methylated analogues of flavonolignans from milk thistle.
AID1698008Hepatic clearance in Wistar Hannover rat at 1 mg/kg, iv
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID387102Antinociceptive activity against formalin-induced paw pain in ip dosed Swiss mouse pretreated 30 mins before formalin challenge assessed after 0 to 5 mins2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis of new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives with anti-nociceptive activity.
AID1743188Antiinflammatory activity in rat model of carrageenan-induced paw edema assessed as inhibition of hind paw swelling at 10 mg/kg, ip measured after 3 hrs relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1334725Anti-inflammatory activity against carrageenan-induced paw edema in albino rat assessed as paw thickness at 60 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured at 7 hrs post carrageenan challenge (Rvb = 0.464 +/- 0.023 mm)
AID450463Binding affinity to D22 ssDNA aptamer2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
ssDNA aptamers that recognize diclofenac and 2-anilinophenylacetic acid.
AID1355797Intrinsic clearance in human liver microsomes assessed per mg protein after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1548577Intrinsic clearance in human liver microsomes in presence of NADPH regenerating system by LC-MS/MS analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID1211172Drug metabolism in human intestinal microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1718810Intrinsic clearance in CD-1 mouse microsomes at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID1564366Microsomal stability in human liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 60 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1584745Drug metabolism in rat liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1524889Half life in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID1211222Ratio of unbound intrinsic glucuronidation clearance in human intestinal microsomes in presence of 1% bovine serum albumin to unbound intrinsic glucuronidation clearance in human intestinal microsomes in absence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID284304Analgesic activity in Wistar Albino mouse at 20 mg/kg, po after 30 mins by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID374577Antiinflammatory activity in Wistar albino rat assessed as reduction in formalin-induced paw edema volume at 50 mg/kg, po administered 30 mins prior to formalin challenge measured after 120 mins by plethysmography2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1422270Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 60 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID284306Analgesic activity in Wistar Albino mouse at 20 mg/kg, po after 2 hrs by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1061773Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID446876Antiinflammatory activity against carrageenan-induced paw edema in rat at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 6 hrs by plethysmometer2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
NO-NSAIDs: Gastric-sparing nitric oxide-releasable prodrugs of non-steroidal anti-inflammatory drugs.
AID1717043Inhibition of trypsin (unknown origin) using casein as substrate preincubated for 5 mins followed by substrate addition and measured after 20 mins2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID1395372Drug metabolism in mouse liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 60 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1777966Antiallodynic activity in Swiss Webster mouse assessed as reversal of carrageenan-induced tactile allodynia at 30 ug/paw local peripheral administration pretreated with carrageenan for 6 days followed by compound addition and measured 6 hrs post compound
AID1582082Metabolic stability in CD1 mouse liver microsomes assessed as compound remaining at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1529178Dissociation constant, pKa1 of compound in aqueous medium by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1394640Drug metabolism in human liver S9 fraction assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 15 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1692513Half life in human liver microsomes measured up to 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1698003Fraction unbound in rat plasma
AID1766124Permeability of compound in PBS at pH 7.4 after 18 hrs by PAMPA2021ACS medicinal chemistry letters, Aug-12, Volume: 12, Issue:8
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID17664Second dissociation constant of the binding of compound to V30M TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID1501467Drug metabolism assessed as UGT1A6 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1706966Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID325049Inhibition of mouse COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1395371Drug metabolism in mouse liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 30 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1604489Inhibition of COX2 in mouse RAW264.7 cells assessed as reduction in LPS-induced inflammation by measuring PGE2 level at 1 uM treated 1 hr after LPS stimulation and measured after 18 hrs by ELISA (Rvb = (2437 +/- 93.17 pg/mL)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis.
AID284301Analgesic activity in Wistar Albino mouse at 10 mg/kg, po after 1 hr by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1717038Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID162494In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 21999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID1582077Metabolic stability in human liver microsomes assessed as half life at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID450464Binding affinity to D16 ssDNA aptamer2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
ssDNA aptamers that recognize diclofenac and 2-anilinophenylacetic acid.
AID1582078Metabolic stability in human liver microsomes assessed as intrinsic clearance at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID166908Variation of intraocular pressure in third day at a dose of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID280215Aqueous solubility in distilled water at pH 4.772007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1608178Selectivity index, ratio of IC50 for ovine COX1 to IC50 for recombinant human COX22019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1777957Antiallodynic activity in Swiss Webster mouse assessed as protection against carrageenan-induced tactile allodynia at 30 ug/paw local peripheral pretreatment with compound for 15 mins followed by carrageenan challenge and measured after 6 hrs
AID736898Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw oedema at 50 mg/kg after 180 mins relative to untreated control2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Regioselective synthesis of isoxazole-mercaptobenzimidazole hybrids and their in vivo analgesic and anti-inflammatory activity studies.
AID678719Metabolic stability in human liver microsomes assessed as medium signal/noise ratio (S/N of 10 to 100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1394648Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 120 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1217729Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID624637Drug glucuronidation reaction catalyzed by human recombinant UGT1A92005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID284302Analgesic activity in Wistar Albino mouse at 10 mg/kg, po after 2 hrs by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1549812Agonist activity at human TRPA1 Phe909Ala mutant expressed in HEK293 cells assessed as Ca2+ influx at 30 uM by fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID325050Inhibition of human COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1211224Drug metabolism in human liver microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1375693Antiarthritic activity in CFA-induced Sprague-Dawley rat rheumatoid arthritis model assessed as increase in tolerated weight on ipsilateral paw at 6.2 mg/kg, po measured at 15 mins by paw pressure test2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Discovery of Novel Nonsteroidal Anti-Inflammatory Drugs and Carbonic Anhydrase Inhibitors Hybrids (NSAIDs-CAIs) for the Management of Rheumatoid Arthritis.
AID1744239Intrinsic clearance in rat liver microsomes at 10 uM incubated for 1 hr in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1584735Drug metabolism in mouse liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID284300Analgesic activity in Wistar Albino mouse at 10 mg/kg, po after 30 mins by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1239060Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
AID493630Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 2 hrs2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1517059Ulcerogenicity in Sprague-Dawley rat assessed as length of lesions at 50 mg/kg, po administered for 5 days (Rvb = 0 millimeter)
AID1663588Clearance in mouse liver microsomes2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Synthesis, in vitro ADME profiling and in vivo pharmacological evaluation of novel glycogen phosphorylase inhibitors.
AID1773844Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1226816Selectivity index, ratio of IC50 for ovine COX-1 to human recombinant COX-22015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID1226806Anti-inflammatory activity against Swiss albino mouse assessed as reduction in paw thickness at 10 mg/kg, ip administered 30 mins prior to dextran injection measured after 4 hrs by vernier calliper analysis relative to control2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID1220249Activity of human UGT2B7 expressed in insect cells assessed as reduction in compound level after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1209251Drug metabolism in human liver microsomes by optimal design approach2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1211213Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1209240Drug metabolism in assessed as human CYP2C9-mediated metabolism2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1571697Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1333581Antiinflammatory activity in rat carrageenan-induced paw edema model assessed as inhibition of paw swelling at 25 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 5 hrs2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Polyfluorinated salicylic acid derivatives as analogs of known drugs: Synthesis, molecular docking and biological evaluation.
AID1323834Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID1301936Inhibition of ovine COX1 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1718811Metabolic stability in CD-1 mouse liver microsomes assessed as half-life at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1582079Metabolic stability in human liver microsomes assessed as compound remaining at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID280223Dissociation constant, pKa at pH 4.772007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID594417Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, ip after 1 hr by plethysmometer2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID405935Solubility of compound in 0.05 M sodium phosphate buffer at pH 7.4 by high throughput assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
High throughput solubility determination with application to selection of compounds for fragment screening.
AID1709155Toxicity in brine shrimp assessed as mortality at 100 uM incubated for 24 hrs by microscopic analysis2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Multicomponent synthesis and preliminary anti-inflammatory activity of lipophilic diphenylamines.
AID1061774Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID1584750Drug metabolism in dog liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1514461Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 60 mins in presence of G-6-P, G-6-PDH, MgCl2 and NADP+ by LC-MS/MS analysis (Rvb = 100%)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID1744369Stability in human liver microsomes assessed as parent compound remaining at 1 uM incubated for 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1271590Binding affinity to human serum albumin by equilibrium dialysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID325070Inhibition of mouse COX2 V349I mutant 20 mins preincubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID26962Calculated partition coefficient (clogP)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Thyroid hormone uptake by hepatocytes: structure-activity relationships of phenylanthranilic acids with inhibitory activity.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1360444Binding affinity to human serum albumin assessed as fraction unbound after 4 hrs by LC-MS method2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1584753Drug metabolism in human liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1895929Metabolic stability in human liver microsomes assessed as parent compound remaining at 60 mins in presence of NADPH regenerating system by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID1294273Antiinflammatory activity in rat adjuvant induced arthritis model assessed as suppression of Mycobacterium tuberculosis H37 RA induced paw swelling at 10 mg/kg measured from day 11 to 15 relative to vehicle control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1226814Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID1549781Agonist activity at human TRPA1 in WI38 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1517058Ulcerogenicity in Sprague-Dawley rat assessed as number of lesions at 50 mg/kg, po administered for 5 days (Rvb = 0 No_unit)
AID1334727Anti-inflammatory activity against carrageenan-induced paw edema in albino rat assessed as inhibition of paw edema at 60 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 1 to 7 hrs relative to control
AID327170Binding affinity to human serum albumin by PAMPA method2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin.
AID1435280Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring parent compound remaining at 10 pmol/ml after 60 mins in presence of NADPH by LC-MS/MS analysis2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1256770Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw oedema at 0.15 mmol/kg, ip administered 5 mins before carrageenan challenge measured after 3.5 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Esters of some non-steroidal anti-inflammatory drugs with cinnamyl alcohol are potent lipoxygenase inhibitors with enhanced anti-inflammatory activity.
AID1810791Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1501492Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced pleural accumulation in eosiniphils at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by May-Grunwald-Giemsa staining-based Neubauer c2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1548598Stability in human liver microsomes assessed as compound remaining level incubated for 60 mins in absence of NADPH regenerating system by LC-MS/MS analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID671814Analgesic activity in monoiodoacetic acid rat model of osteoarthritic pain assessed as decrease in pain at 3 mg/kg, po measured after 29 days relative to control2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Discovery and optimization of novel purines as potent and selective CB2 agonists.
AID1501469Drug metabolism assessed as UGT1A9 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID284308Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 10 mg/kg after 30 mins2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1519609Metabolic stability in human liver microsomes assessed as half life incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID361985Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID1301947Analgesic activity in Swiss albino mouse assessed as reduction in formalin-induced paw flinches in inflammatory phase at 5 mg/kg, ip dosed 30 mins before formalin injection measured after 15 to 30 mins2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID1211283Fraction metabolized glucuronidation in human liver microsomes in presence of UDP-glucuronosyltransferase and bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1061767Antinociceptive activity in Swiss albino mouse assessed as reduction in capsaicin-induced paw licking at 25 mg/kg, ip administered 30 mins prior to capsaicin-challenge2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID1549805Agonist activity at human TRPA1 Cys261Ala mutant expressed in HEK293 cells assessed as Ca2+ influx at 30 uM by fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1630901Analgesic activity in rat assessed as pain threshold time at 10 mg/kg, po measured at 0.5 hr post dose by hot plate method (Rvb = 19.1 to 21.2 sec)2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1306898Antiinflammatory activity in ip dosed rat carrageenan-induced foot paw edema model measured after 2 hrs by plethysmometric analysis2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID624642Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A12005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1128737In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in total cholesterol level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1777960Antiinflammatory activity in Swiss Webster mouse assessed as protection against carrageenan-induced paw edema at 30 ug/paw local peripheral administration and measured after 4 to 6 hrs
AID1501490Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced pleural accumulation in mononuclear cells at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by May-Grunwald-Giemsa staining-based Neub2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1211298Dissociation constant, pKa of the compound2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1413499Half life in human liver microsomes at 10 mM preincubated for 10 mins followed by NADPH addition by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1141095Ulcerogenic activity in albino rat stress model assessed as ulcer index at 10 mg/kg, po after 7 hrs2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID471921Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1403475Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages preincubated for 6 hrs followed by PMA stimulation by phase contrast microscopic method2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID179746In vitro inhibition of prostaglandin synthesis was tested in rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents.
AID1348364Drug metabolism in mouse liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 15 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1403485Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 30 hrs by MTS assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1220258Renal clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1449545Half life in human liver microsomes at 1 uM by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1364858Antinociceptive activity in Wistar Han rat model of CFA-induced mechanical hyperalgesia assessed as reversal of mechanical hyperalgesia by measuring hind paw withdrawal thresholds at 30 mg/kg administered via oral gavage after 3 days of CFA challenge meas2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.
AID589146Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1564368Microsomal stability in mouse liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 30 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1403477Anti-inflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to celecoxib2018European journal of medicinal chemistry, Jan-20, Volume: 144Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
AID1211291Drug metabolism in human intestinal microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1895930Metabolic stability in human liver microsomes assessed as parent compound remaining at 60 mins in absence of NADPH regenerating system by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID1426403Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 3 hrs relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID176482Inhibition of adjuvant-induced polyarthritis in rat following p.o. administration.1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents.
AID280211Intrinsic solubility in 0.15 M KCl at 25 degC by chasing equilibrium2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID471923Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID657311Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 3 mg/kg, po administered 60 mins before DABK challenge2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
AID664056Inhibition of sheep placental cotyledons COX22011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Binding of ibuprofen, ketorolac, and diclofenac to COX-1 and COX-2 studied by saturation transfer difference NMR.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1348377Drug metabolism in human liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 30 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1395373Drug metabolism in mouse liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 15 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID313124Inhibition of mouse COX2 S530A mutant2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1220259Oral absorption in human2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID229532Ratio of IC50 values at Cyclooxygenase-1 and Cyclooxygenase-21999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1223478Total clearance in chimeric mouse with humanized liver at 3 mg/kg, iv by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1271592Binding affinity to human serum albumin assessed as association constant to higher affinity site by HPLC method2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1426404Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 5 hrs relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID387103Antinociceptive activity against formalin-induced paw pain in ip dosed Swiss mouse pretreated 30 mins before formalin challenge assessed after 15 to 30 mins2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis of new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives with anti-nociceptive activity.
AID1549771Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1211207Drug metabolism in human kidney microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1487481Antioxidant activity assessed as DPPH free radical scavenging activity at 20 ug/ml after 15 mins by spectrophotometric method2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis, antioxidant, antifungal, molecular docking and ADMET studies of some thiazolyl hydrazones.
AID1519610Metabolic stability in human liver microsomes assessed as compound remaining incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID161484In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 11999Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
AID1744368Intrinsic clearance in human liver at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID1223483Unbound fraction in iv dosed human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1564365Microsomal stability in human liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 30 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID675289Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 1.5 hrs post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID407369Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Characterization of the drug binding specificity of rat liver fatty acid binding protein.
AID1333708Analgesic activity in Dunkin Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced thermal hyperalgesia at 10 mg/kg, po administered 1 hr prior to LPS stimulation measured after 4.5 hrs
AID1706970Stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining at 10 uM measured after 60 mins in absence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID442514Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID1614346Intrinsic clearance in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1876434Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 60 mins2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1773845Intrinsic clearance in human liver microsomes at 1 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1846850Anti-inflammatory activity against formalin-induced foot paw edema in Wistar rat assessed as oedema inhibition at 10 mg/kg,po measured after 1 hrs by plethysmometric analysis relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID1211186Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1604490Inhibition of COX2 in mouse RAW264.7 cells assessed as reduction in LPS-induced inflammation by measuring PGE2 level at 100 uM treated 1 hr after LPS stimulation and measured after 18 hrs by ELISA (Rvb = (2437 +/- 93.17 pg/mL)2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis.
AID1395381Drug metabolism in human liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 60 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1141080Acute antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 4 hrs by plethysmometric analysis relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1810793Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-22021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1571696Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1706967Intrinsic liver clearance in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1660990Inhibition of human DHFR in presence of DHF and NADPH by UV-vis spectrometry by Lineweaver-Burk plot analysis2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.
AID1271591Binding affinity to bovine serum albumin at 298.15 K by isothermal titration calorimetry2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID1211243Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1809979Metabolic stability in mouse liver microsomes assessed as clearance2021Bioorganic & medicinal chemistry letters, 12-01, Volume: 53Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
AID1211239Fraction unbound in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID624643Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A102005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1576578Fraction absorbed of the compound by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID624645Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1692512Metabolic stability in human liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID552068Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po measured after 3 hrs of carrageenan challenge2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1717040Selectivity index, ratio of IC50 for sheep COX1 to IC50 for recombinant human COX2 expressed in baculovirus infected Sf21 cells2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID216267Second dissociation constant of the binding of compound to wild type TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1593004Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation2019European journal of medicinal chemistry, Apr-01, Volume: 167Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.
AID1895927Metabolic stability in human liver microsome assessed as intrinsic clearance by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID469589Gastrointestinal toxicity in Wistar rat assessed as gastric mucosal layer disruption at 24 mg/kg, po by histopathological study2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs.
AID432207Analgesic activity in albino mouse inhibition of acetic acid-induced writhing response at 10 mg/kg, po2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1810792Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents
AID1128732Inhibition of bovine COX-1 assessed as PGF2-alpha formation using arachidonic acid as substrate at 20 uM by enzyme immunoassay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID189987Gastrointestinal tolerability was evaluated under chronic conditions, in rats. The ulcerogenic dose was reported1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1457811Half life in mouse liver microsomes2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1211193Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1886475Metabolic stability in human liver assessed as parent compound remaining preincubated for 10 mins followed by NADPH addition for 2 hrs and measured at 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID1501495Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced nitric oxide production in pleural washes at 100 ng/kg, ip pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by Lowry/Griess analysis2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1630902Analgesic activity in rat assessed as pain threshold time at 10 mg/kg, po measured at 1 hr post dose by hot plate method (Rvb = 19.1 to 21.2 sec)2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1211215Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1910022Metabolic stability in human liver microsomes at 20 uM assessed as half life measured up to 90 mins by LC-HRMS analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Development of Predictive Classification Models for Whole Cell Antimycobacterial Activity of Benzothiazinones.
AID1394642Drug metabolism in human liver S9 fraction assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 60 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1564361Microsomal stability in human liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 15 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID657309Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 0.3 mg/kg, po administered 60 mins before DABK challenge2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1743193Analgesic activity in rat assessed as prolongation of latency period at 10 mg/kg, ip measured after 2 hrs by hot-plate test relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1426401Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1739434Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM measured per mg protein upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID374252Antiinflammatory activity in albino rat acute inflammatory model assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po dosed 1 hr before carrageenan challenge measured after 4 hrs relative to control2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and pharmacological evaluation of a novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1360429Binding affinity to human serum albumin after 4 hrs by LC-MS method2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1395379Drug metabolism in human liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 15 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1895926Metabolic stability in human liver microsome assessed as half life by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID266764Membrane permeability, CA(t)/CD(0) in 70% silicon-30% IPM membrane2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
AID493625Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 2 hrs (Rvb = 1.905 +/- 0.046 ml)2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID446868AUC in rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
NO-NSAIDs: Gastric-sparing nitric oxide-releasable prodrugs of non-steroidal anti-inflammatory drugs.
AID1422306Half life in human hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID1541341Half life in human liver microsomes at 20 to 40 uM measured for 120 mins in presence of NADPH by RP-HPLC analysis
AID775744Inhibition of purified mouse COX-2 assessed as inhibition of PGE2/PGD2 formation preincubated for 15 mins before arachidonic acid substrate addition measured after 30 seconds by LC-MS-MS method2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID681930TP_TRANSPORTER: inhibition of E217betaG in the presence of Diclofenac at a concentration of 100uM in membrane vesicles from MRP4-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID1323835Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID664066Inhibition of COX22012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Exploring activity cliffs in medicinal chemistry.
AID325071Inhibition of mouse COX2 V349I mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1614348Stability in human liver microsomes assessed as compound remaining in absence of NADPH regenerating system after 60 mins by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1880488Permeability of the compound in PBS buffer at pH 7.4 measured after 18 hrs by UV plate reader based PAMPA assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
AID1449547Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM at 60 mins by LC-MS/MS analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID1909902Displacement of [3H]NCS-382 from CaMK2alpha in rat brain cerebral cortex membrane homogenates assessed as inhibition constant measured after 60 mins by TopCount scintillation counting method
AID1409436Metabolic stability in human liver microsomes assessed as compound remaining at 2 uL after 60 mins by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID221447Analgesic effect measured as % inhibition in PBQ-induced writhing test in mice.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
AID469580Gastrointestinal toxicity in Wistar rat assessed as ulcer index at 24 mg/kg, po2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs.
AID446872Antiinflammatory activity against carrageenan-induced paw edema in rat at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs by plethysmometer2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
NO-NSAIDs: Gastric-sparing nitric oxide-releasable prodrugs of non-steroidal anti-inflammatory drugs.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID313120Inhibition of mouse wild type COX22007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID280209Solubility in 0.5 M NaCl at pH 3.0 and 25 degC by shake flask method2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID426392Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID1211251Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID471926Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID284309Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 10 mg/kg after 1 hr2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1846851Anti-inflammatory activity against formalin-induced foot paw edema in Wistar rat assessed as oedema inhibition at 10 mg/kg,po measured after 3 hrs by plethysmometric analysis relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1461593Inhibition of ovine COX-1 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1450609Intrinsic clearance in human liver microsomes assessed as 4'-hydroxydiclofinac level by LC-MS/MS analysis2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
AID1435279Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring compound intrinsic clearance at 10 pmol/ml preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1524891Hepatic clearance in human liver microsomes further incubated of 5 to 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID386813Antinociceptive efficacy in ip dosed rat assessed as inhibition of carrageenan-induced inflammatory pain in paw after 30 mins by hotbox assay relative to control2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
AID1128739In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in triglyceride level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 hrs2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID456465Inhibition of wild type human TTR aggregation expressed in Escherichia coli assessed as fibril formation at 20 uM after 72 hrs relative by spectrofluorimetry2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Identification of a novel ligand binding motif in the transthyretin channel.
AID347224Ratio of IC50 for COX1 in bovine platelets to IC50 for COX2 in human blood2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1348365Drug metabolism in mouse liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 30 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID624646Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A92005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1272642Antiinflammatory activity in adjuvant-induced arthritis rat model assessed as inhibition of paw swelling at 10 mg/kg administered 15 days post adjuvant challenge2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID28921Partition coefficient (logP) (hexadecane)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID450465Binding affinity to D3 ssDNA aptamer2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
ssDNA aptamers that recognize diclofenac and 2-anilinophenylacetic acid.
AID1272693Anti-inflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced paw edema at 30 mg/kg, po measured every one hour for 5 hrs2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.
AID432208Gastrointestinal toxicity in albino mouse assessed as ulcerogenic indicates at dose 30 mg/kg, po2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1211795Dissociation constant, pKa of the compound2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1743201Acute toxicity in mouse at 70 mg/kg, ip administered as single dose2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1576576Effective permeability of compound by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID1519611Metabolic stability in rat liver microsomes assessed as half life incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID1377475Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1461595Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 6 hrs by plethysmometry method (Rvb = 0%)2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1154876Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 12.5 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID99662Second dissociation constant of the binding of compound to L55P TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID374571Antiinflammatory activity in Wistar albino rat assessed as reduction in formalin-induced paw edema volume at 50 mg/kg, po administered 30 mins prior to formalin challenge measured after 60 mins by plethysmography2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1703888Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID374578Apparent permeability across bovine cornea by UV-visible spectrophotometer2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1650563Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1709156Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 50 uM after 24 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Multicomponent synthesis and preliminary anti-inflammatory activity of lipophilic diphenylamines.
AID1154877Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 25 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
AID1395377Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 30 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1409435Intrinsic clearance in human liver microsomes at 2 uL after 20 mins by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1880388Metabolic stability in human liver microsomes assessed as half life at 1 uM measured up to 45 mins in presence of NADPH by LC-MS/MS analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID426477Inhibition of CXCR1 Lys99Ala mutant transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID193991Gastrointestinal tolerability was evaluated in rats and compound dose that causes lethality was reported1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1501465Drug metabolism assessed as UGT1A3 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID189985Gastrointestinal tolerability was evaluated under acute conditions, in rats. The ulcerogenic dose was reported.1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1054847Inhibition of human recombinant TTR Y78F mutant-mediated fibrillogenesis at 40 uM after 30 mins by turbidimetric assay relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Modulation of the fibrillogenesis inhibition properties of two transthyretin ligands by halogenation.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID736900Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw oedema at 50 mg/kg after 60 mins relative to untreated control2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Regioselective synthesis of isoxazole-mercaptobenzimidazole hybrids and their in vivo analgesic and anti-inflammatory activity studies.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1423032Inhibition of COX1 in human platelet microsomes assessed as reduction in formation of oxidized TMPD using arachidonic acid as substrate preincubated for 3 to 5 mins followed by arachidonic acid addition measured for 25 secs by spectrophotometric assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.
AID1274703Half life of the compound assessed as compound rearrangement2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treat
AID680196TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, Diclofenac: 500 uM) in Xenopus laevis oocytes2000The Journal of biological chemistry, Feb-11, Volume: 275, Issue:6
Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta.
AID213944Inhibition of V30M TTR fibril formation at OD4002002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1876435Metabolic stability in human liver microsomes assessed as parent compound remaining measured after 60 mins in absence of NADPH2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID432206Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID1461599Inhibition of human COX-2 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1232215Intrinsic clearance in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID1211179Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1232214Half life in rat liver microsomes at 1 uM preincubated for 10 mins followed by addition of NADPH regenerating system by LC-MS analysis2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
AID280222Intrinsic solubility in 0.16 M KCl at 25 degC by potentiometric titration2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1199060Inhibition of wild-type N-terminal 6-His tagged AKR1B10 (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as pyridine-3-aldehyde reduction by spectrophotometry2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Targeting aldose reductase for the treatment of diabetes complications and inflammatory diseases: new insights and future directions.
AID1390335Analgesic activity in Dunkin-Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced hyperalgesia at 10 mg/kg, po administered 2 hrs prior to LPS challenge measured after 4.5 hrs relative to control
AID426393Cytotoxicity against of human polymorphonuclear leukocytes assessed as cell viability by trypan blue dye exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID664063Inhibition of COX12012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Exploring activity cliffs in medicinal chemistry.
AID1426402Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX22017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1501462Drug metabolism assessed as CYP2D6 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1571700Metabolic stability in rat liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1423035Inhibition of human COX2 expressed in baculovirus infected sf21 cells assessed as reduction in formation of oxidized TMPD using arachidonic acid as substrate preincubated for 3 to 5 mins followed by arachidonic acid addition measured for 25 secs by spectr2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1873778Metabolic stability in rat liver microsomes assessed as half life incubated for 5 mins in presence of NADPH by HPLC analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1709154Toxicity in brine shrimp assessed as mortality at 10 uM incubated 24 hrs by microscopic analysis2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Multicomponent synthesis and preliminary anti-inflammatory activity of lipophilic diphenylamines.
AID1756360Metabolic stability in human hepatocytes assessed as clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID364309Activity at PPARgamma in human Caco-2 cells assessed as luciferase activity at 200 uM relative to control2008European journal of medicinal chemistry, Sep, Volume: 43, Issue:9
NSAIDs revisited: putative molecular basis of their interactions with peroxisome proliferator-activated gamma receptor (PPARgamma).
AID1334719Analgesic activity in mouse assessed as number of acetic acid-induced writhing pretreated for 1 hr followed by acetic acid challenge measured between 5 to 20 mins after acetic acid injection
AID340309Inhibition of human cyclooxygenase 12008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID1529182Protein binding in plasma (unknown origin)2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID681160TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells2000The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1
Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.
AID166743Variation of intraocular pressure at fifth day of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1604488Inhibition of COX1 in human platelet rich plasma in assessed as inhibition of ADP-induced platelet aggregation at 10 uM incubated for 5 mins by turbidimetry based Born's method relative to control2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Bioisosteric Development of Multitarget Nonsteroidal Anti-Inflammatory Drug-Carbonic Anhydrases Inhibitor Hybrids for the Management of Rheumatoid Arthritis.
AID1630892Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1226808Anti-hyperalgesic activity against Swiss albino mouse assessed as reduction in paw lickings at 10 mg/kg, ip administered 30 mins prior to capsaicin injection relative to control2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID1348373Drug metabolism in mouse liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 30 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1404016Permeability of the compound by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID1220239Unbound intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1271595Binding affinity to bovine serum albumin assessed as association constant to lower affinity site at pH 6.4 to 8.4 by equilibrium dialysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID664483Aqueous solubility of the compound in phosphate based buffer at pH 42012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
AID1461598Gastrointestinal toxicity in adjuvant-induced Wistar rat arthritis model assessed as lesion formation in surface epithelium of stomach treated for 7 days measured on day 21 post arthritis induction by hematoxylin and eosin staining-based analysis2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID1584747Drug metabolism in dog liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1128712Antioxidant activity in rat liver microsome membrane assessed as inhibition of lipid peroxidation after 45 mins by TBARS-based spectrophotometric assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID1223482Ratio of drug level in blood to plasma in iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID284305Analgesic activity in Wistar Albino mouse at 20 mg/kg, po after 1 hr by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1379265Anti-inflammatory activity in human RBC assessed as membrane stabilization relative to control
AID493626Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs (Rvb = 1.63 +/- 0.059 ml)2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID312490Inhibition of human COX1-mediated conversion of arachidonic acid to prostaglandin-E22008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors.
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1169140Retention time of the compound by EPSA supercritical fluid chromatography2014ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
EPSA: A Novel Supercritical Fluid Chromatography Technique Enabling the Design of Permeable Cyclic Peptides.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1141099Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID1261691Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.
AID681026TP_TRANSPORTER: inhibition of PAH uptake (PAH: 20 uM, Diclofenac: 1000 uM) in OAT-expressing COS-7 cells1999The Journal of biological chemistry, Jan-15, Volume: 274, Issue:3
Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells.
AID178646Antiinflammatory activity was evaluated in an carrageenan edema (acute inflammation) test, after administering compound orally in rats1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID594444Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, ip after 2 hrs by plethysmometer2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID280217Intrinsic solubility at pH 7.02007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID233730Activity ratio is the percent inhibition in writhing test at 100 umol/kg, po to that of diclofenac at 100 umol/kg, po administration2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
AID1422274Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 5 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1584739Drug metabolism in mouse liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1223475Elimination half life in chimeric mouse with humanized liver at 3 mg/kg, iv by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID1886472Metabolic stability in human liver microsomes assessed as half-life preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID166763Variation of intraocular pressure in seventh day at a dose of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1272643Analgesic activity in monoiodo acid-induced rat joint pain model assessed as inhibition of differential weight bearing at 5 mg/kg, po measured 30 mins post dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.
AID1394645Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 15 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1548575Stability in human liver microsomes assessed as compound remaining level incubated for 60 mins in presence of NADPH regenerating system by LC-MS/MS analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1630893Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 1 hr relative to control2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID374579Apparent permeability across bovine cornea assessed as lag time of permeation by UV-visible spectrophotometer2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1744366Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1706961Half life in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID325073Inhibition of mouse COX2 at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1698006Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1422272Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 20 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID266766Dissociation constant, pKa of the compound2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
AID1211248Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1209247Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by multiple depletion curves method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1501461Drug metabolism assessed as CYP2C19 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1271589Competitive binding affinity to equine serum albumin assessed as association constant to lower affinity site by isothermal titration calorimetric analysis in presence of naproxen2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1128738In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in LDL-cholesterol level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 hr2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID325068Inhibition of mouse COX2 V349A mutant 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1542241Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID310933Permeability across PAMPA membrane after 7 hrs2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1501501Anti-inflammatory activity in Swiss mouse assessed as inhibition of LPS-induced nitric oxide production in pleural washes at 100 mg/kg, ip pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by Lowry/Griess analysis2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1422269Half life in human liver microsomes at 1 uM by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID594445Antiinflammatory activity in ip dosed Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema after 2 hrs by plethysmometer2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis, anti-inflammatory activity and COX-1/COX-2 inhibition of novel substituted cyclic imides. Part 1: Molecular docking study.
AID1756359Metabolic stability in human hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID313125Inhibition of COX22007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1422309Half life in monkey hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1220241Intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1614345Half life in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1220242Unbound intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1630891Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs relative to control2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1777965Antiinflammatory activity in Swiss Webster mouse assessed as reversal of carrageenan-induced paw edema at 30 ug/paw local peripheral administration pretreated with carrageenan for 6 days followed by compound addition and measured 6 hrs post compound treat
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID284311Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 10 mg/kg after 3 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID675627Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced auricle tumefaction at 0.2 mmol/kg, po qd administered prior to challenge for 5 days measured 30 mins post challenge2012European journal of medicinal chemistry, Sep, Volume: 55Bone-targeting glycol and NSAIDS ester prodrugs of rhein: synthesis, hydroxyapatite affinity, stability, anti-inflammatory, ulcerogenicity index and pharmacokinetics studies.
AID1698009Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
AID1435283Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring parent compound remaining at 10 pmol/ml after 60 mins in absence of NADPH by LC-MS/MS analysis2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID173208Gastrointestinal tolerability was evaluated in rats and amount blood loss was reported1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
AID1377476Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 5 hrs relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID1744240Metabolic stability in human liver microsomes assessed as half-life at 10 uM incubated for 1 hr in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1517056Antiinflammatory activity in Sprague-Dawley rat assessed as carrageenan-induced paw size at 50 mg/kg, ip administered 1 hr before carrageenan stimulation and measured after 3 hrs (Rvb 32.15 =/- 1.08 %)
AID1211257Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1271586Binding affinity to equine serum albumin assessed as association constant to higher affinity site by isothermal titration calorimetric analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID681110TP_TRANSPORTER: inhibition of E217betaG in the presence of Diclofenac at a concentration of 100uM in membrane vesicles from MRP1-expressing Sf9 cells2003Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16
The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs.
AID684907Analgesic activity against po dosed rat assessed as reversal of carrageenan-induced mechanical hyperalgesia at 20 mg/kg, po2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists.
AID775743Inhibition of purified mouse COX-2 assessed as inhibition of PGE2/PGD2 formation preincubated at 10 uM for 15 mins before arachidonic acid substrate addition measured after 30 seconds by LC-MS-MS method2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID241313In vitro inhibitory activity against ovine cyclooxygenase-1 (COX-1) at 200 uM; Inactive2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1394643Drug metabolism in human liver S9 fraction assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 120 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1271593Binding affinity to human serum albumin assessed as association constant to lower affinity site by HPLC method2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1717042Antiinflammatory activity assessed as inhibition of heat-induced albumin denaturation preincubated for 20 mins followed by heating at 51 degC and measured after 2 mins by UV-vis spectrophotometric method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.
AID1223481Elimination half life iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID280210Solubility at acidic pH2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1433583Metabolic stability in Wistar rat liver S9 fraction assessed as UGT-mediated glucuronidation of compound by measuring compound remaining at 5 uM preincubated for 3 mins followed by UDPGA addition measured after 60 mins by HPLC/MS analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A
AID310932Permeability across human Skin2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1582080Metabolic stability in CD1 mouse liver microsomes assessed as half life at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID1576577Effective permeability of compound incubated for 8 hrs by PAMPA2019MedChemComm, Dec-01, Volume: 10, Issue:12
Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling.
AID266765Effective permeability coefficient in 70% silicon-30% IPM membrane2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
AID351394Activity of Agrocybe aegerita peroxygenase assessed as conversion of diclofenac to 4'-hydroxydiclofenac at 5 mM in presence of 5 mM H2O2 and 4 mM ascorbic acid2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Regioselective preparation of 5-hydroxypropranolol and 4'-hydroxydiclofenac with a fungal peroxygenase.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1614347Stability in human liver microsomes assessed as compound remaining in presence of NADPH regenerating system measured after 60 mins by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID426478Cytotoxicity against mouse L1.2 cells assessed as cell viability by trypan blue dye exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1220240Unbound fraction during CYP4500-mediated metabolism in human intestinal microsomes2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID1220237Unbound fraction during UGT-mediated glucuronidation in human intestinal microsomes2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1514446Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins in presence of G-6-P, G-6-PDH, MgCl2 and NADP+ by LC-MS/MS analysis (Rvb = 100%)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1501466Drug metabolism assessed as UGT1A4 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1395375Drug metabolism in mouse liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 60 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID284312Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 20 mg/kg after 30 min2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1422275Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 60 mins in absence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1873779Metabolic stability in rat liver microsomes assessed as intrinsic clearance incubated for 5 mins in presence of NADPH by HPLC analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1209248Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by optimal design approach2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID781325pKa (acid-base dissociation constant) as determined by Liao ref: J Chem Info Model 20092014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1450585In vivo drug metabolism in human assessed as UGT2B7-mediated 4'-hydroxydiclofinac acyl glucuronide level in urine2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
AID1450610Intrinsic clearance in human liver microsomes assessed as 4'-hydroxydiclofinac acyl glucuronide level by LC-MS/MS analysis2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
AID1614372Intrinsic clearance in human liver measured from intrinsic clearance in human liver microsomes in presence of NADPH regenerating system by LC/MS/MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID1379266Anti-inflammatory activity in human RBC assessed as membrane stabilization
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1142445Inhibition of human recombinant COX2 after 2 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1355799Metabolic stability in human liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1348378Drug metabolism in human liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 60 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1529180Binding affinity to human serum albumin assessed as dissociation constant pKa1 at 1:1 ratio by UV-pH titration based spectrophotometric analysis (Rvb = 3.87 No_unit)2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID310931Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1211210Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1348376Drug metabolism in human liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 15 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1501463Drug metabolism assessed as CYP3A4 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1824588Metabolic stability in CD-1 mouse liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID657310Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 1 mg/kg, po administered 60 mins before DABK challenge2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
AID1650564Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1450584In vivo drug metabolism in human assessed as CYP2C9-mediated 4'-hydroxydiclofinac metabolite formation2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1542245Anti-inflammatory activity in lipopolysaccharide challenged rat PC12 cells assessed as decrease in TNFalpha production at 100 uM pre-incubated for 24 hrs before LPS challenge for 48 hrs by immunoblot analysis2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1211200Drug metabolism in human liver microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1876432Metabolic stability in human liver microsomes assessed as intrinsic clearance2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID546254Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.
AID1395376Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 15 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1514462Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 120 mins in presence of G-6-P, G-6-PDH, MgCl2 and NADP+ by LC-MS/MS analysis (Rvb = 100%)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID374254Antiinflammatory activity in albino rat chronic arthritis model assessed as inhibition of Freund's adjuvant-induced paw edema at 13.5 mg/kg, po administered on day 16 to 19 post Freund's adjuvant challenge measured on day 19 relative to control2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and pharmacological evaluation of a novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1209258Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by multiple depletion curves method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1752939Half life in human liver microsomes measured upto 40 mins by LC-MS/MS analysis
AID1141097Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID47749Inhibitory activity against human carbonic anhydrase II was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID675291Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 2.5 hrs post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID1887670Metabolic stability in human liver microsome assessed as parent compound remaining at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID1128731Inhibition of squalene synthase in rat liver microsomes assessed as decrease in conversion of [3H]FPP to squalene2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1703889Permeability of the compound incubated for 8 hrs by PAMPA-TGI assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1211220Ratio of unbound intrinsic glucuronidation clearance in human kidney microsomes in presence of 1% bovine serum albumin to unbound intrinsic glucuronidation clearance in human kidney microsomes in absence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID166759Variation of intraocular pressure in second day at a dose of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1736743Metabolic stability in human liver microsomes assessed as parent compound remaining in absence of NADPH after 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID1211284Glucuronidation clearance in human liver microsomes2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID588998Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, MRP42010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID184053Inhibition of carrageenan-induced 4 hours after 50 mg/kg i.p. administration in rats.1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Molecular design, synthesis, and antiinflammatory activity of a series of beta-aminoxypropionic acids.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1395374Drug metabolism in mouse liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 30 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1777956Antiinflammatory activity in Swiss Webster mouse assessed as protection against carrageenan-induced paw edema at 30 ug/paw local peripheral pretreatment with compound for 15 mins followed by carrageenan challenge and measured after 6 hrs
AID1584743Drug metabolism in rat liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID280216Dissociation constant, pKa at pH 7.02007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1355796Half life in human liver microsomes after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID1809978Metabolic stability in mouse liver microsomes assessed as half-life2021Bioorganic & medicinal chemistry letters, 12-01, Volume: 53Discovery of novel aminosaccharide-based sulfonamide derivatives as potential carbonic anhydrase II inhibitors.
AID1056666Analgesic activity in Lewis rat assessed as reversal of MIA-induced osteoarthritic pain at 5 mg/kg, po administered 1 hr prior to test2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Selective cannabinoid receptor type 2 (CB2) agonists: optimization of a series of purines leading to the identification of a clinical candidate for the treatment of osteoarthritic pain.
AID50345Inhibitory activity against human carbonic anhydrase I was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1593388Half life in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID1333579Antiinflammatory activity in rat carrageenan-induced paw edema model assessed as inhibition of paw swelling at 25 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 3 hrs2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Polyfluorinated salicylic acid derivatives as analogs of known drugs: Synthesis, molecular docking and biological evaluation.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1564364Microsomal stability in human liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 15 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1698010Hepatic clearance in human administered through iv dosing
AID1141078Acute antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 2 hrs by plethysmometric analysis relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID1199061Inhibition of human AR by fluorescence assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Targeting aldose reductase for the treatment of diabetes complications and inflammatory diseases: new insights and future directions.
AID216266First dissociation constant of the binding of compound to wild type TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID1584751Drug metabolism in dog liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1128714Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.
AID1348372Drug metabolism in mouse liver microsomes assessed as CYP450-mediated metabolite formation by measuring parent compound remaining at 5 uM after 15 mins in presence of NADPH by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1698005Ratio of drug level in Wistar Hannover rat blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1542242Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID1887671Metabolic stability in human liver microsome assessed as parent compound remaining at 100 uM measured after 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID1718807Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 100 uM measured after 60 mins by LC-MS/MS analysis
AID754990Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 50 mg/kg administered 30 mins followed by acetic acid challenge measured for 20 mins relative to control2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
A facile synthesis, anti-inflammatory and analgesic activity of isoxazolyl-2,3-dihydrospiro[benzo[f]isoindole-1,3'-indoline]-2',4,9-triones.
AID1222959Cmax in rat hepatocytes assessed as S-acyl-GSH-thioester at 100 uM2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
Metabolic activation of mefenamic acid leading to mefenamyl-S-acyl-glutathione adduct formation in vitro and in vivo in rat.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1876431Metabolic stability in human liver microsomes assessed as half life2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1211271Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1779258Metabolic stability in rat liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID1226815Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis2015European journal of medicinal chemistry, Jun-05, Volume: 97Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
AID403704Inhibition of human COX2 expressed in sf9 cells2005Journal of natural products, Oct, Volume: 68, Issue:10
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
AID1571695Intrinsic clearance in liver by measuring in intrinsic clearance in human liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1824589Metabolic stability in CD-1 mouse liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID1422313Clearance in monkey hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1426399Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1595285Analgesic activity in albino mouse assessed as inhibition of acetic acid induced writhing at 10 mg/kg po2019European journal of medicinal chemistry, Jun-01, Volume: 171Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.
AID1582081Metabolic stability in CD1 mouse liver microsomes assessed as intrinsic clearance at 10 uM incubated for 1 hr2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Discovery and Characterization of 1
AID374574Antiinflammatory activity in Wistar albino rat assessed as reduction in formalin-induced paw edema volume at 50 mg/kg, po administered 30 mins prior to formalin challenge measured after 90 mins by plethysmography2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1141082Analgesic activity in albino mouse assessed as protection against glacial acetic acid-induced writhing at 19.5 mg/kg, po administered 0.5 hrs followed by glacial acetic acid challenge measured for 15 mins relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID284313Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 20 mg/kg after 1 hr2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1548576Intrinsic clearance in human liver derived from clearance in liver microsomes in presence of NADPH regenerating system by LC-MS/MS analysis2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.
AID1435277Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring compound half life at 10 pmol/ml preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis2017ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3
Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1355798Intrinsic clearance in human liver after 10 mins in presence of NADPH by LC/MS/MS analysis2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1461600Inhibition of soybean lipoxygenase preincubated for 5 mins followed by linoleic acid substrate addition measured after 20 mins by spectrophotometric method2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.
AID1564362Microsomal stability in human liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 30 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1779257Metabolic stability in mouse liver microsome assessed as half life2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.
AID1736741Metabolic stability in human liver assessed as intrinsic clearance incubated for 1 hr by LC/MS/MS method2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.
AID351539Activity of Bacillus megaterium CYP450 D6H10 mutant assessed as conversion of diclofenac to 4'-hydroxydiclofenac at 5 mM in presence of 1 mM H2O2 and 4 mM ascorbic acid2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Regioselective preparation of 5-hydroxypropranolol and 4'-hydroxydiclofenac with a fungal peroxygenase.
AID280214Aqueous solubility at pH 7.02007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID280220Intrinsic solubility at 25 degC2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID284307Analgesic activity in Wistar Albino mouse at 20 mg/kg, po after 3 hrs by tail-flick technique2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1301938Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1395370Drug metabolism in mouse liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 15 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1542243Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of ovine COX-22019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID1595207Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg po and measured after 4 hrs of carrageenan addition relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.
AID266771Permeability in human skin2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
AID361986Lipophilicity, log D of compound at pH 7.4 by shake flask method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID284315Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 20 mg/kg after 3 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID775745Inhibition of purified mouse COX-2 assessed as inhibition of PGE2-G/PGD2-G formation preincubated for 15 mins before 2-AG substrate addition measured after 30 seconds by LC-MS-MS method2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID493627Antiinflammatory activity in Albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs (Rvb = 1.44 +/- 0.046 ml)2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID99661First dissociation constant of the binding of compound to L55P TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID1584740Drug metabolism in rat liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1211245Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID99658Inhibition of L55P TTR fibril formation was measured at OD400.2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID1211280Fraction unbound in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID450462Binding affinity to D10/DA24 ssDNA aptamer2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
ssDNA aptamers that recognize diclofenac and 2-anilinophenylacetic acid.
AID1501460Drug metabolism assessed as CYP2C9 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1542251Neuroprotection activity in lipopolysaccharide challenged rat PC12 cells assessed as decrease in ROS production at 100 uM pre-incubated for 24 hrs before LPS challenge for 48 hrs by DHE and DAPI staining based fluorescence assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID239780Percentage plasma protein binding towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID254882Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.
AID446880Gastrointestinal toxicity in rat assessed as ulcerogenic index at 100 mg/kg, po after 3 hrs2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
NO-NSAIDs: Gastric-sparing nitric oxide-releasable prodrugs of non-steroidal anti-inflammatory drugs.
AID1880389Metabolic stability in human liver assessed as intrinsic clearance in microsomes at 1 uM measured up to 45 mins in presence of NADPH by LC-MS/MS analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1306899Analgesic activity in ip dosed albino Swiss mouse assessed as nociceptive response measured after 60 mins by hot plate method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.
AID280221Intrinsic solubility in 0.15 M KCl at 25 degC by potentiometric titration2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1744238Metabolic stability in rat liver microsomes assessed as half-life at 10 uM incubated for 1 hr in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1164212Analgesic activity in Sprague-Dawley rat assessed as protection against acetic acid-induced abdominal constriction dosed 1 hr before acetic acid challenge measured for 20 mins post acetic acid challenge2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID280212Solubility at neutral pH2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID347223Inhibition of 5LOX in bovine polymorphonuclear leucocytes assessed as leukotriene B4 formation2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1584736Drug metabolism in mouse liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1584748Drug metabolism in dog liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1211241Fraction unbound in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1886473Metabolic stability in human liver microsomes assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1501468Drug metabolism assessed as UGT1A8 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID272861Antinociceptive activity in mouse at 5 mg/kg, po measured as number of acetic acid-induced writhes by abdominal constriction assay2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
AID1706969Stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining at 10 uM measured after 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID471927Analgesic activity against Swiss albino mouse assessed as increase in paw licking or jump response at 10 mg/kg, po after 1.5 hrs by hot plate method2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1910023Metabolic stability in human liver microsomes at 20 uM assessed as intrinsic clearance measured up to 90 mins by LC-HRMS analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Development of Predictive Classification Models for Whole Cell Antimycobacterial Activity of Benzothiazinones.
AID1307711Activation of TREK1 (unknown origin) expressed in Xenopus oocytes assessed as increase in channel currents at 100 uM relative to control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID1692508Metabolic stability in mouse liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID374568Antiinflammatory activity in Wistar albino rat assessed as reduction in formalin-induced paw edema volume at 50 mg/kg, po administered 30 mins prior to formalin challenge measured after 30 mins by plethysmography2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, pharmacological screening, quantum chemical and in vitro permeability studies of N-Mannich bases of benzimidazoles through bovine cornea.
AID1164213Anti-inflammatory activity in Swiss mouse model of carrageenan-induced paw edema assessed as reduction in paw swelling at 50 mg/kg, sc dosed 30 mins before carrageenan challenge measured at 1 to 4 hrs post carrageenan challenge by mercury plethysmometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1223477Total clearance in iv dosed human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Prediction of in vivo hepatic clearance and half-life of drug candidates in human using chimeric mice with humanized liver.
AID552071Antiinflammatory activity in rat assessed as inhibition of complete Freund's adjuvant-induced paw swelling at 5 mg/kg, po administered on day 21 post induction of inflammation measured on day 352011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives.
AID1301945Antiinflammatory activity in Swiss albino mouse assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, ip dosed 30 mins before carrageenan injection measured up to 300 mins by vernier calliper method relative to control2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.
AID1744367Intrinsic clearance in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.
AID1739433Metabolic stability in human liver microsomes assessed as half life at 100 uM measured upto 30 mins2020European journal of medicinal chemistry, Aug-15, Volume: 200Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
AID1733222Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 7.5 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 5 days by plethysmometeric method2021Bioorganic & medicinal chemistry, 04-15, Volume: 36Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease.
AID1584755Drug metabolism in human liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 30 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID374251Antiinflammatory activity in albino rat acute inflammatory model assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po dosed 1 hr before carrageenan challenge measured after 2 hrs relative to control2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and pharmacological evaluation of a novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents.
AID1394646Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured after 30 mins in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1272494Anti-inflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 150 umol/kg, ip after 3.5 hrs relative to control2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Amides of non-steroidal anti-inflammatory drugs with thiomorpholine can yield hypolipidemic agents with improved anti-inflammatory activity.
AID432209Inhibition of lipid peroxidation assessed as malondialdehyde level per 100 mg of gastric mucosa isolated from albino mouse at dose 30 mg/kg, po2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID347222Inhibition of COX2 in LPS-stimulated human blood2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID471925Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety.
AID1426400Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 1 hr relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.
AID1422273Stability in human liver microsomes assessed as parent compound remaining at 1 uM after 10 mins in presence of NADPH by LC-MS/MS analysis2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.
AID1141096Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control2014Bioorganic & medicinal chemistry, May-15, Volume: 22, Issue:10
Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents.
AID1744241Intrinsic clearance in human liver microsomes at 10 uM incubated for 1 hr in presence of NADPH by LC-MS/MS analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1334724Anti-inflammatory activity against carrageenan-induced paw edema in albino rat assessed as paw thickness at 60 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured at 3 hrs post carrageenan challenge (Rvb = 0.401 +/- 0.019 mm)
AID1712992Analgesic activity in Swiss albino mouse administered ip and measured after 60 mins by hot plate method2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID1501464Drug metabolism assessed as UGT1A1 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1212341Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID325055Inhibition of mouse COX2 for 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID426476Inhibition of wild type CXCR1 transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1377474Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity.
AID675292Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 3 hrs post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID1271587Binding affinity to equine serum albumin assessed as association constant to lower affinity site by isothermal titration calorimetric analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Structural Insights into the Competitive Binding of Diclofenac and Naproxen by Equine Serum Albumin.
AID280219Kinetic solubility at 25 degC2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1409434Half life in human liver microsomes at 2 uL by LC/MS/MS analysis2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant.
AID1211279Renal clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1608194Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-stimulated ROS production at 20 uM pretreated for 1 hrs followed by LPS addition and measured after 24 hrs by DCFH-DA dye based fluorescence assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1584756Drug metabolism in human liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID17663First dissociation constant of the binding of compound to V30M TTR2002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
AID1422308Half life in dog hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID1209239Drug metabolism in assessed as human CYP2C9-mediated maximum rate of reaction per mg protein2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1524892Stability in human liver microsomes assessed as compound remaining incubated of 60 mins in presence of NADPH regenerating system by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Discovery of novel pyrazole derivatives as potential anticancer agents in MCL.
AID677462Dissociation constant, pKa of the compound2012European journal of medicinal chemistry, Jul, Volume: 53Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach.
AID552066Antiinflammatory activity in bovine serum assessed as denaturation of albumin at 5 mM after 10 mins by spectrophotometry2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives.
AID1876433Metabolic stability in human liver assessed as intrinsic clearance2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
AID1217709Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1054848Inhibition of human recombinant TTR Y78F mutant-mediated fibrillogenesis after 30 mins by turbidimetric assay2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Modulation of the fibrillogenesis inhibition properties of two transthyretin ligands by halogenation.
AID1365602Anti inflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 50 mg/kg measured after 1 to 4 hrs by plethysmographic method relative to control2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Recently reported biological activities of pyrazole compounds.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID493632Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1593389Intrinsic clearance in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1333583Analgesic activity in rat assessed as latent period prolongation at 25 mg/kg, ip measured after 1 hr by hot plate test2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Polyfluorinated salicylic acid derivatives as analogs of known drugs: Synthesis, molecular docking and biological evaluation.
AID1692510Metabolic stability in rat liver microsomes assessed as compound remaining measured after 60 mins by LC/MS-MS analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of a non-zwitterionic oseltamivir analogue as a potent influenza a neuraminidase inhibitor.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1433577Metabolic stability in CD-1 mouse liver S9 fraction assessed as UGT-mediated glucuronidation of compound by measuring compound remaining at 5 uM preincubated for 3 mins followed by UDPGA addition measured after 60 mins by HPLC/MS analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A
AID1756363Metabolic stability in rat hepatocytes assessed as intrinsic clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID469579Gastrointestinal toxicity in Wistar rat assessed as ulcer incidence at 24 mg/kg, po2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs.
AID1846857Anti-inflammatory activity against carrageenan induced paw edema in rat assessed as inhibition of paw edema at 12.5 mg/kg,PO pretreated for 1 hrs followed by carrageenan addition for 4 hrs by plethysmographic analysis relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID284314Anti-inflammatory activity against Carrageenan-induced paw oedema rat model at 20 mg/kg after 2 hrs2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and pharmacological evaluation of some 3-phenyl-2-substituted-3H-quinazolin-4-one as analgesic, anti-inflammatory agents.
AID1501471Drug metabolism assessed as UGT2B7 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1744223Apparent permeability at pH 7.4 by PAMPA2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis.
AID1880390Metabolic stability in human liver assessed as intrinsic clearance at 1 uM measured up to 45 mins in presence of NADPH by LC-MS/MS analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1584742Drug metabolism in rat liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 60 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1824586Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
AID1608177Inhibition of recombinant human COX2 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID1706968Intrinsic microsomal clearance in Sprague-Dawley rat liver microsomes at 10 uM measured up to 60 mins in presence of NADPH regenerating system by HPLC analysis2021European journal of medicinal chemistry, Feb-15, Volume: 212Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.
AID1593390Intrinsic clearance in human liver measured from intrinsic clearance in human liver microsomes2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1164202Inhibition of purified ovine COX1 at saturation drug level pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1564370Microsomal stability in mouse liver microsomes assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM and measured for 15 mins in presence of UDPGA by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID493631Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
Synthesis and anti-inflammatory activity of some 3-(4,6-disubtituted-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl) propanoic acid derivatives.
AID1712991Antiinflammatory activity against Sprague-Dawley rat assessed as reduction in carragenan-induced paw edema administered ip and measured after 2 hrs by plethysmometry2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID1212314Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID1422311Clearance in Sprague-Dawley rat hepatocytes at 1 uM2018Bioorganic & medicinal chemistry letters, 11-15, Volume: 28, Issue:21
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1608176Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
AID1895928Metabolic stability in human liver assessed as intrinsic clearance by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of C5-NH
AID347221Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
AID1061772Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID313122Inhibition of mouse COX2 R120A mutant2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1177997Analgesic activity in Swiss albino mouse assessed as decrease in capsaicin-induced paw lickings at 25 mg/kg, ip administered 30 mins before capsaicin injection2014European journal of medicinal chemistry, Apr-22, Volume: 77Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.
AID1519612Metabolic stability in rat liver microsomes assessed as compound remaining incubated for 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
AID1211264Ratio of UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID28926Effective permeability corrected for ionization2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID308403Displacement of fluorescent 5-Cyano-2-[(E)-2-(1-methyl-1H-indol-2-yl)-vinyl]-benzoic acid from human serum albumin2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.
AID1294300Antiinflammatory activity in rat MIA model assessed as inhibition of differential weight bearing at 5 mg/kg, po measured 30 mins post dose by incapacitance test2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
AID1663586Half life in mouse liver microsomes2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Synthesis, in vitro ADME profiling and in vivo pharmacological evaluation of novel glycogen phosphorylase inhibitors.
AID1211281Ratio of drug level blood to plasma in human2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1650565Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX22020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID1348381Drug metabolism in human liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 60 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID675288Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 1 hr post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID775742Inhibition of purified mouse COX-2 assessed as inhibition of PGE2/PGD2 formation at 10 uM by LC-MS-MS method2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1584754Drug metabolism in human liver microsome S9 fraction assessed as UGT-mediated metabolism by measuring compound remaining at 5 uM pretreated with UDPGA and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID624644Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A62005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID233731Activity ratio is the percent inhibition iof paw volume increase at 100 umol/kg, po to that of diclofenac at 100 umol/kg, po administration2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID280218Intrinsic solubility in distilled water at pH 4.772007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Diclofenac solubility: independent determination of the intrinsic solubility of three crystal forms.
AID1887655Metabolic stability in human liver assessed as intrinsic clearance at 100 uM incubated for 180 mins in presence of NADPH by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.
AID1211231Drug metabolism in human kidney microsomes assessed as UGT1A9/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1164203Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1705462Binding affinity to wild type TTR (unknown origin) expressed in Escherichia coli BL21/DE3 by Circular dichroism spectroscopy2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.
AID1584730Drug metabolism in human liver microsome S9 fraction assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM pretreated with NADPH and measured after 15 mins by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID266763Membrane retention in 70% silicon-30% IPM membrane2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1395378Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 60 mins in presence of NADPH by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID1564369Microsomal stability in mouse liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 60 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID176483Compound administered perorally for inhibition of carrageenan induced paw edema after 3h in rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1404017Permeability of the compound at 500 uM after 8 hrs by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID1070453Activation of NAG-1 in human SW1353 cells at 20 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Octulosonic acid derivatives from Roman chamomile (Chamaemelum nobile) with activities against inflammation and metabolic disorder.
AID1209250Drug metabolism in human liver microsomes by multiple depletion curves method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1542246Anti-inflammatory activity in lipopolysaccharide challenged rat PC12 cells assessed as decrease in interleukin-1 beta production at 100 uM pre-incubated for 24 hrs before LPS challenge for 48 hrs by immunoblot analysis2019European journal of medicinal chemistry, Apr-01, Volume: 167Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1564363Microsomal stability in human liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 60 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1394644Drug metabolism in human liver microsomes assessed as CYP450 mediated compound hydrolysis by measuring parent compound remaining at 5 uM measured immediately in presence of NADPH by RP-HPLC analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID1718808Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 100 uM measured after 60 mins in presence of NADPH by LC-MS/MS analysis
AID1395380Drug metabolism in human liver microsomes assessed as UGT mediated compound hydrolysis by measuring parent compound remaining at 5 uM after 30 mins in presence of UDPGA by UPLC/MS/ESI analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID325072Inhibition of mouse COX2 V349L mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid2007The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
AID1501470Drug metabolism assessed as UGT1A10 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1211285Glucuronidation clearance in human liver microsomes in presence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID442515Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation at 50 uM2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.
AID657312Antihyperalgesic activity in Sprague-Dawley rat assessed as decrease in CFA-induced joint pain at 1 to 3 mg/kg, po administered 3 days post CFA challenge2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID390753Inhibition of cyclooxygenase 12008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.
AID1613067Antinociceptive activity in ICR mouse assessed as reduction in licking time at 31.6 mg/kg, po dosed 30 mins before formalin injection and by formalin test
AID1413501Stability in human liver microsomes assessed as parent compound remaining at 10 mM preincubated for 10 mins followed by NADPH addition and measured after 60 mins by LC-MS analysis2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant.
AID166904Variation of intraocular pressure in sixth day at a dose of 30 mg/kg by systemic administration in hypertensive rabbits2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1846818Anti-inflammatory activity against carrageenan-induced paw edema in rat relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Contemporary advances of cyclic molecules proposed for inflammation.
AID675287Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 0.5 hrs post carrageenan-induced inflammation2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, characterization and pharmacological study of 4,5-dihydropyrazolines carrying pyrimidine moiety.
AID48294Inhibitory activity against human carbonic anhydrase IX was determined2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1164204Inhibition of human recombinant COX2 at saturation drug level pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
AID1886474Metabolic stability in human liver assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition for 2 hrs and measured upto 60 mins by high performance liquid chromatography-tandem mass spectrometry
AID1142446Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX22014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1501459Drug metabolism assessed as CYP1A2 (unknown origin)-mediated metabolite formation2017European journal of medicinal chemistry, Oct-20, Volume: 1391-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
AID1564367Microsomal stability in mouse liver microsomes assessed as CYP450-mediated metabolism by measuring compound remaining at 5 uM and measured for 15 mins in presence of NADPH by UPLC-MS/MS analysis (Rvb = 100%)2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1142444Inhibition of ovine COX1 after 2 mins by EIA2014European journal of medicinal chemistry, Jun-10, Volume: 80Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.
AID1571693Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis2019MedChemComm, Mar-01, Volume: 10, Issue:3
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation.
AID1630903Analgesic activity in rat assessed as pain threshold time at 10 mg/kg, po measured at 1.5 hrs post dose by hot plate method (Rvb = 19.1 to 21.2 sec)2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents.
AID1348380Drug metabolism in human liver microsomes assessed as UGT-mediated metabolite formation by measuring parent compound remaining at 5 uM after 30 mins in presence of UDPGA by UPLC-MS method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1346800Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)2002Molecular pharmacology, Jan, Volume: 61, Issue:1
Diclofenac antagonizes peroxisome proliferator-activated receptor-gamma signaling.
AID1345206Human COX-2 (Cyclooxygenase)2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Structural and functional basis of cyclooxygenase inhibition.
AID1345284Human COX-1 (Cyclooxygenase)2005Journal of natural products, Oct, Volume: 68, Issue:10
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
AID1796989Carbonic Anhydrase Enzyme Inhibition Assay from Article 10.1021/jm030912m: \\Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.\\2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1796990hCA IX Enzyme Inhibition Assay from Article 10.1021/jm030912m: \\Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.\\2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
AID1802994UDP-glucuronosyltransferase Activity Assay from Article 10.3109/14756366.2010.518965: \\The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors.\\2011Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 26, Issue:3
The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors.
AID1801103Fluorophore Displacement Assay from Article 10.1021/cb5005178: \\Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein.\\2014ACS chemical biology, Nov-21, Volume: 9, Issue:11
Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,254)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990665 (8.06)18.7374
1990's1342 (16.26)18.2507
2000's2336 (28.30)29.6817
2010's2940 (35.62)24.3611
2020's971 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 143.04

