Page last updated: 2024-12-05

carbostyril

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2. [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 CID6038
CHEMBL ID186422
CHEBI ID16365
CHEBI ID18289
SCHEMBL ID8621
MeSH IDM0055311

Synonyms (100)

Synonym
AC-3056
hydroxyquinoleine [french]
CHEBI:16365 ,
alpha-quinolone
CHEBI:18289
2-chinolinol
ccris 4327
alpha-hydroxyquinoline
carbostyril (van)
nsc 156783
2-quinolinone
einecs 200-420-6
ai3-00782
AC-907/25014359
2-(1h)-quinolinone
STK097666
inchi=1/c9h7no/c11-9-6-5-7-3-1-2-4-8(7)10-9/h1-6h,(h,10,11
quinolinol
C06338
70254-42-1
2(1h)-quinolinone
59-31-4
quinolin-2-ol ,
quinolin-2(1h)-one
2(1h)-quinolone
o-aminocinnamic acid lactam
2-hydroxyquinoline
.alpha.-hydroxyquinoline
2-quinolinol
nsc-554
2-quinolone
C06415
.alpha.-quinolone
carbostyril
nsc554
nsc-156783
nsc156783
2-oxoquinoline
NCGC00166019-01
DB04745
2-hydroxyquinoline, 98%
quinolin-2-one
STK414900
CHEMBL186422 ,
H0304
1h-quinolin-2-one
AKOS003297745
A836815
quinolones
quinolinone
803bhy7qwu ,
unii-803bhy7qwu
bdbm50366034
1,2-dihydroquinolin-2-one
EN300-67221
hydroxyquinoleine
1321-40-0
hydroquinolin-2-one
104534-80-7
quinolone
einecs 274-516-1
BP-10114
FT-0612637
PS-4021
AKOS015897112
MLS004491723
smr003288680
carbostyril [mi]
hydroxyquinoline, 2-
SCHEMBL8621
3SRG
mfcd00006743
SY003693
a-hydroxyquinoline
2-oxo-1,2-dihydroquinoline
1h-quinolinone
quino- lone
hyroxyquinoline
1h-quinolone
2-[1h]-quinolone
1-h-quinolone
DTXSID1058769
W-104563
STR05548
HMS3604N04
CS-W005598
GS-6597
Z57473020
F0001-1542
Q27095480
AMY23222
SB37816
hydroquinolinone
SB67445
STARBLD0000627
10.14272/LISFMEBWQUVKPJ-UHFFFAOYSA-N.1
doi:10.14272/lisfmebwquvkpj-uhfffaoysa-n.1
E82978
mfcd00463096
SY303522

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse events were minor and transient."( Efficacy and safety of nedocromil sodium ophthalmic solution in the treatment of seasonal allergic conjunctivitis.
Blumenthal, M; Casale, T; Dockhorn, R; Jarmoszuk, I; Kaiser, H; Smith, R; Zeitz, HJ, 1992
)
0.28
" Treatment-related adverse events were reported for 7% of patients in the lomefloxacin group and 5% in the cefaclor group."( Safety and efficacy of lomefloxacin versus cefaclor in the treatment of acute exacerbations of chronic bronchitis.
Ellison, WT; Gotfried, MH, 1992
)
0.28
" Adverse events probably related to treatment occurred in 6% of those treated with lomefloxacin and in 7% of patients treated with TMP/SMX."( Comparison of the safety and efficacy of lomefloxacin and trimethoprim/sulfamethoxazole in the treatment of uncomplicated urinary tract infections: results from a multicenter study.
Aguirre-Avalos, G; Andrade-Villanueva, J; Flores-Gaxiola, A; Lopez-Guillen, P; Morfin-Otero, R; Rodriguez-Noriega, E, 1992
)
0.28
" Two lomefloxacin-treated patients (3%) and four patients treated with ciprofloxacin (5%) withdrew from treatment because of adverse events."( A comparison of the safety and efficacy of lomefloxacin and ciprofloxacin in the treatment of complicated or recurrent urinary tract infections.
Cox, CE, 1992
)
0.28
" Although the quinolone is highly toxic to mammalian cells in culture, its mechanism of cytotoxic action is not known."( Cytotoxicity of quinolones toward eukaryotic cells. Identification of topoisomerase II as the primary cellular target for the quinolone CP-115,953 in yeast.
Elsea, SH; Nitiss, JL; Osheroff, N, 1992
)
0.28
" The frequency and severity of adverse events were similar in both groups, consisting primarily of digestive disorders and skin manifestations."( Efficacy and safety of temafloxacin versus those of amoxicillin in hospitalized adults with community-acquired pneumonia.
Carbon, C; Chauvin, JP; Hazebroucq, J; Léophonte, P; Petitpretz, P, 1992
)
0.28
" On the whole, the treatments were well tolerated, but some minor adverse events (mainly headache, insomnia, or abdominal discomfort) were reported for 7 subjects on abnormalities were detected in the laboratory examinations or in ocular function tests."( Multiple-dose pharmacokinetics and safety of rufloxacin in normal volunteers.
Cohen, GM; Griess, RS; Imbimbo, BP; Kisicki, JC; McCormack, RJ; Ott, CL; Troetel, WM, 1992
)
0.28
" The only adverse event possibly related to the study drug was a case of transient mild tiredness and nervousness."( An open multicentre study on the efficacy and safety of rufloxacin in patients with chronic bacterial prostatitis.
Bischoff, W; Boerema, JB; Focht, J; Naber, KG, 1991
)
0.28
"During the Phase I, II, and III clinical development program, temafloxacin has demonstrated an excellent safety profile, with reported overall rates of adverse events comparable to quinolone and nonquinolone reference agents."( Temafloxacin: a safe antibiotic for the elderly, patients with comorbidities, and other special populations.
Pernet, AG, 1991
)
0.28
"This article summarizes animal studies conducted to determine the toxic and mutagenic potential of temafloxacin."( Comparison of organ-specific toxicity of temafloxacin in animals and humans.
Krasula, RW; Pernet, AG, 1991
)
0.28
" Adverse events were collated by spontaneous reporting by the patients or observations by investigators and, additionally in some studies, by the use of diary cards filled in by the patients."( Assessment of adverse events during drug development: experience with temafloxacin.
Norrby, SR; Pernet, AG, 1991
)
0.28
" The dams were monitored daily for adverse physical signs and maternal blood samples were collected for analyses of serum progesterone (P), 17 beta-estradiol (E2), and chorionic gonadotropin (CG)."( Developmental toxicity of temafloxacin hydrochloride in the long-tailed macaque (Macaca fascicularis).
Hendrickx, AG; Lasley, BL; Lehrer, SB; Tarantal, AF, 1990
)
0.28
" Extensive laboratory monitoring of renal, hepatic and haematological functions before, during and at the end of the study failed to provide any evidence of drug-induced toxic effects."( The acceptability, safety and efficacy of nedocromil sodium in long-term clinical use in patients with perennial asthma.
Carrasco, E; Sepulveda, R,
)
0.13
" The genotoxic and the toxic activities increased in a highly parallel fashion from the parent compounds, nalidixic acid and oxolinic acid, to the new generation fluoroquinolones."( Genotoxicity of 17 gyrase- and four mammalian topoisomerase II-poisons in prokaryotic and eukaryotic test systems.
Albertini, S; Chételat, AA; Gocke, E; Miller, B; Muster, W; Pujadas, E; Strobel, R, 1995
)
0.29
" Generally, adverse effects reported in association with the fluoroquinolones have been those that could have been predicted by previous experience with non-fluorinated derivatives and by animal toxicity studies."( Safety and tolerability of fluoroquinolones.
Lietman, PS; Norrby, SR, 1993
)
0.29
"05%) was uniformly toxic to both cultured human cells and microorganisms; (2) nitrofurazone (0."( Cytotoxicity testing of topical antimicrobial agents on human keratinocytes and fibroblasts for cultured skin grafts.
Boyce, ST; Holder, IA; Warden, GD,
)
0.13
" All 10 patients provided analyzable data even though one patient withdrew before the 144-h sample because of an adverse event unrelated to the study medication."( Pharmacokinetics, safety, and tolerability of flosequinan in patients with hepatic dysfunction.
Hind, ID; Hinson, JL; Weidler, DJ, 1994
)
0.29
" Adverse effects in the lomefloxacin group were observed on 20 occasions in 12 patients (one stopped treatment) compared to nine occasions in five patients treated with norfloxacin (difference not significant)."( Safety and efficacy of lomefloxacin versus norfloxacin in the treatment of complicated urinary tract infections.
Benne, RA; Boon, TA; de Hond, HA; de Wit, MA; Havinga, WH; Hoepelman, IM; van Asbeck, FW; Verhoef, J; Visser, MR; Zwinkels, M, 1993
)
0.29
" Prulifloxacin had no adverse effects on reproductive function of the parent animals, and also on development of the fetuses."( [Reproductive and developmental toxicity studies of prulifloxacin (NM441)(1)--A fertility study in rats by oral administration].
Fujii, S; Furukawa, S; Kikumori, M; Morinaga, T; Shindo, Y; Sumi, N; Watanabe, M; Yasuhira, K, 1996
)
0.29
" Prulifloxacin also did not affect delivery and the number of live newborns and birth index, or have any adverse effects on the postnatal development of the first generation offspring (F1) such as differentiation, functional development, emotionality, motor ability, learning ability or reproductive performance."( [Reproductive and developmental toxicity studies of prulifloxacin (NM441)(2)--A teratogenicity study in rats by oral administration].
Fujii, S; Furukawa, S; Kikumori, M; Morinaga, T; Shindo, Y; Sumi, N; Watanabe, M; Yasuhira, K, 1996
)
0.29
" Prulifloxacin also did not affect the number of live newborns and birth index, and have any adverse effects on the postnatal development of the first generation offspring (F1) such as differentiation, functional development, emotionality, motor ability, learning ability and reproductive performance."( [Reproductive and developmental toxicity studies of prulifloxacin (NM441)(4)--A perinatal and postnatal study in rats by oral administration].
Fujii, S; Kikumori, M; Morinaga, T; Nishimori, T; Okazaki, I; Shindo, Y; Sumi, N; Watanabe, M, 1996
)
0.29
" The incidence of adverse events, the incidence and severity of antibacterial-related adverse events and the incidence of antibacterial discontinuation due to adverse events were no different among patients treated with sparfloxacin compared with those who received a comparator antibacterial agent."( Safety profile of sparfloxacin in the treatment of respiratory tract infections.
Rubinstein, E, 1996
)
0.29
" Few serious adverse cardiovascular events have been reported during post-marketing surveillance of sparfloxacin and all have occurred in patients with an underlying cardiac condition."( Overview of electrocardiographic and cardiovascular safety data for sparfloxacin. Sparfloxacin Safety Group.
Brumpt, I; Jaillon, P; Morganroth, J; Talbot, G, 1996
)
0.29
"(S)-10-[(S)-(8-Amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyli c acid hemihydrate (CAS 151390-79-3, DV-7751a) a new quinolone antibacterial agent, was examined for LD50 value, phototoxicity and convulsion inducing potential in laboratory animals."( LD50 value, phototoxicity and convulsion induction test of the new quinolone antibacterial agent (S)-10-[(S)-(8-amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyl ic acid hemihydrate in la
Akahane, K; Kato, M; Nomura, M; Shimoda, K, 1996
)
0.29
"To elucidate the mechanism of phototoxicity induced as a side effect by some of the new quinolone antibiotics, we studied sparfloxacin (SPFX), lomefloxacin, enoxacin, ofloxacin, and ciprofloxacin."( Participation of reactive oxygen species in phototoxicity induced by quinolone antibacterial agents.
Arakane, K; Hirobe, M; Mashiko, S; Nagano, T; Ryu, A; Umezawa, N, 1997
)
0.3
" Grepafloxacin was well tolerated, with the most frequently reported drug-related adverse events being taste perversion and nausea."( Efficacy and safety of grepafloxacin 600 mg daily for 10 days in patients with community-acquired pneumonia.
Breisch, SA; Maroli, AN; Swarz, H; Topkis, S,
)
0.13
" All treatments were well tolerated, with the most frequently reported drug-related adverse events being nausea, taste perversion, and headache."( Efficacy and safety of a 10-day course of 400 or 600 milligrams of grepafloxacin once daily for treatment of acute bacterial exacerbations of chronic bronchitis: comparison with a 10-day course of 500 milligrams of ciprofloxacin twice daily.
Breisch, S; Chodosh, S; Lakshminarayan, S; Swarz, H, 1998
)
0.3
" The most common adverse events observed for the 400 mg and 600 mg treatments during these studies were gastrointestinal reactions, such as nausea (11% and 15%, respectively), vomiting (1% and 6%) and diarrhoea (3% and 4%)."( Safety profile of grepafloxacin compared with other fluoroquinolones.
Schwabe, R; Stahlmann, R, 1997
)
0.3
" Safety and tolerability were assessed by evaluation of vital signs, electrocardiograms, electroencephalograms, clinical chemistry parameters, results of urinalysis, and adverse events."( Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects.
Dalhoff, A; Kubitza, D; Schühly, U; Stass, H, 1998
)
0.3
"In this study, the anticonvulsant and adverse effects of compounds that belong to four different categories of systemically available N-methyl-D-aspartate (NMDA) receptor ligands were compared, namely the competitive antagonist CGP 40116, the noncompetitive antagonist MK-801 (dizocilpine), the glycineB receptor antagonist L-701,324, and the glycineB receptor high-efficacy partial agonist D-cycloserine."( Anti-convulsant and adverse effects of the glycineB receptor ligands, D-cycloserine and L-701,324: comparison with competitive and non-competitive N-methyl-D-aspartate receptor antagonists.
Wlaź, P, 1998
)
0.3
" In conclusion, DW-116 was safe in this study, the first administration to human subjects."( Safety, tolerability and pharmacokinetics of the new long-acting quinolone DW-116 after single and multiple dosing in healthy subjects.
Choi, MS; Chung, YH; Dilger, C; Lee, CW; Lee, DK; Meyerhoff, C; Pabst, G; Reh, C; Ryu, JM; Yoon, SJ, 1998
)
0.3
" The most common adverse events with grepafloxacin 400 or 600 mg were gastrointestinal, such as nausea, vomiting, and diarrhea."( Grepafloxacin: a review of its safety profile based on clinical trials and postmarketing surveillance.
Elies, W; Lode, H; Vogel, F, 1999
)
0.3
"1%) of 1331 receiving a comparator regimen experienced at least 1 adverse event considered to be related to the study medication."( Safety profile of sparfloxacin, a new fluoroquinolone antibiotic.
Dorr, MB; Lipsky, BA; Magner, DJ; Talbot, GH, 1999
)
0.3
"Today's lifestyle is often associated with frequent exposure to sunlight, but some xenobiotics used in drugs, cosmetics or food chemicals can produce adverse biological effects when irradiated."( Fluoroquinolones as chemical tools to define a strategy for photogenotoxicity in vitro assessment.
Agapakis-Causse, C; Belaidi, JP; Chaubo, C; Marrot, L; Meunier, JR; Perez, P, 2001
)
0.31
" Since that review, some new knowledge allows us to better predict that some structural moieties are more likely than others to form drug reactive metabolites that may be involved in causing toxic effects in humans."( Structure toxicity relationships--how useful are they in predicting toxicities of new drugs?
Nelson, SD, 2001
)
0.31
"Aripiprazole, effective against positive and negative symptoms, is a safe and well-tolerated potential treatment for schizophrenia and schizoaffective disorder."( Efficacy and safety of aripiprazole and haloperidol versus placebo in patients with schizophrenia and schizoaffective disorder.
Ali, MW; Carson, WH; Ingenito, GG; Kane, JM; McQuade, RD; Saha, AR; Zimbroff, DL, 2002
)
0.31
" This includes general adverse events, a low incidence of reported weight gain and a low liability for inducing movement disorders."( Aripiprazole: profile on efficacy and safety.
Goodnick, PJ; Jerry, JM, 2002
)
0.31
" Another manifestation of toxic effects of quinolones on connective tissue structures are tendopathies."( Children as a special population at risk--quinolones as an example for xenobiotics exhibiting skeletal toxicity.
Stahlmann, R, 2003
)
0.32
" The present study was conducted to better understand the teratogenic effects of DW-116 at several developmental toxic doses in rats."( Developmental toxicity evaluation of the new fluoroquinolone antibacterial DW-116 in rats.
Ahn, TH; Chung, MK; Jang, BS; Kang, SS; Kim, CY; Kim, JC; Kim, SH; Shin, DH, 2003
)
0.32
" There were no adverse effects on body weight, food and water consumption, ophthalmoscopy, urinalysis, necropsy findings and histopathology in any treatment group."( 26-Week repeated oral dose toxicity study of the new quinolone antibacterial DW-116 in Sprague-Dawley rats.
Ahn, TH; Chung, MK; Ha, CS; Han, J; Kang, SS; Kim, CY; Kim, JC; Shin, DH; Song, SW, 2003
)
0.32
" Safety assessments included adverse event (AE) reports, EPS scales, ECGs, weight, and prolactin, glucose and cholesterol levels."( Aripiprazole in the treatment of schizophrenia: safety and tolerability in short-term, placebo-controlled trials.
Ali, M; Iwamoto, T; Kaplita, S; Marcus, R; Marder, SR; McQuade, RD; Safferman, AZ; Saha, A; Stock, E, 2003
)
0.32
" The cytotoxicity of tested compounds indicated that compound 1a was the less toxic compound (IC50 > 62."( Antituberculosis agents IV: in vitro antimycobacterial activity and cytotoxicity of N-piperazinyl quinolone derivatives containing 2-thienyl and 2-furyl moiety.
Foroumadi, A; Mirzaei, M; Soltani, F, 2003
)
0.32
" Concentrations between 50 and 5000 microgl(-1) induced both toxic effect and hormesis in plants, by significantly modifying both length of primary root, hypocotyl, cotyledons and the number/length of leaves."( Phytotoxicity to and uptake of enrofloxacin in crop plants.
Cozzolino, S; Fiori, M; Migliore, L, 2003
)
0.32
" Discontinuations due to adverse events did not differ significantly between the aripiprazole and placebo groups."( A placebo-controlled, double-blind study of the efficacy and safety of aripiprazole in patients with acute bipolar mania.
Ali, M; Ingenito, G; Keck, PE; Liebeskind, A; Marcus, R; Saha, A; Tourkodimitris, S, 2003
)
0.32
"Aripiprazole had significantly greater efficacy than placebo for the treatment of bipolar disorder patients in acute manic or mixed episodes and was safe and well tolerated in this randomized controlled trial."( A placebo-controlled, double-blind study of the efficacy and safety of aripiprazole in patients with acute bipolar mania.
Ali, M; Ingenito, G; Keck, PE; Liebeskind, A; Marcus, R; Saha, A; Tourkodimitris, S, 2003
)
0.32
" Time to discontinuation due to adverse events or lack of efficacy was significantly greater with aripiprazole than with haloperidol (p=0."( Efficacy and safety of aripiprazole vs. haloperidol for long-term maintenance treatment following acute relapse of schizophrenia.
Ali, M; Archibald, D; Carson, WH; Ingenito, G; Kasper, S; Lerman, MN; Marcus, R; McQuade, RD; Pigott, T; Saha, A, 2003
)
0.32
" Adverse events were generally mild to moderate, were transient in nature, and commonly occurred within the first 3 days of dosing."( Pharmacokinetics, tolerability, and safety of aripiprazole following multiple oral dosing in normal healthy volunteers.
Bramer, SL; Mallikaarjun, S; Salazar, DE, 2004
)
0.32
" The aim of this study is to determine the potential adverse effects of this chemical on pregnancy, delivery and lactation of dams and on peri- and postnatal development of F1 offspring."( Peri- and postnatal developmental toxicity of the fluoroquinolone antibacterial DW-116 in rats.
Chung, MK; Jung, YH; Kim, JC; Kim, SH; Kwon, HJ; Oh, KS; Shin, DH; Shin, HC; Yun, HI, 2004
)
0.32
"This article reviews the precautions and adverse effects associated with vesnarinone use, and the potential mechanisms responsible for these complications as well as suggested treatment strategies."( Precautions for use and adverse effects of vesnarinone: potential mechanisms and future therapies.
Bertolet, BD, 2004
)
0.32
"To develop the safe formulation that can safely improve bioavailability of poorly absorbable drugs and that is practically available, we prepared the suppositories of rebamipide, a poorly soluble and poorly absorbable antiulcer drug, by employing the combinatorial use of sodium laurate (C12), an absorption enhancer, with taurine (Tau) or L-glutamine (L-Gln), an adjuvant exerting the cytoprotective action."( Development of suppository formulation safely improving rectal absorption of rebamipide, a poorly absorbable drug, by utilizing sodium laurate and taurine.
Higaki, K; Kamada, N; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2004
)
0.32
"Five new antipsychotic drugs introduced in the United States in the last decade offer physicians the ability to treat patients with schizophrenia and bipolar mania without the adverse effects of the first-generation antipsychotics."( The promise of atypical antipsychotics: fewer side effects mean enhanced compliance and improved functioning.
Citrome, L; Volavka, J, 2004
)
0.32
" There were no adverse effects on either pregnant dams or embryo-foetal development at 19."( Developmental toxicity assessment of the new fluoroquinolone antibacterial DW-116 in rabbits.
Bae, CS; Chung, MK; Kim, JC; Kim, JH; Kim, SH; Lim, JH; Oh, KS; Shin, DH; Yun, HI,
)
0.13
" However, there are still significant adverse effects and toxicities with this class of medications."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
"Continued research to evaluate adverse effects and tolerability of atypical antipsychotics compared with first-generation antipsychotics and each other is reviewed."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
"While new atypical antipsychotic medications may have a safer therapeutic and overdose profile than first-generation antipsychotic medications, many adverse and toxic effects still need to be considered in therapeutic monitoring and overdose management."( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer?
Dubois, D, 2005
)
0.33
" Several clinical trials have not shown efficacy, and there have been concerns about adverse events."( Efficacy and adverse effects of atypical antipsychotics for dementia: meta-analysis of randomized, placebo-controlled trials.
Dagerman, K; Insel, PS; Schneider, LS, 2006
)
0.33
" Clinical and trials characteristics, outcomes, and adverse events were extracted."( Efficacy and adverse effects of atypical antipsychotics for dementia: meta-analysis of randomized, placebo-controlled trials.
Dagerman, K; Insel, PS; Schneider, LS, 2006
)
0.33
" Adverse events were mainly somnolence and urinary tract infection or incontinence across drugs, and extrapyramidal symptoms or abnormal gait with risperidone or olanzapine."( Efficacy and adverse effects of atypical antipsychotics for dementia: meta-analysis of randomized, placebo-controlled trials.
Dagerman, K; Insel, PS; Schneider, LS, 2006
)
0.33
" Dropouts and adverse events further limit effectiveness."( Efficacy and adverse effects of atypical antipsychotics for dementia: meta-analysis of randomized, placebo-controlled trials.
Dagerman, K; Insel, PS; Schneider, LS, 2006
)
0.33
" Assessments included monitoring of adverse events (AEs), blood chemistry (including serum potassium and blood glucose), vital signs (blood pressure and heart rate), electrocardiograms and spirometry."( Safety, tolerability and efficacy of indacaterol, a novel once-daily beta(2)-agonist, in patients with COPD: a 28-day randomised, placebo controlled clinical trial.
Bao, W; Beier, J; Chanez, P; Higgins, M; Jack, D; Martinot, JB; Schreurs, AJ; Tkácová, R, 2007
)
0.34
" Extrapyramidal symptoms (EPS), weight gain, serum prolactin level, QTc interval, and self-reported adverse events were assessed as measures of safety and tolerability."( Efficacy and safety of aripiprazole in the acute treatment of schizophrenia in Chinese patients with risperidone as an active control: a randomized trial.
Chan, HY; Chiang, SC; Hwang, TJ; Hwu, HG; Lin, SK; Lin, WW; Su, TP, 2007
)
0.34
" No patient discontinued the study because of treatment-emergent adverse events."( Efficacy and safety of intramuscular aripiprazole in patients with acute agitation: a randomized, double-blind, placebo-controlled trial.
Auby, P; Marcus, RN; McQuade, RD; Oren, DA; Sack, DA; Tran-Johnson, TK, 2007
)
0.34
" Extrapyramidal symptom-related adverse events were lower for aripiprazole (1."( Efficacy and safety of oral aripiprazole compared with haloperidol in patients transitioning from acute treatment with intramuscular formulations.
Allen, MH; Crandall, DT; Currier, GW; Daniel, DG; Manos, G; McQuade, R; Oren, D; Pikalov, AA; Zimbroff, DL, 2007
)
0.34
"Acutely agitated patients with schizophrenia or schizoaffective disorder treated with aripiprazole IM or haloperidol IM demonstrated similar effective and safe transition to their respective oral formulations."( Efficacy and safety of oral aripiprazole compared with haloperidol in patients transitioning from acute treatment with intramuscular formulations.
Allen, MH; Crandall, DT; Currier, GW; Daniel, DG; Manos, G; McQuade, R; Oren, D; Pikalov, AA; Zimbroff, DL, 2007
)
0.34
" Adverse events (AEs) that occurred in > or = 10% of patients with adjunctive placebo or adjunctive aripiprazole were akathisia (4."( The efficacy and safety of aripiprazole as adjunctive therapy in major depressive disorder: a multicenter, randomized, double-blind, placebo-controlled study.
Berman, RM; Carson, WH; Corey-Lisle, PK; Khan, A; Marcus, RN; McQuade, RD; Swanink, R, 2007
)
0.34
" Adverse events (AEs), laboratory assessments, vital signs, electrocardiograms, spirometry and physical examinations were monitored."( Safety and tolerability of indacaterol in asthma: a randomized, placebo-controlled 28-day study.
Bao, W; Cameron, R; Chuchalin, AG; Dahl, R; Higgins, M; Krug, N; Luursema, PB; Richter, K; Tsoi, AN; van As, A; Woessner, R, 2007
)
0.34
" The treatment-emergent adverse events reported in >or=5% of patients aged 18-40 years receiving aripiprazole were similar to those reported for the overall population."( Efficacy and safety of aripiprazole in subpopulations with acute manic or mixed episodes of bipolar I disorder.
Carlson, B; Eudicone, J; McQuade, R; Pikalov, A; Suppes, T, 2008
)
0.35
" Few adverse events were reported; all were mild or moderate in severity."( Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma.
Barbier, M; Brookman, LJ; Elharrar, B; Fuhr, R; Knowles, LJ; Pascoe, S, 2007
)
0.34
" The sustained bronchodilation of indacaterol 1000 microg was not associated with sustained systemic adverse effects."( Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma.
Barbier, M; Brookman, LJ; Elharrar, B; Fuhr, R; Knowles, LJ; Pascoe, S, 2007
)
0.34
" Treatment-emergent adverse events occurring during the pivotal trials revealed statistically significant NNH versus placebo (or placebo equivalent) for aripiprazole for headache (NNH = 20, 95% CI = 11 to 170) and nausea (NNH = 17, 95% CI = 11 to 38), for ziprasidone in the treatment of headache (NNH = 15, 95% CI = 8 to 703), and for olanzapine in treatment-emergent hypotension (NNH = 50, 95% CI = 30 to 154)."( Comparison of intramuscular ziprasidone, olanzapine, or aripiprazole for agitation: a quantitative review of efficacy and safety.
Citrome, L, 2007
)
0.34
" Adverse effects and their impact on treatment course were also evaluated."( Aripiprazole: effectiveness and safety under naturalistic conditions.
Amoretti, A; Di Lorenzo, R; Fiorini, F; Forghieri, M; Genedani, S; Rigatelli, M, 2007
)
0.34
"7%) and treatment-related adverse events (82."( A randomized, multicenter, double-blind, placebo-controlled study of the efficacy and safety of aripiprazole for the treatment of alcohol dependence.
Anton, RF; Breder, C; Carson, WH; Han, J; Kranzler, H; Marcus, RN, 2008
)
0.35
" Indacaterol was well tolerated: the incidence of adverse events (AEs) was similar between the active and placebo groups, and AEs, when they occurred, were mild or moderate for most (98."( Tolerability of indacaterol, a novel once-daily beta2-agonist, in patients with asthma: a randomized, placebo-controlled, 28-day safety study.
Beier, J; Cameron, R; Higgins, M; Magula, D; Martinot, JB; Owen, R; Pohunek, P; Yang, WH, 2007
)
0.34
" Adverse events occurring in 10% of patients or more with adjunctive placebo or aripiprazole were akathisia (4."( The efficacy and safety of aripiprazole as adjunctive therapy in major depressive disorder: a second multicenter, randomized, double-blind, placebo-controlled study.
Berman, RM; Carson, WH; Fava, M; Hennicken, D; Marcus, RN; McQuade, RD; Simon, JS; Thase, ME; Trivedi, MH, 2008
)
0.35
" Aripiprazole is a second-generation antipsychotic that seems to have a favorable side-effect profile."( The safety of the electroconvulsive therapy-aripiprazole combination: four case reports.
Karakatsanis, NA; Karapoulios, E; Kouzoupis, AV; Masdrakis, VG; Oulis, P; Soldatos, CR; Zervas, IM, 2008
)
0.35
" Combined application of clozapine and aripiprazole is in accordance with a neurobiological rationale and appears to be a safe and well tolerated."( Adjunctive aripiprazole decreased metabolic side effects of clozapine treatment.
Libiger, J; Masopust, J; Tůma, I, 2008
)
0.35
"Aripiprazole (15 mg/day) is safe and tolerable when combined with cocaine; however, the usefulness of aripiprazole as a treatment for cocaine-use disorders remains to be determined."( The safety, tolerability, and subject-rated effects of acute intranasal cocaine administration during aripiprazole maintenance II: increased aripipirazole dose and maintenance period.
Hays, LR; Lile, JA; Rush, CR; Stoops, WW, 2008
)
0.35
"Dopamine receptor antagonists are commonly used to counter the adverse effects of opioids such as hallucinations, delusions and emesis."( Suppression of dopamine-related side effects of morphine by aripiprazole, a dopamine system stabilizer.
Amano, T; Asato, M; Hashimoto, K; Ikegami, D; Kuzumaki, N; Matsushima, Y; Nakamura, A; Narita, M; Niikura, K; Shiokawa, M; Suzuki, T; Takagi, S; Takei, D; Tsurukawa, Y, 2008
)
0.35
" No difference in the incidence of adverse events was seen between the two groups, confirming the safety of rebamipide."( Efficacy and safety of rebamipide for the treatment of dry mouth symptoms in patients with Sjögren's syndrome: a double-blind placebo-controlled multicenter trial.
Kawakami, A; Koni, I; Nishinarita, M; Nishiyama, S; Ohta, S; Oka, H; Sawada, S; Sugai, S; Sugiyama, E; Takahashi, H; Takei, M; Umehara, H; Yamaji, K, 2009
)
0.35
" Tolerability and safety were assessed by monitoring the frequency and severity of treatment-emergent adverse events, extrapyramidal symptoms (EPS), vital signs, weight, and laboratory tests."( Long-term efficacy and safety of aripiprazole in patients with schizophrenia, schizophreniform disorder, or schizoaffective disorder: 26-week prospective study.
Cho, SJ; Jang, JH; Kang, DH; Kim, YK; Kwon, JS; Yoo, SY, 2009
)
0.35
"Completion rates were between 84% and 90% and comparable across all subgroups, with low discontinuations due to adverse events."( Adjunctive aripiprazole in major depressive disorder: analysis of efficacy and safety in patients with anxious and atypical features.
Berman, RM; Carlson, BX; Fava, M; Marcus, RN; Nelson, CJ; Pikalov, A; Qi, Y; Thase, ME; Tran, QV; Trivedi, MH; Yang, H, 2008
)
0.35
" Safety and tolerability evaluations included incidence of treatment-emergent adverse events and extrapyramidal symptom assessments (SAS, BARS, and AIMS), and metabolic profile changes including weight and BMI."( The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials.
Assunção-Talbott, S; Eudicone, JM; Glick, ID; Mankoski, R; Marcus, RN; Tran, QV, 2009
)
0.35
"Aripiprazole was generally well tolerated, with agitation/activation the most common side effect reported in elderly inpatients."( Aripiprazole prescribing patterns and side effects in elderly psychiatric inpatients.
Coley, KC; Fabian, TJ; Lenze, EJ; Ruby, C; Scipio, TM, 2009
)
0.35
" These results demonstrate that in both photocatalytic processes studied, toxicity decreases significantly, producing a phototreated sample within safe toxicity limits."( Solar photocatalytic treatment of quinolones: intermediates and toxicity evaluation.
Agüera, A; Fernández-Alba, AR; Gernjak, W; Malato, S; Sirtori, C; Zapata, A, 2009
)
0.35
" Primary endpoint was rate of discontinuation due to adverse events (AEs) during the 12-week study."( Switching to aripiprazole in outpatients with schizophrenia experiencing insufficient efficacy and/or safety/tolerability issues with risperidone: a randomized, multicentre, open-label study.
Kahn, JP; Kerselaers, W; Lissens, J; McQuade, RD; Modell, S; Ryckmans, V; Sanchez, R; Werner, C, 2009
)
0.35
" The ultimate aim for this research is to determine whether this combination is safe and is superior to either drug taken alone in reducing alcohol use in alcohol dependent patients."( A safety and tolerability laboratory study of the combination of aripiprazole and topiramate in volunteers who drink alcohol.
Kenna, GA; Leggio, L; Swift, RM, 2009
)
0.35
" Participants reported adverse events (AEs) daily alcohol use and participated in an alcohol challenge session (ACS)."( A safety and tolerability laboratory study of the combination of aripiprazole and topiramate in volunteers who drink alcohol.
Kenna, GA; Leggio, L; Swift, RM, 2009
)
0.35
" No severe or serious adverse events were observed."( Dose escalation study of the safety, tolerability, and pharmacokinetics of nemonoxacin (TG-873870), a novel potent broad-spectrum nonfluorinated quinolone, in healthy volunteers.
Ajayi, F; Aronstein, WS; Chang, LW; Chung, DT; Hsu, CH; Kuzmak, B; Lin, L; Lyon, RA; Tsai, CY, 2010
)
0.36
" Nemonoxacin was generally safe and well tolerated, with no significant changes in the clinical laboratory tests or electrocardiograms."( Multiple-dose safety, tolerability, and pharmacokinetics of oral nemonoxacin (TG-873870) in healthy volunteers.
Chang, LW; Chang, YT; Chen, SJ; Chiu, KM; Chung, DT; Hsu, CH; Hsu, MC; King, CH; Tan, HC; Tsai, CY, 2010
)
0.36
" Most common adverse effects included appetite increase and weight gain in 5 subjects, mild extrapyramidal effects in 7 subjects, and headaches and tiredness/fatigue in 7 subjects; 1 subject experienced akathisia and muscle cramps."( Aripiprazole in children and adolescents with Tourette's disorder: an open-label safety and tolerability study.
Coffey, BJ; Goldman, R; Hirsch, S; Jummani, R; Lyon, GJ; Samar, S; Spirgel, A, 2009
)
0.35
"Aripiprazole appears to be a safe and tolerable treatment in children and adolescents with TD that appears to reduce tics; it should be further investigated as a treatment option in controlled trials."( Aripiprazole in children and adolescents with Tourette's disorder: an open-label safety and tolerability study.
Coffey, BJ; Goldman, R; Hirsch, S; Jummani, R; Lyon, GJ; Samar, S; Spirgel, A, 2009
)
0.35
" Safety was assessed by adverse events (AEs), mean serum potassium and blood glucose, QTc (Fridericia), and vital signs."( Efficacy and safety of indacaterol 150 microg once-daily in COPD: a double-blind, randomised, 12-week study.
Feldman, G; Higgins, M; Jack, D; Kramer, B; Owen, R; Piggott, S; Prasad, N; Siler, T, 2010
)
0.36
" However, the adverse effects induced by quinolones, such as tendon/articular toxicity, central nervous system toxicity, phototoxicity and dysglycemia, have greatly restricted their therapeutic use."( Possible involvement of DEC1 on the adverse effects of quinolone antibiotics.
Ma, W; Shi, X; Wang, Y; Zheng, Y, 2010
)
0.36
" Frequently reported adverse events (AEs) that occurred with ARI + LI vs."( Assessment of safety, tolerability and effectiveness of adjunctive aripiprazole to lithium/valproate in bipolar mania: a 46-week, open-label extension following a 6-week double-blind study.
Baudelet, C; Marcus, RN; McQuade, RD; Owen, R; Sanchez, R; Vieta, E, 2010
)
0.36
"Long-term aripiprazole adjunctive to lithium/valproate in bipolar mania was safe and well tolerated."( Assessment of safety, tolerability and effectiveness of adjunctive aripiprazole to lithium/valproate in bipolar mania: a 46-week, open-label extension following a 6-week double-blind study.
Baudelet, C; Marcus, RN; McQuade, RD; Owen, R; Sanchez, R; Vieta, E, 2010
)
0.36
" The results of the study suggested that indacaterol has a wide therapeutic index and is safe and well tolerated."( [Efficacy and safety of indacaterol - new long-acting beta(2) agonist].
Chazan, R, 2010
)
0.36
" Early onset schizophrenia warrants effective pharmacological treatment that is safe and well tolerated by children and adolescent population."( The use of aripiprazole in early onset schizophrenia: safety and efficacy.
Hamidin, A; Normala, I, 2009
)
0.35
" The microbial species representing wide diversity, generated 11 microbial toxic concentration (MTC) values were obtained giving a unique "toxic fingerprint" profile of the test sample."( Application of microbial assay for risk assessment biotest in evaluation of toxicity of human and veterinary antibiotics.
Adomas, B; Nałecz-Jawecki, G; Piotrowicz-Cieślak, AI; Sawicki, J; Wadhia, K, 2010
)
0.36
" All three treatments were well tolerated, and no drug-related serious adverse events were observed."( Efficacy and safety of nemonoxacin versus levofloxacin for community-acquired pneumonia.
Bester, AJ; Chang, LW; Chang, YT; Chung, DT; Ho, ML; Hsu, MC; Kasumba, J; King, CH; Mitha, IH; Perng, RP; van Rensburg, DJ; Wu, RG, 2010
)
0.36
" Akathisia was the most common adverse event in both the older (17."( Efficacy and safety of adjunctive aripiprazole in major depressive disorder in older patients: a pooled subpopulation analysis.
Andersson, C; Berman, RM; Carlson, BX; Eudicone, JM; Forbes, RA; Nelson, JC; Steffens, DC; Tran, QV; Yang, H, 2011
)
0.37
" Once-daily QVA149 was well tolerated in COPD patients with a cardiovascular safety profile and overall adverse event rates similar to placebo."( Cardiovascular safety of QVA149, a combination of Indacaterol and NVA237, in COPD patients.
Dolker, M; Fabbri, LM; Horton, R; Martin, C; Overend, T; Van de Maele, B, 2010
)
0.36
" Adverse events (AEs) were analysed overall and according to Anti-Platelet Trialists' Collaboration (APTC) criteria and baseline cardiovascular risk factors."( Cardio- and cerebrovascular safety of indacaterol vs formoterol, salmeterol, tiotropium and placebo in COPD.
Chung, KF; Felser, JM; Hu, H; Rueegg, P; Worth, H, 2011
)
0.37
" Most adverse events were mild or moderate, with none considered serious or leading to withdrawal."( Safety, tolerability and pharmacokinetics of single escalating doses of indacaterol, a once-daily beta2-agonist bronchodilator, in subjects with COPD.
Brookman, L; Hmissi, A; Kaiser, G; Pascoe, S; Perry, S; Pleskow, W; Reynolds, C, 2011
)
0.37
"Even at doses far in excess of the therapeutic range, indacaterol had minimal systemic effects; such changes would be considered within safe limits for a single dose."( Safety, tolerability and pharmacokinetics of single escalating doses of indacaterol, a once-daily beta2-agonist bronchodilator, in subjects with COPD.
Brookman, L; Hmissi, A; Kaiser, G; Pascoe, S; Perry, S; Pleskow, W; Reynolds, C, 2011
)
0.37
" Adverse events, mostly mild or moderate, occurred in 76%, 77%, and 68% of subjects receiving indacaterol, 150 μg; indacaterol, 300 μg; and placebo, respectively."( Long-term safety and efficacy of indacaterol, a long-acting β₂-agonist, in subjects with COPD: a randomized, placebo-controlled study.
Chapman, KR; Dogra, A; Kramer, B; Lassen, C; Owen, R; Rennard, SI, 2011
)
0.37
" Safety and tolerability measures included incidences of adverse events, extrapyramidal symptoms, weight, metabolic measures, vital signs, and other clinical assessments."( Safety and tolerability of aripiprazole for irritability in pediatric patients with autistic disorder: a 52-week, open-label, multicenter study.
Carson, WH; Findling, RL; Kamen, L; Mankoski, R; Manos, G; Marcus, RN; McQuade, RD; Owen, R, 2011
)
0.37
" Adverse events were experienced by 286/330 subjects (86."( Safety and tolerability of aripiprazole for irritability in pediatric patients with autistic disorder: a 52-week, open-label, multicenter study.
Carson, WH; Findling, RL; Kamen, L; Mankoski, R; Manos, G; Marcus, RN; McQuade, RD; Owen, R, 2011
)
0.37
"Aripiprazole was generally safe and well tolerated in the long-term treatment of irritability associated with autistic disorder in pediatric subjects."( Safety and tolerability of aripiprazole for irritability in pediatric patients with autistic disorder: a 52-week, open-label, multicenter study.
Carson, WH; Findling, RL; Kamen, L; Mankoski, R; Manos, G; Marcus, RN; McQuade, RD; Owen, R, 2011
)
0.37
" Although they have been known to have various adverse effects, most of the mechanisms remain still unknown."( [Safety profile of antimicrobial agents].
Hori, S, 2011
)
0.37
" Adverse events (mostly mild or moderate) were reported for 52% and 46% of patients receiving indacaterol and placebo, respectively, and serious adverse events for 4% and 5%."( Bronchodilator efficacy and safety of indacaterol 150 μg once daily in patients with COPD: an analysis of pooled data.
Bleecker, ER; Kramer, B; Owen, R; Siler, T, 2011
)
0.37
" Outcomes were adverse events, serious adverse events and deaths, plasma potassium, blood glucose, and QTc interval and vital signs."( Safety of indacaterol in the treatment of patients with COPD.
Donohue, JF; Kornmann, O; Kramer, B; Lassen, C; Lawrence, D; Singh, D, 2011
)
0.37
"The commonest adverse events with indacaterol were COPD worsening, nasopharyngitis, and headache; most cases were mild or moderate and incidence was generally similar to placebo and other active treatments."( Safety of indacaterol in the treatment of patients with COPD.
Donohue, JF; Kornmann, O; Kramer, B; Lassen, C; Lawrence, D; Singh, D, 2011
)
0.37
" Three patients allocated elvitegravir had serious adverse events related to study drugs compared with seven assigned raltegravir; two and eight patients died, respectively."( Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study.
Andrade-Villanueva, J; Cheng, AK; Chuck, SL; Clotet, B; Clumeck, N; Lamarca, A; Liu, YP; Margot, N; Molina, JM; Zhong, L, 2012
)
0.38
" Adverse events for indacaterol (49."( Efficacy and safety of indacaterol 150 and 300 µg in chronic obstructive pulmonary disease patients from six Asian areas including Japan: a 12-week, placebo-controlled study.
Fukuchi, Y; Hang, LW; Hosoe, M; Ichinose, M; Kinoshita, M; Kramer, B; Lee, SH; Okino, N; Prasad, N, 2012
)
0.38
" The Systematic Assessment of Treatment Emergent Events-General Inquiry was used to assess adverse effects."( The effectiveness and safety of adjunctive aripiprazole in Taiwanese patients with antidepressant-refractory major depressive disorder: a prospective, open-label trial.
Chen, SJ; Chen, ST; Hsiao, YL; Shen, TW, 2012
)
0.38
" Patients with RFP-associated adverse effects were subdivided into RFP-maintenance (RFP-M; n = 18) and QNL-conversion (QNL-C; n = 8) groups."( Safety and efficacy of a quinolone-based regimen for treatment of tuberculosis in renal transplant recipients.
Chang, YK; Choi, BS; Chung, HW; Hwang, HS; Jeon, YJ; Kim, SY; Kim, YS; Lee, SJ; Park, CW; Shin, SJ; Yang, CW; Yoon, HE, 2012
)
0.38
"A QNL-based regimen may be safe and effective for treatment of tuberculosis and may lower the risk of graft failure in renal transplant recipients."( Safety and efficacy of a quinolone-based regimen for treatment of tuberculosis in renal transplant recipients.
Chang, YK; Choi, BS; Chung, HW; Hwang, HS; Jeon, YJ; Kim, SY; Kim, YS; Lee, SJ; Park, CW; Shin, SJ; Yang, CW; Yoon, HE, 2012
)
0.38
" The most common adverse events (> 15% of patients; aripiprazole vs."( A placebo-controlled, double-blind study of the efficacy and safety of aripiprazole for the treatment of acute manic or mixed episodes in Asian patients with bipolar I disorder (the AMAZE study).
Ishigooka, J; Kanba, S; Kawasaki, H; Kinoshita, T; Kuroki, T; Sakamoto, K, 2014
)
0.4
" Treatment was generally safe and well tolerated."( A placebo-controlled, double-blind study of the efficacy and safety of aripiprazole for the treatment of acute manic or mixed episodes in Asian patients with bipolar I disorder (the AMAZE study).
Ishigooka, J; Kanba, S; Kawasaki, H; Kinoshita, T; Kuroki, T; Sakamoto, K, 2014
)
0.4
"No severe or serious adverse events (AEs) occurred in this study, and no clinically significant abnormalities were noted in the vital signs or on physical examination."( Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses.
Cao, G; Guo, B; Shi, Y; Wu, X; Yu, J; Zhang, J; Zhang, Y, 2012
)
0.38
"Primary metabolic markers (body mass index, blood pressure, fasting blood glucose, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and triglycerides), percentage of patients who stay on the randomly assigned atypical antipsychotic for at least 6 months, psychopathology, percentage of patients who develop metabolic syndrome, and percentage of patients who develop serious and nonserious adverse events."( Comparison of longer-term safety and effectiveness of 4 atypical antipsychotics in patients over age 40: a trial using equipoise-stratified randomization.
Arndt, S; Glorioso, DK; Golshan, S; Henry, R; Jeste, DV; Jin, H; Kraemer, HC; Mudaliar, S; Shih, PA, 2013
)
0.39
"Because of a high incidence of serious adverse events, quetiapine was discontinued midway through the trial."( Comparison of longer-term safety and effectiveness of 4 atypical antipsychotics in patients over age 40: a trial using equipoise-stratified randomization.
Arndt, S; Glorioso, DK; Golshan, S; Henry, R; Jeste, DV; Jin, H; Kraemer, HC; Mudaliar, S; Shih, PA, 2013
)
0.39
" We summarized data relating to exacerbations and adverse events, particularly events related to COPD."( The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary disease.
Decramer, ML; Hanania, NA; Lötvall, JO; Yawn, BP, 2013
)
0.39
"From 20 studies examined (8774 LABA-treated patients), there was no evidence of an association between LABA treatment and increased exacerbations, COPD-related adverse events, or deaths."( The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary disease.
Decramer, ML; Hanania, NA; Lötvall, JO; Yawn, BP, 2013
)
0.39
" Double-blind, randomized, controlled trials investigating the metabolic adverse effects (weight gain, lipid, glucose, and prolactin level abnormalities) associated with atypical antipsychotic use in children and adolescents aged ≤ 18 years were included, irrespective of whether the investigation of adverse effects was a primary or secondary endpoint."( Weight gain and other metabolic adverse effects associated with atypical antipsychotic treatment of children and adolescents: a systematic review and meta-analysis.
Aitchison, KJ; Almandil, NB; Besag, FM; Liu, Y; Murray, ML; Wong, IC, 2013
)
0.39
" However, data on the long-term exposure to these therapeutic options are needed, and a handful of case reports are emerging, reporting rare but potentially life-threatening adverse hepatic events in patients with hepatitis co-infection or taking other hepatotoxic drugs."( Hepatoxicity of new antiretrovirals: a systematic review.
Lacombe, K; Surgers, L, 2013
)
0.39
" Systemic pharmacodynamics (potassium, heart rate, glucose and QTc), adverse events and systemic pharmacokinetics were also assessed."( Bronchodilation and safety of supratherapeutic doses of salbutamol or ipratropium bromide added to single dose GSK961081 in patients with moderate to severe COPD.
Ambery, C; Norris, V, 2013
)
0.39
" The incidence of adverse events was similar in the two groups."( Efficacy and safety of ivacaftor in patients aged 6 to 11 years with cystic fibrosis with a G551D mutation.
Ahrens, R; Canny, GJ; Chilvers, MA; Davies, JC; Howenstine, MS; Li, H; Mainz, JG; Munck, A; Ordoñez, CL; Rodriguez, S; Wainwright, CE; Yen, K, 2013
)
0.39
" Safety was assessed across study phases by the time of first onset of adverse events, as were objective measures of extrapyramidal symptoms, fasting metabolic parameters, and body weight."( Long-term safety and tolerability of aripiprazole once-monthly in maintenance treatment of patients with schizophrenia.
Baker, RA; Carson, W; Fleischhacker, WW; Forbes, RA; Jin, N; Johnson, B; Kane, JM; McQuade, R; Sanchez, R, 2013
)
0.39
"5%) in the SOC group discontinued due to adverse events (physician and subject decision combined, P = ."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39
"These data provide further evidence that the potential antipsychotic LY2140023 monohydrate, with a glutamatergic mechanism of action, may have a unique tolerability profile characterized by a low association with some adverse events such as extrapyramidal symptoms and weight gain that may characterize currently available dopaminergic antipsychotics."( A long-term, phase 2, multicenter, randomized, open-label, comparative safety study of pomaglumetad methionil (LY2140023 monohydrate) versus atypical antipsychotic standard of care in patients with schizophrenia.
Adams, DH; Baygani, S; Kinon, BJ; Kollack-Walker, S; Millen, BA; Velona, I; Walling, DP, 2013
)
0.39
" Adverse events were assessed."( A head-to-head comparison of aripiprazole and risperidone for safety and treating autistic disorders, a randomized double blind clinical trial.
Berk, M; Ghanizadeh, A; Sahraeizadeh, A, 2014
)
0.4
" Adverse events were similar irrespective of prior atypical antipsychotic and duration of oral antipsychotic overlap, suggesting that patients can be safely switched from their existing oral antipsychotic to aripiprazole once monthly without requiring an intermediate stabilization phase with oral aripiprazole."( Safety and tolerability of once monthly aripiprazole treatment initiation in adults with schizophrenia stabilized on selected atypical oral antipsychotics other than aripiprazole.
Baker, RA; Bricmont, P; Eramo, A; Kasper, W; Mallikaarjun, S; McQuade, R; Peters-Strickland, T; Potkin, SG; Raoufinia, A; Sanchez, R, 2013
)
0.39
" Primary endpoint was safety and tolerability for treatment-emergent adverse events (AEs)."( Safety and efficacy of dual bronchodilation with QVA149 in COPD patients: the ENLIGHTEN study.
Alagappan, VK; Banerji, D; Chapman, KR; Chen, H; Dahl, R; Kho, P; Mehta, R; Rudolf, M, 2013
)
0.39
" The most common treatment-emergent adverse events were vomiting (13."( Pharmacokinetics, tolerability and safety of aripiprazole once-monthly in adult schizophrenia: an open-label, parallel-arm, multiple-dose study.
Bricmont, P; Carson, W; Fleischhacker, WW; Forbes, RA; Kane, JM; Mallikaarjun, S; McQuade, R; Sanchez, R, 2013
)
0.39
" Subjects were stratified by PAE; adverse events (AEs), and changes in weight, and metabolic measures were evaluated."( Aripiprazole treatment of irritability associated with autistic disorder and the relationship between prior antipsychotic exposure, adverse events, and weight change.
Forbes, RA; Mankoski, R; Manos, G; Marcus, R; Marler, S; McQuade, R; Stockton, G, 2013
)
0.39
"2% in the IND+GLY group experienced an adverse event, with the majority being mild-to-moderate in severity."( Efficacy and safety of QVA149 compared to the concurrent administration of its monocomponents indacaterol and glycopyrronium: the BEACON study.
Alagappan, VK; Banerji, D; Chen, H; Dahl, R; Jadayel, D, 2013
)
0.39
" Overall incidence of adverse events (including COPD exacerbations) was 55·4% (143 of 258) for the QVA149 group and 60·2% (159 of 264) for the SFC group."( Efficacy and safety of once-daily QVA149 compared with twice-daily salmeterol-fluticasone in patients with chronic obstructive pulmonary disease (ILLUMINATE): a randomised, double-blind, parallel group study.
Alagappan, VK; Banerji, D; Bateman, ED; Chen, H; D'Andrea, P; Pallante, J; Vogelmeier, CF, 2013
)
0.39
"The purpose of this project was to provide evidence-based guidance concerning when and how it is appropriate to undertake elective changes in antipsychotic medications in order to reduce adverse effects, with a focus on those adverse effects associated with increased long-term health risks."( Switching antipsychotic medications to reduce adverse event burden in schizophrenia: establishing evidence-based practice.
Buchanan, RW; Newcomer, JW; Weiden, PJ, 2013
)
0.39
"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 most common adverse events during phase 1 were weight increase (25."( A randomized controlled trial investigating the safety and efficacy of aripiprazole in the long-term maintenance treatment of pediatric patients with irritability associated with autistic disorder.
Amatniek, J; Eudicone, JM; Findling, RL; Lears, K; Mankoski, R; Marcus, RN; McCartney, T; McQuade, RD; Sheehan, JJ; Timko, K, 2014
)
0.4
" The treatment-emergent adverse event (AE) incidences were comparable between the groups; all study drug-related AEs were mild."( Pharmacokinetics and safety of boosted elvitegravir in subjects with hepatic impairment.
Custodio, JM; Kearney, BP; Ling, KH; Ramanathan, S; Rhee, M; Shen, G, 2014
)
0.4
" Primary outcomes were trough FEV1, severe adverse events, and serious cardiovascular events."( Efficacy and safety of a fixed-dose combination of indacaterol and Glycopyrronium for the treatment of COPD: a systematic review.
Plaza, V; Rodrigo, GJ, 2014
)
0.4
" There were no deaths or serious adverse events."( Effect of dual bronchodilation with QVA149 on cardiac safety in healthy volunteers.
Brown, M; Drollmann, A; Febbraro, S; Hara, H; Jones, I; Perry, S; Sechaud, R, 2014
)
0.4
" The incidence of adverse events was similar for the two treatment groups."( Efficacy and safety of coadministration of once-daily indacaterol and glycopyrronium versus indacaterol alone in COPD patients: the GLOW6 study.
Aumann, J; Chen, H; Goyal, P; Henley, M; McBryan, D; Vincken, W, 2014
)
0.4
" Adverse events were assessed within each subgroup."( Effect of symptom severity on efficacy and safety of aripiprazole adjunctive to antidepressant monotherapy in major depressive disorder: a pooled analysis.
Berman, RM; Hatch, A; Largay, K; Marler, SV; Nelson, JC; Sheehan, JJ; Stewart, TD, 2014
)
0.4
" Common treatment-emergent adverse events included akathisia and restlessness."( Effect of symptom severity on efficacy and safety of aripiprazole adjunctive to antidepressant monotherapy in major depressive disorder: a pooled analysis.
Berman, RM; Hatch, A; Largay, K; Marler, SV; Nelson, JC; Sheehan, JJ; Stewart, TD, 2014
)
0.4
" No serious adverse events were observed in either group."( Efficacy and safety of proton pump inhibitors (PPIs) plus rebamipide for endoscopic submucosal dissection-induced ulcers: a meta-analysis.
Cao, Z; Dong, W; Guo, X; Liu, M; Song, J; Wang, J; Ye, C; Yu, S; Zhang, J, 2014
)
0.4
" The expression of lgaqnr in Escherichia coli reduced the susceptibility to quinolones, producing an adverse effect."( Lactococcus garvieae carries a chromosomally encoded pentapeptide repeat protein that confers reduced susceptibility to quinolones in Escherichia coli producing a cytotoxic effect.
Blanco, MM; Cutuli, MT; Díaz de Alba, P; Gibello, A; Machuca, J; Rodríguez-Martínez, JM, 2014
)
0.4
" Safety and tolerability assessments included adverse event reporting, pulse and blood pressure monitoring, 12-lead electrocardiograms, laboratory tests, and physical examination."( First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of abediterol (LAS100977), a novel long-acting Β2 -agonist.
de Miquel, G; Jimenez, E; Massana, E; Ruiz, S; Seoane, B; Timmer, W, 2014
)
0.4
" Extrapyramidal symptoms (EPS), weight gain, serum prolactin level, QTc interval, and self-reported adverse events were also assessed as measures of safety and tolerability."( Efficacy and safety of aripiprazole in Chinese Han schizophrenia subjects: a randomized, double-blind, active parallel-controlled, multicenter clinical trial.
Gu, N; Kane, JM; Li, H; Luo, J; Wang, C; Wang, X; Xie, S; Xu, X; Yu, W, 2014
)
0.4
" 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
" Drug-related adverse events (AEs) were mild, transient, and confined to local irritation at the injection site."( Safety, tolerability, and pharmacokinetics of intravenous nemonoxacin in healthy chinese volunteers.
Cao, GY; Chen, YC; Guo, BN; Shi, YG; Wu, JF; Wu, XJ; Yu, JC; Zhang, J; Zhang, YY, 2014
)
0.4
" No serious adverse events were observed in any of the patients in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" Serious adverse events were not observed in either group."( Efficacy and safety of 1-week Helicobacter pylori eradication therapy and 7-week rebamipide treatment after endoscopic submucosal dissection of early gastric cancer in comparison with 8-week PPI standard treatment: a randomized, controlled, prospective, m
Azuma, T; Higuchi, K; Iguchi, M; Machida, H; Morita, Y; Naito, Y; Takeuchi, T; Takeuchi, Y; Tamada, T; Tominaga, K; Uedo, N; Yagi, N; Yamao, J; Yazumi, S, 2015
)
0.42
" Overall hazard ratio (HR) was assessed between the active treatments and placebo and in various subgroups related to severity of airways obstruction, inhaled corticosteroid use, cardiovascular risk factors, sex, age and body mass index for death, serious cases of cardio- and cerebrovascular (CCV) events, major adverse cardiovascular events (MACEs), pneumonia, COPD exacerbations requiring hospitalisation or atrial flutter/fibrillation (AF/F)."( Pooled safety analysis of the fixed-dose combination of indacaterol and glycopyrronium (QVA149), its monocomponents, and tiotropium versus placebo in COPD patients.
Banerji, D; Buhl, R; Chen, H; D'Andrea, P; Dahl, R; Fogel, R; Schubert-Tennigkeit, A; Wedzicha, JA, 2014
)
0.4
" The most common treatment-related adverse events were application-site reactions (erythema and pruritus), but the differences in local tolerability between ozenoxacin and placebo were not clinically significant."( Systemic bioavailability, safety and tolerability of topical ozenoxacin in healthy adult volunteers.
Albareda, N; Febbraro, S; Gropper, S; Santos, B, 2014
)
0.4
" Only a few adverse events were reported across repeated-dose studies, and virtually all events were considered to be unrelated or unlikely to be related to ozenoxacin application."( Cumulative irritation, sensitizing potential, phototoxicity and photoallergy of ozenoxacin in healthy adult volunteers.
Cepero, AL; Dosik, JS; Gropper, S; LaStella, P; Siemetzki, H; Wigger-Alberti, W, 2014
)
0.4
" The profile of treatment-emergent adverse events judged as related to abediterol was consistent with that seen after adrenergic stimulation and occurred exclusively in patients who received abediterol 10 μg or 25 μg."( Abediterol (LAS100977), a novel long-acting β2-agonist: efficacy, safety and tolerability in persistent asthma.
Beier, J; de Miquel, G; Fuhr, R; Jiménez, E; Massana, E; Ruiz, S; Seoane, B, 2014
)
0.4
" The most common adverse events were injection site pain in 20 subjects (43."( Relative bioavailability and safety of aripiprazole lauroxil, a novel once-monthly, long-acting injectable atypical antipsychotic, following deltoid and gluteal administration in adult subjects with schizophrenia.
Du, Y; Ehrich, EW; Hard, M; Risinger, R; Turncliff, R, 2014
)
0.4
" The primary objective was to assess the long-term safety profile of ivacaftor as assessed by adverse events, clinical laboratory assessments, electrocardiograms, vital signs, and physical examination; secondary measures included change in forced expiratory volume in one second (FEV1), weight, and pulmonary exacerbations."( Long-term safety and efficacy of ivacaftor in patients with cystic fibrosis who have the Gly551Asp-CFTR mutation: a phase 3, open-label extension study (PERSIST).