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index143.04 (24.57)
Research Supply Index9.28 (2.92)
Research Growth Index4.88 (4.65)
Search Engine Demand Index289.38 (26.88)
Search Engine Supply Index2.11 (0.95)

This Compound (143.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,874 (21.12%)5.53%
Reviews477 (5.38%)6.00%
Case Studies683 (7.70%)4.05%
Observational24 (0.27%)0.25%
Other5,816 (65.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (364)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Sustained Acoustic Medicine (SAM) for Symptomatic Treatment of Knee Pain Related to Osteoarthritis [NCT05882812]Phase 2120 participants (Anticipated)Interventional2023-06-03Recruiting
Clinical Efficacy and Safety of Benjakul Recipe in Treating Primary Osteoarthritis of Knee Compared With Diclofenac (Clinical Trial Phase II) [NCT02286453]Phase 284 participants (Actual)Interventional2014-09-30Completed
The Effect of Topical Sodium Diclofenac on Macular Thickness in Diabetic Eyes After Phacoemulsification: A Randomized Controlled Trial [NCT02306031]Phase 2108 participants (Anticipated)Interventional2013-06-30Active, not recruiting
A Cumulative Skin Irritation Study Investigating the Skin Irritancy Potential of MFC51123 Diclofenac-Menthol Gel [NCT02169154]Phase 136 participants (Actual)Interventional2014-06-01Completed
MuscleCare™ Pain Relief Therapy vs. Voltaren® in the Relief of Trapezius Trigger Point Musculoskeletal Pain. [NCT03939884]Phase 4120 participants (Actual)Interventional2017-03-28Completed
Use of Etoricoxib Compared to Diclofenac in the Perioperative Treatment of Patients After Total Hip Arthroplasty, a Prospective, Double Blind, Phase III Study [NCT01229774]Phase 3100 participants (Actual)Interventional2011-02-28Completed
Oral Pregabalin Versus Intravenous Hydrocortisone in Treatment of Postdural Puncture Headache After Spinal Anesthesia for Elective Cesarean Section [NCT03910088]Phase 430 participants (Actual)Interventional2019-04-20Completed
Topical Diclofenac for the Treatment of Noncyclic Breast Pain [NCT00276419]Phase 2/Phase 325 participants (Actual)Interventional2005-06-30Terminated(stopped due to Lack of funds; FDA approved a topical form of diclofenac during study, no need to continue study of pharmacy-compounded drug.)
Efficacy of PENNSAID® for Pain Management in the Emergency Department [NCT01350622]0 participants (Actual)Interventional2011-12-31Withdrawn(stopped due to Study never initiated)
COMPARISON OF EFFICACY OF DICLOFENAC VERSUS DICLOFENAC PLUS CODEINE AND DICLOFENAC PLUS LACOSAMIDE IN ACUTE SCIATICA [NCT05626140]Phase 3120 participants (Actual)Interventional2021-09-28Completed
Efficacy of Diclofenac Potassium Versus Nimesulide in the Treatment of Fever and Pain in Children Aged 3 to 7 Years With Community Acquired, Non-complicated, Upper Respiratory Tract Infection [NCT01257126]Phase 40 participants (Actual)Interventional2011-04-30Withdrawn
Long-term Outcomes of Breast Cancer Patients Receiving Levobupivacaine Wound Infiltration or Diclofenac for Postoperative Pain Relief [NCT05829707]Phase 4120 participants (Actual)Interventional2009-01-05Completed
A Randomized, Double-blind, Multi-site, Comparator-controlled, Phase III Trial to Evaluate the Efficacy and Safety of a Fixed-dose Combination of Tramadol Hydrochloride and Diclofenac Sodium in Acute Moderate to Severe Pain After Third Molar Extraction [NCT03714672]Phase 31,151 participants (Actual)Interventional2017-08-26Completed
An Open-label, Single-dose, Active-controlled Randomized Phase IIa Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of RPH-104 (RPH-104/L04018) Administered at Different Doses to Patients With Acute Gout Attack [NCT04067492]Phase 247 participants (Actual)Interventional2018-03-26Terminated(stopped due to In view of the continuing insufficient patient recruitment in the study due to the difficult epidemiological situation and the need for rational allocation of company resources, as well as based on the results of the interim analysis.)
A Phase 1, Randomized, Single Center, Open-Label, Multiple-Dose, Three-Way Crossover Study to Evaluate the Pharmacokinetics, Bioavailability and Safety of PENNSAID Gel in Comparison With Sandoz 75 mg Diclofenac Sodium Delayed Release Tablet and PENNSAID ( [NCT01202799]Phase 130 participants (Actual)Interventional2010-09-30Completed
Proof of Concept: Diclofenac as a KMO Inhibitor in Individuals With Alcohol Use Disorder [NCT06029296]Early Phase 112 participants (Anticipated)Interventional2023-11-30Not yet recruiting
Tubal Flushing Using Water Soluble Media for Unexplained Infertility: A Randomized Controlled Trial [NCT02433418]Phase 3300 participants (Anticipated)Interventional2015-05-31Recruiting
Acute Neuroendocrine Response to Intravenous Infusion of Diclofenac Sodium [NCT05188131]Phase 412 participants (Actual)Interventional2021-10-01Completed
Effect of Pre-operative Diclofenac Potassium on the Anesthetic Efficacy of Inferior Alveolar Nerve Block in Cases With Symptomatic Irreversible Pulpitis: A Randomized Controlled Trial [NCT03163420]Phase 2/Phase 368 participants (Anticipated)Interventional2016-07-31Active, not recruiting
A Randomized, Double-Blind, Placebo-Controlled, Parallel Arm, Steady-State Pharmacokinetic and Disposition Study Characterizing Diclofenac's Plasma and Knee Exposure in Osteoarthritis (OA) Subjects Undergoing Scheduled Arthroplasty After Treatment With Di [NCT03497039]Phase 147 participants (Actual)Interventional2018-07-19Completed
Diclophenac Versus Placebo for Pain Control in Diagnostic Colonoscopy: a Randomized Controlled Study [NCT02339428]Phase 390 participants (Actual)Interventional2015-01-31Completed
A Double-Blind, Parallel-group, 4-Week Trial to Assess the Efficacy and Safety of Etoricoxib 60 mg and Diclofenac 150 mg in Patients With Chronic Low Back Pain [NCT00090181]Phase 4401 participants (Actual)Interventional2004-06-30Completed
The Underlying Mechanisms of Diameter Changes in Retinal Vessels During Hypoxia [NCT02059018]20 participants (Actual)Interventional2014-02-28Completed
Evaluation of the Effects of Different Analgesics on Pain and Health-related Quality of Life of Patients With Pericoronitis in the Short-term Period: A Randomized, Double-blind, Clinical Trial [NCT03745599]Phase 460 participants (Actual)Interventional2017-11-01Completed
Prospective Controlled Study of Surgical Management of Unstable Thoracic Cage Injuries and Chest Wall Deformity in Trauma [NCT02132416]92 participants (Actual)Interventional2014-05-31Completed
Phase II Study of Simvastatin, Zoledronic Acid, Bortezomib, Bendamustine and Methylprednisolone for Relapsed/Refractory Myeloma [NCT01332617]Phase 20 participants (Actual)Interventional2011-04-30Withdrawn(stopped due to Investigators no longer interested in activating study)
Topical Vitamin D3, Diclofenac or a Combination of Both to Treat Basal Cell Carcinoma [NCT01358045]Phase 2128 participants (Actual)Interventional2011-11-30Completed
Electroacupuncture for Sciatica Due to Intervertebral Disc Displacement [NCT02087462]324 participants (Anticipated)Interventional2012-01-31Recruiting
A Comparison of Analgesic İmpacts of Piroxicam and Diclofenac Sodium in the Treatment of Primary Dysmenorrhea:A Double-Blind, Randomized Trial [NCT02253446]Phase 4400 participants (Actual)Interventional2013-05-31Completed
Diclofenac Potassium With or Without Vaginal Dinoprostone Prior to Hysterosalpingography in Primarily Infertile Patients: a Randomized Controlled Trial [NCT04500509]200 participants (Actual)Interventional2020-09-01Completed
Pilot Study to Test Uniformity of Transdermal Drug Delivery to the Breast Using Diclofenac Epolamine as a Model [NCT01380353]Early Phase 130 participants (Actual)Interventional2011-06-30Completed
Analgesic Effect of a New Metamizol Oral Pharmaceutical Form for the Treatment of the Neoplastic Chronic Pain: Randomized, Double-blind Crossover Clinical Trial Between Metamizol, Diclofenac and Placebo [NCT02181920]Phase 46 participants (Actual)Interventional2000-03-31Terminated
The Relationship Between Patient Preferences, Analgesic Delivery Method and Pain Reduction in Spine Patients [NCT01263652]0 participants (Actual)Interventional2010-12-31Withdrawn(stopped due to inability to complete recruitment as planned)
Collagen Crosslinking With Ultraviolet-A in Asymmetric Corneas [NCT01189864]3,493 participants (Actual)Observational2010-02-01Terminated(stopped due to Terminated to initiate FDA IND-cleared study protocol)
A Randomized Study Comparing Etoricoxib and Diclofenac Sodium in Post Hallux Valgus Surgery Pain [NCT01190722]Phase 40 participants (Actual)Interventional2010-11-10Withdrawn(stopped due to The study site was closed down)
Evaluation of Efficacy and Tolerability of a Fixed Dose Combination of Eperisone Hydrochloride and Diclofenac Sodium in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain: An Observer Blind, Prospective, Randomized, Controlled Stud [NCT01300312]Phase 3239 participants (Actual)Interventional2011-02-28Completed
Double-Blind, Triple Dummy, Parallel-Group, Randomized, Six-Month Study To Compare Celecoxib (200 Mg BID) With Diclofenac Sr (75 Mg BID) Plus Omeprazole (20 Mg QD) For Gastrointestinal Events In Subjects With Osteoarthritis And Rheumatoid Arthritis At Hig [NCT00141102]Phase 44,484 participants (Actual)Interventional2005-10-31Completed
A Clinical Study in Healthy Male Volunteers to Compare the Bioequivalence of Fixed Dose Combination of Eperisone Hydrochloride 50mg Plus Diclofenac Sodium 50mg as Capsule With Eperisone Hydrochloride 50mg and Diclofenac Sodium 50mg Tablets Under Fasting C [NCT01306318]24 participants (Actual)Interventional2011-02-28Completed
Study of Non-pharmacokinetic Interaction Between Diclofenac 25 mg and 25 mg Tramadol With the Fixed-dose Combination Tablets of the Two Drugs Administered to Healthy Subjects of Both Genders in Fasting State [NCT03766984]Phase 136 participants (Actual)Interventional2015-06-07Completed
A Randomized, Double Blind, Multi Center, Active-controlled, 2 Treatment Arm, Parallel Group Non Inferiority Study to Evaluate the Efficacy and Safety of Diclofenac Diethylamine 2.32% Gel Versus 1.16% Gel in Subjects With Acute Ankle Sprain [NCT04052620]Phase 3313 participants (Actual)Interventional2019-10-24Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Comparison Study to Determine the Therapeutic Equivalence of GDC 695 and Diclofenac Sodium Gel, 3% in Subjects With Actinic Keratoses [NCT02952898]Phase 3665 participants (Actual)Interventional2016-10-27Completed
Randomized, Open-label, Controlled Trial to Assess the Clinical Efficacy and Safety of Meloxicam Suspension 0.25 mg/kg/Day Once a Day, Versus Diclofenac 1 mg/kg/Day Twice a Day or Nimesulide 4 mg/kg/Day Twice a Day, for Five Days in the Treatment of Patie [NCT02229747]Phase 4128 participants (Actual)Interventional2001-08-31Completed
Lidocaine Infusion On Hysteroscopic Media Versus Oral Diclofinac For Pain Relief During Outpatient Hysteroscopy: A Randomized Controlled Trial [NCT03298646]44 participants (Anticipated)Interventional2017-10-31Recruiting
The Outcome of Preoperative Administration of Single-dose Ketorolac, Non-steroidal Anti-inflammatory Drug and Placebo on Postoperative Pain in Teeth With Irreversible Pulpitis and Apical Periodontitis [NCT03116672]3 participants (Actual)Interventional2016-02-02Completed
Effect of Preoperative Diclofenac Potassium on Articaine Buccal Infitration Success in Mandibular Molars With Symptomatic Irreversible Pulpitis: A Randomized Controlled Trial [NCT03174860]Phase 2/Phase 370 participants (Actual)Interventional2016-10-31Completed
Efficacy and Safety of Ingenol Mebutate Gel 0.015% Compared to Diclofenac Sodium Gel 3% in Subjects With Actinic Keratoses on the Face or Scalp [NCT02406014]Phase 4502 participants (Actual)Interventional2015-04-30Completed
Effect of Pre-medication in Pain Measures on Office Hysteroscopy - Randomized Clinical Trial [NCT03506763]Phase 4231 participants (Anticipated)Interventional2017-08-01Recruiting
Prospective Randomized Study on the Effects of Valgus Knee Brace for Knee Osteoarthritis in Chinese Patients [NCT04056845]80 participants (Anticipated)Interventional2019-09-01Recruiting
Efficacy of a Topical Pain Relief Spray Containing Herbal Oil Extracts (Bonipar) Among Individuals With Acute and Chronic Musculoskeletal Pain [NCT03471507]Phase 2164 participants (Actual)Interventional2020-12-15Completed
Rectal Disclofenac Versus Indomethacin for Prevention of Post-ERCP Pancreatitis (DIPPP): A Multicentre, Double-blind, Randomised, Controlled Trial [NCT05947461]3,612 participants (Anticipated)Interventional2023-06-01Recruiting
A Double Blind, Multi-arm Randomized Control Trial, for Efficacy of Intramuscular Diclofenac Versus Intravenous Morphine Versus Intravenous Paracetamol, in Renal Colic Emergency Department Pain Management [NCT02187614]Phase 41,645 participants (Actual)Interventional2014-08-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of a Diclofenac Sodium Patch for the Topical Treatment of Acute Pain Due to Mild to Moderate Ankle Sprain [NCT00869180]Phase 3219 participants (Actual)Interventional2009-02-28Completed
Effect of Submucosal Cryotherapy Compared to Steroidal and Non-Steroidal Anti-Inflammatory Drugs Injection on Postoperative Endodontic Pain [NCT06090500]40 participants (Anticipated)Interventional2023-03-20Recruiting
Randomised Controlled Trial on the Efficacy of Fenugreek Wraps in Symptomatic Primary Gonarthrosis [NCT03528824]81 participants (Actual)Interventional2018-06-01Completed
To Compare Efficacy of Low Dose Diclofenac (25mg) in Management of Postoperative Pain After Periodontal Flap Surgery: A Clinical Trail. [NCT03519152]Phase 1/Phase 220 participants (Actual)Interventional2016-03-20Completed
Pilot Study to Assess the Contribution of UGT2B17 and Associated Genetic Polymorphisms on the Pharmacokinetics of Diclofenac Alone and Upon Co-administration With Curcumin [NCT06053411]Early Phase 130 participants (Anticipated)Interventional2024-01-01Not yet recruiting
A Pharmacokinetics Study Comparing Systemic Exposure of Topical Diclofenac/Menthol Gels Versus Voltaren Gel and Oral Diclofenac Sodium in Healthy Volunteers at Steady State [NCT02201238]Phase 118 participants (Actual)Interventional2014-10-01Completed
Combination of Diclofenac Potassium and Propolis in the Therapy of Oral Aphthosis [NCT05413096]Early Phase 1100 participants (Actual)Interventional2021-06-01Completed
The Effect of Preoperative Anxiety Level to Postoperative Pain and Analgesic Consumption in Patients Who Had Laparoscopic Sleeve Gastrectomy [NCT04432558]42 participants (Actual)Observational [Patient Registry]2017-04-12Completed
Tamsulosin as Adjunctive Therapy After Extracorporeal Shock Wave Lithotripsy for Renal Stones [NCT04819828]Phase 460 participants (Actual)Interventional2010-01-01Completed
The Safety and Efficacy of an Enzyme Combination in Managing Knee Osteoarthritis Pain in Adults: a Randomized, Double-blind, Placebo-controlled Trial. [NCT02088411]Phase 2150 participants (Actual)Interventional2000-11-30Completed
A Prospective Randomized Controlled Trial of Pain as Indication for Operative Treatment of Traumatic Rib Fractures. [NCT02094807]0 participants (Actual)Interventional2014-04-30Withdrawn(stopped due to Slow inclusion rate. Awaiting results from NCT02132416.)
A Randomized, Open-label, Single Dose, 3-way Crossover Study to Evaluate the Drug-drug Interaction Between Aceclofenac 200 mg and Esomeprazole 20 mg in Healthy Male Volunteers [NCT03127046]Phase 130 participants (Actual)Interventional2017-03-31Enrolling by invitation
Clinical Efficacy and Safety of Compound Methyl Salicylate Liniment in the Treatment of Acute and Chronic Soft Tissue Pain:a Multicenter, Randomized, Positive Controlled Clinical Trial [NCT03362216]216 participants (Actual)Interventional2009-04-07Completed
A Phase IV Open Label Randomized Multicenter Comparative Study Of Celecoxib Efficacy And Safety Versus Standard Doses Of Oral Diclofenac In Acute Pain Due To Cervical Sprain Related To Motor Vehicle Accident [NCT00894790]Phase 48 participants (Actual)Interventional2009-11-30Terminated(stopped due to See termination reason in detailed description.)
A Multicenter, Prospective, Randomized, Controlled Clinical Study of Ningmitai Capsule to Promote the Passage of Residual Fragments After Ureteroscopic Lithotripsy [NCT06105827]Phase 4251 participants (Actual)Interventional2016-10-02Completed
A Twelve Week, Randomized, Double Blind Parallel Group Study Of Two Doses Of Celecoxib Compared To Diclofenac In Patients With Ankylosing Spondylitis [NCT02528201]Phase 4330 participants (Actual)Interventional2002-09-30Completed
A SINGLE CENTER, MULTIPLE DOSE, OPEN-LABEL, RANDOMIZED, THREE-PERIOD CROSSOVER STUDY TO DETERMINE THE RELATIVE BIOAVAILABILITY OF DICLOFENAC IN THE TOPICAL GEL COMBINATION PRODUCT (DICLOFENAC 2% + CAPSAICIN 0.075%) COMPARED TO DICLOFENAC MONO GEL 2% AND V [NCT03074162]Phase 148 participants (Actual)Interventional2017-04-20Completed
[NCT02506348]30 participants (Anticipated)Interventional2015-07-31Recruiting
Effect of Preoperative, Single-dose Diclofenac Potassium on Postoperative Endodontic Pain in Patients With Symptomatic Irreversible Pulpitis: A Double Blind Randomized Controlled Trial [NCT03341260]Phase 2/Phase 370 participants (Actual)Interventional2016-12-31Completed
Comparison of Bupivacaine Peritoneal Infiltration and Intramuscular Diclofenac Versus Bupivacaine Peritoneal Infiltration Alone for Postoperative Pain Relief in Gynecologic Cancer Patients Undergoing Open Surgery [NCT03796403]140 participants (Actual)Interventional2019-02-15Terminated(stopped due to Diclofenac is no longer recommend for intramuscular administration by the Medical Council of Thailand)
Effectiveness of Non-steroidal Anti-inflammatory Diclofenac and Its Association to the Opioid Codeine for Pain, Swelling and Trismus in the Bilateral Mandibular Third Molar Extraction With a High Degree of Difficulty Model. [NCT02547896]Phase 450 participants (Actual)Interventional2014-09-30Completed
A Comparative Double Blind, Double Dummy, Randomized Study on the Effectiveness of Diclofenac Potassium vs. Acetaminophen in Febrile Children With Acute Upper Respiratory Tract Infections [NCT01019980]Phase 42 participants (Actual)Interventional2010-03-31Terminated(stopped due to Placebo - Active Drug Not Available. No patients received drug. There are no study results to disclose.)
Evaluation of the Effect of Different Acupuncture Dose on Premenstrual Syndrome and the Relationship Between Premenstrual Syndrome and TCM Syndrome Complex [NCT04296422]105 participants (Anticipated)Interventional2019-01-01Enrolling by invitation
Evaluation of Two Pharmacological Protocols for Pre-emptive Analgesia in Impacted Third Molar Surgery [NCT02665533]18 participants (Actual)Interventional2016-01-31Completed
An Open-Label, Multiple-Dose, Multiple-Day, Non-Randomized, Single-Arm Safety Study Of Repeat-Doses Of DIC075V (Intravenous Diclofenac Sodium) In Patients With Acute Post-Operative Pain [NCT00726388]Phase 31,050 participants (Actual)Interventional2008-09-15Completed
Diclofenac for Prevention of Post-ERC Pancreatitis [NCT03595150]Phase 2/Phase 31,000 participants (Anticipated)Interventional2024-01-01Not yet recruiting
Phase 4 Study of Efficacy of Gabapentin in the Treatment of Chest Pain and Paresthesia in Patients With Sternotomy [NCT00800527]Phase 4110 participants (Actual)Interventional2007-11-30Completed
A Multicenter, Randomized, Parallel-group, 4-Week, Double-Blind and Active Comparator-Controlled Study to Assess Efficacy, Safety, and Tolerability of Etoricoxib 60 mg Once Daily Versus Diclofenac Sodium 75 mg Twice Daily in the Treatment of Chinese Patie [NCT00140972]Phase 4160 participants (Actual)Interventional2004-12-03Completed
[NCT02545777]Phase 2120 participants (Anticipated)Interventional2014-05-31Recruiting
A Relative Bioavailability Study of Diclofenac Sodium 75 mg Enteric-Coated Tablets Under Non-Fasting Conditions [NCT00913887]Phase 118 participants (Actual)Interventional1994-04-30Completed
The Effect of Voltaren-ophtha 0.1% (Diclofenac Sodium 0.1%) Eye Drops After Cataract Surgery on INR Levels (International Normalized Ratio) in Patients Taking Warfarin [NCT02782338]100 participants (Anticipated)Observational2016-05-31Not yet recruiting
A Multicenter Randomized Controlled Trial in Elderly Patients With Hip Fractures Comparing Continuous Fascia Iliaca Compartment Block to Systemic Opioids and Its Effect on Delirium Occurrence [NCT02689024]Phase 4239 participants (Actual)Interventional2016-05-31Terminated(stopped due to recruitment too slow; intervention was standard care in patients who were not included; acute care pathways changed due to policy regarding hip fracture patients)
Evaluation of the Effect of a Vaginal Ring With Meloxicam on Primary Dysmenorrhea in Women of Childbearing Age [NCT02255045]Phase 2/Phase 368 participants (Actual)Interventional2014-06-27Completed
Relative Bioavailability of Dabigatran and Diclofenac After 150 mg b.i.d. Dabigatran Etexilate and Diclofenac at 50 mg Single Dose Alone or Following Concomitant Multiple Oral Administrations in Healthy Male and Female Volunteers (an Open Label, Randomise [NCT02171507]Phase 124 participants (Actual)Interventional2006-05-31Completed
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
Randomised Controlled Trial on the Efficacy of Cabbage Leaf Wraps in Symptomatic Primary Osteoarthritis of the Knee [NCT02027792]81 participants (Actual)Interventional2014-01-31Completed
Effect of Non-steroid Anti-inflammatory Drug on Travoprost-induced Conjunctival Hyperemia and Intraocular Pressure Reduction in Normal Eyes [NCT02136589]Phase 440 participants (Actual)Interventional2008-09-30Completed
Topical Voltaren as an Alternative Treatment for Otitis Externa [NCT00523120]Phase 220 participants (Actual)Interventional2008-09-30Terminated
Treatment of Knee Pain With Topical Diclofenac Cream 8% or Diclofenac Gel 1% [NCT02068859]Phase 3106 participants (Anticipated)Interventional2014-01-31Recruiting
Long-term Effects of Aldara® 5% Cream and Solaraze® 3% Gel in the Treatment of Actinic Keratoses on the Face or Scalp With Respect to the Risk of Progression to In-situ and Invasive Squamous Cell Carcinoma [NCT01453179]Phase 4221 participants (Actual)Interventional2011-10-31Completed
Comparative Study Between the Effect of Diclofanic and Ketorolac in Post Tonsillectomy Pain Management [NCT03178539]Phase 2/Phase 3100 participants (Actual)Interventional2017-01-31Completed
Efficacy of Pain Control Following Root Canal Treatment Using Paracetamol Alone and in Combination With Three Different Non-Steroidal Anti-Inflammatory Analgesics [NCT02417337]Phase 2170 participants (Actual)Interventional2012-08-31Completed
PROUD Study - Preventing Opioid Use Disorders [NCT04766996]Phase 457 participants (Actual)Interventional2021-05-17Terminated(stopped due to Loss of surgery team member deemed the study procedures impossible to achieve, and no replacement could be found in a timely manner to complete trial as initially planned.)
Safety Study to Investigate the Skin Sensitization Potential of MFC51123 [NCT02192203]Phase 1227 participants (Actual)Interventional2014-04-01Completed
Effects of NSAIDs on RAdiographic Damage in Ankylosing Spondylitis (ENRADAS) - a Prospective Randomised Controlled Trial [NCT00715091]Phase 4180 participants (Actual)Interventional2008-09-30Completed
Sustained Acoustic Medicine (SAM) for Symptomatic Treatment of Pain Related to Bone Fracture [NCT05883241]Phase 190 participants (Anticipated)Interventional2023-06-01Recruiting
Sustained Acoustic Medicine for Knee Osteoarthritis Pain [NCT05254574]Phase 130 participants (Actual)Interventional2022-02-14Completed
Comparative Usability Evaluation of Sustained Acoustic Medicine (SAM) Devices and Topical Gel for Knee Pain Related to Osteoarthritis [NCT05050448]Phase 1/Phase 260 participants (Actual)Interventional2021-08-01Completed
Multicenter Study to Evaluate the Analgesic Efficacy of XP21L in Subjects With Pain Following Bunionectomy Surgery [NCT00375934]Phase 3200 participants (Actual)Interventional2006-09-30Completed
Oral Tramadol Versus Diclofenac For Pain Relief Before Outpatient Hysteroscopy: A Randomized Controlled Trial [NCT02760888]Phase 3102 participants (Anticipated)Interventional2016-05-31Not yet recruiting
Multicenter, Open-Label Study to Assess the Effectiveness and Safety of FLECTOR Patch for Treatment of Acute Back Strain [NCT01054820]Phase 4123 participants (Actual)Interventional2010-01-31Completed
Platelet Rich Plasma Injection Versus Surgical and Medical Treatment of Mild-moderate Carpel Tunnel Syndrome. [NCT04235426]Phase 190 participants (Actual)Interventional2018-01-26Active, not recruiting
The Effectiveness of Moxibustion Treatment for Osteoarthritis of the Knee : a Double-blinded, Double-dummy, Randomized Controlled Trial [NCT02769572]Phase 3144 participants (Actual)Interventional2016-05-31Completed
A 12-Week Symptomatic Effect Evaluation to Compare Celecoxib 200 mg QD, Celecoxib 200 mg BID and Diclofenac 75 mg SR BID in Patients With Ankylosing Spondylitis [NCT00648141]Phase 3458 participants (Actual)Interventional2003-01-31Completed
Randomized Clinical Trial of Oral Diclofenac Potassium With Cervical Lidocaine Cream in Reducing Pain During HSG [NCT02709590]Phase 3140 participants (Actual)Interventional2016-03-31Completed
Effect of Opioids and NSAIDs on Sympathetic Nervous System and Vascular Function in Healthy Subjects and Patients With Osteoarthritis [NCT03781544]Phase 490 participants (Anticipated)Interventional2019-01-01Recruiting
Pharmacological Intervention Against Diabetic Retinal Flow Disturbances. [NCT00619034]87 participants (Actual)Interventional2007-09-30Completed
A Multicentre, Double-Blind, Double-Dummy, Randomised Study of the Analgesic Efficacy and Safety of Valdecoxib Compared to Diclofenac Sodium in Patients Undergoing Knee Arthroscopy Procedure for Anterior Cruciate Ligament Reconstruction [NCT00650598]Phase 4328 participants (Actual)Interventional2004-03-31Completed
Effect of Dexmedetomidine Infusion on Desflurane Consumption and Hemodynamics During BIS Guided Laparoscopic Surgery: A Randomized Controlled Study [NCT02652312]40 participants (Actual)Interventional2016-02-29Completed
Phase IIB Study to Evaluate the Safety and Efficacy of Topical Difluoromethylornithine and Topical Diclofenac in the Treatment of Sun-Damaged Skin on the Forearm [NCT00601640]Phase 2184 participants (Actual)Interventional2007-01-31Completed
IM Ketorolac vs Diclofenac Potassium Powder for Oral Solution (Cambia) for the Acute Treatment of Severe Migraine [NCT02664116]Phase 440 participants (Anticipated)Interventional2016-01-31Recruiting
Randomized, Double Blind, Multicenter Study of the Safety and Efficacy of Valdecoxib 40 mg Once Daily vs. Diclofenac 75 mg Twice Daily in Subjects With Acute Low Back Pain [NCT00649610]Phase 4340 participants (Actual)Interventional2002-11-30Completed
A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of a Diclofenac Sodium Patch for the Topical Treatment of Acute Pain Due to Mild to Moderate Wrist Sprain, Strain or Contusion [NCT00869063]Phase 3214 participants (Actual)Interventional2009-02-28Completed
Intra-nasal Ketorolac Versus Oral Diclofenac for Acute Ureteral Stent-associated Pain Following Ureteroscopy for Stone Disease [NCT06158620]Phase 1/Phase 280 participants (Anticipated)Interventional2024-02-01Not yet recruiting
Comparison of Topical 1% Diclofenac and Topical 2.5% Hydrocortisone for TMJ Arthralgia [NCT05816226]Phase 390 participants (Anticipated)Interventional2023-06-01Recruiting
Open, Randomized, Controlled Clinical Trial of Lornoxicam as Compared to Diclofenac in Osteoarthritis of Knee Joint in Patients of Tertiary Care Hospital of Gujarat. [NCT01055470]40 participants (Actual)Interventional2008-12-31Completed
Battlefield Acupuncture for Acute/Subacute Back Pain in the Emergency Department [NCT03996564]26 participants (Actual)Interventional2016-02-22Completed
Symptomatic Therapy of Uncomplicated Lower Urinary Tract Infections in the Ambulatory Setting. A Randomized, Double Blind Trial [NCT01039545]Phase 4253 participants (Actual)Interventional2012-02-29Terminated(stopped due to New power calculation (reduction of necessary patient number))
A Randomized Double-blinded Trial Comparing the Clinical Efficacy and Pharmacokinetic Parameters of Oral Diclofenac and Intramuscular Diclofenac in Patients With Acute Limb Injuries [NCT03472339]Phase 4300 participants (Anticipated)Interventional2018-01-15Recruiting
The Efficacy and Safety of Administration of the COX-2 Selective NSAID, Etoricoxib (120mg od. for 7 Days) Compared to Diclofenac (50 mg Tds. for 7 Days) and Placebo as Adjunct Treatment in the First 7 Days of Treatment of Acute Grade II Lateral Ankle Liga [NCT00954785]Phase 40 participants (Actual)Interventional2009-11-30Withdrawn(stopped due to The study was terminated by Merck USA. The company did not supply drugs for the study.)
Randomized, Double-Blind, Active-and Placebo-Controlled Study of the Analgesic Efficacy and Safety of Repeated Dosing of DIC075V Versus Parenteral Ketorolac and Placebo in Acute Post-Operative Pain After Elective Orthopedic Surgery [NCT00507026]Phase 3277 participants (Actual)Interventional2007-07-25Completed
6-Month, Randomized, Double-blind, Parallel-group, Controlled, Multi-center Study of Gastric Ulcer Incidence With PN400 (Esomeprazole/Naproxen) Versus Diclofenac/Misoprostol in Subjects at High Risk for Developing NSAID-Associated Ulcers [NCT00594854]Phase 320 participants (Actual)Interventional2007-09-30Terminated(stopped due to POZEN agreed with FDA to stop study due to low and inadequate enrollment)
A Relative Bioavailability Study of Diclofenac Sodium 50 mg Enteric-Coated Tablets [NCT00913224]Phase 138 participants (Actual)Interventional1993-04-30Completed
Efficacy of Preprocedural Diclofenac in Males Undergoing Double J Stent Removal Under Local Anesthesia [NCT02598102]Phase 2150 participants (Actual)Interventional2015-04-30Completed
A Study to Evaluate the Clinical Benefits of Tramadol/Acetaminophen (Ultracet®) vs. Diclofenac (Voltaren®) in the Treatment of Pain in Patients With Ankylosing Spondylitis Receiving Stable Treatment of Disease Modifying Anti-rheumatic Drugs (DMARDs) [NCT00766402]Phase 48 participants (Actual)Interventional2008-10-31Terminated
A Randomised Multi-centre Feasibility Study Investigating Post-operative Pain Following Single-port or Multi-port Video Assisted Thoracoscopic Surgical (VATS) Procedures [NCT02556970]0 participants (Actual)InterventionalWithdrawn(stopped due to Study never started and was abandoned.)
Comparison of Photobiomodulation Therapy and Sonophoresis in Improving Tempomandibular Joint Mobility and Quality of Life Among Head and Neck Cancer Survivors (PBMT-S Trial): A Triple-Blind, Randomized Controlled Trial. [NCT04082793]48 participants (Anticipated)Interventional2020-06-01Not yet recruiting
"NSAIDs in Acute Achilles Tendinopathy: Effect on Pain Control, Leg Stiffness and Functional Recovery in Athletes" [NCT00792376]Phase 456 participants (Actual)Interventional2009-08-31Completed
A Relative Bioavailability Study of Diclofenac Sodium 50 mg Enteric-Coated Tablets Under Non-Fasting Conditions [NCT00914160]Phase 118 participants (Actual)Interventional1993-08-31Completed
Effectiveness of Chiropractic Application in Patients With Acute Low Back Pain Presenting to the Emergency Department and Receiving Drug Treatment [NCT04110119]Phase 298 participants (Actual)Interventional2018-10-01Completed
A Randomized, Double-Blind, Vehicle-Controlled, Single Center, Intra-Individual Comparative Study of the Efficacy and Safety of Diclofenac Sodium 1 mg/g (0.1%) Gel in Subjects With Painful UV-Induced Erythema [NCT00441051]Phase 345 participants Interventional2006-11-30Completed
An Open-Label, Single-Dose Study to Evaluate the Safety and Pharmacokinetics of DIC075V in Subjects With Mild or Moderate Chronic Renal Insufficiency and in Subjects With Mild Chronic Hepatic Impairment Compared to Healthy Adult Volunteers and a Randomize [NCT00805090]Phase 137 participants (Actual)Interventional2008-12-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of a Diclofenac Sodium Patch for the Topical Treatment of Pain Due to Mild to Moderate Tendonitis or Bursitis [NCT00640939]Phase 2/Phase 3308 participants (Actual)Interventional2007-12-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of a Diclofenac Sodium Patch for the Topical Treatment of Pain Due to Mild to Moderate Ankle Sprain. [NCT00640705]Phase 2/Phase 3170 participants (Actual)Interventional2008-01-31Terminated(stopped due to Sponsor decision)
A Cyclic Regimen of Diclofenac Potassium May be Efficacious in the Management of Chronic Periodontitis in Adults [NCT02658799]Phase 249 participants (Actual)Interventional2000-01-31Completed
Open Label Study to Assess the Efficacy and Safety of Meloxicam 7.5mg vs. Diclofenac 100mg SR in Patients With Osteoarthritis of the Knee [NCT02183129]Phase 491 participants (Actual)Interventional1999-04-01Completed
Analgesic Effect of Topical and Oral Diclofenac on Pain Related to Intravitreal Injections, a Randomized, Triple-arm, Double-blind, Placebo-controlled Study. [NCT02837770]76 participants (Actual)Interventional2016-07-31Completed
The Comparison Between the Therapeutic Affect of Intravitreal Diclophenac and Triamcinolone in Persistent Uveitic Cystoids Macular Edema [NCT00893854]Phase 10 participants InterventionalRecruiting
A PHASE 3, RANDOMIZED, DOUBLE BLIND, CONTROLLED, MULTI CENTER STUDY OF THE ANALGESIC EFFICACY AND SAFETY OF TANEZUMAB ADDED ON TO DICLOFENAC SR IN PATIENTS WITH OSTEOARTHRITIS OF THE KNEE OR HIP [NCT00864097]Phase 3607 participants (Actual)Interventional2009-08-11Terminated(stopped due to See termination reason in detailed description.)
A Pharmacoscintigraphic Clinical Study to Investigate the in Vivo Behaviour of a Novel Delayed-release Formulation of Diclofenac in Comparison to the Voltaren® Enteric Coated Tablet Commercial Formulation in Healthy Volunteers [NCT02714842]Phase 136 participants (Actual)Interventional2016-03-31Completed
A Randomized, Double Blind, Three-arm, Parallel, Placebocontrolled, Clinical Study to Evaluate the Bioequivalence Using Clinical Endpoint of Diclofenac Sodium Gel, 1% (Mylan Inc.) to Voltaren® Gel (Diclofenac Sodium Topical Gel) 1% (Novartis Consumer Heal [NCT03172780]Phase 31,220 participants (Actual)Interventional2017-05-24Completed
Comparison of the Use of Dexamethasone and Diclofenac Sodium in Immediate Post-Operative Care in Third Molar Surgery [NCT02698306]30 participants (Anticipated)Interventional2015-02-28Recruiting
A Multicenter, Randomized, Double-Blind, Double-Dummy Study Of The Safety, Tolerability And Efficacy Of Celecoxib 200 Mg Twice A Day (With A 400 Mg Attack Dose) Versus Sodium Diclofenac 75 Mg Twice A Day In Subjects With Acute Low Back Pain [NCT00640432]Phase 4244 participants (Actual)Interventional2003-10-31Completed
Open-Label, Randomized, Single-Dose, Four-Treatment Crossover Study to Evaluate Platelet Function in Healthy Adult Males After Administration of IV Diclofenac Sodium, Oral Diclofenac Potasssium, IV Ketorolac Tromethamine, and Acetylsalicylic Acid [NCT00548678]Phase 130 participants (Actual)Interventional2007-10-31Completed
Effect of Diclofenac Potassium Versus Prednisolone as a Premedication on Post-endodontic Pain and Pulpal Interleukin (IL)-8 Expression in Symptomatic Irreversible Pulpitis Cases: A Randomized Clinical Trial [NCT04608981]Phase 436 participants (Anticipated)Interventional2021-03-31Not yet recruiting
A Double Blind, Double Dummy, Multicenter, Randomized, Placebo- and Active-controlled Clinical Trial to Evaluate Effectiveness of Tricortin 1000 in Patients Affected by Chronic Low Back Pain [NCT04585334]Phase 4300 participants (Anticipated)Interventional2019-03-25Recruiting
A 12-Week, Randomized, Double-blind, Placebo-controlled, Parallel-group Phase 3 Study to Evaluate the Efficacy and Safety of HP-5000 Topical System (Patch) in Subjects With Osteoarthritis Pain of the Knee [NCT04683627]Phase 3370 participants (Actual)Interventional2020-12-29Completed
Sterile Water Injections as a Complementary Method for Relieving Ureterolithiasis Pain- a Randomized Controlled Trial [NCT01412840]0 participants (Actual)Interventional2014-01-31Withdrawn
The Analgesic Efficacy of Continuous Wound Instillation With Diclofenac or Ropivacaine Following Cesarean Section: a Randomized, Double-blind, Placebo Controlled Study [NCT00801528]Phase 475 participants (Anticipated)Interventional2008-04-30Completed
A Randomized, Double-Blind, Parallel-Group, Vehicle-Controlled, Multicenter Study Comparing Diclofenac Sodium Gel, 3% to Solaraze® Gel, 3% in the Treatment of Actinic Keratosis on the Face or Bald Scalp [NCT02611804]Phase 3492 participants (Actual)Interventional2015-10-31Completed
A Randomized, Double-Blind, Multicenter Study to Evaluate the Tolerability and Effectiveness of Etoricoxib 90 mg q.d. vs. Diclofenac Sodium 75 mg b.i.d. in Patients With Rheumatoid Arthritis [NCT00092742]Phase 34,086 participants (Actual)Interventional2003-02-28Completed
Surgical Wound Infiltration With Sodium Diclofenac Versus Bupivacaine in the Treatment of Acute Postoperative Pain Following Appendectomy [NCT02752971]Phase 343 participants (Actual)Interventional2015-02-28Completed
A Randomized, Placebo-controlled, Double-blind, Phase II Chemoprevention Clinical Trial of Topical Diclofenac and DFMO in Subjects With a History of Skin Cancer [NCT04091022]Phase 2138 participants (Anticipated)Interventional2021-01-18Active, not recruiting
A Non-blinded, Non-placebo Controlled, Compassionate Use, Open Treatment, Open-ended Program of the Safety of Pennsaid Topical Lotion (Diclofenac) in the Treatment of Osteo or Rheumatoid Arthritis [NCT01579890]0 participants Expanded AccessApproved for marketing
Evaluation the Effect of Diclofenac Drops vs Dexamethasone Drops in Trabeculectomy and Cataract Surgery [NCT00825864]50 participants (Anticipated)Interventional2004-01-31Completed
Supersaturation and Precipitation of Diclofenac in the Stomach of Healthy Volunteers [NCT02007161]10 participants (Anticipated)Interventional2013-12-31Not yet recruiting
A Randomized, Double-blind, Multi-center, Vehicle-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Diethylamine 2.32% Gel Applied Once or Twice Daily in Patients With Acute Ankle Sprain [NCT00573768]Phase 2271 participants (Actual)Interventional2007-11-30Completed
Efficacy and Safety of Diclofenac Sodium Gel in Knee Osteoarthritis [NCT00171678]Phase 3480 participants Interventional2004-10-31Completed
The Effect of Intracervical Lidocaine Versus Intramuscular Diclofenac for Pain Relief During Hysterosalpingography Among Infertile Women In A Tertiary Hospital In Kano: A Randomized Controlled Trial [NCT02918812]Phase 4140 participants (Anticipated)Interventional2016-09-30Recruiting
[NCT00536068]11 participants (Actual)Interventional2006-08-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of a Diclofenac Sodium Patch for the Topical Treatment of Acute Pain Due to Mild to Moderate Soft Tissue Injuries [NCT00931866]Phase 3407 participants (Actual)Interventional2009-04-30Completed
The Efficacy and Safety of TDS-943 in the Treatment of Osteoarthritis of the Knee: Pivotal Study II [NCT00546832]Phase 3650 participants (Actual)Interventional2007-10-31Completed
[NCT00999791]Phase 10 participants Interventional2009-07-31Recruiting
Collagen Crosslinking With Ultraviolet-A in Asymmetric Corneas [NCT01024322]1,189 participants (Actual)Observational2009-10-01Terminated(stopped due to Terminated to initiate FDA IND-cleared study protocol)
Multicenter Study to Evaluate the Analgesic Efficacy of XP21L in Subjects With Pain Following Bunionectomy Surgery [NCT00366444]Phase 3201 participants (Actual)Interventional2006-08-31Completed
A Randomized, Placebo-Controlled, Double-Blind, Multicenter, Parallel-Group, 12-Week Study to Assess the Clinically Effective Dose Range of Etoricoxib and to Assess Its Safety and Tolerability in Patients With Rheumatoid Arthritis [NCT00264147]Phase 2761 participants (Actual)Interventional2006-01-31Completed
Randomized,Fully-replicated,Single Oral Dose,Open-label,Crossover BE Study to Compare Diclofenac Potassium Coated Tablet (50 mg Diclofenac Potassium) Versus Cataflam® 50 Coated Tablet (50 mg Diclofenac Potassium) in Healthy Subjects in Fasting State [NCT05082662]Phase 1/Phase 236 participants (Actual)Interventional2020-08-25Completed
Comparison of the Effect of Etoricoxib and Diclofenac on Early Morning Activity in Rheumatoid Arthritis. [NCT01067430]Phase 40 participants (Actual)Interventional2010-04-30Withdrawn
Evaluation of CYP4A11 and CYP4F2 Gene Variants as Makers in Edema and Elevated Blood Pressure Occurrence After Nonsteroidal Anti-inflammatory (NSAID) Use [NCT02779530]Phase 420 participants (Actual)Interventional2011-10-31Completed
A Randomized, Open-Label, Single-dosing and Cross-over Clinical Trial to Investigate the Safety and Pharmacokinetic Drug-Drug Interaction of YH4808 and Diclofenac in Healthy Male Volunteers [NCT01876615]Phase 149 participants (Actual)Interventional2013-07-31Completed
Preoperatively Administered Single Dose Diclofenac Reduces the Intensity of Acute Postcraniotomy Headache and Decreases Postoperative Analgesic Requirements- a Randomized, Controlled Trial [NCT01907984]Phase 4200 participants (Actual)Interventional2012-12-31Completed
Prospective, Controlled and Monocentric Study to Evaluate the Effects of Topical 3% Diclofenac in 2.5% Hyaluronic Acid Gel on Tumor Metabolism in the Treatment of Actinic Keratoses in Immunocompetent and Immunocompromised Patients [NCT01935531]Phase 438 participants (Actual)Interventional2013-06-30Completed
Comparison of the Efficacy and Tolerability of Solaraze for 3 vs. 6 Months in Patients With Mild to Moderate Actinic Keratosis Located at the Face and Head [NCT00204542]Phase 4418 participants (Actual)Interventional2005-06-30Completed
Diclofenac Suppository As a Preemptive Analgesia in Ultrasound Guided Biopsy of Prostate: Randomized Controlled Trial [NCT01939743]Phase 2100 participants (Actual)Interventional2011-10-31Completed
Double-blinded Multicenter Randomized Clinical Trial to Evaluate the Efficacy and Safety of CLIFE1 and CLIFE2 Gels in Benign Anorectal Surgery [NCT02961855]Phase 4120 participants (Actual)Interventional2011-01-31Completed
Intramuscular Diclofenac vs. Placebo in a Randomized Double Blind Controlled Trial, In Post ERCP Pancreatitis. [NCT01946984]Phase 1182 participants (Actual)Interventional2012-06-30Completed
The Effect of Diclofenac Potassium Insitu Gel Versus Calcium Hydroxide as Intra-canal Medications on Post-operative Pain and Anti-bacterial Effect in Lower Non Vital Premolars With Symptomatic Apical Periodontitis [NCT04622488]44 participants (Anticipated)Interventional2020-11-30Not yet recruiting
A Multicenter Single-Blind, Single Dose Efficacy and Safety Pilot Study Comparing Intramuscular Parecoxib and Diclofenac in Renal Colic [NCT00139646]Phase 350 participants Interventional2002-04-30Terminated(stopped due to See Detailed Description)
Efficacy of Preoperative Diclofenac Potassium- Acetaminophen Combination on Anesthetic Success in Patients With Symptomatic Irreversible Pulpitis: a Randomized Controlled Trial [NCT04593160]72 participants (Anticipated)Interventional2021-01-31Not yet recruiting
Efficacy and Safety of Sahastara Remedy Extract Capsules in Treating Primary Osteoarthritis of the Knee Compared With Diclofenac (Clinical Trial Phase II) [NCT04591795]Phase 280 participants (Anticipated)Interventional2018-01-01Recruiting
Evaluation of Trans-mucosal Bio-adhesive Discs of Diclofenac Potassium on the Anesthetic Success and Postoperative Pain in Patients With Symptomatic Irreversible Pulpitis: A Randomized Clinical Trial [NCT04585438]Phase 448 participants (Anticipated)Interventional2021-09-21Not yet recruiting
Comparative Bioavailability and Local Tolerability of Two Topical Diclofenac Plasters Applied Once and Twice a Day to Healthy Volunteers With a Repeat Dose Regimen [NCT04585321]Phase 152 participants (Actual)Interventional2017-11-28Completed
A Pilot Pharmacoscintigraphic Clinical Study to Investigate the Behaviour of Delayed-release Tablets Consisting of a Diclofenac Potassium Core Coated With Barrier Granules, in Healthy Volunteers [NCT02004301]Phase 112 participants (Actual)Interventional2014-01-31Completed
A Phase 1, Single-Center, Randomized, Open-Label, Bioavailability and Safety Three Period Crossover Multiple-Dose Study Comparing Two Dose Levels of AMZ001 (Diclofenac Sodium Gel 3.06%) and One Dose Level of Diclofenac Sodium 1% Gel in Healthy Subjects [NCT05968482]Phase 175 participants (Anticipated)Interventional2023-07-11Recruiting
A Randomized, Double-Blind, Multicenter Study to Evaluate the Tolerability and Effectiveness of Etoricoxib 90 mg q.d. vs. Diclofenac Sodium 50 mg t.i.d. in Patients With Osteoarthritis [NCT00092703]Phase 36,000 participants Interventional2002-06-27Completed
Antipyretics for Preventing Recurrences of Febrile Seizures [NCT00568217]Phase 4231 participants (Actual)Interventional1997-09-30Completed
A Phase 2, Randomized, Double-Blind, Vehicle-Controlled, Parallel Group Clinical Study to Evaluate the Safety and Efficacy of PENNSAID Gel in the Symptomatic Treatment of Osteoarthritis of the Knee [NCT01119898]Phase 2260 participants (Actual)Interventional2010-08-02Completed
Treatment of Renal Colic in the Emergency Department: Comparison Between Magnesium Sulfate and Lidocaine. A Double-blind, Randomised Controlled Trial. [NCT05653401]Phase 2800 participants (Actual)Interventional2022-11-20Completed
Comparison of Commonly Used Treatment Approaches in the Treatment of Gonarthrosis: Platelet-Rich Plasma, Topical Diclofenac, and Exercise [NCT05877027]84 participants (Anticipated)Interventional2024-01-31Not yet recruiting
Randomized, Double Blind, Parallel-groups, Non-inferiority Versus Flector® and Superiority Versus Placebo, Phase III Clinical Trial With Diclofenac Sodium 140 mg Medicated Plaster in Patients With Impact Injuries of the Limbs [NCT04976088]Phase 3214 participants (Actual)Interventional2018-05-25Completed
A Randomized, Open-label, Single Dose, Two-Treatment, Two Period Crossover Design (2x2), Comparative Bioequivalence Study of Deflox® Tablets 50 mg vs Cataflam DD ® Tablets 50 mg (Innovator) in Healthy Volunteers [NCT04132583]Phase 116 participants (Actual)Interventional2019-09-21Completed
Randomized Clinical Trial of Oral Hyoscine Butyl Bromide Versus Diclofenac Potassium in Reducing Pain During Office Hysteroscopy [NCT02714699]Phase 2/Phase 3129 participants (Actual)Interventional2016-10-31Completed
A Randomized Controlled Trial of 2 Different Methods for Pain Relief During Intrauterine Device Insertion [NCT02714231]Phase 4100 participants (Actual)Interventional2016-03-31Completed
Analgesic Effectiveness of Potassium Diclofenac for Retinal Photocoagulation in Patients With High-risk Proliferative Diabetic Retinopathy [NCT01009021]30 participants (Actual)Interventional2008-03-31Completed
Effects of Addition of Systemic Tramadol or Adjunct Tramadol to Lidocaine Used for Intravenous Regional Anesthesia in Patients Undergoing Hand Surgery [NCT02658721]Phase 360 participants (Actual)Interventional2013-01-31Completed
The Effect of Kinesio Taping Application for Dysmenorrhea: A Randomized Controlled Clinical Trial [NCT02663050]150 participants (Anticipated)Interventional2016-02-29Not yet recruiting
A Multi-Center, Randomized, Double-Blind, Parallel Group Study To Compare The Efficacy And Tolerability Of Valdecoxib Vs. Diclofenac In Ankle Sprain [NCT00671320]Phase 4202 participants (Actual)Interventional2002-12-31Completed
Diclofenac Gel in the Treatment of Cervicogenic Headache: A Randomized, Double-Blind, Controlled Trial [NCT05312645]Phase 350 participants (Anticipated)Interventional2024-01-31Recruiting
Comparison of the Effects on Renal Function of Lumiracoxib and Diclofenac in Patients With Chronic Kidney Failure K/DOQI Stage III at the HCSAE PEMEX [NCT01481610]Phase 228 participants (Actual)Interventional2012-01-31Terminated(stopped due to Interim analysis shows harma to one of the study arms.)
"Antiinflammatoriska läkemedels Effekt för Att Minska Suicidalitet Hos Deprimerade Patienter Som Nyligen Har Gjort självmordsförsök" [NCT01413854]Phase 1/Phase 20 participants (Actual)Interventional2011-08-31Withdrawn(stopped due to Not enough recources.)
NSAID With IV-PCA Morphine is an Alternative to Thoracic Epidural Analgesia in Post-thoracotomy Pain [NCT01541137]30 participants (Actual)Interventional2004-03-31Completed
Efficacy and Safety of Diclofenac Sodium Gel in Knee Osteoarthritis [NCT00171626]Phase 3480 participants Interventional2004-08-31Completed
Efficacy and Safety of Diclofenac Sodium Gel in Hand Osteoarthritis [NCT00171665]Phase 3360 participants Interventional2005-05-31Completed
Evaluating Acupuncture in the Treatment of Low Back Pain in Athletes and the Relationship With the Catecholaminergic Pathway [NCT02876432]30 participants (Actual)Interventional2016-10-31Completed
A 6-Week, Randomized, Double-Blind, Parallel-Group Study To Evaluate The Symptomatic Effects And Safety Of Celecoxib 200mg QD Compared To Diclofenac 75mg SR QD In Chinese Patients With Ankylosing Spondylitis, With 6-Week Extension Phase Treatment On Celec [NCT00762463]Phase 3240 participants (Actual)Interventional2009-07-31Completed
Efficiency and Safety a Fixed Combination of Orphenadrine and Diclofenac for Postoperative Analgesia in Cardiac Surgery Patients [NCT05322603]60 participants (Actual)Interventional2022-03-18Completed
A Comparative Double-Blinded Randomized Study: Clinical Safety and Efficacy of Sahasthara Microemulsion Versus Diclofenac Microemulsion for Treating Primary Knee Osteoarthritis [NCT06184685]Phase 287 participants (Actual)Interventional2021-10-20Completed
Efficacy and Safety of Diclofenac Sodium Gel in Hand Osteoarthritis [NCT00171652]Phase 3360 participants Interventional2005-05-31Completed
A Phase 4, Open-Label Study of the Pharmacokinetics and Safety of Diclofenac Potassium Oral Solution in Pediatric Subjects (Ages 2-12 Years) With Mild to Moderate Acute Pain [NCT02287350]Phase 451 participants (Actual)Interventional2014-09-30Completed
An Open-Label, Single-Dose Study to Assess the Effects of Age, Weight, and Body Composition on the Pharmacokinetic Profile, Safety, and Tolerability of Intravenous Diclofenac Sodium (DIC075V) in Adult Volunteers [NCT00509743]Phase 189 participants (Anticipated)Interventional2007-09-30Completed
Retinal Optical Coherence Tomography and Multifocal Electroretinogram; Establishing Normal Ranges Related to Age and Reproductive Factors; With the Use of Anti-inflammatory Medications;In Uncomplicated Anterior Uveitis; Anatomy and Function. [NCT00476593]218 participants (Actual)Interventional2005-09-30Completed
Relation Between Reduction of the Inflammatory Status and Glucose Metabolism in Healthy Overweight Men [NCT00221052]20 participants Interventional2005-06-30Completed
Comparative Evaluation of the Effectiveness of Diclofenac Sodium Versus Vitamin D Supplements on Symptoms in Individuals With Myofascial Pain and Vitamin D Deficiency [NCT06111573]Phase 440 participants (Actual)Interventional2022-06-01Completed
Comparison of Intrathecal Levobupivacaine Combined With Sufentanil, Fentanyl, or Placebo for Elective Caesarean Section: A Prospective, Randomized, Double-blind, Controlled Study [NCT01858090]Phase 393 participants (Actual)Interventional2009-01-31Completed
EFFECTS OF NSAIDs ON CLINICAL OUTCOMES, SYNOVIAL FLUID CYTOKINE CONCENTRATION AND SIGNAL TRANSDUCTION PATHWAYS IN KNEE OSTEOARTHRITIS [NCT01860833]Phase 490 participants (Actual)Interventional2010-04-30Completed
The Efficacy and Safety of TDS-943 in the Treatment of Osteoarthritis of the Knee: Pivotal Study I [NCT00546507]Phase 3650 participants (Actual)Interventional2007-10-31Completed
Incidence Of Hemidiaphragmatic Paralysis With Patient Controlled Infusion Of Low Volume Of Ropivacaine After Usg Guided Low Dose Interscalene Brachial Plexus Block [NCT03081728]56 participants (Actual)Interventional2017-04-01Completed
Phase 4 Study A Large Streamline Safety Study Designed to Compare the Cardiovascular Safety od Celecoxib Versus Traditional Non-selective NSAID's [NCT00447759]Phase 47,297 participants (Actual)Interventional2007-06-30Completed
Randomized, Double-Blind, Active- and Placebo-Controlled Study of the Efficacy and Safety of Repeated Dosing of DIC075V Relative To Parenteral Ketorolac and Placebo in Patients With Acute Post-Op Pain After Abdominal or Pelvic Surgery [NCT00448110]Phase 3331 participants (Actual)Interventional2006-05-31Completed
Double-blind Randomized Clinical Study on Topical Diclofenac Efficacy in Symptomatic Relief of Temporomandibular Degenerative Joint Disease in Women. [NCT00471393]28 participants (Actual)Interventional2006-05-31Completed
Normothermia in Patients With Acute Cerebral Damage [NCT00491192]Phase 40 participants Interventional2007-06-30Recruiting
Comparative Effectiveness of Acupuncture and Nonsteroidal Anti-inflammatory Drugs for the Management of Aromatase Inhibitor Induced Arthralgia Among Breast Cancer Survivors [NCT04511832]54 participants (Actual)Interventional2018-03-28Completed
Safety of Diclofenac Sodium Gel in Knee Osteoarthritis [NCT00171691]Phase 3450 participants Interventional2004-10-31Completed
A Prospective, Open, Multi-Centre Photopatch Test Study of Patients Suspected of Photoallergy to Organic Sunscreens and Topical Nonsteroidal Anti-inflammatory Drugs Used Within Europe. [NCT00530387]1,000 participants (Actual)Interventional2008-07-31Completed
[NCT00595543]Phase 4166 participants (Anticipated)Interventional2008-01-31Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Sodium Topical Gel (DSG) 1% Applied 4 Times Daily in Subjects With Acute Ankle Sprain [NCT01255423]Phase 3206 participants (Actual)Interventional2010-11-30Completed
Study to Evaluate Arthroplasty Specimens in the Phase 3 Fasinumab Program for Osteoarthritis of the Knee and Hip [NCT03949673]Phase 223 participants (Actual)Interventional2019-04-08Terminated(stopped due to Lack of enrollment)
Synergistic Effect Of Parenteral Diclofenac And Paracetamol In The Pain Management Of Acute Limb Injuries [NCT04199572]Phase 4162 participants (Actual)Interventional2022-10-16Completed
Intravenous Magnesium Sulfate Combined to Diclofenac Versus Intravenous Lidocaine Combined to Diclofenac Versus Diclofenac Alone in the ED Treatment of Renal Colic. A Randomized Double Blind Study. [NCT03199924]Phase 2600 participants (Actual)Interventional2016-07-01Completed
A Randomized, Controlled, Multi-center Study on the Effectiveness of Traumeel S (Both Ointment and Gel) in Terms of Pain and Function Compared With a Topical NSAID in Athletes With Acute Ankle Sprain [NCT01066520]Phase 3449 participants (Actual)Interventional2009-08-31Completed
A Phase 4, Multi-centre, Randomized, Evaluator-blinded, Active-controlled Study to Determine the Incidence of Squamous Cell Carcinoma and Evaluate the Long-term Safety of Tirbanibulin 10 mg/g Ointment and Diclofenac Sodium 3% Gel for the Treatment of Adul [NCT05387525]Phase 4540 participants (Anticipated)Interventional2022-10-24Recruiting
A Phase 1, Multi-site, Randomized, Placebo-Controlled, Double-Blind Study to Evaluate the Pharmacokinetics, Safety and Preliminary Efficacy of Two Strengths of DARE-PDM1 (1% or 3%) Versus Placebo Among Women With Symptomatic Primary Dysmenorrhea [NCT05752526]Phase 136 participants (Anticipated)Interventional2023-05-19Active, not recruiting
A Randomized, Double-Blind, Placebo- and Active-Comparator-Controlled, Parallel-Group Study of Rofecoxib and Diclofenac Sodium in the Treatment of Post-Bunionectomy Surgery Pain [NCT00092378]Phase 3251 participants (Actual)Interventional2003-09-01Completed
[NCT00108992]Phase 3750 participants Interventional2004-02-29Completed
Open-Label, Randomized, Single Center Study to Compare the Pharmacokinetics of IV Diclofenac Sodium (2 Doses) Versus Oral Diclofenac Potassium in Healthy Adult Volunteers Following Single- and Multiple-Dose Administration [NCT00474136]Phase 136 participants (Actual)Interventional2007-03-31Completed
A 4-week, Randomized, Double-blind, Multicenter, Placebo-controlled Phase 2 Study to Evaluate the Efficacy and Safety of HP-5000 in Subjects With Osteoarthritis (OA) of the Knee [NCT03277066]Phase 2289 participants (Actual)Interventional2017-09-07Completed
Proof-of Concept Study to Evaluate the Safety and Analgesic Efficacy of Topical 3%-Diclofenac-Nano-Emulsion Cream Versus Placebo for Knee Osteoarthritis [NCT00484120]Phase 2123 participants (Actual)Interventional2007-06-30Completed
Study of the Cutaneous Microcirculation: ASIC Involvement. [NCT01246180]20 participants (Actual)Interventional2010-10-31Completed
Steroids and/ or Non-steroidal Anti-inflammatory Drugs in the Postoperative Regime After Trabeculectomy. An Investigator-initiated Randomized Study (The SNAP Study) [NCT04054830]Phase 470 participants (Actual)Interventional2019-08-01Active, not recruiting
A Randomized, Double-Blind, 7-Day Study of the Efficacy and Safety of Rofecoxib Versus Placebo and Diclofenac in Patients With Acute Painful Rotator Cuff Syndrome [NCT00140933]Phase 3274 participants Interventional2003-04-30Terminated
Efficacy for Acute Pain Alleviation of 50 mg Diclofenac 1 Hour Prior to Endometrial Sampling in Cases of Abnormal Uterine Bleeding [NCT01762306]90 participants (Anticipated)Interventional2012-11-30Recruiting
Dr. Bill Antifungal Nail Gel Study [NCT04341402]Phase 230 participants (Anticipated)Interventional2020-05-01Recruiting
Efficacy and Safety of a Single s.c. Diclofenac HPBCD 75mg/1ml Injection as Compared to a Single i.m. Voltarol® 75mg/3ml, in the Treatment of Acute Moderate-to-severe Post-surgical Pain Following Dental Surgery (Impacted 3rd Molar Removal). [NCT00943098]Phase 3142 participants (Actual)Interventional2009-09-30Completed
Intravitreal Diclofenac Versus Intravitreal Ranibizumab for the Treatment of Diabetic Macular Edema. [NCT03458923]Phase 430 participants (Anticipated)Interventional2015-01-31Recruiting
Clinical Protocol For A Multicentre, Double-Blind, Randomised, Parallel Group Study To Compare The Efficacy and Tolerability Of Celecoxib Vs. Diclofenac In The Treatment Of Subjects With Osteoarthritis Of The Hip Requiring Joint Replacement Therapy [NCT00174317]Phase 4250 participants Interventional2003-08-31Completed
Evidence Based Management of Acute Biliary Pancreatitis [NCT04615702]30 participants (Actual)Observational [Patient Registry]2017-05-15Completed
Drug Interaction Study of Safinamide and a BCRP Substrate, Diclofenac, Concomitantly Administered to Healthy Volunteers [NCT02495831]Phase 124 participants (Actual)Interventional2015-05-31Completed
Evaluation of Bioavailability of Diclofenac Dermal Products [NCT03145259]Early Phase 112 participants (Actual)Interventional2017-04-19Completed
A Study to Compare Pre-Operative Administration of Rofecoxib Vs Post-Operative Administration of Diclofenac or Rofecoxib in the Treatment of Post-Operative Pain After Total Knee Joint Replacement in Patients With Osteoarthritis of the Knee. [NCT00140920]Phase 411 participants (Actual)Interventional2004-05-25Terminated(stopped due to Recruitment/study discontinued after withdrawal of marketing authorisation. No data entered.)
A Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of Etoricoxib 60 mg and Diclofenac Sodium 150 mg in Patient With Osteoarthritis of the Knee or Hip [NCT00542087]Phase 3516 participants (Actual)Interventional2002-03-22Completed
Long-term Effects of Aldara® 5% Cream and Solaraze® 3% Gel in the Treatment of Actinic Keratoses on the Face or Scalp (LEIDA) [NCT00777127]Phase 4258 participants (Actual)Interventional2008-12-31Completed
Diclofenac Premedication, as the Effect of Preemptive Analgesia After Post-thoracotomy Chest and Shoulder Pain, as Well as the Changes of the Postoperative Breathing Function Values, a Randomized, Controlled, Prospective Trial [NCT02445599]Phase 43 participants (Actual)Interventional2014-04-30Completed
Tramadol Versus Diclofenac for Prevention of Pain in Operative Outpatient Hysteroscopy: A Randomized Double Blind Placebo Controlled Trial [NCT02428777]Phase 3210 participants (Anticipated)Interventional2015-04-30Recruiting
A Randomized, Double-Blind, Active-Comparator-Controlled, Parallel-Group Study to Evaluate the Safety of Etoricoxib in Patients With Osteoarthritis or Rheumatoid Arthritis [NCT00250445]Phase 323,498 participants (Actual)Interventional2003-01-31Completed
A Placebo-Controlled, Parallel-Group, Double-Blind Study to Assess Safety and to Define the Clinically Effective Dose Range of MK0663 in Patients With Osteoarthritis of the Knee, Followed by a Double-Blind, Active-Comparator-Controlled Extension. [NCT00242489]Phase 21,167 participants (Actual)Interventional1998-06-30Completed
The Effect of Preemptive Analgesia On The Comfort Of Patient and Doctor, in Cystoscopy [NCT03831321]Phase 4144 participants (Anticipated)Interventional2018-12-11Recruiting
Open Randomised Comparative Study of the Efficacy and Safety of Neuromultivit (Solution for Injections, 2 ml) in Patients With Vertebrogenic Radiculopathy [NCT02508805]Phase 3100 participants (Actual)Interventional2015-05-31Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Sodium Topical Gel (DSG) 1% Applied Four Times Daily in Subjects With Acute Blunt Soft Tissue Injuries/Contusions of the L [NCT01272947]Phase 3204 participants (Actual)Interventional2011-01-31Completed
Phase 3 Randomized, Double-Blind, Multi-Dose, Placebo And NSAID Controlled Study To Evaluate The Efficacy And Safety Of Fasinumab In Patients With Pain Due To Osteoarthritis Of The Knee Or Hip [NCT03304379]Phase 31,650 participants (Actual)Interventional2017-10-26Completed
A One Week, Double-Blind, Adaptive, Randomized, Multicenter Study to Compare the Efficacy, Safety and Tolerability of Topical Diclofenac Gel Versus Placebo in Patients With Superficial Thrombophlebitis [NCT00377806]Phase 4200 participants Interventional2003-01-31Completed
Prediction of Potential Drug Interaction With CYP2C9 Substrate by Using Phenytoin Metabolic Ratio as a Marker of Its Activity in-Vivo. [NCT00226538]16 participants Interventional1999-08-31Completed
the Post Operative Pericardial Effusion (POPE) Treatment Study [NCT00247052]Phase 4200 participants (Anticipated)Interventional2006-03-31Completed
Effect of Diclofenac Sodium Versus Calcium Hydroxide as Intracanal Medication on the Intensity of Postoperative Pain, Bacterial Load Reduction and MMP-9 Levels in Patients With Necrotic Pulp: A Randomized Clinical Trial [NCT05582421]Early Phase 130 participants (Anticipated)Interventional2022-12-31Not yet recruiting
The Real Life Topical Field Treatment of Actinic Keratosis Study. An Observational Study Focusing on Patient Reported Outcomes [NCT02362152]1,168 participants (Actual)Observational2014-07-31Completed
The Effect on Knee Joint Loads of Instruction in Analgesic Use Compared With NEUROMUSCULAR Exercise in Patients With Knee Osteoarthritis - A Single Blind RCT [NCT01638962]93 participants (Actual)Interventional2012-08-31Completed
Tramadol Versus Diclofenac for Reducing Pain Associated With Outpatient Hysteroscopy: A Randomized Double Blind Placebo-Controlled Trial [NCT02419651]Phase 3210 participants (Anticipated)Interventional2015-04-30Recruiting
Effect of Perioperative Topical Diclofenac on Intraocular Inflammation After Cataract Surgery and the Incidence of Postoperative Macular Edema in Patients With Diabetic Retinopathy [NCT01694212]55 participants (Actual)Interventional2012-10-31Completed
[NCT01717599]343 participants (Actual)Interventional2012-08-29Completed
A Randomized, Double-Blind, Multiple-Site, Placebo-Controlled, Parallel Design Study Comparing Diclofenac Sodium Gel 3% (Taro Pharmaceuticals Inc.) to Solaraze® (Diclofenac Sodium) Gel 3% (Fougera Pharms) in the Treatment of Actinic Keratosis. [NCT01742663]Phase 1435 participants (Actual)Interventional2012-10-31Completed
[NCT01761071]Phase 394 participants (Actual)Interventional2012-01-31Completed
A Randomized, Single-Dose, Comparative, Positive and Placebo Controlled, Four-Way, Four Period, Cross-Over Study to Evaluate the Effect of DIC075V on QTc Intervals in Healthy Subjects [NCT01812538]Phase 170 participants (Actual)Interventional2009-05-31Completed
Phase 2 Study of Diclofenac Suppository to Control Pain During Flexible Cystoscopy [NCT01812928]Phase 260 participants (Actual)Interventional2013-03-31Completed
Potential for Improved Analgesia From Combined Medication for Superficial Pain [NCT02194088]Phase 3100 participants (Actual)Interventional2014-04-30Completed
Preliminary Evaluation of the Efficacy and Local Tolerability of Injectable Diclofenac at 5, 12.5, 25 and 50 mg/mL, Administered Locally Prior to Surgery for the Prevention of Post-operative Pain After Third Molar Surgery [NCT01706588]Phase 275 participants (Actual)Interventional2013-01-31Completed
A Single Center, Open-label, Clinical Study to Evaluate the Ability of Dermal Open Flow Microperfusion (dOFM) for Bioequivalence Testing of Topically Applied Diclofenac Sodium Products in Healthy Subjects [NCT04592016]22 participants (Actual)Interventional2020-10-08Completed