Borowitz, D; Davies, JC; Drevinek, P; Gilmartin, G; Griese, M; Jiang, Y; Konstan, MW; McKone, EF; Munck, A; Plant, B; Ratjen, F; Sermet-Gaudelus, I; Wainwright, C, 2014
)
0.4
" Across both trials, 38 (20%) patients had a serious adverse event during the first 48 weeks and 44 (23%) during the subsequent 48 weeks."( Long-term safety and efficacy of ivacaftor in patients with cystic fibrosis who have the Gly551Asp-CFTR mutation: a phase 3, open-label extension study (PERSIST).
Borowitz, D; Davies, JC; Drevinek, P; Gilmartin, G; Griese, M; Jiang, Y; Konstan, MW; McKone, EF; Munck, A; Plant, B; Ratjen, F; Sermet-Gaudelus, I; Wainwright, C, 2014
)
0.4
" Risk assessment for the potential use of a drug, such as aripiprazole (Abilify), should not focus on any particular adverse effect, but rather should consider risk assessment in a broader context."( Atypical antipsychotics are not all alike: side effects and risk assessment.
Howland, RH, 2014
)
0.4
" Nevertheless, accumulating clinical data suggest that they may be safe during pregnancy."( The safety of quinolones in pregnancy.
Akel, H; Chazan, B; Nachum, Z; Romano, S; Salim, R; Yefet, E, 2014
)
0.4
" Indirect forms of quinolone toxicity such as Clostridium difficile infections or adverse reactions associated with drug-drug interactions are also discussed."( Safety issues and drug-drug interactions with commonly used quinolones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
" Although several adverse events have been associated with their use, taking into consideration risk factors, contraindications and potential drug-drug interactions can drastically reduce the respective risks."( Safety issues and drug-drug interactions with commonly used quinolones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
"The reports submitted to the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) from 1997 to 2011 were reviewed to assess serious adverse events induced by the administration of antipsychotics to children."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
" Signals in the data that signified a drug-associated adverse event were detected via quantitative data mining algorithms."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
" Significant signals of the QT prolongation adverse event were detected only for ziprasidone and risperidone."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
"It was suggested that there is a level of diversity in the strength of the association between various first- and second-generation antipsychotics with associated serious adverse events, which possibly lead to fatal outcomes."( Antipsychotics-associated serious adverse events in children: an analysis of the FAERS database.
Brown, JB; Kadoyama, K; Kimura, G; Miki, I; Nakamura, T; Nisiguchi, K; Okuno, Y; Sakaeda, T, 2015
)
0.42
" The incidence of adverse events was comparable between both treatments (QVA149=43."( Efficacy and safety of once-daily QVA149 compared with the free combination of once-daily tiotropium plus twice-daily formoterol in patients with moderate-to-severe COPD (QUANTIFY): a randomised, non-inferiority study.
Buhl, R; Foerster, K; Gessner, C; Hiltl, S; Korn, S; Schuermann, W; Sieder, C, 2015
)
0.42
" The primary endpoint was safety as determined by adverse events."( Effect of ivacaftor in patients with advanced cystic fibrosis and a G551D-CFTR mutation: Safety and efficacy in an expanded access program in the United States.
Gilmartin, G; Niknian, M; Pilewski, JM; Taylor-Cousar, J, 2016
)
0.43
"The rate of serious adverse events was consistent with disease severity."( Effect of ivacaftor in patients with advanced cystic fibrosis and a G551D-CFTR mutation: Safety and efficacy in an expanded access program in the United States.
Gilmartin, G; Niknian, M; Pilewski, JM; Taylor-Cousar, J, 2016
)
0.43
" Brexpiprazole was well tolerated - for schizophrenia, discontinuation rates because of an adverse event (AE) were overall lower for patients receiving brexpiprazole vs."( Brexpiprazole for schizophrenia and as adjunct for major depressive disorder: a systematic review of the efficacy and safety profile for this newly approved antipsychotic - what is the number needed to treat, number needed to harm and likelihood to be hel
Citrome, L, 2015
)
0.42
" Outcomes of interest were progression-free survival, objective response rate (ORR), overall survival, discontinuation of treatment due to adverse events (DAE) and occurrence of specific toxicities."( Efficacy and Safety of Selective Vascular Endothelial Growth Factor Receptor Inhibitors Compared with Sorafenib for Metastatic Renal Cell Carcinoma: a Meta-analysis of Randomised Controlled Trials.
Balar, AV; Bangalore, S; Kang, SK; Ohmann, EL; Volodarskiy, A, 2016
)
0.43
" Most drug-related adverse events were mild and transient, mainly gastrointestinal symptoms such as nausea and vomiting, transient neutropenia, and elevated liver enzymes."( A randomized, double-blind, multicenter Phase II study comparing the efficacy and safety of oral nemonoxacin with oral levofloxacin in the treatment of community-acquired pneumonia.
Cao, Z; Chang, L; Chen, P; Cui, S; Hu, C; Kuang, J; Li, J; Liang, Y; Liu, H; Liu, S; Liu, Y; Lv, X; Lv, Y; Ren, Z; Sun, S; Wang, C; Wang, D; Wang, X; Wu, J; Xiao, Z; Xiu, Q; Yang, H; Zhang, Y; Zhao, L; Zhu, D, 2017
)
0.46
" Common adverse events in part B included cough (in 19 [56%] of 34 patients) and vomiting (in ten [29%])."( Safety, pharmacokinetics, and pharmacodynamics of ivacaftor in patients aged 2-5 years with cystic fibrosis and a CFTR gating mutation (KIWI): an open-label, single-arm study.
Cooke, J; Cunningham, S; Davies, JC; Green, Y; Harris, WT; Lapey, A; Regelmann, WE; Robertson, S; Rosenfeld, M; Sawicki, GS; Southern, KW, 2016
)
0.43
"Ivacaftor at doses of 50 mg and 75 mg seems to be safe in children aged 2-5 years with cystic fibrosis with a gating mutation followed up for 24 weeks, although the frequency of elevated LFTs suggests that monitoring should be frequent in young children, particularly those with a history of elevated LFTs."( Safety, pharmacokinetics, and pharmacodynamics of ivacaftor in patients aged 2-5 years with cystic fibrosis and a CFTR gating mutation (KIWI): an open-label, single-arm study.
Cooke, J; Cunningham, S; Davies, JC; Green, Y; Harris, WT; Lapey, A; Regelmann, WE; Robertson, S; Rosenfeld, M; Sawicki, GS; Southern, KW, 2016
)
0.43
" Ivacaftor and its M1 metabolite may inhibit CYP3A and P-gp; therefore, ivacaftor may increase systemic exposure to drugs which are substrates of CYP3A and/or P-gp, increasing the potential for adverse events."( A safety evaluation of ivacaftor for the treatment of cystic fibrosis.
McColley, SA, 2016
)
0.43
" We aimed to quantify co-administration of MQAB with interacting drugs and associated adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Electrocardiographic (ECG) monitoring and associated adverse events were validated in medical records."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" Forty-four MQAB users had contraindicated co-administrations of simvastatin, atorvastatin, or tizanidine and three of those related adverse drug reactions."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" However, adverse drug reactions were rarely found, and costs vs."( Drug safety of macrolide and quinolone antibiotics in a tertiary care hospital: administration of interacting co-medication and QT prolongation.
Corti, N; Hoppe, L; Kovari, H; Maechler, S; Niedrig, D; Russmann, S, 2016
)
0.43
" In the short-term studies, there were no reports of treatment-emergent adverse events (TEAEs) with an incidence≥5% and twice that of placebo in patients treated with brexpiprazole 2-4mg."( Overview of short- and long-term tolerability and safety of brexpiprazole in patients with schizophrenia.
Correll, CU; Hobart, M; Kane, JM; Ouyang, J; Skuban, A; Weiller, E; Weiss, C, 2016
)
0.43
" There was no statistically significant differences in the risk difference for serious adverse events (5."( An Indirect Comparison of Efficacy and Safety of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate and Abacavir/Lamivudine + Dolutegravir in Initial Therapy.
Behrens, G; Borg, P; Bouee, S; M Llibre, J; Moyle, G; Piontkowsky, D; Raffi, F; Reilly, G; Rogatto, F, 2016
)
0.43
" The primary objective was to assess the safety and tolerability in terms of adverse event (AE) reporting rates over 52 weeks."( Long-term safety of glycopyrrolate: A randomized study in patients with moderate-to-severe COPD (GEM3).
Banerjee, R; D'Andrea, P; Eckert, JH; Gifford, AH; Jessop, N; Mahler, DA; Mota, F; Satti, A, 2016
)
0.43
" The incidence of major adverse cardiovascular events was low and comparable between the groups."( Long-term safety of glycopyrrolate: A randomized study in patients with moderate-to-severe COPD (GEM3).
Banerjee, R; D'Andrea, P; Eckert, JH; Gifford, AH; Jessop, N; Mahler, DA; Mota, F; Satti, A, 2016
)
0.43
" Treatment was generally well tolerated, although the incidence of some respiratory adverse events was higher with lumacaftor/ivacaftor than with placebo in all subgroups."( Efficacy and safety of lumacaftor/ivacaftor combination therapy in patients with cystic fibrosis homozygous for Phe508del CFTR by pulmonary function subgroup: a pooled analysis.
Boyle, MP; Elborn, JS; Huang, X; Konstan, MW; Marigowda, G; Ramsey, BW; Wainwright, CE; Waltz, D, 2016
)
0.43
" The most common grade 3 or higher adverse events were fatigue (19."( Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study.
Ahn, JS; Ahn, MJ; Ahn, S; Cho, BC; Choi, YL; Kim, HR; Kim, JH; Lee, JY; Lee, SH; Lim, SH; Park, K; Sun, JM, 2016
)
0.43
" Abediterol had low systemic exposure; incidence of treatment-emergent adverse events was similar between treatment groups."( Abediterol, a novel long-acting β2-agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD.
Astbury, C; Beier, J; de Miquel, G; Jimenez, E; Massana, E; Pujol, H; Ruiz, S; Seoane, B, 2016
)
0.43
" All doses of abediterol were safe and well tolerated in patients with COPD."( Abediterol, a novel long-acting β2-agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD.
Astbury, C; Beier, J; de Miquel, G; Jimenez, E; Massana, E; Pujol, H; Ruiz, S; Seoane, B, 2016
)
0.43
" The most common treatment-emergent adverse event (TEAE) was injection site pain (35."( [Pharmacokinetics and safety of aripiprazole long-acting injection, following multiple deltoid administrations in schizophrenia patients in Japan].
Ishigooka, J; Nishiyama, K; Noda, T; Shima, T; Tadori, Y; Tamaru, N; Yamasaki, Y, 2016
)
0.43
" During the maintenance phase, the incidence of adverse events was comparable to placebo."( Efficacy and Safety of Brexpiprazole (OPC-34712) as Maintenance Treatment in Adults with Schizophrenia: a Randomized, Double-Blind, Placebo-Controlled Study.
Carson, WH; Fleischhacker, WW; Forbes, A; Hobart, M; McQuade, RD; Nyilas, M; Ouyang, J; Pfister, S; Sanchez, R; Weiller, E, 2017
)
0.46
" The regimen was well tolerated and no discontinuations related to adverse events occurred."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
"To systematically review relevant literature comparing the oncological outcomes and adverse events of different systemic therapies for patients with metastatic non-ccRCC."( A Systematic Review and Meta-analysis Comparing the Effectiveness and Adverse Effects of Different Systemic Treatments for Non-clear Cell Renal Cell Carcinoma.
Albiges, L; Bensalah, K; Bex, A; Canfield, SE; Dabestani, S; Fernández-Pello, S; Giles, RH; Hofmann, F; Hora, M; Kuczyk, MA; Lam, TB; Ljungberg, B; Marconi, L; Merseburger, AS; Powles, T; Staehler, M; Tahbaz, R; Volpe, A, 2017
)
0.46
" Sunitinib was associated with more Grade 3-4 adverse events than everolimus, although this was not statistically significant."( A Systematic Review and Meta-analysis Comparing the Effectiveness and Adverse Effects of Different Systemic Treatments for Non-clear Cell Renal Cell Carcinoma.
Albiges, L; Bensalah, K; Bex, A; Canfield, SE; Dabestani, S; Fernández-Pello, S; Giles, RH; Hofmann, F; Hora, M; Kuczyk, MA; Lam, TB; Ljungberg, B; Marconi, L; Merseburger, AS; Powles, T; Staehler, M; Tahbaz, R; Volpe, A, 2017
)
0.46
" Efficacy (by intention to treat) was analyzed using the inverse variance method; safety data were recorded as the occurrence of any adverse event."( Efficacy and Safety of Quinolone-Containing Rescue Therapies After the Failure of Non-Bismuth Quadruple Treatments for Helicobacter pylori Eradication: Systematic Review and Meta-Analysis.
Gisbert, JP; Marin, AC; McNicholl, AG; Nyssen, OP, 2017
)
0.46
" The incidences of adverse events potentially related to the study drug were 16%, 26%, and 13% in the placebo, rebamipide 2%, and rebamipide 4% groups, respectively."( Efficacy and safety of rebamipide liquid for chemoradiotherapy-induced oral mucositis in patients with head and neck cancer: a multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II study.
Beppu, T; Fujii, M; Fujii, T; Fujimoto, Y; Hasegawa, Y; Hirano, S; Iwae, S; Kojima, H; Matsushima, Y; Matsuura, K; Monden, N; Naka, Y; Nishimori, H; Ogawa, T; Okami, K; Ota, I; Sasaki, K; Tahara, M; Takahashi, S; Tanaka, K; Ueda, S; Ueda, T; Yokota, T, 2017
)
0.46
"The present phase II study suggests that mouth washing with rebamipide may be effective and safe for patients with HNC receiving chemoradiotherapy, and 4% liquid is the optimal dose of rebamipide."( Efficacy and safety of rebamipide liquid for chemoradiotherapy-induced oral mucositis in patients with head and neck cancer: a multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II study.
Beppu, T; Fujii, M; Fujii, T; Fujimoto, Y; Hasegawa, Y; Hirano, S; Iwae, S; Kojima, H; Matsushima, Y; Matsuura, K; Monden, N; Naka, Y; Nishimori, H; Ogawa, T; Okami, K; Ota, I; Sasaki, K; Tahara, M; Takahashi, S; Tanaka, K; Ueda, S; Ueda, T; Yokota, T, 2017
)
0.46
" Phase II and III randomized clinical trials evaluate the efficacy and safety of EVG/c/TAF/FTC and tenofovir disoproxil fumerate (TDF)-containing arms; renal impairment, bone mineral density, metabolic effects, and other adverse events are topics explored within this review."( A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection.
Angione, SA; Cherian, SM; Özdener, AE, 2018
)
0.48
" The most common adverse events were diarrhea, nausea, and headache."( A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection.
Angione, SA; Cherian, SM; Özdener, AE, 2018
)
0.48
" Data seem to suggest it may also be effective and safe in patients with mild to moderate renal impairment."( A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection.
Angione, SA; Cherian, SM; Özdener, AE, 2018
)
0.48
"5% of those treated with EVG discontinued due to adverse events (AE)."( Clinical Experience with the Integrase Inhibitors Dolutegravir and Elvitegravir in HIV-infected Patients: Efficacy, Safety and Tolerance.
Balboa-Barreiro, V; Castro-Iglesias, Á; Cid-Silva, P; Fernández-Bargiela, N; Llibre, JM; Margusino-Framiñán, L; Martín-Herranz, I; Pernas-Souto, B; Poveda, E, 2017
)
0.46
"Patients initiating EVG/COBI/FTC/TDF were enrolled in the SCOLTA project, a multicenter observational study reporting grade 3-4 Adverse Events in subjects beginning new antiretroviral drug regimens."( Safety and tolerability of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil fumarate in a real life setting: Data from surveillance cohort long-term toxicity antiretrovirals/antivirals (SCOLTA) project.
Bandera, A; Bonfanti, P; Calza, L; Carenzi, L; Celesia, BM; Cordier, L; De Socio, GV; Di Biagio, A; Falasca, K; Gori, A; Madeddu, G; Maggi, P; Martinelli, C; Orofino, G; Pellicanò, GF; Quirino, T; Ricci, E; Rusconi, S; Squillace, N; Vichi, F, 2017
)
0.46
" Adverse events (AEs) were recorded."( Pharmacokinetics and Safety of Brexpiprazole Following Multiple-Dose Administration to Japanese Patients With Schizophrenia.
Higashi, K; Ishigooka, J; Iwashita, S; Liew, EL; Tadori, Y, 2018
)
0.48
" One serious adverse event (SAE) of perichondritis was reported, which was unrelated to laquinimod (0."( Safety and in vivo immune assessment of escalating doses of oral laquinimod in patients with RRMS.
Bar-Ilan, O; Hayardeny, L; Mimrod, D; Paul, F; Richter, N; Samara, E; Sehr, T; Sorani, E; Spiegelstein, O; Thomas, K; Tumani, H; Ziemssen, T, 2017
)
0.46
"Treatment of chronic Q fever with TET plus QNL appears to be a safe alternative for TET plus HCQ, for example, if TET plus HCQ cannot be tolerated due to side effects."( Treatment of Chronic Q Fever: Clinical Efficacy and Toxicity of Antibiotic Regimens.
Bleeker-Rovers, CP; de Regt, MJA; Hoepelman, AIM; Kampschreur, LM; Oosterheert, JJ; van Roeden, SE; Wever, PC, 2018
)
0.48
" The most frequent treatment-emergent adverse events in patients receiving brexpiprazole were akathisia (6."( Efficacy and safety of flexibly dosed brexpiprazole for the adjunctive treatment of major depressive disorder: a randomized, active-referenced, placebo-controlled study.
Augustine, C; Brewer, C; Hefting, N; Hobart, M; Josiassen, MK; McQuade, RD; Sanchez, R; Skuban, A; Zhang, P, 2018
)
0.48
" The primary outcome variable was the frequency and severity of treatment-emergent adverse events."( A Long-Term, Open-Label Study to Evaluate the Safety and Tolerability of Brexpiprazole as Maintenance Treatment in Adults with Schizophrenia.
Forbes, A; Hakala, M; Hobart, M; Ouyang, J; Pfister, S; Shi, L, 2018
)
0.48
"6% discontinued due to treatment-emergent adverse events, most commonly schizophrenia (8."( A Long-Term, Open-Label Study to Evaluate the Safety and Tolerability of Brexpiprazole as Maintenance Treatment in Adults with Schizophrenia.
Forbes, A; Hakala, M; Hobart, M; Ouyang, J; Pfister, S; Shi, L, 2018
)
0.48
" Treatment-emergent adverse events (TEAE) were experienced by 235/281 patients (83."( Long-term safety and effectiveness of brexpiprazole in Japanese patients with schizophrenia: A 52-week, open-label study.
Ishigooka, J; Iwashita, S; Tadori, Y, 2018
)
0.48
"Brexpiprazole was generally safe and well tolerated and maintained therapeutic effects in the long-term treatment of Japanese patients with schizophrenia."( Long-term safety and effectiveness of brexpiprazole in Japanese patients with schizophrenia: A 52-week, open-label study.
Ishigooka, J; Iwashita, S; Tadori, Y, 2018
)
0.48
" INSTIs have also been demonstrated as safe and tolerable."( Dolutegravir Neuropsychiatric Adverse Events: Specific Drug Effect or Class Effect.
Yombi, JC,
)
0.13
" The question if long-acting beta-agonist and long-acting muscarinic antagonist could be associated with the increased prevalence of CV-related adverse effects has puzzled, particularly in the past, specialists involved in the management of respiratory diseases."( Combination Therapy of Inhaled Indacaterol/Glycopyrronium for Chronic Obstructive Pulmonary Disease in the Very Elderly: Is It Safe? An Electrocardiographic Evaluation.
Bernardi, B; Bordoni, V; Borioni, E; Cesari, V; Cocci, G; Francioso, A; Giordano, P; Giulietti, F; Iacoacci, C; Landi, L; Lombardi, FE; Rosettani, G; Sarzani, R; Spannella, F,
)
0.13
" Nevertheless, physicians must be alerted to use indacaterol only according to its approved indications They must be aware of the possible adverse events since side effects may appear when the medicine is used for a prolonged period of time."( The safety of indacaterol for the treatment of COPD.
Balis, E; Metaxas, EI, 2018
)
0.48
" Treatment-emergent adverse events with an incidence of ≥5% and ≥2 times the rate of placebo in the brexpiprazole groups were vomiting, elevated blood prolactin, diarrhea, nausea, and dental caries."( Efficacy and safety of brexpiprazole for the treatment of acute schizophrenia in Japan: A 6-week, randomized, double-blind, placebo-controlled study.
Ishigooka, J; Iwashita, S; Tadori, Y, 2018
)
0.48
" Ozenoxacin was well tolerated, with 8 of 206 patients experiencing adverse effects, with only 1 of these potentially related to the study treatment; none were serious."( Efficacy and Safety of Ozenoxacin Cream for Treatment of Adult and Pediatric Patients With Impetigo: A Randomized Clinical Trial.
Albareda, N; Alonso, FG; Hebert, AA; Rosen, T; Rosenberg, N; Roth, S; Zsolt, I, 2018
)
0.48
" Safety outcomes included adverse events (AEs), movement disorder scales, and standard safety assessments (vital signs, laboratory safety parameters, physical examination, electrocardiograms)."( Adjunctive brexpiprazole for elderly patients with major depressive disorder: An open-label, long-term safety and tolerability study.
Hefting, N; Hobart, M; Lepola, U; Zhang, D, 2018
)
0.48
" Clinical, microbiological response and adverse events were assessed."( Safety and efficacy of oral nemonoxacin versus levofloxacin in treatment of community-acquired pneumonia: A phase 3, multicenter, randomized, double-blind, double-dummy, active-controlled, non-inferiority trial.
Cao, Z; Chang, L; Cheng, SL; Lv, Y; Ma, Z; Mo, B; Sun, S; Tong, Z; Wu, J; Wu, R; Yang, Y; Yuan, J; Zhang, Y; Zhu, D, 2019
)
0.51
" The incidence of adverse events (AEs) was comparable between nemonoxacin (33."( Safety and efficacy of oral nemonoxacin versus levofloxacin in treatment of community-acquired pneumonia: A phase 3, multicenter, randomized, double-blind, double-dummy, active-controlled, non-inferiority trial.
Cao, Z; Chang, L; Cheng, SL; Lv, Y; Ma, Z; Mo, B; Sun, S; Tong, Z; Wu, J; Wu, R; Yang, Y; Yuan, J; Zhang, Y; Zhu, D, 2019
)
0.51
"Nemonoxacin 500 mg once daily for 7-10 days is as effective and safe as levofloxacin for treating adult CAP patients in terms of clinical cure rates, microbiological success rates, and safety profile."( Safety and efficacy of oral nemonoxacin versus levofloxacin in treatment of community-acquired pneumonia: A phase 3, multicenter, randomized, double-blind, double-dummy, active-controlled, non-inferiority trial.
Cao, Z; Chang, L; Cheng, SL; Lv, Y; Ma, Z; Mo, B; Sun, S; Tong, Z; Wu, J; Wu, R; Yang, Y; Yuan, J; Zhang, Y; Zhu, D, 2019
)
0.51
" The elvitegravir group showed more discontinuations because of renal adverse events (2."( Efficacy and safety of switching to dolutegravir plus emtricitabine/tenofovir disoproxil fumarate (TDF) or elvitegravir/cobicistat/emtricitabine/TDF in virologically suppressed HIV-infected patients in clinical practice: results from a multicentre, observ
Bagella, P; Baldin, G; Capetti, A; Ciccullo, A; Cossu, MV; De Luca, A; Di Giambenedetto, S; Giacomelli, A; Lagi, F; Latini, A; Madeddu, G; Rusconi, S; Sterrantino, G, 2019
)
0.51
"To analyse the frequency and causes of treatment discontinuation in patients who were treated with an integrase strand transfer inhibitor (INSTI), with a focus on neuropsychiatric adverse events (NPAEs)."( Integrase strand transfer inhibitors and neuropsychiatric adverse events in a large prospective cohort.
Allavena, C; Bani-Sadr, F; Bregigeon, S; Cabié, A; Cuzin, L; Ferry, T; Katlama, C; Lourenco, J; Pugliese, P; Rey, D; Reynes, J, 2019
)
0.51
" Dual mTORC1/mTORC2 inhibitor AZD2014 showed no considerable effects on embryonic cells of zebrafish in concentrations substantially toxic in cancer cells."( Comparative toxicity evaluation of targeted anticancer therapeutics in embryonic zebrafish and sea urchin models.
Babic, T; Buric, SS; Dinic, J; Hadzic, S; Pesic, M; Radojkovic, D; Rankov, AD, 2018
)
0.48
" The incidence of adverse events (AEs) was the highest (54."( Integrated safety summary of phase II and III studies comparing oral nemonoxacin and levofloxacin in community-acquired pneumonia.
Chang, LW; Chang, YT; Cheng, SL; Chuang, YC; Hsu, MC; Perng, WC; Tsao, SM; Wu, RG, 2019
)
0.51
" In part B, most children (59 [98%] of 60 children) had one or more treatment-emergent adverse events; most events were mild to moderate in severity."( Safety, pharmacokinetics, and pharmacodynamics of lumacaftor and ivacaftor combination therapy in children aged 2-5 years with cystic fibrosis homozygous for F508del-CFTR: an open-label phase 3 study.
Li, C; Liu, F; Marigowda, G; McColley, SA; McNamara, JJ; Owen, CA; Sawicki, GS; Stiles, D; Tian, S; Waltz, D; Wang, LT, 2019
)
0.51
"Lumacaftor and ivacaftor were generally safe and well tolerated in children aged 2-5 years with cystic fibrosis for 24 weeks."( Safety, pharmacokinetics, and pharmacodynamics of lumacaftor and ivacaftor combination therapy in children aged 2-5 years with cystic fibrosis homozygous for F508del-CFTR: an open-label phase 3 study.
Li, C; Liu, F; Marigowda, G; McColley, SA; McNamara, JJ; Owen, CA; Sawicki, GS; Stiles, D; Tian, S; Waltz, D; Wang, LT, 2019
)
0.51
"The aim of the study was to assess the rates of discontinuation of integrase inhibitor regimens because of any neuropsychiatric adverse event (NPAE) and the factors associated with discontinuation."( Discontinuation of dolutegravir, elvitegravir/cobicistat and raltegravir because of toxicity in a prospective cohort.
Abdulghani, N; Ambrosioni, J; Casabona, J; Curran, A; Domingo, P; Force, L; Homar, F; Llibre, JM; Miró, JM; Montoliu, A; Peraire, J; Riera, M; Tiraboschi, J, 2019
)
0.51
" Every discontinuation because of adverse events (AEs) was double-checked directly with treating physicians."( Discontinuation of dolutegravir, elvitegravir/cobicistat and raltegravir because of toxicity in a prospective cohort.
Abdulghani, N; Ambrosioni, J; Casabona, J; Curran, A; Domingo, P; Force, L; Homar, F; Llibre, JM; Miró, JM; Montoliu, A; Peraire, J; Riera, M; Tiraboschi, J, 2019
)
0.51
" The rate of discontinuations because of NPAEs was low, but was significantly higher for dolutegravir than for elvitegravir/cobicistat, with significant differences among centres, suggesting that greater predisposition to believe that a given adverse event is caused by a given drug of some treating physicians might play a role in the discordance seen between cohorts."( Discontinuation of dolutegravir, elvitegravir/cobicistat and raltegravir because of toxicity in a prospective cohort.
Abdulghani, N; Ambrosioni, J; Casabona, J; Curran, A; Domingo, P; Force, L; Homar, F; Llibre, JM; Miró, JM; Montoliu, A; Peraire, J; Riera, M; Tiraboschi, J, 2019
)
0.51
" Adverse events were recorded by patients in specially developed diaries."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
" The incidence of adverse events between the groups was comparable: 22."( Efficacy and safety of the use of rebamipide in the scheme of triple eradication therapy of Helicobacter pylori infection: a prospective randomized comparative study.
Andreev, DN; Dicheva, DT; Maev, IV; Partzvania-Vinogradova, EV; Samsonov, AA, 2018
)
0.48
" The primary outcome variable was the frequency and severity of treatment-emergent adverse events (TEAEs)."( A Long-Term, Open-Label Study to Evaluate the Safety and Tolerability of Brexpiprazole as Adjunctive Therapy in Adults With Major Depressive Disorder.
Brewer, C; Hefting, N; Hobart, M; McQuade, RD; Sanchez, R; Skuban, A; Zhang, P,
)
0.13
" No significant differences were observed in the incidence rates of drug-related adverse events between the sitafloxacin (20."( The efficacy and safety of sitafloxacin and garenoxacin for the treatment of pneumonia in elderly patients: A randomized, multicenter, open-label trial.
Fukuda, Y; Fukushima, K; Hashiguchi, K; Higashiyama, Y; Imamura, Y; Inoue, Y; Izumikawa, K; Kobayashi, T; Koga, H; Kohno, S; Kondo, A; Mikushi, S; Miyazaki, T; Morinaga, Y; Mukae, H; Nagayoshi, Y; Nakamura, S; Saijo, T; Sasaki, E; Takazono, T; Yamamoto, K; Yanagihara, K; Yoshida, M, 2019
)
0.51
" Several of the recently reported untoward effects are not new to the class, and they are very rare compared with the relatively common neuropsychiatric adverse events."( [Toxicity of quinolone antibiotics - new untoward effects and reevaluation of known side effects].
Kern, WV, 2019
)
0.51
" Risk of adverse events: The risk of diarrhea, nausea, abdominal pain, and all adverse events did not significantly increase (p > 0."( The effects and side effects of laquinimod for the treatment of multiple sclerosis patients: a systematic review and meta-analysis of clinical trials.
Abbastabar, H; Bitarafan, S; Harirchian, MH; Mohammadpour, Z; Noureini, SK; Rouhi, F, 2020
)
0.56
" For premenopausal women, ofloxacin had a 57% probability of achieving remission but an 83% frequency of adverse events."( Efficacy and safety of quinolones for the treatment of uncomplicated urinary tract infections in women: a network meta-analysis.