A Phase 4, Open-Label Study of the Pharmacokinetics and Safety of Cambia® (Diclofenac Potassium for Oral Solution) for the Acute Treatment of Migraine Attacks With or Without Aura in Pediatric Subjects (Ages 12-17 Years) [NCT02287376]Phase 425 participants (Actual)Interventional2015-01-31Completed
A Double-Blind, Randomized, Placebo-Controlled, Parallel Group, Three-Arm, Multi-Site Study to Evaluate the Clinical Equivalence of Diclofenac Sodium Topical Gel 1% (Hi-Tech Pharmacal Co., Inc.) With Voltaren® Gel (Diclofenac Sodium Topical Gel) 1% (Novar [NCT02913521]Phase 3934 participants (Actual)Interventional2015-06-30Completed
Randomized, Controlled, Double-blind, Placebo-controlled, Multi-center Hypothesis-finding Trial to Compare the Efficacy and Safety of a 10% Naproxen Gel vs. a 2.32% Diclofenac Diethylamine Gel and Placebo in the Treatment of Acute Soft Tissue Injuries of [NCT05026320]Phase 276 participants (Actual)Interventional2021-08-08Completed
Axillary Phonophoresis Versus Post Isometric Facilitation in the Treatment of Shoulder Adhesive Capsulitis [NCT05475639]45 participants (Anticipated)Interventional2023-02-25Not yet recruiting
Clinical Efficacy of Ginkgo Biloba Extract in the Treatment of Knee Osteoarthritis [NCT05398874]60 participants (Actual)Interventional2021-11-01Completed
A Randomized, Double-Blind, Placebo-Controlled, Three-Arm, Parallel-Design, Multiple-Site Study to Evaluate the Therapeutic Equivalence of Diclofenac Sodium Gel 3% (Encube Ethicals) Compared to Solaraze® (Diclofenac Sodium) Gel 3% (Fougera Pharmaceuticals [NCT03826550]Phase 3655 participants (Actual)Interventional2018-01-12Completed
Diclofenac Potassium Alone Versus Diclofenac Potassium With Hyoscine-N-butyl Bromide (HBB in Endoscopy [NCT04125771]64 participants (Actual)Interventional2020-02-16Completed
Single Center, Open-label Study of Effect of PENNSAID (Diclofenac Sodium Solution Topical) on Coagulation Parameters (PT, PTT, INR and Platelet Function) in Patients With Moderate to Severe Osteoarthritis Pain of the Knee Taking Anticoagulant Medication [NCT01511939]Phase 322 participants (Actual)Interventional2012-02-29Completed
Neodolpasse® Infusion Solution Versus Diclofenac 75 mg Infusion in the Treatment of Postoperative Pain After Elective Knee Surgery - an Exploratory Placebo-controlled Clinical Study to Investigate the Analgesic Properties of the Combination of Diclofenac [NCT03493490]Phase 472 participants (Actual)Interventional2018-03-01Completed
Impact of Gel Aromatherapy on Pain for Patients With De Quervain Disease : Monocentric Study, Controlled, Randomized, Partially Blinded, in Paralleled Groups [NCT06012097]Phase 470 participants (Anticipated)Interventional2024-01-01Not yet recruiting
A Randomized, Parallel-Group, Single-Attack, Open-Label Study to Evaluate the Efficacy of Diclofenac Potassium and Rimegepant for the Acute Treatment of Migraine (ATOM) [NCT05211154]Phase 4645 participants (Anticipated)Interventional2022-05-05Recruiting
A Randomized Controlled Clinical Trial on the Antipyretic Efficacy of Oral Paracetamol, Intravenous Paracetamol and Intramuscular Diclofenac in Patients Presenting With Fever to Emergency Department [NCT01891435]434 participants (Actual)Interventional2010-01-31Completed
A Phase 2, Randomized, Double-Blind, Single-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Diclofenac [Test] Capsules for the Treatment of Pain After Surgical Removal of Impacted Third Molars [NCT00985439]Phase 2202 participants (Actual)Interventional2009-09-30Completed
A Randomized Comparison of Bupivacaine Peritoneal and Subcutaneous Infiltration Versus Diclofenac Intramuscular Injection for Postoperative Pain Relief in Patient Undergoing Cesarean Delivery [NCT03039426]Phase 4120 participants (Actual)Interventional2017-01-01Completed
A Comparative Evaluation of Diclofenac Sodium Transdermal Patch, Oral Diclofenac Sodium With Intramuscular Injections of Diclofenac Sodium in Patients Suffering From Oral Pain: A Randomized Control Trial [NCT03221946]Phase 490 participants (Actual)Interventional2016-01-31Completed
Electromagnetic Field Versus Diclofenac Drugs on Primary Dysmenorrhea: Arandomized Controlled Trial in the Egyptian Women [NCT03269591]50 participants (Actual)Interventional2016-02-01Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Potassium 25 mg Tablet Taken Three Times Daily in Subjects With Acute Joint Pain [NCT01666197]Phase 4100 participants (Actual)Interventional2012-08-31Completed
A Single Blinded, Open-labelled, Randomized Control Trial Comparing Acetaminophen Rectal Suppository With Diclofenac Rectal Suppository as Analgesia for Perineal Injury Following Childbirth [NCT03041779]Phase 2909 participants (Actual)Interventional2015-10-31Completed
Inhalation of Vapor With Medication (Diclofenac Sodium, Menthol, Methyl Salicylate and N-Acetyl Cysteine) Reduces Oxygen Need and Hospital Stay in COVID-19 Patients - A Case Control Study [NCT04900129]Phase 143 participants (Actual)Interventional2020-12-01Completed
Comparison of Preoperative Analgesics on the Efficacy of Inferior Alveolar Nerve Block on Patients With Symptomatic Irreversible Pulpitis: a Double Blinded, Randomized Controlled Trial. [NCT05488925]Phase 4120 participants (Actual)Interventional2021-06-21Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, 3-treatment Arm, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Diethylamine 2.32% Gel Applied Twice or Three Times Daily in Patients With Acute Ankle Sprain [NCT00955513]Phase 3242 participants (Actual)Interventional2009-07-31Completed
Are NSAIDs Effective Enough for Postoperative Pain Control After Functional Endoscopic Sinus Surgery and Septoplasty [NCT03605914]Phase 4100 participants (Actual)Interventional2018-08-01Completed
Efficacy of Diclofenac for Patients With Acute Submassive Pulmonary Embolism: a Randomized Clinical Trial [NCT01590342]Phase 2/Phase 334 participants (Actual)Interventional2012-05-31Terminated(stopped due to Low recruitment rate)
Use of Dermal Microdialysis to Evaluate the Effect of Skin Properties and Application Site on the Topical Bioequivalence of Diclofenac: The Main Study [NCT01592019]Early Phase 16 participants (Actual)Interventional2012-04-30Completed
A Phase I, Multi-center, Open-label, Drug-drug Interaction Study to Assess the Effect of TKI258 on the Pharmacokinetics of Caffeine, Diclofenac, Omeprazole and Midazolam Administered as a Four-drug Cocktail in Patients With Advanced Solid Tumors, Excludin [NCT01596647]Phase 139 participants (Actual)Interventional2012-05-31Completed
Adjuvant Treatment of Graves´ Ophthalmopathy With NSAID (aGO Study) [NCT01458600]Phase 465 participants (Actual)Interventional2006-09-30Completed
A Randomized, Double-Blind, Within-Subject, Proof of Concept Study to Assess the Analgesic Efficacy and Safety of Voltaren Gel (1% Diclofenac Sodium) Compared to Placebo in Subjects Experiencing Delayed Onset Muscle Soreness [NCT02087748]Phase 424 participants (Actual)Interventional2014-03-31Completed
Penile Fracture: A Prospective Randomized Study Comparing Erectile Function at 12 Months After Immediate Degloving Repair Versus Delayed Localized Repair [NCT03449940]46 participants (Actual)Interventional2015-01-31Completed
A 12-Week, Randomized, Double-Blind, Multi-Center, Vehicle-Controlled, Parallel Group Study to Assess the Efficacy and Safety of the Diclofenac Sodium Gel 1% for the Relief of Signs and Symptoms in Patients With Osteoarthritis of the Knee. [NCT00426621]Phase 3420 participants (Actual)Interventional2006-11-30Completed
Diclofenac for the Prevention of Post-ERCP Pancreatitis in Higher Risk Patients: A Prospective, Randomized, Double Blind, Placebo Controlled Trial. [NCT00428025]Phase 423 participants (Actual)Interventional2006-10-31Terminated(stopped due to slow recruitment)
Diclofenac Phonophoresis Versus High Power Pain Threshold Ultrasound in Patients With Mechanical Non-specific Neck Pain [NCT05434039]60 participants (Anticipated)Interventional2022-07-30Not yet recruiting
A Randomized, Double-blind, Placebo-controlled, Multi-center Parallel Group Phase IV Study to Evaluate the Efficacy and Safety of Diclofenac 1.16% Gel in Subjects With Acute Neck Pain [NCT01335724]Phase 472 participants (Actual)Interventional2011-04-30Completed
Rectal Versus Oral Diclofenac Sodium in Relieving Post Episiotomy Pain [NCT04331210]1,024 participants (Anticipated)Interventional2020-09-01Not yet recruiting
A Study to Comparing the Efficacy and Safety of the Ketoprofen and Diclofenac in Patients With Osteoarthritis [NCT04421911]Phase 3236 participants (Actual)Interventional2020-03-20Completed
Prospective, Three-armed, Randomised, Double-blind Study to Evaluate the Efficacy and Safety of the Treatment of Mild and Moderate Actinic Keratosis With a 5% Potassium Hydroxide Solution (Solcera, Medical Device) Versus Placebo and Investigator-blinded C [NCT04552327]Phase 3631 participants (Actual)Interventional2020-10-14Completed
Topical Chemoprevention of Skin Cancer Biomarkers [NCT02636569]Phase 224 participants (Actual)Interventional2017-10-25Active, not recruiting
An Open-label, Prospective, Uncontrolled Study of the Safety and Local Tolerability of the Diclofenac Epolamine Patch (Flector Patch) in Pediatric Patients With Minor Soft Tissue Injuries [NCT02132247]Phase 4104 participants (Actual)Interventional2014-05-31Completed
A 4-week, Randomized, Double-blind, Multi-center, Vehicle-controlled, Parallel Group Study to Assess the Efficacy and Safety of Diclofenac Diethylamine 2.32% Gel for the Relief of Signs and Symptoms in Patients With Knee Osteoarthritis [NCT01967550]Phase 3304 participants (Actual)Interventional2013-10-31Completed
Randomized, Double-Blind, Multiple-Center, Placebo-Controlled Study Comparing the Safety and Efficacy of Generic Diclofenac Epolamine to Flector® Patch in the Treatment of Acute Pain Due to Minor Ankle Sprain [NCT02324270]Phase 3658 participants (Actual)Interventional2014-05-31Completed
A Randomized, Double-Blind, Multiple-Site, Placebo-Controlled, Parallel Design Study Comparing Diclofenac Sodium Gel 3% (Actavis) to Solaraze ® (Diclofenac Sodium) Gel 3% (Fougera Pharms) in the Treatment of Actinic Keratosis [NCT01962987]Phase 3476 participants (Actual)Interventional2013-03-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Multiple-Site Clinical Study to Evaluate the Therapeutic Equivalence of Diclofenac Sodium Gel, 1% (Glenmark Pharmaceuticals Ltd) to Voltaren® Gel (Diclofenac Sodium Topical Gel) 1% (Novartis [NCT02596451]Phase 31,164 participants (Actual)Interventional2015-08-31Completed
A Randomized Study of Topical Diclofenac Versus Oral Ibuprofen for Acute Non-radicular Low Back Pain [NCT04611529]Phase 4198 participants (Anticipated)Interventional2021-03-02Recruiting
A Multicenter, Open-Label, Safety Study of Diclofenac [Test] Capsules in Subjects With Osteoarthritis of the Knee or Hip [NCT01510912]Phase 3602 participants (Actual)Interventional2012-01-31Completed
An Open-Label Study of the Safety and Efficacy of Zipsor® (Diclofenac Potassium) Liquid Filled Capsules in Pediatric Subjects (Ages 12-17 Years) With Mild to Moderate Acute Pain [NCT01982539]Phase 425 participants (Actual)Interventional2013-11-30Completed
Sustained Acoustic Medicine (SAM) Combined With a Diclofenac Ultrasound Coupling Patch for Knee Osteoarthritis [NCT04391842]Phase 134 participants (Actual)Interventional2019-09-01Completed
Post-Operative Pain Control Following Shoulder Surgery [NCT04622839]74 participants (Actual)Interventional2020-12-01Completed
A Randomised, Double Blind, Cross Over Clinical Study in Healthy Human Volunteers to Assess the Efficacy and Safety of Three Different Topical Analgesics (DCF100, TIB200 And SPR300) Versus in a Model of UV-Induced Inflammatory Pain [NCT02666846]Phase 160 participants (Actual)Interventional2015-03-31Completed
Pilot Study of the Feasibility of n-of-1 Trials: the Individualisation of Treatments for Osteoarthritis [NCT00371696]Phase 210 participants Interventional2001-12-31Completed
Non-Steroidal Anti-inflammatory Drugs in Axial Spondyloarthritis: a Pilot Study [NCT03473665]Phase 49 participants (Actual)Interventional2018-03-01Terminated(stopped due to Slow recruitment)
National Clinical Study, Phase III, Multicenter, Randomized, Double-blind, Controlled, Parallel, to Evaluate the Superiority of the Fixed Association (Orfenadrine 35mg, Acetaminophen 325mg, Caffeine 65mg and Diclofenac Sodium 50mg) Compared to the Drug Co [NCT02985671]Phase 3110 participants (Anticipated)Interventional2021-01-31Not yet recruiting
A Phase 3, Randomized, Double-Blind, Multiple-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Diclofenac [Test] Capsules for the Treatment of Acute Postoperative Pain After Bunionectomy [NCT01462435]Phase 3428 participants (Actual)Interventional2011-10-31Completed
The Analgesic Activity of a Topical Formulation in Patients With Osteoarthritis of the Hands [NCT02485145]Early Phase 140 participants (Anticipated)Interventional2015-07-31Not yet recruiting
Tramadol Versus Diclofenac for Reducing Pain Before Outpatient Hysteroscopy in Post Menopausal Women: A Randomized Double Blind Placebo Controlled Trial [NCT02425709]Phase 3210 participants (Anticipated)Interventional2015-04-30Recruiting
A Clinical Study to Assess the Efficacy and Onset of Pain Relief of Topical MFC51123 Diclofenac-Menthol Gel Versus Controls in Ankle Sprain [NCT02100670]Phase 3385 participants (Actual)Interventional2013-11-01Completed
A Randomized, Controlled Multi-centre Parallel Group Study to Assess the Efficacy and Safety of Multiple Doses of a Topically Applied Combination Containing Diclofenac 2% + Capsaicin 0.075% (2 g Formulation Per Application; 2-times Daily for 5 Days) Compa [NCT02700815]Phase 3746 participants (Actual)Interventional2016-05-09Completed
To Compare the Efficacy and Patients' Satisfaction for the Treatment of Post Cesarean Pain of Two Protocols: Oral Medications in Fixed Time Interval Administration Versus Spinal Morphine [NCT02440399]200 participants (Actual)Interventional2015-07-31Completed
Local Anesthesia Versus Combined Local Anesthesia With Single Dose Analgesia on Pain Control During Thoracic Ultrasound Guided Procedures [NCT05121233]Phase 4100 participants (Anticipated)Interventional2021-11-30Not yet recruiting
An Open-label Crossover Trial Assessing the Value of Dabigatran in a Drug Interaction Cocktail in Healthy Young Volunteers [NCT02361619]Phase 116 participants (Actual)Interventional2015-02-28Completed
Clinical Assessment of the Use of Topical Liquid Diclofenac Following Laser Microporation of Cutaneous Neurofibromas in Patients With Neurofibromatosis Type 1 [NCT03090971]Phase 27 participants (Actual)Interventional2017-02-15Completed
Diclofenac Plus Lidocaine Gel for Pain Relief During Intrauterine Device (IUD) Insertion. A Randomized Double Blinded Placebo-controlled Study [NCT02332057]Phase 290 participants (Actual)Interventional2015-02-28Completed
Phase 1 Study of the Effects of Combining Topical FDA-approved Drugs on Age-related Pathways on the Skin of Healthy Volunteers [NCT03072485]Phase 110 participants (Actual)Interventional2017-03-01Completed
Diclofenac Sodium Topical Gel to Reduce Injection Site Discomfort in Patients With Multiple Sclerosis Taking Glatiramer Acetate: A Randomized Controlled Double- Blind Crossover Trial [NCT01454791]Phase 440 participants (Actual)Interventional2011-01-31Completed
A Randomized, Double-blind, Double-dummy, Active-controlled Study to Assess the Efficacy and Tolerability of 50 mg Diclofenac Potassium Soft Gelatin Capsules Compared With 400 mg Ibuprofen Tablets in Patients With Moderate to Severe Postoperative Dental P [NCT02476422]Phase 3328 participants (Actual)Interventional2015-04-30Completed
Dry Needling and Spinal Manipulation or Interocclusal Appliance (Splint), NSAIDs and Joint Mobs for Temporomandibular Dysfunction [NCT03409874]120 participants (Actual)Interventional2018-02-01Completed
"Effectiveness and Safety of Breeded Leech Medileech by BioRepro GmbH for Symptomatic Primary Arthrosis of the First Carpometacarpal Joint: a Randomized Controlled Clinical Trial" [NCT03020368]52 participants (Actual)Interventional2017-01-31Terminated
Lidocaine Infusion Versus Oral Diclofenac During Outpatient Hystroscopy: A Randomized Clinical Trial [NCT03825016]Phase 244 participants (Actual)Interventional2017-08-01Completed
A Multi-center, Prospective, Open-label, Controlled Study of the Pharmacokinetics and Safety of the LicartTM Topical System in Pediatric and Adult Participants With Minor Soft Tissue Injuries [NCT05171673]Phase 3150 participants (Anticipated)Interventional2021-10-31Recruiting
A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Fixed-Dose, Parallel-Group, Efficacy and Safety Study of Diclofenac [Test] Capsules in Subjects With Osteoarthritis of the Knee or Hip [NCT01461369]Phase 3305 participants (Actual)Interventional2011-10-31Completed
Vitreous pge2 Level Changes After Topical Administration of Diclofenac 0.1%, Nepafenac 0.3%, Indomethacin 0.5% and Bromfenac 0.09% in Vitrectomy Patients [NCT03597867]Phase 3104 participants (Actual)Interventional2018-04-25Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Diclofenac Sodium Topical Gel (DSG) 1% Applied Four Times Daily in Subjects With Acute Ankle Sprain [NCT01272934]Phase 3205 participants (Actual)Interventional2011-01-31Completed
A Comparison of Non-Surgical Treatment Methods for Patients With Lumbar Spinal Stenosis [NCT01943435]259 participants (Actual)Interventional2013-11-20Completed
Efficacy and Safety Study of Diclofenac HPBCD 25, 50 mg/ml Administered as Single s.c. Dose, in the Treatment of Acute Moderate-to-severe Post-surgical Pain From Dental Surgery (Impacted 3rd Molar Extraction) [NCT00942448]Phase 3306 participants (Actual)Interventional2009-09-30Completed
Electroacupuncture vs Topical Diclofenac Sodium Gel for Patients With Hand Osteoarthritis: Study Protocol for a Randomized Controlled Trial [NCT04402047]108 participants (Anticipated)Interventional2020-09-01Recruiting
A Randomised Control Clinical Trial Comparing Diclofenac / Acetaminophen /Codeine and Ibuprofen/Acetaminophen/Codeine Combination for Pain Management After Third Molars Surgery [NCT04874675]78 participants (Actual)Interventional2023-03-31Suspended(stopped due to Covid 19 lockdown)
Propofol Sedation During Endoscopic Retrograde Cholangiopancreatography: A Comparison Between Conventional Versus Bispectral Index Guided Approach and Effect of Diclofenac Sodium Along With Topical Pharyngeal Anaesthesia [NCT04860167]90 participants (Actual)Interventional2018-09-10Completed
Effect of Topical Diclofenac on Clinical Outcome in Breast Cancer Patients Treated With Capecitabine: A Randomized Controlled Trial. [NCT05641246]Phase 266 participants (Anticipated)Interventional2022-12-08Active, not recruiting
A Double-Blind, Randomized, Placebo-Controlled, Parallel Group, Multi-Site Study to Evaluate the Clinical Equivalence of Diclofenac Sodium 1% Gel (Anchen Pharmaceuticals, Inc.) With Voltaren® Gel (Diclofenac Sodium Topical Gel) 1% (Novartis) in Patients W [NCT01456611]Phase 3749 participants (Actual)Interventional2011-09-30Completed
Effects of Pennsaid on Clinical Neuropathic Pain [NCT01508676]35 participants (Actual)Interventional2011-11-30Completed
The Efficacy of Diclofenac Gel for Breakthrough Pain and the Neuropathic Components of Pain in Knee Osteoarthritis [NCT01383954]Phase 452 participants (Actual)Interventional2011-06-30Completed
Randomized Controlled Trial to Evaluate the Efficiency of IV Fluids in the Treatment of Renal Colic [NCT03529097]Phase 40 participants (Actual)Interventional2018-06-01Withdrawn(stopped due to No participants enrolles)
Analgesic Efficacy of Arnica Montana in Comparison With Diclofenac Sodium Following a Periodontal Surgical Procedure: A Placebo Control Trial [NCT03520595]60 participants (Actual)Interventional2016-12-01Completed
A Phase IIA, Open-Label, Safety and Pharmacokinetic Study of Diclofenac Capsules in Pediatric Subjects 6 to <17 Years of Age With Mild to Moderate Acute Postoperative Pain Following Elective Surgery [NCT02424578]Phase 230 participants (Actual)Interventional2015-05-31Completed
A Comparison of NSAIDs for Acute, Non-radicular Low Back Pain. A Randomized Trial [NCT03861611]Phase 4198 participants (Actual)Interventional2019-07-12Completed
Randomized Controlled Study to Evaluate the Safety and Efficacy of SFPP in Knee Osteoarthritis Using Diclofenac Gel as the Comparator [NCT03434197]Phase 3313 participants (Actual)Interventional2018-02-05Completed
A Multi-Center, Double-Blind, Vehicle-Controlled, Parallel-Group Study Comparing a Generic Diclofenac Sodium Topical Gel, 1% to Voltaren® Gel (Diclofenac Sodium Topical Gel) 1% in the Treatment of Subjects With Osteoarthritis of the Knee [NCT02121002]Phase 31,176 participants (Actual)Interventional2014-04-30Completed
Effectiveness and Safety of a Phytopharmaceutical Produced With an Extract of Sphaeralcea Angustifolia as a Topical Treatment of Knee Osteoarthritis: A Randomized Double Blind Clinical Trial [NCT04511195]Phase 2100 participants (Anticipated)Interventional2020-07-10Recruiting
A Randomized, Double-blind, Placebo-controlled, Within-subject Study to Evaluate the Efficacy and Safety of Diclofenac Sodium Topical Gel (DSG) 1% Applied Four Times Daily in Subjects Experiencing Acute Delayed Onset Muscle Soreness (DOMS) of the Lower Li [NCT02271854]Phase 3102 participants (Actual)Interventional2014-10-31Completed
The Incidence of Thoracic Disc Herniation in Patients Presenting With Chronic Upper Back Pain, A Follow-Up Study [NCT05313997]194 participants (Actual)Observational2022-05-24Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIEs by History of GD Ulceration
NCT00141102 (17) [back to overview]Number of Subjects With SUs
NCT00141102 (17) [back to overview]Number of Subjects With Moderate to Severe Abdominal Symptoms
NCT00141102 (17) [back to overview]Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)
NCT00141102 (17) [back to overview]Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)
NCT00141102 (17) [back to overview]Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin
NCT00141102 (17) [back to overview]Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview
NCT00141102 (17) [back to overview]Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)
NCT00141102 (17) [back to overview]Change From Baseline in Iron Binding Capacity to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Hemoglobin at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Hematocrit at Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in Ferretin to Month 6/ET
NCT00141102 (17) [back to overview]Change From Baseline in C-Reactive Protein to Month 6/ET
NCT00141102 (17) [back to overview]Number of Subjects Withdrawn Due to GI Adverse Events (AEs)
NCT00141102 (17) [back to overview]Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET
NCT00141102 (17) [back to overview]Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)
NCT00141102 (17) [back to overview]Number of Subjects Alive at the Post Trial Interview
NCT00264147 (6) [back to overview]Tender Joint Count (Out of 68 Joints) Time-Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment Period (All Patients-Treated Population)
NCT00264147 (6) [back to overview]Swollen Joint Count (Out of 66 Joints) Time-Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment Period (All Patients-Treated Population)
NCT00264147 (6) [back to overview]Proportion of Patients Who Met the ACR20 Responder Index Criteria
NCT00264147 (6) [back to overview]Patient Global Assessment of Pain (0- to 100-mm Visual Analog Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)
NCT00264147 (6) [back to overview]Patient Global Assessment of Disease Activity (0- to 100-mm Visual Analog Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)
NCT00264147 (6) [back to overview]Investigator Global Assessment of Disease Activity (0- to 4-Likert Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)
NCT00366444 (11) [back to overview]Total Pain Relief (TOTPAR) Scores 8 Hours Post Initial Dose of Study Drug
NCT00366444 (11) [back to overview]Time to Onset of at Least 30% Reduction in Pain Intensity After First Dose of Study Drug
NCT00366444 (11) [back to overview]Number of Patients With Meaningful Pain Relief on Day 1
NCT00366444 (11) [back to overview]Number of Patients With at Least 30% Reduction in Pain Intensity After First Dose of Study Drug
NCT00366444 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 3
NCT00366444 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 2
NCT00366444 (11) [back to overview]Median Time to Onset of Pain Relief in Patients With Meaningful Pain Relief on Day 1
NCT00366444 (11) [back to overview]Median Time to Onset of Pain Relief in Patients With Perceptible Pain Relief on Day 1
NCT00366444 (11) [back to overview]Average Numeric Pain Rating Score (NPRS) Over 48 Hours After Bunionectomy
NCT00366444 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 1
NCT00366444 (11) [back to overview]Number of Patients With Perceptible Pain Relief on Day 1
NCT00375934 (11) [back to overview]Number of Patients With at Least 30% Reduction in Pain Intensity After First Dose of Study Drug
NCT00375934 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 3
NCT00375934 (11) [back to overview]Total Pain Relief (TOTPAR) Scores 8 Hours Post Initial Dose of Study Drug
NCT00375934 (11) [back to overview]Time to Onset of at Least 30% Reduction in Pain Intensity After First Dose of Study Drug
NCT00375934 (11) [back to overview]Number of Patients With Perceptible Pain Relief on Day 1
NCT00375934 (11) [back to overview]Number of Patients With Meaningful Pain Relief on Day 1
NCT00375934 (11) [back to overview]Average Numeric Pain Rating Score (NPRS) Over 48 Hours After Bunionectomy
NCT00375934 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 2
NCT00375934 (11) [back to overview]Number of Patients Who Required Rescue Medication on Day 1
NCT00375934 (11) [back to overview]Median Time to Onset of Pain Relief in Patients With Perceptible Pain Relief on Day 1
NCT00375934 (11) [back to overview]Median Time to Onset of Pain Relief in Patients With Meaningful Pain Relief on Day 1
NCT00476593 (1) [back to overview]Macular Thickness Measured With the OCT; in Relation to Age, Sex, Reproductive Factors and the Use of Anti-inflammatory Eye Drops in Health; in Uncomplicated Anterior Uveitis.
NCT00507026 (16) [back to overview]Total Pain Relief (TOTPAR)
NCT00507026 (16) [back to overview]Sum of the Pain Intensity Differences (SPID) Over 120 Hours
NCT00507026 (16) [back to overview]Sum of the Pain Intensity Differences (SPID) Over 24 Hours
NCT00507026 (16) [back to overview]Percentage of Participants Attaining Greater Than or Equal to (>=) 30 Percent (%) Reduction From Baseline in Pain Intensity
NCT00507026 (16) [back to overview]Participant Global Evaluation Over Time
NCT00507026 (16) [back to overview]Pain Intensity Differences (PID) Over Time
NCT00507026 (16) [back to overview]Pain Intensity Differences (PID) Over Time
NCT00507026 (16) [back to overview]Number of Participants According to Frequency of Use of Rescue Medication
NCT00507026 (16) [back to overview]Sum of the Pain Intensity Differences (SPID) Over 72 Hours
NCT00507026 (16) [back to overview]Cumulative Amount of Rescue Medication
NCT00507026 (16) [back to overview]Time to Perceptible Relief
NCT00507026 (16) [back to overview]Time to Meaningful Relief
NCT00507026 (16) [back to overview]Time From Administration of Study Drug to Administration of Rescue Medication
NCT00507026 (16) [back to overview]Sum of the Pain Intensity Differences (SPID) Over 96 Hours
NCT00507026 (16) [back to overview]Visual Analog Pain Relief Values Over the Time
NCT00507026 (16) [back to overview]Sum of the Pain Intensity Differences (SPID) Over 48 Hours
NCT00573768 (1) [back to overview]Pain on Movement on Day 5 (Change From Baseline). A Greater Change From Baseline on Day 5 Equates to a Better Outcome.
NCT00594854 (3) [back to overview]Number of Participants With Duodenal Ulcers Confirmed by Endoscopy
NCT00594854 (3) [back to overview]Number of Participants With Gastric Ulcer Confirmed by Endoscopy
NCT00594854 (3) [back to overview]Number of Participants With Upper Gastro-intestinal Injury Grade 4 as Measured by Lanza (1991) Score
NCT00601640 (3) [back to overview]Safety of Combination Therapy With Topical Eflornithine Hydrochloride Ointment and Topical Diclofenac Sodium Gel Over 3-months
NCT00601640 (3) [back to overview]Changes in Putrescine Over 3 Months
NCT00601640 (3) [back to overview]Change in Histologic Score Diagnosis and Treatment Group
NCT00726388 (14) [back to overview]Change From Baseline in Blood Pressure at Study Discharge/Early Termination
NCT00726388 (14) [back to overview]Change From Baseline in Blood Pressure at Clinic Follow-up Visit
NCT00726388 (14) [back to overview]Number of Participants With Clinically Significant Electrocardiogram (ECG) Abnormalities at Study Discharge/Early Termination
NCT00726388 (14) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT00726388 (14) [back to overview]Number of Participants With Clinically Significant Physical Examination Abnormalities at Clinic Follow-up Visit
NCT00726388 (14) [back to overview]Number of Participants With Clinically Significant Electrocardiogram (ECG) Abnormalities at Baseline
NCT00726388 (14) [back to overview]Number of Participants With Abnormal Urinalysis Findings
NCT00726388 (14) [back to overview]Number of Participants Who Took at Least 1 Concomitant Medication
NCT00726388 (14) [back to overview]Change From Baseline in Respiratory Rate at Study Discharge/Early Termination
NCT00726388 (14) [back to overview]Change From Baseline in Respiratory Rate at Clinic Follow-up Visit
NCT00726388 (14) [back to overview]Change From Baseline in Heart Rate at Study Discharge/Early Termination
NCT00726388 (14) [back to overview]Number of Participants With Wound Assessment at Study Discharge/Early Termination
NCT00726388 (14) [back to overview]Number of Participants With Clinically Significant Physical Examination Abnormalities at Screening
NCT00726388 (14) [back to overview]Change From Baseline in Heart Rate at Clinic Follow-up Visit
NCT00762463 (26) [back to overview]Change From Baseline in Fingertips to Floor Distance at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Nocturnal Pain at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Weeks 2 and 4
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Global Assessment of Disease Activity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Global Assessment of Disease Activity at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Physician's Global Assessment of Disease Activity at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Physician's Global Assessment of Disease Activity at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Percentages of Participants Responding to Assessment in Ankylosing Spondylitis (ASAS)-20
NCT00762463 (26) [back to overview]Change From Baseline in Nocturnal Pain at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in C-Reactive Protein (CRP) at Week 6
NCT00762463 (26) [back to overview]Change From Baseline in Erythrocyte Sedimentation Rate (ESR) at Week 6
NCT00762463 (26) [back to overview]Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 6
NCT00762463 (26) [back to overview]Paracetamol Tablets Taken Per Day by Participant
NCT00762463 (26) [back to overview]Participant's Assessment of Global Pain Intensity at Baseline
NCT00762463 (26) [back to overview]Percentage of Days With Concomitant Administration of Paracetamol
NCT00762463 (26) [back to overview]Percentage of Participants With Concomitant Use of Paracetamol
NCT00762463 (26) [back to overview]Change From Baseline in BASDAI at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in BASFI at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Bath Ankylosing Spondylitis Functional Index (BASFI) at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in Chest Expansion at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Chest Expansion at Weeks 2, 4, and 6
NCT00762463 (26) [back to overview]Change From Baseline in CRP at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in ESR at Week 12
NCT00762463 (26) [back to overview]Change From Baseline in Fingertips to Floor Distance at Week 12
NCT00864097 (24) [back to overview]Time to Discontinuation (TTD) Due to Lack of Efficacy
NCT00864097 (24) [back to overview]Percentage of Participants With Outcome Measures in Rheumatology - Osteoarthritis Research Society International (OMERACT-OARSI) Response; LOCF
NCT00864097 (24) [back to overview]Percentage of Participants With Improvement of at Least 2 Points in Patient Global Assessment (PGA) of Osteoarthritis; LOCF
NCT00864097 (24) [back to overview]Percentage of Participants With Improvement of at Least 2 Points in Patient Global Assessment (PGA) of Osteoarthritis; Baseline Observation Carried Forward (BOCF)
NCT00864097 (24) [back to overview]Percentage of Participants With Cumulative Reduction From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Week 16 and 24
NCT00864097 (24) [back to overview]Percentage of Participants With At Least 30%, 50%, 70% and 90% Reduction From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score; LOCF
NCT00864097 (24) [back to overview]Number of Participants With Intravenous Doses of Study Medication
NCT00864097 (24) [back to overview]Number of Participants With Change From Baseline in European Quality of Life - 5 Dimension (EQ-5D) Individual Health State Profile at Week 24
NCT00864097 (24) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00864097 (24) [back to overview]Change From Baseline in 36-Item Short-Form Health Survey Version 2 (SF-36v2) Domain Scores at Week 12 and 24
NCT00864097 (24) [back to overview]Number of Participants Who Discontinued Due to Lack of Efficacy
NCT00864097 (24) [back to overview]Change From Baseline in 36-Item Short-Form Health Survey Version 2 (SF-36v2) Physical and Mental Component Scores at Week 12 and 24
NCT00864097 (24) [back to overview]Change From Baseline in Average Pain Score in the Index Knee or Hip at Weeks 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, and 24
NCT00864097 (24) [back to overview]Change From Baseline in European Quality of Life - 5 Dimension (EQ-5D) Index Score at Week 24
NCT00864097 (24) [back to overview]Change From Baseline in Patient Global Assessment (PGA) of Osteoarthritis Score at Week 16
NCT00864097 (24) [back to overview]Change From Baseline in Patient Global Assessment (PGA) of Osteoarthritis Score at Weeks 2, 4, 8, 12, and 24
NCT00864097 (24) [back to overview]Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Weeks 2, 4, 8, 12 and 24
NCT00864097 (24) [back to overview]Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Physical Function Subscale Score at Weeks 2, 4, 8, 12, and 24
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Average Score at Weeks 2, 4, 8, 12, 16, and 24
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Item: Pain When Going Up or Downstairs at Weeks 2, 4, 8, 12, 16, and 24
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Item: Pain When Walking on a Flat Surface at Weeks 2, 4, 8, 12, 16, and 24
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Week 16
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Physical Function Subscale Score at Week 16
NCT00864097 (24) [back to overview]Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Stiffness Subscale Score at Weeks 2, 4, 8, 12, 16, and 24
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]Pain Intensity Difference (PID) on a 0-100 VAS
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00942448 (13) [back to overview]PID
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]Pain Intensity Difference (PID)
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00943098 (13) [back to overview]PIDs
NCT00955513 (1) [back to overview]Measure: Pain on Movement on Day 5 (Change From Baseline).
NCT00985439 (1) [back to overview]Total Patient Pain Relief Over 0 to 12 Hours.
NCT01054820 (11) [back to overview]Mean Change From Baseline to End of Treatment (EOT) in Response to Modified Brief Pain Inventory (mBPI) Question 5: Average Pain Over the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Beck Depression Inventory® Il
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 3: Pain at Its Worst in the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 4: Pain at Its Least in the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 6: Pain Right Now
NCT01054820 (11) [back to overview]Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Investigator
NCT01054820 (11) [back to overview]Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Participant
NCT01054820 (11) [back to overview]Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by Participant
NCT01054820 (11) [back to overview]Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by the Investigator
NCT01054820 (11) [back to overview]Number of Participants With Change From Baseline (Bsl) to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 1: Pain Other Than Everyday Kind of Pain
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 8: Percent Reduction in Pain From Baseline
NCT01066520 (3) [back to overview]Patient's Assessment of Ankle Pain (VAS)- Absolute Value Decrease on Day 7
NCT01066520 (3) [back to overview]Change of the Foot and Ankle Ability Measurement (FAAM), Activity of Daily Living Subscale (ADL) From Baseline to Day 7
NCT01066520 (3) [back to overview]Patient's Assessment of Ankle Pain (VAS)- Percentage Decrease on Day 7
NCT01255423 (5) [back to overview]Ankle Joint Function
NCT01255423 (5) [back to overview]Tenderness
NCT01255423 (5) [back to overview]Onset of Pain Relief
NCT01255423 (5) [back to overview]Pain on Movement
NCT01255423 (5) [back to overview]Pain on Movement
NCT01272934 (2) [back to overview]Onset of Pain Relief
NCT01272934 (2) [back to overview]Pain on Movement
NCT01272947 (2) [back to overview]Pain on Movement
NCT01272947 (2) [back to overview]Onset of Pain Relief
NCT01335724 (3) [back to overview]Neck Disability Index
NCT01335724 (3) [back to overview]Pain at Rest
NCT01335724 (3) [back to overview]Pain on Movement
NCT01383954 (2) [back to overview]Percent Change From Baseline in Pain Score During Week 2
NCT01383954 (2) [back to overview]Percent Change From Baseline in Pain Score During Week 1
NCT01454791 (3) [back to overview]Subject Global Impression at 2 Weeks
NCT01454791 (3) [back to overview]Pain Scale at 2 Weeks
NCT01454791 (3) [back to overview]Local Injection Site Reaction (0-6) Scale at Baseline, 2 Weeks
NCT01461369 (6) [back to overview]Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.
NCT01461369 (6) [back to overview]Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Osteoarthritis Pain, Stiffness, and Function Measured Using the Total (Composite) Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Score.
NCT01461369 (6) [back to overview]Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale.
NCT01461369 (6) [back to overview]Change From Baseline to Week 12 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.
NCT01461369 (6) [back to overview]Change From Baseline to Week 2 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.
NCT01461369 (6) [back to overview]Change From Baseline to Week 6 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.
NCT01462435 (8) [back to overview]Total Pain Relief (TOTPAR) Over 0 to 4 Hours. TOTPAR-4.
NCT01462435 (8) [back to overview]TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours
NCT01462435 (8) [back to overview]TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours
NCT01462435 (8) [back to overview]TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours
NCT01462435 (8) [back to overview]VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry.
NCT01462435 (8) [back to overview]VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.
NCT01462435 (8) [back to overview]VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.
NCT01462435 (8) [back to overview]The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48), ANCOVA Model.
NCT01508676 (3) [back to overview]Clinical Neuropathic Pain Features- Burning After Treatment
NCT01508676 (3) [back to overview]Clinical Neuropathic Pain Features- Constant Pain and Hypersensitivity After Treatment
NCT01508676 (3) [back to overview]VAS After Treatment
NCT01510912 (3) [back to overview]Mean Short Form-36 Mental Component Summary Scores at Week 52/Early Termination (ET) and Change From Baseline to Week 52/ET
NCT01510912 (3) [back to overview]Mean Short Form-36 Physical Component Summary Scores at Week 52/Early Termination (ET) and Change From Baseline to Week 52/ET
NCT01510912 (3) [back to overview]Safety of Diclofenac 35 mg Capsules as Assessed by the Incidence of Adverse Events From Baseline to Week 52 or Early Termination
NCT01511939 (4) [back to overview]Change From Baseline to Week 4 in Laboratory Results of International Normalized Ratio (INR)
NCT01511939 (4) [back to overview]Change From Baseline to Week 4 in Laboratory Results of Partial Thromboplastin Time (PTT)
NCT01511939 (4) [back to overview]Change From Baseline to Week 4 in Laboratory Results of Platelet Aggregation
NCT01511939 (4) [back to overview]Change From Baseline to Week 4 in Laboratory Results of Prothrombin Time (PT)
NCT01666197 (1) [back to overview]Pain on Movement
NCT01706588 (1) [back to overview]Area Under the Curve (AUC) of the Pain Scores.
NCT01943435 (3) [back to overview]Sense Wear Armband
NCT01943435 (3) [back to overview]Swiss Spinal Stenosis (SSS) Questionnaire Score
NCT01943435 (3) [back to overview]Self Paced Walking Test (SPWT)
NCT01967550 (1) [back to overview]Measure: Pain On Movement (POM)
NCT01982539 (3) [back to overview]Percentage Difference of Numeric Pain Rating Scale (NPRS) Pain Score From Baseline to (1) the First Hour and (2) the Second Hour After the First Dose of Zipsor® Administration.
NCT01982539 (3) [back to overview]Changes in the Numeric Pain Rating Scale (NPRS) Pain Score From Baseline to (1) the First Hour and (2) the Second Hour After the First Dose of Zipsor® Administration.
NCT01982539 (3) [back to overview]Safety and Tolerability of Zipsor® in Pediatric Subjects, Ages 12 to 17 Years
NCT02087748 (3) [back to overview]Mean Reduction in SPID Scores of DOMS at Rest Over 24 Hours
NCT02087748 (3) [back to overview]Mean Reduction in SPID Scores of DOMS on Walking Over 24 Hours
NCT02087748 (3) [back to overview]Mean Reduction in SPID Scores of DOMS While Standing Over 24 Hours
NCT02100670 (14) [back to overview]Pain Relief Score (PRS)
NCT02100670 (14) [back to overview]Pain Intensity Difference (PID) on Movement
NCT02100670 (14) [back to overview]Ankle Swelling
NCT02100670 (14) [back to overview]Time to Complete Recovery
NCT02100670 (14) [back to overview]Total Pain Relief (TOTPAR)
NCT02100670 (14) [back to overview]Time of Onset of Pain Relief (TOPR)
NCT02100670 (14) [back to overview]Time of Onset of Meaningful Pain Relief (TOMR)
NCT02100670 (14) [back to overview]Time of Onset of Cooling Sensation (TOCS)
NCT02100670 (14) [back to overview]AUC1-3 Days of PI on Movement for Diclofenac Sodium + Methanol, Diclofenac, Methanol and Placebo
NCT02100670 (14) [back to overview]Sum of Pain Intensity Difference (SPID)
NCT02100670 (14) [back to overview]Area Under the Curve From Day 1 to Day 3 (AUC1-3 Days) of Pain Intensity(PI) on Movement for Diclofenac/Methanol Gel and Placebo Gel
NCT02100670 (14) [back to overview]Skin Temperature
NCT02100670 (14) [back to overview]PID at Rest
NCT02100670 (14) [back to overview]Patient's Global Assessment in Response to Treatment (PGART)
NCT02121002 (1) [back to overview]Change From Baseline to 4 Weeks in WOMAC Pain Score
NCT02132247 (4) [back to overview]Dermatologic Assessment at the Patch Application Site
NCT02132247 (4) [back to overview]Investigator Assessment of the Global Response to Therapy on a 5-point Scale
NCT02132247 (4) [back to overview]Plasma Concentration of Diclofenac
NCT02132247 (4) [back to overview]Patient Assessment of Pain on a 6-point Scale
NCT02194088 (1) [back to overview]Pain Scores on Standardized Experimental Pain Testing
NCT02271854 (2) [back to overview]Sum of Pain Intensity Differences Over 48 Hours After Initiating Treatment (SPID 48), Derived From POW.
NCT02271854 (2) [back to overview]Sum of Pain Intensity Differences Over 24 Hours After Initiating Treatment (SPID 24), Derived From POW.
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.6 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.7 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.8 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.9 of 7).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (2 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (3 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (4 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (7 of 8).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (8 of 8).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (1 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (2 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (3 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (4 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (7 of 7).
NCT02287350 (42) [back to overview]To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (1 of 8).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.1 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.2 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.3 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.4 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.5 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.1 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.10 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.11 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.12 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.13 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.14 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.15 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.16 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.17 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.18 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.19 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.2 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.20 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.21 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.22 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.23 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.24 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.3 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.4 of 7).
NCT02287350 (42) [back to overview]To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.5 of 7).
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (6 of 6)
NCT02287376 (40) [back to overview]Safety Outcome (6.14 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.15 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.16 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.17 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.18 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.19 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.20 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.21 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.22 of 7)
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (3 of 6)
NCT02287376 (40) [back to overview]Safety Outcome (6.23 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.24 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.3 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.4 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.5 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.6 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.7 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.8 of 7)
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (2 of 6)
NCT02287376 (40) [back to overview]Safety Outcome (6.9 of 7)
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (4 of 6)
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (5 of 6)
NCT02287376 (40) [back to overview]Safety Outcome (6.2 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (1 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (2 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (3 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (4 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (7 of 7)
NCT02287376 (40) [back to overview]Pharmacokinetics Outcome (1 of 6)
NCT02287376 (40) [back to overview]Safety Outcome (5.1 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (5.2 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (5.3 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (5.4 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (5.5 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.1 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.10 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.11 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.12 of 7)
NCT02287376 (40) [back to overview]Safety Outcome (6.13 of 7)
NCT02324270 (2) [back to overview]Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment
NCT02324270 (2) [back to overview]Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment
NCT02424578 (1) [back to overview]Plasma Concentration of Diclofenac
NCT02476422 (13) [back to overview]Area Under the Curve (AUC) of Visual Analog Scale of Pain Intensity (VASPI) Measuring Change From Baseline at Different Time Points
NCT02476422 (13) [back to overview]Summed Total Pain Relief (TOTPAR) at Different Time Points
NCT02476422 (13) [back to overview]Sum of Pain Intensity Difference (SPID)
NCT02476422 (13) [back to overview]Peak Analgesic Effect
NCT02476422 (13) [back to overview]Number of Patients With Different Responses Based on Patient's Global Assessment of Response to Treatment (PGART)
NCT02476422 (13) [back to overview]Number of Patients With Any Adverse Events, Serious Adverse Events and Death
NCT02476422 (13) [back to overview]Change From Baseline in Visual Analog Scale of Pain Intensity (VASPI) at Different Time Points
NCT02476422 (13) [back to overview]Time to Onset of Meaningful Pain Relief (MPR)
NCT02476422 (13) [back to overview]Time to Onset of First Perceptible Pain Relief (FPR)
NCT02476422 (13) [back to overview]Time to Confirmed First Perceptible Pain Relief
NCT02476422 (13) [back to overview]Number of Patients Needing Rescue Medication
NCT02476422 (13) [back to overview]Duration of Analgesia
NCT02476422 (13) [back to overview]Change From Baseline in Visual Analog Scale of Pain Intensity (VASPI) at 60 Minutes Post Dose
NCT02495831 (5) [back to overview]Tmax and T1/2
NCT02495831 (5) [back to overview]To Evaluate Plasma Diclofenamic Acid Extent of Exposure Reported as Plasma AUC After Single Administration of 50 mg Diclofenac Sodium, With and Without Co-administration of a Single 200 mg Dose of Safinamide.
NCT02495831 (5) [back to overview]Relative Bioavailability (Frel)
NCT02495831 (5) [back to overview]Lamda z
NCT02495831 (5) [back to overview]Evaluate Diclofenac Rate of Absorption Reported as Plasma Cmax After Single Administration of 50 mg Diclofenac With and Without 200 mg of Safinamide.
NCT02596451 (1) [back to overview]Absolute Change in the Total WOMAC (Western Ontario and McMaster Universities Arthritis Index) Pain Subscale Score for the Target Knee
NCT02666846 (8) [back to overview]Physical Exams to Ensure Safety and Well Being of the Subjects
NCT02666846 (8) [back to overview]To Determine Vital Signs and Electrocardiograms (ECGs) That Were Abnormal to Ensure Safety and Well Being of the Subjects
NCT02666846 (8) [back to overview]Peak Plasma Concentration (Cmax)
NCT02666846 (8) [back to overview]Number of Recorded Abnormal Clinical Assessments
NCT02666846 (8) [back to overview]Intensity of the UVB-induced Erythema (Determined by Assessment of Skin Blood Flow by Laser Doppler Imaging [Flux Units])
NCT02666846 (8) [back to overview]Heat Pain Tolerance Test (HPTT) Measured the Point at Which the Heat Became Painful - Degrees Centigrade -
NCT02666846 (8) [back to overview]Area Under the Plasma Concentration Versus Time Curve
NCT02666846 (8) [back to overview]Adverse Events (AEs)
NCT02700815 (8) [back to overview]Number of Patients With Decrease in POMwp of at Least 30% From Baseline
NCT02700815 (8) [back to overview]Change in POM Between Baseline and Day 2 Evening, 1 Hour After Drug Application
NCT02700815 (8) [back to overview]Change From Baseline in Pressure Algometry (PA) at Day 6 Morning
NCT02700815 (8) [back to overview]Change From Baseline in Pressure Algometry (PA) at Day 2 Evening, Before Drug Application
NCT02700815 (8) [back to overview]Number of Patients With Decrease in POMwp of at Least 50% From Baseline
NCT02700815 (8) [back to overview]Change From Baseline in POMwp (cm) at Day 6 Morning
NCT02700815 (8) [back to overview]POMwp Area Under the Curve (AUC) Calculated From 0 to 72 Hours (h) (POMwp AUC(0-72 h))
NCT02700815 (8) [back to overview]POMwp Area Under the Curve (AUC) Calculated From 0 to 120 Hours (h) (POMwp AUC(0-120 h))
NCT02913521 (2) [back to overview]Mean Change From Baseline to Week 8 in WOMAC Pain Scale, Bioequivalence of Test to Reference.
NCT02913521 (2) [back to overview]An Evaluation to Determine Superiority of Test and Reference Against Placebo in the Mean Change From Baseline to Week 8 in the Total WOMAC Pain Score.
NCT02952898 (1) [back to overview]Number of Subjects With Complete Clearance of AK Lesions
NCT03074162 (5) [back to overview]Area Under the Plasma Concentration-time Curve (AUC) Over One Dosing Interval for Diclofenac at Steady State (AUC0-τ,ss) (τ = 12 Hours) (Day 7)
NCT03074162 (5) [back to overview]Average Plasma Concentration (Cav,ss) for Diclofenac at Steady State
NCT03074162 (5) [back to overview]Maximum Plasma Concentration During a Dosage Interval (Cmax,ss) Obtained Directly From the Concentration-time Data for Diclofenac at Steady State (Day 7)
NCT03074162 (5) [back to overview]Percentage Peak-trough Fluctuation (%PTF), Calculated as [100*(Cmax,ss - Cpre,ss)/Cav,ss]
NCT03074162 (5) [back to overview]Time to Maximum Observed Plasma Concentration at Steady State for Diclofenac at Steady State (Tmax,ss) (Day 7)
NCT03145259 (1) [back to overview]Serum Diclofenac Concentrations
NCT03172780 (2) [back to overview]Mean Change in the Total WOMAC Pain Subscale Score
NCT03172780 (2) [back to overview]Change From Baseline in WOMAC Pain Subscale Score
NCT03277066 (4) [back to overview]WOMAC Stiffness Score Change From Baseline
NCT03277066 (4) [back to overview]WOMAC Physical Function Score
NCT03277066 (4) [back to overview]WOMAC Pain Score Week 2 Change From Baseline
NCT03277066 (4) [back to overview]Evaluate Efficacy & Safety of HP-5000 Topical Patches in Subjects With Osteoarthritis of the Knee: Change in Osteoarthritis Pain Score
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Number of Participants With At-least One Positive Anti-Drug Antibody (ADA) Development
NCT03304379 (18) [back to overview]Serum Concentrations of Functional Fasinumab
NCT03304379 (18) [back to overview]Change From Baseline in PGA Score up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs
NCT03304379 (18) [back to overview]Change From Baseline in Patient Global Assessment (PGA) Score up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Change From Baseline in Weekly Average Walking Index Joint Pain Score up to Week 24 by Using the Numeric Rating Scale (NRS) Pain Scale
NCT03304379 (18) [back to overview]Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 24
NCT03304379 (18) [back to overview]Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 44
NCT03304379 (18) [back to overview]Number of Participants With AA Events Meeting Destructive Arthropathy (DA) Criteria
NCT03304379 (18) [back to overview]Number of Participants With Adjudicated Arthropathy (AA) Events
NCT03304379 (18) [back to overview]Number of Participants With At-least One Peripheral Sensory Adverse Events (AEs)
NCT03304379 (18) [back to overview]Number of Participants With Joint Replacement (JR) Surgery Reported at End of Study (EOS) (Week 72)
NCT03304379 (18) [back to overview]Number of Participants With Sympathetic Nervous System (SNS) Dysfunction Events
NCT03304379 (18) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT03304379 (18) [back to overview]Percentage of Participants With Greater Than or Equal to (≥) 30 Percent (%) Reduction From Baseline up to Week 24 in WOMAC Pain Subscale Score in Participants Treated With Fasinumab Compared to Placebo
NCT03304379 (18) [back to overview]Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo
NCT03471507 (3) [back to overview]Time to the Onset of Action (the First Feeling of 20% Pain Reduction)
NCT03471507 (3) [back to overview]Number of Participants Who Experienced Adverse Effects and/or Complications
NCT03471507 (3) [back to overview]Change in Pain as Measured by Subjective Pain Intensity Rating (SPIR)
NCT03473665 (4) [back to overview]Change of Bath Ankylosing Spondylitis Function Index (BASFI)
NCT03473665 (4) [back to overview]Change of Pain Score
NCT03473665 (4) [back to overview]Change of ASAS Endorsed Disease Activity Score (ASDAS)
NCT03473665 (4) [back to overview]Change of Bath Ankylosing Spondylitis Disease Activity Index (BASDAI)
NCT03497039 (4) [back to overview]Ratio Between Diclofenac Concentration in Treated Knee Synovial Tissue and Plasma After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)
NCT03497039 (4) [back to overview]Ratio Between Diclofenac Concentration in Treated Knee Synovial Fluid and Plasma After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)
NCT03497039 (4) [back to overview]Diclofenac Concentration in Treated Knee Synovial Fluid After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)
NCT03497039 (4) [back to overview]Diclofenac Concentration in Treated Knee Synovial Tissue After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)
NCT03605914 (5) [back to overview]Number of Participants With Bleeding Complications
NCT03605914 (5) [back to overview]Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)
NCT03605914 (5) [back to overview]Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)
NCT03605914 (5) [back to overview]Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)
NCT03605914 (5) [back to overview]Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)
NCT03714672 (10) [back to overview]Subject's Global Evaluation of the Treatment
NCT03714672 (10) [back to overview]Time to Achieve a 50 Percent Reduction in Baseline Pain (Pain at Least Half Gone)
NCT03714672 (10) [back to overview]Time to Onset of First Perceptible Pain Relief
NCT03714672 (10) [back to overview]Pain Relief Expressed as Total Pain Relief (TOTPAR) Over the 4 Hours Post-dose Period (TOTPAR4)
NCT03714672 (10) [back to overview]Time to Intake of First Rescue Medication Dose
NCT03714672 (10) [back to overview]Time to Onset of Meaningful Pain Relief
NCT03714672 (10) [back to overview]Total Pain Relief at 6 Hours Post-dose (TOTPAR6)
NCT03714672 (10) [back to overview]Total Pain Relief at 8 Hours Post-dose (TOTPAR8)
NCT03714672 (10) [back to overview]Incidence and Type of Adverse Events
NCT03714672 (10) [back to overview]Summed Pain Intensity Difference (SPID) at 4, 6, 8, and 24 Hours Post-dose
NCT03861611 (4) [back to overview]Change From Baseline to Day 5 in Functional Impairment
NCT03861611 (4) [back to overview]Frequency of LBP 2 Days After ED Visit
NCT03861611 (4) [back to overview]How Often Participants Used Assigned Medication
NCT03861611 (4) [back to overview]Worst LBP 2 Days After ED Visit
NCT03949673 (3) [back to overview]Number of Participants by Degree of Cartilage Loss
NCT03949673 (3) [back to overview]Number of Participants by Degree of Bony Changes
NCT03949673 (3) [back to overview]Number of Participants by Degree of Synovial Lymphocytic Inflammation
NCT04052620 (11) [back to overview]Total Pain Relief (TOTPAR) From 0 to 24 Hours Post First Dose (Day 1) and From 96 to 120 Hours Post First Dose (Day 5)
NCT04052620 (11) [back to overview]Change From Baseline in Pain on Movement (POM) on Day 5 of Treatment as Assessed by a 100 Millimeter (mm) Visual Analogue Scale (VAS)
NCT04052620 (11) [back to overview]Sum of Pain Intensity Difference (SPID) From 0 to 24 Hours Post First Dose (Day 1) and From 96 to 120 Hours Post First Dose (Day 5)
NCT04052620 (11) [back to overview]Number of Participants With Severity of Adverse Events (AEs) Following Dosing With Study Medication
NCT04052620 (11) [back to overview]Changes From Baseline in Difference of Tenderness Between Affected Ankle and Contralateral Ankle Measured by Algometry on Days 3, 5 and 8
NCT04052620 (11) [back to overview]Change From Baseline of POM on VAS on Day 3 and Day 8 of Treatment Assessed by 100 mm VAS
NCT04052620 (11) [back to overview]Change From Baseline in Tenderness as Measured by Pressure Algometry on Days 3, 5 and 8
NCT04052620 (11) [back to overview]Change From Baseline in Difference of Circumference (Swelling) Between Affected Ankle and Contralateral Ankle by Figure of Eight Method on Days 3, 5 and 8
NCT04052620 (11) [back to overview]Mean Number of Rescue Medication Tablets Used to Treat Ankle Pain
NCT04052620 (11) [back to overview]Change From Baseline in Circumference of Affected Ankle (Swelling) as Measured by Figure of Eight Method on Days 3, 5 and 8
NCT04052620 (11) [back to overview]Change From Baseline in Ankle Joint Function (Karlsson Scoring Scale) on Days 3, 5 and 8
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: IL-8
NCT04067492 (31) [back to overview]Proportion of Patients Who Received a Rescue Therapy Agent
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: IL-1β
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: IL-1α
NCT04067492 (31) [back to overview]Change in the Serum Rate of High-sensitive CRP (Hs-CRP) in Specified Timeframes
NCT04067492 (31) [back to overview]Time to Achieve the 50% Decrease in Pain Intensity in the Assessed Joint Relative to the Baseline
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: IL-6
NCT04067492 (31) [back to overview]Time to Use of the Rescue Medication
NCT04067492 (31) [back to overview]"Proportion of Patients Who Assessed the Response to Therapy With the Test Drug as Excellent or Good"
NCT04067492 (31) [back to overview]Change in Pain Intensity in the Assessed Joint in 15, 30, 45 Minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 Hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 Following the Initiation of Treatment and Compared to Baseline
NCT04067492 (31) [back to overview]Change in the Rate of Serum Amyloid Protein A in the Specified Timeframes
NCT04067492 (31) [back to overview]Proportion of Patients Who Received a Rescue Therapy Agent
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) -Time to Reach Maximum Concentration of the Active Substance - of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) - Terminal Half-life -of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) - Maximum Concentration of the Active Substance -of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) - Area Under the Plasma concentration-of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: Tumor Necrosis Factor (TNF-α)
NCT04067492 (31) [back to overview]Pharmacokinetics (PK) - Area Under the Active Substance Concentration- of RPH-104 Under the Subcutaneous Administration
NCT04067492 (31) [back to overview]Change in the Serum Rates of Cytokines: Interleukin -1 Receptor Antagonist (IL-1RA)
NCT04067492 (31) [back to overview]Change in Pain Intensity in the Assessed Joint 72 Hours After the Initiation of Treatment in Comparison to Baseline
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Disability Index
NCT04067492 (31) [back to overview]Change in the Rate of Erythema of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Eating
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Grip
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Hygiene
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Walking
NCT04067492 (31) [back to overview]Change in the Rate of Movement Restrictions in the Specified Timeframes After Initiation of Treatment
NCT04067492 (31) [back to overview]Change in the Rate of Swelling of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug
NCT04067492 (31) [back to overview]Change in the Rate of Tenderness of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug
NCT04067492 (31) [back to overview]Changes in the Health Assessment Questionnaire (HAQ) Parameters: Arising
NCT04391842 (2) [back to overview]Change in Pain Units on a Scale (0-10) 0 Being Least, 10 Being Worst Pain From Baseline
NCT04391842 (2) [back to overview]Change in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Scores, Ranging From 0 Being No Difficulty to 2400 Being Extreme Difficulty, From Baseline
NCT04766996 (2) [back to overview]Total Post-operative Opioid Requirements With Non-opioid Drug Regimen
NCT04766996 (2) [back to overview]Nebraska Interprofessional Education Attitude Scale (NIPEAS) Score for Professional Staff Arm

Number of Subjects With CSULGIEs by History of GD Ulceration

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
History of GD Ulceration (n=395, 400)No History of GD Ulceration (n=1843, 1846)
Celecoxib713
Oral Diclofenac Plus Omeprazole1368

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Number of Subjects With SUs

Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib5
Oral Diclofenac Plus Omeprazole11

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Number of Subjects With Moderate to Severe Abdominal Symptoms

"Abdominal symptoms were defined by the Medical Dictionary for Regulatory Activities MedDRA System Organ Class (SOC) 'Gastrointestinal Disorders' and keeping high level group term (HLGT) equal to Gastrointestinal Signs and Symptoms." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib132
Oral Diclofenac Plus Omeprazole162

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Number of Subjects With CSULGIES or Symptomatic Ulcers (SUs)

CSULGIE=any of the following: GD hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects with evaluation at an event visit and found to have an ulcer on endoscopy, but did not meet any criteria considered for the primary endpoint by the GI committee were designated as having an SU. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib25
Oral Diclofenac Plus Omeprazole92

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Number of Subjects With Clinically Significant Upper and/or Lower Gastrointestinal Events (CSULGIEs)

CSULGIE=any of the following: gastroduodenal (GD) hemorrhage; gastric outlet obstruction; GD, small or large bowel perforation; small or large bowel hemorrhage; clinically significant anemia of defined GI origin; acute GI hemorrhage of unknown origin, including presumed small bowel hemorrhage; clinically significant anemia of presumed occult GI origin including possible small bowel blood loss. Subjects were assessed by an independent GI Events Adjudication Committee, who were blinded to study treatment assignments. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib20
Oral Diclofenac Plus Omeprazole81

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Number of Subjects With a Clinically Significant Decrease From Baseline in Hematocrit and/or Hemoglobin

A clinically significant decrease from baseline was defined as a fall in hematocrit > = 10 percentage points and/or hemoglobin > = 2 g/dL. (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib45
Oral Diclofenac Plus Omeprazole123

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Number of Subjects Hospitalized in Last 6 Months at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib82
Oral Diclofenac Plus Omeprazole79

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Change From Baseline in Patient's Global Arthritis Assessment at Month 6/Early Termination (ET)

"Subjects rated response to question: Considering all the ways the osteoarthritis or rheumatoid arthritis affects you, how are you doing today? using a 1 to 5 grading scale where 1=very good and 5=very poor." (NCT00141102)
Timeframe: Month 6/Early Termination (ET)

Interventionscores on a scale (Least Squares Mean)
Celecoxib0.754
Oral Diclofenac Plus Omeprazole0.773

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Change From Baseline in Iron Binding Capacity to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmicrogram (ug)/dL (Least Squares Mean)
Celecoxib2.517
Oral Diclofenac Plus Omeprazole1.952

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Change From Baseline in Hemoglobin at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventiongrams (g)/deciliter (dL) (Least Squares Mean)
Celecoxib-0.017
Oral Diclofenac Plus Omeprazole-0.423

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Change From Baseline in Hematocrit at Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionpercent (Least Squares Mean)
Celecoxib-0.306
Oral Diclofenac Plus Omeprazole-1.425

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Change From Baseline in Ferretin to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionug/dL (Least Squares Mean)
Celecoxib-3.396
Oral Diclofenac Plus Omeprazole-1.990

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Change From Baseline in C-Reactive Protein to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

Interventionmg/dL (Least Squares Mean)
Celecoxib0.058
Oral Diclofenac Plus Omeprazole0.073

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Number of Subjects Withdrawn Due to GI Adverse Events (AEs)

"GI AEs were defined using MedDRA SOC Gastrointestinal Disorders but excluding the following HLGTs: Benign Neoplasms Gastrointestinal; Dental and Gingival Conditions; Oral Soft Tissue Conditions; Salivary Gland Conditions; and Tongue Conditions." (NCT00141102)
Timeframe: 6 month treatment duration

Interventionparticipants (Number)
Celecoxib114
Oral Diclofenac Plus Omeprazole167

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Change From Baseline in Hepatic Measures of GGT, AST or ALT to Month 6/ET

(NCT00141102)
Timeframe: Month 6/ET

,
InterventionIU/L (Least Squares Mean)
GGTASTALT
Celecoxib-2.689-0.901-1.151
Oral Diclofenac Plus Omeprazole7.4551.4905.213

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Number of Subjects With Hepatic AEs in Gamma Glutamyl-Transferase (GGT), Aspartate Aminotransferase (AST) or Alanine Aminotransferase (ALT) of 3 Times the Upper Limit of Normal (ULN)

GGT ULN was 49 international units (IU)/liter (L) for females and 61 IU/L for males, AST ULN was 37 IU/L for females and 39 IU/L for males, and ALT ULN was 43 IU/L for females and 45 IU/L for males. (NCT00141102)
Timeframe: 6 month treatment duration

,
Interventionparticipants (Number)
GGTASTALT
Celecoxib26813
Oral Diclofenac Plus Omeprazole861227

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Number of Subjects Alive at the Post Trial Interview

Interview occurred via telephone to obtain follow-up mortality and hospitalization information. (NCT00141102)
Timeframe: 6 months following last dose

Interventionparticipants (Number)
Celecoxib2018
Oral Diclofenac Plus Omeprazole2023

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Tender Joint Count (Out of 68 Joints) Time-Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment Period (All Patients-Treated Population)

(NCT00264147)
Timeframe: Time-weighted average change from baseline across Weeks 2, 7, and 12

InterventionTender Joint Count (Mean)
Placebo-8.13
Etoricoxib 10 mg-11.01
Etoricoxib 30 mg-10.96
Etoricoxib 60 mg-9.56
Etoricoxib 90 mg-12.06

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Swollen Joint Count (Out of 66 Joints) Time-Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment Period (All Patients-Treated Population)

(NCT00264147)
Timeframe: Time-weighted average change from baseline across Weeks 2, 7, and 12

InterventionSwollen Joint Count (Mean)
Placebo-5.39
Etoricoxib 10 mg-6.58
Etoricoxib 30 mg-6.91
Etoricoxib 60 mg-6.25
Etoricoxib 90 mg-7.77

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Proportion of Patients Who Met the ACR20 Responder Index Criteria

Proportion of Patients Who Met the American College of Rheumatology Response Index (20%) Criteria (ACR20) (Based on the Time-Weighted Average Responses of the 12-Week Treatment I Period and Completed the Treatment I Period) (All Patients-Treated Population) (NCT00264147)
Timeframe: 12 weeks

InterventionProportion of Patients (Number)
Placebo28.57
Etoricoxib 10 mg35.06
Etoricoxib 30 mg37.75
Etoricoxib 60 mg38.57
Etoricoxib 90 mg47.10

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Patient Global Assessment of Pain (0- to 100-mm Visual Analog Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)

0-mm indicates very well, 100-mm indicates very poor. (NCT00264147)
Timeframe: Time-weighted average change from baseline across Weeks 2, 7, and 12

InterventionUnits on a Scale (Mean)
Placebo-17.44
Etoricoxib 10 mg-21.95
Etoricoxib 30 mg-22.75
Etoricoxib 60 mg-22.25
Etoricoxib 90 mg-31.07

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Patient Global Assessment of Disease Activity (0- to 100-mm Visual Analog Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)

0-mm indicates very well, 100-mm indicates very poor. (NCT00264147)
Timeframe: Time-weighted average change from baseline across Weeks 2, 7, and 12

InterventionUnits on a Scale (Mean)
Placebo-12.32
Etoricoxib 10 mg-19.90
Etoricoxib 30 mg-21.12
Etoricoxib 60 mg-21.49
Etoricoxib 90 mg-25.75

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Investigator Global Assessment of Disease Activity (0- to 4-Likert Scale) Time Weighted Average Change From Baseline (Flare/Randomization Visit) in the 12-Week Treatment I Period (All Patients-Treated Population)

0 indicates very well, 4 indicates very poor. (NCT00264147)
Timeframe: Time-weighted average change from baseline across Weeks 2, 7, and 12

InterventionUnits on a Scale (Mean)
Placebo-0.68
Etoricoxib 10 mg-0.93
Etoricoxib 30 mg-1.09
Etoricoxib 60 mg-1.01
Etoricoxib 90 mg-1.24

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Total Pain Relief (TOTPAR) Scores 8 Hours Post Initial Dose of Study Drug

Pain relief was rated using a 5-point categorial scale (0=none, 1=a little, 2=some, 3=a lot, and 4=complete) at time of dose (time=0) and over 15 time points afterwards (10, 15, 20, 30, 45, and 60 minutes and at 1.5, 2, 2.5, 3, 4, 5, 6, 7, and 8 hours after the initial dose on Day 1 or until time of re-medication). A score of 0 across all time points would be the lowest (worst) and a score of 60 (4 X 15 time points) would be the highest (best) possible score. (NCT00366444)
Timeframe: 8 hours post single dose

Interventionunits on a scale (Mean)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule8.2
Placebo2.6

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Time to Onset of at Least 30% Reduction in Pain Intensity After First Dose of Study Drug

(NCT00366444)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule60

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Number of Patients With Meaningful Pain Relief on Day 1

Times to onset of Perceptible and Meaningful Relief were determined using the double-stopwatch method. (NCT00366444)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule58
Placebo35

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Number of Patients With at Least 30% Reduction in Pain Intensity After First Dose of Study Drug

(NCT00366444)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule62
Placebo40

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Number of Patients Who Required Rescue Medication on Day 3

Day 3 data reflect the use of rescue medication only up to the time of discharge (NCT00366444)
Timeframe: Day 3

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule5
Placebo29

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Number of Patients Who Required Rescue Medication on Day 2

(NCT00366444)
Timeframe: Day 2

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule22
Placebo64

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Median Time to Onset of Pain Relief in Patients With Meaningful Pain Relief on Day 1

(NCT00366444)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule70.2

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Median Time to Onset of Pain Relief in Patients With Perceptible Pain Relief on Day 1

(NCT00366444)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule26.0
Placebo22.2

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Average Numeric Pain Rating Score (NPRS) Over 48 Hours After Bunionectomy

Pain intensity scores were measured using an 11-point numerical pain rating scale (NPRS) with 0=no pain to 10=worst possible pain (NCT00366444)
Timeframe: Over 48 hours after bunionectomy

Interventionunits on a scale (Mean)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule2.5
Placebo5.6

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Number of Patients Who Required Rescue Medication on Day 1

(NCT00366444)
Timeframe: Day 1

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule40
Placebo87

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Number of Patients With Perceptible Pain Relief on Day 1

Times to onset of Perceptible and Meaningful Relief were determined using the double-stopwatch method. (NCT00366444)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule84
Placebo69

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Number of Patients With at Least 30% Reduction in Pain Intensity After First Dose of Study Drug

(NCT00375934)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule51
Placebo31

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Number of Patients Who Required Rescue Medication on Day 3

Day 3 data reflect the use of rescue medication only up to the time of discharge. (NCT00375934)
Timeframe: Day 3

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule4
Placebo19

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Total Pain Relief (TOTPAR) Scores 8 Hours Post Initial Dose of Study Drug

Pain relief was rated using a 5-point categorial scale (0=none, 1=a little, 2=some, 3=a lot, and 4=complete) at time of dose (time=0) and over 15 time points afterwards (10, 15, 20, 30, 45, and 60 minutes and at 1.5, 2, 2.5, 3, 4, 5, 6, 7, and 8 hours after the initial dose on Day 1 or until time of re-medication). A score of 0 across all time points would be the lowest (worst) and a score of 60 (4 X 15 time points) would be the highest (best) possible score. (NCT00375934)
Timeframe: 8 hourse post single dose

Interventionunits on a scale (Mean)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule5.9
Placebo1.9

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Time to Onset of at Least 30% Reduction in Pain Intensity After First Dose of Study Drug

(NCT00375934)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule110
Placebo300

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Number of Patients With Perceptible Pain Relief on Day 1

Times to onset of Perceptible and Meaningful Relief were determined using the double-stopwatch method. (NCT00375934)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule72
Placebo63

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Number of Patients With Meaningful Pain Relief on Day 1

Times to onset of Perceptible and Meaningful Relief were determined using the double-stopwatch method. (NCT00375934)
Timeframe: 8 hours post single dose

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule50
Placebo30

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Average Numeric Pain Rating Score (NPRS) Over 48 Hours After Bunionectomy

Pain intensity scores were measured using an 11-point numerical pain rating scale (NPRS) with 0=no pain to 10=worst possible pain (NCT00375934)
Timeframe: Over 48 hours after bunionectomy

Interventionunits on a scale (Mean)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule3.3
Placebo5.7

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Number of Patients Who Required Rescue Medication on Day 2

(NCT00375934)
Timeframe: Day 2

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule30
Placebo68

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Number of Patients Who Required Rescue Medication on Day 1

(NCT00375934)
Timeframe: Day 1

Interventionparticipants (Number)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule53
Placebo93

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Median Time to Onset of Pain Relief in Patients With Perceptible Pain Relief on Day 1

(NCT00375934)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule42.9
Placebo36.0

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Median Time to Onset of Pain Relief in Patients With Meaningful Pain Relief on Day 1

(NCT00375934)
Timeframe: 8 hours post single dose

Interventionminutes (Median)
Zipsor (Diclofenac Potassium) Liquid Filled Capsule90.6

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Macular Thickness Measured With the OCT; in Relation to Age, Sex, Reproductive Factors and the Use of Anti-inflammatory Eye Drops in Health; in Uncomplicated Anterior Uveitis.

Macular thickness was assessed with the OCT in healthy subjects and in patients with anterior uveitis. Data was analyzed with respect to age, sex, parity, the use of hormonal therapy, after treatment with to types of anti-inflammatory eye drops, and in uncomplicated uveitis. (NCT00476593)
Timeframe: Macular thickness measured with the OCT

InterventionMacular Thickness in micron (Mean)
A Diclofenac268
B Dexamethasone272
Patients With Anterior Uveitis276
Healthy Volunteers267

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Total Pain Relief (TOTPAR)

Pain relief values at specified time points were measured on a 0 to 100 mm VAS, where higher values indicate greater pain relief. TOTPAR over specified time interval was calculated as area under pain relief curve over specified time intervals using trapezoidal approximation. For 0-24 hours score range was 0-2400, for 0-48 hours score range was 0- 4800, for 0-96 hours score range was 0-9600 and for 0-120 hours score range was 0-12000. Higher TOTPAR values indicated more relief. (NCT00507026)
Timeframe: 0-24, 0-48, 0-72, 0-96 and 0-120 hours post first dose

,,
Interventionmm*hours (Mean)
0-24 hours0-48 hours0-72 hours0-96 hours0-120 hours
Diclofenac (DIC075V)1177.62768.34471.06252.28042.5
Ketorolac1065.42453.83983.65575.77178.0
Placebo484.71327.92214.63159.44105.4

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Sum of the Pain Intensity Differences (SPID) Over 120 Hours

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). A positive difference is indicative of improvement. SPIDs was calculated by multiplying the PID score at each post-dose time point by the duration (in hours) since the preceding time point and then summing these values over the specific time period. SPID over 120 hours ranges from -12000 to 12000. A higher value indicates a better pain reduction. (NCT00507026)
Timeframe: Over 120 hours post first dose

Interventionmm*hours (Mean)
Diclofenac (DIC075V)4835.6
Ketorolac4359.1
Placebo1840.5

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Sum of the Pain Intensity Differences (SPID) Over 24 Hours

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, pain intensity difference (PID) is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). A positive difference is indicative of improvement. SPIDs was calculated by multiplying the PID score at each post-dose time point by the duration (in hours) since the preceding time point and then summing these values over the specific time period. SPID over 24 hours ranges from -2400 to 2400. A higher value indicates a better pain reduction. (NCT00507026)
Timeframe: Over 24 hours post first dose

Interventionmm*hours (Mean)
Diclofenac (DIC075V)577.0
Ketorolac563.2
Placebo28.0

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Percentage of Participants Attaining Greater Than or Equal to (>=) 30 Percent (%) Reduction From Baseline in Pain Intensity

Pain intensity was measured on a 0 to 100 mm VAS, larger values indicate greater pain intensity. In this outcome measure, percentage of participants attaining >= 30 % reduction in pain intensity from baseline to specified time points was reported. (NCT00507026)
Timeframe: Baseline (0 hour), 5, 30 minutes post first dose, 1, 24, 48, 72, 90, 120 hours post first dose

,,
InterventionPercentage of participants (Number)
At 5 minutesAt 30 minutesAt 1 hourAt 24 hoursAt 48 hoursAt 72 hoursAt 90 hoursAt 120 hours
Diclofenac (DIC075V)13.843.444.862.175.280.080.080.7
Ketorolac10.035.041.756.763.371.775.075.0
Placebo8.325.015.331.0941.741.743.143.1

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Participant Global Evaluation Over Time

Participants global evaluation of study medication was accessed on a scale ranging from scale 0 to 4 where 0= poor, 1= fair, 2= good, 3= very good, 4= excellent where higher score represented better outcome. (NCT00507026)
Timeframe: 0-24, 0-48, 0-120 hours post-dose

,,
InterventionUnits on a scale (Mean)
0-24 Hours0-48 Hours0-120 Hours
Diclofenac (DIC075V)2.62.92.9
Ketorolac2.42.62.6
Placebo1.11.91.3

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Pain Intensity Differences (PID) Over Time

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). PID score range at any post dose (post baseline) evaluation time point was -100 to 100. A positive difference score is indicative of improvement. (NCT00507026)
Timeframe: Baseline (0 hour), 5, 10, 15, 30, 45 minutes post first dose, 1, 2, 3, 5, 6, 9, 12, 15, 18, 21, 24, 48, 72, 96, 120 hours post first dose

,
Interventionmm (Mean)
At 5 minutesAt 10 minutesAt 15 minutesAt 30 minutesAt 45 minutesAt 1 hourAt 2 hoursAt 3 hoursAt 5 hoursAt 6 hoursAt 9 hoursAt 12 hoursAt 15 hoursAt 18 hoursAt 21 hoursAt 24 hoursAt 48 hoursAt 72 hoursAt 96 hoursAt 120 hours
Diclofenac (DIC075V)5.29.113.417.718.518.717.313.510.812.623.623.428.530.236.331.842.947.046.846.9
Ketorolac3.25.59.816.718.419.716.914.715.112.521.323.723.230.139.127.535.541.043.042.9

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Pain Intensity Differences (PID) Over Time

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). PID score range at any post dose (post baseline) evaluation time point was -100 to 100. A positive difference score is indicative of improvement. (NCT00507026)
Timeframe: Baseline (0 hour), 5, 10, 15, 30, 45 minutes post first dose, 1, 2, 3, 5, 6, 9, 12, 15, 18, 21, 24, 48, 72, 96, 120 hours post first dose

Interventionmm (Mean)
At 5 minutesAt 10 minutesAt 15 minutesAt 30 minutesAt 45 minutesAt 1 hourAt 2 hoursAt 3 hoursAt 5 hoursAt 6 hoursAt 9 hoursAt 12 hoursAt 15 hoursAt 18 hoursAt 21 hoursAt 24 hoursAt 48 hoursAt 72 hoursAt 120 hours
Placebo1.22.42.22.6-1.2-4.2-7.8-8.9-7.3-6.1-1.81.41.18.78.812.919.420.320.9

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Number of Participants According to Frequency of Use of Rescue Medication

In this outcome measure, number of participants are reported according to number of times they received rescue medication. Rescue medication was additional pain medication, available to participants if they did not receive pain relief from the study drug. Rescue medication available during this study was IV morphine. Only those categories with at least one nonzero value are reported. (NCT00507026)
Timeframe: 0-24, 0-48, 0-72, 0-96 and 0-120 hours post first dose

,,
InterventionParticipants (Count of Participants)
0 - 24 Hours: 00 - 24 Hours: 10 - 24 Hours: 20 - 24 Hours: 30 - 24 Hours: 40 - 24 Hours: 50 - 24 Hours: 60 - 24 Hours: 70 - 24 Hours: 80 - 24 Hours: 90 - 24 Hours: 110 - 24 Hours: 120 - 24 Hours: 130 - 24 Hours: 140 - 24 Hours: 150-48 hours: 00-48 hours: 10-48 hours: 20-48 hours: 30-48 hours: 40-48 hours: 50-48 hours: 60-48 hours: 70-48 hours: 80-48 hours: 90-48 hours: 100-48 hours: 110-48 hours: 120-48 hours: 130-48 hours: 140-48 hours: 150-48 hours: 170-48 hours: 200-72 hours: 00-72 hours: 10-72 hours: 20-72 hours: 30-72 hours: 40-72 hours: 50-72 hours: 60-72 hours: 70-72 hours: 80-72 hours: 90-72 hours: 100-72 hours: 110-72 hours: 120-72 hours: 130-72 hours: 140-72 hours: 150-72 hours: 170-72 hours: 190-72 hours: 200-72 hours: 210-96 hours: 00-96 hours: 10-96 hours: 20-96 hours: 30-96 hours: 40-96 hours: 50-96 hours: 60-96 hours: 70-96 hours: 80-96 hours: 90-96 hours: 100-96 hours: 110-96 hours: 120-96 hours: 130-96 hours: 140-96 hours: 150-96 hours: 170-96 hours: 190-96 hours: 200-96 hours: 210-120 hours: 00-120 hours: 10-120 hours: 20-120 hours: 30-120 hours: 40-120 hours: 50-120 hours: 60-120 hours: 70-120 hours: 80-120 hours: 90-120 hours: 100-120 hours: 110-120 hours: 120-120 hours: 130-120 hours: 140-120 hours: 150-120 hours: 170-120 hours: 190-120 hours: 200-120 hours: 21
Diclofenac (DIC075V)392626198973231110038232414117863423110000382322151168443532100000038232215116753353310000003823221511675335331000000
Ketorolac176984335211100016510523243421210000165105222421421102100016510522242133110210001651052224213221021000
Placebo476119937443211114761038583505311111476103576299023120111476103567290231220111476103567290231220111

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Sum of the Pain Intensity Differences (SPID) Over 72 Hours

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). A positive difference is indicative of improvement. SPIDs was calculated by multiplying the PID score at each post-dose time point by the duration (in hours) since the preceding time point and then summing these values over the specific time period. SPID over 72 hours ranges from -7200 to 7200. A higher value indicates a better pain reduction. (NCT00507026)
Timeframe: Over 72 hours post first dose

Interventionmm*hours (Mean)
Diclofenac (DIC075V)2592.1
Ketorolac2312.1
Placebo836.8

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Cumulative Amount of Rescue Medication

In this outcome measure, cumulative amount of rescue medication used over 0-24, 0-48, 0-72, 0-96, and 0-120 hours were reported. Rescue medication was additional pain medication, available to participants if they did not receive pain relief from the study drug. Rescue medication available during this study was IV morphine. (NCT00507026)
Timeframe: 0-24, 0-48, 0-72, 0-96 and 0-120 hours

,,
Interventionmg (Mean)
0-24 hours0-48 hours0-72 hours0-96 hours0-120 hours
Diclofenac (DIC075V)9.411.111.711.811.8
Ketorolac11.515.518.018.118.1
Placebo16.019.020.520.520.5

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Time to Perceptible Relief

Participants were instructed to stop the first stopwatch at the onset of perceptible pain relief after first dose. Event times of participants not reporting perceptible relief were censored at 6 hours; event times of participants who withdrew or were administered rescue medication were censored at time of withdrawal or rescue. Kaplan-Meier estimate was used for analysis. (NCT00507026)
Timeframe: Within 6 hours of first dose on Day 1

InterventionMinutes (Median)
Diclofenac (DIC075V)10.0
Ketorolac14.4
Placebo15.0

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Time to Meaningful Relief

Participants were instructed to stop the second stopwatch at the onset of meaningful pain relief after first dose. Event times of participants not reporting meaningful relief were censored at 6 hours; event times of participants who withdrew or were administered rescue medication were censored at time of withdrawal or rescue. Kaplan-Meier estimate was used for analysis. (NCT00507026)
Timeframe: Within 6 hours of first dose on Day 1

InterventionMinutes (Median)
Diclofenac (DIC075V)41.6
Ketorolac42.5
PlaceboNA

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Time From Administration of Study Drug to Administration of Rescue Medication

Time from administration of study drug to administration of rescue medication were censored at time of last pain assessment for participants who did not receive rescue medication. Rescue medication was additional pain medication, available to participants if they did not receive pain relief from the study drug. Rescue medication available during this study was IV morphine. (NCT00507026)
Timeframe: Maximum up to 5 days

InterventionMinutes (Median)
Diclofenac (DIC075V)220.0
Ketorolac137.0
Placebo51.0

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Sum of the Pain Intensity Differences (SPID) Over 96 Hours

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). A positive difference is indicative of improvement. SPIDs was calculated by multiplying the PID score at each post-dose time point by the duration (in hours) since the preceding time point and then summing these values over the specific time period. SPID over 96 hours ranges from -9600 to 9600. A higher value indicates a better pain reduction. (NCT00507026)
Timeframe: Over 96 hours post first dose

Interventionmm*hours (Mean)
Diclofenac (DIC075V)3711.3
Ketorolac3331.9
Placebo1337.8

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Visual Analog Pain Relief Values Over the Time

Pain relief values at specified time points were measured on a 0 to 100 mm VAS, where higher values indicate greater pain relief. (NCT00507026)
Timeframe: 5, 10, 15, 30, 45 minutes post first dose, 1, 2, 3, 5, 6, 9, 12, 15, 18, 21, 24, 48, 72, 96, 120 hours post first dose

,,
Interventionmm (Mean)
At 5 minutesAt 10 minutesAt 15 minutesAt 30 minutesAt 45 minutesAt 1 hourAt 2 hoursAt 3 hoursAt 5 hoursAt 6 hoursAt 9 hoursAt 12 hoursAt 15 hoursAt 18 hoursAt 21 hoursAt 24 hoursAt 48 hoursAt 72 hoursAt 96 hoursAt 120 hours
Diclofenac (DIC075V)21.927.133.539.741.640.035.333.528.836.749.551.655.756.663.659.769.474.474.674.6
Ketorolac17.923.627.233.933.337.833.229.531.033.939.446.345.953.663.253.460.864.867.066.9
Placebo15.319.021.623.119.917.110.18.08.012.617.521.621.428.327.432.538.238.839.439.4

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Sum of the Pain Intensity Differences (SPID) Over 48 Hours

Pain intensity was measured on VAS (from 0 mm to 100 mm: 0 = no pain, 100 = worst possible pain). For each post dose time point, PID is derived by subtracting the pain intensity at the post dose time point from the baseline intensity score (baseline score - post-baseline score). A positive difference is indicative of improvement. SPIDs was calculated by multiplying the PID score at each post-dose time point by the duration (in hours) since the preceding time point and then summing these values over the specific time period. SPID over 48 hours ranges from -4800 to 4800. A higher value indicates a better pain reduction. (NCT00507026)
Timeframe: Over 48 hours post first dose

Interventionmm*hours (Mean)
Diclofenac (DIC075V)1527.5
Ketorolac1371.8
Placebo400.4

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Pain on Movement on Day 5 (Change From Baseline). A Greater Change From Baseline on Day 5 Equates to a Better Outcome.