González-Garay, A; Ochoa-Hein, E; Rivera-Luna, R; Velasco-Hidalgo, L, 2021
)
0.62
" Any studies reporting the administration of quinolones to children and including a methodology for identifying or reporting adverse events were identified by two authors who worked independently."( Seizures and quinolone antibiotics in children: a systematic review of adverse events.
Hawcutt, DB; Iyer, A; King, C; Kneen, R; Neame, M; Riordan, A; Sinha, I, 2020
)
0.56
" The quality of adverse event reporting in included studies was low."( Seizures and quinolone antibiotics in children: a systematic review of adverse events.
Hawcutt, DB; Iyer, A; King, C; Kneen, R; Neame, M; Riordan, A; Sinha, I, 2020
)
0.56
" Further evaluations of quinolone use in children should include methodologies for actively identifying and reporting adverse neurological events."( Seizures and quinolone antibiotics in children: a systematic review of adverse events.
Hawcutt, DB; Iyer, A; King, C; Kneen, R; Neame, M; Riordan, A; Sinha, I, 2020
)
0.56
"5%), occurrence of adverse events (5."( Post-hoc analysis investigating the safety and efficacy of brexpiprazole in Japanese patients with schizophrenia who were switched from other antipsychotics in a long-term study (Secondary Publication).
Ishigooka, J; Iwashita, S; Kojima, Y; Matsuo, S; Usami, T, 2020
)
0.56
"The CFTR modulator tezacaftor/ivacaftor was efficacious and generally safe and well tolerated in Phase 3 studies in participants ≥12 years of age with cystic fibrosis (CF) homozygous for the F508del-CFTR mutation or heterozygous with a residual function-CFTR mutation (F/F or F/RF respectively)."( A phase 3, double-blind, parallel-group study to evaluate the efficacy and safety of tezacaftor in combination with ivacaftor in participants 6 through 11 years of age with cystic fibrosis homozygous for F508del or heterozygous for the F508del-CFTR mutati
Ahluwalia, N; Campbell, D; Davies, JC; Harris, RS; Haseltine, E; Naehrlich, L; Owen, CA; Panorchan, P; Saunders, C; Sermet-Gaudelus, I; Short, C; Wainwright, CE, 2021
)
0.62
" Tezacaftor/ivacaftor was safe and well tolerated; no new safety concerns were identified."( A phase 3, double-blind, parallel-group study to evaluate the efficacy and safety of tezacaftor in combination with ivacaftor in participants 6 through 11 years of age with cystic fibrosis homozygous for F508del or heterozygous for the F508del-CFTR mutati
Ahluwalia, N; Campbell, D; Davies, JC; Harris, RS; Haseltine, E; Naehrlich, L; Owen, CA; Panorchan, P; Saunders, C; Sermet-Gaudelus, I; Short, C; Wainwright, CE, 2021
)
0.62
"6%) patients because of adverse effects."( Efficacy and Safety of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide as Maintenance Treatment in HIV/HBV-Coinfected Patients.
Cheng, CY; Cheng, SH; Ho, MW; Huang, SH; Huang, YS; Hung, CC; Lee, CH; Lee, YT; Lin, SP; Liou, BH; Liu, CE; Lu, PL; Sun, HY; Tang, HJ; Tsai, HC; Yang, CJ, 2021
)
0.62
"Quinolone (QN) antibiotics are widely used, which lead to their accumulation in soil and toxic effects on ryegrass in pasture."( Environmentally Friendly Quinolones Design for a Two-Way Choice between Biotoxicity and Genotoxicity through Double-Activity 3D-QSAR Model Coupled with the Variation Weighting Method.
Ren, Z; Sun, P; Yang, L; Zhao, W; Zhao, Y, 2020
)
0.56
" Secondary evaluations were related to efficacy, treatment emergent adverse events (TEAEs), extrapyramidal symptoms, and corrected QT interval (QTc)."( Safety of switching to brexpiprazole in Japanese patients with schizophrenia: A post-hoc analysis of a long-term open-label study.
Aoki, K; Inada, K; Ishigooka, J; Iwashita, S; Kojima, Y; Niidome, K; Yamada, S, 2021
)
0.62
" Most children (236 [99%] of 239 children) had adverse events that were mild (49 [21%] of 239) or moderate (148 [62%] of 239) in severity, and there was a low rate of adverse events leading to treatment discontinuation."( Long-term safety and efficacy of lumacaftor-ivacaftor therapy in children aged 6-11 years with cystic fibrosis homozygous for the F508del-CFTR mutation: a phase 3, open-label, extension study.
Chilvers, MA; Cornell, AG; Davies, JC; Han, Z; Milla, C; Owen, CA; Ratjen, F; Tian, S, 2021
)
0.62
"Lumacaftor-ivacaftor therapy in children homozygous for F508del-CFTR who initiated treatment at age 6-11 years was generally safe and well tolerated, and efficacy was sustained for up to 120 weeks."( Long-term safety and efficacy of lumacaftor-ivacaftor therapy in children aged 6-11 years with cystic fibrosis homozygous for the F508del-CFTR mutation: a phase 3, open-label, extension study.
Chilvers, MA; Cornell, AG; Davies, JC; Han, Z; Milla, C; Owen, CA; Ratjen, F; Tian, S, 2021
)
0.62
"Tezacaftor-ivacaftor is an approved cystic fibrosis transmembrane conductance regulator (CFTR) modulator shown to be efficacious and generally safe and well tolerated over 8-24 weeks in phase 3 clinical studies in participants aged 12 years or older with cystic fibrosis homozygous for the Phe508del CFTR mutation (F/F; study 661-106 [EVOLVE]) or heterozygous for the Phe508del CFTR mutation and a residual function mutation (F/RF; study 661-108 [EXPAND])."( Long-term safety and efficacy of tezacaftor-ivacaftor in individuals with cystic fibrosis aged 12 years or older who are homozygous or heterozygous for Phe508del CFTR (EXTEND): an open-label extension study.
Ahluwalia, N; Biner, RF; Brown, C; Campbell, D; Chang, P; De Boeck, K; Downey, DG; Fischer, R; Flume, PA; Hu, X; Jain, M; Millar, SJ; Owen, CA; Pasta, DJ; Paz-Diaz, H; Rubin, JL; Sawicki, GS; Wainwright, CE; Wang, X; Yang, Y, 2021
)
0.62
"Quinolones are ranked as the second most commonly used class of antibiotics in China, despite their adverse clinical and environmental effects."( In vivo and in silico evaluations of survival and cardiac developmental toxicity of quinolone antibiotics in zebrafish embryos (Danio rerio).
Han, Y; Hu, C; Ma, Y; Yao, S; Zhang, J, 2021
)
0.62
"A previous phase 3 study showed that lumacaftor-ivacaftor was generally safe and well tolerated over 24 weeks of treatment in children aged 2-5 years with cystic fibrosis homozygous for the F508del-CFTR mutation."( Long-term safety of lumacaftor-ivacaftor in children aged 2-5 years with cystic fibrosis homozygous for the F508del-CFTR mutation: a multicentre, phase 3, open-label, extension study.
Chilvers, M; Cornell, AG; Hoppe, JE; McColley, SA; McNamara, JJ; Owen, CA; Ratjen, F; Tian, S; Zahigian, R, 2021
)
0.62
" Most participants (56 [98%] of 57) had at least one adverse event during study 116, most of which were mild (19 [33%] participants) or moderate (29 [51%] participants) in severity."( Long-term safety of lumacaftor-ivacaftor in children aged 2-5 years with cystic fibrosis homozygous for the F508del-CFTR mutation: a multicentre, phase 3, open-label, extension study.
Chilvers, M; Cornell, AG; Hoppe, JE; McColley, SA; McNamara, JJ; Owen, CA; Ratjen, F; Tian, S; Zahigian, R, 2021
)
0.62
"Lumacaftor-ivacaftor was generally safe and well tolerated, and treatment effects were generally maintained for the duration of the extension study."( Long-term safety of lumacaftor-ivacaftor in children aged 2-5 years with cystic fibrosis homozygous for the F508del-CFTR mutation: a multicentre, phase 3, open-label, extension study.
Chilvers, M; Cornell, AG; Hoppe, JE; McColley, SA; McNamara, JJ; Owen, CA; Ratjen, F; Tian, S; Zahigian, R, 2021
)
0.62
"Quinolones comprise a class of antibiotics that are globally preferred for treating a wide range of bacterial infections due to their potency, broad coverage, favorable pharmacologic profile, and mostly mild to moderate adverse reactions."( Systemic quinolones and risk of retinal detachment I: analysis of data from the US FDA adverse event reporting system.
Alami, A; Bjerre, LM; Gravel, CA; Krewski, D; Mattison, D; Momoli, F; Taher, MK; Tsui, D, 2022
)
0.72
" Regarding the adverse drug reactions (ADRs), quinolones did not bring higher risks, while the incidence of ADRs in the quinolone group was also even significantly lower (P < 0."( Efficacy and safety of quinolones vs. other antimicrobials for the treatment of uncomplicated urinary tract infections in adults: a systematic review and meta-analysis.
Cai, Y; Jia, Y; Wang, J; Yan, K; Zhu, M, 2022
)
0.72
"Elexacaftor plus tezacaftor plus ivacaftor is a triple-combination cystic fibrosis transmembrane conductance regulator (CFTR) modulator regimen shown to be generally safe and efficacious in people with cystic fibrosis aged 12 years or older with at least one F508del-CFTR allele."( Efficacy and safety of elexacaftor plus tezacaftor plus ivacaftor versus tezacaftor plus ivacaftor in people with cystic fibrosis homozygous for F508del-CFTR: a 24-week, multicentre, randomised, double-blind, active-controlled, phase 3b trial.
Ahluwalia, N; Bruinsma, BG; Downey, DG; Duckers, J; Harris, C; Lam, AP; Lou, Y; MacGregor, G; Mall, MA; McKone, EF; Moskowitz, SM; Sutharsan, S; Tian, S; Tullis, E; Van Braeckel, E; Wainwright, CE; Waltz, D; Watson, D; Yuan, J, 2022
)
0.72
"The elexacaftor plus tezacaftor plus ivacaftor regimen was safe and well tolerated, and led to significant and clinically meaningful improvements in respiratory-related quality of life and lung function, as well as improved CFTR function, changes that were durable over 24 weeks and superior to those seen with tezacaftor plus ivacaftor in this patient population."( Efficacy and safety of elexacaftor plus tezacaftor plus ivacaftor versus tezacaftor plus ivacaftor in people with cystic fibrosis homozygous for F508del-CFTR: a 24-week, multicentre, randomised, double-blind, active-controlled, phase 3b trial.
Ahluwalia, N; Bruinsma, BG; Downey, DG; Duckers, J; Harris, C; Lam, AP; Lou, Y; MacGregor, G; Mall, MA; McKone, EF; Moskowitz, SM; Sutharsan, S; Tian, S; Tullis, E; Van Braeckel, E; Wainwright, CE; Waltz, D; Watson, D; Yuan, J, 2022
)
0.72
" Safety pharmacology studies following single dose revealed no adverse effects on central nervous system (including seizure) in mice and cardiovascular system (hERG and monkey telemetry)."( Preclinical safety evaluation of levonadifloxacin, a novel anti-methicillin-resistant Staphyloccocus aureus benzoquinolizine fluoroquinolone by intravenous and oral administration.
Gupta, S; Kansagara, A; Nandanwar, M; Patel, A; Patel, M; Patel, MA; Thorve, D; Yeole, R, 2022
)
0.72
"Two previous Phase 3 studies ("parent studies") showed that tezacaftor/ivacaftor was generally safe and efficacious for up to 24 weeks in children 6 through 11 years of age with cystic fibrosis (CF) and F508del/F508del (F/F) or F508del/residual function (F/RF) genotypes."( A Phase 3, open-label, 96-week trial to study the safety, tolerability, and efficacy of tezacaftor/ivacaftor in children ≥ 6 years of age homozygous for F508del or heterozygous for F508del and a residual function CFTR variant.
Ahluwalia, N; Campbell, D; Chilvers, M; Davies, JC; Harris, RS; McNamara, J; Naehrlich, L; Paz-Diaz, H; Saunders, C; Sawicki, GS; Sermet-Gaudelus, I; Shih, JL; Wainwright, CE, 2022
)
0.72
" Most (n = 129) had ≥ 1 treatment-emergent adverse event (TEAE), the majority of which were mild or moderate in severity and generally consistent with common manifestations of CF."( A Phase 3, open-label, 96-week trial to study the safety, tolerability, and efficacy of tezacaftor/ivacaftor in children ≥ 6 years of age homozygous for F508del or heterozygous for F508del and a residual function CFTR variant.
Ahluwalia, N; Campbell, D; Chilvers, M; Davies, JC; Harris, RS; McNamara, J; Naehrlich, L; Paz-Diaz, H; Saunders, C; Sawicki, GS; Sermet-Gaudelus, I; Shih, JL; Wainwright, CE, 2022
)
0.72
"Tezacaftor/ivacaftor is generally safe and well tolerated, and treatment effects are maintained for up to 120 weeks."( A Phase 3, open-label, 96-week trial to study the safety, tolerability, and efficacy of tezacaftor/ivacaftor in children ≥ 6 years of age homozygous for F508del or heterozygous for F508del and a residual function CFTR variant.
Ahluwalia, N; Campbell, D; Chilvers, M; Davies, JC; Harris, RS; McNamara, J; Naehrlich, L; Paz-Diaz, H; Saunders, C; Sawicki, GS; Sermet-Gaudelus, I; Shih, JL; Wainwright, CE, 2022
)
0.72
" Adverse events were observed in 15% of the patients, and the regimen was discontinued in only six patients."( Effectiveness and safety of elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate single-tablet combination among HIV-infected patients in Turkey: results from a real world setting.
Aydin, OA; Bilge, B; Bolukcu, S; Dokmetas, I; Gumuser, F; Gunduz, A; Karaosmanoglu, HK; Mete, B; Tabak, F; Yildiz, DS, 2021
)
0.62
"Real world data on the effectiveness and safety of E/C/F/TDF is comparable with the phase 3 trial results Adverse events are uncommon and manageable."( Effectiveness and safety of elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate single-tablet combination among HIV-infected patients in Turkey: results from a real world setting.
Aydin, OA; Bilge, B; Bolukcu, S; Dokmetas, I; Gumuser, F; Gunduz, A; Karaosmanoglu, HK; Mete, B; Tabak, F; Yildiz, DS, 2021
)
0.62
"This study aimed to detect safety signals of rebamipide and search for adverse events (AEs) of rebamipide that are more common than those of other drugs for peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD) in the elderly population."( Frequently reported adverse events of rebamipide compared to other drugs for peptic ulcer and gastroesophageal reflux disease.
Jang, E; Jeong, JE; Kim, MG; Lee, JY; Park, M, 2022
)
0.72
" Our study investigated the FDA Adverse Event Reporting System and the pharmacodynamic CHEMBL database to further characterize TGA-induced ICDs."( Impulse Control Disorders by Dopamine Partial Agonists: A Pharmacovigilance-Pharmacodynamic Assessment Through the FDA Adverse Event Reporting System.
De Ponti, F; Fusaroli, M; Giunchi, V; Menchetti, M; Poluzzi, E; Raschi, E; Rimondini Giorgini, R, 2022
)
0.72
"We downloaded and pre-processed the FDA Adverse Event Reporting System up to December 2020."( Impulse Control Disorders by Dopamine Partial Agonists: A Pharmacovigilance-Pharmacodynamic Assessment Through the FDA Adverse Event Reporting System.
De Ponti, F; Fusaroli, M; Giunchi, V; Menchetti, M; Poluzzi, E; Raschi, E; Rimondini Giorgini, R, 2022
)
0.72
"000 1) and incidence of adverse reactions(RR=0."( [Systematic review and Meta-analysis of efficacy and safety of Ningmitai Capsules in treatment of urinary tract infection].
Li, JB; Lyu, J; Wang, ZQ; Xie, YM, 2022
)
0.72
" Cell culture studies have shown quinolones to be highly toxic to TM fibroblasts."( Cytotoxicity of Tetracyclines in Human Tympanic Membrane Fibroblasts.
Antonelli, PJ; Dirain, CO, 2023
)
0.91
"Tetracyclines are less toxic to cultured TM fibroblasts than ciprofloxacin."( Cytotoxicity of Tetracyclines in Human Tympanic Membrane Fibroblasts.
Antonelli, PJ; Dirain, CO, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" The elimination half-life was 28."( Steady-state pharmacokinetics of rufloxacin in elderly patients with lower respiratory tract infections.
Cogo, R; Imbimbo, BP; Mattina, R; Rimoldi, R, 1992
)
0.28
" An example of a pharmacokinetic study of rufloxacin and its metabolites in monkeys is shown."( High-performance liquid chromatography and preliminary pharmacokinetics of rufloxacin and its metabolites, N-desmethylrufloxacin and rufloxacinsulfoxide, in urine of rhesus monkey Macaca mulatta.
Imbimbo, BP; Peeters, A; van den Biggelaar-Martea, M; Vree, TB, 1992
)
0.28
" The distributional phase was rapid with a half-life of 6-7 min for both doses."( Pharmacokinetics of enrofloxacin in fingerling rainbow trout (Oncorhynchus mykiss).
Babish, JG; Bowser, PR; St Leger, J; Wooster, GA, 1992
)
0.28
"Fluoroquinolones have similar chemical structures but wide differences in their pharmacokinetic profiles."( Influence of renal function on the pharmacokinetics of lomefloxacin compared with other fluoroquinolones.
Blum, RA, 1992
)
0.28
"The pharmacokinetic properties of rufloxacin, a new quinolone antibacterial agent, were evaluated in ten patients with lower respiratory tract infections."( Pharmacokinetics of rufloxacin once daily in patients with lower respiratory tract infections.
Albrici, A; Fioretti, M; Imbimbo, BP; Rimoldi, R,
)
0.13
" Pharmacokinetic analyses showed that cimetidine did not affect the rate or extent of temafloxacin absorption, as evidenced by unchanged peak plasma concentration, time to peak plasma concentration, and terminal-phase volume of distribution."( Effect of cimetidine on the pharmacokinetics of temafloxacin.
Granneman, GR; Locke, C; Sörgel, F; Stephan, U, 1992
)
0.28
"h) and terminal-phase half-life (9."( Effects of temafloxacin and ciprofloxacin on the pharmacokinetics of caffeine.
Fuhr, U; Granneman, GR; Kinzig, M; Mahr, G; Muth, P; Nickel, P; Patterson, K; Sörgel, F; Stephan, U, 1992
)
0.28
" absorption and a higher tissue/plasma concentration than that of other quinolones, are its interesting pharmacokinetic properties."( Ocular pharmacokinetics of rufloxacin a new fluoroquinolone antibiotic.
Brancato, R; Cremonesi, F; Ghione, M; Lombardo, N; Manitto, MP; Nucci, P, 1992
)
0.28
"The purpose of the present work was to investigate the 48 h pharmacokinetic and biliary elimination of temafloxacin, administered intraduodenally at a single dose of 10 mg/kg to six conscious pigs provided with a double terminal choledocal fistula allowing the collection and the reinstillation of bile."( Pharmacokinetics and biliary elimination of temafloxacin in pigs.
Bresler, L; Didelot, JP; Hazebroucq, J; Jehl, F; Koechlin, C; Merle-Melet, M, 1992
)
0.28
" After IV administration, a rapid distribution phase was followed by a slower elimination phase, with a half-life of 131."( Pharmacokinetics of enrofloxacin after intravenous and intramuscular injection in rabbits.
Arboix, M; Cabanes, A; Garcia Anton, JM; Reig, F, 1992
)
0.28
" Pharmacokinetic studies demonstrated that THEO serum levels and elimination were not altered by concurrent CP administration."( Effects of fluoroquinolone antimicrobials alone and in conjunction with theophylline on seizures in amygdaloid kindled rats. Mechanistic and pharmacokinetic study.
Schwark, WS; Vancutsem, PM, 1992
)
0.28
" Compared with the data reported for young adults, the elimination half-life (12."( Steady-state pharmacokinetics and sputum penetration of lomefloxacin in patients with chronic obstructive pulmonary disease and acute respiratory tract infections.
Glerum, JH; Hoepelman, AI; Kovarik, JM; Rozenberg-Arska, M; Sips, PA; Smit, JM; Verhoef, J, 1992
)
0.28
" The pharmacokinetic analysis based on the physiological model indicated that fenbufen did not affect the permeability across the blood-brain or blood-CSF barrier."( Effect of fenbufen on the pharmacokinetics of sparfloxacin in rats.
Iwamoto, K; Katagiri, Y; Naora, K; Sekine, Y; Tanaka, K; Yamaguchi, T, 1992
)
0.28
" There was no significant difference in theophylline half-life before treatment (7."( [The influence of repirinast, an anti-allergic drug, on theophylline pharmacokinetics in patients with bronchial asthma].
Dohi, Y; Houya, I; Kiuchi, H; Nagata, M; Sakamoto, Y; Tabe, K; Yamamoto, K, 1991
)
0.28
" The drug was rapidly absorbed (absorption half-life 17 +/- 6 min in the 300 + 150 mg and 11 +/- 5 min in the 400 + 200 mg dose regimen group) and reached maximal serum concentrations (2."( Pharmacokinetics of rufloxacin in healthy volunteers after repeated oral doses.
Bonfiglio, G; Cesana, M; Cocuzza, CE; Gulisano, G; Imbimbo, BP; Mattina, R, 1991
)
0.28
" The longer half-life of temafloxacin enables a once-daily dose regimen, whereas the usual recommended dosage of ciprofloxacin is twice daily."( Comparative pharmacokinetics of ciprofloxacin and temafloxacin in humans: a review.
Kinzig, M; Mahr, G; Muth, P; Naber, KG; Sorgel, F, 1991
)
0.28
" Compared with the young group, mean peak plasma concentration in the elderly was 45% higher, the area under the plasma concentration versus time curve was 70% higher, the terminal elimination half-life was 18% higher, and the apparent beta-phase volume of distribution was 30% lower in the elderly group."( The influence of age on the pharmacokinetics of temafloxacin.
Granneman, GR; Guay, DR, 1991
)
0.28
" Theophylline pharmacokinetic parameters were determined noncompartmentally, and results of single and combined administration were compared."( Effect of temafloxacin on the pharmacokinetics of theophylline.
Callens, E; Chauvin, JP; Hazebroucq, J; Ruff, F; Santais, MC, 1991
)
0.28
" The mean serum half-life on the first day was 10."( The pharmacokinetics of lomefloxacin in elderly patients with urinary tract infection following daily dosing with 400 mg.
Cowling, P; Lovering, AM; MacGowan, AP; McMullin, CM; Reeves, DS; Rogers, S; White, LO, 1991
)
0.28
" Its in vitro activity and pharmacokinetic properties have been investigated to assess its potential for use in the therapy of respiratory disease in cattle."( Clinical pharmacokinetics of parenterally administered danofloxacin in cattle.
Giles, CJ; Grimshaw, WT; Lynch, MJ; Magonigle, RA; Rice, JR; Risk, JE; Tanner, AC, 1991
)
0.28
" The pharmacokinetic parameters of the two drugs were estimated by model-independent methods."( Pharmacokinetic characteristics of N7-substituted theophylline derivatives and their interaction with quinolone in rats.
Apichartpichean, R; Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K, 1991
)
0.28
"The pharmacokinetic properties of the fluoroquinolone antimicrobial enrofloxacin were studied in New Zealand White rabbits."( Pharmacokinetic properties of enrofloxacin in rabbits.
Babish, JG; Brooks, DL; Broome, RL; Conzelman, GM; Copeland, DD, 1991
)
0.28
"We studied the pharmacokinetic parameters of four fluoroquinolones--ofloxacin, ciprofloxacin, temafloxacin and sparfloxacin--in a mouse model of Streptococcus pneumoniae-infected lung."( Pharmacokinetics of four fluoroquinolones in an animal model of infected lung.
Azoulay-Dupuis, E; Bergogne-Bérézin, E; Pocidalo, JJ; Vallée, E, 1991
)
0.28
" The long serum elimination half-life (approximately 8 h in patients with normal renal function) allows for single or twice-daily dosing."( A review of the pharmacokinetic profile of temafloxacin.
Dudley, MN, 1991
)
0.28
" Total plasma clearance (CL), volume of distribution (Vd), and half-life (T1/2) of evocarpine were 60 ml/min."( Pharmacological properties of galenical preparation. XV. Pharmacokinetics study of evocarpine and its metabolite in rats.
Chen, XF; Kanemaki, S; Kano, Y; Komatsu, K; Zong, Q, 1991
)
0.28
" The half-life (mean +/- standard deviation) increased from 10."( Temafloxacin pharmacokinetics in subjects with normal and impaired renal function.
Braeckman, R; Craft, JC; Granneman, GR; Kraut, J; Shupien, S, 1991
)
0.28
" The mean plasma elimination half-life was 28."( Pharmacokinetics and tissue penetration of rufloxacin, a long acting quinolone antimicrobial agent.
Andrews, JM; Imbimbo, BP; Johnson, J; O'Sullivan, N; Wise, R, 1991
)
0.28
" There were considerable variations in the plasma concentration-time profiles among subjects; for example, the elimination half-life in plasma varied from 14."( Inter- and intrasubject variabilities in the pharmacokinetics of rufloxacin after single oral administration to healthy volunteers.
Attardo-Parrinello, G; Broccali, G; Cesana, M; Crema, F; Imbimbo, BP, 1991
)
0.28
" For the other new quinolones, a decrease in glomerular filtration rate below 20-30 ml/min induces an increase in terminal half-life and a decrease in plasma and renal clearance, related to the degree of renal impairment."( Pharmacokinetics of quinolones in renal insufficiency.
Borsa-Lebas, F; Dhib, M; Fillastre, JP; Humbert, G; Leroy, A; Moulin, B, 1990
)
0.28
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" Mean Cmax values (0."( Pharmacokinetics and safety of single oral doses of lomefloxacin.
Morse, IS,
)
0.13
" The results of simulating the antibiotic pharmacokinetic profiles by the Kd values known from the literature and the values estimated with the proposed method were compared."( [Physiologic model of NY-198 pharmacokinetics using a new method of determining tissue/blood distribution coefficient].
Manuĭlov, KK, 1990
)
0.28
" Because the transintestinal route of elimination compensates for loss of renal elimination, the serum half-life of ciprofloxacvin is raised only to 5-10 hours even in total renal failure."( Pharmacokinetics of ciprofloxacin with reference to other fluorinated quinolones.
Bergan, T, 1989
)
0.28
"A possible pharmacokinetic interaction between theophylline and repirinast has been investigated in asthmatic patients."( Lack of effect of repirinast on the pharmacokinetics of theophylline in asthmatic patients.
Apichartpichean, R; Hasegawa, T; Horiuchi, T; Kuzuya, T; Nadai, M; Ogura, Y; Takagi, K, 1989
)
0.28
" Plasma half-life was approximately 8 hr."( Pharmacokinetics and safety of lomefloxacin following multiple doses.
Adams, MA; Hunt, TL,
)
0.13
"Comparative physiological pharmacokinetic analysis has been carried out to elucidate the different tissue distribution characteristics among eight pyridonecarboxylic acids including newly developed NY-198."( Structure-tissue distribution relationship based on physiological pharmacokinetics for NY-198, a new antimicrobial agent, and the related pyridonecarboxylic acids.
Kato, H; Nagata, O; Nakamura, M; Okezaki, E; Terasaki, T; Tsuji, A,
)
0.13
" The mean time to Cmax (Tmax) values averaged 64."( Pharmacokinetics and tolerance of lomefloxacin after sequentially increasing oral doses.
Kunka, RL; Mant, TG; Morrison, PJ; Norman, GT; Robinson, J, 1988
)
0.27
"The pharmacokinetic and haemodynamic effects of a 200 mg oral dose of BTS 49 465 (7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone) were investigated in a double-blind placebo controlled study."( The pharmacokinetics and haemodynamics of BTS 49 465 and its major metabolite in healthy volunteers.
Crampton, EL; Hind, ID; Wynne, RD, 1985
)
0.27
" The plasma data for each subject were described by an open one-compartment body model with first-order absorption, and the pharmacokinetic parameters were determined."( Pharmacokinetics of rosoxacin in human volunteers.
Edelson, J; Park, GB; Saneski, J; Weng, T, 1982
)
0.26
" Pharmacokinetic values analyzed by use of multivariant stepwise linear regression analysis indicated that the area under the concentration-time curve, but not time above minimum inhibitory concentration, was significant in predicting efficacy of enrofloxacin treatment."( Pharmacokinetics of enrofloxacin in clinically normal dogs and mice and drug pharmacodynamics in neutropenic mice with Escherichia coli and staphylococcal infections.
McClure, JT; Meinen, JB; Rosin, E, 1995
)
0.29
" None of the pharmacokinetic parameters differed significantly after prior treatment with omeprazole compared with placebo."( Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics.
Koeppe, P; Lode, H; Rost, KL; Schaberg, T; Stuht, H, 1995
)
0.29
" The aims of this study were to examine and compare the pharmacokinetic properties of the quinolones oxolinic acid, flumequine, sarafloxacin, and enrofloxacin after intravascular and oral administration to Atlantic salmon (Salmo salar) by using identical experimental designs."( Comparative single-dose pharmacokinetics of four quinolones, oxolinic acid, flumequine, sarafloxacin, and enrofloxacin, in Atlantic salmon (Salmo salar) held in seawater at 10 degrees C.
Horsberg, TE; Martinsen, B, 1995
)
0.29
" Plasma concentration-time profiles and pharmacokinetic parameters of balofloxacin in male rats were similar to those in female rats, indicating no sex-related differences."( Pharmacokinetics of the new fluoroquinolone balofloxacin in mice, rats, and dogs.
Hayakawa, N; Ishigai, M; Kato, M; Kinoshita, H; Nakagawa, T; Ohkubo, K; Okazaki, A; Okutomi, T, 1995
)
0.29
"The pharmacokinetic properties of enrofloxacin were determined in broiler chickens after single IV and orally administered doses of 10 mg/kg of body weight."( Pharmacokinetics and residues of enrofloxacin in chickens.
Anadón, A; Bringas, P; Díaz, MJ; Fernández, MC; Fernández, R; Fernàndez-Cruz, ML; Martínez, MA; Martínez-Larrañaga, MR, 1995
)
0.29
" Mean Cmax values ranged from 705 +/- 158 to 1966 +/- 620 ng/mL for the 200 to 800 mg doses, at median tmax ranging from 4 to 5 hours."( Pharmacokinetics of sparfloxacin in humans after single oral administration at doses of 200, 400, 600, and 800 mg.