Pain on movement: visual analogue scale (VAS) with anchors at 0 mm (no pain) and 100 mm (extreme pain) (NCT00573768)
Timeframe: change from baseline (on day 1) to day 5

Interventionmm (Mean)
Diclofenac Diethylamine (DDEA) 2.32% Gel BID38.3
DDEA 2.32% Gel OD35.7
Vehicle Gel33.4

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Number of Participants With Duodenal Ulcers Confirmed by Endoscopy

Number of participants with duodenal ulcers confirmed by endoscopy following administration of PN 400 VIMOVO)or Arthrotec in a high risk population (NCT00594854)
Timeframe: 6 months

Interventionparticipants (Number)
PN400 (VIMOVO)0
Arthrotec1

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Number of Participants With Gastric Ulcer Confirmed by Endoscopy

Number of participants with gastric ulcers confirmed by endoscopy following administration of PN 400 (VIMOVO) or Arthrotec in a high risk population over six months. (NCT00594854)
Timeframe: 6 months

InterventionParticipants (Number)
PN400 (VIMOVO)2
Arthrotec1

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Number of Participants With Upper Gastro-intestinal Injury Grade 4 as Measured by Lanza (1991) Score

The degree of upper gastrointestinal (UGI) injury as measured by Lanza scores (1991) during treatment with PN 400 and ARTHROTEC® in a high-risk population. The Lanza (1991) score is based on endoscopic obeservations and rating these, with no damage, petecchiae, erosions and ulcers. On the 1991 scale, a Lanza score of 0 represents normal mucosa (no damage), while a score of 4 indicates 6-10 erosions, and a score of 7 indicates an ulcer. (NCT00594854)
Timeframe: 6 months

Interventionparticipants (Number)
PN400 (VIMOVO)2
Arthrotec2

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Safety of Combination Therapy With Topical Eflornithine Hydrochloride Ointment and Topical Diclofenac Sodium Gel Over 3-months

Adverse events were compared across three treatment groups by severity determined by the clinician. All adverse events were resolved by the end of follow up. (NCT00601640)
Timeframe: 3 months

,,
Interventionparticipants (Number)
Burning and Stinging NoneBurning and stinging Mildburning and stinging ModerateBurning and Stinging SeverePruritis NonePruritis MildPruritis ModeratePruritis SevereRash, Redness. Erythema-NoneRash, Redness. Erythema-MildRash, Redness. Erythema-ModerateRash, Redness. Erythema-Severe
Diclofenac Sodium44800331261341080
Eflornithine Hydrochloride484004291046510
Eflornithine Hydrochloride/Diclofenac Sodium483104066040750

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Changes in Putrescine Over 3 Months

Putrescine is measured in nmole/g skin per biopsy. Baseline and End of Study biopsies were measured and the change was produced by subtracting baseline levels from End of Study levels. There was one baseline biopsy and one End of Study biopsy per participant. (NCT00601640)
Timeframe: 3 months

Interventionnmol/g skin (Mean)
Eflornithine Hydrochloride0.03
Diclofenac Sodium1.45
Eflornithine Hydrochloride/Diclofenac Sodium0.2

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Change in Histologic Score Diagnosis and Treatment Group

Change scores were computed by subtracting baseline histologic score from End of Study histologic score. Slides were formalin fixed. Histologic Score has been developed by this research group over the course of Grant (reference below). A standardized form captures data on the following criteria: basal or suprabasilar pleomorphism (atypia); inflammation; hyperkeratosis; parakeratosis. The atypia and inflammation were rated as: none (0), mild to moderate(1), and severe (2). The remaining criteria were rated as present (1) or absent (0). Histologic Scores were computed by adding together the codes for the histologic criteria. Higher scores reflected higher level of epidermal /dermal damage. (NCT00601640)
Timeframe: 3 months

Interventionunits on a scale (Mean)
Eflornithine Hydrochloride0.33
Diclofenac Sodium0.26
Eflornithine Hydrochloride/Diclofenac Sodium0.64

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Change From Baseline in Blood Pressure at Study Discharge/Early Termination

Change from baseline in systolic blood pressure (SBP) and diastolic blood pressure (DBP) in millimeter of mercury (mmHg) was reported. The blood pressure was assessed after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Study discharge/early termination (maximum up to 5 days)

InterventionmmHg (Mean)
SBPDBP
DIC075V-2.2-0.5

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Change From Baseline in Blood Pressure at Clinic Follow-up Visit

Change from baseline in SBP and DBP in mmHg was reported. The blood pressure was assessed after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Clinic follow-up visit (4-10 days after last dose, maximum up to 15 days)

InterventionmmHg (Mean)
SBPDBP
DIC075V0.24.4

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Number of Participants With Clinically Significant Electrocardiogram (ECG) Abnormalities at Study Discharge/Early Termination

12-lead ECG parameters were evaluated. Clinically significant abnormal ECG findings were based on investigator's discretion. (NCT00726388)
Timeframe: Study discharge/early termination (maximum up to Day 5)

InterventionParticipants (Count of Participants)
DIC075V13

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Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An adverse event (AE) was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. TEAEs were events between first dose of study drug and up to 37 days after last dose that were absent before treatment or that worsened relative to pretreatment state. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. TEAEs included SAEs and all non-SAEs that occurred during the study. (NCT00726388)
Timeframe: Day 1 of dosing up to maximum of 37 days after last dose (maximum up to 42 days)

InterventionParticipants (Count of Participants)
TEAEsSAEs
DIC075V82373

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Number of Participants With Clinically Significant Physical Examination Abnormalities at Clinic Follow-up Visit

Physical examination included the assessment of general appearance, skin; HEENT; neck/thyroid; oral cavity; lymph nodes; cardiovascular; lungs; abdomen; genitourinary; neurologic and joints/extremities. Clinically significant physical examination findings were based on investigator's discretion. (NCT00726388)
Timeframe: Clinic follow-up visit (4-10 days after last dose, maximum up to 15 days)

InterventionParticipants (Count of Participants)
General appearanceSkinHEENTNeck/ThyroidOral CavityLymph NodesCardiovascularLungsBreastsAbdomenGenitourinaryNeurologicJoints/Extremities
DIC075V8132100550121541

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Number of Participants With Clinically Significant Electrocardiogram (ECG) Abnormalities at Baseline

12-lead ECG parameters were evaluated. Clinically significant abnormal ECG findings were based on investigator's discretion. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing)

InterventionParticipants (Count of Participants)
DIC075V14

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Number of Participants With Abnormal Urinalysis Findings

Urine parameters included gravity, glucose, protein, and bilirubin. Abnormalities were judged by the investigator. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing) up to study discharge/early termination (maximum up to Day 5)

InterventionParticipants (Count of Participants)
DIC075V2

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Number of Participants Who Took at Least 1 Concomitant Medication

Concomitant medications were medications that were taken concurrently on or after first dose of study drug. (NCT00726388)
Timeframe: Day 1 of dosing up to maximum of 37 days after last dose (maximum up to 42 days)

InterventionParticipants (Count of Participants)
DIC075V971

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Change From Baseline in Respiratory Rate at Study Discharge/Early Termination

Respiratory rate was measured after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Study discharge/early termination (maximum up to 5 days)

InterventionBreaths per minute (Mean)
DIC075V1.3

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Change From Baseline in Respiratory Rate at Clinic Follow-up Visit

Respiratory rate was measured after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Clinic follow-up visit (4-10 days after last dose, maximum up to 15 days)

InterventionBreaths per minute (Mean)
DIC075V1.0

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Change From Baseline in Heart Rate at Study Discharge/Early Termination

Change from baseline in heart rate in beats per minute was reported. The heart rate was assessed after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Study discharge/early termination (maximum up to 5 days)

InterventionBeats per minute (Mean)
DIC075V3.8

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Number of Participants With Wound Assessment at Study Discharge/Early Termination

"Wound assessment had 6 questions, completed by investigator/sub-investigator. Question related to extent of healing; extent and degree of inflammation and extent of drainage had options: much better than expected, better than expected, normal, slower than expected, and much slower than expected. Question related to separation of surgical incision had options: no separation, barely detectible separation, localized separation, mostly separated, and complete separation (dehiscence). Question related to infection at surgical site had options: definitely, no infection, possibly infected, probably infected, certainly infected, and abscess/gross cellulitis. Question related to prescription of postoperative systemic antibiotics had options: no, yes for prophylaxis, and yes for infection. Every question there was category Not Done for participants with no wound assessment other than the reason 'missing' and category Missing, where participants were missing for wound assessment." (NCT00726388)
Timeframe: Study discharge/early termination (maximum up to Day 5)

InterventionParticipants (Count of Participants)
Extent of healing: Much better than expectedExtent of healing: Better than expectedExtent of healing: NormalExtent of healing: Slower than expectedExtent of healing: Much slower than expectedExtent of healing: Not doneExtent of healing: MissingExtent and degree of Inflammation: Much better than expectedExtent and degree of inflammation: Better than expectedExtent and degree of Inflammation: NormalExtent and degree of Inflammation: Slower than expectedExtent and degree of Inflammation: Much slower than expectedExtent and degree of inflammation: Not doneExtent and degree of inflammation: MissingExtent of drainage: Much better than expectedExtent of drainage: Better than expectedExtent of drainage: NormalExtent of drainage: Slower than expectedExtent of drainage: Much slower than expectedExtent of drainage: Not doneExtent of drainage: MissingSeparation of Incision: No separationSeparation of Incision: Barely detectable separationSeparation of incision: Localized separationSeparation of incision: Mostly separatedSeparation of incision: Complete separationSeparation of incision: Not doneSeparation of incision: MissingInfection at surgical site: Definitely, No infectionInfection at surgical site: Possibly infectedInfection at surgical site: Probably infectedInfection at surgical site: Certainly infectedInfection at surgical site: Abscess or gross cellulitisInfection at surgical site: Not doneInfection at surgical site: MissingPostoperative systemic antibiotics: NoPostoperative systemic antibiotics: Yes, for prophylaxisPostoperative systemic antibiotics: Yes, for infectionPostoperative systemic antibiotics: Not donePostoperative systemic antibiotics: Missing
DIC075V401547271103365021465711033678195633291332809873500337921121103336732621332

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Number of Participants With Clinically Significant Physical Examination Abnormalities at Screening

Physical examination included the assessment of general appearance, skin; head, ears, eyes, nose, and throat (HEENT); neck/thyroid; oral cavity; lymph nodes; cardiovascular; lungs; abdomen; genitourinary; neurologic and joints/extremities. Clinically significant physical examination findings were based on investigator's discretion. (NCT00726388)
Timeframe: Screening (0 to 21 days prior to surgery)

InterventionParticipants (Count of Participants)
General AppearanceSkinHEENTNeck/ThyroidOral CavityLymph NodesCardiovascularLungsBreastsAbdomenGenitourinaryNeurologicJoints/Extremities
DIC075V837120300293210295

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Change From Baseline in Heart Rate at Clinic Follow-up Visit

Change from baseline in heart rate in beats per minute was reported. The heart rate was assessed after the participant had taken rest for 5 minutes. (NCT00726388)
Timeframe: Baseline (Day 1, immediately before dosing), Clinic follow-up visit (4-10 days after last dose, maximum up to 15 days)

InterventionBeats per minute (Mean)
DIC075V2.4

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Change From Baseline in Fingertips to Floor Distance at Weeks 2, 4, and 6

Fingertips to floor distance measured in centimeter (cm) from the tip of the fingers to the floor with participants standing erect and feet together, knees as straight as possible, then bending forward as far as possible with fingers reaching towards the floor. The better of 2 tries was recorded. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventioncm (Least Squares Mean)
Week 2 (n=117, 115)Week 4 (n=118, 115)Week 6 (n=118, 115)
Celecoxib 200 mg-1.6-1.9-2.8
Diclofenac SR 75 mg-1.6-2.2-3.1

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Change From Baseline in Nocturnal Pain at Weeks 2, 4, and 6

"100-mm VAS scores specified participant's nocturnal pain in response to the following question Did you have any pain in the neck, back or hips during the previous night? 0=no pain to 100=worst pain possible. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-12.0-14.5-15.4
Diclofenac SR 75 mg-16.3-17.1-19.4

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 12

"100-mm VAS score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Lower scores indicated less pain. Change from baseline of <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg63.4-28.4
Celecoxib 200 mg, Then Celecoxib 400 mg63.4-20.8
Diclofenac SR 75 mg61.1-30.9
Diclofenac SR 75 mg, Then Celecoxib 400 mg65.6-28.1

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Weeks 2 and 4

"100-mm VAS score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Change from baseline of <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)
Celecoxib 200 mg-18.6-20.7
Diclofenac SR 75 mg-17.9-23.3

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Change From Baseline in Participant's Global Assessment of Disease Activity at Week 12

"5-point Likert scale scores specified participant's current situation in response to the following question Considering all the ways your Ankylosing Spondylitis affects you, how are you doing today? 1=very good to 5=very poor. Lower scores indicated better health. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionunits on a scale (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.1-0.6
Celecoxib 200 mg, Then Celecoxib 400 mg3.2-0.4
Diclofenac SR 75 mg3.0-0.6
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.2-0.6

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Change From Baseline in Participant's Global Assessment of Disease Activity at Weeks 2, 4, and 6

"5-point Likert scale scores specified participant's current situation in response to the following question Considering all the ways your Ankylosing Spondylitis affects you, how are you doing today? 1=very good to 5=very poor. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionunits on a scale (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.4-0.3-0.3
Diclofenac SR 75 mg-0.4-0.4-0.4

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Change From Baseline in Physician's Global Assessment of Disease Activity at Week 12

5-point Likert scale scores specified physician's subjective assessment on how the overall ankylosing spondylitis appeared at the time of the participant's visit and participant's disease signs. 1=very good to 5=very poor. Lower scores indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionunits on a scale (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.2-0.7
Celecoxib 200 mg, Then Celecoxib 400 mg3.2-0.5
Diclofenac SR 75 mg3.0-0.5
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.3-0.7

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Change From Baseline in Physician's Global Assessment of Disease Activity at Weeks 2, 4, and 6

5-point Likert scale scores specified physician's subjective assessment on how overall ankylosing spondylitis appeared at the time of participant's visit and participant's disease signs. 1=very good to 5=very poor. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionunits on a scale (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.4-0.4-0.5
Diclofenac SR 75 mg-0.4-0.5-0.5

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Percentages of Participants Responding to Assessment in Ankylosing Spondylitis (ASAS)-20

Percentages of participants who demonstrated an improvement of greater than or equal to (≥) 20% from baseline and an absolute improvement of ≥10 mm from baseline on a 100-mm VAS in ≥3 of the 4 domains proposed by the Ankylosing Spondylitis Assessment Working Group (ASAS-20). (NCT00762463)
Timeframe: Weeks 2, 4, 6, 12

,,,
Interventionpercentage of participants (Number)
Week 2 (n=115, 114)Week 4 (n=116, 114)Week 6 (n=54, 54, 54, 54)Week 12 (n=51, 53, 46, 51)
Celecoxib 200 mg23.526.740.749.0
Celecoxib 200 mg, Then Celecoxib 400 mg0022.232.6
Diclofenac 75 mg, Then Celecoxib 400 mg0029.637.3
Diclofenac SR 75 mg25.431.642.647.2

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Change From Baseline in Nocturnal Pain at Week 12

"100-mm VAS scores specified participant's nocturnal pain in response to the following question Did you have any pain in the neck, back or hips during the previous night? 0=no pain to 100=worst pain possible. Lower scores indicated less pain. Change from baseline <0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg52.2-19.4
Celecoxib 200 mg, Then Celecoxib 400 mg54.5-12.5
Diclofenac SR 75 mg55.1-27.5
Diclofenac SR 75 mg, Then Celecoxib 400 mg61.5-22.6

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Change From Baseline in C-Reactive Protein (CRP) at Week 6

C-Reactive Protein (CRP) was a marker of inflammation, measured in milligram per liter (mg/L). Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, 6 Weeks

Interventionmg/L (Least Squares Mean)
Celecoxib 200 mg-4.16
Diclofenac SR 75 mg-2.72

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Change From Baseline in Erythrocyte Sedimentation Rate (ESR) at Week 6

Erythrocyte Sedimentation Rate (ESR) was a laboratory test that providee a non-specific measure of inflammation. The test assessed the rate at which red blood cells fell in a test tube and was measured in millimeter per hour (mm/h). Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 6

Interventionmm/h (Least Squares Mean)
Celecoxib 200 mg-2.5
Diclofenac SR 75 mg-1.8

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Change From Baseline in Participant's Assessment of Global Pain Intensity at Week 6

"100-millimeter (mm) Visual Analog Scale (VAS) score specified participant's assessment of overall pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Change from baseline of less than (<) 0 indicated improvement." (NCT00762463)
Timeframe: Baseline, Week 6

Interventionmm (Least Squares Mean)
Celecoxib 200 mg-23.8
Diclofenac SR 75 mg-27.1

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Paracetamol Tablets Taken Per Day by Participant

Calculated as the total number of paracetamol tablets taken divided by days of exposure in the study. (NCT00762463)
Timeframe: Week 6

Interventiontablets per day (Mean)
Celecoxib 200 mg0.2
Diclofenac SR 75 mg0.0

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Participant's Assessment of Global Pain Intensity at Baseline

"100-mm VAS scores specified participant's assessment of global pain intensity in the previous 48 hours, in response to the following question What has been your global pain intensity in the last 48 hours? 0=no pain to 100=worst pain. Lower scores indicated less pain." (NCT00762463)
Timeframe: Baseline

Interventionmm (Mean)
Celecoxib 200 mg62.9
Diclofenac SR 75 mg63.6

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Percentage of Days With Concomitant Administration of Paracetamol

Calculated as days on rescue medication divided by days of exposure in the study at the end of Week 6. (NCT00762463)
Timeframe: Week 6

Interventionpercentage of days (Mean)
Celecoxib 200 mg0.1
Diclofenac SR 75 mg0.0

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Percentage of Participants With Concomitant Use of Paracetamol

Percentage of participants who concomitantly took at least 1 paracetamol tablet as rescue medication at Week 6 (NCT00762463)
Timeframe: Week 6

Interventionpercentage of participants (Number)
Celecoxib 200 mg2.5
Diclofenac SR 75 mg0.0

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Change From Baseline in BASDAI at Week 12

BASDAI is comprised of 6 specific questions, each answered on a 10-mm VAS. Scores for the first 5 questions: 0=none to 10=severe. Score for the sixth question: 0=0 hours to 10=2 hours. BASDAI score was defined as the mean of the scaled responses to these 6 questions. Lower scores indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg4.71-1.7
Celecoxib 200 mg, Then Celecoxib 400 mg4.7-0.6
Diclofenac SR 75 mg4.9-2.1
Diclofenac SR 75 mg, Then Celecoxib 400 mg4.9-1.4

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Change From Baseline in BASFI at Week 12

BASFI was comprised of 10 specific questions, each answered on a 10-mm VAS scale. 0=easy to 10=impossible. BASFI score was defined as the mean of the scaled responses to these 10 questions. Lower scores indicated better functional health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.4-0.9
Celecoxib 200 mg, Then Celecoxib 400 mg3.5-0.6
Diclofenac SR 75 mg3.5-1.0
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.5-1.0

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Change From Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) at Weeks 2, 4, and 6

Baseline in Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) was comprised of 6 specific questions, each answered on a 10-mm VAS scale. Scores for the first 5 questions: 0=none to 10=severe. Score for the sixth question: 0=0 hours to 10=2 hours. BASDAI score was defined as the mean of the scaled responses to these 6 questions. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.8-0.9-1.1
Diclofenac SR 75 mg-0.9-1.1-1.4

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Change From Baseline in Bath Ankylosing Spondylitis Functional Index (BASFI) at Weeks 2, 4, and 6

Bath Ankylosing Spondylitis Functional Index (BASFI) was comprised of 10 specific questions, each answered on a 10-mm VAS scale. 0=easy to 10=impossible. BASFI score was defined as the mean of the scaled responses to these 10 questions. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventionmm (Least Squares Mean)
Week 2 (n=116, 115)Week 4 (n=117, 115)Week 6 (n=117, 115)
Celecoxib 200 mg-0.3-0.4-0.5
Diclofenac SR 75 mg-0.3-0.6-0.8

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Change From Baseline in Chest Expansion at Week 12

Chest expansion, measured in cm, is defined as the difference in thoracic circumference during full expiration versus full inspiration, measured at the fourth intercostal space (nipple line). The better of 2 tries was recorded. Higher scores indicate better health. Change from baseline greater than (>) 0 represented improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventioncm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg3.90.8
Celecoxib 200 mg, Then Celecoxib 400 mg3.60.8
Diclofenac SR 75 mg3.80.8
Diclofenac SR 75 mg, Then Celecoxib 400 mg3.80.8

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Change From Baseline in Chest Expansion at Weeks 2, 4, and 6

Chest expansion, measured in cm, is defined as the difference in thoracic circumference during full expiration versus full inspiration, measured at the fourth intercostal space (nipple line). The better of 2 tries was recorded. Change from baseline greater than (>) 0 represented improvement. (NCT00762463)
Timeframe: Baseline, Weeks 2, 4, 6

,
Interventioncm (Least Squares Mean)
Week 2 (n=117, 115)Week 4 (n=118, 115)Week 6 (n=118, 115)
Celecoxib 200 mg0.20.60.7
Diclofenac SR 75 mg0.30.40.6

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Change From Baseline in CRP at Week 12

CRP was a marker of inflammation. Lower values indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmg/L (Mean)
Baseline (n=53, 55, 53, 54)Change from Baseline at Week 12 (n=47, 49, 42, 47)
Celecoxib 200 mg18.53-4.58
Celecoxib 200 mg, Then Celecoxib 400 mg18.80-4.77
Diclofenac SR 75 mg15.84-2.99
Diclofenac SR 75 mg, Then Celecoxib 400 mg21.01-2.13

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Change From Baseline in ESR at Week 12

ESR was a laboratory test that provided a non-specific measure of inflammation. The test assessed the rate at which red blood cells fell in a test tube. Lower values indicated better health. Change from baseline <0 indicated improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventionmm/h (Mean)
Baseline (n=54, 54, 52, 54)Change from Baseline at Week 12 (n=45, 44, 41, 43)
Celecoxib 200 mg20.9-3.5
Celecoxib 200 mg, Then Celecoxib 400 mg22.8-6.3
Diclofenac SR 75 mg20.8-1.3
Diclofenac SR 75 mg, Then Celecoxib 400 mg23.6-0.7

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Change From Baseline in Fingertips to Floor Distance at Week 12

Fingertips to floor distance measured in cm from the tip of the fingers to the floor with participant standing erect and feet together, knees as straight as possible, then bending forward as far as possible with fingers reaching towards the floor. The better of 2 tries was recorded. Lower scores indicated better health. Change from baseline <0 represented improvement. (NCT00762463)
Timeframe: Baseline, Week 12

,,,
Interventioncm (Mean)
Baseline (n=55, 55, 54, 54)Change from Baseline at Week 12 (n=52, 54, 46, 51)
Celecoxib 200 mg14.8-3.0
Celecoxib 200 mg, Then Celecoxib 400 mg22.9-3.1
Diclofenac SR 75 mg17.6-3.7
Diclofenac SR 75 mg, Then Celecoxib 400 mg14.6-1.3

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Time to Discontinuation (TTD) Due to Lack of Efficacy

Median time to discontinuation due to lack of efficacy was estimated using Kaplan-Meier method. (NCT00864097)
Timeframe: Baseline up to Week 16 and 24

,,,
Interventiondays (Median)
Week 16Week 24
Placebo + DiclofenacNANA
Tanezumab 10 mg + DiclofenacNANA
Tanezumab 2.5 mg + DiclofenacNANA
Tanezumab 5 mg + DiclofenacNANA

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Percentage of Participants With Outcome Measures in Rheumatology - Osteoarthritis Research Society International (OMERACT-OARSI) Response; LOCF

OMERACT-OARSI responder: participant has >=50 percent (%) change and >=2 absolute change from Baseline in either WOMAC pain or physical function subscale scores or at least 2 of the following being true: >=20% change and >=1 absolute change from Baseline in WOMAC pain subscale; >=20% change and >=1 absolute change from Baseline in the WOMAC physical function subscale; >=20% change and >=1 absolute change from Baseline in PGA of osteoarthritis. WOMAC pain and physical function score: 0 to 10 with higher score = worse response. PGA score: 1 = very good and 5 = very poor. (NCT00864097)
Timeframe: Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionpercentage of participants (Number)
Week 2Week 4Week 8Week 12Week 16Week 24
Placebo + Diclofenac44.751.357.260.557.955.3
Tanezumab 10 mg + Diclofenac34.559.369.773.172.467.6
Tanezumab 2.5 mg + Diclofenac37.257.158.367.366.765.4
Tanezumab 5 mg + Diclofenac43.365.368.073.366.764.7

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Percentage of Participants With Improvement of at Least 2 Points in Patient Global Assessment (PGA) of Osteoarthritis; LOCF

"Participants answered: Considering all the ways your osteoarthritis in your index joint (knee/hip) affects you, how are you doing today? Participants responded by using a 5-point Likert scale, where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (severe symptoms and inability to carry out most normal activities), and 5 = very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher score indicated worst condition. A decrease of at least 2 points on the 5-point scale relative to baseline value indicated improvement." (NCT00864097)
Timeframe: Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionpercentage of participants (Number)
Week 2Week 4Week 8Week 12Week 16Week 24
Placebo + Diclofenac5.96.65.36.64.65.9
Tanezumab 10 mg + Diclofenac5.512.414.512.416.612.4
Tanezumab 2.5 mg + Diclofenac5.83.26.46.45.85.8
Tanezumab 5 mg + Diclofenac4.714.718.014.014.712.7

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Percentage of Participants With Improvement of at Least 2 Points in Patient Global Assessment (PGA) of Osteoarthritis; Baseline Observation Carried Forward (BOCF)

"Participants answered: Considering all the ways your osteoarthritis in your index joint (knee/hip) affects you, how are you doing today? Participants responded by using a 5-point Likert scale, where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (severe symptoms and inability to carry out most normal activities), and 5 = very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher score indicated worst condition. A decrease of at least 2 points on the 5-point scale relative to baseline value indicates improvement." (NCT00864097)
Timeframe: Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionpercentage of participants (Number)
Week 2Week 4Week 8Week 12Week 16Week 24
Placebo + Diclofenac5.96.65.36.64.65.3
Tanezumab 10 mg + Diclofenac5.511.713.810.314.59.7
Tanezumab 2.5 mg + Diclofenac5.83.26.46.45.84.5
Tanezumab 5 mg + Diclofenac4.714.717.313.314.010.0

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Percentage of Participants With Cumulative Reduction From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Week 16 and 24

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with osteoarthritis (OA). WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 5 individual questions, each scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Total score range for WOMAC pain subscale score is 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Greater percentage reduction indicates greater improvement. Percentage of participants with cumulative reduction (as percent) (greater than 0%; >= 10, 20, 30, 40, 50, 60, 70, 80 and 90%; = 100 %) in WOMAC pain subscale from Baseline to Weeks 16 and 24 were reported. (NCT00864097)
Timeframe: Baseline, Week 16 and 24

,,,
Interventionpercentage of participants (Number)
Week 16: Greater than 0% reductionWeek 16: >=10% reductionWeek 16: >=20% reductionWeek 16: >=30% reductionWeek 16: >=40% reductionWeek 16: >=50% reductionWeek 16: >=60% reductionWeek 16: >=70% reductionWeek 16: >=80% reductionWeek 16: >=90% reductionWeek 16: 100% reductionWeek 24: Greater than 0% reductionWeek 24: >=10% reductionWeek 24: >=20% reductionWeek 24: >=30% reductionWeek 24: >=40% reductionWeek 24: >=50% reductionWeek 24: >=60% reductionWeek 24: >=70% reductionWeek 24: >=80% reductionWeek 24: >=90% reductionWeek 24: 100% reduction
Placebo + Diclofenac84.273.761.850.038.830.921.713.25.92.00.781.672.460.548.035.528.320.412.56.63.90.7
Tanezumab 10 mg + Diclofenac84.177.975.266.260.749.031.719.313.86.92.884.875.269.759.351.042.131.721.413.88.32.8
Tanezumab 2.5 mg + Diclofenac88.582.769.954.548.735.926.317.39.05.82.682.776.967.358.347.438.526.318.611.58.33.8
Tanezumab 5 mg + Diclofenac88.776.768.761.350.740.028.720.010.76.72.082.074.765.359.347.340.034.022.714.78.03.3

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Percentage of Participants With At Least 30%, 50%, 70% and 90% Reduction From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score; LOCF

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with osteoarthritis (OA). WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 5 individual questions, each scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Total score range for WOMAC pain subscale score is 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Greater percentage reduction indicates greater improvement. Percentage of participants with reduction in WOMAC pain intensity of at least (>=) 30%, 50%, 70% and 90% at Weeks 2, 4, 8, 12, 16, 24 and 32 compared to baseline were classified as responders to WOMAC pain subscale and are reported here. (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionpercentage of participants (Number)
Week 2: At least 30% reductionWeek 2: At least 50% reductionWeek 2: At least 70% reductionWeek 2: At least 90% reductionWeek 4: At least 30% reductionWeek 4: At least 50% reductionWeek 4: At least 70% reductionWeek 4: At least 90% reductionWeek 8: At least 30% reductionWeek 8: At least 50% reductionWeek 8: At least 70% reductionWeek 8: At least 90% reductionWeek 12: At least 30% reductionWeek 12: At least 50% reductionWeek 12: At least 70% reductionWeek 12: At least 90% reductionWeek 16: At least 30% reductionWeek 16: At least 50% reductionWeek 16: At least 70% reductionWeek 16: At least 90% reductionWeek 24: At least 30% reductionWeek 24: At least 50% reductionWeek 24: At least 70% reductionWeek 24: At least 90% reduction
Placebo + Diclofenac30.313.84.62.042.117.15.92.043.425.03.92.048.727.07.22.050.030.913.22.048.028.312.53.9
Tanezumab 10 mg + Diclofenac24.19.02.80.750.330.311.72.163.438.619.36.263.442.824.84.866.249.019.36.959.342.121.48.3
Tanezumab 2.5 mg + Diclofenac28.816.06.41.351.926.910.31.951.927.69.65.157.136.516.76.454.535.917.35.858.338.518.68.3
Tanezumab 5 mg + Diclofenac32.016.77.31.357.334.012.76.057.338.017.34.764.046.724.08.761.340.020.06.759.340.022.78.0

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Number of Participants With Intravenous Doses of Study Medication

Number of participants were reported based on the maximum number of intravenous (IV) doses of either tanezumab or placebo received. (NCT00864097)
Timeframe: Day 1 up to Week 16

,,,
InterventionParticipants (Count of Participants)
Number of IV Doses: 1Number of IV Doses: 2Number of IV Doses: 3
Placebo + Diclofenac1438100
Tanezumab 10 mg + Diclofenac1331101
Tanezumab 2.5 mg + Diclofenac934114
Tanezumab 5 mg + Diclofenac1526109

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Number of Participants With Change From Baseline in European Quality of Life - 5 Dimension (EQ-5D) Individual Health State Profile at Week 24

"EQ-5D was a standardized, participant-administered measure of health outcome. It provides a descriptive profile for 5 dimensions (mobility, self-care, usual activities, pain/discomfort, anxiety/depression), using 3 levels (no, moderate, or extreme dysfunction) and a single index value characterizing current health status using a visual analog scale with score ranging from 0 (worst) to 100 (best). Baseline EQ-5D individual health state profile was determined as number of participants no dysfunction, moderate or some dysfunction and extreme dysfunction and change from baseline in EQ-5D individual health state profile was determined as number of participants improved, no change or worsened." (NCT00864097)
Timeframe: Baseline, Week 24

,,,
InterventionParticipants (Count of Participants)
Baseline: Mobility-No DysfunctionBaseline: Mobility-Moderate DysfunctionBaseline: Mobility-Extreme DysfunctionBaseline: Self Care-No DysfunctionBaseline: Self Care-Moderate DysfunctionBaseline: Self Care-Extreme DysfunctionBaseline: Usual Activities-No DysfunctionBaseline: Usual Activities-Moderate DysfunctionBaseline: Usual Activities-Extreme DysfunctionBaseline: Pain/Discomfort-No DysfunctionBaseline: Pain/Discomfort-Moderate DysfunctionBaseline: Pain/Discomfort-Extreme DysfunctionBaseline: Anxiety/Depression-No DysfunctionBaseline: Anxiety/Depression-Moderate DysfunctionBaseline: Anxiety/Depression-Extreme DysfunctionChange at Week 24: Mobility-ImprovedChange at Week 24: Mobility-No ChangeChange at Week 24: Mobility-WorsenedChange at Week 24: Self Care-ImprovedChange at Week 24: Self Care-No ChangeChange at Week 24: Self Care-WorsenedChange at Week 24: Usual Activities-ImprovedChange at Week 24: Usual Activities-No ChangeChange at Week 24: Usual Activities-WorsenedChange at Week 24: Pain/Discomfort-ImprovedChange at Week 24: Pain/Discomfort-No ChangeChange at Week 24: Pain/Discomfort-WorsenedChange at Week 24: Anxiety/Depression-ImprovedChange at Week 24: Anxiety/Depression-No ChangeChange at Week 24: Anxiety/Depression-Worsened
Placebo + Diclofenac8143165870251161101143874726211274191181516125112811682710619
Tanezumab 10 mg + Diclofenac101350529211812341111337366625120030104112711173310571910719
Tanezumab 2.5 mg + Diclofenac71481619231314120125318272225129233112112712542912522611119
Tanezumab 5 mg + Diclofenac141360539612012642115337075530114632110831106133410972810913

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 112 days after last dose that were absent before treatment or that worsened relative to pretreatment state. AEs included SAEs as well as non-serious AEs which occurred during the trial. (NCT00864097)
Timeframe: Baseline up to 112 days after last intravenous dose (up to Week 32)

,,,
InterventionParticipants (Count of Participants)
AEsSAEs
Placebo + Diclofenac538
Tanezumab 10 mg + Diclofenac7210
Tanezumab 2.5 mg + Diclofenac7112
Tanezumab 5 mg + Diclofenac738

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Change From Baseline in 36-Item Short-Form Health Survey Version 2 (SF-36v2) Domain Scores at Week 12 and 24

SF-36v2 was a standardized survey evaluating 8 aspects of functional health and well-being: physical and social functioning, physical and role limitations due to emotional problems, bodily pain, general health, vitality, and mental health. The total score and the score for a section was an average of the individual question scores, which were scaled 0-100. Higher scores reflected better participant status and positive change indicated an improvement. (NCT00864097)
Timeframe: Baseline, Week 12, and 24

,,,
Interventionunits on a scale (Mean)
Baseline: General HealthBaseline: Physical FunctionBaseline: Role PhysicalBaseline: Bodily PainBaseline: VitalityBaseline: Social FunctionBaseline: Role EmotionalBaseline: Mental HealthChange at Week 12: General HealthChange at Week 12: Physical FunctionChange at Week 12: Role PhysicalChange at Week 12: Bodily PainChange at Week 12: VitalityChange at Week 12: Social FunctionChange at Week 12: Role EmotionalChange at Week 12: Mental HealthChange at Week 24: General HealthChange at Week 24: Physical FunctionChange at Week 24: Role PhysicalChange at Week 24: Bodily PainChange at Week 24: VitalityChange at Week 24: Social FunctionChange at Week 24: Role EmotionalChange at Week 24: Mental Health
Placebo + Diclofenac46.3733.5146.6732.9949.0861.0268.1562.804.677.367.618.763.805.021.923.132.416.215.179.141.664.36-0.551.27
Tanezumab 10 mg + Diclofenac49.3136.5247.4635.0651.2966.5569.7765.484.969.908.4912.765.344.22-1.261.663.088.505.9111.522.761.38-1.950.45
Tanezumab 2.5 mg + Diclofenac49.4136.2247.4435.6652.2267.6368.9666.575.2910.968.8112.514.236.252.241.554.518.788.4112.542.434.090.692.06
Tanezumab 5 mg + Diclofenac47.0034.7048.5033.9553.0065.8368.4464.636.5512.837.7115.183.794.172.172.204.9410.506.9613.272.583.67-1.331.63

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Number of Participants Who Discontinued Due to Lack of Efficacy

Number of participants who discontinued due to lack of efficacy were reported. (NCT00864097)
Timeframe: Baseline up to end of study (Week 32)

InterventionParticipants (Count of Participants)
Placebo + Diclofenac9
Tanezumab 2.5 mg + Diclofenac3
Tanezumab 5 mg + Diclofenac7
Tanezumab 10 mg + Diclofenac2

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Change From Baseline in 36-Item Short-Form Health Survey Version 2 (SF-36v2) Physical and Mental Component Scores at Week 12 and 24

SF-36v2: standardized survey evaluating 8 aspects of functional health and wellbeing (physical and social functioning, role limitations due to physical and emotional problems, bodily pain, general health, vitality, mental health). Total score for each aspect were scaled 0-100. Higher scores reflect better participant status and positive change indicated an improvement. For obtaining physical and mental component scores, z-score for each scale=(observed score - mean score for general 1990 United States [US] population)/corresponding standard deviation. The 2 component scores were obtained by multiplying each aspect z-score by physical or mental factor score coefficient (1990 general US population) and summing the eight products. Component scores indicated how many standard deviations higher (in case of positive z-score [better functioning])/lower (in case of negative z-score [worse functioning]) participant's value was relative to the mean of the reference population. (NCT00864097)
Timeframe: Baseline, Week 12 and 24

,,,
Interventionz-score (Mean)
Baseline: Physical Component ScoreBaseline: Mental Component ScoreChange at Week 12: Physical Component ScoreChange at Week 12: Mental Component ScoreChange at Week 24: Physical Component ScoreChange at Week 24: Mental Component Score
Placebo + Diclofenac-1.84-0.300.350.080.32-0.03
Tanezumab 10 mg + Diclofenac-1.76-0.150.51-0.060.43-0.14
Tanezumab 2.5 mg + Diclofenac-1.76-0.110.500.010.45-0.03
Tanezumab 5 mg + Diclofenac-1.80-0.170.56-0.030.50-0.10

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Change From Baseline in Average Pain Score in the Index Knee or Hip at Weeks 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, and 24

Participants were asked to assess index joint (knee/hip) pain during the past 24 hours on an 0-10 point integer scale ranging from 0 (no pain) to 10 (worst possible pain). Baseline score was calculated as the mean of the scores in the index joint over the 3 days days in the initial pain assessment period and a weekly mean was calculated using the daily pain scores in the index joint within each study week. The change from Baseline was calculated using the difference between each post-baseline weekly mean and the baseline mean score, where negative change indicated an improvement. (NCT00864097)
Timeframe: Baseline, Weeks 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, and 24

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 1Change at Week 2Change at Week 3Change at Week 4Change at Week 6Change at Week 8Change at Week 10Change at Week 12Change at Week 16Change at Week 20Change at Week 24
Placebo + Diclofenac6.31-0.55-0.95-1.19-1.28-1.38-1.41-1.41-1.49-1.53-1.61-1.65
Tanezumab 10 mg + Diclofenac6.34-0.96-1.03-1.08-1.44-1.69-1.80-2.06-2.06-2.15-2.15-2.03
Tanezumab 2.5 mg + Diclofenac6.29-0.74-0.91-1.19-1.45-1.57-1.62-1.79-1.91-1.87-1.95-1.84
Tanezumab 5 mg + Diclofenac6.38-1.22-1.28-1.40-1.77-1.88-1.84-2.09-2.06-2.07-2.19-2.07

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Change From Baseline in European Quality of Life - 5 Dimension (EQ-5D) Index Score at Week 24

EQ-5D was a standardized, participant-administered measure of health outcome. It provides a descriptive profile for 5 dimensions (mobility, self-care, usual activities, pain/discomfort, anxiety/depression), using 3 levels (no, moderate, or extreme dysfunction) and a single index value characterizing current health status using a visual analog scale with score ranging from 0 (worst) to 100 (best). EQ-5D summary index was obtained with a formula that weights each level of the dimensions. The index-based score was interpreted along a continuum of 0 (death) to 1 (perfect health). Negative change from baseline represented worsening. (NCT00864097)
Timeframe: Baseline, Week 24

,,,
Interventionunits on a scale (Mean)
Baseline: Index ScoreChange at Week 24: Index Score
Placebo + Diclofenac0.450.11
Tanezumab 10 mg + Diclofenac0.470.16
Tanezumab 2.5 mg + Diclofenac0.480.15
Tanezumab 5 mg + Diclofenac0.470.14

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Change From Baseline in Patient Global Assessment (PGA) of Osteoarthritis Score at Week 16

"Participants answered: Considering all the ways your osteoarthritis in your index joint (knee/hip) affects you, how are you doing today? Participants responded by using a 5-point Likert scale, where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (severe symptoms and inability to carry out most normal activities), and 5 = very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher score indicated worst condition." (NCT00864097)
Timeframe: Baseline, Week 16

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 16
Placebo + Diclofenac3.39-0.41
Tanezumab 10 mg + Diclofenac3.37-0.63
Tanezumab 2.5 mg + Diclofenac3.28-0.49
Tanezumab 5 mg + Diclofenac3.43-0.61

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Change From Baseline in Patient Global Assessment (PGA) of Osteoarthritis Score at Weeks 2, 4, 8, 12, and 24

"Participants answered: Considering all the ways your osteoarthritis in your index joint (knee/hip) affects you, how are you doing today? Participants responded by using a 5-point Likert scale, where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (severe symptoms and inability to carry out most normal activities), and 5 = very poor (very severe symptoms which are intolerable and inability to carry out all normal activities). Higher score indicated worst condition." (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, and 24

,,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 24
Placebo + Diclofenac-0.36-0.40-0.37-0.45-0.45
Tanezumab 10 mg + Diclofenac-0.28-0.54-0.66-0.61-0.57
Tanezumab 2.5 mg + Diclofenac-0.37-0.45-0.44-0.52-0.46
Tanezumab 5 mg + Diclofenac-0.40-0.65-0.71-0.69-0.57

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Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Weeks 2, 4, 8, 12 and 24

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with OA. WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 5 individual questions, each scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Total score range for WOMAC pain subscale score is 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, and 24

,,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 24
Placebo + Diclofenac-1.30-1.51-1.63-1.81-1.81
Tanezumab 10 mg + Diclofenac-0.86-1.93-2.34-2.42-2.19
Tanezumab 2.5 mg + Diclofenac-1.22-1.76-1.88-2.23-2.11
Tanezumab 5 mg + Diclofenac-1.21-2.12-2.22-2.50-2.24

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Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Physical Function Subscale Score at Weeks 2, 4, 8, 12, and 24

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with OA. WOMAC physical function is a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 17 individual questions, each scored on a NRS of 0 (no difficulty) to 10 (extreme difficulty), where higher scores indicate worse function. Total score range for WOMAC physical function subscale score is 0 (no difficulty) to 10 (extreme difficulty), where higher scores indicate worse function. Physical function refers to participant's ability to move around and perform usual activities of daily living. (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, and 24

,,,
Interventionunits on a scale (Mean)
Change at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 24
Placebo + Diclofenac-1.31-1.46-1.59-1.75-1.70
Tanezumab 10 mg + Diclofenac-1.06-1.81-2.13-2.28-2.08
Tanezumab 2.5 mg + Diclofenac-1.18-1.58-1.76-2.13-1.99
Tanezumab 5 mg + Diclofenac-1.30-2.09-2.22-2.43-2.17

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Average Score at Weeks 2, 4, 8, 12, 16, and 24

WOMAC Index: self-administered, disease-specific 24 item questionnaire which assesses clinically important, participant-relevant symptoms for pain (5 items), stiffness (2 items), and physical function (17 items) in participants with osteoarthritis of the hip and/or knee. WOMAC average score is the mean of the WOMAC pain, physical function and stiffness subscale scores and ranges from 0 to 10, with higher score indicating worse response. Greater reduction in WOMAC average score indicated greater improvement. (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 16Change at Week 24
Placebo + Diclofenac6.05-1.31-1.45-1.59-1.74-1.80-1.74
Tanezumab 10 mg + Diclofenac5.80-1.06-1.92-2.27-2.42-2.43-2.17
Tanezumab 2.5 mg + Diclofenac5.75-1.23-1.68-1.83-2.24-2.19-2.05
Tanezumab 5 mg + Diclofenac5.72-1.30-2.14-2.21-2.45-2.22-2.16

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Item: Pain When Going Up or Downstairs at Weeks 2, 4, 8, 12, 16, and 24

"Participants answered the question: How much pain have you had when going up or down the stairs? Participants responded by using an 11-point scale, where 0 = no pain and 10 = extreme pain. Where 0 is the best response and negative change indicated an improvement." (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 16Change at Week 24
Placebo + Diclofenac7.24-1.38-1.58-1.78-2.03-2.00-1.95
Tanezumab 10 mg + Diclofenac7.06-1.21-2.10-2.64-2.77-2.79-2.56
Tanezumab 2.5 mg + Diclofenac7.04-1.49-2.10-2.15-2.54-2.54-2.44
Tanezumab 5 mg + Diclofenac7.05-1.55-2.39-2.51-2.86-2.53-2.53

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Item: Pain When Walking on a Flat Surface at Weeks 2, 4, 8, 12, 16, and 24

"Participants answered the question: How much pain have you had when walking on a flat surface? Participants responded by using an 11-point scale where 0 = no pain and 10 = extreme pain. Where 0 is the best response and negative change indicated an improvement." (NCT00864097)
Timeframe: Baseline, Week 2, 4, 8, 12, 16, 24

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 16Change at Week 24
Placebo + Diclofenac6.12-1.34-1.47-1.62-1.83-1.95-1.84
Tanezumab 10 mg + Diclofenac5.99-0.89-1.87-2.25-2.41-2.34-2.10
Tanezumab 2.5 mg + Diclofenac5.91-1.23-1.75-1.81-2.15-2.14-2.08
Tanezumab 5 mg + Diclofenac5.81-1.07-2.01-2.05-2.35-2.09-2.09

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score at Week 16

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with osteoarthritis (OA). WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 5 individual questions, each scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. Total score range for WOMAC pain subscale score is 0 (no pain) to 10 (extreme pain), where higher scores indicate higher pain. (NCT00864097)
Timeframe: Baseline, Week 16

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 16
Placebo + Diclofenac6.06-1.91
Tanezumab 10 mg + Diclofenac5.87-2.42
Tanezumab 2.5 mg + Diclofenac5.78-2.18
Tanezumab 5 mg + Diclofenac5.76-2.28

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Physical Function Subscale Score at Week 16

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with OA. WOMAC physical function is a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 17 individual questions, each scored on a NRS of 0 (no difficulty) to 10 (extreme difficulty), where higher scores indicate worse function. Total score range for WOMAC physical function subscale score is 0 (no difficulty) to 10 (extreme difficulty), where higher scores indicate worse function. Physical function refers to participant's ability to move around and perform usual activities of daily living. (NCT00864097)
Timeframe: Baseline, Week 16

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 16
Placebo + Diclofenac6.24-1.76
Tanezumab 10 mg + Diclofenac5.91-2.35
Tanezumab 2.5 mg + Diclofenac5.86-2.11
Tanezumab 5 mg + Diclofenac5.90-2.23

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Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Stiffness Subscale Score at Weeks 2, 4, 8, 12, 16, and 24

WOMAC: Self-administered, disease-specific questionnaire which assesses clinically important, participant-relevant symptoms for pain, stiffness and physical function in participants with OA. WOMAC stiffness subscale is a 2-item questionnaire used to assess the amount of stiffness experienced due to osteoarthritis in index knee or hip during past 48 hours. It is calculated as mean of the scores from 2 individual questions scored on NRS of (no stiffness) to 10 (extreme stiffness), with higher scores indicate higher stiffness. Total score range for WOMAC stiffness subscale score is (no stiffness) to 10 (extreme stiffness), where higher scores indicate higher stiffness. Stiffness is defined as a sensation of decreased ease in movement of knee/hip. Negative change indicated an improvement. (NCT00864097)
Timeframe: Baseline, Weeks 2, 4, 8, 12, 16, and 24

,,,
Interventionunits on a scale (Mean)
BaselineChange at Week 2Change at Week 4Change at Week 8Change at Week 12Change at Week 16Change at Week 24
Placebo + Diclofenac5.84-1.31-1.37-1.56-1.66-1.72-1.70
Tanezumab 10 mg + Diclofenac5.60-1.27-2.01-2.34-2.55-2.53-2.22
Tanezumab 2.5 mg + Diclofenac5.61-1.29-1.71-1.86-2.36-2.27-2.06
Tanezumab 5 mg + Diclofenac5.51-1.38-2.21-2.20-2.42-2.15-2.08

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 3 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml41.2
Diclofenac HPBCD s.c. 50mg/ml45.5
Diclofenac HPBCD s.c. 75mg/ml45.6
Placebo s.c. 1ml25.3

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 5 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml37.5
Diclofenac HPBCD s.c. 50mg/ml42.2
Diclofenac HPBCD s.c. 75mg/ml45.6
Placebo s.c. 1ml31.8

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 45 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml24.7
Diclofenac HPBCD s.c. 50mg/ml27.5
Diclofenac HPBCD s.c. 75mg/ml27.8
Placebo s.c. 1ml9.00

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 4 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml38.1
Diclofenac HPBCD s.c. 50mg/ml46.3
Diclofenac HPBCD s.c. 75mg/ml48.0
Placebo s.c. 1ml29.1

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 30 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml15.9
Diclofenac HPBCD s.c. 50mg/ml18.5
Diclofenac HPBCD s.c. 75mg/ml18.6
Placebo s.c. 1ml4.68

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 2 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml38.8
Diclofenac HPBCD s.c. 50mg/ml43.9
Diclofenac HPBCD s.c. 75mg/ml42.5
Placebo s.c. 1ml26.5

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 90 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml36.2
Diclofenac HPBCD s.c. 50mg/ml40.1
Diclofenac HPBCD s.c. 75mg/ml39.0
Placebo s.c. 1ml18.0

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 60 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml30.7
Diclofenac HPBCD s.c. 50mg/ml34.6
Diclofenac HPBCD s.c. 75mg/ml34.6
Placebo s.c. 1ml15.3

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 6 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml41.5
Diclofenac HPBCD s.c. 50mg/ml40.9
Diclofenac HPBCD s.c. 75mg/ml41.7
Placebo s.c. 1ml36.5

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Pain Intensity Difference (PID) on a 0-100 VAS

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 1.5 hours after treatment administration

Interventionmm (Least Squares Mean)
Diclofenac HPBCD s.c. 25mg/ml36.5
Diclofenac HPBCD s.c. 50mg/ml37.3
Diclofenac HPBCD s.c. 75mg/ml37.7
Placebo s.c. (1ml)12.3

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 15 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml8.39
Diclofenac HPBCD s.c. 50mg/ml8.28
Diclofenac HPBCD s.c. 75mg/ml9.46
Placebo s.c. 1ml1.59

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 7 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml43.2
Diclofenac HPBCD s.c. 50mg/ml41.6
Diclofenac HPBCD s.c. 75mg/ml43.0
Placebo s.c. 1ml39.1

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PID

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assigned by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00942448)
Timeframe: at 8 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 25mg/ml45.0
Diclofenac HPBCD s.c. 50mg/ml43.8
Diclofenac HPBCD s.c. 75mg/ml43.6
Placebo s.c. 1ml37.0

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PIDs

(NCT00943098)
Timeframe: at 45 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml31.2
Voltarol 75mg/3ml i.m.37.9

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Pain Intensity Difference (PID)

Pain intensity difference (PID) was derived by subtracting each pain intensity score (PI) from the baseline PI score (t0), where PI was assessed by the patient on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT00943098)
Timeframe: 1.5 hours

Interventionmm (Least Squares Mean)
Diclofenac HPBCD s.c. 75mg/ml44.8
Voltarol 75mg/3ml i.m.45.5
Diclofenac HPBCD s.c. 75mg/ml44.2
Voltarol 75mg/3ml i.m.44.7

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PIDs

(NCT00943098)
Timeframe: at 15 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml7.37
Voltarol 75mg/3ml i.m.6.83

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PIDs

(NCT00943098)
Timeframe: at 2 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml49.0
Voltarol 75mg/3ml i.m.50.3

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PIDs

(NCT00943098)
Timeframe: at 3 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml49.7
Voltarol 75mg/3ml i.m.53.3

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PIDs

(NCT00943098)
Timeframe: at 30 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml19.8
Voltarol 75mg/3ml i.m.18.4

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PIDs

(NCT00943098)
Timeframe: at 4 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml50.6
Voltarol 75mg/3ml i.m.53.9

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PIDs

(NCT00943098)
Timeframe: at 5 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml48.7
Voltarol 75mg/3ml i.m.52.3

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PIDs

(NCT00943098)
Timeframe: at 60 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml37.6
Voltarol 75mg/3ml i.m.37.9

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PIDs

(NCT00943098)
Timeframe: at 7 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml42.8
Voltarol 75mg/3ml i.m.49.6

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PIDs

(NCT00943098)
Timeframe: at 6 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml47.5
Voltarol 75mg/3ml i.m.51.2

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PIDs

(NCT00943098)
Timeframe: at 8 hours post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml43.7
Voltarol 75mg/3ml i.m.47.1

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PIDs

(NCT00943098)
Timeframe: at 90 minutes post-dose.

Interventionmm (Mean)
Diclofenac HPBCD s.c. 75mg/ml44.0
Voltarol 75mg/3ml i.m.45.0

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Measure: Pain on Movement on Day 5 (Change From Baseline).

Visual analog scale (0 to 100 mm) A greater change from baseline equates to a better outcome. (NCT00955513)
Timeframe: baseline and day 5

Interventionmm (Mean)
Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day49.1
Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day49.7
Placebo. Applied 3 Times a Day.25.4

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Total Patient Pain Relief Over 0 to 12 Hours.

"Total patient pain relief was assessed as a time-weighted sum of the patient pain assessments at each individual time point from 0-12 hours.~Values for TOTPAR are measured from 0 to 4 on the Pain Relief Scale 0 None Min; 1 A little; 2 Some; 3 A lot; 4 Complete Max~The TOTPAR is a weighted measure of the observations; the minimum possible value is 0 and the maximum possible value is 60." (NCT00985439)
Timeframe: 12 hours.

Interventionunits on a scale (Least Squares Mean)
Diclofenac Test (Lower Dose)17.770
Diclofenac Test (Upper Dose)16.893
Celecoxib 400 mg14.685
Placebo5.486

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Mean Change From Baseline to End of Treatment (EOT) in Response to Modified Brief Pain Inventory (mBPI) Question 5: Average Pain Over the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 5: Please rate your pain by marking the box beside the number that best describes your pain on the average (over the last 24 hours); rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6.46-3.95

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Mean Change From Baseline to EOT in Beck Depression Inventory® Il

The Beck Depression Inventory® II consisted of 21 items, each with 4 categorical responses ranging from 0 (I do not feel sad) to 3 (I am so sad or unhappy that I can't stand it) with maximum possible score of 63; increase in the number reflected an increase in severity. Total Beck Depression Inventory® II scores classified as follows: 1 to 10=normal ups and downs; 11 to 16=mild mood disturbance; 17 to 20=borderline clinical depression; 21 to 30=moderate depression; 31 to 40=severe depression; and >40=extreme depression. (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.3.44-1.54

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Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 3: Pain at Its Worst in the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 3: Rate your pain at its worst in the last 24 hours; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.7.59-4.50

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Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 4: Pain at Its Least in the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 4: Rate your pain at its least in the last 24 hours; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.5.46-3.50

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Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 6: Pain Right Now

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 6: Rate your pain right now; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6.49-4.28

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Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Investigator

Participants' global pain relief as assessed by investigator using a 5-point scale where 5 = complete relief, 4=a lot of improvement, 3=moderate improvement, 2=slight improvement, and 1=no change. (NCT01054820)
Timeframe: End of Treatment (up to Day 15)

Interventionparticipants (Number)
5=Complete Relief4=A Lot Of Improvement3=Moderate Improvement2=Slight Improvement1=No Change
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.58428105

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Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Participant

Global pain relief as assessed by participant using a 5-point scale where 5 = complete relief, 4=a lot of improvement, 3=moderate improvement, 2=slight improvement, and 1=no change. (NCT01054820)
Timeframe: End of Treatment (up to Day 15)

Interventionparticipants (Number)
5=Complete Relief4=A Lot Of Improvement3=Moderate Improvement2=Slight Improvement1=No Change
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.534212124

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Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by Participant

Participant satisfaction with the FLECTOR® Patch rated on a 5-point scale scored as 5=Very Satisfied, 4=Satisfied, 3=No Preference, 2=Dissatisfied, and 1=Very Dissatisfied. (NCT01054820)
Timeframe: End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
5=Very Satisfied4=Satisfied3=No Preference2=Dissatisfied1=Very Dissatisfied
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6345681

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Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by the Investigator

Investigator's assessment of participants' satisfaction with the FLECTOR® Patch rated on a 5-point scale scored as 5=Very Satisfied, 4=Satisfied, 3=No Preference, 2=Dissatisfied, and 1=Very Dissatisfied. (NCT01054820)
Timeframe: End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
5=Very Satisfied4=Satisfied3=No Preference2=Dissatisfied1=Very Dissatisfied
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6639981

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Number of Participants With Change From Baseline (Bsl) to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 1: Pain Other Than Everyday Kind of Pain

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 1: Have you had pain other than everyday kinds of pain?; response = Yes or No. (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
Change at EOT: Bsl=Yes, EOT=YesChange at EOT: Bsl=Yes, EOT=NoChange at EOT: Bsl=No, EOT=YesChange at EOT: Bsl=No, EOT=No
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.932109

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Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 8: Percent Reduction in Pain From Baseline

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 8: Rate your percent reduction in pain from Baseline (0% = no relief to 100% = complete relief). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionpercent (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.2.9467.30

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Patient's Assessment of Ankle Pain (VAS)- Absolute Value Decrease on Day 7

"Pain evaluated by a 100 mm visual analogue scale (VAS) where 0 means no pain and 100 means the highest, unbearable pain. The absolute values of VAS have been the basis of analysis.~The highest is the change in negative, the better are the results in absolute values." (NCT01066520)
Timeframe: From baseline (day 1) visit to day 7

InterventionAbsolute value units on a scale VAS (Median)
Traumeel S Ointment-33.00
Traumeel S Gel-37.10
Diclofenac Gel-37.10

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Change of the Foot and Ankle Ability Measurement (FAAM), Activity of Daily Living Subscale (ADL) From Baseline to Day 7

"The Foot and Ankle Ability Measure (FAAM) is a self-report outcome instrument developed to assess physical function for individuals with foot and ankle related impairments. The Foot and Ankle Ability Measure is a 29-item questionnaire divided into two subscales: the Foot and Ankle Ability Measure, 21-item Activities of Daily Living Subscale and the Foot and Ankle Ability Measure, 8-item Sports Subscale.~Each item is scored on a 5-point Likert scale (4 to 0) from 'no difficulty at all' (score 4), ´slight difficulty´, ´moderate difficulty´, éxtreme difficulty´ to 'unable to do' (score 0). Responses marked as ´not applicable´were not counted.~Item score totals, which range from 0 to 84 for the ADL subscale and 0 to 32 for the Sports subscale, were transformed to percentage scores. Higher scores represent higher levels of function for each subscale, with 100% representing no dysfunction." (NCT01066520)
Timeframe: Day 1 to day 7

InterventionScores on a scale (Median)
Traumeel S Ointment26.20
Traumeel S Gel26.20
Diclofenac Gel25.00

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Patient's Assessment of Ankle Pain (VAS)- Percentage Decrease on Day 7

"Pain evaluated by a 100 mm visual analogue scale (VAS) where 0 means no pain and 100 means the highest, unbearable pain. The absolute values of VAS have been the basis of analysis.~The highest is the change in negative, the better are the results in percentages." (NCT01066520)
Timeframe: From baseline (day 1) visit to day 7

InterventionPercentage change in scale VAS (Median)
Traumeel S Ointment-60.55
Traumeel S Gel-71.10
Diclofenac Gel-68.90

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Ankle Joint Function

"Ankle joint function score (Karlsson Scoring scale which ranges from 0 worst possible score to 90 best possible score)at 24 and 72 hours and 7 days." (NCT01255423)
Timeframe: 24 and 72 hours, 7 days

,
InterventionTotal score (Mean)
24 Hours72 Hours7 days
Diclofenac Sodium Topical Gel 1%30.147.268.8
Placebo30.746.166.4

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Tenderness

Tenderness at 24 and 72 hours and 7 days. Change from baseline. Tenderness was measured by a calibrated algometer in order to quantify the pressure pain threshold, a measure of tenderness. (NCT01255423)
Timeframe: Change from baseline at 24 and 72 hours, 7 days

,
InterventionN/cm^2 (Mean)
Change from baseline at 24 HoursChange from baseline at 72 HoursChange from baseline at 7 Days
Diclofenac Sodium Topical Gel 1%2.36.412.1
Placebo1.35.511.9

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Onset of Pain Relief

Onset of perceptible pain relief (NCT01255423)
Timeframe: Day 1

InterventionHour (Median)
Diclofenac Sodium Topical Gel 1%2
Placebo2

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Pain on Movement

"Pain on movement at 72 hours assessed on a 100 mm visual analog scale with anchors at 0= No pain and 100= Extreme pain" (NCT01255423)
Timeframe: 72 hours

Interventionmm (Mean)
Diclofenac Sodium Topical Gel 1%37.4
Placebo38.8

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Pain on Movement

"Pain on movement at 24 hours and 7 days assessed on a 100 mm visual analog scale with anchors at 0= No pain and 100= Extreme pain" (NCT01255423)
Timeframe: 24 hours and 7 days

,
Interventionmm (Mean)
24 hours7 days
Diclofenac Sodium Topical Gel 1%52.919.4
Placebo53.122

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Onset of Pain Relief

Onset of perceptible pain relief. (NCT01272934)
Timeframe: On day 1

InterventionHours (Median)
Diclofenac Sodium Topical Gel 1%4
PlaceboNA

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Pain on Movement

"Pain on Movement at 72 hours assessed on a 100 mm visual analog scale with anchors at 0=No pain and 100= Extreme pain" (NCT01272934)
Timeframe: 72 hours

Interventionmm (Mean)
Diclofenac Sodium Topical Gel 1%25.6
Placebo61.2

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Pain on Movement

"Visual analog scale (VAS) assessed on a 100 mm scale with anchors at 0= No pain and 100= Extreme pain" (NCT01272947)
Timeframe: VAS Score at 24 hours

Interventionmm (Mean)
Diclofenac Sodium Topical Gel 1%33.1
Placebo65.4

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Onset of Pain Relief

Onset of perceptible pain relief. (NCT01272947)
Timeframe: From randomization to end of day 1

InterventionHours (Median)
Diclofenac Sodium Topical Gel 1%2
PlaceboNA

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Neck Disability Index

"Neck Disability Index total score. Minimum = 0 Best. Maximum = 50 Worst" (NCT01335724)
Timeframe: 96h

InterventionTotal Score (Mean)
Diclofenac Diethylamine 1.16% Gel2.8
Placebo Gel14.6

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Pain at Rest

"Pain at Rest on a 100 mm visual analog scale. Minimum score =0 mm no pain. Maximum score =100 mm extreme pain." (NCT01335724)
Timeframe: 96h

Interventionmm (Mean)
Diclofenac Diethylamine 1.16% Gel1.2
Placebo Gel19.2

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Pain on Movement

"Pain on movement on a 100 mm visual analog scale. Minimum score =0 mm no pain. Maximum score =100 mm extreme pain." (NCT01335724)
Timeframe: 48 h

Interventionmm (Mean)
Diclofenac Diethylamine 1.16% Gel19.5
Placebo Gel56.9

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Percent Change From Baseline in Pain Score During Week 2

Participants assessed their knee pain using a visual analog scale (VAS) where 0=no pain and 100=worst possible pain. Pain scores were recorded in an electronic diary prior to and 4 hours after the first daily application of diclofenac gel for breakthrough pain. The daily percent change in pain scores over the 7 days prior to Week 2 were averaged. Percent change from baseline (average pain score 7 days prior to first treatment) was calculated as (value at baseline - value at post-baseline visit)/ (value at baseline) x 100. A positive change from baseline indicates improvement. (NCT01383954)
Timeframe: Baseline and Week 2

Interventionpercent change (Mean)
Diclofenac Gel33.3

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Percent Change From Baseline in Pain Score During Week 1

Participants assessed their knee pain using a visual analog scale (VAS) where 0=no pain and 100=worst possible pain. Pain scores were recorded in an electronic diary prior to and 4 hours after the first daily application of diclofenac gel for breakthrough pain. The daily percent change in pain scores over the 7 days prior to Week 1 were averaged. Percent change from Baseline (average pain score 7 days prior to first treatment) was calculated as (value at baseline - value at post-baseline visit) / (value at baseline) x 100. A positive change from Baseline indicates improvement. (NCT01383954)
Timeframe: Baseline and Week 1

Interventionpercent change (Mean)
Diclofenac Gel33.3

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Subject Global Impression at 2 Weeks

"This is a single question: How would you rate your level of comfort with Copaxone injection during the past two weeks? Responses include Extremely good, Quite good, Better than average, Average, Below Average, Quite bad, Extremely bad." (NCT01454791)
Timeframe: 2 weeks

InterventionLikert scale 1-7 (7= best) (Mean)
Diclofenac Sodium Topical Gel4.68
Placebo4.50

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Pain Scale at 2 Weeks

0-10 subjective Likert scale for severity of injection site reaction associated pain. Zero is best and 10 is worst (NCT01454791)
Timeframe: 2 weeks

Interventionunits on a scale (Mean)
Diclofenac Sodium Topical Gel2.44
Placebo2.60

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Local Injection Site Reaction (0-6) Scale at Baseline, 2 Weeks

patients will complete a daily diary rating their reaction for elements including pain and inflammation or no reaction to all 6 elements listed on the local injection site reaction scale. Range of scores is 0-6 with zero best and 6 worst. (NCT01454791)
Timeframe: 2 weeks

Interventionunits on a scale (Mean)
Diclofenac Sodium Topical Gel3.39
Placebo3.47

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Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.