Bruno, R; Chassard, D; Ebmeier, M; Frydman, A; Guimart, C; Le Roux, Y; Montay, G; Thebault, JJ; Vergniol, JC, 1994
)
0.29
" The Cmax, AUC, and urinary excretion rates were not altered by food intake, whereas the Tmax was prolonged slightly."( Pharmacokinetics and safety of NM441, a new quinolone, in healthy male volunteers.
Kosuge, K; Morino, A; Nakashima, M; Okuyama, Y; Ozaki, M; Takebe, Y; Uematsu, T, 1994
)
0.29
" A significant relationship between pharmacokinetic parameters and creatinine clearance was observed only for renal clearance of parent or conjugated sparfloxacin."( Pharmacokinetics of sparfloxacin in patients with renal impairment.
Bruno, R; Dhib, M; Etienne, I; Fillastre, JP; Gay, G; Guimart, C; Le Roux, Y; Montay, G; Schott, D; Vivier, N, 1994
)
0.29
" It is not clear whether this pharmacokinetic interaction might be clinically important."( Renal clearance of lomefloxacin is decreased by furosemide.
Ebihara, A; Fujimura, A; Harada, K; Ohashi, K; Sasaki, M; Shiga, T; Sudoh, T; Tateishi, T, 1994
)
0.29
" Pharmacokinetic parameters of both substances were calculated by use of statistical moments and were compared to those of enrofloxacin described in the veterinary literature."( Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin after intravenous and oral administration of enrofloxacin in dogs.
Küng, K; Riond, JL; Wanner, M, 1993
)
0.29
"In a randomized, double-blind, placebo-controlled, multiple-dose pharmacokinetic study, the safety and effect on intestinal flora of sparfloxacin (SPX) were determined in 12 healthy male volunteers (8 received SPX and 4 received a placebo)."( Multiple-dose pharmacokinetics of sparfloxacin and its influence on fecal flora.
Borner, K; Fassbender, M; Koeppe, P; Lode, H; Nord, CE; Ritz, M, 1994
)
0.29
" Interpatient variability was appreciable for the plasma and urine concentrations was well as for the calculated pharmacokinetic parameters."( Pharmacokinetics, safety, and tolerability of flosequinan in patients with hepatic dysfunction.
Hind, ID; Hinson, JL; Weidler, DJ, 1994
)
0.29
" Pharmacokinetic parameters were calculated by use of a noncompartment model."( [The effect of pregnancy and lactation in sows on the pharmacokinetics of the gyrase inhibitor marbofloxacin].
Petracca, K; Wanner, M, 1993
)
0.29
" Pharmacokinetic parameters after tablet did not differ significantly from the corresponding values after capsule."( Pharmacokinetics and relative bioavailability of lomefloxacin preparations in 10 healthy Chinese volunteers.
Diao, Y; Ji, G; Li, L; Lu, J; Wang, EH; Zhu, XD, 1993
)
0.29
"An in vitro pharmacodynamic system has been successfully adapted to simulate in vivo antimicrobial pharmacokinetics under anaerobic conditions."( Evaluation of activity of temafloxacin against Bacteroides fragilis by an in vitro pharmacodynamic system.
Krinke, AJ; Moody, JA; Rotschafer, JC; Vance-Bryan, K; Walker, KJ; Zabinski, RA, 1993
)
0.29
" This is followed by a monophasic slow decrease, with an elimination half-life (t1/2) of 15 to 20 hours."( Clinical pharmacokinetics of sparfloxacin.
Ishibashi, Y; Nogita, T; Shimada, J, 1993
)
0.29
" Pharmacokinetic analyses indicate nonlinearity of 349U85 and 661U88, suggestive of saturation of metabolism and large interindividual variability in maximum plasma drug concentration and area under the plasma concentration-time curve."( Pharmacokinetics and pharmacodynamics of a new cardiotonic vasodilator agent, 349U85, in normal subjects.
Brown, AR; Clifton, GD; Fleck, RJ; Harrison, MR; Long, RA; Rolleri, RL; Welch, RM; Weller, S; Wermeling, DP, 1994
)
0.29
" Pharmacokinetic parameters were calculated by use of statistical moments."( Pharmacokinetics of the gyrase inhibitor marbofloxacin: influence of pregnancy and lactation in sows.
Graser, T; Petracca, K; Riond, JL; Wanner, M, 1993
)
0.29
" A two-compartment model was used to calculate rufloxacin pharmacokinetic parameters."( Pharmacokinetics of rufloxacin in patients with impaired renal function.
Imbimbo, BP; Mant, TG; Morrison, PJ; Perry, G; Sacks, S; Wise, R; Woodcook, J, 1993
)
0.29
"The pharmacokinetic properties of nedocromil sodium give this agent a high safety margin in the treatment of asthma."( General pharmacology, pharmacokinetics, and toxicology of nedocromil sodium.
Clark, B, 1993
)
0.29
" The outstanding pharmacokinetic features of lomefloxacin are its high degree of tissue distribution, lack of significant metabolism (and, therefore, no competitive drug interactions with other metabolised drugs showing a common metabolic pathway), and good oral absorption."( Lomefloxacin clinical pharmacokinetics.
Belliveau, PP; Freeman, CD; Nicolau, DP; Nightingale, CH, 1993
)
0.29
" Overall, results indicated (1) no marked differences in pharmacokinetic parameters in pregnant versus nonpregnant females, (2) fleroxacin levels in embryonic tissues were similar to maternal plasma levels, and (3) there was a correlation between exposure and embryolethal doses for all fluoroquinolones which resulted in embryolethality except norfloxacin."( Developmental toxicity of fleroxacin and comparative pharmacokinetics of four fluoroquinolones in the cynomolgus macaque (Macaca fascicularis).
Hendrickx, AG; Hummler, H; Richter, WF, 1993
)
0.29
" A one-compartment model applied to the high-performance liquid chromatography data was used to calculate the pharmacokinetic parameters of rufloxacin."( Multiple-dose pharmacokinetics of rufloxacin in patients with cirrhosis.
Granai, F; Imbimbo, BP; Triger, DR; Wise, R; Woodcock, J, 1993
)
0.29
" The elimination half-life was 7 to 8 h, independently of the doses."( Single- and multiple-dose pharmacokinetics of AM-1155, a new 6-fluoro-8-methoxy quinolone, in humans.
Ishida, R; Kosuge, K; Kusajima, H; Masuda, Y; Nakashima, M; Ooie, T; Uchida, H; Uematsu, T, 1995
)
0.29
" No statistically significant differences were observed in the pharmacokinetic parameters (Cmax-AUC-T1/2-urinary excretion and metabolic ratio) of sparfloxacin following the 2 treatment."( Cimetidine does not alter sparfloxacin pharmacokinetics.
Alvarez, MP; Azanza, JR; Gries, JM; Honorato, J; Sadaba, B; Singlas, E; Taburet, AM, 1995
)
0.29
" The time course of ENR and CIP was fitted by nonlinear least squares regression analysis, and the pharmacokinetic variables were compared."( Penetration of enrofloxacin and ciprofloxacin into breast milk, and pharmacokinetics of the drugs in lactating rabbits and neonatal offspring.
Abadía, AR; Aramayona, JJ; Bregante, MA; Fraile, LJ; García, MA; Mora, J, 1996
)
0.29
"The pathophysiology associated with major burns is complex and subject to a state of flux (coexistence of pain, infectious diseases, multiple trauma, disturbances of metabolism and acid-base status, etc) which could affect the disposition and the pharmacokinetic behaviour of drugs."( [Pharmacokinetics of antibiotics in burn patients].
Bourget, P; Carsin, H; Lesne-Hulin, A,
)
0.13
" In addition, urine levels, drug level/MIC ratio, and urine antibacterial activity 72 to 84 h after treatment initiation were determined in a subgroup of patients for pharmacodynamic assessment."( Single-dose rufloxacin versus 3-day norfloxacin treatment of uncomplicated cystitis: clinical evaluation and pharmacodynamic considerations.
Aguilar, L; Caffaratti, J; Dal-Ré, R; Dalet, F; Del Río, G, 1996
)
0.29
" Although such titers were not sufficient to predict a clinical response based on previous pharmacodynamic studies using quinolone antibiotics, data obtained with volunteers may only partially reflect the clinical situation in which a rise of humoral antibodies directed against pneumococcal antigens may help to reinforce the bactericidal action of the antibiotic."( Pharmacokinetics of sparfloxacin and serum bactericidal activity against pneumococci.
Borner, K; Koeppe, P; Ruhnke, M; Trautmann, M; Wagner, J, 1996
)
0.29
"The area under the plasma concentration-time curve and the elimination half-life of lomefloxacin were significantly increased following coadministration with ranitidine."( Effect of ranitidine on renal clearance of lomefloxacin.
Fujimura, A; Harada, K; Ohmori, M; Sakamoto, K; Sudoh, T; Sunaga, K, 1996
)
0.29
" Doses of pefloxacin and concentrations in cerebrospinal fluid and plasma (total and unbound) at the pharmacodynamic endpoint were all independent of infusion rate, whereas only cerebrospinal fluid concentrations of norfloxacin were independent of infusion rate."( Pharmacokinetic-pharmacodynamic contributions to the convulsant activity of pefloxacin and norfloxacin in rats.
Bouquet, S; Couet, W; Courtois, P; Delon, A; Huguet, F; Vierfond, JM, 1997
)
0.3
" At 0, 2, 4 and 6 h 300 microL of CSF was withdrawn for pharmacodynamic measurements."( Pharmacodynamics and pharmacokinetics of A-80556 using microdialysis in a Streptococcus pneumoniae meningitis model.
Destache, CJ; Pakiz, CB; Stoysich, AM, 1996
)
0.29
" Clinafloxacin was rapidly absorbed, with Cmax occurring at approximately 40 min postdose."( The tolerance and pharmacokinetics of clinafloxacin (CI-960) in healthy subjects.
Bron, NJ; Dorr, MB; Mant, TG; Vassos, AB; Webb, CL, 1996
)
0.29
" The plasma terminal elimination half-life and urinary recovery remained unchanged."( Comparative study of pharmacokinetics of two new fluoroquinolones, balofloxacin and grepafloxacin, in elderly subjects.
Kanamaru, M; Kozawa, O; Matsuno, H; Nagashima, S; Niwa, M; Uematsu, T, 1996
)
0.29
"-10), providing pharmacokinetic evidence to justify therapeutic efficacy trials with the lower dose."( Multiple route and dose pharmacokinetics of enrofloxacin in juvenile Atlantic salmon.
Babish, JG; Bowser, PR; Bustos, PS; Stoffregen, DA; Wooster, GA, 1997
)
0.3
" The pharmacodynamic data demonstrated that BAY 12-8039 has marked activity against gram-positive and gram-negative organisms (under both anaerobic and aerobic conditions) and anaerobes."( Pharmacodynamic properties of BAY 12-8039 on gram-positive and gram-negative organisms as demonstrated by studies of time-kill kinetics and postantibiotic effect.
Andrews, JM; Boswell, FJ; Wise, R, 1997
)
0.3
"632 micrograms/ml and an elimination half-life of 41."( Pharmacokinetics of a single intravenous enrofloxacin dose in scimitar-horned oryx (Oryx dammah).
Boothe, DM; Gamble, KC; Heatley, JJ; Helmick, KE; Jensen, JM, 1997
)
0.3
"The pharmacokinetic behaviour of enrofloxacin was compared in four one-day-old and four one-week-old calves in order to find out if there were any age-related differences."( Pharmacokinetics of enrofloxacin in newborn and one-week-old calves.
Kaartinen, L; Moilanen, M; Pyörälä, S; Räisänen, S, 1997
)
0.3
" The half-life of grepafloxacin was about 12 hours after single doses and about 15 hours after repeat doses."( Pharmacokinetics of grepafloxacin after oral administration of single and repeat doses in healthy young males.
Bramer, SL; Efthymiopoulos, C; Maroli, A, 1997
)
0.3
" Child-Pugh scores and components of the scores showed no correlation with any pharmacokinetic variables."( Grepafloxacin pharmacokinetics in individuals with hepatic dysfunction.
Bass, N; Bramer, SL; Efthymiopoulos, C; Flaherty, JF; Maroli, A; Somberg, K; Wolfe, E, 1997
)
0.3
" Population pharmacokinetic analysis was accomplished using iterative two-stage analysis."( Pharmacokinetics and pharmacodynamics of oral grepafloxacin in patients with acute bacterial exacerbations of chronic bronchitis.
Amantea, MA; Chodosh, S; Collins, DA; Forrest, A; Schentag, JJ, 1997
)
0.3
" Pharmacokinetic parameters were characterized with RSTRIP, an iterative, nonlinear, weighted, least-squares-regression program."( Pharmacokinetics of sparfloxacin in the serum and vitreous humor of rabbits: physicochemical properties that regulate penetration of quinolone antimicrobials.
Drusano, G; Liu, QF; Liu, W; Louie, A; Madu, A; Mayers, M; Mian, U; Miller, MH; Perkins, R, 1998
)
0.3
"We looked for associations between pharmacokinetic (Pk) and pharmacodynamic (Pd) parameters of ciprofloxacin (CPFX) and sparfloxacin (SPFX) and the in vivo efficacy of these antimicrobials in an immunocompetent mouse model of severe Streptococcus pneumoniae pneumonia."( Pharmacodynamic activities of ciprofloxacin and sparfloxacin in a murine pneumococcal pneumonia model: relevance for drug efficacy.
Azoulay-Dupuis, E; Bédos, JP; Moine, P; Muffat-Joly, M; Pocidalo, JJ; Vallée, E; Veber, B, 1998
)
0.3
" Within 4 to 5 h they fell to about 30 to 55% of the Cmax, and thereafter a terminal half-life of 11 to 14 h accounted for the major part of the area under the concentration-time curve (AUC)."( Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects.
Dalhoff, A; Kubitza, D; Schühly, U; Stass, H, 1998
)
0.3
" To compare the treatments, analysis of variance-based point estimates and 90% confidence intervals (given in parentheses) were calculated for the mean ratios of the pharmacokinetic parameters from the test (rufloxacin coadministration) over those from the reference (theophylline without rufloxacin) period."( Absence of effect of rufloxacin on theophylline pharmacokinetics in steady state.
Cesana, M; Fuhr, U; Kinzig-Schippers, M; Müller, C; Rietbrock, S; Sörgel, F; Staib, AH, 1998
)
0.3
"A rapid and sensitive high-performance thin-layer chromatographic (HPTLC) method has been developed for the measurement of sparfloxacin in human plasma and its use for pharmacokinetic study has been evaluated."( High performance thin-layer chromatographic method for the determination of sparfloxacin in human plasma and its use in pharmacokinetic studies.
Gandhi, TP; Modi, IA; Modi, RI; Mody, VD; Pandya, KK; Satia, MC, 1998
)
0.3
" The present study investigated the ability of sub-MICs of rufloxacin, an orally absorbed monofluorinated quinolone with a long half-life (28 to 30 h), to interfere with the bacterial virulence parameters of adhesiveness, hemagglutination, hydrophobicity, motility, and filamentation, as well as their interactions with host neutrophilic defenses such as phagocytosis, killing, and oxidative bursts."( Pharmacodynamic effects of subinhibitory concentrations of rufloxacin on bacterial virulence factors.
Braga, PC; Dal Sasso, M; Sala, MT, 1999
)
0.3
" time were analysed by a compartmental independent pharmacokinetic model that provided the most important kinetic parameters."( Comparative pharmacokinetics of enrofloxacin and ciprofloxacin in chickens.
Errecalde, C; García Ovando, H; Gorla, N; Luders, C; Poloni, G; Prieto, G; Puelles, I, 1999
)
0.3
" administration, the mean Cmax observed (2."( Pharmacokinetics of enrofloxacin given by the oral, intravenous and intramuscular routes in broiler chickens.
Black, WD; Bugyei, K; McEwen, S, 1999
)
0.3
"To compare pharmacokinetic variables of enrofloxacin (ENR) after IV administration in mice, rats, rabbits, sheep, and cows and to perform allometric analysis of ENR."( Comparative pharmacokinetics of enrofloxacin in mice, rats, rabbits, sheep, and cows.
Aramayona, JJ; Bregante, MA; Fraile, L; Garcia, MA; Saez, P; Solans, C, 1999
)
0.3
" Pharmacokinetic variables were correlated further with body weight."( Comparative pharmacokinetics of enrofloxacin in mice, rats, rabbits, sheep, and cows.
Aramayona, JJ; Bregante, MA; Fraile, L; Garcia, MA; Saez, P; Solans, C, 1999
)
0.3
"In all species studied, the best fit was obtained for a two-compartment open model; ENR half-life ranged from 89 minutes in mice to 169 minutes in cows."( Comparative pharmacokinetics of enrofloxacin in mice, rats, rabbits, sheep, and cows.
Aramayona, JJ; Bregante, MA; Fraile, L; Garcia, MA; Saez, P; Solans, C, 1999
)
0.3
"To determine the maximum-tolerated dose, toxicities, and pharmacokinetic profile of the farnesyl protein transferase inhibitor R115777 when administered orally bid for 5 days every 2 weeks."( Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer.
Belly, RT; Bol, CJ; Bowden, C; Chiao, J; Chow, C; Cowan, KH; End, DW; Gress, RE; Hakim, FT; Horak, ID; Kohler, DR; Kopp, WC; Kremer, AB; Larkin, G; Noone, M; Nussenblatt, RB; Piotrovsky, VK; Todd, A; Woestenborghs, R; Zujewski, J, 2000
)
0.31
" Based upon pharmacokinetic data, the recommended dose for phase II trials is 500 mg orally bid (total daily dose, 1, 000 mg) for 5 consecutive days followed by 9 days of rest."( Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer.
Belly, RT; Bol, CJ; Bowden, C; Chiao, J; Chow, C; Cowan, KH; End, DW; Gress, RE; Hakim, FT; Horak, ID; Kohler, DR; Kopp, WC; Kremer, AB; Larkin, G; Noone, M; Nussenblatt, RB; Piotrovsky, VK; Todd, A; Woestenborghs, R; Zujewski, J, 2000
)
0.31
" The plasma concentration of DW116 declined monoexponentially with a half-life range of 16-22 hr."( Pharmacokinetics and urinary excretion of DW116, a new fluoroquinolone antibacterial agent, in humans as a phase I study.
Choi, MH; Chung, BC; Jung, BH, 2000
)
0.31
"06 ml/kg/h, half-life (t1/2beta) was 17."( Pharmacokinetics of enrofloxacin administered intravenously and orally to foals.
Bermingham, EC; Papich, MG; Vivrette, SL, 2000
)
0.31
" Time of maximum plasma concentration (Tmax) was similar for MAR and DIF; Tmax occurred earlier for ENR and later for CIP."( Comparison of fluoroquinolone pharmacokinetic parameters after treatment with marbofloxacin, enrofloxacin, and difloxacin in dogs.
Evans, EI; Frazier, DL; Thompson, L; Trettien, A, 2000
)
0.31
"Three pharmacokinetic/pharmacodynamic parameters--(i) the peak concentration to the minimum inhibitory concentration ratio (C(max)/MIC); (ii) the area under the concentration-time curve to MIC ratio (AUC(24h)/MIC); and (iii) the time the concentration exceeds the MIC (T>MIC)--are important predictors of the clinical efficacy of antibiotics."( Macrolides: pharmacokinetics and pharmacodynamics.
Tulkens, PM; Van Bambeke, F, 2001
)
0.31
"Antitumor and pharmacodynamic studies were performed in MCF-7 human breast cancer cells and companion xenografts with the farnesyl protein transferase inhibitor, R115777, presently undergoing Phase II clinical trials, including in breast cancer."( Preclinical antitumor activity and pharmacodynamic studies with the farnesyl protein transferase inhibitor R115777 in human breast cancer.
Clarke, PA; Detre, S; Dowsett, M; End, D; Howes, AJ; Johnston, SR; Kelland, LR; Patterson, L; Smith, V; Valenti, M; Workman, P, 2001
)
0.31
" The plasma concentration-time data for both enrofloxacin and ciprofloxacin were best described by a one-compartment open pharmacokinetic model."( Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin in goats given enrofloxacin alone and in combination with probenecid.
Ahmad, AH; Malik, JK; Ramesh, S; Rao, GS; Sharma, LD; Tripathi, HC, 2002
)
0.31
" The mean peak concentration in plasma of 10."( Single-dose pharmacokinetics and penetration of BMS 284756 into an inflammatory exudate.
Andrews, JM; Gee, T; Marshall, G; Wise, R, 2002
)
0.31
" Pharmacokinetic parameters were calculated by noncompartmental methods."( Comparative serum pharmacokinetics of the fluoroquinolones enrofloxacin, difloxacin, marbofloxacin, and orbifloxacin in dogs after single oral administration.
Heinen, E, 2002
)
0.31
"The pharmacokinetic behavior of marbofloxacin was studied in goats after single-dose intravenous (i."( Pharmacokinetic behavior of marbofloxacin after intravenous and intramuscular administrations in adult goats.
De Vicente, ML; González, F; Rodríguez, C; San Andrés, MD; San Andrés, MI; Waxman, S, 2001
)
0.31
"The impact of Actinobacillus pleuropneumoniae (APP) infection in swine on the pharmacokinetic parameters of enrofloxacin were determined."( Influence of porcine Actinobacillus pleuropneumoniae infection and dexamethasone on the pharmacokinetic parameters of enrofloxacin.
Baker, JD; Cope, CV; Farrell, DE; Myers, MJ; Post, LO, 2002
)
0.31
"Harmonic mean half-life for oral administration was 14."( Pharmacokinetics after intravenous and oral administration of enrofloxacin in sheep.
Bermingham, EC; Papich, MG, 2002
)
0.31
"Enrofloxacin administered orally to sheep has a prolonged half-life and high oral bioavailability."( Pharmacokinetics after intravenous and oral administration of enrofloxacin in sheep.
Bermingham, EC; Papich, MG, 2002
)
0.31
"To determine pharmacokinetic characteristics of marbofloxacin after a single IV and oral administration and tissue residues after serial daily oral administration in chickens."( Pharmacokinetic characteristics and tissue residues for marbofloxacin and its metabolite N-desmethyl-marbofloxacin in broiler chickens.
Anadón, A; Castellano, VJ; Díaz, MJ; Frejo, MT; Martínez, M; Martínez, MA; Martínez-Larrañaga, MR; Tafur, M, 2002
)
0.31
"Analysis of pharmacokinetic data obtained in this study reveals that a minimal therapeutic dose of 2 mg/kg, PO, every 24 hours should be appropriate for control of most infections in chickens."( Pharmacokinetic characteristics and tissue residues for marbofloxacin and its metabolite N-desmethyl-marbofloxacin in broiler chickens.
Anadón, A; Castellano, VJ; Díaz, MJ; Frejo, MT; Martínez, M; Martínez, MA; Martínez-Larrañaga, MR; Tafur, M, 2002
)
0.31
"The pharmacokinetic disposition of enrofloxacin was studied in goats after subcutaneous (s."( Pharmacokinetic disposition of subcutaneously administered enrofloxacin in goats.
Malik, JK; Ramesh, S; Rao, GS, 2002
)
0.31
" No significant differences were observed in mean toborinone pharmacokinetic parameters among the four study groups."( The pharmacokinetics of toborinone in subjects with congestive heart failure and concomitant renal impairment and/or concomitant hepatic impairment.
Bramer, SL; Kitani, M; Miyamoto, G; Tammara, B; Trang, JM, 2002
)
0.31
"The impact of Escherichia coli-derived lipopolysaccharide (LPS) on the pharmacokinetic parameters of enrofloxacin in swine was assessed to determine whether this model would substitute for a pleuropneumonia infection model for pharmacokinetic evaluation of drugs."( The effect of endotoxin and dexamethasone on enrofloxacin pharmacokinetic parameters in swine.
Baker, JD; Cope, CV; Farrell, DE; Myers, MJ; Post, LO, 2003
)
0.32
"The pharmacokinetic behavior of marbofloxacin was studied in seven healthy goats and in the same goats with induced fever after single-dose intravenous (i."( Influence of Escherichia coli endotoxin-induced fever on the pharmacokinetic behavior of marbofloxacin after intravenous administration in goats.
De Lucas, JJ; González, F; Rodríguez, C; San Andrés, MD; San Andrés, MI; Waxman, S, 2003
)
0.32
"The pharmacokinetic properties and tolerability of three different strengths of prulifloxacin (CAS 123447-62-1), a new antibacterial agent prodrug of AF3013 (CAS 112984-60-8), have been investigated in a randomized, cross-over study performed in 12 Caucasian male subjects (age range 19-34 years)."( Pharmacokinetics and tolerability of prulifloxacin after single oral administration.
Brion, N; Dionisio, P; Gualano, V; Marchetti, M; Millérioux, L; Picollo, R; Rosignoli, MT, 2003
)
0.32
" The objective of this study was to define the pharmacodynamic profile of BMS-284756 against Streptococcus pneumoniae."( Pharmacodynamics of a novel des-F(6)-quinolone, BMS-284756, against Streptococcus pneumoniae in the thigh infection model.
Banevicius, M; Mattoes, HM; Nicolau, DP; Nightingale, CH; Xuan, D, 2003
)
0.32
" After iv ENR injection (as a bolus), the elimination half-life (t(1/2beta)), the volume of distribution (Vd(area)), and the area under the concentration vs."( Pharmacokinetics of enrofloxacin in lactating sheep.
Haritova, A; Lashev, L; Pashov, D, 2003
)
0.32
" The T(1/2)abs, T(1/2)beta, AUC, Tmax and Cmax in the maternal plasma were approximately 6 min, 13."( Transplacental pharmacokinetics of the new fluoroquinolone DW-116 in pregnant rats.
Bae, CS; Chung, MK; Han, J; Kim, JC; Kim, SH; Park, SC; Shin, HC; Yun, HI, 2003
)
0.32
" The mean elimination half-life for garenoxacin in plasma appeared to be independent of dose and ranged from 13."( Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects.
Bello, A; Christopher, L; Gajjar, DA; Ge, Z; Grasela, DM, 2003
)
0.32
" In the post-distributive phase, marbofloxacin disappeared from aqueous humor with a half-life of 780 minutes."( Population pharmacokinetics of marbofloxacin in aqueous humor after intravenous administration in dogs.
Boisramé, B; Concordet, D; Regnier, A; Schneider, M; Toutain, PL, 2003
)
0.32
"The pharmacokinetic properties of the antibacterial agent oxolinic acid and vetoquinol, the carbitol ester of oxolinic acid, were studied after intravenous (i."( A single-dose pharmacokinetic study of oxolinic acid and vetoquinol, an oxolinic acid ester, in cod, Gadus morhua L., held in sea water at 8 degrees C and in vitro antibacterial activity of oxolinic acid against Vibrio anguillarum strains isolated from di
Bergh, O; Ervik, A; Samuelsen, OB, 2003
)
0.32
" The study also sought to identify drug-drug pharmacokinetic interactions, evaluate effects on protein farnesylation, and seek preliminary evidence for clinical activity."( A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Eckhardt, SG; Gentner, L; Goetz, A; Hammond, LA; Izbicka, E; McCreery, H; Mori, M; Patnaik, A; Richards, H; Rowinsky, EK; Rybak, ME; Schwartz, G; Takimoto, CH; Terada, K; Tolcher, AA; Zhang, S, 2003
)
0.32
" To identify pharmacokinetic interactions, the treatment and plasma sampling schemes were designed to permit comparisons of the pharmacokinetic behavior of each agent administered alone and together."( A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Eckhardt, SG; Gentner, L; Goetz, A; Hammond, LA; Izbicka, E; McCreery, H; Mori, M; Patnaik, A; Richards, H; Rowinsky, EK; Rybak, ME; Schwartz, G; Takimoto, CH; Terada, K; Tolcher, AA; Zhang, S, 2003
)
0.32
" There was no evidence of clinically relevant pharmacokinetic interactions between tipifarnib and gemcitabine."( A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Eckhardt, SG; Gentner, L; Goetz, A; Hammond, LA; Izbicka, E; McCreery, H; Mori, M; Patnaik, A; Richards, H; Rowinsky, EK; Rybak, ME; Schwartz, G; Takimoto, CH; Terada, K; Tolcher, AA; Zhang, S, 2003
)
0.32
" We therefore compared the in vitro pharmacodynamic activity of ABT-492 to that of levofloxacin, an antibiotic commonly used for the treatment of pneumonia, through MIC determination and time-kill kinetic analysis."( In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.
Danziger, LH; Gunderson, SM; Hayes, RA; Quinn, JP, 2004
)
0.32
"Modifications to the basic side-chain of early lead structures of the indolyl quinolinone class of KDR kinase inhibitors resulted in improved pharmacokinetic and ancillary profiles."( Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Arrington, KL; Buser, CA; Ciecko, PA; Coll, KE; Fernandes, C; Fraley, ME; Hartman, GD; Hoffman, WF; Lynch, JJ; McFall, RC; Rickert, K; Singh, R; Smith, S; Thomas, KA; Wong, BK, 2004
)
0.32
"The plasma and milk pharmacokinetics of marbofloxacin, a fluoroquinolone antibacterial compound, were evaluated in dairy cows, as well as its pharmacodynamic characteristics against mastitis-isolated pathogens."( Pharmacokinetics of marbofloxacin in lactating cows after repeated intramuscular administrations and pharmacodynamics against mastitis isolated strains.
Boisramé, B; Schneider, M; Vallé, M; Woehrlé, F, 2004
)
0.32
"The purpose of this study was to examine the allometric analysis of ciprofloxacin and enrofloxacin using pharmacokinetic data from the literature."( Allometric analysis of ciprofloxacin and enrofloxacin pharmacokinetics across species.
Bartges, J; Cottrell, MB; Cox, SK; Frazier, DL; Papich, MG; Smith, L, 2004
)
0.32
" Despite having different pharmacokinetic profiles, ibafloxacin and marbofloxacin produced similar results when used under field conditions at the recommended dosages."( Treatment of canine pyoderma with ibafloxacin and marbofloxacin--fluoroquinolones with different pharmacokinetic profiles.
Horspool, LJ; Mawhinney, I; van den Bos, R; van Laar, P, 2004
)
0.32
"Population pharmacokinetic of marbofloxacin was investigated on 21 healthy and 16 diseased horses to assess interindividual variability of drug exposure."( Population pharmacokinetics of marbofloxacin in horses: preliminary analysis.