"The pain in subjects with osteoarthritis was measured using the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain subscale score. The WOMAC pain subscale score is calculated as the average of the visual analogue scale (VAS) scores from 5 pain subscale questions. Subjects mark the VAS, which is a horizontal line 100 mm in length, with a single vertical line to indicate their pain level over the last 24 hours, with 0 mm representing No Pain and 100 mm representing Extreme Pain.~The WOMAC pain subscale score difference was calculated as the WOMAC pain subscale score assessed at Weeks 2, 6, and 12 minus the average of the WOMAC pain subscale score assessed at baseline." (NCT01461369)
Timeframe: Baseline to Week 12/Early Termination

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-35.62
Diclofenac 35 mg Three Times Daily-41.38
Placebo-28.14

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Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Osteoarthritis Pain, Stiffness, and Function Measured Using the Total (Composite) Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Score.

"Pain, stiffness, and function in subjects with osteoarthritis were measured using the Western Ontario and McMaster Universities (WOMAC) Index, which is a 24-item questionnaire. The total (composite) WOMAC score is calculated as the average of the mean visual analogue scale (VAS) scores from the questions in the pain, stiffness, and function subscales. Subjects mark the VAS, which is a horizontal line 100 mm in length, with a single vertical line to indicate their response to each of the questions, with 0 mm representing No Pain, Stiffness, or Difficulty and 100 mm representing Extreme Pain, Stiffness, and Difficulty.~The total (composite) WOMAC score difference was calculated as the total (composite) WOMAC score assessed at Weeks 2, 6, and 12 minus the total (composite) WOMAC score assessed at baseline." (NCT01461369)
Timeframe: Baseline to Week 12/Early Termination

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-30.25
Diclofenac 35 mg Three Times Daily-35.86
Placebo-23.22

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Change From Baseline to the Average of Weeks 2, 6, and 12 After Trial Entry in Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Pain Imaginable.~The VAS pain intensity difference is calculated as the average of the VAS pain intensity scores at Weeks 2, 6, and 12 minus the VAS pain intensity at baseline." (NCT01461369)
Timeframe: Baseline to Week 12/Early Termination

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-36.41
Diclofenac 35 mg Three Times Daily-41.33
Placebo-30.95

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Change From Baseline to Week 12 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.

"The pain in subjects with osteoarthritis was measured using the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain subscale score. The WOMAC pain subscale score is calculated as the average of the visual analogue scale (VAS) scores from 5 pain subscale questions. Subjects mark the VAS, which is a horizontal line 100 mm in length, with a single vertical line to indicate their pain level over the last 24 hours, with 0 mm representing No Pain and 100 mm representing Extreme Pain.~The WOMAC pain subscale score difference is calculated as the WOMAC pain subscale score assessed at Week 12 minus the WOMAC pain subscale score assessed at baseline." (NCT01461369)
Timeframe: Baseline to Week 12/Early Termination

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-39.04
Diclofenac 35 mg Three Times Daily-44.14
Placebo-32.46

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Change From Baseline to Week 2 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.

"The pain in subjects with osteoarthritis was measured using the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain subscale score. The WOMAC pain subscale score is calculated as the average of the visual analogue scale (VAS) scores from 5 pain subscale questions. Subjects mark the VAS, which is a horizontal line 100 mm in length, with a single vertical line to indicate their pain level over the last 24 hours, with 0 mm representing No Pain and 100 mm representing Extreme Pain.~The WOMAC pain subscale score difference was calculated as the WOMAC pain subscale score assessed at Week 2 minus the WOMAC pain subscale score assessed at baseline." (NCT01461369)
Timeframe: Baseline to Week 2

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-31.40
Diclofenac 35 mg Three Times Daily-37.42
Placebo-21.60

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Change From Baseline to Week 6 After Trial Entry in Osteoarthritis Pain Measured on the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Score.

"The pain in subjects with osteoarthritis was measured using the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain subscale score. The WOMAC pain subscale score is calculated as the average of the visual analogue scale (VAS) scores from 5 pain subscale questions. Subjects mark the VAS, which is a horizontal line 100 mm in length, with a single vertical line to indicate their pain level over the last 24 hours, with 0 mm representing No Pain and 100 mm representing Extreme Pain.~The WOMAC pain subscale score difference was calculated as the WOMAC pain subscale score assessed at Week 6 minus the WOMAC pain subscale score assessed at baseline." (NCT01461369)
Timeframe: Baseline to Week 6

Interventionmm (Least Squares Mean)
Diclofenac 35 mg Two Times Daily-36.64
Diclofenac 35 mg Three Times Daily-43.51
Placebo-31.08

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Total Pain Relief (TOTPAR) Over 0 to 4 Hours. TOTPAR-4.

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight.The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 16 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 4 hours

Interventionunits on a scale*hour (Mean)
Celecoxib2.226
Diclofenac Test (Lower Dose)2.112
Diclofenac Test (Upper Dose)2.530
Placebo1.387

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TOTPAR-24. Total Pain Relief (TOTPAR) Over 0 to 24 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 96 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 24 hours

Interventionunits on a scale*hour (Mean)
Celecoxib10.670
Diclofenac Test (Lower Dose)10.186
Diclofenac Test (Upper Dose)13.325
Placebo3.566

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TOTPAR-48. Total Pain Relief (TOTPAR) Over 0 to 48 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 192 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 48 hours

Interventionunits on a scale*hour (Mean)
Celecoxib22.972
Diclofenac Test (Lower Dose)21.635
Diclofenac Test (Upper Dose)28.054
Placebo4.925

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TOTPAR-8. Total Pain Relief (TOTPAR) Over 0 to 8 Hours

"Pain relief was assessed using a 5-point categorical scale at all assessment time points after time 0. Subjects were asked How much relief have you had since your starting pain? with response choices of none = 0, a little = 1, some = 2, a lot = 3, and complete = 4.~The Total Pain Relief (TOTPAR) score for a given time interval is calculated as the sum of the pain relief scores at each follow-up time point (as recorded on the categorical pain relief scale) over that interval multiplied by the amount of time (in hours) since the prior assessment. In this way individual scores covering a longer time period were given more weight. The minimum theoretical score is 0 units, which represent no relief from pain (score of 0 on categorical scale) at all time points after time 0. The maximum theoretical score is 32 units, which represents complete relief from pain (score of 4 on a categorical scale) at all time points after time 0." (NCT01462435)
Timeframe: 0 - 8 hours

Interventionunits on a scale*hour (Mean)
Celecoxib3.840
Diclofenac Test (Lower Dose)3.690
Diclofenac Test (Upper Dose)4.652
Placebo1.943

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VASSPID-24. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 24 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 24 hours

Interventionmm*hour (Mean)
Celecoxib170.845
Diclofenac Test (Lower Dose)177.101
Diclofenac Test (Upper Dose)230.708
Placebo48.811

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VASSPID-8. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 8 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 8 hours

Interventionmm*hour (Mean)
Celecoxib51.675
Diclofenac Test (Lower Dose)56.404
Diclofenac Test (Upper Dose)64.689
Placebo23.151

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VASSPID-4. The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale (VASSPID) From 0 to 4 Hours After Trial Entry.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 4 hours

Interventionmm*hour (Mean)
Celecoxib25.109
Diclofenac Test (Lower Dose)27.450
Diclofenac Test (Upper Dose)31.568
Placebo14.406

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The Time-Weighted Summed Pain Intensity Difference Measured Using the 100-mm Visual Analogue Scale From 0 to 48 Hours After Trial Entry (VASSPID-48), ANCOVA Model.

"The pain intensity is assessed using a visual analogue scale (VAS), which is a horizontal line 100 mm in length. Subjects mark the VAS with a single vertical line to indicate their current pain level, with 0 mm representing No Pain and 100 mm representing Worst Possible Pain.~The VAS summed pain intensity difference (VASSPID) is calculated as the sum of the pain intensity difference values at each follow-up time point (difference between the starting pain intensity and the pain intensity at the given assessment time) multiplied by the amount of time (in hours) since the prior assessment." (NCT01462435)
Timeframe: 0 - 48 hours

Interventionmm*hour (Mean)
Celecoxib390.468
Diclofenac Test (Lower Dose)392.954
Diclofenac Test (Upper Dose)524.315
Placebo76.887

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Clinical Neuropathic Pain Features- Burning After Treatment

"Subjects rated their burning pain using the Visual Analog Scale after a 2 week phase of using pennsaid lotion and after a 2 week phase of using placebo lotion.~The Visual Analog Scale is subject reported on a scale of 0-10 with 0 being no pain, and 10 being the worst pain they can imagine. Results reported are an average of reported VAS scores for the 28 subjects who completed both phase I and phase II of the study." (NCT01508676)
Timeframe: 2 weeks

InterventionVisual Analog Scale (Mean)
Pennsaid2.9
Placebo4.3

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Clinical Neuropathic Pain Features- Constant Pain and Hypersensitivity After Treatment

"Subjects rated their constant pain and hypersensitivity using the Visual Analog Scale after a 2 week phase of using pennsaid lotion and after a 2 week phase of using placebo lotion.~The Visual Analog Scale is subject reported on a scale of 0-10 with 0 being no pain, and 10 being the worst pain they can imagine. Results reported are an average of reported VAS scores for the 28 subjects who completed both phase I and phase II of the study." (NCT01508676)
Timeframe: 2 weeks

InterventionVisual Analog Scale (Mean)
Pennsaid4.0
Placebo4.3

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VAS After Treatment

"Subjects rated their pain using the Visual Analog Scale after a 2 week phase of using pennsaid lotion and after a 2 week phase of using placebo lotion.~The Visual Analog Scale is subject reported on a scale of 0-10 with 0 being no pain, and 10 being the worst pain they can imagine. Results reported are an average of reported VAS scores for the 28 subjects who completed both phase I and phase II of the study." (NCT01508676)
Timeframe: 2 weeks.

InterventionVisual Analog Scale (Mean)
Pennsaid4.9
Placebo5.6

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Mean Short Form-36 Mental Component Summary Scores at Week 52/Early Termination (ET) and Change From Baseline to Week 52/ET

The Short Form-36 is a validated 11-item health survey that assesses subject views about his/her functional health and well-being. The survey consists of 36 questions concerning daily or recent health-related activities and assesses 8 health domains using scaled scores. The mental component score is composed of a subset of the 8 health domains. Each scale is directly transformed into a 0 to 100 scale on the assumption that each question carries equal weight. A score of 0 is equal to maximum disability, and a score of 100 is equivalent to no disability. (NCT01510912)
Timeframe: Baseline to Week 52/Early Termination

Interventionunits on a scale (Mean)
Mean score at Week 52/early termination (ET)Change from baseline to Week 52/ET
Diclofenac 35 mg Capsules52.30.1

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Mean Short Form-36 Physical Component Summary Scores at Week 52/Early Termination (ET) and Change From Baseline to Week 52/ET

The Short Form-36 is a validated 11-item health survey that assesses subject views about his/her functional health and well-being. The survey consists of 36 questions concerning daily or recent health-related activities and assesses 8 health domains using scaled scores. The physical component score is composed of a subset of the 8 health domains. Each scale is directly transformed into a 0 to 100 scale on the assumption that each question carries equal weight. A score of 0 is equal to maximum disability, and a score of 100 is equivalent to no disability. (NCT01510912)
Timeframe: Baseline to Week 52/Early Termination

Interventionunits on a scale (Mean)
Mean score at Week 52/early termination (ET)Mean change from baseline to Week 52/ET
Diclofenac 35 mg Capsules44.24.5

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Safety of Diclofenac 35 mg Capsules as Assessed by the Incidence of Adverse Events From Baseline to Week 52 or Early Termination

The safety of Diclofenac 35 mg capsules was assessed by the number of subjects with treatment-emergent adverse events (TEAEs), severe TEAEs, and serious adverse events. (NCT01510912)
Timeframe: Baseline to Week 52/Early Termination

Interventionparticipants (Number)
Subjects with at least 1 TEAESubjects with at least 1 severe TEAESubjects with at least 1 serious adverse event
Diclofenac 35 mg Capsules4514142

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Change From Baseline to Week 4 in Laboratory Results of International Normalized Ratio (INR)

INR will be evaluated to determine if there is any significant effect of Pennsaid on coagulation parameters. (NCT01511939)
Timeframe: Baseline to Week 4

Interventionratio (Mean)
Pennsaid, Warfarin0.63
Pennsaid, Dabigatran0.09
Pennsaid, Aspirin and/or Clopidogrel0.00

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Change From Baseline to Week 4 in Laboratory Results of Partial Thromboplastin Time (PTT)

PTT will be evaluated to determine if there is any significant effect of Pennsaid on coagulation parameters. (NCT01511939)
Timeframe: Baseline to Week 4

InterventionSeconds (Mean)
Pennsaid, Warfarin2.68
Pennsaid, Dabigatran1.50
Pennsaid, Aspirin and/or Clopidogrel-0.29

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Change From Baseline to Week 4 in Laboratory Results of Platelet Aggregation

Platelet Aggregation will be evaluated to determine if there is any significant effect of Pennsaid on coagulation parameters. (NCT01511939)
Timeframe: Baseline to Week 4

InterventionSeconds (Mean)
Pennsaid, Warfarin8.14
Pennsaid, Dabigatran-39.25
Pennsaid, Aspirin and/or Clopidogrel-13.30

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Change From Baseline to Week 4 in Laboratory Results of Prothrombin Time (PT)

PT will be evaluated to determine if there is any significant effect of Pennsaid on coagulation parameters. (NCT01511939)
Timeframe: Baseline to week 4

Interventionseconds (Mean)
Pennsaid, Warfarin6.97
Pennsaid, Dabigatran0.96
Pennsaid, Aspirin and/or Clopidogrel-0.04

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Pain on Movement

"Change on a Visual analog scale from Baseline. Pain on Movement at 48 hours assessed on a 100 mm visual analog scale with anchors at 0=No pain and 100= Extreme pain" (NCT01666197)
Timeframe: 48 hours

Interventionmm (Mean)
Diclofenac Potassium 25 mg Tablet31.3
Placebo59.2

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Area Under the Curve (AUC) of the Pain Scores.

Pain will be scored by the patient at the end of surgery (time 0) and at 15-minute intervals after surgery for a total of 6 hours on a 0-100 mm VAS (from 0 = no pain to 100 = worst pain imaginable). (NCT01706588)
Timeframe: Pain scores will be measured over the time from end of surgery (time 0) to the 6 hour post-surgery

Interventionmm*minutes (Mean)
Diclofenac Sodium 5 mg/mL6843
Diclofenac Sodium 12.5 mg/mL8832
Diclofenac Sodium 25 mg/mL9998
Diclofenac Sodium 50 mg/mL7290
Placebo 1 mL15539

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Sense Wear Armband

Our secondary aim was to measure the change in physical activity between baseline and 8 weeks using the Sense Wear armband (SWA). The outcome measure was the average number of minutes spent daily performing physical activities >1.5 metabolic equivalents (METs).The SWA is a small device that collects information from multiple sensors: a triaxial accelerometer, heat flux, skin temperature, and galvanic signal. The information is integrated and processed by software using proprietary algorithms utilizing subjects' demographic characteristics (gender, age, height, and weight) to provide minute-by-minute estimates of physical activity. The SWA has shown good reliability and validity. The research participants in our study will wear the SWA for a week before and after they complete the treatment interventions. (NCT01943435)
Timeframe: Primary End-Point was 8 weeks ( 2 weeks after completion of 6-week intervention).

Interventionminutes per day (Mean)
Medical Care-23.1
Group Exercise4.3
Manual Therapy and Exercise-6.0

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Swiss Spinal Stenosis (SSS) Questionnaire Score

Our primary aim included a primary outcome measure of self-reported pain/function, which was the change in SSS total score between baseline and 8 weeks. The Swiss Spinal Stenosis Questionnaire (SSS) is a validated 12-item condition-specific instrument for patients with lumbar spinal stenosis. It provides a patient self-report measure of pain and physical function. Higher scores represent worse symptoms and less physical function. The 12-item SSS total score range is 12-55. For our analysis, we compared the change in the 12-item Total score from baseline to 8 weeks. (NCT01943435)
Timeframe: Primary End-Point was 8 weeks ( 2 weeks after completion of 6-week intervention).

Interventionunits on a scale (Mean)
Medical Care-2.0
Group Exercise-1.7
Manual Therapy and Exercise-4.1

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Self Paced Walking Test (SPWT)

Our primary aim also included a performance-based outcome measure, which was the distance walked during the SPWT. The analysis was a comparison of between-group changes in SPWT between baseline and 8 weeks. The Self-Paced Walking Test (SPWT) is a validated objective measure of a patient's walking capacity, which is performed on a level walking surface. The patient is instructed to walk at their own pace and to stop when the symptoms are troublesome enough that s/he needs to sit down to rest. The total time and total distance walked are measured by the research assistant. Our unit of measure was the total distance walked, expressed in meters. (NCT01943435)
Timeframe: Primary end-point was 8 weeks ( 2 weeks after 6 week intervention is completed).

Interventionmeters (Mean)
Medical Care130.5
Group Exercise219.2
Manual Therapy and Exercise267.8

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Measure: Pain On Movement (POM)

POM will be assessed by subject on a 100 mm Visual Analog Scale (VAS). The VAS ranges from 0 to 100 with higher score indicating higher levels of pain. (NCT01967550)
Timeframe: 2 weeks

Interventionunits on a scale (Mean)
Diclofenac Diethylamine, DDEA 2.32% Gel42.9
Placebo42.1

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Percentage Difference of Numeric Pain Rating Scale (NPRS) Pain Score From Baseline to (1) the First Hour and (2) the Second Hour After the First Dose of Zipsor® Administration.

Numeric Pain Rating Scale (NPRS) measures the subject intensity of pain on an 11-point scale. 0 = No Pain, 10 = Worst Pain at baseline to (1) the first hour and (2) the second hour after the first dose of Zipsor® administration. (NCT01982539)
Timeframe: From Baseline to 1st and 2nd hour

InterventionPercent Change of NPRS Score (Mean)
Percent Change from baseline to 1 hour postdosePercent Change from Baseline to 2 hours post dose
Zipsor® (Liquid Filled Capsules)-55.32-60.25

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Changes in the Numeric Pain Rating Scale (NPRS) Pain Score From Baseline to (1) the First Hour and (2) the Second Hour After the First Dose of Zipsor® Administration.

Numeric Pain Rating Scale (NPRS) measures the subject intensity of pain on an 11-point scale. 0 = No Pain, 10 = Worst Pain at baseline to (1) the first hour and (2) the second hour after the first dose of Zipsor® administration. (NCT01982539)
Timeframe: From Baseline to 1st and 2nd hour

Interventionscore on a scale (Mean)
Baseline1st Hour2nd Hour
Zipsor® (Liquid Filled Capsules)4.12.01.7

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Safety and Tolerability of Zipsor® in Pediatric Subjects, Ages 12 to 17 Years

"Safety Endpoints:~Treatment emergent AEs (TEAEs)~Serious adverse events (SAEs)~Withdrawals due to AEs~Deaths~Observed values and changes in vital sign measurements~Observed values and changes in clinical laboratory results~Physical examination findings" (NCT01982539)
Timeframe: First dose to 30 days after the last dose

Interventionparticipants (Number)
Treatment-emergent adverse events (TEAEs)Severe TEAEsSerious TEAEsSerious Adverse Events (SAEs)Withdrawals due to AEsDeaths
Zipsor® (Liquid Filled Capsules)1201100

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Mean Reduction in SPID Scores of DOMS at Rest Over 24 Hours

"The secondary outcome is the mean reduction in DOMS scores at rest in the leg receiving Topical Voltaren® gel versus the leg receiving placebo over the first 24 hours post treatment initiation.~Pain intensity was assessed at predefined time points (at Predose, 3, 9, 15, 21, and 24 hours after first drug administration) using an 11-point Numeric Rating Scale (NPRS) where a score of zero indicates no pain and a score of 10 indicates pain as bad as you can imagine. Pain Intensity Differences at each predefined time point (calculated as post-baseline NPRS values - baseline NPRS values) were analyzed. The theoretical maximum range of Sum of pain intensity differences (SPID24) is from -50 (indicative of an increase in pain) to 50 (indicative of a decrease in pain)." (NCT02087748)
Timeframe: 7 days

Interventionunits on a scale (Mean)
1% Diclofenac Sodium Gel28.06
Placebo24.81

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Mean Reduction in SPID Scores of DOMS on Walking Over 24 Hours

"The primary outcome is the analgesic efficacy of Topical Voltaren® gel compared to placebo in the reduction of the pain associated with DOMS. The statistical comparison of interest will be the mean reduction in DOMS scores upon walking in the leg receiving Topical Voltaren® gel vs the leg receiving placebo over the first 24 hours post treatment. Pain intensity was assessed at predefined time points (Predose, 3, 9, 15, 21, and 24 hours after first drug administration) using an 11-point Numeric Rating Scale (NPRS) where a score of zero indicates no pain and 10 indicates pain as bad as you can imagine. Pain Intensity Differences at each predefined time point (calculated as post-baseline NPRS values - baseline NPRS values) were analyzed. The theoretical maximum range of Sum of pain intensity differences (SPID24) is from -50 (indicative of an increase in pain) to 50 (indicative of a decrease in pain)." (NCT02087748)
Timeframe: 7 days

Interventionunits on a scale (Mean)
1% Diclofenac Sodium Gel34.87
Placebo23.62

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Mean Reduction in SPID Scores of DOMS While Standing Over 24 Hours

"The secondary outcome is the mean reduction in DOMS scores while standing in the leg receiving Topical Voltaren® gel versus the leg receiving placebo over the first 24 hours post treatment initiation.~Pain intensity was assessed at predefined time points (at Predose, 3, 9, 15, 21, and 24 hours after first drug administration) using an 11-point Numeric Rating Scale (NPRS) where a score of zero indicates no pain and a score of ten indicates pain as bad as you can imagine. Pain Intensity Differences at each predefined time point (calculated as post-baseline NPRS values - baseline NPRS values) were analyzed. The theoretical maximum range of Sum of pain intensity differences (SPID24) is from -50 (indicative of an increase in pain) to 50 (indicative of a decrease in pain)." (NCT02087748)
Timeframe: 7 days

Interventionunits on a scale (Mean)
1% Diclofenac Sodium Gel33.9
Placebo21.62

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Pain Relief Score (PRS)

Pain relief was measured at each time point using a 5-point Pain Relief Scale ranging from 0-4 while at rest (Where: 0- No pain relief; 1- A little or perceptible pain relief; 2- Meaningful pain relief; 3- A lot of relief; 4- Complete relief). Participants assessed the degree of ankle pain relief using the PRS scores at 10, 30 minutes and 1, 4, 6, 12, 18 and 24 hours after the first dose of treatment and twice daily after the first day of treatment. (NCT02100670)
Timeframe: Day 1 to Day 7

,,,
Interventionscore on a scale (Mean)
At 10 min. (n= 117, 111, 77, 74)At 30 min. (n=117, 111, 77, 75)At 1 hour (n=116, 112, 77, 75)At 4 hour (n= 115, 110, 74, 71)At 6 hour (n= 109, 105, 70, 69)At 12 hour (n= 77, 89, 53, 58)At 18 hour (n= 76, 78, 53, 57)At 24 hour (n= 111, 105, 72, 72)At 36 hour (n= 116, 112, 77, 74)At 48 hour (n= 116, 112, 77, 75)At 60 hour (n=115, 111, 77, 75)At 72 hour (n= 114, 109, 75, 74)At 84 hour (n= 113, 106, 75, 75)At 96 hour (n= 112, 106, 75, 74)At 108 hour (n= 111, 105, 75, 74)At 120 hour (n= 111, 107, 74, 72)At 132 hour (n= 110, 107, 73, 74)At 144 hour (n= 110, 107, 74, 73)At 156 hour (n= 109, 106, 74, 74)At 168 hour (n= 105, 103, 73, 73)
1% Diclofenac Sodium0.290.360.460.450.540.720.730.740.840.841.001.061.001.031.131.141.241.211.301.31
1% Diclofenac Sodium+3% Menthol0.330.440.480.470.500.600.710.790.840.901.070.931.071.091.181.111.341.211.411.41
3% Menthol0.320.490.570.510.630.740.830.900.880.991.161.161.251.011.281.241.341.301.471.34
Placebo0.360.440.400.490.450.620.700.810.780.990.960.971.111.091.151.101.301.271.321.40

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Pain Intensity Difference (PID) on Movement

"PID on movement, calculated as PI at a given time 't' (after walking 5 steps on a flat surface) subtracted by the PI at baseline.~Participants assessed the severity of ankle pain (PI) using the NRS scale from 0 (no pain) to 10 (extreme pain). PI was measured at baseline (prior to treatment) and at 10, 30 minutes (min.) and 1, 4, 6, 12, 18 and 24 hours after the first dose of treatment and twice daily after dosing." (NCT02100670)
Timeframe: Baseline to 10 days

,,,
Interventionscore on scale (Mean)
PI at Baseline (n=117, 112, 77, 75)PID at 10 min. (n=117, 112, 77, 75)PID at 30 min. (n=117, 112, 77, 75)PID at 1 hour (n=117, 112, 77, 75)PID at 4 hour (n=117, 112, 77, 75)PID at 6 hour (n=117, 112, 77, 75)PID at 12 hour (n= 117, 112, 77, 75)PID at 18 hour (n=117, 112, 77, 75)PID at 24 hour (n=117, 112, 77, 75)PID at 36 hour (n=117, 112, 77, 75)PID at 48 hour (n=117, 112, 77, 75)PID at 60 hour (n=117, 112, 77, 75)PID at 72 hour (n=117, 112, 77, 75)PID at 84 hour (n=113, 107, 75, 75)PID at 96 hour (n=112, 107, 75, 74)PID at 108 hour (n=112, 107, 75, 74)PID at 120 hour (n=111, 107, 74, 74)PID at 132 hour (n=110, 107, 74, 74)PID at 144 hour (n=110, 107, 74, 74)PID at 156 hour (n=109, 107, 74, 74)PID at 168 hour (n=105, 104, 73, 74)PID at 180 hour (n=105, 104, 73, 72)PID at 192 hour (n=101, 102, 71, 72)PID at 204 hour (n=101, 100, 71, 72)PID at 216 hour (n=95, 100, 69, 72)PID at 228 hour (n=95, 100, 69, 72)PID at 240 hour (n=32, 43, 22, 42)
1% Diclofenac Sodium7.40.190.360.500.480.670.991.321.581.652.012.262.422.682.783.013.173.533.784.054.114.454.594.945.215.625.44
1% Diclofenac Sodium+3% Menthol7.80.230.440.560.710.790.841.191.621.591.912.412.552.843.103.343.383.703.764.174.264.584.555.175.285.715.56
3% Menthol7.80.290.490.640.790.911.171.441.751.552.042.562.553.083.033.483.353.723.683.953.904.374.214.874.875.285.41
Placebo7.70.320.550.640.690.870.951.161.531.321.922.052.282.682.783.183.143.473.593.883.954.084.224.564.785.015.60

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Ankle Swelling

"Ankle swelling measured by figure of eight method of injured ankle." (NCT02100670)
Timeframe: Day 1 (baseline), 3, and 7

,,,
InterventionMillimeters (Mean)
At Day 1At Day 3At Day 7
1% Diclofenac Sodium573.6566.9558.8
1% Diclofenac Sodium+3% Menthol573.9566.2558.3
3% Menthol577.1567.0558.4
Placebo576.1565.4557.0

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Time to Complete Recovery

Time to complete recovery measured as the day with complete relief of ankle pain (Participant-rated NRS scores were 0 for pain intensity at rest and pain) and swelling (Participants did not have any apparent swelling nor experience any pain or limitation of movement of the injured ankle as determined by the Principal Investigator or designee during the course of an ankle exam). (NCT02100670)
Timeframe: up to 240 hours

InterventionHours (Median)
1% Diclofenac Sodium+3% Menthol240.00
1% Diclofenac Sodium240.00
3% Menthol240.00
Placebo240.00

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Total Pain Relief (TOTPAR)

TOTPAR was calculated as sum of the products of PRS with time interval from one time point to the other. PRS was measured at each time point on a scale: 0= No pain relief, 1= A little or perceptible pain relief, 2= Meaningful pain relief, 3= A lot of relief, 4= Complete relief. The possible range of TOTPAR for 0-6 hours was from 0 to 24, for 0-12 hours was from 0 to 48, for 0-24 hours was from 0 to 96, for 0-72 hours was from 0 to 288, for 24-72 hours was from 0 to 192 and for 0-168 hours was from 0 to 672. (NCT02100670)
Timeframe: Baseline to 168 hours

,,,
InterventionPRS Score (0 - 4 scale) (Mean)
0-6 hours0-12 hours0- 24 hours0-72 hours24-72 hours0-168 hours
1% Diclofenac Sodium2.646.8116.1461.2445.11170.73
1% Diclofenac Sodium+3% Menthol2.816.8616.0460.1444.10172.97
3% Menthol3.278.0218.8566.6947.84184.17
Placebo2.756.3515.7158.7543.04174.00

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Time of Onset of Pain Relief (TOPR)

"TOPR was measured by time when participants reported PRS ≥ 1, i.e. a little or perceptible pain relief'." (NCT02100670)
Timeframe: Baseline to 10 days (end of study)

InterventionHours (Median)
1% Diclofenac Sodium+3% Menthol1.03
1% Diclofenac Sodium4.00
3% Menthol1.00
Placebo4.00

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Time of Onset of Meaningful Pain Relief (TOMR)

"TOMR was measured by time when participants reported PRS ≥ 2, i.e. some or meaningful pain relief" (NCT02100670)
Timeframe: up to 10 days (end of study)

InterventionHours (Median)
1% Diclofenac Sodium+3% Menthol92.50
1% Diclofenac Sodium76.83
3% Menthol72.00
Placebo93.50

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Time of Onset of Cooling Sensation (TOCS)

"Time of onset of cooling sensation measured by time when subjects reported to have a 'cooling effect as an enhancement of pain relief'. To assess this endpoint, participants were asked at 10, 30 minutes and at 1, 4, 6 hours post first dose Do you feel a cooling sensation at the injured ankle from the study gel?" (NCT02100670)
Timeframe: up to 6 hours

InterventionHours (Median)
1% Diclofenac Sodium+3% Menthol0.17
1% Diclofenac Sodium0.17
3% Menthol0.17
Placebo0.17

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AUC1-3 Days of PI on Movement for Diclofenac Sodium + Methanol, Diclofenac, Methanol and Placebo

AUC of PI on movement was measured by a numerical rating scale (NRS) during the 48 hour time interval from Day 1 to 3. AUC1-3 day was calculated based on trapezoidal method. Pain intensity was measured in NRS scale from 0 (no pain) to 10 (extreme pain). Participants assessed the severity of ankle pain using the NRS scale at baseline (prior to treatment) and at 10, 30 minutes and 1, 4, 6, 12, 18 and 24 hours after the first dose of treatment and twice daily after dosing. (NCT02100670)
Timeframe: up to 72 hours

InterventionNRS Score (0 - 10 scale) * hrs (Mean)
1% Diclofenac Sodium+3% Menthol276.97
1% Diclofenac Sodium261.11
3% Menthol272.65
Placebo282.88

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Sum of Pain Intensity Difference (SPID)

SPID was calculated as the time weighted sum of pain intensity differences (PID) from 0 to 7 Days. PID was calculated as PI at a given time point 't' subtracted by the PI at baseline. PI was measured on NRS scale from 0 (no pain) to 10 (extreme pain). The possible range of SPID for 0-6 hours was from -60 to 60, for 0-12 hours was from -120 to 120, for 0-1 day was from -240 to 240, for 0-3 days was from -720 to 720, for 0-7 days was from -1680 to 1680. A higher value of SPID indicates greater pain relief. (NCT02100670)
Timeframe: Baseline to Day 7

,,,
Interventionscore on a scale (Mean)
At 0-6 hoursAt 0-12 hoursAt 0-1 daysAt 1 to 3 daysAt 0 to 7 days
1% Diclofenac Sodium3.199.1326.54100.07452.44
1% Diclofenac Sodium+3% Menthol4.169.1926.01101.54451.12
3% Menthol4.7211.7430.91104.26464.96
Placebo4.3710.0526.2190.88438.45

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Area Under the Curve From Day 1 to Day 3 (AUC1-3 Days) of Pain Intensity(PI) on Movement for Diclofenac/Methanol Gel and Placebo Gel

AUC of PI on movement was measured by a numerical rating scale (NRS) during the 48 hour time interval from Day 1 to 3. AUC1-3 day was calculated based on trapezoidal method. Pain intensity was measured in NRS scale from 0 (no pain) to 10 (extreme pain). Participants assessed the severity of ankle pain using the NRS scale at baseline (prior to treatment) and at 10, 30 minutes and 1, 4, 6, 12, 18 and 24 hours after the first dose of treatment and twice daily after dosing. (NCT02100670)
Timeframe: up to 72 hours

InterventionNRS Score (0 - 10 scale) * hrs (Mean)
1% Diclofenac Sodium Plus (+) 3% Menthol276.97
Placebo282.88

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Skin Temperature

Skin temperature was measured by thermal imaging. (NCT02100670)
Timeframe: At 10, 30, 60 minutes, 4 and 6 hours

,,,
Interventiondegree celsius (°C) (Mean)
At 10 min.At 30 min.At 60 min.At 240 min.At 360 min.
1% Diclofenac Sodium29.3129.8130.7431.2631.53
1% Diclofenac Sodium+3% Menthol27.6928.2628.6430.5231.02
3% Menthol29.9230.5030.2231.1531.27
Placebo30.9331.4731.7831.5732.07

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PID at Rest

"PID at rest was calculated as PI at a given time point't' (at rest) subtracted by the PI at baseline. Participants assessed the severity of ankle pain (PI) using the NRS scale from 0 (no pain) to 10 (extreme pain).~PI was measured at baseline (prior to treatment) and at 10, 30 minutes and 1, 4, 6, 12, 18 and 24 hours after the first dose of treatment and twice daily after dosing." (NCT02100670)
Timeframe: Baseline to 10 days

,,,
Interventionscore on a scale (Mean)
PI at Baseline (n=117, 112, 77, 75)PID at 10 min. (n=117, 112, 77, 75)PID at 30 min. (n=117, 112, 77, 75)PID at 1 hour (n=117, 112, 77, 75)PID at 4 hour (n=117, 112, 77, 75)PID at 6 hour (n= 117, 112, 77, 75)PID at 12 hour (n= 117, 112, 77, 75)PID at 18 hour (n= 117, 112, 77, 75)PID at 24 hour (n= 117, 112, 77, 75)PID at 36 hour (n= 117, 112, 77, 75)PID at 48 hour (n=117, 112, 77, 75)PID at 60 hour (n= 117, 112, 77, 75)PID at 72 hour (n= 117, 112, 77, 75)PID at 84 hour (n= 113, 107, 75, 75)PID at 96 hour (n= 112, 107, 75, 74)PID at 108 hour (n=112, 107, 75, 74)PID at 120 hour (n= 111, 107, 74, 74)PID at 132 hour (n= 110, 107, 74, 74)PID at 144 hour (n= 110, 107, 74, 74)PID at 156 hour (n= 109, 107, 74, 74)PID at 168 hour (n= 105, 104, 73, 74)PID at 180 hour (n= 105, 104, 73, 72)PID at 192 hour (n= 101, 102, 71, 72)PID at 204 hour (n= 101, 100, 71, 72)PID at 216 hour (n= 95, 100, 69, 72)PID at 228 hour (n= 95, 100, 69, 72)PID at 240 hour (n= 32, 43, 22, 42)
1% Diclofenac Sodium7.40.430.450.620.530.620.861.141.391.321.531.831.912.192.172.432.482.782.773.113.153.383.303.613.874.024.23
1% Diclofenac Sodium+3% Menthol7.80.340.560.640.620.680.761.031.321.201.431.911.912.112.262.462.592.762.773.063.083.373.383.673.774.093.94
3% Menthol7.80.170.320.480.660.750.901.101.471.221.511.881.862.192.232.482.302.682.592.772.752.952.903.373.223.643.36
Placebo7.70.250.440.410.430.530.680.851.131.091.451.641.762.032.002.272.092.492.492.652.642.883.003.213.263.533.67

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Patient's Global Assessment in Response to Treatment (PGART)

PGART was measured at the end of study in a scale from 0-4 (Where: 0- Poor; 1- Fair; 2- Good; 3- Very Good; 4- Excellent) (NCT02100670)
Timeframe: up to Day 10

,,,
InterventionParticipants (Number)
Poor=0Fair=1Good=2Very Good=3Excellent=4
1% Diclofenac Sodium132046266
1% Diclofenac Sodium+3% Menthol32444359
3% Menthol61226265
Placebo91427214

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Change From Baseline to 4 Weeks in WOMAC Pain Score

"Mean change from baseline to week 4 in the Western Ontario McMaster~Osteoarthritis (WOMAC) pain score:~5-point Likert scale: none=o, mild=1, moderate=2, severe=3, extreme=4" (NCT02121002)
Timeframe: Baseline and Week 4

Interventionscore on a scale (Least Squares Mean)
Diclofenac Sodium Topical Gel, 1%2.2332
Voltaren Topical Gel, 1%2.0287
Vehicle Diclofenac Sodium Topical Gel-0.6387

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Dermatologic Assessment at the Patch Application Site

None - 0; Faint redness - 1; Moderate redness - 2; Intense redness - 3; Redness with edema or papules - 4; Redness with weeping vesicles, blisters or bullae - 5; Redness with extension of effect beyond margin of contact site - 6. (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
InterventionUnits on a scale (Mean)
Day1-2Day 3-4Day 5-7Day 8-11Day 12-15
Flector Patch/Age 12-160.040.060.000.060.00
Flector Patch/Age 6-110.100.040.110.000.00

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Investigator Assessment of the Global Response to Therapy on a 5-point Scale

5-point scale: No clinical improvement in pain intensity and/or functional performance - 1; Slight clinical improvement in pain intensity and/or functional performance - 2; Moderate clinical improvement in pain intensity and/or functional performance - 3; Marked clinical improvement in pain intensity and/or functional performance - 4; Restoration of normal functional performance in the absence of any pain - 5. (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
InterventionParticipants (Count of Participants)
No clinical improvementSlight clinical improvementModerate clinical improvementMarked clinical improvementNormal function with no pain
Flector Patch/Age 12-16102940
Flector Patch/Age 6-11102247

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Plasma Concentration of Diclofenac

(NCT02132247)
Timeframe: Day 2 and either Day 4, 7 or 14, depending upon pain resolution

,
Interventionng/mL (Mean)
24-hourFinal Visit
Flector Patch/Age 12-161.461.11
Flector Patch/Age 6-111.832.49

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Patient Assessment of Pain on a 6-point Scale

"Wong-Baker FACES Scale 6-point scale:~No Hurt - 0; Hurts Little Bit - 1; Hurts Little More - 2; Hurts Even More - 3; Hurts Whole Lot - 4; Hurts Worst - 5." (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
Interventionunits on a scale (Mean)
BaselineFinal Visit
Flector Patch/Age 12-163.580.27
Flector Patch/Age 6-113.370.12

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Pain Scores on Standardized Experimental Pain Testing

Pain scores on standardized experimental pain testing, with collection of Visual analog scales (VAS) on a 0-100 scale 0 (no pain)- 100 (worst pain imaginable) Higher values represent a worse outcome (more pain) (NCT02194088)
Timeframe: baseline and 1 hour pain measurement

,
Interventionunits on a scale (Mean)
Baseline1 hour Assessment
Pain Medication: Diclofenac and Atropine59.644.1
Placebo54.045.3

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Sum of Pain Intensity Differences Over 48 Hours After Initiating Treatment (SPID 48), Derived From POW.

"Sum of pain intensity differences over 48 hours after initiating treatment (SPID 48) (POW) was a secondary outcome.~Sum of pain intensity differences over 48 hours after initiating treatment (SPID 48) for the modified ITT population. SPID 48 derived from Pain on Walking (POW) scores assessed over 48 hours on a 0 (No pain) - 10 (Pain as bad as you can imagine) Numerical Rating Scale. SPID 48 was computed using the trapezoidal rule, i.e. Σ [T(i) - T(i-1)] x [((PID)(i-1) + PID(i))/2] in an obvious notation, where T(i) is nominal time and PID(i), the pain intensity difference at Time i, is the baseline pain intensity (PI) score - PI score at Time i." (NCT02271854)
Timeframe: 48 hours

Interventionunits on a scale (NRS) (Mean)
Diclofenac Sodium Gel 1%151.8
Placebo160.84

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Sum of Pain Intensity Differences Over 24 Hours After Initiating Treatment (SPID 24), Derived From POW.

The primary efficacy outcome was the time-weighted SPID 24 (POW). Sum of pain intensity differences over 24 hours after initiating treatment (SPID 24) for the modified ITT population. SPID 24 derived from Pain on Walking (POW) scores assessed over 24 hours on a 0 (No pain) - 10 (Pain as bad as you can imagine) Numerical Rating Scale. SPID 24 was computed using the trapezoidal rule, i.e. Σ [T(i) - T(i-1)] x [((PID)(i-1) + PID(i))/2] in an obvious notation, where T(i) is nominal time and PID(i), the pain intensity difference at Time i, is the baseline pain intensity (PI) score - PI score at Time i. (NCT02271854)
Timeframe: 24 hours

Interventionunits on a scale (NRS) (Mean)
Diclofenac Sodium Gel 1%50.15
Placebo54.83

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.6 of 7).

• Changes in clinical laboratory results: Hematology - Eosinophils (%). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention% Eosinophils (Mean)
Baseline (% Eosinophils)Final Visit (% Eosinophils)Change from Baseline to Final Visit(% Eosinophils)
Diclofenac Potassium Oral Solution3.9114.5140.532

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.7 of 7).

• Changes in clinical laboratory results: Hematology - Neutrophils (%). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention% Neutrophils (Mean)
Baseline (% Neutrophils)Final Visit (% Neutrophils)Change from Baseline to Final Visit(% Neutrophils)
Diclofenac Potassium Oral Solution49.64948.740-0.791

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.8 of 7).

• Changes in clinical laboratory results: Hematology - Lymphocytes (%). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention% Lymphocytes (Mean)
Baseline (% Lymphocytes)Final Visit (% Lymphocytes)Change from Baseline to Final Visit(% Lymphocytes)
Diclofenac Potassium Oral Solution37.19538.1860.866

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.9 of 7).

• Changes in clinical laboratory results: Hematology - Monocytes (%). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention% Monocytes (Mean)
Baseline (% Monocytes)Final Visit (% Monocytes)Change from Baseline to Final Visit (% Monocytes)
Diclofenac Potassium Oral Solution8.5697.859-0.643

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (2 of 8).

• Tmax: time to maximum concentration (hr) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionhr (Median)
Diclofenac Potassium Oral Solution0.250

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (3 of 8).

• λz: elimination rate constant (1/hr) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Intervention1/hr (Mean)
Diclofenac Potassium Oral Solution0.47329

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (4 of 8).

• t1/2: terminal elimination half-life (hr) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionhr (Mean)
Diclofenac Potassium Oral Solution1.692

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5 of 8).

• AUC 0-t: area under the concentration-time curve from time 0 to last time point (t) where diclofenac could be measured (hr*ng/mL) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionhr*ng/mL (Mean)
Diclofenac Potassium Oral Solution454.544

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6 of 8).

• AUC 0-∞: area under the concentration-time curve from time 0 to infinity (∞) (hr*ng/mL) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionhr*ng/mL (Mean)
Diclofenac Potassium Oral Solution491.915

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (7 of 8).

• CL/F: apparent clearance (mL/hr). (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

InterventionmL/hr (Mean)
Diclofenac Potassium Oral Solution25927.177

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (8 of 8).

• Vz/F: apparent volume of distribution (mL). (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

InterventionmL (Mean)
Diclofenac Potassium Oral Solution66845.275

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (1 of 7).

• Treatment emergent AEs (TEAEs) (NCT02287350)
Timeframe: 4 weeks (first dose of study drug and up to 30 days after the date of the last dose of study drug)

InterventionParticipants (Count of Participants)
Diclofenac Potassium Oral Solution16

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (2 of 7).

• Serious adverse events (SAEs) (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to 30 days after the last dose of study drug)

InterventionParticipants (Count of Participants)
Diclofenac Potassium Oral Solution2

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (3 of 7).

• Withdrawals due to AEs (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to 30 days after the last dose of study drug)

InterventionParticipants (Count of Participants)
Diclofenac Potassium Oral Solution0

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (4 of 7).

• Deaths (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to 30 days after the last dose of study drug)

InterventionParticipants (Count of Participants)
Diclofenac Potassium Oral Solution0

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (7 of 7).

• Physical examination findings including abnormal clinically significant findings (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionParticipants (Count of Participants)
Diclofenac Potassium Oral Solution1

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To Characterize the Pharmacokinetic (PK) Profile of a Single Dose of Diclofenac Potassium Oral Solution, With Weight-based Dosing, in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (1 of 8).

• Cmax: maximum concentration (ng/mL) (NCT02287350)
Timeframe: 6 hours (pre-dose, 15, 30, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionng/mL (Mean)
Cmax (ng/mL)pre-dose concentrations (ng/mL)15 min post-dose concentrations (ng/mL)30 min post-dose concentrations (ng/mL)60 min post-dose concentrations (ng/mL)2 hrs post-dose concentrations (ng/mL)4 hrs post-dose concentrations (ng/mL)6 hrs post-dose concentrations (ng/mL)
Diclofenac Potassium Oral Solution433.90.000378.471260.484178.54467.39422.96415.042

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.1 of 7).

• Changes in vital sign measurements: Temperature (degrees C). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventiondegrees C (Mean)
Baseline (degrees C)Final Visit (degrees C)Change from Baseline to Final Visit (degrees C)
Diclofenac Potassium Oral Solution36.9436.67-0.29

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.2 of 7).

• Changes in vital sign measurements: Pulse Rate (beats/min). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionbeats/min (Mean)
Baseline (beats/min)Final Visit (beats/min)Change from Baseline to Final Visit (beats/min)
Diclofenac Potassium Oral Solution103.793.4-10.5

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.3 of 7).

• Changes in vital sign measurements: Respiratory Rate (breaths/min). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionbreaths/min (Mean)
Baseline (breaths/min)Final Visit (breaths/min)Change from Baseline to Final Visit (breaths/min)
Diclofenac Potassium Oral Solution19.719.0-0.9

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.4 of 7).

• Changes in vital sign measurements: Systolic Blood Pressure (mmHg). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionmmHg (Mean)
Baseline (mmHg)Final Visit (mmHg)Change from Baseline to Final Visit (mmHg)
Diclofenac Potassium Oral Solution110.8106.6-4.5

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (5.5 of 7).

• Changes in vital sign measurements: Diastolic Blood Pressure (mmHg). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionmmHg (Mean)
Baseline (mmHg)Final Visit (mmHg)Change from Baseline to Final Visit (mmHg)
Diclofenac Potassium Oral Solution70.165.1-5.2

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.1 of 7).

• Changes in clinical laboratory results: Hematology - Hematocrit (L/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionL/L (Mean)
Baseline (L/L)Final Visit (L/L)Change from Baseline to Final Visit (L/L)
Diclofenac Potassium Oral Solution0.3570.3630.006

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.10 of 7).

• Changes in clinical laboratory results: Chemistry - Albumin (g/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventiong/L (Mean)
Baseline (g/L)Final Visit (g/L)Change from Baseline to Final Visit (g/L)
Diclofenac Potassium Oral Solution40.88242.3411.114

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.11 of 7).

• Changes in clinical laboratory results: Chemistry - Alkaline Phosphatase (U/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Diclofenac Potassium Oral Solution219.471206.545-10.614

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.12 of 7).

• Changes in clinical laboratory results: Chemistry - ALT (SGPT) (U/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Diclofenac Potassium Oral Solution21.56917.727-1.136

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.13 of 7).

• Changes in clinical laboratory results: Chemistry - AST (SGOT) (U/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Diclofenac Potassium Oral Solution29.39225.818-2.568

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.14 of 7).

• Changes in clinical laboratory results: Chemistry - Bicarbonate (CO2) (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution23.59024.7481.109

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.15 of 7).

• Changes in clinical laboratory results: Chemistry - Bilirubin Total (umol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionumol/L (Mean)
Baseline (umol/L)Final Visit (umol/L)Change from Baseline to Final Visit (umol/L)
Diclofenac Potassium Oral Solution4.6954.042-0.319

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.16 of 7).

• Changes in clinical laboratory results: Chemistry - BUN (Urea) (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution4.2414.3800.326

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.17 of 7).

• Changes in clinical laboratory results: Chemistry - Chloride (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution102.959101.839-0.773

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.18 of 7).

• Changes in clinical laboratory results: Chemistry - Creatinine (umol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionumol/L (Mean)
Baseline (umol/L)Final Visit (umol/L)Change from Baseline to Final Visit (umol/L)
Diclofenac Potassium Oral Solution32.03235.2604.159

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.19 of 7).

• Changes in clinical laboratory results: Chemistry - Glucose (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution5.1674.851-0.361

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.2 of 7).

• Changes in clinical laboratory results: Hematology - Hemoglobin (g/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventiong/L (Mean)
Baseline (g/L)Final Visit (g/L)Change from Baseline to Final Visit (g/L)
Diclofenac Potassium Oral Solution120.5121.00.4

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.20 of 7).

• Changes in clinical laboratory results: Chemistry - LDH (U/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Diclofenac Potassium Oral Solution253.085253.071-1.256

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.21 of 7).

• Changes in clinical laboratory results: Chemistry - Potassium (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution4.3664.337-0.038

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.22 of 7).

• Changes in clinical laboratory results: Chemistry - Sodium (mmol/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Diclofenac Potassium Oral Solution138.510139.8181.409

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.23 of 7).

• Changes in clinical laboratory results: Urinalysis - pH. (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionpH (Mean)
Baseline (pH)Final Visit (pH)Change from Baseline to Final Visit (pH)
Diclofenac Potassium Oral Solution6.2816.5980.276

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.24 of 7).

• Changes in clinical laboratory results: Urinalysis - Specific Gravity. (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

InterventionSpecific Gravity (Mean)
Baseline (Specific Gravity)Final Visit (Specific Gravity)Change from Baseline to Final Visit (Spec.Gravity)
Diclofenac Potassium Oral Solution1.0221.0200.000

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.3 of 7).

• Changes in clinical laboratory results: Hematology - Platelet Count (10^9/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention10^9/L (Mean)
Baseline (10^9/L)Final Visit (10^9/L)Change from Baseline to Final Visit (10^9/L)
Diclofenac Potassium Oral Solution315.2402.285.6

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.4 of 7).

• Changes in clinical laboratory results: Hematology - White Blood Cells (10^9/L). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention10^9/L (Mean)
Baseline (10^9/L)Final Visit (10^9/L)Change from Baseline to Final Visit (10^9/L)
Diclofenac Potassium Oral Solution8.7498.807-0.054

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To Determine the Safety and Tolerability of Diclofenac Potassium Oral Solution in Pediatric Subjects, Ages 2-12 Years Experiencing Mild to Moderate Acute Pain (6.5 of 7).