Bousquet-Mélou, A; Concordet, D; Doucet, MY; Peyrou, M; Schneider, M; Vrins, A, 2004
)
0.32
"96 L/kg, with a harmonic mean elimination half-life of 21."( Pharmacokinetics of enrofloxacin after single-dose oral and intravenous administration in the American alligator (Alligator mississippiensis).
Bennett, RA; Helmick, KE; Jacobson, ER; Papich, MG; Vliet, KA, 2004
)
0.32
" Coadministration with lithium increased mean Cmax and AUC values of aripiprazole by about 19% and 15%, respectively, whereas the apparent oral clearance decreased by 15%."( Pharmacokinetics of aripiprazole and concomitant lithium and valproate.
Bark, N; Citrome, L; Josiassen, R; Mallikaarjun, S; Salazar, DE, 2005
)
0.33
" Tipifarnib pharmacokinetic and pharmacodynamic variables were similar in the presence and absence of tamoxifen."( A phase I trial and pharmacokinetic study of tipifarnib, a farnesyltransferase inhibitor, and tamoxifen in metastatic breast cancer.
Balis, FM; Chow, C; Clark, G; Eng-Wong, J; Gantz, SB; Jayaprakash, N; Lebowitz, PF; Venzon, D; Widemann, BC; Zujewski, J, 2005
)
0.33
"Pharmacokinetic and pharmacodynamic properties of tolfenamic acid (TA) in calves were determined in serum and fluids of inflamed (carrageenan administered) and non-inflamed subcutaneously implanted tissue cages after intramuscular administration both alone and in combination with marbofloxacin (MB)."( Influence of marbofloxacin on the pharmacokinetics and pharmacodynamics of tolfenamic acid in calves.
Landoni, MF; Lees, P; Sidhu, PK, 2005
)
0.33
"The pharmacokinetic behaviour of enrofloxacin (ENR) and its active metabolite ciprofloxacin (CIP) were determined in six greater rheas following a single intravenous (i."( Pharmacokinetics of enrofloxacin following intravenous administration to greater rheas: a preliminary study.
de Lucas, JJ; Lábaque, MC; Martella, MB; Navarro, JL; Rodríguez, C; San Andrés, MI, 2005
)
0.33
" The pharmacokinetic parameters of ARIPIPRAZOLE and its main metabolite OPC-14857 were determined."( Influence of itraconazole co-administration and CYP2D6 genotype on the pharmacokinetics of the new antipsychotic ARIPIPRAZOLE.
Azuma, J; Fukuda, T; Inaba, A; Koue, T; Kubo, M; Maune, H; Takeda, H, 2005
)
0.33
" Validated HPLC methods were successfully applied to pharmacokinetic study of aripiprazole in rats, demonstrating brain concentrations after oral administration five times higher than plasma concentrations."( High performance liquid chromatographic methods for the determination of aripiprazole with ultraviolet detection in rat plasma and brain: application to the pharmacokinetic study.
Akiyama, H; Kashiyama, E; Koga, T; Miyamoto, G; Shimokawa, Y, 2005
)
0.33
"Pharmacokinetic and pharmacodynamic properties in goats of the non-steroidal anti-inflammatory drug tolfenamic acid (TA), administered both alone and in combination with the fluoroquinolone marbofloxacin (MB), were established in a tissue cage model of acute inflammation."( Pharmacokinetic and pharmacodynamic interactions of tolfenamic acid and marbofloxacin in goats.
Landoni, MF; Lees, P; Sidhu, PK, 2006
)
0.33
" The ISF and plasma-unbound concentrations were similar during the steady-state period despite differences in lipophilicity and pharmacokinetic parameters of the drugs."( Plasma and interstitial fluid pharmacokinetics of enrofloxacin, its metabolite ciprofloxacin, and marbofloxacin after oral administration and a constant rate intravenous infusion in dogs.
Bidgood, TL; Papich, MG, 2005
)
0.33
" The pharmacodynamic parameters from time-kill kinetic studies provide a useful means of studying antimicrobial activity."( Comparison of faecal and optimal growth conditions on in vitro pharmacodynamic activity of marbofloxacin against Escherichia coli.
Gicquel-Bruneau, M; Laurentie, M; Pellet, T; Sanders, P, 2006
)
0.33
"The pharmacokinetic properties of marbofloxacin, a third generation fluoroquinolone, were investigated in six cats after single intravenous (IV) and repeat oral (PO) administration at a daily dose of 2 mg/kg."( Pharmacokinetics of marbofloxacin after single intravenous and repeat oral administration to cats.
Albarellos, GA; Landoni, MF; Montoya, L, 2005
)
0.33
" The pharmacokinetic parameter of the area under the concentration-time curve (AUC)/MIC ratio in the lungs for DX-619, sitafloxacin, and ciprofloxacin were 171."( In vivo efficacies and pharmacokinetics of DX-619, a novel des-fluoro(6) quinolone, against Streptococcus pneumoniae in a mouse lung infection model.
Fukuda, Y; Higashiyama, Y; Hirakata, Y; Kohno, S; Miyazaki, Y; Mizuta, Y; Ohno, H; Tashiro, T; Tomono, K; Tsukamoto, K; Yanagihara, K, 2006
)
0.33
" Pharmacokinetic sampling was performed for 36 hours after the first dose and peripheral-blood mononuclear cells (PBMCs) were collected at baseline and steady state for determination of farnesyl protein transferase (FTase) activity and HDJ-2 farnesylation."( Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Arceci, RJ; Balis, FM; Blaney, SM; End, D; Fox, E; Gillespie, A; Jayaprakash, N; Palumbo, JS; Pitney, A; Salzer, WL; Whitcomb, P; Widemann, BC; Zannikos, P, 2006
)
0.33
" The pharmacokinetic profile of tipifarnib in children is similar to that in adults, and at the MTD, FTase is inhibited in PBMC in vivo."( Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Arceci, RJ; Balis, FM; Blaney, SM; End, D; Fox, E; Gillespie, A; Jayaprakash, N; Palumbo, JS; Pitney, A; Salzer, WL; Whitcomb, P; Widemann, BC; Zannikos, P, 2006
)
0.33
"The pharmacodynamic properties governing the activities of antibiotics against intracellular Staphylococcus aureus are still largely undetermined."( Pharmacodynamic evaluation of the intracellular activities of antibiotics against Staphylococcus aureus in a model of THP-1 macrophages.
Barcia-Macay, M; Mingeot-Leclercq, MP; Seral, C; Tulkens, PM; Van Bambeke, F, 2006
)
0.33
"To evaluate the aqueous humor pharmacokinetics of rufloxacin in rabbits after topical administration of different formulations, and to individuate the ones showing the best pharmacokinetic profile."( Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits.
Burgalassi, S; Cappello, B; Chetoni, P; Iervolino, M; Monti, D; Saettone, MF,
)
0.13
" The main pharmacokinetic parameters of RUF in the aqueous humor produced by the different formulations were calculated and statistical differences were assessed."( Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits.
Burgalassi, S; Cappello, B; Chetoni, P; Iervolino, M; Monti, D; Saettone, MF,
)
0.13
"The pharmacokinetic behavior of marbofloxacin was studied in goats after single-dose subcutaneous (SC) administration of 2mg/kg bodyweight."( Pharmacokinetic behavior and pharmacokinetic/pharmacodynamic integration of marbofloxacin after subcutaneous administration in goats.
De Lucas, JJ; Dova, SW; González, F; Rodríguez, C; San Andrés, MD; San Andrés, MI, 2007
)
0.34
" Due to increasing resistance of causative pathogens, antibiotics should be used by considering their pharmacodynamic and pharmacokinetic characteristics."( Pharmacokinetic and pharmacodynamic aspects of antimicrobial agents for the treatment of uncomplicated urinary tract infections.
Arrigucci, S; Cassetta, MI; Fallani, S; Mazzei, T; Novelli, A, 2006
)
0.33
" For example, the longer half-life of marbofloxacin in many animal species has been appreciated in veterinary practice."( Integration of pharmacokinetic and pharmacodynamic indices of marbofloxacin in turkeys.
Fink-Gremmels, J; Haritova, AM; Lashev, LD; Parvanov, PR; Rusenova, NV, 2006
)
0.33
" A repeated measures study has been designed to compare their pharmacokinetic parameters, to investigate their bioavailability and to estimate their absorbed fraction and first-pass effect by using plasma, urinary and metabolite data collected from five healthy mares."( Enrofloxacin and marbofloxacin in horses: comparison of pharmacokinetic parameters, use of urinary and metabolite data to estimate first-pass effect and absorbed fraction.
Bousquet-Melou, A; Doucet, MY; Laroute, V; Peyrou, M; Vrins, A, 2006
)
0.33
" In conclusion, our developed methods were found to be selective, sensitive, robust and suitable for applications in clinical pharmacokinetic profiling."( Determination of the immunomodulator laquinimod in human plasma by liquid chromatography/tandem mass spectrometry; development, validation and application of two methods in clinical pharmacokinetic profiling.
Edman, K; Gunnarsson, PO; Hansson, G; Olin, M; Sennbro, CJ; Svensson, LD, 2006
)
0.33
" The suitability of the method for pharmacokinetic studies was evaluated by determining the concentrations of enrofloxacin (ENR) and ciprofloxacin (CIP) also in pig plasma, after administration of 200mg of enrofloxacin per kilogram of fodder during 5 consecutive days."( Determination of a series of quinolones in pig plasma using solid-phase extraction and liquid chromatography coupled with mass spectrometric detection Application to pharmacokinetic studies.
Barbosa, J; Barrón, D; Garcés, A; Kucera, R; Zerzanová, A, 2006
)
0.33
" administration of the drug, the elimination half-life (t(1/2 beta)) and mean residence time (MRT) were significantly longer in diseased calves (8."( Comparative pharmacokinetics of marbofloxacin in healthy and Mannheimia haemolytica infected calves.
El-Kattan, YA; Ismail, M, 2007
)
0.34
" This study investigated the pharmacokinetic variability of aripiprazole and the active metabolite dehydroaripiprazole on the basis of 155 drug monitoring samples from psychiatric patients treated with therapeutic doses of aripiprazole (10-30 mg/day)."( Pharmacokinetic variability of aripiprazole and the active metabolite dehydroaripiprazole in psychiatric patients.
Lunde, H; Lunder, N; Molden, E; Refsum, H, 2006
)
0.33
"3 mg/lb) and to compare pharmacokinetic variables after pharmacokinetic analysis by naïve averaged, naïve pooled, and nonlinear mixed-effects modeling."( Naïve averaged, naïve pooled, and population pharmacokinetics of orally administered marbofloxacin in juvenile harbor seals.
Huff, D; KuKanich, B; Papich, MG; Riviere, JE, 2007
)
0.34
" Maximum plasma concentration and area under the plasma-time concentration curve were approximately 3 microg/mL and 30 h x microg/mL, respectively."( Naïve averaged, naïve pooled, and population pharmacokinetics of orally administered marbofloxacin in juvenile harbor seals.
Huff, D; KuKanich, B; Papich, MG; Riviere, JE, 2007
)
0.34
"Values of pharmacokinetic variables were similar regardless of the analytic method used."( Naïve averaged, naïve pooled, and population pharmacokinetics of orally administered marbofloxacin in juvenile harbor seals.
Huff, D; KuKanich, B; Papich, MG; Riviere, JE, 2007
)
0.34
" Pharmacokinetic (PK) blood draws were performed on days 7, 17, and 27."( Pharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137.
Cheng, A; Kearney, BP; Ramanathan, S; Shen, G, 2007
)
0.34
"Although the high incidence of febrile neutropenia necessitated a multiple scheduling adaptation of tipifarnib compared to the original protocol, the apparent lack of mutual pharmacokinetic interactions, the ability to coadminister tipifarnib and docetaxel near single-agent MTDs, and suggestive evidence of efficacy make this drug combination attractive for further examination."( A phase I clinical and pharmacokinetic study of tipifarnib in combination with docetaxel in patients with advanced solid malignancies.
Awada, A; De Porre, P; de Valeriola, D; Gil, T; Lalami, Y; Piccart-Gebhart, MJ; Zhang, S, 2007
)
0.34
" Principal pharmacokinetic parameters were determined and two efficacy indices were computed by using pharmacokinetic parameters and selected mic90 values of marbofloxacin against pathogenic equine strains to predict the efficacy of the drug at this dose."( Pharmacokinetics of a single intravenous dose of marbofloxacin in adult donkeys.
De Lucas, JJ; González, F; Nieto, J; Rodríguez, C; San Andrés, MD; San Andrés, MI; Serres, C; Waxman, S, 2007
)
0.34
" The method was applied to a preliminary pharmacokinetic study in rats."( Validation of a simple HPLC method for assay of haplamine and its metabolites in plasma suitable for pharmacokinetic application in rats.
Aubert, C; Bun, H; Ciccolini, J; Ea, S; Giacometti, S; Siv, C, 2008
)
0.35
"The purpose of this study was to examine the allometric analyses of marbofloxacin, moxifloxacin, danofloxacin and difloxacin using pharmacokinetic data from the literature."( Allometric scaling of marbofloxacin, moxifloxacin, danofloxacin and difloxacin pharmacokinetics: a retrospective analysis.
Cox, SK, 2007
)
0.34
"To investigate the effect of GrlA mutation on the development of quinolone resistance in Staphylococcus aureus in an in vitro pharmacokinetic (PK) model and to examine the relationship between the emergence of resistance and PK/pharmacodynamic parameters."( Effect of GrlA mutation on the development of quinolone resistance in Staphylococcus aureus in an in vitro pharmacokinetic model.
Mitsuyama, J; Oonishi, Y; Yamaguchi, K, 2007
)
0.34
" The half-life of aripiprazole following repeated administration was similar to that following single administration, suggesting that pharmacokinetics was constant during 14-day administration."( Pharmacokinetics of aripiprazole, a new antipsychotic, following oral dosing in healthy adult Japanese volunteers: influence of CYP2D6 polymorphism.
Azuma, J; Fukuda, T; Koue, T; Kubo, M; Maune, H, 2007
)
0.34
"The population pharmacokinetic parameters of aripiprazole in healthy Japanese males were estimated using a nonlinear mixed effects model (NONMEM) program."( Nonlinear mixed effects model analysis of the pharmacokinetics of aripiprazole in healthy Japanese males.
Azuma, J; Fukuda, T; Funaki, T; Hashimoto, Y; Kayano, Y; Koue, T; Kubo, M; Takaai, M, 2007
)
0.34
" Marbofloxacin concentrations were determined via reverse-phase high-performance liquid chromatography, and pharmacokinetic analysis of the data was performed with a mono-compartmental model."( Intraocular pharmacokinetics of intravenously administered marbofloxacin in rabbits with experimentally induced acute endophthalmitis.
Concordet, D; Regnier, A; Schneider, M; Toutain, PL, 2008
)
0.35
"To determine the maximum tolerated dose (MTD) dose-limiting toxicity, and pharmacokinetic and pharmacodynamic profile of TKI258 (formerly CHIR-258)."( A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors.
Aziz, N; Braendle, E; Butzberger-Zimmerli, P; de Bono, JS; Evans, TR; Fox, JA; Garzon, F; Hardie, M; Heise, C; Jadayel, D; Judson, IR; Louie, S; Marriott, C; Michelson, G; Molife, R; Morrison, R; Sarker, D, 2008
)
0.35
" Further pharmacodynamic evaluation is required in these studies to evaluate the biological effects of TKI258."( A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors.
Aziz, N; Braendle, E; Butzberger-Zimmerli, P; de Bono, JS; Evans, TR; Fox, JA; Garzon, F; Hardie, M; Heise, C; Jadayel, D; Judson, IR; Louie, S; Marriott, C; Michelson, G; Molife, R; Morrison, R; Sarker, D, 2008
)
0.35
"The noncompartmental pharmacokinetic parameters for plasma concentrations of aripiprazole and its active metabolite dehydro-aripiprazole were determined."( Pharmacokinetics and tolerability of intramuscular, oral and intravenous aripiprazole in healthy subjects and in patients with schizophrenia.
Boulton, DW; Kollia, G; Komoroski, B; Kovalick, LJ; Mallikaarjun, S; Reeves, RA; Sharma, A, 2008
)
0.35
" In study 2, the proportionality of the C(max) and AUC to doses ranging from 1 mg to 45 mg suggests a linear pharmacokinetic profile for intramuscular aripiprazole."( Pharmacokinetics and tolerability of intramuscular, oral and intravenous aripiprazole in healthy subjects and in patients with schizophrenia.
Boulton, DW; Kollia, G; Komoroski, B; Kovalick, LJ; Mallikaarjun, S; Reeves, RA; Sharma, A, 2008
)
0.35
" PHARMACOKINETIC ANALYSES: Noncompartmental pharmacokinetic analysis was performed using plasma aripiprazole and dehydro-aripiprazole concentration-time data."( Effects of hepatic or renal impairment on the pharmacokinetics of aripiprazole.
Boulton, DW; Bramer, SL; Mallikaarjun, S; Shoaf, SE, 2008
)
0.35
"Study 1 (hepatic impairment study): apparent oral clearance of unbound drug (CL/Fu) and the maximum plasma concentration (Cmax) of aripiprazole; Study 2 (renal impairment study): CL/Fu, Cmax and renal clearance (CL(R))."( Effects of hepatic or renal impairment on the pharmacokinetics of aripiprazole.
Boulton, DW; Bramer, SL; Mallikaarjun, S; Shoaf, SE, 2008
)
0.35
" Two studies evaluated pharmacokinetic (PK) interactions among EVG and RTV-boosted tipranavir (TPV/r) or darunavir (DRV/r)."( Effect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravir.
Enejosa, J; Hinkle, J; Kearney, BP; Mack, R; Mathias, AA; Piliero, PJ; Sekar, V; Shen, G; Tomaka, F, 2008
)
0.35
" Studies were powered to conclude lack of an interaction if the 90% confidence interval for the geometric mean ratios of the AUCtau and Cmax for EVG, TPV, and DRV were within predefined no-effect boundaries."( Effect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravir.
Enejosa, J; Hinkle, J; Kearney, BP; Mack, R; Mathias, AA; Piliero, PJ; Sekar, V; Shen, G; Tomaka, F, 2008
)
0.35
" On coadministration, AUCtau and Cmax of EVG and TPV and EVG and DRV were within prespecified no-effect boundaries versus treatment alone; trough concentrations were also not substantially altered."( Effect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravir.
Enejosa, J; Hinkle, J; Kearney, BP; Mack, R; Mathias, AA; Piliero, PJ; Sekar, V; Shen, G; Tomaka, F, 2008
)
0.35
" Blood samples were collected for pharmacokinetic analysis of ADTs."( The pharmacokinetics of standard antidepressants with aripiprazole as adjunctive therapy: studies in healthy subjects and in patients with major depressive disorder.
Balch, AH; Berman, RM; Boulton, DW; Mallikaarjun, S; Patel, CG; Reeves, RA; Royzman, K, 2010
)
0.36
" The mechanisms responsible for the tissue-selective activity of SARMs are not fully understood, and the pharmacokinetic (PK)/pharmacodynamic (PD) relationships are poorly described."( Pharmacokinetics and pharmacodynamics of LGD-3303 [9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator.
Chang, WY; Chen, Y; Hill, R; Lee, KJ; Lee, YH; López, FJ; Meglasson, MD; O'Brien, Z; Rix, P; Vajda, EG, 2009
)
0.35
"The aims of this study were to develop a combined population pharmacokinetic model for both aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients and to identify to what extent the genetic polymorphisms of cytochrome P450 (CYP) enzymes contribute to the variability in pharmacokinetics (PK)."( Population pharmacokinetic modelling of aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients.
Bahk, WM; Cho, JY; Jang, IJ; Kang, DH; Kim, JR; Kim, YK; Kwon, JS; Seo, HB; Shin, SG; Yu, KS, 2008
)
0.35
"A population pharmacokinetic analysis was performed using NONMEM software based on 141 plasma concentrations at steady state from 80 patients receiving multiple oral doses of aripiprazole (10-30 mg day(-1))."( Population pharmacokinetic modelling of aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients.
Bahk, WM; Cho, JY; Jang, IJ; Kang, DH; Kim, JR; Kim, YK; Kwon, JS; Seo, HB; Shin, SG; Yu, KS, 2008
)
0.35
"This population pharmacokinetic model provided an adequate fit to the data for both aripiprazole and dehydroaripiprazole in psychiatric patients."( Population pharmacokinetic modelling of aripiprazole and its active metabolite, dehydroaripiprazole, in psychiatric patients.
Bahk, WM; Cho, JY; Jang, IJ; Kang, DH; Kim, JR; Kim, YK; Kwon, JS; Seo, HB; Shin, SG; Yu, KS, 2008
)
0.35
" The developed method was successfully applied to the pharmacokinetic study of bis(12)-hupyridone after intravenous administration of 5mg/kg and intraperitoneal administration of 10 and 20mg/kg in rats."( Development and validation of an HPLC-DAD method for bis(12)-hupyridone and its application to a pharmacokinetic study.
Carlier, PR; Chan, K; Cheung, MC; Gu, ZM; Han, YF; Huang, M; Li, WM; Wang, YT; Yu, H; Zuo, Z, 2009
)
0.35
" Blood samples were collected on Days -1 and 14 for determination of lamotrigine steady-state pharmacokinetic parameters."( A non-randomized study to investigate the effects of the atypical antipsychotic aripiprazole on the steady-state pharmacokinetics of lamotrigine in patients with bipolar I disorder.
Balch, AH; Benson, J; Boulton, DW; Carlson, BX; Croop, R; Mallikaarjun, S; Schieber, FC, 2009
)
0.35
" Lack of pharmacokinetic alteration bounds for 90% confidence intervals (CI) about the geometric mean ratio (GMR; coadministration versus alone) were 70-143% for elvitegravir and ritonavir pharmacokinetics (maximum concentration [C(max)], concentration at the end of the dosing interval [C(tau)] and area under the plasma concentration-time curve [AUC(tau); 0-24 h] and 80-125% for etravirine pharmacokinetics (AUC(tau) 0-12 h)."( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine.
Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008
)
0.35
" Elvitegravir pharmacokinetic GMR was 6-7% higher following elvitegravir/r plus etravirine dosing versus elvitegravir/r."( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine.
Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008
)
0.35
" This article focuses on the standardization of drug analysis in bone, the extent and rate of bone penetration of antibacterials, and the design, evaluation and reporting techniques of pharmacokinetic studies of bone penetration."( Penetration of antibacterials into bone: pharmacokinetic, pharmacodynamic and bioanalytical considerations.
Bulitta, JB; Holzgrabe, U; Kinzig, M; Landersdorfer, CB; Sörgel, F, 2009
)
0.35
"Pharmacokinetic and pharmacodynamic interactions between carbamazepine and aripiprazole were studied in 18 inpatients with schizophrenia being treated with aripiprazole."( Pharmacokinetic and pharmacodynamic interactions between carbamazepine and aripiprazole in patients with schizophrenia.
Kondo, T; Mihara, K; Nagai, G; Nakamura, A; Suzuki, T, 2009
)
0.35
"The pharmacokinetic (PK) interaction between ritonavir-boosted elvitegravir (elvitegravir/r) and maraviroc was evaluated."( Pharmacokinetic interaction of ritonavir-boosted elvitegravir and maraviroc.
Abel, S; Hui, J; Kearney, BP; Ramanathan, S; Tweedy, S; West, S, 2010
)
0.36
" Lack of PK alteration was defined as 90% confidence intervals for ratio of geometric least squares means ratio (coadministration:alone) between 70% and 143% for elvitegravir and ritonavir Cmax (maximum concentration), Ctau (trough), and AUCtau (area under plasma concentration-time curve; 0-24 hours); for maraviroc, given a 100% increase in Cmax and AUCtau (0-12 hours); the predicted 90% confidence intervals were 162% to 247% and 136% to 295%, respectively."( Pharmacokinetic interaction of ritonavir-boosted elvitegravir and maraviroc.
Abel, S; Hui, J; Kearney, BP; Ramanathan, S; Tweedy, S; West, S, 2010
)
0.36
" The peak time and elimination half-life of nemonoxacin were 1 to 2 h and 9 to 16 h, respectively."( Dose escalation study of the safety, tolerability, and pharmacokinetics of nemonoxacin (TG-873870), a novel potent broad-spectrum nonfluorinated quinolone, in healthy volunteers.
Ajayi, F; Aronstein, WS; Chang, LW; Chung, DT; Hsu, CH; Kuzmak, B; Lin, L; Lyon, RA; Tsai, CY, 2010
)
0.36
" Pharmacokinetic parameters were determined using a noncompartmental method."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" No significant sequence, subject, formulation, or period effects were detected for any pharmacokinetic parameter."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" There was no evidence that rebamipide pharmacokinetic parameters were influenced by genetic polymorphisms in the ABCB1 gene (exons 21 and 26)."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" Plural simultaneously - operant pharmacodynamic mechanisms may explain catatonia of unclear etiology and reconcile a seemingly contradictory literature (e."( Catatonia and CPK elevation in neurosyphilis: role of plural pharmacodynamic mechanisms.
Carter, WG; Lauterbach, EC; Norris, BK; Shillcutt, SD, 2009
)
0.35
" Pharmacokinetic sampling was performed for 36 hr after the first dose and leukemic blasts were collected pre-treatment and at steady state for determination of FTase activity."( Phase 1 trial and pharmacokinetic study of the farnesyl transferase inhibitor tipifarnib in children and adolescents with refractory leukemias: a report from the Children's Oncology Group.
Adamson, PC; Arceci, RJ; Balis, FM; Blaney, SM; Fox, E; Goodspeed, W; Goodwin, A; Jayaprakash, N; Widemann, BC; Wright, JJ; Zannikos, P, 2011
)
0.37
"Of 29 patients enrolled, 18 were fully evaluable for toxicity, and 23 for response; 26 had pharmacokinetic and pharmacodynamic sampling."( Phase 1 trial and pharmacokinetic study of the farnesyl transferase inhibitor tipifarnib in children and adolescents with refractory leukemias: a report from the Children's Oncology Group.
Adamson, PC; Arceci, RJ; Balis, FM; Blaney, SM; Fox, E; Goodspeed, W; Goodwin, A; Jayaprakash, N; Widemann, BC; Wright, JJ; Zannikos, P, 2011
)
0.37
" This method was applied to pharmacokinetic study in human volunteers and patients taking aripiprazole."( A sensitive column-switching HPLC method for aripiprazole and dehydroaripiprazole and its application to human pharmacokinetic studies.
Akamine, Y; Inoue, Y; Kojima, M; Uno, T; Yasui-Furukori, N, 2010
)
0.36
" In both populations, the average maximum serum concentration (Cmax) of indacaterol was observed at the first sampling time point and pharmacokinetic profiles were similar between populations."( Efficacy, safety and pharmacokinetics of indacaterol in Caucasian and Japanese patients with chronic obstructive pulmonary disease: a comparison of data from two randomized, placebo-controlled studies.
Hosoe, M; Kramer, B; Lawrence, D; Matsushima, S; Woessner, R, 2011
)
0.37
"Indacaterol provided 24-hour bronchodilation with a fast onset of action and similar pharmacokinetic and safety profiles in Caucasian and Japanese patients."( Efficacy, safety and pharmacokinetics of indacaterol in Caucasian and Japanese patients with chronic obstructive pulmonary disease: a comparison of data from two randomized, placebo-controlled studies.
Hosoe, M; Kramer, B; Lawrence, D; Matsushima, S; Woessner, R, 2011
)
0.37
" The terminal elimination phase with a half-life of 50 - 63 h could only be seen for doses of 1,000 µg or higher."( Safety, tolerability and pharmacokinetics of single escalating doses of indacaterol, a once-daily beta2-agonist bronchodilator, in subjects with COPD.
Brookman, L; Hmissi, A; Kaiser, G; Pascoe, S; Perry, S; Pleskow, W; Reynolds, C, 2011
)
0.37
" Because elvitegravir is metabolized primarily by cytochrome P450 (CYP) 3A enzymes, coadministration with a strong CYP3A inhibitor such as ritonavir or cobicistat (also known as GS-9350), an investigational pharmacoenhancer, substantially increases (boosts) elvitegravir plasma exposures and prolongs its elimination half-life to ∼9."( Clinical pharmacokinetic and pharmacodynamic profile of the HIV integrase inhibitor elvitegravir.
German, P; Kearney, BP; Mathias, AA; Ramanathan, S, 2011
)
0.37
" The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents."( Pharmacokinetics and metabolism update for some recent antipsychotics.
Caccia, S, 2011
)
0.37
"Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not."( Pharmacokinetics and metabolism update for some recent antipsychotics.
Caccia, S, 2011
)
0.37
"The bactericidal activity and resistance selectivity of garenoxacin against Streptococcus pneumoniae with mutations in ParC (S79F) or both GyrA (S81F) and ParC (D83Y and K137N) were investigated using in vitro pharmacokinetic models simulating plasma concentrations for a standard clinical regimen [400mg once daily (q."( In vitro pharmacodynamic evaluation of garenoxacin against quinolone-resistant Streptococcus pneumoniae.
Fukuda, Y; Nomura, N; Shinmura, Y; Sugiura, Y; Takahata, M, 2012
)
0.38
" Typically, studies of antipsychotics have applied pharmacodynamic (PD) modeling alone to characterize the relationship between antipsychotic dose and its effect on the brain."( Predicting brain occupancy from plasma levels using PET: superiority of combining pharmacokinetics with pharmacodynamics while modeling the relationship.
Howes, OD; Jang, IJ; Jeong, JM; Kapur, S; Kim, BH; Kim, E; Kwon, JS; Lee, JS; Shin, SG; Turkheimer, FE, 2012
)
0.38
" The method was successfully applied to a pharmacokinetic study enrolling 12 healthy Chinese volunteers administered nemonoxacin malate capsules."( A liquid chromatography-tandem mass spectrometry assay for the determination of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, in human plasma and urine and its application to a single-dose pharmacokinetic study in healthy Chinese volunteers.
Guo, B; Shi, Y; Tsai, CY; Wu, X; Yu, J; Zhang, J, 2012
)
0.38
"This study was conducted primarily to improve the solubility of rebamipide, a poorly water-soluble anti-ulcer drug, using novel ternary solid dispersion (SD) systems and secondly to evaluate the effect of solubility enhancement on its pharmacokinetic (PK) and pharmacodynamic (PD) profile."( Physicochemical, pharmacokinetic and pharmacodynamic evaluations of novel ternary solid dispersion of rebamipide with poloxamer 407.
Chi, SC; Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2013
)
0.39
" The elimination half-life was 10-12 hours."( Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses.
Cao, G; Guo, B; Shi, Y; Wu, X; Yu, J; Zhang, J; Zhang, Y, 2012
)
0.38
" The NLME model analyzed pharmacokinetic data from nine indacaterol studies; the LME model analyzed peak (C(max)) and trough (C(min)) serum concentration using data from four of these studies."( Systemic pharmacokinetics of indacaterol, an inhaled once-daily long-acting beta2-agonist, in different ethnic populations.
Hara, H; Matsushima, S; Matthews, I; Pinault, G; Sekiguchi, K; Wilkins, J; Woessner, R, 2012
)
0.38
"In the all-Asian study, indacaterol serum concentration-time pharmacokinetic profiles in Japanese patients (n = 102) were similar to those in the overall population (n = 229)."( Systemic pharmacokinetics of indacaterol, an inhaled once-daily long-acting beta2-agonist, in different ethnic populations.
Hara, H; Matsushima, S; Matthews, I; Pinault, G; Sekiguchi, K; Wilkins, J; Woessner, R, 2012
)
0.38
"No ethnicity effect was observed on indacaterol systemic pharmacokinetic profile for Japanese patients when compared with the overall Asian patient population or with the Caucasian patient population."( Systemic pharmacokinetics of indacaterol, an inhaled once-daily long-acting beta2-agonist, in different ethnic populations.
Hara, H; Matsushima, S; Matthews, I; Pinault, G; Sekiguchi, K; Wilkins, J; Woessner, R, 2012
)
0.38
" The main pharmacokinetic parameters were T(max) = (4."( Development and validation of an LC-ESI-MS method for quantitative determination of aripiprazole in human plasma and an application to pharmacokinetic study.
Bapuji, AT; Mukkanti, K; Raju, DR; Ravikiran, HL; Ravinder, S; Reddy, DC,
)
0.13
" Pharmacokinetic simulation suggested in vivo relevance of CYP3A4 inhibition by DX-619."( Effect of the fluoroquinolone antibacterial agent DX-619 on the apparent formation and renal clearances of 6β-hydroxycortisol, an endogenous probe for CYP3A4 inhibition, in healthy subjects.
Imamura, Y; Inoue, K; Izumi, T; Kurihara, A; Kusuhara, H; Murayama, N; Okudaira, N; Sugiyama, Y; Yuasa, H, 2013
)
0.39
" The method was successfully applied to human pharmacokinetic study of urapidil and aripiprazole in healthy human male volunteers."( Liquid chromatography-tandem mass spectrometry method for simultaneous quantification of urapidil and aripiprazole in human plasma and its application to human pharmacokinetic study.
Ambavaram, VB; Gajulapalle, M; Kalluru, GR; Nandigam, V; Vemula, M, 2013
)
0.39
" No clinically relevant systemic pharmacodynamic effects were observed."( Pharmacodynamics of GSK961081, a bi-functional molecule, in patients with COPD.
Ambery, C; Bateman, ED; Kornmann, O; Norris, V, 2013
)
0.39
" When the MIC is high, the time (T) dependency is important and the valid PK/PD index should be the cumulative percentage of a 24-h period in which the drug concentration exceeds the MIC under steady-state pharmacokinetic conditions (f%T>MIC), which means that to split the maximum daily dose into several separate doses will benefit the eradication of the bacteria."( Pharmacokinetics and pharmacodynamics of nemonoxacin against Streptococcus pneumoniae in an in vitro infection model.
Cao, YR; Chen, YC; Guo, QL; Hu, JL; Huang, J; Liang, W; Liu, XF; Wu, XJ; Zhang, J; Zhang, SJ; Zhang, YY; Zhao, M; Zhu, DM, 2013
)
0.39
"We performed a within-subject open-labeled pharmacokinetic and pharmacodynamic study in 17 HIV-seronegative subjects stabilized on at least 2 weeks of buprenorphine/naloxone therapy."( The pharmacokinetic and pharmacodynamic interactions between buprenorphine/naloxone and elvitegravir/cobicistat in subjects receiving chronic buprenorphine/naloxone treatment.
Bruce, RD; Custodio, JM; Friedland, GH; Kearney, BP; Ramanathan, S; Rhee, MS; Wei, LX; Winkle, P, 2013
)
0.39
"6 hr*ng/mL) and mean Cmax (8."( The pharmacokinetic and pharmacodynamic interactions between buprenorphine/naloxone and elvitegravir/cobicistat in subjects receiving chronic buprenorphine/naloxone treatment.
Bruce, RD; Custodio, JM; Friedland, GH; Kearney, BP; Ramanathan, S; Rhee, MS; Wei, LX; Winkle, P, 2013
)
0.39
" Here we tested the pharmacodynamic consequences of these properties in a P-gp deficient mouse model by studying the effects of aripiprazole and of ziprasidone on motor coordination."( Pharmacodynamic effects of aripiprazole and ziprasidone with respect to p-glycoprotein substrate properties.
Frisch, J; Hiemke, C; Holthoewer, D; Kirschbaum, KM; Schmitt, U, 2013
)
0.39
"Evidence was given that P-gp substrate properties have pharmacodynamic consequences for aripiprazole but not for ziprasidone and thus affect dopamine receptor related motor behaviour."( Pharmacodynamic effects of aripiprazole and ziprasidone with respect to p-glycoprotein substrate properties.
Frisch, J; Hiemke, C; Holthoewer, D; Kirschbaum, KM; Schmitt, U, 2013
)
0.39
" Lack of PK alteration was defined as 90% confidence intervals about the geometric least squares means ratio (coadministration:alone) being within 70%-143% for elvitegravir Cmax (maximum concentration), Ctau (trough), and AUCtau (area under plasma concentration-time curve; 0-24 hours); cobicistat PK were explored."( Pharmacokinetics of once-daily boosted elvitegravir when administered in combination with acid-reducing agents.
Cheng, A; Kearney, BP; Koziara, J; Mathias, A; Ramanathan, S; Shen, G; Wei, X, 2013
)
0.39
"  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
)
0.4
" In contrast, plasma concentrations following administration of aripiprazole once-monthly at a dose of 200mg were below the therapeutic range and pharmacokinetic parameters were not proportional to the administered dose compared with the 300 mg and 400mg doses."( Pharmacokinetics, tolerability and safety of aripiprazole once-monthly in adult schizophrenia: an open-label, parallel-arm, multiple-dose study.
Bricmont, P; Carson, W; Fleischhacker, WW; Forbes, RA; Kane, JM; Mallikaarjun, S; McQuade, R; Sanchez, R, 2013
)
0.39
"This review considers indacaterol in chronic obstructive pulmonary disease patients, in whom it is rapidly absorbed into the systemic circulation with serum levels measurable after 5 min and Cmax being reached approximately 15 min post-dose."( Use of indacaterol for the treatment of COPD: a pharmacokinetic evaluation.
Calzetta, L; Cazzola, M; Matera, MG; Page, CP, 2014
)
0.4
" 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
)
0.4
" The pharmacokinetic interaction between cobicistat-boosted elvitegravir (EVG/co) and rosuvastatin was evaluated."( Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin.
Andrews, J; Cheng, A; Custodio, JM; Hao, J; Kearney, BP; Lepist, EI; Ling, KH; Ramanathan, S; Ray, AS; Wang, H, 2014
)
0.4
" In dose response sessions, all doses were given 1 hr apart in ascending order for pharmacodynamic and pharmacokinetic assessment."( Aripiprazole effects on self-administration and pharmacodynamics of intravenous cocaine and cigarette smoking in humans.
Campbell, C; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2014
)
0.4
" EVG/co (150/150 mg) was administered once daily for 10 days, followed by pharmacokinetic (PK) sampling."( Pharmacokinetics and safety of boosted elvitegravir in subjects with hepatic impairment.
Custodio, JM; Kearney, BP; Ling, KH; Ramanathan, S; Rhee, M; Shen, G, 2014
)
0.4
" In this open-label, randomized, three-way crossover study, the pharmacokinetic profiles of elvitegravir, cobicistat, emtricitabine, and tenofovir were evaluated when administered with a standard breakfast, under fasting conditions, or with a nutritional protein-rich drink."( Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Matsuki, S; Nishino, N; Shiomi, M, 2014
)
0.4
" The pharmacokinetic parameters were analyzed using non-compartmental analysis and included C max, T max, and AUC0-24h on Day 1 and AUC0-24h,ss, C max,ss, C min,ss, C av,ss, T max,ss, T 1/2, T 1/2,acc, CL/F, V z/F, and R acc on Day 14 (after repeated once-daily doses)."( Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteers.
Emotte, C; Jiang, J; Khindri, S; Li, L; Li, R; Pei, H; Woessner, R; Yin, H, 2015
)
0.42
" Pharmacodynamic assessments included whole body plethysmography to determine the bronchodilatory effect by means of airway conductance and resistance."( First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of abediterol (LAS100977), a novel long-acting Β2 -agonist.
de Miquel, G; Jimenez, E; Massana, E; Ruiz, S; Seoane, B; Timmer, W, 2014
)
0.4
" This first-in-human study was aimed at assessing the safety, tolerability, and pharmacokinetic properties of intravenous nemonoxacin in healthy Chinese volunteers."( Safety, tolerability, and pharmacokinetics of intravenous nemonoxacin in healthy chinese volunteers.
Cao, GY; Chen, YC; Guo, BN; Shi, YG; Wu, JF; Wu, XJ; Yu, JC; Zhang, J; Zhang, YY, 2014
)
0.4
"After single doses of setrobuvir (400-3000 mg) to volunteers in a fasted state, peak Cmax and AUC0-∞ increased in a less than dose-proportional manner."( Pharmacokinetics and pharmacodynamics of setrobuvir, an orally administered hepatitis C virus non-nucleoside analogue inhibitor.
Appleman, JR; Crowley, CA; Freddo, JL; Mallalieu, NL; Rahimy, MH; Smith, PF, 2014
)
0.4
" Clinical investigation in healthy volunteers and cancer patients was undertaken to evaluate its pharmacokinetic properties and early safety profile."( Pharmacokinetic/pharmacodynamic-based decision making in the development of MK-0888, a VEGFR-2/FLT-3 kinase inhibitor.
Agrawal, NG; Friedman, EJ; Iwamoto, M; Sepp-Lorenzino, L; Talaty, JE; Wagner, JA, 2015
)
0.42
" Pharmacokinetics: After single-dose administration, MK-0888 was readily absorbed with a T(max) of 4-5 h and a half-life of 11."( Pharmacokinetic/pharmacodynamic-based decision making in the development of MK-0888, a VEGFR-2/FLT-3 kinase inhibitor.
Agrawal, NG; Friedman, EJ; Iwamoto, M; Sepp-Lorenzino, L; Talaty, JE; Wagner, JA, 2015
)
0.42
"The pharmacokinetic behavior of MK-0888 does not support continued development."( Pharmacokinetic/pharmacodynamic-based decision making in the development of MK-0888, a VEGFR-2/FLT-3 kinase inhibitor.
Agrawal, NG; Friedman, EJ; Iwamoto, M; Sepp-Lorenzino, L; Talaty, JE; Wagner, JA, 2015
)
0.42
" Pharmacokinetic parameters were derived from plasma concentrations of aripiprazole and its active metabolite, dehydro-aripiprazole, obtained over 16 days after each aripiprazole administration."( Evaluation of Potential Pharmacokinetic Drug-Drug Interaction between Armodafinil and Aripiprazole in Healthy Adults.
Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015
)
0.42
"Of 36 subjects enrolled, 24 were evaluable for pharmacokinetic analysis."( Evaluation of Potential Pharmacokinetic Drug-Drug Interaction between Armodafinil and Aripiprazole in Healthy Adults.
Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015
)
0.42
" Herein we developed and validated a quantitative HPLC-MS/MS analytical method for one of the lead novel anticancer makaluvamine analog, TCBA-TPQ, and conducted a pharmacokinetic study in laboratory rats."( Development and validation of an HPLC-MS/MS analytical method for quantitative analysis of TCBA-TPQ, a novel anticancer makaluvamine analog, and application in a pharmacokinetic study in rats.
Li, DD; Nag, S; Qin, JJ; Velu, SE; Voruganti, S; Wang, W; Xu, S; Yu, JX; Zhang, R, 2015
)
0.42
"This article reviews the clinical pharmacology, pharmacodynamic and pharmacokinetic (PK) properties, clinical efficacy and tolerability, drug interactions, and dosing and administration of cobicistat."( Cobicistat: Review of a Pharmacokinetic Enhancer for HIV Infection.
Gauthier, TP; Schafer, JJ; Sherman, EM; Unger, NR; Worley, MV, 2015
)
0.42
" Secondary outcomes were absolute change from baseline in sweat chloride concentrations and bodyweight, body-mass index (BMI), and height Z scores, and pharmacokinetic parameter estimation of ivacaftor."( Safety, pharmacokinetics, and pharmacodynamics of ivacaftor in patients aged 2-5 years with cystic fibrosis and a CFTR gating mutation (KIWI): an open-label, single-arm study.
Cooke, J; Cunningham, S; Davies, JC; Green, Y; Harris, WT; Lapey, A; Regelmann, WE; Robertson, S; Rosenfeld, M; Sawicki, GS; Southern, KW, 2016
)
0.43
" Results of ivacaftor pharmacokinetics suggested that exposure was similar to that reported in adults (median Cmin were 536 ng/mL for the 50 mg dose; 580 ng/mL for the 75 mg dose; median ivacaftor AUC values were 9840 ng × h/mL and 10 200 ng × h/mL, respectively)."( Safety, pharmacokinetics, and pharmacodynamics of ivacaftor in patients aged 2-5 years with cystic fibrosis and a CFTR gating mutation (KIWI): an open-label, single-arm study.
Cooke, J; Cunningham, S; Davies, JC; Green, Y; Harris, WT; Lapey, A; Regelmann, WE; Robertson, S; Rosenfeld, M; Sawicki, GS; Southern, KW, 2016
)
0.43
" We describe here a study designed to assess any pharmacokinetic (PK) and/or biopharmaceutical interaction between indacaterol and mometasone furoate when administered via the Breezhaler(®) device, either alone or in a free or fixed combination (QMF149) in healthy adult subjects."( Pharmacokinetics of indacaterol and mometasone furoate delivered alone or in a free or fixed dose combination in healthy subjects.
Calder, N; Febbraro, S; Fuhr, R; Hara, H; Khindri, S; Machineni, S; Majumdar, T; Vaidya, SS; Woessner, R, 2016
)
0.43
"Elvitegravir and cobicistat pharmacokinetic variability appears to be mainly explained by drug-drug interactions that may be encountered in routine clinical practice."( Population pharmacokinetic analysis of elvitegravir and cobicistat in HIV-1-infected individuals.
Aouri, M; Barceló, C; Buclin, T; Cavassini, M; Csajka, C; Decosterd, LA; Gaspar, F; Guidi, M; Panchaud, A; Rotger, M, 2016
)
0.43
" A population pharmacokinetic (PK) analysis was performed to describe the PK profiles of indacaterol and glycopyrronium following the twice daily (b."( Population pharmacokinetics of IND/GLY (indacaterol/glycopyrronium) in COPD patients.
Bartels, C; Bieth, B; Demin, I; Gautier, A; Graham, G; Sechaud, R; Tillmann, HC, 2016
)
0.43
"There was no pharmacokinetic interaction when GSK961081 and FP were administered concurrently."( Pharmacokinetics and pharmacodynamics of GSK961081, a novel inhaled muscarinic antagonist β2 -agonist, and fluticasone propionate administered alone, concurrently and as a combination blend formulation in healthy volunteers.
Ambery, C; Norris, V; Riley, T, 2014
)
0.4
" The pharmacokinetic parameters (Cmax , AUCtau , and Ctau ) of elvitegravir were investigated at Day 10 after each treatment, together with safety and tolerability."( Pharmacokinetic and bioequivalence evaluation of single-tablet and separate-tablet regimens for once-daily cobicistat-boosted elvitegravir in healthy Japanese male subjects: A randomized, two-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Kumagai, Y; Matsuki, S; Nishino, N; Shiomi, M,
)
0.13
" Pharmacokinetic data were analyzed using noncompartmental methods."( Open-Label, Randomized, 6-Way Crossover, Single-Dose Study to Determine the Pharmacokinetics of Batefenterol (GSK961081) and Fluticasone Furoate When Administered Alone or in Combination.
Ambery, C; Daley-Yates, P; Riddell, K, 2016
)
0.43
" This review focuses on recent advances concerning quinolones and fluoroquinolones, we will be summarising chemical structure, mode of action, pharmacokinetic properties and toxicity."( Chemical structure and pharmacokinetics of novel quinolone agents represented by avarofloxacin, delafloxacin, finafloxacin, zabofloxacin and nemonoxacin.
Domokos, J; Kocsis, B; Szabo, D, 2016
)
0.43
" A precise method is required to quantify the drug concentration in biological matrices to study pharmacokinetic behavior and tissue distribution profile in animals and/or humans."( Simultaneous quantification of tenofovir, emtricitabine, rilpivirine, elvitegravir and dolutegravir in mouse biological matrices by LC-MS/MS and its application to a pharmacokinetic study.
Destache, CJ; Mandal, S; Prathipati, PK, 2016
)
0.43
" After the fifth AOM 400 injection, mean aripiprazole AUC(28d), C(max) and C(min) were 165 μg x h/ml, 331 ng/ml and 201 ng/ml, respectively, which were similar to previously published pharmacokinetic parameters after the fifth gluteal injection of AOM 400."( [Pharmacokinetics and safety of aripiprazole long-acting injection, following multiple deltoid administrations in schizophrenia patients in Japan].
Ishigooka, J; Nishiyama, K; Noda, T; Shima, T; Tadori, Y; Tamaru, N; Yamasaki, Y, 2016
)
0.43
"Between May 22, 2013, and July 22, 2014, we enrolled 50 participants, and all 50 received the assigned treatment; 24 participated in the intensive pharmacokinetic assessment."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
"The elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide regimen was well tolerated and achieved component plasma pharmacokinetic exposures similar to those in adults."( Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Batra, J; Chakraborty, R; Gaur, AH; Kizito, H; Kosalaraksa, P; Luesomboon, W; Myers, M; Porter, D; Prasitsueubsai, W; Quirk, E; Rakhmanina, N; Rassool, M; Rhee, MS; SenGupta, D; Shao, Y; Ting, L, 2016
)
0.43
"EVG is currently available as a single tablet regimen and requires cobisistat, a pharmacokinetic booster and CYP3A inhibitor to allow QD dosing."( How recent findings on the pharmacokinetics and pharmacodynamics of integrase inhibitors can inform clinical use.
Boffito, M; Chirwa, M; Elliot, E, 2017
)
0.46
" In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells."( Alterations in cellular pharmacokinetics and pharmacodynamics of elvitegravir in response to ethanol exposure in HIV-1 infected monocytic (U1) cells.
Kumar, S; Lukka, PB; Meibohm, B; Midde, NM; Sinha, N, 2017
)
0.46
"In this study, the population pharmacokinetic (PK) analysis of rebamipide (Reba) in healthy male Korean subjects was analyzed using the nonlinear mixed effects modeling method."( Population pharmacokinetic analysis of rebamipide in healthy Korean subjects with the characterization of atypical complex absorption kinetics.
Cho, HY; Lee, YB; Ngo, L; Tran, P; Yoo, HD, 2017
)
0.46
"The aim of this study was to determine the pharmacokinetic interaction between ivacaftor and ritonavir."( The pharmacokinetic interaction between ivacaftor and ritonavir in healthy volunteers.
Barry, MG; D'Arcy, DM; Liddy, AM; McLaughlin, G; Schmitz, S, 2017
)
0.46
" Three pharmacokinetic profiles were assessed for each volunteer: ivacaftor 150 mg alone (study A), ivacaftor 150 mg plus ritonavir 50 mg daily (study B), and ivacaftor 150 mg plus ritonavir 50 mg daily after two weeks of ritonavir 50 mg daily (study C)."( The pharmacokinetic interaction between ivacaftor and ritonavir in healthy volunteers.
Barry, MG; D'Arcy, DM; Liddy, AM; McLaughlin, G; Schmitz, S, 2017
)
0.46
"A literature search of MEDLINE was performed (1985 to April 2017) using the following search terms: cobicistat, ritonavir, pharmacokinetic, drug interactions, booster, pharmacokinetic enhancer, HIV, antiretrovirals."( Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences.
Hughes, CA; Phillips, EJ; Seet, J; Tseng, A; Wu, J, 2017
)
0.46
" Pharmacokinetic properties of the boosted antiretroviral can also affect interaction outcome with comedications."( Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences.
Hughes, CA; Phillips, EJ; Seet, J; Tseng, A; Wu, J, 2017
)
0.46
" typhimurium, there are no systematic review outlining the pharmacokinetic and pharmacodynamic parameters of quinolones."( Quinolones and Fluoroquinolones to Treat Salmonella Typhimurium: A Review of Metabolism and Pharmacokinetics.
Balasundaram, P; Karuppasamy, R; Veerappapillai, S, 2017
)
0.46
"Overall, the findings of this review highlight the importance of pharmacokinetic profiling of different quinolones in developing novel drugs to overcome drug resistance in the near future."( Quinolones and Fluoroquinolones to Treat Salmonella Typhimurium: A Review of Metabolism and Pharmacokinetics.
Balasundaram, P; Karuppasamy, R; Veerappapillai, S, 2017
)
0.46
"Intensive steady-state 24-h pharmacokinetic profiles after 150 mg of elvitegravir and 150 mg of cobicistat given orally in fixed dose combination once-daily were performed during the second trimester, third trimester, and postpartum."( Elvitegravir/cobicistat pharmacokinetics in pregnant and postpartum women with HIV.
Acosta, EP; Badell, ML; Barr, E; Best, BM; Burchett, S; Capparelli, EV; Chakhtoura, N; Mirochnick, M; Momper, JD; Park, K; Purswani, M; Shapiro, DE; Smith, E; Stek, A; Wang, J, 2018
)
0.48
" Blood samples for pharmacokinetic profiling of laquinimod, EE and LNG were collected on day 21 and day 22 of Cycles 1 and 3 pre-dose and multiple times post-dose."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
0.51
"The combination of COC and laquinimod treatment was found to be safe, tolerable, and devoid of any noticeable pharmacokinetic interaction."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
0.51
" The goals of this study were to evaluate the pharmacokinetic (PK) and population PK parameters of nemonoxacin and to provide the appropriate dose adjustment recommendations for patients with hepatic impairment."( Population Pharmacokinetics Study of Nemonoxacin Among Chinese Patients With Moderate Hepatic Impairment.
Chen, Y; Guo, B; Kang, Y; Li, Y; Wang, K; Wu, J; Xu, F; Yu, J; Zhang, J; Zhang, Y, 2019
)
0.51
" The developed method could be efficiently used for pharmacokinetic studies of dovitinib."( A New Validated HPLC-MS/MS Method for Quantification and Pharmacokinetic Evaluation of Dovitinib, a Multi-Kinase Inhibitor, in Mouse Plasma.
Al-Shakliah, NS; Aljohar, HI; AlRabiah, H; Attia, SM; Attwa, MW; Kadi, AA; Mostafa, GA, 2020
)
0.56
" These results indicate that coadministration of laquinimod with moderate to strong inhibitors of CYP3A or strong inducers of CYP3A may give rise to significant pharmacokinetic drug interactions."( The Effect of CYP3A Induction and Inhibition on the Pharmacokinetics of Laquinimod, a Novel Neuroimmunomodulator.
Elgart, A; Greenblatt, DJ; Loupe, PS; Mimrod, D; Spiegelstein, O; Weiss, S; Zur, AA, 2020
)
0.56
" There was no clinically relevant pharmacokinetic interaction between IND, GLY and MF when administered as IND/GLY/MF."( Pharmacokinetics of indacaterol, glycopyrronium and mometasone furoate following once-daily inhalation as a combination in healthy subjects.
Abdallah, N; Drollmann, A; Ethell, B; Hahn, M; Heudi, O; Ignatenko, S; Jauernig, J; Last, S; Machineni, S; Radhakrishnan, R; Tillmann, HC; Vaidya, S, 2020
)
0.56
"To optimize the dosing regimen in patients with severe renal impairment based on population pharmacokinetic (PPK)/pharmacodynamic analysis."( Nemonoxacin dosage adjustment in patients with severe renal impairment based on population pharmacokinetic and pharmacodynamic analysis.
Chen, Y; Fan, Y; Guo, B; Hu, J; Kang, Y; Li, X; Li, Y; Liu, X; Lu, J; Wang, K; Wang, Y; Wu, H; Wu, J; Xu, X; Xue, J; Yu, J; Zeng, X; Zhang, J; Zhang, Y; Zhao, M, 2021
)
0.62
" Ivacaftor concentrations were measured in all blood samples in order to calculate the pharmacokinetic parameters for ivacaftor."( Pharmacokinetic interactions between ivacaftor and cytochrome P450 3A4 inhibitors in people with cystic fibrosis and healthy controls.
Heijerman, HGM; Sturm, R; van der Meer, R; Wilms, EB, 2021
)
0.62
"Clinical evidence suggests no clinically relevant pharmacokinetic interactions between indacaterol (IND), glycopyrronium (GLY) and mometasone furoate (MF)."( Population Pharmacokinetic Analysis of Indacaterol/Glycopyrronium/Mometasone Furoate After Administration of Combination Therapies Using the Breezhaler
Bartels, C; Jain, M; Tillmann, HC; Vaidya, S; Yu, J, 2021
)
0.62
"The final pharmacokinetic models were two-compartment disposition models with first-order elimination and sequential zero-order/first-order absorption (IND), with bolus administration and first-order elimination (GLY), and with mixed zero-order/first-order absorption and first-order elimination (MF)."( Population Pharmacokinetic Analysis of Indacaterol/Glycopyrronium/Mometasone Furoate After Administration of Combination Therapies Using the Breezhaler
Bartels, C; Jain, M; Tillmann, HC; Vaidya, S; Yu, J, 2021
)
0.62
" The pharmacokinetic profiles of MF were comparable for combination products at corresponding medium- or high-dose inhaled corticosteroids."( Population Pharmacokinetic Analysis of Indacaterol/Glycopyrronium/Mometasone Furoate After Administration of Combination Therapies Using the Breezhaler
Bartels, C; Jain, M; Tillmann, HC; Vaidya, S; Yu, J, 2021
)
0.62
" In this study, phenotype-related physiologically based pharmacokinetic models were developed and evaluated to suggest phenotype-guided dose adjustments."( Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach.
Abad-Santos, F; Hempel, G; Kneller, LA; Koller, D; Zubiaur, P, 2021
)
0.62
"Physiologically based pharmacokinetic models for single dose (oral and orodispersible formulation), multiple dose, and steady-state condition were built using trial data from genotyped healthy volunteers."( Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach.
Abad-Santos, F; Hempel, G; Kneller, LA; Koller, D; Zubiaur, P, 2021
)
0.62
"Physiologically based pharmacokinetic models were able to accurately predict the pharmacokinetics of aripiprazole and dehydro-aripiprazole according to CYP2D6 phenotypes, illustrated by a minimal bias and a good precision."( Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach.
Abad-Santos, F; Hempel, G; Kneller, LA; Koller, D; Zubiaur, P, 2021
)
0.62
" The present study describes the influence of GFJ, PJ and TJ on the pharmacokinetic parameters of BRX in rats."( Investigation of the impact of grapefruit juice, pomegranate juice and tomato juice on pharmacokinetics of brexpiprazole in rats using UHPLC-QTOF-MS.
Kate, AS; Rathod, R; Sahu, AK; Sengupta, P; Thakkar, D, 2021
)
0.62
" This study uses a whole-body physiologically based pharmacokinetic (PBPK) model to compare the pharmacokinetics of brexpiprazole in patients known to be extensive metabolizers (EMs) and poor metabolizers (PMs)."( Brexpiprazole Pharmacokinetics in CYP2D6 Poor Metabolizers: Using Physiologically Based Pharmacokinetic Modeling to Optimize Time to Effective Concentrations.
Bruno, CD; Chow, CR; Elmokadem, A; Greenblatt, DJ; Housand, C; Jordie, EB; Lesko, LJ, 2022
)
0.72
" There is an urgent need for reliable methods such as physiologically-based pharmacokinetic (PBPK) model to assist in the development of inhaled drugs."( Prediction of pharmacokinetic parameters of inhaled indacaterol formulation in healthy volunteers using physiologically-based pharmacokinetic (PBPK) model.
Chen, WJ; Cui, C; Guo, C; Huang, J; Lin, Y; Ou-Yang, CX; Pei, Q; Tang, C; Yang, GP; Yang, S; Yang, XY; Zou, C, 2022
)
0.72
" The PBPK model was established and the predicted plasma concentration curve was obtained by inputting the physicochemical properties of indacaterol and adjusting model parameters."( Prediction of pharmacokinetic parameters of inhaled indacaterol formulation in healthy volunteers using physiologically-based pharmacokinetic (PBPK) model.
Chen, WJ; Cui, C; Guo, C; Huang, J; Lin, Y; Ou-Yang, CX; Pei, Q; Tang, C; Yang, GP; Yang, S; Yang, XY; Zou, C, 2022
)
0.72
" CYP3A-mediated DDI of elexacaftor-tezacaftor-ivacaftor was evaluated using a physiologically-based pharmacokinetic modeling approach."( Physiologically-Based Pharmacokinetic-Led Guidance for Patients With Cystic Fibrosis Taking Elexacaftor-Tezacaftor-Ivacaftor With Nirmatrelvir-Ritonavir for the Treatment of COVID-19.
Almond, LM; Beringer, PM; Chung, PS; Hong, E; Rao, AP, 2022
)
0.72
" Our study investigated the FDA Adverse Event Reporting System and the pharmacodynamic CHEMBL database to further characterize TGA-induced ICDs."( Impulse Control Disorders by Dopamine Partial Agonists: A Pharmacovigilance-Pharmacodynamic Assessment Through the FDA Adverse Event Reporting System.
De Ponti, F; Fusaroli, M; Giunchi, V; Menchetti, M; Poluzzi, E; Raschi, E; Rimondini Giorgini, R, 2022
)
0.72
" In order to accelerate pediatric drug development, the US Food and Drug Administration (FDA) released a general advice letter to sponsors permitting the effectiveness of atypical antipsychotics for the treatment of schizophrenia in adults to be extrapolated to adolescents based on a pharmacokinetic (PK) analysis to support dose selection, plus a safety study."( Population Pharmacokinetic Analysis of Brexpiprazole to Support its Indication and Dose Selection in Adolescents With Schizophrenia.