• Changes in clinical laboratory results: Hematology - Basophils (%). (NCT02287350)
Timeframe: 4 weeks (signed informed consent/assent to the final visit)

Intervention% Basophils (Mean)
Baseline (% Basophils)Final Visit (% Basophils)Change from Baseline to Final Visit (% Basophils)
Diclofenac Potassium Oral Solution0.4140.4960.085

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Pharmacokinetics Outcome (6 of 6)

• AUC 0-∞: area under the concentration-time curve from time 0 to infinity (∞) (min*ng/mL) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionmin*ng/mL (Mean)
Cambia®84388.75

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Safety Outcome (6.14 of 7)

• Changes in clinical laboratory results: Chemistry - Bicarbonate (CO2) (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®23.40023.9200.520

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Safety Outcome (6.15 of 7)

• Changes in clinical laboratory results: Chemistry - Bilirubin Total (umol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionumol/L (Mean)
Baseline (umol/L)Final Visit (umol/L)Change from Baseline to Final Visit (umol/L)
Cambia®9.02910.1921.163

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Safety Outcome (6.16 of 7)

• Changes in clinical laboratory results: Chemistry - BUN (Urea) (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®4.5124.5940.081

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Safety Outcome (6.17 of 7)

• Changes in clinical laboratory results: Chemistry - Chloride (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®105.480104.880-0.600

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Safety Outcome (6.18 of 7)

• Changes in clinical laboratory results: Chemistry - Creatinine (umol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionumol/L (Mean)
Baseline (umol/L)Final Visit (umol/L)Change from Baseline to Final Visit (umol/L)
Cambia®66.76067.4670.707

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Safety Outcome (6.19 of 7)

• Changes in clinical laboratory results: Chemistry - Glucose (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®4.7584.483-0.275

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Safety Outcome (6.20 of 7)

• Changes in clinical laboratory results: Chemistry - LDH (U/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Cambia®157.882159.708-0.882

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Safety Outcome (6.21 of 7)

• Changes in clinical laboratory results: Chemistry - Potassium (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®3.9644.0600.096

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Safety Outcome (6.22 of 7)

• Changes in clinical laboratory results: Chemistry - Sodium (mmol/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmmol/L (Mean)
Baseline (mmol/L)Final Visit (mmol/L)Change from Baseline to Final Visit (mmol/L)
Cambia®138.640138.8400.200

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Pharmacokinetics Outcome (3 of 6)

• λz: elimination rate constant associated with the terminal (log linear) portion of the curve (1/min) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Intervention1/min (Mean)
Cambia®0.01

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Safety Outcome (6.23 of 7)

• Changes in clinical laboratory results: Urinalysis - pH. (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionpH (Mean)
Baseline (pH)Final Visit (pH)Change from Baseline to Final Visit (pH)
Cambia®6.2206.3000.080

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Safety Outcome (6.24 of 7)

• Changes in clinical laboratory results: Urinalysis - Specific Gravity. (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionSpecific Gravity (Mean)
Baseline (Specific Gravity)Final Visit (Specific Gravity)Change from Baseline to Final Visit (Spec.Gravity)
Cambia®1.0201.0220.002

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Safety Outcome (6.3 of 7)

• Changes in clinical laboratory results: Hematology - Platelet Count (Cells * 10^9/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionCells * 10^9/L (Mean)
Baseline (Cells * 10^9/L)Final Visit (Cells * 10^9/L)Change from Baseline to Final Visit (Cells*10^9/L)
Cambia®233.640244.96011.320

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Safety Outcome (6.4 of 7)

• Changes in clinical laboratory results: Hematology - White Blood Cells (Cells * 10^9/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionCells * 10^9/L (Mean)
Baseline (Cells * 10^9/L)Final Visit (Cells * 10^9/L)Change from Baseline to Final Visit (Cells*10^9/L)
Cambia®6.5126.262-0.249

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Safety Outcome (6.5 of 7)

• Changes in clinical laboratory results: Hematology - Basophils (%). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Intervention% Basophils (Mean)
Baseline (% Basophils)Final Visit (% Basophils)Change from Baseline to Final Visit (% Basophils)
Cambia®0.3240.3500.026

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Safety Outcome (6.6 of 7)

• Changes in clinical laboratory results: Hematology - Eosinophils (%). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Intervention% Eosinophils (Mean)
Baseline (% Eosinophils)Final Visit (% Eosinophils)Change from Baseline to Final Visit(% Eosinophils)
Cambia®2.7302.036-0.694

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Safety Outcome (6.7 of 7)

• Changes in clinical laboratory results: Hematology - Neutrophils (%). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Intervention% Neutrophils (Mean)
Baseline (% Neutrophils)Final Visit (% Neutrophils)Change from Baseline to Final Visit(% Neutrophils)
Cambia®54.53057.9323.402

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Safety Outcome (6.8 of 7)

• Changes in clinical laboratory results: Hematology - Lymphocytes (%). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Intervention% Lymphocytes (Mean)
Baseline (% Lymphocytes)Final Visit (% Lymphocytes)Change from Baseline to Final Visit(% Lymphocytes)
Cambia®36.26033.745-2.515

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Pharmacokinetics Outcome (2 of 6)

• tmax: time to maximum concentration (min) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionmin (Mean)
Cambia®18.00

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Safety Outcome (6.9 of 7)

• Changes in clinical laboratory results: Hematology - Monocytes (%). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Intervention% Monocytes (Mean)
Baseline (% Monocytes)Final Visit (% Monocytes)Change from Baseline to Final Visit (% Monocytes)
Cambia®6.0305.847-0.183

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Pharmacokinetics Outcome (4 of 6)

• t1/2: terminal elimination half-life (min) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionmin (Mean)
Cambia®66.79

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Pharmacokinetics Outcome (5 of 6)

• AUC 0-t: area under the concentration-time curve from time 0 to last time point (t) where diclofenac could be measured (min*ng/mL) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionmin*ng/mL (Mean)
Cambia®82920.03

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Safety Outcome (6.2 of 7)

• Changes in clinical laboratory results: Hematology - Hemoglobin (g/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventiong/L (Mean)
Baseline (g/L)Final Visit (g/L)Change from Baseline to Final Visit (g/L)
Cambia®128.000132.7204.720

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Safety Outcome (1 of 7)

• Treatment emergent AEs (TEAEs) (NCT02287376)
Timeframe: 3 months (time of first dose of study medication taken to 30 days after the last dose of study medication taken)

InterventionParticipants (Count of Participants)
Cambia®10

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Safety Outcome (2 of 7)

• Serious adverse events (SAEs) (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to 30 days post Day 90 or last dose of study medication taken)

InterventionParticipants (Count of Participants)
Cambia®1

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Safety Outcome (3 of 7)

• Withdrawals due to AEs (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to 30 days after the last dose of study medication taken)

InterventionParticipants (Count of Participants)
Cambia®0

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Safety Outcome (4 of 7)

• Deaths (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to 30 days post Day 90 or last dose of study medication taken)

InterventionParticipants (Count of Participants)
Cambia®0

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Safety Outcome (7 of 7)

• Physical examination findings including abnormal clinically significant findings (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionParticipants (Count of Participants)
Cambia®1

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Pharmacokinetics Outcome (1 of 6)

• Cmax: maximum concentration (ng/mL) (NCT02287376)
Timeframe: 6 hours (pre-dose, 5, 10, 15, 20, 30, 40, and 60 min, and 2, 4, and 6 hrs post-dose)

Interventionng/mL (Mean)
Cmax (ng/mL)pre-dose concentrations (ng/mL)5 min post-dose concentrations (ng/mL)10 min post-dose concentrations (ng/mL)15 min post-dose concentrations (ng/mL)20 min post-dose concentrations (ng/mL)30 min post-dose concentrations (ng/mL)40 min post-dose concentrations (ng/mL)60 min post-dose concentrations (ng/mL)2 hrs post-dose concentrations (ng/mL)4 hrs post-dose concentrations (ng/mL)6 hrs post-dose concentrations (ng/mL)
Cambia®1411.960.00649.781123.881247.721084.52855.92629.96535.44164.2540.2014.26

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Safety Outcome (5.1 of 7)

• Changes in vital sign measurements: Temperature (degrees C). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventiondegrees C (Mean)
Baseline (degrees C)Final Visit (degrees C)Change from Baseline to Final Visit (degrees C)
Cambia®36.5236.720.20

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Safety Outcome (5.2 of 7)

• Changes in vital sign measurements: Heart Rate (beats/min). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionbeats/min (Mean)
Baseline (beats/min)Final Visit (beats/min)Change from Baseline to Final Visit (beats/min)
Cambia®74.674.70.2

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Safety Outcome (5.3 of 7)

• Changes in vital sign measurements: Respiratory Rate (breaths/min). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionbreaths/min (Mean)
Baseline (breaths/min)Final Visit (breaths/min)Change from Baseline to Final Visit (breaths/min)
Cambia®15.415.60.1

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Safety Outcome (5.4 of 7)

• Changes in vital sign measurements: Systolic Blood Pressure (mmHg). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmm Hg (Mean)
Baseline (mm Hg)Final Visit (mm Hg)Change from Baseline to Final Visit (mm Hg)
Cambia®112.7109.6-3.1

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Safety Outcome (5.5 of 7)

• Changes in vital sign measurements: Diastolic Blood Pressure (mmHg). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventionmm Hg (Mean)
Baseline (mm Hg)Final Visit (mm Hg)Change from Baseline to Final Visit (mm Hg)
Cambia®68.867.1-1.7

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Safety Outcome (6.1 of 7)

• Changes in clinical laboratory results: Hematology - Hematocrit (L/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionL/L (Mean)
Baseline (L/L)Final Visit (L/L)Change from Baseline to Final Visit (L/L)
Cambia®0.3880.4080.020

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Safety Outcome (6.10 of 7)

• Changes in clinical laboratory results: Chemistry - Albumin (g/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

Interventiong/L (Mean)
Baseline (g/L)Final Visit (g/L)Change from Baseline to Final Visit (g/L)
Cambia®43.80047.2003.400

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Safety Outcome (6.11 of 7)

• Changes in clinical laboratory results: Chemistry - Alkaline Phosphatase (U/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Cambia®98.960103.7604.800

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Safety Outcome (6.12 of 7)

• Changes in clinical laboratory results: Chemistry - ALT (SGPT) (U/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Cambia®12.68013.0800.400

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Safety Outcome (6.13 of 7)

• Changes in clinical laboratory results: Chemistry - AST (SGOT) (U/L). (NCT02287376)
Timeframe: 3 months (signed informed consent/assent to the final visit)

InterventionU/L (Mean)
Baseline (U/L)Final Visit (U/L)Change from Baseline to Final Visit (U/L)
Cambia®17.24018.0400.800

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Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment

"To demonstrate the superiority (P<0.05) of the efficacy of the test and reference products over that of the vehicle control in the treatment of acute pain utilizing a 100 mm VAS (in the mITT population) - changes from baseline.~The Visual Analogue Scale (VAS) consists of a straight line with the endpoints defining extreme limits such as lower values of 'no pain at all' and higher values relating to 'pain as bad as it could be' ." (NCT02324270)
Timeframe: Baseline, 3 days

,,
Interventionscore on a scale (Mean)
Baseline72 hours after Initial treatmentChange from baseline
Diclofenac Epolamine Patch (Test Product)68.7525.83-42.91
Flector (Reference Product)68.9326.16-42.80
Placebo70.0927.16-42.88

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Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment

"To evaluate the therapeutic equivalence (90% CI) of generic diclofenac epolamine 1.3% patch (Watson Laboratories, Inc.) and Flector® (diclofenac epolamine 1.3% patch) (Pfizer) using a 100mm VAS scoring in the treatment of acute pain due to minor ankle sprain (in the per protocol population); changes from baseline.~The Visual Analogue Scale (VAS) consists of a straight line with the endpoints defining extreme limits such as lower values of 'no pain at all' and higher values relating to 'pain as bad as it could be' .~Percent improvement in VAS score is the percentage part of - change from baseline in VAS / Baseline VAS." (NCT02324270)
Timeframe: Baseline, 3 days

,
Interventionscore on a scale (Mean)
Baseline72 Hours after Initial treatmentChange from Baseline
Diclofenac Epolamine Patch (Test Product)68.5625.34-43.22
Flector (Reference Product)69.0325.78-43.25

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Plasma Concentration of Diclofenac

The estimated typical value for clearance (tvCl) following a single diclofenac dose based on population pharmacokinetic (PopPK) modeling using sparse plasma concentration data in pediatric subjects. (NCT02424578)
Timeframe: 0-6 hours after first dose of diclofenac

InterventionmL/hr (Mean)
Diclofenac Capsules Low Dose29647.9
Diclofenac Capsules High Dose35131.0

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Area Under the Curve (AUC) of Visual Analog Scale of Pain Intensity (VASPI) Measuring Change From Baseline at Different Time Points

"VASPI reduction from baseline is the difference between the Baseline VASPI score and the VASPI score at a specific observation point. Subjects were asked to identify their pain intensity using the 100 mm VASPI to indicate their current level of pain intensity on the 100 mm VASPI labeled no pain (0 mm) as the left anchor and worst possible pain (100 mm) as the right anchor. A positive change shows reduction in pain.~AUC of VASPI reduction from baseline for each time point was calculated using the trapezoidal rule." (NCT02476422)
Timeframe: 15, 30, 45, 60 and 90 minutes, and 2, 4, 5, 6, 7, and 8 hours post dose

,
Interventionunits on a scale*hours (Least Squares Mean)
15 minutes30 minutes45 minutes60 minutes90 minutes2 hours4 hours5 hours6 hours7 hours8 hours
Dilcofenac Potassium + Placebo to Ibuprofen16.191429.375938.857045.432154.933062.367496.7669119.0564145.6112177.2751212.9300
Ibuprofen + Placebo to Diclofenac Potassium15.626227.921637.344844.588255.988565.165498.9982117.4797138.6947163.8821193.4450

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Summed Total Pain Relief (TOTPAR) at Different Time Points

"After the administration of the single dose of the assigned study treatment, at the defined study time points, the clinical site staff captured pain relief information from each subject.~The subject was asked What is the amount of pain relief as compared to the starting pain? and the response was recorded as 0 = none, 1 = a little, 2 = some, 3 = a lot, or 4 = complete.~Total pain relief (TOTPAR) was the weighted sum of the pain relief scores from the 15-minute to the 8-hour observation points (TOTPAR8). Additionally, TOTPARs at 1, 2, 4 and 6 hours were calculated. The weights used for these values (evaluation time points) were 0.25 for the 15-, 30-, 45-, and 60-minute observations, 0.5 for the 90-minute, 2- and 4-hour observations, and 1 for the remaining observations." (NCT02476422)
Timeframe: 1, 2, 4, 6, and 8 hours postdose

,
Interventionunits on a scale (Least Squares Mean)
TOTPAR1TOTPAR2TOTPAR4TOTPAR6TOTPAR8
Dilcofenac Potassium + Placebo to Ibuprofen1.8075.03210.64215.64719.679
Ibuprofen + Placebo to Diclofenac Potassium1.7804.81710.84816.49921.341

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Sum of Pain Intensity Difference (SPID)

"At baseline and at each defined study time point, the clinical site staff captured pain intensity information from each subject using the 4-point categorical VRS. The subject was asked What is your pain level at this time? and the response was recorded as 0 = none, 1 = mild, 2 = moderate, and 3 = severe. Pain intensity difference (PID) was the difference between the baseline pain intensity score and the pain intensity score at a specific observation point. SPID is the weighted sum of PIDs from the 15-minute to the 8-hour observation point (SPID8). Additionally, SPID evaluations were also be done at 1 (SPID1), 2 (SPID2), 4 (SPID4) and 6 (SPID6) hours post dose. The weights used for these values were 0.25 for the 15-, 30-, 45-, and 60-minute observations, and 0.5 for the 90-minute, 2- and 4-hour observations, and 1 for the remaining observations." (NCT02476422)
Timeframe: 1, 2, 4, 6, and 8 hours postdose

,
Interventionunits on a scale (Least Squares Mean)
SPID1SPID2SPID4SPID6SPID8
Dilcofenac Potassium + Placebo to Ibuprofen1.0772.9556.1658.97011.099
Ibuprofen + Placebo to Diclofenac Potassium1.0492.7726.1969.32311.904

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Peak Analgesic Effect

"Peak analgesic relief is represented through highest pain intensity difference (PID), highest VASPI reduction, and highest pain relief scores. Pain intensity was measured on a verbal rating scale (VRS) ranging from 0 to 3 (none to severe, with higher score for higher pain intensity). PID represents difference in this score at baseline and specific time points, larger change indicating larger reduction in pain, with highest PID representing the largest difference. Pain relief was recorded on a scale ranging from 0 to 4 (none to complete, with higher score for higher pain relief), with highest pain relief representing maximum relief obtained. Pain intensity was also measured through a 100 mm visual analogue scale (VASPI), ranging from no pain (0 mm) to worst possible pain (100 mm). A positive change in VASPI indicates reduction in pain, with highest VASPI reduction representing highest change." (NCT02476422)
Timeframe: From dose administration to 8 hours post dose

,
Interventionunits on a scale (Mean)
Highest Mean PIDHighest pain reliefHighest VASPI reduction
Dilcofenac Potassium + Placebo to Ibuprofen1.93.661.3
Ibuprofen + Placebo to Diclofenac Potassium1.83.560.2

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Number of Patients With Different Responses Based on Patient's Global Assessment of Response to Treatment (PGART)

PGART was measured by asking patients to give a score on a scale from 0 to 4, where 0 = poor; 1 = fair; 2 = good; 3 = very good; 4 = excellent. This measurement was taken at the end of 8 hours, or before the use of rescue medication (for a patient who takes rescue medciation within the 8 hour period). (NCT02476422)
Timeframe: At 8 hour postdose prior to use of rescue medication

,
InterventionParticipants (Number)
Poor (0)Fair (1)Good (2)Very good (3)Excellent (4)
Dilcofenac Potassium + Placebo to Ibuprofen67495549
Ibuprofen + Placebo to Diclofenac Potassium107346447

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Number of Patients With Any Adverse Events, Serious Adverse Events and Death

Treatment emergent adverse events are reported in the below data table. (NCT02476422)
Timeframe: time of dosage administration up to the follow-up phone call on study Day 3 (maximum 3 days)

,
InterventionParticipants (Number)
any adverse eventsserious adverse eventsDeath
Dilcofenac Potassium + Placebo to Ibuprofen4700
Ibuprofen + Placebo to Diclofenac Potassium4700

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Change From Baseline in Visual Analog Scale of Pain Intensity (VASPI) at Different Time Points

"VASPI reduction from baseline is the difference between the Baseline VASPI score and the VASPI score at a specific observation point. Subjects were asked to identify their current level of pain intensity on the 100 mm VASPI, labeled no pain (0 mm) as the left anchor and worst possible pain (100 mm) as the right anchor. A positive change represents a reduction in pain." (NCT02476422)
Timeframe: 15, 30, 45, and 90 minutes, and 2, 4, 5, 6, 7, and 8 hours post dose

,
InterventionUnits on a scale (Least Squares Mean)
15 minutes30 minutes45 minutes90 minutes2 hours4 hours5 hours6 hours7 hours8 hours
Dilcofenac Potassium + Placebo to Ibuprofen9.224.138.953.555.648.845.440.335.232.3
Ibuprofen + Placebo to Diclofenac Potassium13.726.636.749.153.051.949.846.541.937.7

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Time to Onset of Meaningful Pain Relief (MPR)

Using the double stopwatch technique, participant started two stopwatches at dosing, and stopped the second stopwatch as soon as he/she began to experience 'meaningful' relief from pain. Time elapsed is recorded as the MPR. (NCT02476422)
Timeframe: Within 8 hours postdose

Interventionminutes (Median)
Dilcofenac Potassium + Placebo to Ibuprofen41.67500
Ibuprofen + Placebo to Diclofenac Potassium42.02500

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Time to Onset of First Perceptible Pain Relief (FPR)

Using the double stopwatch technique, participant started two stopwatches at dosing, and stopped the first stopwatch as soon as he/she first began to feel 'any' relief from pain. The time elapsed was recorded as the FPR. (NCT02476422)
Timeframe: Within 8 hours postdose

Interventionminutes (Median)
Dilcofenac Potassium + Placebo to Ibuprofen15.81665
Ibuprofen + Placebo to Diclofenac Potassium14.85000

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Time to Confirmed First Perceptible Pain Relief

Time to onset of first perceptible pain relief (FPR), provided the FPR was subsequently 'confirmed' through the achievement of meaningful pain relief (MPR). Participant started two stopwatches at dosing, and recorded FPR by stopping the first stopwatch when he/she first experienced 'any' pain relief. FPR is 'confirmed' only if the participant also stopped the second stopwatch indicating 'meaningful pain relief'. (NCT02476422)
Timeframe: Within 8 hours postdose

Interventionminutes (Median)
Dilcofenac Potassium + Placebo to Ibuprofen15.81665
Ibuprofen + Placebo to Diclofenac Potassium14.98335

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Number of Patients Needing Rescue Medication

The number of patients needing rescue medication within the 8 hour treatment period was evaluated. (NCT02476422)
Timeframe: From dose administration to 8 hours post dose

InterventionParticipants (Number)
Dilcofenac Potassium + Placebo to Ibuprofen47
Ibuprofen + Placebo to Diclofenac Potassium36

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Duration of Analgesia

Duration of analgesia (time to first use of rescue medication) was evaluated, from dose administration to the time of first use of rescue medication within the 8-hour treatment period. Censored observations were included in calculating this endpoint. Censored subjects include any subject who did not take rescue medication prior to the end of the assessment period of 480 minutes (8 hours). (NCT02476422)
Timeframe: From dose administration to 8 hours post dose

Interventionminutes (Median)
Dilcofenac Potassium + Placebo to Ibuprofen480.0
Ibuprofen + Placebo to Diclofenac Potassium480.0

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Change From Baseline in Visual Analog Scale of Pain Intensity (VASPI) at 60 Minutes Post Dose

"VASPI reduction from baseline is the difference between the Baseline VASPI score and the VASPI score at a specific observation point. Subjects were asked to identify their current level of pain intensity on the 100 mm VASPI, labeled no pain (0 mm) as the left anchor and worst possible pain (100 mm) as the right anchor. A positive change represents a reduction in pain." (NCT02476422)
Timeframe: 60 minutes postdose

Interventionunits on a scale (Least Squares Mean)
Dilcofenac Potassium + Placebo to Ibuprofen47.3
Ibuprofen + Placebo to Diclofenac Potassium44.1

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Tmax and T1/2

(NCT02495831)
Timeframe: 24 hours

,
Interventionhours (Least Squares Mean)
TmaxT1/2
Diclofenac Sodium0.881.24
Diclofenac Sodium and Safinamide1.01.19

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To Evaluate Plasma Diclofenamic Acid Extent of Exposure Reported as Plasma AUC After Single Administration of 50 mg Diclofenac Sodium, With and Without Co-administration of a Single 200 mg Dose of Safinamide.

Plasma diclofenamic acid AUC0-t after T2 single dose, with and without T1 co-administration. To measure AUC plasma samples were taken by the participants at different time points, and the concentrations of diclofenac and safinamide were measured. AUC0-t is the area under the concentration-time curve from administration to the last observed concentration time t; PK parameters AUC0-t were analysed using analysis of variance (ANOVA). Before analysis, the data were transformed using a neperian logarithmic transformation. ANOVA was performed taking into account treatment, period, sequence and subject (sequence) as fixed effects with a variance components structure of the covariance matrix. (NCT02495831)
Timeframe: 24 hours

Interventionh X ng per mL (Mean)
Diclofenac Sodium1323.28
Diclofenac Sodium and Safinamide1381.32

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Relative Bioavailability (Frel)

calculated as ratio between AUC0-t (test) / AUC0-t (reference) (NCT02495831)
Timeframe: 24 hours

Interventionratio (Mean)
Diclofenac Sodium107.67
Diclofenac Sodium and Safinamide109.61

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Lamda z

(NCT02495831)
Timeframe: 24 hours

Intervention1/hours (Mean)
Diclofenac Sodium0.63
Diclofenac Sodium and Safinamide0.63

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Evaluate Diclofenac Rate of Absorption Reported as Plasma Cmax After Single Administration of 50 mg Diclofenac With and Without 200 mg of Safinamide.

Cmax, of plasma diclofenamic acid after T2 single dose, with and without T1 co-administration. The parametric point estimators (PE) for the ratios of T2 treatment with T1 co-administration / T2 treatment without T1 co-administration for the PK parameters under consideration, and the two-sided 90% confidence interval (CI), were calculated using the adjusted least squares means (LSMEANS) from the ANOVA. LSmeans differences obtained in the log scale for Cmax were back-transformed to obtain the PE (i.e. geometric mean ratio) and the two-sided 90% CI as percentages. (NCT02495831)
Timeframe: 24 hours

Interventionng/mL (Least Squares Mean)
Diclofenac Sodium766.59
Diclofenac Sodium and Safinamide833.50

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Absolute Change in the Total WOMAC (Western Ontario and McMaster Universities Arthritis Index) Pain Subscale Score for the Target Knee

The total WOMAC Pain Subscale score was determined by summing the individual scores from each of the five questions using a 5-point Likert scale (i.e., 'none'=0; 'mild'=1, 'moderate'=2; 'severe'=3; 'extreme'=4) comprising the WOMAC Pain Subscale Rating for the Target Knee. (NCT02596451)
Timeframe: Baseline and week 4

Interventionunits on a scale (Mean)
Test5.8
Reference5.9

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Physical Exams to Ensure Safety and Well Being of the Subjects

Physical examinations - including assessments of the application site. examination. (NCT02666846)
Timeframe: Estimated study duration for each subject will be approximately 6 weeks

InterventionAbnormalities (Number)
Cohort 1: TIB200 Gel 10%0
Cohort 1: Nurofen Gel 10%0
Cohort 1: Nurofen Tablets0
Cohort 1: TIB200 Placebo Gel0
Cohort 2: DCF100 Gel 2%0
Cohort 2: DCF100 Gel 4%0
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet0
Cohort 2: DCF100 Placebo Gel0
Cohort 3: SPR300 Gel (15%:7%)0
Cohort 3: SPR300 Placebo Gel0

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To Determine Vital Signs and Electrocardiograms (ECGs) That Were Abnormal to Ensure Safety and Well Being of the Subjects

To determine Vital Signs and Electrocardiograms (ECGs) that were abnormal to ensure safety and well being of the subjects (NCT02666846)
Timeframe: Estimated study duration for each subject will be approximately 6 weeks

InterventionAbnormal readings (Number)
Cohort 1: TIB200 Gel 10%0
Cohort 1: Nurofen Gel 10%0
Cohort 1: Nurofen Tablets0
Cohort 1: TIB200 Placebo Gel0
Cohort 2: DCF100 Gel 2%0
Cohort 2: DCF100 Gel 4%0
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet0
Cohort 2: DCF100 Placebo Gel0
Cohort 3: SPR300 Gel (15%:7%)0
Cohort 3: SPR300 Placebo Gel0

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Peak Plasma Concentration (Cmax)

Maximum observed plasma concentration (Cmax), time corresponding to occurrence of Cmax (tmax) (up to 6 subjects per cohort only) laser Doppler imaging [flux units], up to 6 subjects per cohort) (NCT02666846)
Timeframe: 15 minutes before and 1, 2, 4 and 6 hours post administration

Interventionng/ml (Mean)
Cohort 1: TIB200 Gel 10%11.5
Cohort 1: Nurofen Gel 10%5.15
Cohort 1: Nurofen Tablets29900
Cohort 2: DCF100 Gel 2%0
Cohort 2: DCF100 Gel 4%0
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet772
Cohort 3: SPR300 Gel (15%:7%)0
Cohort 3: SPR300 Placebo Gel0

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Number of Recorded Abnormal Clinical Assessments

"Laboratory assessments - standard clinical trial assessments for clinical chemistry and haematology~Listing of individual laboratory measurements by subjects and evaluation of each laboratory parameter" (NCT02666846)
Timeframe: Estimated study duration for each subject will be approximately 6 weeks

InterventionAssessments (Number)
Cohort 1: TIB200 Gel 10%0
Cohort 1: Nurofen Gel 10%0
Cohort 1: Nurofen Tablets0
Cohort 1: TIB200 Placebo Gel0
Cohort 2: DCF100 Gel 2%0
Cohort 2: DCF100 Gel 4%0
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet0
Cohort 2: DCF100 Placebo Gel0
Cohort 3: SPR300 Gel (15%:7%)0
Cohort 3: SPR300 Placebo Gel0

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Intensity of the UVB-induced Erythema (Determined by Assessment of Skin Blood Flow by Laser Doppler Imaging [Flux Units])

Intensity of the Ultra Violet B radiation (UVB)-induced erythema (determined by assessment of skin blood flow by laser Doppler imaging [flux units], up to 8 subjects per cohort) - Change from baseline (NCT02666846)
Timeframe: 15 minutes before to 6 hours post administration

InterventionLaser doppler imaging (Flux Units) (Least Squares Mean)
Cohort 1: TIB200 Gel 10%-313.3879
Cohort 1: Nurofen Gel 10%-171.5589
Cohort 1: Nurofen Tablets-262.0693
Cohort 1: TIB200 Placebo Gel-95.3974
Cohort 2: DCF100 Gel 2%-228.3016
Cohort 2: DCF100 Gel 4%-278.1918
Cohort 2: Voltaren Gel 2%-198.1408
Cohort 2: Voltarol Oral Tablet-198.1408
Cohort 2: DCF100 Placebo Gel-45.376
Cohort 3: SPR300 Gel (15%:7%)12.2265
Cohort 3: SPR300 Placebo Gel67.3931

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Heat Pain Tolerance Test (HPTT) Measured the Point at Which the Heat Became Painful - Degrees Centigrade -

To assess the pharmacodynamic effect by Heat Pain Tolerance Test (HPTT) which measured the point at which the heat became painful (degrees centigrade) of three topical analgesics, DCF100, TIB200, and SPR300 versus topical placebo and active topical reference products in a model of UV-induced inflammatory pain. (NCT02666846)
Timeframe: 15 minutes before to 6 hours post administration

InterventionDegrees Centigrade (Mean)
Cohort 1: TIB200 Gel 10%0.3635
Cohort 1: Nurofen Gel 10%0.7358
Cohort 1: Nurofen Tablets0.0887
Cohort 1: TIB200 Placebo Gel-0.1983
Cohort 2: DCF100 Gel 2%0.6679
Cohort 2: DCF100 Gel 4%0.8722
Cohort 2: Voltaren Gel 2%0.7978
Cohort 2: Voltarol Oral Tablet0.6835
Cohort 2: DCF100 Placebo Gel0.1688
Cohort 3: SPR300 Gel (15%:7%)0.3934
Cohort 3: SPR300 Placebo Gel-0.0123

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Area Under the Plasma Concentration Versus Time Curve

Area under the concentration vs. time curve from time zero to 6 hours (AUC0-6h) (up to 6 subjects per cohort only) laser Doppler imaging [flux units], up to 6 subjects per cohort) (NCT02666846)
Timeframe: 15 minutes before and 1, 2, 4 and 6 hours post administration

Interventionh*ng/ml (Mean)
Cohort 1: TIB200 Gel 10%47.7
Cohort 1: Nurofen Gel 10%19.9
Cohort 1: Nurofen Tablets90000
Cohort 2: DCF100 Gel 2%0
Cohort 2: DCF100 Gel 4%0
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet1030
Cohort 3: SPR300 Gel (15%:7%)0
Cohort 3: SPR300 Placebo Gel0

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Adverse Events (AEs)

Local and systemic Adverse Events (AEs). (NCT02666846)
Timeframe: Estimated study duration for each subject will be approximately 6 weeks

InterventionEvents (Number)
Cohort 1: TIB200 Gel 10%5
Cohort 1: Nurofen Gel 10%5
Cohort 1: Nurofen Tablets1
Cohort 1: TIB200 Placebo Gel1
Cohort 2: DCF100 Gel 2%1
Cohort 2: DCF100 Gel 4%1
Cohort 2: Voltaren Gel 2%0
Cohort 2: Voltarol Oral Tablet2
Cohort 2: DCF100 Placebo Gel0
Cohort 3: SPR300 Gel (15%:7%)3
Cohort 3: SPR300 Placebo Gel1

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Number of Patients With Decrease in POMwp of at Least 30% From Baseline

This outcome measures the pattern of number of patients with a decrease in POMwp of at least 30% from baseline at 1 hour after dosing on Day 2 evening. (NCT02700815)
Timeframe: Baseline and day 2

InterventionParticipants (Number)
Placebo Gel34
Capsaicin (0.075%) Gel150
Diclofenac (2%) Gel107
Diclofenac (2%) +Capsaicin (0.075%) Gel134

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Change in POM Between Baseline and Day 2 Evening, 1 Hour After Drug Application

Pain on movement (POM) was used to assess pain measurement for back and neck pain. The standardized movements have been established for which the measurement was taken. POMwp was the POM measure that gave the highest score at baseline; i.e. POM of worst procedure. Pain intensity was assessed at rest after standing in an upright position relatively motionless for 1 minute. The pain was evaluated by asking patient 'How would you rate your pain right now?' and by using a visual analogue scale (VAS) ranging from 0-10 centimeters (cm) wherein 0 cm = no pain to 10 cm = worst pain possible. The results presented here are adjusted mean change from baseline and standard error for POMwp in cm. (NCT02700815)
Timeframe: Baseline and Day 2

InterventionUnits on a scale (Least Squares Mean)
Placebo Gel-2.45
Capsaicin (0.075%) Gel-3.26
Diclofenac (2%) Gel-2.33
Diclofenac (2%) +Capsaicin (0.075%) Gel-3.05

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Change From Baseline in Pressure Algometry (PA) at Day 6 Morning

PA is a method described to determine pressure pain threshold (PPT) by applying controlled pressure to a given body point. The results presented here are adjusted mean change from baseline and standard error for PA. (NCT02700815)
Timeframe: Baseline and Day 6

InterventionNewton/centimeter square (N/cm^2) (Least Squares Mean)
Placebo Gel8.01
Capsaicin (0.075%) Gel9.38
Diclofenac (2%) Gel7.64
Diclofenac (2%) +Capsaicin (0.075%) Gel9.66

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Change From Baseline in Pressure Algometry (PA) at Day 2 Evening, Before Drug Application

PA is a method described to determine pressure pain threshold (PPT) by applying controlled pressure to a given body point. The results presented here are adjusted mean change from baseline and standard error for PA. (NCT02700815)
Timeframe: Baseline and Day 2

InterventionNewton/centimeter square (N/cm^2) (Least Squares Mean)
Placebo Gel3.89
Capsaicin (0.075%) Gel3.46
Diclofenac (2%) Gel3.00
Diclofenac (2%) +Capsaicin (0.075%) Gel3.77

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Number of Patients With Decrease in POMwp of at Least 50% From Baseline

This outcome measures the pattern of number of patients with a decrease in POMwp of at least 50% from baseline at 1 hour after dosing on Day 2 evening. (NCT02700815)
Timeframe: Baseline and day 2

InterventionParticipants (Number)
Placebo Gel20
Capsaicin (0.075%) Gel95
Diclofenac (2%) Gel50
Diclofenac (2%) +Capsaicin (0.075%) Gel85

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Change From Baseline in POMwp (cm) at Day 6 Morning

Pain on movement (POM) was used to assess pain measurement for back and neck pain. The standardized movements have been established for which the measurement was taken. POMwp was the POM measure that gave the highest score at baseline; i.e. POM of worst procedure. Pain intensity was assessed at rest after standing in an upright position relatively motionless for 1 minute. The pain was evaluated by asking patient 'How would you rate your pain right now?' and by using a visual analogue scale (VAS) ranging from 0-10 cm wherein 0 cm = no pain to 10 cm = worst pain possible. The results presented here are adjusted mean change from baseline and standard error for POMwp in centimeters (cm). (NCT02700815)
Timeframe: Baseline and Day 6

InterventionUnits on a scale (Least Squares Mean)
Placebo Gel-3.83
Capsaicin (0.075%) Gel-5.08
Diclofenac (2%) Gel-3.77
Diclofenac (2%) +Capsaicin (0.075%) Gel-4.88

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POMwp Area Under the Curve (AUC) Calculated From 0 to 72 Hours (h) (POMwp AUC(0-72 h))

This is a key secondary endpoint. AUC for POMwp calculated from 0 to 72 h that is for first three treatment days using the trapezoidal rule divided by the observation time. The results presented here are adjusted mean and standard error for POMwp AUC (0-72 h) in centimeters (cm). The AUC represents POMwp as an average over the first 3 treatment days (Day 1 until Day 4 morning) - it is not meant here as a pharmacokinetics (PK) parameter (concentration over time). (NCT02700815)
Timeframe: 0 to 72 hours after start of treatment

Interventioncm (Least Squares Mean)
Placebo Gel4.62
Capsaicin (0.075%) Gel3.95
Diclofenac (2%) Gel4.81
Diclofenac (2%) +Capsaicin (0.075%) Gel4.25

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POMwp Area Under the Curve (AUC) Calculated From 0 to 120 Hours (h) (POMwp AUC(0-120 h))

This is a key secondary endpoint. AUC for POMwp calculated from 0 to 120 h that is for first five treatment days using the trapezoidal rule divided by the observation time. The results presented here are adjusted mean and standard error for POMwp AUC (0-120 h) in centimeters (cm). The AUC represents POMwp as an average over the first 5 treatment days (Day 1 until Day 6 morning) - it is not meant here as a PK parameter (concentration over time). (NCT02700815)
Timeframe: 0 to 120 hours after start of treatment

Interventioncm (Least Squares Mean)
Placebo Gel3.92
Capsaicin (0.075%) Gel3.10
Diclofenac (2%) Gel4.10
Diclofenac (2%) +Capsaicin (0.075%) Gel3.41

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Mean Change From Baseline to Week 8 in WOMAC Pain Scale, Bioequivalence of Test to Reference.

WOMAC = Western Ontario and McMaster Universities Arthritis Index. The higher number is more pain. Change from baseline to Week 8 as indicated in the title. Scale is 5 questions with a scale of 0-4, higher number is more pain. Therefore, if you have 5 questions and the max score for each is 4, the maximum number on the scale is 20 (5 questions x 4 units on the scale = 20). (NCT02913521)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Diclofenac Sodium Gel 1%6.8
Voltaren Gel6.7
Placebo5.9

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An Evaluation to Determine Superiority of Test and Reference Against Placebo in the Mean Change From Baseline to Week 8 in the Total WOMAC Pain Score.

WOMAC = Western Ontario and McMaster Universities Arthritis Index. The higher number is more pain. Change from baseline to Week 8 as indicated in the title. Scale is 5 questions with a scale of 0-4, higher number is more pain. Therefore, if you have 5 questions and the max score for each is 4, the maximum number on the scale is 20 (5 questions x 4 units on the scale = 20). (NCT02913521)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Diclofenac Sodium Gel 1%6.8
Voltaren Gel6.6
Placebo5.9

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Number of Subjects With Complete Clearance of AK Lesions

Complete Clearance was defined as 100% clearance of all Actinic Keratosis (AK) lesions (having a count of zero AKs) in the treatment area (face or bald scalp) at the Day 90 visit (30 Days Post Treatment). (NCT02952898)
Timeframe: Day 90 (30 days after completion of 60 days of treatment)

Interventionpercentage of participants (Number)
GDC 695 Gel30.2
Diclofenac Sodium Gel25.7
Placebo9.5

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Area Under the Plasma Concentration-time Curve (AUC) Over One Dosing Interval for Diclofenac at Steady State (AUC0-τ,ss) (τ = 12 Hours) (Day 7)

AUC0-τ,ss, Area under the plasma concentration-time curve (AUC) over one dosing interval at steady state for diclofenac at day 7 (τ = 12 hours). Stratification by race was analysed using a supportive Analysis of Variance (ANOVA) yielding point estimates for each underlying pairwise comparison analog to the main analysis. As the resulting two Least Square Means and Geometric Means (gMeans) per treatment and race are very similar, only gMeans per treatment and race are presented. (NCT03074162)
Timeframe: Pharmacokinetic samples were collected on Day 7 at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after the drug administration

,,
InterventionHour*nanogram/millilitre (h*ng/mL) (Geometric Mean)
OverallBy race: BlackBy race: Caucasian
Diclofenac 2% (A)46.85560.93035.182
Diclofenac 2% + Capsaicin 0.075% (B)40.17553.62829.704
Voltarol® 2.32% Gel (R)83.644105.67067.513

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Average Plasma Concentration (Cav,ss) for Diclofenac at Steady State

Average plasma concentration (Cav,ss) calculated as AUC0-t,ss divided by τ=12 hours (τ is the duration of the dosing interval). Descriptive statistics by race are reported in addition. (NCT03074162)
Timeframe: Pharmacokinetic samples were collected on Day 7 at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after the drug administration

,,
Interventionnanogram/ millilitre (ng/mL) (Geometric Mean)
OverallBy Race: BlackBy Race: Caucasian
Diclofenac 2% (A)3.90465.07752.9317
Diclofenac 2% + Capsaicin 0.075% (B)3.34804.46912.4754
Voltarol® 2.32% Gel (R)6.97028.80555.6259

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Maximum Plasma Concentration During a Dosage Interval (Cmax,ss) Obtained Directly From the Concentration-time Data for Diclofenac at Steady State (Day 7)

Cmax,ss, Maximum plasma of diclofenac concentration during a dosage interval obtained directly from the concentration-time data at steady state for diclofenac on day 7. Stratification by race was analysed using a supportive Analysis of Variance (ANOVA) yielding point estimates for each underlying pairwise comparison analog to the main analysis. As the resulting two Least Square Means and gMeans per treatment and race are very similar, only gMeans per treatment and race are presented. (NCT03074162)
Timeframe: Pharmacokinetic samples were collected on Day 7 at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after the drug administration

,,
InterventionNanogram/millilitre (ng/mL) (Geometric Mean)
OverallBy Race: BlackBy Race: Caucasian
Diclofenac 2% (A)6.78259.39234.7551
Diclofenac 2% + Capsaicin 0.075% (B)5.69647.38634.3416
Voltarol® 2.32% Gel (R)10.833014.80408.1371

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Percentage Peak-trough Fluctuation (%PTF), Calculated as [100*(Cmax,ss - Cpre,ss)/Cav,ss]

Percentage peak-trough fluctuation (%PTF) which was calculated as [100*(Cmax,ss - Cpre,ss)/Cav,ss] for Diclofenac. Descriptive statistics by race are reported in addition. (NCT03074162)
Timeframe: Pharmacokinetic samples were collected on Day 7 at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after the drug administration

,,
InterventionPercentage of Cav,ss (%) (Geometric Mean)
OverallBy Race: BlackBy Race: Caucasian
Diclofenac 2% (A)33.9553348.5571226.75129
Diclofenac 2% + Capsaicin 0.075% (B)26.6962015.0712839.96865
Voltarol® 2.32% Gel (R)24.7555825.8525724.25970

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Time to Maximum Observed Plasma Concentration at Steady State for Diclofenac at Steady State (Tmax,ss) (Day 7)

tmax,ss, Time to maximum observed plasma concentration at steady state for diclofenac at day 7 (tmax,ss). Descriptive statistics by race are reported in addition. (NCT03074162)
Timeframe: Pharmacokinetic samples were collected on Day 7 at pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after the drug administration

,,
InterventionHour (h) (Median)
OverallBy Race: BlackBy Race: Caucasian
Diclofenac 2% (A)0.750.002.00
Diclofenac 2% + Capsaicin 0.075% (B)1.000.503.50
Voltarol® 2.32% Gel (R)0.000.004.00

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Serum Diclofenac Concentrations

Study Session 1: within 60 min prior to dosing, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 24, 27, 30, 32, 51 h Study Session 2: within 60 min prior to dosing, 1, 2, 3, 4, 5, 6, 7, 23, 26, 29, 31, 47 h Study Session 3: no blood samples obtained (NCT03145259)
Timeframe: blood samples obtained over 51 hour time period for study session 1 and over 47 hour time period for study session 2; through study completion

Interventionng/mL (Mean)
Diclofenac Epolamine Patches5.6
Diclofenac Sodium Solution40.0

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Mean Change in the Total WOMAC Pain Subscale Score

"Mean change in the total WOMAC (Western Ontario and McMaster Universities Osteoarthritis Index) pain subscale score for the target knee was compared to determine the clinical equivalence of Test Drug (Diclofenac sodium gel of 1% of Mylan Inc.) with the Reference Listed Drug (RLD) (Voltaren® Gel 1% of Novartis Consumer Health, Inc.) Measure Description: Western Ontario and McMaster Universities Osteoarthritis Index WOMAC pain subscale score (pain score = min 0 to max 20), was determined by the sum of subject's responses to five questions (S1-S5) using a 5-point Likert scale (i.e., 'none'=0; 'mild'=1, 'moderate'=2; 'severe'=3; 'extreme'=4). Higher values represent worse outcome.~'How much pain do you have' when 'Walking on a flat surface' (S1), 'Going up or down stairs' (S2), 'at night while in bed' (S3), 'Sitting or lying' (S4), 'Standing upright' (S5)].~The timepoints considered for the primary outcomes include baseline and week 4." (NCT03172780)
Timeframe: From baseline to week 4

Interventionscore on a scale (Mean)
Diclofenac Sodium Gel-4.3
Voltaren® Gel-4.6

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Change From Baseline in WOMAC Pain Subscale Score

"Mean change in the total WOMAC (Western Ontario and McMaster Universities Osteoarthritis Index) pain subscale score for the target knee was compared to determine the superiority of the Test Drug and Reference Listed Drug (RLD) over placebo.~Measure Description: Western Ontario and McMaster Universities Osteoarthritis Index WOMAC pain subscale score (pain score = min 0 to max 20), was determined by the sum of subject's responses to five questions (S1-S5) using a 5-point Likert scale (i.e., 'none'=0; 'mild'=1, 'moderate'=2; 'severe'=3; 'extreme'=4). Higher values represent worse outcome.~'How much pain do you have' when 'Walking on a flat surface' (S1), 'Going up or down stairs' (S2), 'at night while in bed' (S3), 'Sitting or lying' (S4), 'Standing upright' (S5)].~The timepoints considered for the primary outcomes include baseline and week 4." (NCT03172780)
Timeframe: 4 weeks

Interventionscore on a scale (Mean)
Diclofenac Sodium Gel-4.2
Voltaren® Gel-4.4
Placebo Gel-3.2

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WOMAC Stiffness Score Change From Baseline

To evaluate efficacy of HP-5000 Active Topical Patch 1 and HP-5000 Active Topical Patch 2 compared with placebo for the treatment of Osteoarthritis of the knee as evaluated by change in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Stiffness Score from baseline to week 4. The WOMAC Stiffness scale assesses 2 items including morning stiffness and stiffness occurring later in the day. Each item is rated on a scale of 0 to 4, with 0 being no difficulty and 4 being extremely difficulty. The total score is the sum of two items range from 0 to 8 with a low score considered as a better outcome. (NCT03277066)
Timeframe: Baseline and 4 weeks

Interventionscore on a scale (Mean)
Diclofenac Sodium Active Topical Patch 1-2.4
Diclofenac Sodium Active Topical Patch 2-2.1
Placebo Patch-1.7

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WOMAC Physical Function Score

To evaluate efficacy of HP-5000 Active Topical Patch 1 and HP-5000 Active Topical Patch 2 compared with placebo for the treatment of Osteoarthritis of the knee as evaluated by change in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) physical function score from baseline to week 4. The WOMAC Physical Function assesses the following 17 items using the 0 to 4 scale. These 17 items include: 1. descending stairs; 2. ascending stairs; 3. rising from sitting; 4. standing; 5. bending to floor; 6. walking on a flat surface; 7. getting in/getting out of car; 8. going shopping; 9. putting on socks; 10. lying in bed; 11. taking off socks; 12. rising from bed; 13. getting in/out of bath; 14. sitting; 15. getting on/off toilet; 16. heavy domestic duties; 17. light domestic duties. Each item is rated on a scale of 0 to 4, with 0 being no difficulty and 4 being extremely difficulty. Total score range from 0 to 68 with lower score considered a better outcome. (NCT03277066)
Timeframe: Baseline and 4 weeks

Interventionscore on a scale (Mean)
Diclofenac Sodium Active Topical Patch 1-19.8
Diclofenac Sodium Active Topical Patch 2-19.3
Placebo Patch-15.6

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WOMAC Pain Score Week 2 Change From Baseline

To evaluate efficacy of HP-5000 Active Topical Patch 1 and HP-5000 Active Topical Patch 2 compared with placebo for the treatment of Osteoarthritis of the knee as evaluated by change in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain score from baseline to week 2. WOMAC pain score is a scale that evaluate five items including walking, stair climbing, nocturnal, rest and weight bearing. Each item is rated on a scale of 0 to 4, with 0 being no difficulty and 4 being extremely difficulty. The total score is the sum of five items. The total score range from 0 to 20 with a low score considered a better outcome and a high score considered a worse outcome. The total score range from 0 to 20 with a low score considered a better outcome and a high score considered a worse outcome. (NCT03277066)
Timeframe: Baseline and 2 weeks

Interventionscore on a scale (Mean)
Diclofenac Sodium Active Topical Patch 1-5.8
Diclofenac Sodium Active Topical Patch 2-5.3
Placebo Patch-5.0

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Evaluate Efficacy & Safety of HP-5000 Topical Patches in Subjects With Osteoarthritis of the Knee: Change in Osteoarthritis Pain Score

To evaluate efficacy of HP-5000 Active Topical Patch 1 and HP-5000 Active Topical Patch 2 compared with placebo for the treatment of Osteoarthritis of the knee as evaluated by change in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain score from baseline to week 4. WOMAC pain score is a scale that evaluate five items including walking, stair climbing, nocturnal, rest and weight bearing. Each item is rated on a scale of 0 to 4, with 0 being no difficulty and 4 being extremely difficulty. The total score is the sum of five items. The total score range from 0 to 20 with a low score considered a better outcome and a high score considered a worse outcome. (NCT03277066)
Timeframe: Baseline and 4 weeks

Interventionscore on a scale (Mean)
Diclofenac Sodium Active Topical Patch 1-6.3
Diclofenac Sodium Active Topical Patch 2-5.6
Placebo Patch-5.2

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Change From Baseline in WOMAC Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

WOMAC pain subscale is a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index joint (knee or hip) in the past 48 hours. It is calculated as the mean of the scores from the 5 individual questions scored on a NRS of 0 (no pain) to 10 (higher pain), where higher scores indicated higher pain. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.84-2.78
NSAIDs-2.60-2.48

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Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

Physical function referred to participant's ability to move around and perform usual activities of daily living. The WOMAC physical function subscale was a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index joint (knee or hip) during past 48 hours. It was calculated as mean of the scores from 17 individual questions scored on a NRS of 0 (minimum difficulty) to 10 (maximum difficulty), where higher scores indicated maximum difficulty. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.65-2.62
NSAIDs-2.33-2.26

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Change From Baseline in WOMAC Physical Function Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

Physical function referred to participant's ability to move around and perform usual activities of daily living. The WOMAC physical function subscale was a 17-item questionnaire used to assess the degree of difficulty experienced due to osteoarthritis in index joint (knee or hip) during past 48 hours. It was calculated as mean of the scores from 17 individual questions scored on a NRS of 0 (minimum difficulty) to 10 (maximum difficulty), where higher scores indicated maximum difficulty. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.65-2.62
Placebo-2.02-1.80

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Number of Participants With At-least One Positive Anti-Drug Antibody (ADA) Development

Immunogenicity was characterized by ADA responses & titers. Responses categories: Pre-existing immunoreactivity - ADA positive response at baseline with all post first dose negative results or positive response at baseline with all post first dose ADA responses < 9-fold over baseline titer levels; Treatment-boosted response - positive response in the assay post first dose, >= 9-fold over baseline titer levels, when baseline results are positive; Treatment-emergent response - ADA positive response post first dose when baseline results = negative or missing. (NCT03304379)
Timeframe: Baseline up to Week 44

,,
InterventionParticipants (Count of Participants)
Pre-Existing ImmunoreactivityTreated-Boosted ResponseTreatment-Emergent Response
Fasinumab 1 mg1504
NSAIDs901
Placebo1003

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Serum Concentrations of Functional Fasinumab

(NCT03304379)
Timeframe: At Weeks 0, 4, 8, 16, 24 and 44

InterventionMilligrams per Liter (mg/L) (Mean)
Week 0Week 4Week 8Week 16Week 24Week 44
Fasinumab 1 mg0.0001550.04690.06440.07380.07130.000349

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Change From Baseline in PGA Score up to Week 24 in Participants Treated With Fasinumab Compared to Participants Treated With NSAIDs

The PGA was a patient-rated assessment of current disease state on a 5-point Likert scale where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (Severe symptoms and inability to carry out most normal activities) and, 5 =very poor (Very severe symptoms which were intolerable and inability to carry out all normal activities). Higher score indicated severe condition. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
NSAIDs-0.75
Fasinumab 1 mg-0.81

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Change From Baseline in Patient Global Assessment (PGA) Score up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

The PGA was a patient-rated assessment of current disease state on a 5-point Likert scale where 1 = very good (asymptomatic and no limitation of normal activities), 2 = good (mild symptoms and no limitation of normal activities), 3 = fair (moderate symptoms and limitation of some normal activities), 4 = poor (Severe symptoms and inability to carry out most normal activities) and, 5 =very poor (Very severe symptoms which were intolerable and inability to carry out all normal activities). Higher score indicated severe condition. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
Placebo-0.66
Fasinumab 1 mg-0.81

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Change From Baseline in Weekly Average Walking Index Joint Pain Score up to Week 24 by Using the Numeric Rating Scale (NRS) Pain Scale

Participants reported weekly average walking index joint pain based on NRS. The NRS was nationally recognized numeric scale from 0 to 10, where 0 would demonstrate no pain, 1 to 3 would demonstrate mild pain, 4 to 6 would be moderate pain, 7 to 9 would be severe pain and 10 would be the worst pain possible. Higher score indicated greater pain. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionScore on a Scale (Least Squares Mean)
Pooled Placebo-1.85
NSAIDs-2.13
Fasinumab 1 mg-2.51

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Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 24

Number of participants who underwent a JR surgery from baseline up to Week 24 were reported. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionParticipants (Count of Participants)
Placebo2
NSAIDs7
Fasinumab 1 mg3

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Number of Participants Who Underwent a Joint Replacements (JR) Surgery From Baseline up to Week 44

Number of participants who underwent a JR surgery from baseline up to follow-up period (Week 44) were reported. (NCT03304379)
Timeframe: Baseline up to Week 44

InterventionParticipants (Count of Participants)
Placebo6
NSAIDs13
Fasinumab 1 mg10

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Number of Participants With AA Events Meeting Destructive Arthropathy (DA) Criteria

DA is a unique clinical form of rapidly destructive arthropathy over and above that seen in the normal progression of OA. DA criteria can be associated with Rapidly Progressive OA type 2, Subchondral Insufficiency fracture, and Primary Osteonecrosis confirmed by an arthropathy adjudication committee. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo0
NSAIDs0
Fasinumab 1 mg2

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Number of Participants With Adjudicated Arthropathy (AA) Events

AA was a composite term that encompasses the following conditions: Rapidly progressive Osteoarthritis (OA) type 1 and 2, Subchondral insufficiency fractures, and Primary Osteonecrosis confirmed by an arthropathy adjudication committee. AAs were also evaluated to determine if they met Destructive Arthropathy criteria. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo5
NSAIDs9
Fasinumab 1 mg34

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Number of Participants With At-least One Peripheral Sensory Adverse Events (AEs)

Any participants with a peripheral sensory event that persisted for 2 months was referred for a neurology or other specialty consultation and reported as an Adverse Events of Special Interest (AESI). (NCT03304379)
Timeframe: Baseline up to Week 44

InterventionParticipants (Count of Participants)
Placebo8
NSAIDs24
Fasinumab 1 mg31

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Number of Participants With Joint Replacement (JR) Surgery Reported at End of Study (EOS) (Week 72)

An EOS phone contact was conducted at Week 72 following the last dose of study drug (Week 24) to evaluate the number of participants who had undergone or were scheduled for JR surgery. (NCT03304379)
Timeframe: At Week 72

InterventionParticipants (Count of Participants)
Placebo11
NSAIDs29
Fasinumab 1 mg21

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Number of Participants With Sympathetic Nervous System (SNS) Dysfunction Events

Potential events of SNS dysfunction were monitored throughout the study through physical examination, AE reporting, assessment of orthostatic hypotension, and the Survey of Autonomic Symptoms. Sympathetic nervous system dysfunction was diagnosed after consultation with an appropriate specialist, such as a neurologist and/or cardiologist. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo0
NSAIDs0
Fasinumab 1 mg0

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

An adverse event (AE) was defined as any untoward medical occurrence in a participant administered a study drug which may or may not have a causal relationship with the study drug. TEAE was defined as an AE with an onset that occurs after receiving study drug. A serious adverse event (SAE) was defined as any untoward medical occurrence that resulted in any of the following outcomes: death, life-threatening, required initial or prolonged in-patient hospitalization, persistent or significant disability/incapacity, congenital anomaly/birth defect, or considered as medically important event. Any TEAE included participants with both serious and non-serious TEAEs. (NCT03304379)
Timeframe: Baseline up to follow-up period (Week 44)

InterventionParticipants (Count of Participants)
Pooled Placebo186
NSAIDs406
Fasinumab 1 mg403

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Percentage of Participants With Greater Than or Equal to (≥) 30 Percent (%) Reduction From Baseline up to Week 24 in WOMAC Pain Subscale Score in Participants Treated With Fasinumab Compared to Placebo

WOMAC pain subscale was a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index knee during past 48 hours. It was calculated as mean of the scores from 5 individual questions scored on a NRS of 0 (minimum pain) to 10 (maximum pain), where higher scores indicate more pain. (NCT03304379)
Timeframe: Baseline up to Week 24

InterventionPercentage of Participants (Number)
Placebo48.7
Fasinumab 1 mg59.8

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Change From Baseline in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Pain Subscale Scores up to Week 24 in Participants Treated With Fasinumab Compared to Placebo

WOMAC pain subscale was a 5-item questionnaire used to assess the amount of pain experienced due to osteoarthritis in the index joint (knee or hip) in past 48 hours. It was calculated as the mean of the scores from the 5 individual questions scored on a numerical rating scale (NRS) of 0 (no pain) to 10 (higher pain), where higher scores indicated higher pain. (NCT03304379)
Timeframe: Baseline up to Week 24

,
InterventionScore on a Scale (Least Squares Mean)
FASmFAS
Fasinumab 1 mg-2.84-2.78
Placebo-2.21-2.01

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Time to the Onset of Action (the First Feeling of 20% Pain Reduction)

Time to the onset of action measured in minutes. (NCT03471507)
Timeframe: Up to 1 hour

Interventionminutes (Median)
Bonipar21
Diclofenac Topical Solution 1.5%30

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Number of Participants Who Experienced Adverse Effects and/or Complications

(NCT03471507)
Timeframe: Up to approximately 1 week

InterventionParticipants (Count of Participants)
Bonipar18
Diclofenac Topical Solution 1.5%21

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Change in Pain as Measured by Subjective Pain Intensity Rating (SPIR)

The SPIR is a patient-reported graduated scale where 0 = no pain and 10 = the maximum pain imaginable. (NCT03471507)
Timeframe: Baseline (approximately 24 hours before consent) to approximately 1 week post administration of study drug (or comparator)

Interventionscore on a scale (Mean)
Bonipar-2.3
Diclofenac Topical Solution 1.5%-2.6

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Change of Bath Ankylosing Spondylitis Function Index (BASFI)

Change of BASFI by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-0.8
NSAIDs x 6 Weeks-1.2

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Change of Pain Score

Change of pain score by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-2
NSAIDs x 6 Weeks-2

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Change of ASAS Endorsed Disease Activity Score (ASDAS)

Change of ASDAS by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-0.37
NSAIDs x 6 Weeks-0.84

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Change of Bath Ankylosing Spondylitis Disease Activity Index (BASDAI)

Change of BASDAI by numerical rating score from baseline [scale range: 0 (better) -10 (worse)] (NCT03473665)
Timeframe: Baseline, Week 4, and Week 6

Interventionunits on a scale (Median)
NSAIDs x 4 Weeks-1.7
NSAIDs x 6 Weeks-2.09

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Ratio Between Diclofenac Concentration in Treated Knee Synovial Tissue and Plasma After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)

Synovial tissue was collected during surgery (participant's scheduled arthroplasty of the target knee on which study treatment was applied). Samples were analyzed for diclofenac levels using a validated bio analytical method in compliance with the applicable standard operating procedures of the bioanalytical laboratory. Diclofenac concentration values that were below the LOQ were replaced by 0 for placebo group. The ratio between diclofenac concentration in treated knee synovial tissue and plasma was calculated. (NCT03497039)
Timeframe: At Day 8 (up to a maximum of Day 15 in case of surgery delay)

Intervention(ng/g)/(ng/mL) (Geometric Mean)
Diclofenac Diethylamine (DDEA) Gel0.320
Placebo GelNA

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Ratio Between Diclofenac Concentration in Treated Knee Synovial Fluid and Plasma After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)

Synovial fluid was collected during surgery (participant's scheduled arthroplasty of the target knee on which study treatment was applied). Samples were analyzed for diclofenac levels using a validated bio analytical method in compliance with the applicable standard operating procedures of the bioanalytical laboratory. Diclofenac concentration values that were below the limit of quantification (LOQ) were replaced by 0 for placebo group. The ratio between diclofenac concentration in treated knee synovial fluid and plasma was calculated. (NCT03497039)
Timeframe: At Day 8 (up to a maximum of Day 15 in case of surgery delay)

Intervention(ng/mL)/(ng/mL) (Geometric Mean)
Diclofenac Diethylamine (DDEA) Gel0.463
Placebo GelNA

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Diclofenac Concentration in Treated Knee Synovial Fluid After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)

Synovial fluid was collected during surgery (participant's scheduled arthroplasty of the target knee on which study treatment was applied). Samples were analyzed for diclofenac levels using a validated bio analytical method in compliance with the applicable standard operating procedures of the bioanalytical laboratory. Synovial fluid diclofenac concentration was summarized by treatment group. Number of participants with diclofenac concentration values that were below the LOQ were replaced by 0 for placebo group. The geometric mean was calculated with a two-sided 95% confidence interval assuming data on the logarithmic scale were normally distributed. (NCT03497039)
Timeframe: At Day 8 (up to a maximum of Day 15 in case of surgery delay)

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Diclofenac Diethylamine (DDEA) Gel2.274
Placebo GelNA

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Diclofenac Concentration in Treated Knee Synovial Tissue After 7 Days Topical Application of Study Treatment to the Knee (12 Hours After Last Administration of Study Treatment)

Synovial tissue was collected during surgery (participant's scheduled arthroplasty of the target knee on which study treatment was applied). Samples were analyzed for diclofenac levels using a validated bio analytical method in compliance with the applicable standard operating procedures of the bioanalytical laboratory. Synovial tissue diclofenac concentration was summarized by treatment group. Number of participants with diclofenac concentration values that were below the limit of quantification (LOQ) were replaced by 0 for placebo group. The geometric mean was calculated with a two-sided 95% confidence interval assuming data on the logarithmic scale were normally distributed. (NCT03497039)
Timeframe: At Day 8 (up to a maximum of Day 15 in case of surgery delay)

Interventionnanograms per gram (ng/g) (Geometric Mean)
Diclofenac Diethylamine (DDEA) Gel1.573
Placebo GelNA

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Number of Participants With Bleeding Complications

Bleeding complications are defined as complications necessitating a trip to the emergency room or requiring intervention for epistaxis. (NCT03605914)
Timeframe: 5 days after operation

InterventionParticipants (Count of Participants)
NSAID0
Opioid0

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Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)

The range of scores on the VAS is 0 to 100, with 100 being the highest level of pain. (NCT03605914)
Timeframe: 48 hours (day 2 after operation)

Interventionunits on a scale (Mean)
NSAID24.2
Opioid28.3

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Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)

The range of scores on the VAS is 0 to 100, with 100 being the highest level of pain. (NCT03605914)
Timeframe: 24 hours (day 1 after operation)

Interventionunits on a scale (Mean)
NSAID30.2
Opioid40.7

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Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)

The range of scores on the VAS is 0 to 100, with 100 being the highest level of pain. (NCT03605914)
Timeframe: 72 hours (day 3 after operation)

Interventionunits on a scale (Mean)
NSAID22.9
Opioid27.9

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Pain Score as Assessed by a 100mm Visual Analogue Scale (VAS)

The range of scores on the VAS is 0 to 100, with 100 being the highest level of pain. (NCT03605914)
Timeframe: 120 hours (day 5 after operation)

Interventionunits on a scale (Mean)
NSAID17.2
Opioid18.9

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Subject's Global Evaluation of the Treatment

Participants documented their overall impression of the analgesic efficacy of the IMPs on a 5-point Likert scale from Excellent (4) to Poor (0). (NCT03714672)
Timeframe: 8 hours after the first dose of IMP or before first intake of rescue medication (whatever the first) and 24 hours after the first dose of IMPs

InterventionParticipants (Count of Participants)
8-Hours724888628-Hours724888588-Hours724888598-Hours7248886024-Hours7248885924-Hours7248886024-Hours7248886224-Hours72488858
PoorFairExcellentGoodVery Good
Tramadol/Diclofenac 50/504
Tramadol/Diclofenac 25/257
Tramadol 5028
Diclofenac 5023
Tramadol/Diclofenac 50/5010
Tramadol/Diclofenac 25/2512
Tramadol 5030
Diclofenac 5025
Tramadol/Diclofenac 50/5017
Tramadol/Diclofenac 25/2533
Tramadol 5036
Diclofenac 5035
Tramadol/Diclofenac 50/5073
Tramadol/Diclofenac 25/2564
Tramadol 5052
Tramadol/Diclofenac 50/50103
Tramadol/Diclofenac 25/2583
Tramadol 5051
Diclofenac 5051
Tramadol/Diclofenac 50/503
Tramadol/Diclofenac 25/254
Tramadol 507
Diclofenac 507
Tramadol/Diclofenac 25/255
Tramadol 5023
Diclofenac 5013
Tramadol/Diclofenac 50/5012
Tramadol/Diclofenac 25/2518
Tramadol 5034
Diclofenac 5039
Tramadol/Diclofenac 50/5057
Tramadol/Diclofenac 25/2565
Tramadol 5059
Diclofenac 5067
Tramadol/Diclofenac 50/50132
Tramadol/Diclofenac 25/25109
Tramadol 5082
Diclofenac 5080

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Time to Achieve a 50 Percent Reduction in Baseline Pain (Pain at Least Half Gone)

Time (hours) when the participant achieved a 50 percent reduction of baseline (starting) pain. It was assessed at defined time points after the first IMP dose using a YES or NO question for pain half gone. (NCT03714672)
Timeframe: Up to 24 hours after first dose

Interventionhours (Mean)
Tramadol/Diclofenac 50/501.27
Tramadol/Diclofenac 25/251.73
Tramadol 503.01
Diclofenac 502.53

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Time to Onset of First Perceptible Pain Relief

Participants used one stopwatch to document the time between first IMP dose and when they begin to feel any pain-relieving effect from the IMP. (NCT03714672)
Timeframe: Up to 8 hours after first dose

Interventionhours (Mean)
Tramadol/Diclofenac 50/500.57
Tramadol/Diclofenac 25/250.67
Tramadol 501.07
Diclofenac 501.12

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Pain Relief Expressed as Total Pain Relief (TOTPAR) Over the 4 Hours Post-dose Period (TOTPAR4)

Pain relief was assessed by the participant at defined time points after the first IMP dose using a 5-point verbal rating scale (VRS) with categories 0 (none), 1 (a little), 2 (some), 3 (a lot), or 4 (complete). Total Pain Relief (TOTPAR4) is a time-weighted summary measure of the total area under the pain relief curve that integrates serial assessments of a participant's pain over the duration of 4 hours after IMP intake. Minimum and maximum values for TOTPAR4 were 0=worst score and 16=best score, a higher score indicates more pain relief. (NCT03714672)
Timeframe: Up to 4 hours after first dose

Interventionunits on a scale (Least Squares Mean)
Tramadol/Diclofenac 50/509.9
Tramadol/Diclofenac 25/258.6
Tramadol 505.4
Diclofenac 505.8

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Time to Intake of First Rescue Medication Dose

The time from first IMP dose to first dose of rescue medication (ibuprofen or ketorolac), if needed, within 24 hours post-dose was calculated. (NCT03714672)
Timeframe: First dose to 24 hours after first dose

Interventionhours (Mean)
Tramadol/Diclofenac 50/5021.84
Tramadol/Diclofenac 25/2520.99
Tramadol 5017.37
Diclofenac 5017.38

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Time to Onset of Meaningful Pain Relief

Participants used a second stopwatch to document the time between first IMP dose and when they felt their pain relief was meaningful to them. (NCT03714672)
Timeframe: Up to 8 hours after first dose

Interventionhours (Mean)
Tramadol/Diclofenac 50/501.47
Tramadol/Diclofenac 25/252.04
Tramadol 502.93
Diclofenac 502.75

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Total Pain Relief at 6 Hours Post-dose (TOTPAR6)

Pain relief was assessed by the participant at defined time points after the first IMP dose using a 5-point VRS with categories 0 (none), 1 (a little), 2 (some), 3 (a lot), or 4 (complete). Total Pain Relief (TOTPAR6) is a time-weighted summary measure of the total area under the pain relief curve that integrates serial assessments of a participant's pain over the duration of 6 hours after IMP intake. Minimum and maximum values for TOTPAR6 were 0=worst score and 24=best score, a higher score indicates more pain relief. (NCT03714672)
Timeframe: Up to 6 hours after first dose

Interventionunits on a scale (Least Squares Mean)
Tramadol/Diclofenac 50/5015.2
Tramadol/Diclofenac 25/2513.3
Tramadol 509.3
Diclofenac 509.8

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Total Pain Relief at 8 Hours Post-dose (TOTPAR8)

Pain relief was assessed by the participant at defined time points after the first IMP dose using a 5-point VRS with categories 0 (none), 1 (a little), 2 (some), 3 (a lot), or 4 (complete). Total Pain Relief (TOTPAR8) is a time-weighted summary measure of the total area under the pain relief curve that integrates serial assessments of a participant's pain over the duration of 8 hours after IMP intake. Minimum and maximum values for TOTPAR8 were 0=worst score and 32=best score, a higher score indicates more pain relief. (NCT03714672)
Timeframe: Up to 8 hours after first dose

Interventionunits on a scale (Least Squares Mean)
Tramadol/Diclofenac 50/5020.1
Tramadol/Diclofenac 25/2517.8
Tramadol 5013.1
Diclofenac 5013.7

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Incidence and Type of Adverse Events

The incidence of treatment emergent adverse events (TEAE) reported from first dose (Day 1) to last scheduled contact with the participant on Day 14 was descriptively summarized. Selected TEAEs were events with preferred terms of nausea, vomiting, abdominal pain, gastrointestinal bleeding, dizziness, or hypotension. (NCT03714672)
Timeframe: Day 1 to Day 14

,,,
Interventionparticipants (Number)
TEAESevere TEAETEAE related to IMP or rescue medicationSerious TEAETEAE with outcome of deathSelected TEAETEAE leading to dose reductionTEAE leading to dose interruptionTEAE leading to IMP withdrawalDose reduction, interruption, or withdrawal
Diclofenac 504821000130000
Tramadol 5010536400770112
Tramadol/Diclofenac 25/256212310260213
Tramadol/Diclofenac 50/509664900680123

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Summed Pain Intensity Difference (SPID) at 4, 6, 8, and 24 Hours Post-dose

"Pain intensity was assessed by the participant before and at defined time points after the first IMP dose using an 11-point NRS with anchors at 0 for no pain and 10 for pain as bad as you can imagine. Pain Intensity Difference (PIDt) was defined as the difference between baseline pain intensity and pain intensity at time point t, and SPID defined as summed PIDt x [time (hours) elapsed since previous observation]. The SPID scores are the sum of the differences at each time point multiplied by the duration in hours since the previous time point. Positive numbers indicate a reduction in pain [maximum=10 at each time point], and negative numbers indicate an increase in pain [minimum=-10 at each time point]. The overall minimum and maximum are -10 and 10 times the number of hours specified (SPID-4=[-40 to 40], SPID-6=[-60 to 60], SPID-8=[-80 to 80], and SPID-24=[-240 to 240])." (NCT03714672)
Timeframe: Baseline; up to 24 hours after first dose

,,,
Interventionunits on a scale (Least Squares Mean)
4 Hours6 Hours8 Hours24 Hours
Diclofenac 507.7214.3620.5472.08
Tramadol 506.4312.8919.1071.41
Tramadol/Diclofenac 25/2513.6721.8628.9091.99
Tramadol/Diclofenac 50/5016.2425.5433.70107.15

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Change From Baseline to Day 5 in Functional Impairment

The change will be assessed by Roland Morris Disability Questionnaire between the baseline ED visit and the five day follow-up. The Roland-Morris Questionnaire (RMQ) is a self-administered disability measure in which greater levels of disability are reflected by higher numbers on a 24-point scale (0-24). (NCT03861611)
Timeframe: Baseline to 5 days

Interventionscore on a scale (Mean)
Ketorolac + Educational Intervention11.9
Ibuprofen + Educational Intervention9.4
Diclofenac + Educational Intervention10.9

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Frequency of LBP 2 Days After ED Visit

Participants were called 2 days after ED visit and asked to report the frequency of LBP experienced over the previous 24 hours. Frequency was assessed using the five point Likert scale: Not at all, Rarely, Sometimes, Usually, Always (NCT03861611)
Timeframe: 2 days after Emergency department visit

,,
InterventionParticipants (Count of Participants)
NeverRarelySometimesFrequentlyAlways
Diclofenac + Educational Intervention101421711
Ibuprofen + Educational Intervention71021915
Ketorolac + Educational Intervention6182656

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How Often Participants Used Assigned Medication

(NCT03861611)
Timeframe: 24 hours to 5 days

,,
InterventionParticipants (Count of Participants)
NeverOnly OnceSometimesOnce a dayTwice or more a day
Diclofenac + Educational Intervention0371538
Ibuprofen + Educational Intervention1541833
Ketorolac + Educational Intervention23102618

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Worst LBP 2 Days After ED Visit

Participants were called 2 days after ED visit and asked to report their worst LBP experienced over the previous 24 hours, using a four point ordinal scale: severe, moderate, mild, or none. (NCT03861611)
Timeframe: 2 days after Emergency department visit

,,
InterventionParticipants (Count of Participants)
NoneMildModerateSevere
Diclofenac + Educational Intervention1325187
Ibuprofen + Educational Intervention10182311
Ketorolac + Educational Intervention829186

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Number of Participants by Degree of Cartilage Loss

Microscopic articular features including degree of cartilage were evaluated and scored (Superficial Fibrillation, Deep fissuring, Loss to Tide Mark, Loss to Exposed Bone). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
Superficial FibrillationDeep fissuringLoss to Tide MarkLoss to Exposed Bone
Fasinumab2029
Non-steroidal Anti-inflammatory Drug (NSAID)1013
Placebo0101

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Number of Participants by Degree of Bony Changes

Microscopic articular features including degree of bony changes were evaluated and scored (Normal, Sclerosis [Lamellar/Mixed], Subarticular Fracture/Collapse). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
NormalSclerosis (Lamellar/Mixed)Subarticular Fracture/Collapse
Fasinumab175
Non-steroidal Anti-inflammatory Drug (NSAID)122
Placebo110

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Number of Participants by Degree of Synovial Lymphocytic Inflammation

Inflammatory cells including lymphocytes, mast cells, neutrophils, and eosinophils were scored by presence and degree (None present, Slight/Mild, Moderate, Marked/Band). (NCT03949673)
Timeframe: Up to 24 weeks from the last dose of study drug in the parent study, an average of approximately 3 months

,,
InterventionParticipants (Count of Participants)
None presentSlight/MildModerateMarked/Band
Fasinumab3532
Non-steroidal Anti-inflammatory Drug (NSAID)2210
Placebo0020

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Total Pain Relief (TOTPAR) From 0 to 24 Hours Post First Dose (Day 1) and From 96 to 120 Hours Post First Dose (Day 5)

Pain relief was assessed in the diary on a categorical scale ranging from 0 to 4, where 0 = no relief, 1 = a little relief, 2 = some relief, 3 = a lot of relief, 4 = complete relief. A higher value indicates greater pain relief. Pain relief was assessed at Baseline (immediately prior to first dose) and every 2 hours (after starting study product) until the participant went to bed on the evening of Day 1. The same assessment and recording frequency were also followed starting with the first dose on Day 5. (NCT04052620)
Timeframe: 0 to 24 hours (Day 1) and 96 to 120 hours (Day 5) post first dose

,
InterventionScores on a scale (Least Squares Mean)
Sum of 0-12 hours post first dose (Day 1)Sum of 96-120 hours post first dose (Day 5)
DDEA 1.16% Gel8.5327.68
DDEA 2.32% Gel/Placebo8.4728.48

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Change From Baseline in Pain on Movement (POM) on Day 5 of Treatment as Assessed by a 100 Millimeter (mm) Visual Analogue Scale (VAS)

The investigator performed a movement of the ankle and the pain assessment was done by the participant using a 100 mm VAS by describing ankle pain on movement. The POM was registered by the participant by drawing a perpendicular line on the 100 mm VAS with anchors at 0 = no pain and 100 = extreme pain. Higher scores indicate a worse outcome. Change from Baseline in POM was calculated by subtracting the Baseline value from the Day 5 value. (NCT04052620)
Timeframe: Baseline and Day 5

Interventionmm (Least Squares Mean)
DDEA 2.32% Gel/Placebo-42.36
DDEA 1.16% Gel-43.47

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Sum of Pain Intensity Difference (SPID) From 0 to 24 Hours Post First Dose (Day 1) and From 96 to 120 Hours Post First Dose (Day 5)

Pain intensity was assessed in the diary on a categorical scale ranging from 0 to 3, where 0 = no pain, 1 = mild pain, 2 = moderate pain, 3 = severe pain. A higher value indicates more severe pain. Pain intensity was assessed at Baseline (immediately prior to first dose) and every 2 hours (after starting study product) until the participant went to bed on the evening of Day 1. The same assessment and recording frequency were also followed starting with the first dose on Day 5. (NCT04052620)
Timeframe: 0 to 24 hours (Day 1) and 96 to 120 hours (Day 5) post first dose

,
InterventionScores on a scale (Least Squares Mean)
Sum of 0 - 12 hours post first dose (Day 1)Sum of 96 - 120 hours post first dose (Day 5)
DDEA 1.16% Gel15.4310.29
DDEA 2.32% Gel/Placebo15.809.80

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Number of Participants With Severity of Adverse Events (AEs) Following Dosing With Study Medication

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study product including any washout or lead-in product or investigational assessment, whether or not considered related to the study product. The investigator or medically qualified designee assessed the intensity for each AE reported during the study and categorized it on the basis of severity as Mild (an event that is easily tolerated by the participant, causing minimal discomfort and not interfering with everyday activities), Moderate (an event that is sufficiently discomforting to interfere with normal everyday activities or Severe (an event that prevents normal everyday activities). (NCT04052620)
Timeframe: up to 28 days following last administration of the study product (or last procedure)

,
InterventionParticipants (Count of Participants)
MildModerateSevere
DDEA 1.16% Gel840
DDEA 2.32% Gel/Placebo920

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Changes From Baseline in Difference of Tenderness Between Affected Ankle and Contralateral Ankle Measured by Algometry on Days 3, 5 and 8

"'Tenderness' was the sensation of pain expressed by a participant when pressure was applied to the body. Tenderness was measured by calibrated algometers in an area of 1 cm^2 at the center of the injured area. The investigator applied the pressure gauge to the marked tender point of maximum sensitivity by placing the gauge at a 90 degree angle vertical to the skin. The participant was instructed to indicate the onset of pain with a verbal cue such as Yes or Stop. Difference in tenderness between affected ankle and contralateral ankle is presented. Change from Baseline in tenderness on Day 3, 5 and 8 was calculated by subtracting the Baseline value from the Day 3, Day 5 and Day 8 values respectively." (NCT04052620)
Timeframe: Baseline and Days 3, 5 and 8

,
InterventionN/cm^2 (Least Squares Mean)
Day 3Day 5Day 8
DDEA 1.16% Gel7.5912.5914.98
DDEA 2.32% Gel/Placebo7.8511.3416.64

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Change From Baseline of POM on VAS on Day 3 and Day 8 of Treatment Assessed by 100 mm VAS

The investigator performed a movement of the ankle and the pain assessment was done by the participant using a 100 mm VAS by describing ankle pain on movement. The POM was registered by the participant by drawing a perpendicular line on the 100 mm VAS with anchors at 0 = no pain and 100 = extreme pain. Higher scores indicate a worse outcome. Change from Baseline in POM on Day 3 and Day 8 was calculated by subtracting the Baseline value from the Day 3 and Day 8 values respectively. (NCT04052620)
Timeframe: Baseline and Days 3 and 8

,
Interventionmm (Least Squares Mean)
Day 3Day 8
DDEA 1.16% Gel-25.86-54.62
DDEA 2.32% Gel/Placebo-28.29-55.38

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Change From Baseline in Tenderness as Measured by Pressure Algometry on Days 3, 5 and 8

"'Tenderness' was the sensation of pain expressed by a participant when pressure was applied to the body. Tenderness was measured by calibrated algometers in an area of 1 cm^2 at the center of the injured area. The investigator applied the pressure gauge to the marked tender point of maximum sensitivity by placing the gauge at a 90 degree angle vertical to the skin. The participant was instructed to indicate the onset of pain with a verbal cue such as Yes or Stop. Change from Baseline in tenderness on Day 3, 5 and 8 was calculated by subtracting the Baseline value from the Day 3, Day 5 and Day 8 values respectively" (NCT04052620)
Timeframe: Baseline and Days 3, 5 and 8

,
InterventionNewton per square centimeter (N/cm^2) (Least Squares Mean)
Day 3Day 5Day 8
DDEA 1.16% Gel5.7210.7615.60
DDEA 2.32% Gel/Placebo6.929.8417.06

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Change From Baseline in Difference of Circumference (Swelling) Between Affected Ankle and Contralateral Ankle by Figure of Eight Method on Days 3, 5 and 8

Each participant was seated comfortably in a long sitting position with both feet extended beyond the end of the plinth in a slight dorsiflexion position. The Figure of Eight Method was applied to both feet and the tape measure was wrapped around the ankle along the following course: the beginning of the tape was placed midway between the tibialis anterior tendon and lateral malleolus and was then continued across anatomically defined points in the form of a figure of eight around the ankle joint. The tape localization of the first measurement was marked with an appropriate marker. Each ankle was measured three times and the average was calculated. Difference of circumference (swelling) between affected ankle and contralateral ankle is presented. Change from Baseline in circumference on Days 3, 5 and 8 was calculated by subtracting the Baseline value from the Day 3, Day 5 and Day 8 values respectively. (NCT04052620)
Timeframe: Baseline and Days 3, 5 and 8

,
Interventioncm (Least Squares Mean)
Day 3Day 5Day 8
DDEA 1.16% Gel-0.29-0.66-0.92
DDEA 2.32% Gel/Placebo-0.41-0.83-1.12

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Mean Number of Rescue Medication Tablets Used to Treat Ankle Pain

Participants were instructed to take only the rescue medication provided for pain in the ankle or any other pain (for example, headache) or fever (for example, due to common cold) they experienced during the trial. One tablet was taken, repeated after at least 4 hours, if needed, up to a maximum of 2000 milligram (mg) (4 tablets) per day. No rescue medication was allowed within 6 hours prior to the study visits or within 12 hours of study Visit 3. (NCT04052620)
Timeframe: Up to Day 8

InterventionNumber of Tablets (Mean)
DDEA 2.32% Gel/Placebo2.4
DDEA 1.16% Gel2.6

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Change From Baseline in Circumference of Affected Ankle (Swelling) as Measured by Figure of Eight Method on Days 3, 5 and 8

Each participant was seated comfortably in a long sitting position with both feet extended beyond the end of the plinth in a slight dorsiflexion position. The Figure of Eight Method was applied to both feet and the tape measure was wrapped around the ankle along the following course: the beginning of the tape was placed midway between the tibialis anterior tendon and lateral malleolus and was then continued across anatomically defined points in the form of a figure of eight around the ankle joint. The tape localization of the first measurement was marked with an appropriate marker. Each ankle was measured three times and the average was calculated. Change from Baseline in circumference on Days 3, 5 and 8 was calculated by subtracting the Baseline value from the Day 3, Day 5 and Day 8 values respectively. (NCT04052620)
Timeframe: Baseline and Days 3, 5 and 8

,
InterventionCentimeter (cm) (Least Squares Mean)
Day 3Day 5Day 8
DDEA 1.16% Gel-0.24-0.57-0.87
DDEA 2.32% Gel/Placebo-0.42-0.97-1.25

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Change From Baseline in Ankle Joint Function (Karlsson Scoring Scale) on Days 3, 5 and 8

Ankle Joint Function was assessed by the participants using Karlsson Scoring Scale. The scoring scale measured recovery of ankle joint function after an acute ligament injury. Assessments were made in the following eight categories (score): pain (20), swelling (10), instability (subjective) (15), stiffness (5), stair climbing (10), running (10), work activities (15), and the use of a support device (5). The total score ranges in value from 0 (worst possible score) to 90 (best possible score). Change from Baseline in the ankle joint function on Days 3, 5 and 8 was calculated by subtracting the Baseline value from the Day 3, Day 5 and Day 8 values respectively. (NCT04052620)
Timeframe: Baseline and Days 3, 5 and 8

,
InterventionScores on a scale (Least Squares Mean)
Day 3Day 5Day 8
DDEA 1.16% Gel15.5228.2239.75
DDEA 2.32% Gel/Placebo16.2627.9441.87

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Change in the Serum Rates of Cytokines: IL-8

Change in the serum rates of IL-8 in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg12.3182.6688.14811.19010.7453.0609.2437.927
RPH - 20 mg21.9649.3048.7084.3138.01520.88425.6225.468
RPH - 4 mg12.3848.22815.60113.52116.9699.76519.76612.664
RPH - 40 mg9.2779.0309.0208.0327.93711.5208.0035.807
RPH - 80 mg18.30512.3045.95210.5187.59416.3958.5967.223
Voltaren® (Diclofenac)10.86317.14115.98015.18819.88134.7708.55411.763

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Proportion of Patients Who Received a Rescue Therapy Agent

The proportion of patients who received the rescue medication over the entire treatment period (NCT04067492)
Timeframe: up to day 60

InterventionParticipants (Count of Participants)
RPH - 4 mg13
RPH - 20 mg1
RPH - 40 mg4
RPH - 80 mg4
RPH - 160 mg2
Voltaren® (Diclofenac)3

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Change in the Serum Rates of Cytokines: IL-1β

Change in the serum rates of IL-1β in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg0.2900.2900.2900.2900.2900.2900.2900.290
RPH - 20 mg1.0800.2900.2900.2900.2901.2221.3200.290
RPH - 4 mg39.03533.88533.75933.75333.99838.73033.8110.290
RPH - 40 mg0.2900.2900.2900.2900.2900.2900.4170.290
RPH - 80 mg2.5581.1002.1120.2902.3621.9651.7460.290
Voltaren® (Diclofenac)0.2900.2900.2900.2900.2900.2900.2900.290

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Change in the Serum Rates of Cytokines: IL-1α

Change in the serum rates of IL-1α in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg1.0901.0901.0901.0901.0901.0901.0901.090
RPH - 20 mg1.0901.0901.0901.0901.0901.0901.0901.090
RPH - 4 mg1.0901.0901.0901.0901.0901.1321.0971.090
RPH - 40 mg1.0901.0971.0901.0901.0901.0901.0901.090
RPH - 80 mg1.7521.7821.6881.7901.6121.0901.0901.090
Voltaren® (Diclofenac)1.0901.0901.0901.0901.0901.0901.0901.090

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Change in the Serum Rate of High-sensitive CRP (Hs-CRP) in Specified Timeframes

Change in the serum rate of high-sensitive CRP (hs-CRP) in 24, 72 hours, on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours, on Days 5, 6, 15, 29 and 45 after the initiation of treatment with the test drug

,,,,,
Interventionmg/L (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg35.39612.0008.6786.1783.1904.04210.99814.500
RPH - 20 mg8.29520.3383.4083.0902.7102.6427.5323.570
RPH - 4 mg36.67335.46833.89432.27929.06521.01716.81124.958
RPH - 40 mg10.10524.48312.9007.1423.6503.3042.7502.445
RPH - 80 mg37.90828.86411.8468.6964.6045.1155.0143.093
Voltaren® (Diclofenac)15.76922.7169.2798.8778.4176.5797.59511.734

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Time to Achieve the 50% Decrease in Pain Intensity in the Assessed Joint Relative to the Baseline

"Time to achieve the 50% decrease in pain intensity in the assessed joint relative to the baseline VAS level.~VAS is a hard copy 100 mm scale with the indications: Absence of pain on the left side of the scale (0 mm point) and The most severe pain ever experienced on the right side of the scale (100 mm point)). The better outcome would be Absence of pain, the worse outcome would be The most severe pain ever experienced." (NCT04067492)
Timeframe: Baseline and one of the pain intensity measurements in accordance with the schedule: 15, 30, 45 minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 after the initiation of treatment

Interventionhours (Median)
RPH - 4 mgNA
RPH - 20 mg6.0
RPH - 40 mgNA
RPH - 80 mgNA
RPH - 160 mg8.0
Voltaren® (Diclofenac)47.3

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Change in the Serum Rates of Cytokines: IL-6

Change in the serum rates of IL-6 in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg13.6669.0654.6984.9056.22012.85817.9033.753
RPH - 20 mg5.0052.0842.2362.6953.5652.8702.7584.608
RPH - 4 mg26.03527.03014.94323.9998.39110.59518.6436.466
RPH - 40 mg34.30737.7882.1452.3782.9652.4343.2783.370
RPH - 80 mg5.6236.2843.1421.3961.2721.7931.4821.537
Voltaren® (Diclofenac)6.0582.3611.7021.8232.1572.0365.3042.607

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Time to Use of the Rescue Medication

Time to use of the rescue medication was calculated as the time in hours from the date/time of administration (first dose) of the investigational product to the date/time of the first use of the rescue medication. (NCT04067492)
Timeframe: from the date/time of IP administration (first dose) to the date/time of the first use of the rescue medication, up to day 60

Interventionhours (Median)
RPH - 4 mg23.7
RPH - 20 mgNA
RPH - 40 mg71.8
RPH - 80 mg84.6
RPH - 160 mgNA
Voltaren® (Diclofenac)NA

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"Proportion of Patients Who Assessed the Response to Therapy With the Test Drug as Excellent or Good"

"Proportion of patients who assessed the response to therapy with the test drug as Excellent or Good in 15, 30, 45 minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug.~The patient's response to therapy was assessed in the form of frequency tables by assessment point and therapy group. The rates of the response were specified in the evaluation form as: Excellent, Good, Fair, Weak, Poor (where excellent represents the best possible response to treatment and poor indicates the worst treatment response)." (NCT04067492)
Timeframe: 15, 30, 45 minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 after the initiation of treatment with the test drug

,,,,,
InterventionParticipants (Count of Participants)
Day 1/15 minutesDay 1/30 minutesDay 1/45 minutesDay 1/ 1 hourDay 1/ 1.5 hoursDay 1/ 2 hoursDay 1/ 4 hoursDay 1/ 8 hoursDay 2Day 3Day 4Day 5Day 6Day 10Day 15Day 18Day 22Day 29Day 45
RPH - 160 mg0000001222222222211
RPH - 20 mg1110000101112121221
RPH - 4 mg0233332211111111010
RPH - 40 mg0000112222111111111
RPH - 80 mg1122111111332211111
Voltaren® (Diclofenac)1221112425666664533

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Change in Pain Intensity in the Assessed Joint in 15, 30, 45 Minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 Hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 Following the Initiation of Treatment and Compared to Baseline

"Change in pain intensity in the assessed joint in 15, 30, 45 minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug measured using the Visual Analogue Scale (VAS) and compared to baseline. VAS is a hard copy 100 mm scale with the indications: Absence of pain on the left side of the scale (0 mm point) and The most severe pain ever experienced on the right side of the scale (100 mm point)) The better outcome would be Absence of pain, the worse outcome would be The most severe pain ever experienced." (NCT04067492)
Timeframe: Baseline and 15, 30, 45 minutes, 1, 1.5, 2, 4, 8, 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 after the initiation of treatment

,,,,,
Interventionmm (VAS scale) (Least Squares Mean)
Day 1/15 minutesDay 1/30 minutesDay 1/45 minutesDay 1/ 1 hourDay 1/ 1.5 hoursDay 1/ 2 hoursDay 1/ 4 hoursDay 1/ 8 hoursDay 2Day 3Day 4Day 5Day 6Day 10Day 15Day 18Day 22Day 29Day 45
RPH - 160 mg-5.75-10.57-11.77-15.99-17.79-19.59-20.35-25.35-30.35-30.15-30.75-31.35-29.15-29.15-28.95-29.75-28.35-17.95-19.75
RPH - 20 mg-6.97-14.16-16.14-15.81-15.14-25.14-27.27-29.61-37.77-35.77-38.77-31.27-34.44-37.27-41.77-42.61-44.61-44.94-46.94
RPH - 4 mg-2.00-10.00-16.20-19.67-22.47-22.07-21.87-14.20-10.60-3.33-6.67-4.73-4.80-6.73-4.13-4.07-3.20-4.07-2.60
RPH - 40 mg-5.91-6.43-7.91-11.76-21.26-24.63-21.44-18.93-20.94-27.94-18.91-13.64-12.43-12.43-12.41-12.74-13.58-13.58-13.58
RPH - 80 mg-1.52-5.19-9.36-12.52-14.69-13.86-14.36-16.52-25.52-34.69-34.52-35.86-22.86-23.52-12.69-12.69-12.69-12.69-12.69
Voltaren® (Diclofenac)-3.78-5.45-8.56-12.67-13.67-20.56-22.67-25.67-30.34-38.67-38.12-42.78-42.45-37.78-38.34-28.45-30.34-23.89-23.34

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Change in the Rate of Serum Amyloid Protein A in the Specified Timeframes

Change in the rate of serum amyloid protein A in 24, 72 hours and on Day 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Day 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionng/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg16291.6053659.77810596.4235952.4606117.7772732.5983618.8439885.230
RPH - 20 mg2516.60611078.3001171.2031195.9751847.9231525.6124255.7562086.198
RPH - 4 mg13493.68717424.06017588.73517360.20118553.9559272.7828918.43913858.845
RPH - 40 mg16764.02020104.55512162.6125680.1904781.1738899.9821645.1071269.680
RPH - 80 mg16168.13015581.48614419.7608228.2725799.6084582.3383626.7021567.040
Voltaren® (Diclofenac)5033.1517294.6317362.3228252.6336165.7796031.1463779.4107289.553

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Proportion of Patients Who Received a Rescue Therapy Agent

The proportion of patients who received the rescue medication within 72 hours of starting the investigational product therapy (NCT04067492)
Timeframe: 72 hours after the initiation of treatment with the test drug

InterventionParticipants (Count of Participants)
RPH - 4 mg12
RPH - 20 mg1
RPH - 40 mg3
RPH - 80 mg3
RPH - 160 mg2
Voltaren® (Diclofenac)2

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Pharmacokinetics (PK) of RPH-104 Under the Subcutaneous Administration

Including elimination constant (Kel) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Intervention1/h (Mean)
RPH - 4 mg0.00298
RPH - 20 mg0.00314
RPH - 40 mg0.00304
RPH - 80 mg0.00317
RPH - 160 mg0.00294

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Pharmacokinetics (PK) -Time to Reach Maximum Concentration of the Active Substance - of RPH-104 Under the Subcutaneous Administration

Including Time to reach maximum concentration of the active substance (tmax) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Interventionhours (Median)
RPH - 4 mg93.7
RPH - 20 mg47.5
RPH - 40 mg84.8
RPH - 80 mg82.7
RPH - 160 mg94.4

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Pharmacokinetics (PK) - Terminal Half-life -of RPH-104 Under the Subcutaneous Administration

Including terminal half-life (T 1/2) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Interventionhours (Median)
RPH - 4 mg248
RPH - 20 mg235
RPH - 40 mg223
RPH - 80 mg231
RPH - 160 mg241

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Pharmacokinetics (PK) - Maximum Concentration of the Active Substance -of RPH-104 Under the Subcutaneous Administration

Including Maximum concentration of the active substance (Cmax) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Interventionng/mL (Geometric Mean)
RPH - 4 mg142
RPH - 20 mg2220
RPH - 40 mg2380
RPH - 80 mg4860
RPH - 160 mg9760

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Pharmacokinetics (PK) - Area Under the Plasma concentration-of RPH-104 Under the Subcutaneous Administration

Including area under the plasma concentration-time curve over the dosing interval (AUC0-tau) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Interventionh*ng/mL (Geometric Mean)
RPH - 4 mg38000
RPH - 20 mg762000
RPH - 40 mg845000
RPH - 80 mg1620000
RPH - 160 mg3230000

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Change in the Serum Rates of Cytokines: Tumor Necrosis Factor (TNF-α)

Change in the serum rates of TNF-α in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg2.2902.2902.2902.2902.2902.2902.2902.290
RPH - 20 mg2.2902.2902.2902.2902.2902.2902.2902.290
RPH - 4 mg2.2902.2902.2902.2902.2902.2902.2902.290
RPH - 40 mg2.2902.2902.2902.2902.2902.2902.2902.290
RPH - 80 mg2.2902.2902.2902.2902.2902.2902.2902.290
Voltaren® (Diclofenac)2.2902.2902.2902.2902.2902.2902.2902.290

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Pharmacokinetics (PK) - Area Under the Active Substance Concentration- of RPH-104 Under the Subcutaneous Administration

Including Area under the active substance concentration-time curve from zero (before drug administration) to infinity (AUC0-∞) (NCT04067492)
Timeframe: Baseline and in 2,8,24,48,72 hours,on Days 5,6,10,15,18,22,29,45 following the initiation of treatment with the test drug and on the follow-up visit (in case of premature withdrawal of patient)

Interventionh*ng/mL (Geometric Mean)
RPH - 4 mg47900
RPH - 20 mg816000
RPH - 40 mg901000
RPH - 80 mg1720000
RPH - 160 mg3380000

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Change in the Serum Rates of Cytokines: Interleukin -1 Receptor Antagonist (IL-1RA)

Change in the serum rates of IL-1RA in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug as compared to baseline (NCT04067492)
Timeframe: Baseline and in 24, 72 hours and on Days 5, 6, 15, 29 and 45 following the initiation of treatment with the test drug

,,,,,
Interventionpg/mL (Mean)
Baseline valueDay 2/ 24 hoursDay 4/ 72 hoursDay 5Day 6Day 15Day 29Day 45
RPH - 160 mg2619.45629.99029.99029.99029.990257.492471.178518.063
RPH - 20 mg1448.978229.842156.216187.223214.610374.900563.892915.010
RPH - 4 mg2400.5001700.1801295.7431364.9931407.2301620.3321928.4171806.647
RPH - 40 mg1671.010153.098140.108154.463203.688474.542583.062808.212
RPH - 80 mg2240.15529.990157.65487.214180.492645.085686.992711.997
Voltaren® (Diclofenac)2090.7212483.8912297.6512417.9912426.7612249.7941870.8151969.547

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Change in Pain Intensity in the Assessed Joint 72 Hours After the Initiation of Treatment in Comparison to Baseline

"Change in pain intensity in the assessed joint 72 hours after the initiation of treatment with the test drug measured using the Visual Analogue Scale (VAS) in comparison to baseline. VAS is a hard copy 100 mm scale with the indications: Absence of pain on the left side of the scale (0 mm point) and The most severe pain ever experienced on the right side of the scale (100 mm point)) The better outcome would be Absence of pain, the worse outcome would be The most severe pain ever experienced." (NCT04067492)
Timeframe: Baseline and Day 4 (72 hours after the initiation of treatment with the test drug)

Interventionmm (VAS scale) (Least Squares Mean)
RPH - 4 mg-7.88
RPH - 20 mg-38.56
RPH - 40 mg-19.80
RPH - 80 mg-33.39
RPH - 160 mg-30.55
Voltaren® (Diclofenac)-36.51

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Disability Index

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~(The result for each of the 8 categories (Dressing and Grooming, Arising, Eating, Walking, Hygiene, Reach, Grip, Activities) of the HAQ questionnaire was calculated as the maximum score of responses (on an ordinal scale from 0 (best) to 3 (worst): without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3)) to questions included in this category. If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2. The sum of points for the evaluated categories was calculated and divided by the number of categories, which gives a disability index in the range of 0 to 3.)" (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg1.6-1.06-0.5-0.56
RPH - 20 mg1.23-0.63-1.09-1.42
RPH - 4 mg1.3-0.75-0.13-0.38
RPH - 40 mg1.75-0.88-1.25-1.38
RPH - 80 mg1.1-0.63-0.63-0.63
Voltaren® (Diclofenac)1.32-0.56-0.38-0.44

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Change in the Rate of Erythema of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug

"Change in the rate of erythema of the assessed joint evaluated in 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug compared to baseline.The rates of erythema were specified as absence, presence, impossible to evaluate." (NCT04067492)
Timeframe: Baseline and 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug

InterventionParticipants (Count of Participants)
Baseline72491713Baseline72491715Baseline72491716Baseline72491711Baseline72491712Baseline72491714Day 2/ 24 hours72491711Day 2/ 24 hours72491714Day 2/ 24 hours72491712Day 2/ 24 hours72491713Day 2/ 24 hours72491715Day 2/ 24 hours72491716Day 3/ 48 hours72491711Day 3/ 48 hours72491714Day 3/ 48 hours72491715Day 3/ 48 hours72491716Day 3/ 48 hours72491713Day 3/ 48 hours72491712Day 4/ 72 hours72491711Day 4/ 72 hours72491715Day 4/ 72 hours72491714Day 4/ 72 hours72491716Day 4/ 72 hours72491712Day 4/ 72 hours72491713Day 572491711Day 572491713Day 572491715Day 572491716Day 572491714Day 572491712Day 672491714Day 672491716Day 672491711Day 672491712Day 672491713Day 672491715Day 1072491715Day 1072491716Day 1072491711Day 1072491712Day 1072491713Day 1072491714Day 1572491714Day 1572491711Day 1572491712Day 1572491713Day 1572491715Day 1572491716Day 1872491711Day 1872491714Day 1872491715Day 1872491716Day 1872491713Day 1872491712227249171122724917152272491716227249171222724917132272491714297249171129724917152972491712297249171329724917142972491716457249171545724917144572491711457249171245724917134572491716
evaluation impossibleabsencepresence
RPH - 4 mg3
RPH - 4 mg12
RPH - 20 mg6
RPH - 40 mg6
RPH - 80 mg5
RPH - 160 mg5
RPH - 4 mg5
RPH - 20 mg2
RPH - 4 mg7
RPH - 40 mg4
RPH - 80 mg4
RPH - 160 mg1
Voltaren® (Diclofenac)5
RPH - 80 mg1
RPH - 160 mg2
RPH - 160 mg0
Voltaren® (Diclofenac)7
RPH - 40 mg2
RPH - 40 mg0
RPH - 40 mg1
RPH - 80 mg3
RPH - 4 mg2
RPH - 80 mg2
RPH - 80 mg0
RPH - 4 mg0
RPH - 20 mg3
Voltaren® (Diclofenac)4
RPH - 20 mg0
Voltaren® (Diclofenac)0
Voltaren® (Diclofenac)6
RPH - 4 mg1
RPH - 160 mg3
Voltaren® (Diclofenac)2
RPH - 20 mg4
RPH - 20 mg1

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Eating

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~The result was calculated as the maximum score of responses (on an ordinal scale from 0 to 3) to questions included in this category. Patients were asked about their ability to complete these tasks in the past week using the following categories: without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3). Scores on each task were summed and averaged to provide an overall score ranging from 0 (best) to 3 (worst).~If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2." (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg1.00.0-0.5-0.5
RPH - 20 mg0.7-0.5-1.0-1.3
RPH - 4 mg1.00.00.00.0
RPH - 40 mg1.30.00.00.0
RPH - 80 mg0.80.00.00.0
Voltaren® (Diclofenac)0.7-0.3-0.3-0.3

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Grip

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~The result was calculated as the maximum score of responses (on an ordinal scale from 0 to 3) to questions included in this category. Patients were asked about their ability to complete these tasks in the past week using the following categories: without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3). Scores on each task were summed and averaged to provide an overall score ranging from 0 (best) to 3 (worst).~If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2." (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg1.20.0-0.5-1.0
RPH - 20 mg1.0-0.5-1.0-1.3
RPH - 4 mg1.4-1.0-1.0-1.0
RPH - 40 mg1.20.00.00.0
RPH - 80 mg1.0-1.0-1.0-1.0
Voltaren® (Diclofenac)0.4-0.2-0.30.3

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Hygiene

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~The result was calculated as the maximum score of responses (on an ordinal scale from 0 to 3) to questions included in this category. Patients were asked about their ability to complete these tasks in the past week using the following categories: without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3). Scores on each task were summed and averaged to provide an overall score ranging from 0 (best) to 3 (worst).~If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2." (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg2.2-2.5-0.5-0.5
RPH - 20 mg1.2-0.3-1.3-1.7
RPH - 4 mg1.2-1.01.00.0
RPH - 40 mg1.7-1.0-1.0-1.0
RPH - 80 mg1.5-1.0-1.0-1.0
Voltaren® (Diclofenac)1.3-0.5-0.5-1.0

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Walking

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~The result was calculated as the maximum score of responses (on an ordinal scale from 0 to 3) to questions included in this category. Patients were asked about their ability to complete these tasks in the past week using the following categories: without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3). Scores on each task were summed and averaged to provide an overall score ranging from 0 (best) to 3 (worst).~If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2." (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg1.6-1.5-0.5-0.5
RPH - 20 mg1.8-1.3-1.3-1.3
RPH - 4 mg1.40.00.00.0
RPH - 40 mg1.8-1.0-2.0-2.0
RPH - 80 mg1.3-1.0-1.0-1.0
Voltaren® (Diclofenac)1.8-0.7-0.3-0.8

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Change in the Rate of Movement Restrictions in the Specified Timeframes After Initiation of Treatment

"Change in the rate of movement restrictions in the assessed joint evaluated in 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug compared to baseline. For the assessment, the categorical scale consistent with the Form for evaluation (Investigator's Assessment) of the restriction of movements was used. The rates of movement restrictions (amplitude of movements) were specified in the evaluation form as 1 - Normal range, 2 - Slightly limited range, 3 - Moderately limited range ,4 - Severely limited range and 5 - Joint movement is impossible (where higher score means worse outcome)." (NCT04067492)
Timeframe: Baseline and in 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug

InterventionParticipants (Count of Participants)
Baseline72491714Baseline72491715Baseline72491716Baseline72491711Baseline72491712Baseline72491713Day 2/ 24 hours72491716Day 2/ 24 hours72491713Day 2/ 24 hours72491714Day 2/ 24 hours72491715Day 2/ 24 hours72491711Day 2/ 24 hours72491712Day 3/ 48 hours72491715Day 3/ 48 hours72491716Day 3/ 48 hours72491713Day 3/ 48 hours72491711Day 3/ 48 hours72491712Day 3/ 48 hours72491714Day 4/ 72 hours72491713Day 4/ 72 hours72491714Day 4/ 72 hours72491715Day 4/ 72 hours72491711Day 4/ 72 hours72491716Day 4/ 72 hours72491712Day 572491711Day 572491713Day 572491715Day 572491714Day 572491712Day 572491716Day 672491712Day 672491713Day 672491714Day 672491715Day 672491711Day 672491716Day 1072491714Day 1072491715Day 1072491711Day 1072491712Day 1072491713Day 1072491716Day 1572491711Day 1572491715Day 1572491716Day 1572491712Day 1572491713Day 1572491714Day 1872491715Day 1872491716Day 1872491714Day 1872491713Day 1872491711Day 1872491712Day 2272491715Day 2272491712Day 2272491716Day 2272491711Day 2272491713Day 2272491714Day 2972491713Day 2972491714Day 2972491715Day 2972491712Day 2972491711Day 2972491716Day 4572491713Day 4572491716Day 4572491714Day 4572491711Day 4572491712Day 4572491715
12534
RPH - 160 mg0
RPH - 4 mg5
RPH - 80 mg3
RPH - 160 mg2
Voltaren® (Diclofenac)6
RPH - 4 mg9
RPH - 20 mg4
RPH - 40 mg5
Voltaren® (Diclofenac)3
RPH - 80 mg1
RPH - 160 mg1
RPH - 4 mg7
RPH - 40 mg3
RPH - 4 mg3
Voltaren® (Diclofenac)1
RPH - 20 mg5
RPH - 40 mg2
Voltaren® (Diclofenac)4
RPH - 20 mg2
Voltaren® (Diclofenac)2
Voltaren® (Diclofenac)5
Voltaren® (Diclofenac)0
RPH - 20 mg3
RPH - 80 mg2
RPH - 20 mg1
RPH - 4 mg1
RPH - 4 mg0
RPH - 20 mg0
RPH - 40 mg0
RPH - 40 mg1
RPH - 80 mg0

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Change in the Rate of Swelling of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug

"Change in the rate of swelling of the assessed joint evaluated in 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug compared to baseline. The rates of swelling were specified in the evaluation form as: absence = no swelling, mild = palpable swelling, moderate = visible swelling, severe = bulging outside the joint (where severe represented the worst possible degree of swelling and absence was the best outcome)." (NCT04067492)
Timeframe: Baseline and 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug

InterventionParticipants (Count of Participants)
Baseline72491713Baseline72491715Baseline72491716Baseline72491712Baseline72491714Baseline72491711Day 2/ 24 hours72491711Day 2/ 24 hours72491712Day 2/ 24 hours72491713Day 2/ 24 hours72491715Day 2/ 24 hours72491716Day 2/ 24 hours72491714Day 3/ 48 hours72491713Day 3/ 48 hours72491716Day 3/ 48 hours72491712Day 3/ 48 hours72491711Day 3/ 48 hours72491714Day 3/ 48 hours72491715Day 4/ 72 hours72491711Day 4/ 72 hours72491713Day 4/ 72 hours72491714Day 4/ 72 hours72491716Day 4/ 72 hours72491715Day 4/ 72 hours72491712Day 572491713Day 572491714Day 572491711Day 572491712Day 572491715Day 572491716Day 672491714Day 672491711Day 672491712Day 672491713Day 672491715Day 672491716Day 1072491711Day 1072491712Day 1072491713Day 1072491716Day 1072491714Day 1072491715Day 1572491712Day 1572491713Day 1572491715Day 1572491716Day 1572491711Day 1572491714Day 1872491713Day 1872491711Day 1872491715Day 1872491716Day 1872491712Day 1872491714227249171422724917132272491711227249171222724917152272491716297249171329724917142972491711297249171229724917162972491715457249171445724917114572491715457249171645724917124572491713
absencemildmoderatesevere
RPH - 4 mg9
RPH - 40 mg2
RPH - 80 mg4
RPH - 4 mg5
RPH - 40 mg4
RPH - 160 mg4
RPH - 4 mg2
RPH - 4 mg8
RPH - 40 mg3
Voltaren® (Diclofenac)5
RPH - 80 mg1
RPH - 4 mg1
RPH - 80 mg3
Voltaren® (Diclofenac)2
Voltaren® (Diclofenac)1
RPH - 80 mg2
RPH - 160 mg1
Voltaren® (Diclofenac)4
RPH - 80 mg0
RPH - 160 mg2
Voltaren® (Diclofenac)3
RPH - 40 mg1
RPH - 40 mg0
RPH - 160 mg0
Voltaren® (Diclofenac)0
Voltaren® (Diclofenac)6
RPH - 20 mg2
RPH - 20 mg3
RPH - 20 mg1
RPH - 20 mg0
RPH - 20 mg4
RPH - 4 mg0

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Change in the Rate of Tenderness of the Assessed Joint Evaluated After the Initiation of Treatment With the Test Drug

"Change in the rate of tenderness of the assessed joint evaluated in 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug compared to baseline. Tenderness degrees: absent = no tenderness, mild = tenderness when touched, moderate = pain and flinching, severe = pain, flinching and withdrawal of the limb (where severe represents the worst possible degree of tenderness and absent is the best outcome)." (NCT04067492)
Timeframe: Baseline and 24, 48, 72 hours, on Days 5, 6, 10, 15, 18, 22, 29 and 45 following the initiation of treatment with the test drug

InterventionParticipants (Count of Participants)
Baseline72491711Baseline72491712Baseline72491715Baseline72491714Baseline72491716Baseline72491713Day 2/ 24 hours72491712Day 2/ 24 hours72491715Day 2/ 24 hours72491716Day 2/ 24 hours72491711Day 2/ 24 hours72491713Day 2/ 24 hours72491714Day 3/ 48 hours72491711Day 3/ 48 hours72491715Day 3/ 48 hours72491716Day 3/ 48 hours72491712Day 3/ 48 hours72491713Day 3/ 48 hours72491714Day 4/ 72 hours72491711Day 4/ 72 hours72491713Day 4/ 72 hours72491716Day 4/ 72 hours72491712Day 4/ 72 hours72491714Day 4/ 72 hours72491715Day 572491711Day 572491713Day 572491714Day 572491716Day 572491712Day 572491715Day 672491711Day 672491712Day 672491713Day 672491714Day 672491715Day 672491716Day 1072491716Day 1072491711Day 1072491712Day 1072491713Day 1072491714Day 1072491715Day 1572491715Day 1572491716Day 1572491711Day 1572491714Day 1572491712Day 1572491713Day 1872491713Day 1872491714Day 1872491716Day 1872491711Day 1872491712Day 1872491715227249171122724917122272491715227249171322724917162272491714297249171229724917132972491715297249171629724917112972491714457249171345724917114572491712457249171445724917154572491716
absencemildmoderatesevere
RPH - 4 mg12
RPH - 20 mg4
RPH - 80 mg4
RPH - 160 mg2
Voltaren® (Diclofenac)6
RPH - 4 mg2
RPH - 40 mg3
RPH - 80 mg2
RPH - 160 mg3
RPH - 20 mg0
RPH - 4 mg4
RPH - 20 mg5
RPH - 4 mg6
RPH - 80 mg3
Voltaren® (Diclofenac)2
RPH - 40 mg2
RPH - 20 mg2
RPH - 20 mg3
Voltaren® (Diclofenac)5
RPH - 4 mg0
RPH - 40 mg1
RPH - 80 mg1
RPH - 160 mg1
Voltaren® (Diclofenac)1
RPH - 4 mg1
RPH - 20 mg1
RPH - 40 mg0
RPH - 160 mg0
Voltaren® (Diclofenac)0
RPH - 80 mg0
Voltaren® (Diclofenac)3
Voltaren® (Diclofenac)4

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Changes in the Health Assessment Questionnaire (HAQ) Parameters: Arising

"Changes in the Health Assessment Questionnaire (HAQ) parameters in 15, 29 and 45 days following the initiation of treatment with the test drug as compared to baseline.~The result was calculated as the maximum score of responses (on an ordinal scale from 0 to 3) to questions included in this category. Patients were asked about their ability to complete these tasks in the past week using the following categories: without any difficulty (0); with some difficulty (1); with much difficulty (2); and unable to do (3). Scores on each task were summed and averaged to provide an overall score ranging from 0 (best) to 3 (worst).~If the patient required outside help or any of the specified aids or devices to perform actions related to a certain category, then this category was assigned 2 points, if the point was not equal to 3, i.e. points 0 and 1 increased to 2." (NCT04067492)
Timeframe: Baseline and 15, 29 and 45 days following the initiation of treatment with the test drug

,,,,,
Interventionunits of the HAQ index (Mean)
Baseline valueChange Day 15Change Day 29Change Day 45
RPH - 160 mg1.4-1.0-0.5-0.5
RPH - 20 mg1.3-1.0-1.3-1.3
RPH - 4 mg0.9-1.0-1.0-1.0
RPH - 40 mg1.5-1.0-1.0-1.0
RPH - 80 mg0.70.00.00.0
Voltaren® (Diclofenac)1.2-0.50.00.0

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Change in Pain Units on a Scale (0-10) 0 Being Least, 10 Being Worst Pain From Baseline

Change in the self described pain units on a scale by patient at baseline and post-treatment on the range of 0 - 10, 0 being the least pain and 10 being the worst pain. (NCT04391842)
Timeframe: 7 days

Interventionpain units on a scale (Mean)
Experimental: SAM Ultrasound and Diclofenac Patch2.00

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Change in the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Scores, Ranging From 0 Being No Difficulty to 2400 Being Extreme Difficulty, From Baseline

WOMAC questionnaire will be utilized (Western Ontario and McMaster Universities Arthritis Index) at baseline and post-treatment to calculate the change in the scores. WOMAC was divided into 3 categories: pain, stiffness, function and total score. The pain category consists of five scores from 0-10, 0 is no pain 10 is worst pain possible for a range of 0 - 50 points. The stiffness category consists of two scores from 0-10, 0 is no stiffness 10 is worst stiffness possible for a range of 0 - 20 points. The function score consists of 17 scores from 0-10, 0 is normal function and 10 is severely limited function, for a range of 0 - 170 points. Categories were multiplied by 10 for analysis. Total score is the sum of pain, stiffness, and function scores (range of 0 - 2400) (NCT04391842)
Timeframe: 7 days

Interventionscores on a scale (Mean)
Experimental: SAM Ultrasound and Diclofenac Patch-353

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Total Post-operative Opioid Requirements With Non-opioid Drug Regimen

Total post-operative opioid requirements (opioid dose) were calculated for participants receiving the non-opioid drug regimen, among participants who required post-operative opioid medication. (NCT04766996)
Timeframe: Up to 5 weeks

Interventionmilligrams (Mean)
Prospective Cases Undergoing Non-opioid Drug Regimen400

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Nebraska Interprofessional Education Attitude Scale (NIPEAS) Score for Professional Staff Arm

The Nebraska Interprofessional Education Attitude Scale (NIPEAS) was developed to measure the attitudes of pre-clinical learners to practicing health professionals. The NIPEAS is a 19-item questionnaire assessing attitudes related to interprofessional collaboration. Responses were given using a 5-point Likert scale where 1 = Strongly Disagree to 5 = Strongly Agree. The total score is the average of the average scores for each item and ranges from 1 to 5. A higher total score indicates increased positive perceptions toward interprofessional collaboration. (NCT04766996)
Timeframe: Prior to protocol implementation (baseline), halfway through the recruitment period (2 months) and after the last participant has been discharged from the hospital (4 months)

Interventionscore on a scale (Mean)
Baseline
Professional Staff4.35

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