Cahill, D; Kohegyi, E; Larsen, F; Raoufinia, A; Wang, X; Wang, Y; Ward, C; Zoubroulis, A, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"The present study evaluated the therapeutic effects of rebamipide alone and in combination with cimetidine on experimental gastritis established by the administration of 5 mM sodium taurocholate (TCA) for 6 months in rats."( Therapeutic effects of oral rebamipide and in combination with cimetidine on experimental gastritis in rats.
Fujimura, J; Haruma, K; Kajiyama, G; Kishimoto, S; Kobayashi, H; Machino, H; Sakurai, K; Shimamoto, T; Shimizu, S; Yamasaki, K, 1992
)
0.28
" When combined with amphotericin B (AmB), however, DU-6859a clearly enhanced the in vitro antifungal activity of AmB against Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, and Cryptococcus neoformans in microdilution checkerboard studies."( In vitro and in vivo antifungal activities of DU-6859a, a fluoroquinolone, in combination with amphotericin B and fluconazole against pathogenic fungi.
Kitamura, A; Nakajima, R; Sato, K; Someya, K; Tanaka, M, 1995
)
0.29
"The fluoroquinolones have been shown to interact with the hepatic metabolism of theophylline and increase serum theophylline concentrations."( Clinafloxacin-theophylline drug interaction.
Matuschka, PR; Vissing, RS, 1995
)
0.29
" Unfortunately, the emergence of multiple drug-resistant tuberculosis in many parts of the world is leading to a diversification of drug regimens and to the use of drugs that are more toxic per se and more likely to interact with others."( Clinically significant drug interactions with antituberculosis agents.
Davies, PD; Grange, JM; Winstanley, PA, 1994
)
0.29
" The effects of the drug alone and in combination with the non-inotropic PDE IV inhibitor rolipram were analysed using hearts from guinea-pigs and ferrets."( The inotropic mechanism of the phosphodiesterase inhibitor OPC 3911 alone and in combination with rolipram, studied in papillary muscles of ferret and guinea-pig and isolated myocytes of guinea-pig ventricular muscle.
Arlock, P; Lindgren, S; Mörner, SE, 1994
)
0.29
"Sparfloxacin and clinafloxacin alone and in combination with gentamicin, were evaluated for the treatment of experimental endocarditis in rabbits caused by ampicillin-resistant enterococci."( Sparfloxacin and clinafloxacin alone or in combination with gentamicin for therapy of experimental ampicillin-resistant enterococcal endocarditis in rabbits.
Donabedian, SA; Perri, MB; Thal, LA; Vazquez, J; Zervos, MJ, 1993
)
0.29
"The in vitro activity of rufloxacin, alone and in combination with its metabolite (MF 922) against common respiratory and urinary tract pathogens and anaerobes was assessed."( Bactericidal activity, morphological alterations, and synergistic interactions of rufloxacin, a new fluoroquinolone, alone and in combination with its N-desmethylate D derivative (MF 922).
Debbia, EA; Marchese, A; Pesce, A; Schito, GC,
)
0.13
" The potential therapeutic activities of these agents both alone and combined with ethambutol were evaluated in a human macrophage test system and in the beige mouse animal test system with MAC strain 101."( Activities of bay Y 3118, levofloxacin, and ofloxacin alone or in combination with ethambutol against Mycobacterium avium complex in vitro, in human macrophages, and in beige mice.
Barbara-Burnham, L; Bermudez, LE; Inderlied, CB; Kolonoski, P; Wu, M; Young, LS, 1996
)
0.29
"Ten clinical isolates of Streptococcus pneumoniae (six intermediately penicillin-sensitive, one penicillin-resistant and three penicillin-sensitive strains) were studied by kill-kinetic experiments using sparfloxacin alone and in combination with amoxicillin."( Bactericidal effect of sparfloxacin alone and in combination with amoxicillin against Streptococcus pneumoniae as determined by kill-kinetic studies.
Barakett, V; Delisle, F; Lesage, D; Petit, JC; Richard, G,
)
0.13
"The in vitro activity of DU-6859a (DU) alone and in combination with various antimicrobials was evaluated against multiresistant enterococci including some isolates with defined gyrA mutations."( Bactericidal activity of the fluoroquinolone DU-6859a alone and in combination with other antimicrobial agents against multiresistant enterococci.
Erdem, I; Korten, V; Murray, BE, 1996
)
0.29
"The purpose of the present clinical studies was to determine the clinical efficacy of a combined parenteral and oral treatment with Bisolvon in combination with antibiotics in bovines suffering from acute respiratory disease."( [Treatment of acute respiratory tract diseases in cattle with Bisolvon in combination with either enrofloxacin, cefquinome, ceftiofur or florfenicol].
Hamel, U; Philipp, H; Quirke, JF; Schmidt, H, 1998
)
0.3
" It is concluded that DU-6859a and trovafloxacin are very potent against enterococci, especially when combined with gentamicin."( In vitro activity of quinupristin/dalfopristin and newer quinolones combined with gentamicin against resistant isolates of Enterococcus faecalis and Enterococcus faecium.
Giamarellos-Bourboulis, EJ; Giamarellou, H; Grecka, P; Sambatakou, H, 1998
)
0.3
" When eliprodil was combined with an ineffective dose of L-701,324 (2."( Anticonvulsant effects of eliprodil alone or combined with the glycineB receptor antagonist L-701,324 or the competitive NMDA antagonist CGP 40116 in the amygdala kindling model in rats.
Ebert, U; Löscher, W; Wlaź, P, 1999
)
0.3
"The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in goats given enrofloxacin alone or in combination with probenecid."( Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin in goats given enrofloxacin alone and in combination with probenecid.
Ahmad, AH; Malik, JK; Ramesh, S; Rao, GS; Sharma, LD; Tripathi, HC, 2002
)
0.31
"Convulsant activity of pazufloxacin mesilate (PZFX mesilate), a new quinolone antibacterial agent for intravenous use, in combination with nonsteroidal anti-inflammatory drug (NSAID) was investigated in mice after intravenous or intracerebroventricular administration."( [Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration].
Fukuda, H; Kawamura, Y, 2002
)
0.31
" The potential of M17055, a novel diuretic candidate, to affect the activities of human CYP enzymes, alter the plasma unbound fraction and compete with concomitant drugs in renal secretion as part of an assessment for drug-drug interactions in metabolism, distribution and excretion was investigated."( Studies on the metabolic fate of M17055, a novel diuretic (6). Assessment for drug-drug interactions of M17055 in metabolism, distribution and excretion.
Ida, K; Matsumoto, S; Naba, H; Nagasawa, K; Nakai, K; Nakajima, H; Nakanishi, T; Ogihara, T; Ohzawa, N, 2002
)
0.31
" Amphotericin B was combined with flucytosine and ciprofloxacin, whereas itraconazole was combined with ciprofloxacin, levofloxacin, lomefloxacin and sulfadiazine."( In vitro activity of amphotericin B and itraconazole in combination with flucytosine, sulfadiazine and quinolones against Exophiala spinifera.
Afeltra, J; de Hoog, GS; Rijs, AJ; Verweij, PE; Vitale, RG, 2003
)
0.32
"To assess the feasibility of administering tipifarnib, an oral nonpeptidomimetic competitive inhibitor of farnesyltransferase, in combination with gemcitabine and recommend doses for disease-directed clinical trials."( A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Eckhardt, SG; Gentner, L; Goetz, A; Hammond, LA; Izbicka, E; McCreery, H; Mori, M; Patnaik, A; Richards, H; Rowinsky, EK; Rybak, ME; Schwartz, G; Takimoto, CH; Terada, K; Tolcher, AA; Zhang, S, 2003
)
0.32
"The aims of this study were to determine the maximum-tolerated dose (MTD), toxicity profile, and pharmacokinetics of irinotecan given with oral R115777 (tipifarnib), a farnesyl protein transferase inhibitor."( Phase I and pharmacokinetic study of irinotecan in combination with R115777, a farnesyl protein transferase inhibitor.
de Bruijn, P; de Heus, G; de Jonge, MJ; Eskens, FA; Kehrer, DF; Klaren, A; Mathijssen, RH; Palmer, PA; Planting, AS; Sparreboom, A; Verhaeghe, T; Verheij, C; Verweij, J; Xie, R; Zhang, S, 2004
)
0.32
"We evaluated the efficacy of enrofloxacin, alone or combined with metronidazole, against Leishmania infantum."( The efficacy of enrofloxacin, alone or combined with metronidazole, in the therapy of canine leishmaniasis.
Bianciardi, P; Fasanella, A; Foglia Manzillo, V; Gradoni, L; Oliva, G; Pagano, A; Sorino, S; Trotta, T, 2004
)
0.32
"This phase I trial was designed to determine the safety and maximum tolerated dose (MTD) of tipifarnib in combination with gemcitabine and cisplatin in patients with advanced solid tumours."( Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours.
Beijnen, JH; Crul, M; Howes, A; Pluim, D; Schellens, JH; Siegel-Lakhai, WS; Solanki, B; Sparidans, RW; Zhang, S, 2005
)
0.33
"This review focuses on drug-drug interactions with three major groups of antimicrobial agents: macrolides (including azalides and ketolides), quinolones, which are widely used for the treatment of bacterial infections, and azoles, which are used for antifungal therapy."( Drug interactions during therapy with three major groups of antimicrobial agents.
Shakeri-Nejad, K; Stahlmann, R, 2006
)
0.33
" According to this concept, even chemically inert drugs can stimulate T cells because certain drugs interact in a direct way with T-cell receptors (TCR) and possibly major histocompatibility complex molecules without the need for metabolism and covalent binding to a carrier."( Transfection of drug-specific T-cell receptors into hybridoma cells: tools to monitor drug interaction with T-cell receptors and evaluate cross-reactivity to related compounds.
Depta, JP; Lüthi, M; Pichler, WJ; Schmid, DA, 2006
)
0.33
" The comet tail lengths of epidermal cells of the mice were statistically significantly increased for all three fluoroquinolones (FQ) tested in combination with UV irradiation."( Photo-chemically induced DNA effects in the comet assay with epidermal cells of SKH-1 mice after a single oral administration of different fluoroquinolones and 8-methoxypsoralen in combination with exposure to UVA.
Gross-Tholl, N; Herbold, B; von Keutz, E; Wirnitzer, U, 2006
)
0.33
" This review focuses on the influence of transporters on the pharmacokinetics of beta-lactam antibiotics, new quinolones, and other antimicrobial agents, as well as focusing on the drug-drug interactions associated with transporter-mediated uptake from the small intestine and transporter-mediated elimination from the kidney and liver."( Impact of transporter-mediated drug absorption, distribution, elimination and drug interactions in antimicrobial chemotherapy.
Tsuji, A, 2006
)
0.33
") administration of D-serine, a selective agonist for the glycine site of the NMDA receptors, alone or in combination with morphine using the tail-flick test."( Activation of supraspinal NMDA receptors by both D-serine alone or in combination with morphine leads to the potentiation of antinociception in tail-flick test of rats.
Akahori, K; Hashimoto, A; Ito, K; Jin, XL; Kobayashi, H; Maeda, M; Matsuda, M; Oka, T; Suzuki, T; Takahashi, S; Yoshikawa, M, 2007
)
0.34
"Although the high incidence of febrile neutropenia necessitated a multiple scheduling adaptation of tipifarnib compared to the original protocol, the apparent lack of mutual pharmacokinetic interactions, the ability to coadminister tipifarnib and docetaxel near single-agent MTDs, and suggestive evidence of efficacy make this drug combination attractive for further examination."( A phase I clinical and pharmacokinetic study of tipifarnib in combination with docetaxel in patients with advanced solid malignancies.
Awada, A; De Porre, P; de Valeriola, D; Gil, T; Lalami, Y; Piccart-Gebhart, MJ; Zhang, S, 2007
)
0.34
"To explore the efficacy and safety of Jieyu Anshen Decoction (JAD) combined with aripiprazole in treating chronic schizophrenia."( [Clinical observation on effect of Jieyu Anshen Decoction combined with aripiprazole in treating chronic schizophrenia].
Fan, XW; Luo, JW; Zeng, DZ, 2007
)
0.34
"All 100 patients with chronic schizophrenia diagnosed according to CCMD-3 criteria were equally randomly assigned to the study group (treated with JAD combined with aripiprazole) and the control group (treated with aripiprazole alone) for 12 weeks."( [Clinical observation on effect of Jieyu Anshen Decoction combined with aripiprazole in treating chronic schizophrenia].
Fan, XW; Luo, JW; Zeng, DZ, 2007
)
0.34
"JAD combined with aripiprazole has definite effect in treating chronic schizophrenia, shows advantages of quickly initiating effect, high safety and with no harm for increasing adverse reactions, so it is better than using aripiprazole alone."( [Clinical observation on effect of Jieyu Anshen Decoction combined with aripiprazole in treating chronic schizophrenia].
Fan, XW; Luo, JW; Zeng, DZ, 2007
)
0.34
"This study assessed the clinical efficacy of the farnesyltransferase inhibitor, tipifarnib, combined with letrozole in patients with advanced breast cancer and disease progression following antiestrogen therapy."( A phase II, randomized, blinded study of the farnesyltransferase inhibitor tipifarnib combined with letrozole in the treatment of advanced breast cancer after antiestrogen therapy.
Bessems, A; De Porre, PM; Dodwell, DJ; Howes, AJ; Johnston, SR; Manikhas, GM; Neven, P; Park, YC; Perez Ruixo, JJ; Romieu, G; Semiglazov, VF; Spaeth, D; Wardley, AM, 2008
)
0.35
" We therefore investigated the efficacy of the farnesyltransferase inhibitor (FTI) R115777 (tipifarnib) in combination with tamoxifen in MCF-7 human breast cancer models both in vitro and in vivo."( The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.
Detre, S; Dowsett, M; Head, JE; Howes, A; Johnston, SR; Kaye, S; Martin, LA; Pancholi, S; Quinn, E; Salter, J, 2007
)
0.34
" Since NMDA receptors play a crucial role in trigeminal pain processing, the aim of our experiments was to compare the effects of L-kynurenine (L-KYN) combined with probenecid (PROB) or with 2-(2-N,N-dimethylaminoethylamine-1-carbonyl)-1H-quinolin-4-one hydrochloride alone, a newly synthetized KYNA derivative, on the NTG-induced nNOS expression in the rat TNC."( l-kynurenine combined with probenecid and the novel synthetic kynurenic acid derivative attenuate nitroglycerin-induced nNOS in the rat caudal trigeminal nucleus.
Bohár, Z; Fülöp, F; Párdutz, A; Tajti, J; Toldi, J; Vámos, E; Varga, H; Vécsei, L, 2009
)
0.35
" We conducted a randomized crossover trial with MPH and placebo (2 weeks each) combined with aripiprazole in children and adolescents (n = 16; 8-17 years old) with JBPD and ADHD who had a significant response in manic symptoms with aripiprazole but still presented clinically significant symptoms of ADHD."( Methylphenidate combined with aripiprazole in children and adolescents with bipolar disorder and attention-deficit/hyperactivity disorder: a randomized crossover trial.
Ketzer, CR; Pheula, GF; Rohde, LA; Tramontina, S; Zeni, CP, 2009
)
0.35
" The risk of adverse drug-drug interaction(s) is present when metabolic inhibitors are combined with known or suspected substrates of a given enzyme."( Identification of selected therapeutic agents as inhibitors of carboxylesterase 1: potential sources of metabolic drug interactions.
Appel, DI; Markowitz, JS; Peterson, YK; Wang, Z; Zhu, HJ, 2010
)
0.36
" After acquiring the discrimination, the effects of cocaine (0, 25, 50, 100 and 200 mg) administered alone and in combination with aripiprazole (15 mg) were determined."( Discriminative stimulus, subject-rated and cardiovascular effects of cocaine alone and in combination with aripiprazole in humans.
Glaser, PE; Hays, LR; Lile, JA; Rush, CR; Stoops, WW, 2011
)
0.37
"The authors conducted a phase 1/2 study of tipifarnib in combination with idarubicin and cytarabine (IA) in 95 patients with previously untreated acute myeloid leukemia (AML) or high-risk myelodysplastic syndrome."( A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome.
Cortes, J; Estrov, Z; Faderl, S; Garcia-Manero, G; Jabbour, E; Kantarjian, H; O'Brien, S; Ravandi, F; Thomas, DA; Verstovsek, S; Wright, JJ, 2011
)
0.37
"To determine the safety, target inhibition, and signals of clinical activity of tipifarnib in combination with bortezomib in patients with advanced acute leukemias."( A phase I clinical-pharmacodynamic study of the farnesyltransferase inhibitor tipifarnib in combination with the proteasome inhibitor bortezomib in advanced acute leukemias.
Blaskovich, MA; Burton, M; Cubitt, C; Duong, VH; Lancet, JE; Sebti, S; Stuart, RK; Sullivan, DM; Winton, EF; Wright, JJ; Zhang, S, 2011
)
0.37
" Safety and tolerability results revealed no unexpected adverse events for ARI combination with LTG."( Aripiprazole in combination with lamotrigine for the long-term treatment of patients with bipolar I disorder (manic or mixed): a randomized, multicenter, double-blind study (CN138-392).
Carlson, BX; Ketter, TA; Marcus, R; McQuade, RD; Sanchez, R; Sun, W; Timko, K; Vester-Blokland, E, 2012
)
0.38
" Using phosphokinome profiling and immunofluorescence in the TF-1a cell line, we demonstrate that the drug combination is characterised by the activation of a DNA damage response (induction of γH2A."( Targeting of CD34+CD38- cells using Gemtuzumab ozogamicin (Mylotarg) in combination with tipifarnib (Zarnestra) in Acute Myeloid Leukaemia.
Jawad, M; Pallis, M; Russell, NH; Seedhouse, C; Tandon, K; Yu, N, 2012
)
0.38
"The chemosensitivity of the CD34+CD38- subset, combined with enhanced damage indicators, suggest that this subset is primed to favour programmed cell death as opposed to repairing damage."( Targeting of CD34+CD38- cells using Gemtuzumab ozogamicin (Mylotarg) in combination with tipifarnib (Zarnestra) in Acute Myeloid Leukaemia.
Jawad, M; Pallis, M; Russell, NH; Seedhouse, C; Tandon, K; Yu, N, 2012
)
0.38
"In this work, a dispersive liquid-liquid microextraction (DLLME) procedure combined with ultra-high performance liquid chromatography with diode-array detection was developed to determine 25 antibiotics in mineral and run-off waters."( Dispersive liquid-liquid microextraction combined with ultra-high performance liquid chromatography for the simultaneous determination of 25 sulfonamide and quinolone antibiotics in water samples.
Borges-Miquel, TM; Hernández-Borges, J; Herrera-Herrera, AV; Rodríguez-Delgado, MÁ, 2013
)
0.39
" Healthy subjects (N = 12) received a single dose of rosuvastatin 10 mg alone and in combination with EVG/co."( Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin.
Andrews, J; Cheng, A; Custodio, JM; Hao, J; Kearney, BP; Lepist, EI; Ling, KH; Ramanathan, S; Ray, AS; Wang, H, 2014
)
0.4
" Treatment was administered with gemcitabine (1,000 mg/m(2) on days 1 and 8), cisplatin (70 mg/m(2)), or carboplatin (AUC 5) on day 1, and dovitinib (orally on days 1-5, 8-12, and 15-19), every 21 days."( Phase Ib study of dovitinib in combination with gemcitabine plus cisplatin or gemcitabine plus carboplatin in patients with advanced solid tumors.
Galsky, MD; Gimpel-Tetra, K; Godbold, J; Holcombe, RF; Lee, KM; Lowe, N; Misiukiewicz, K; Oh, WK; Posner, M; Soto, R; Tsao, CK, 2014
)
0.4
"Dovitinib in combination with gemcitabine plus cisplatin or gemcitabine plus carboplatin was poorly tolerated due to myelosuppression."( Phase Ib study of dovitinib in combination with gemcitabine plus cisplatin or gemcitabine plus carboplatin in patients with advanced solid tumors.
Galsky, MD; Gimpel-Tetra, K; Godbold, J; Holcombe, RF; Lee, KM; Lowe, N; Misiukiewicz, K; Oh, WK; Posner, M; Soto, R; Tsao, CK, 2014
)
0.4
" Based on these results, a series of clinical drug-drug interaction (DDI) studies were conducted to evaluate the effect of ivacaftor on sensitive substrates of CYP2C8 (rosiglitazone), CYP3A (midazolam), CYP2D6 (desipramine), and P-gp (digoxin)."( Clinical drug-drug interaction assessment of ivacaftor as a potential inhibitor of cytochrome P450 and P-glycoprotein.
Chavan, AB; Dubey, N; Gilmartin, GS; Higgins, M; Li, C; Luo, X; Mahnke, L; Robertson, SM, 2015
)
0.42
" By combination with the mTOR inhibitor RAD001, a synergistic effect on cell proliferation was observed in these cell lines."( The multi-tyrosine kinase inhibitor TKI258, alone or in combination with RAD001, is effective for treatment of human leukemia with BCR-ABL translocation in vitro.
Eucker, J; Habbel, P; Li, X; Liu, H; Neumann, C; Scholz, C; Zang, C; Zhou, Y, 2014
)
0.4
"TKI258 may become a potent therapeutic agent, either alone or in combination with RAD001, for treatment of BCR-ABL(+) leukemia."( The multi-tyrosine kinase inhibitor TKI258, alone or in combination with RAD001, is effective for treatment of human leukemia with BCR-ABL translocation in vitro.
Eucker, J; Habbel, P; Li, X; Liu, H; Neumann, C; Scholz, C; Zang, C; Zhou, Y, 2014
)
0.4
" Indirect forms of quinolone toxicity such as Clostridium difficile infections or adverse reactions associated with drug-drug interactions are also discussed."( Safety issues and drug-drug interactions with commonly used quinolones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
" Although several adverse events have been associated with their use, taking into consideration risk factors, contraindications and potential drug-drug interactions can drastically reduce the respective risks."( Safety issues and drug-drug interactions with commonly used quinolones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
"No more effective than tiotropium combined with formoterol."( Glycopyrronium + indacaterol. A fixed-dose combination with no advantages in COPD.
, 2014
)
0.4
" Mechanisms through which polypharmacy may increase adverse health outcomes include decreased adherence, increased drug side effects, higher use of potentially inappropriate medications, and more frequent drug-drug interactions."( Appropriate prescribing and important drug interactions in older adults.
Paauw, DS; Wallace, J, 2015
)
0.42
" Because of their ability to strongly compete for the ivacaftor binding sites on HSA and AGP, drug-drug interactions between ivacaftor are to be expected with ducosate, montelukast, ibuprofen, dicloxacillin, omeprazole, and loratadine."( Drug-drug plasma protein binding interactions of ivacaftor.
Azad, MA; Baker, M; Carbone, V; Cooper, MA; Huang, JX; Li, J; Schneider, EK; Velkov, T, 2015
)
0.42
"The ability of a chronic treatment with indacaterol, a new ultra-long-acting β2 -adrenoceptor agonist, to reverse cardiac remodelling and its effects in combination with metoprolol, a selective β1 -adrenoceptor antagonist, were investigated on myocardial infarction in a rat model of heart failure (HF)."( Effects of chronic treatment with the new ultra-long-acting β2 -adrenoceptor agonist indacaterol alone or in combination with the β1 -adrenoceptor blocker metoprolol on cardiac remodelling.
Calzetta, L; Capuano, A; Donniacuo, M; Gritti, G; Martuscelli, E; Matera, MG; Orlandi, A; Rafaniello, C; Rinaldi, B; Rossi, F; Sodano, L, 2015
)
0.42
" Dovitinib in combination with several agents inhibits growth more effectively than either agent alone."( The broad-spectrum receptor tyrosine kinase inhibitor dovitinib suppresses growth of BRAF-mutant melanoma cells in combination with other signaling pathway inhibitors.
Bosenberg, MW; Held, MA; Iyidogan, P; Klein, M; Koo, AB; Langdon, CG; Liu, Z; Mamillapalli, R; Meeth, K; Platt, JT; Stern, DF, 2015
)
0.42
" Given the toxicity and the pharmacokinetic interaction, further investigation with this drug combination will not be pursued."( Dovitinib and erlotinib in patients with metastatic non-small cell lung cancer: A drug-drug interaction.
Das, M; Frymoyer, A; Neal, JW; Padda, SK; Riess, JW; Wakelee, HA; Zhou, L, 2015
)
0.42
" Lumacaftor in combination with ivacaftor, a modulator of CFTR gating defects, improves clinical outcome measures in patients homozygous for the F508del mutation."( Lumacaftor alone and combined with ivacaftor: preclinical and clinical trial experience of F508del CFTR correction.
Brewington, JJ; Clancy, JP; McPhail, GL, 2016
)
0.43
" While studies have demonstrated that boosting with either cobicistat or ritonavir results in comparable plasma exposure of the target antiretroviral agent, a better understanding of drug-drug interactions between cobicistat- and ritonavir-boosted antiretrovirals and other medications will inform treatment decisions in HIV-infected patients."( Drug Interactions with Cobicistat- or Ritonavir-Boosted Elvitegravir.
Custodio, JM; McNicholl, I; Nguyen, T; Piontkowsky, D; Szwarcberg, J,
)
0.13
"The aac(6')-Ib-cr gene, in spite of producing low-level resistance by itself, plays a relevant role in acquisition of a clinical level of ciprofloxacin and norfloxacin resistance, when combined with three or four chromosomal mutations, both in vitro and in vivo."( Impact of AAC(6')-Ib-cr in combination with chromosomal-mediated mechanisms on clinical quinolone resistance in Escherichia coli.
Díaz-De-Alba, P; Docobo-Perez, F; Machuca, J; Ortiz, M; Pascual, Á; Recacha, E; Rodríguez-Martínez, JM, 2016
)
0.43
" This study aimed to investigate the synergistic antibacterial activity of polymyxin B in combination with the cystic fibrosis (CF) drugs KALYDECO (ivacaftor) and ORKAMBI (ivacaftor + lumacaftor) against Gram-negative pathogens that commonly colonize the CF lung, in particular, the problematic Pseudomonas aeruginosa."( An "Unlikely" Pair: The Antimicrobial Synergy of Polymyxin B in Combination with the Cystic Fibrosis Transmembrane Conductance Regulator Drugs KALYDECO and ORKAMBI.
Azad, MA; Baker, MA; Bergen, PJ; Cooper, MA; Doi, Y; Han, ML; Huang, JX; Li, J; Muller, MT; Schneider, EK; Tony Zhou, Q; Velkov, T; Wang, J, 2016
)
0.43
"We investigated whether a fixed-dose combination tablet of elvitegravir, cobicistat, emtricitabine, and tenofovirDF (Stribild) can be crushed and combined with enteral nutrition without influencing pharmacokinetics."( Brief Report: Pharmacokinetics of Crushed Elvitegravir Combination Tablet Given With or Without Enteral Nutrition.
Abbink, E; Burger, D; Colbers, A; Duisenberg-van Essenberg, M; Jongbloed-de Hoon, M; Kruijssen, M; van Crevel, R; Velthoven-Graafland, K, 2017
)
0.46
" Dovitinib in combination with fulvestrant showed promising clinical activity in the FGF pathway-amplified subgroup."( Phase II, randomized, placebo-controlled study of dovitinib in combination with fulvestrant in postmenopausal patients with HR
André, F; Barrios, CH; Blackwell, K; Bonnefoi, H; Campone, M; Cortes, J; Denduluri, N; Deudon, S; Kahan, Z; Musolino, A; Neven, P; Shi, MM; Soliman, H; Squires, M; Zhang, Y, 2017
)
0.46
"Antiretroviral agents pose a high risk for drug-drug interactions (DDIs), mainly but not limited to being a substrate, inducer or inhibitor of P450 cytochrome enzymes."( Prevalence of drug-drug interactions in the era of HIV integrase inhibitors: a retrospective clinical study.
Baecke, C; Decoutere, L; Gyssens, IC; Messiaen, P; van der Hilst, JCH, 2017
)
0.46
"ART regimens pose a dissimilar risk for drug-drug interactions in clinical practice."( Prevalence of drug-drug interactions in the era of HIV integrase inhibitors: a retrospective clinical study.
Baecke, C; Decoutere, L; Gyssens, IC; Messiaen, P; van der Hilst, JCH, 2017
)
0.46
" Because it is a substrate of the cytochrome P450 system, specifically CYP3A4/5, ivacaftor is subject to significant drug-drug interactions, including due to commonly used antimicrobials such as rifampin."( Sensitivity of ivacaftor to drug-drug interactions with rifampin, a cytochrome P450 3A4 inducer.
Acosta, EP; Guimbellot, JS; Rowe, SM, 2018
)
0.48
" The MTD was reached at erlotinib 150 mg once daily combined with tipifarnib 300 mg twice daily."( A phase I study of the farnesyltransferase inhibitor Tipifarnib in combination with the epidermal growth factor tyrosine kinase inhibitor Erlotinib in patients with advanced solid tumors.
Adjei, A; Allred, J; Goetz, M; Jazieh, K; Kaufmann, SH; Lim, VS; Molina, J; Reid, J; Yin, J, 2019
)
0.51
"We report the cases of two treatment-experienced HIV-infected patients with complex antiretroviral regimens that showed significant drug-drug interactions with etravirine."( Optimizing concentrations of concomitant antiretrovirals by reducing etravirine doses: two case reports of complex drug-drug interactions.
Cabot, JF; Denault, JS; Langlois, H; Marcotte, S; Sheehan, NL, 2019
)
0.51
" We report a potential drug-drug interaction in 2 female patients both receiving treatment for HIV and cerebral toxoplasmosis: one case between E/C/F/TAF with calcium carbonate and a second case involving leucovorin as calcium salt."( HIV Viral Rebound Due to a Possible Drug-Drug Interaction between Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide and Calcium-Containing Products: Report of 2 Cases.
El-Sayed, D; Kang-Birken, SL; Prichard, J,
)
0.13
" Observed safety results support further evaluation of GLPG2222, including in combination with other CFTR modulators."( CFTR activity is enhanced by the novel corrector GLPG2222, given with and without ivacaftor in two randomized trials.
Barry, PJ; Bell, SC; Bellaire, S; Conrath, K; De Boeck, K; de Kock, H; Drevinek, P; Elborn, JS; Geller, DE; Kanters, D; Minić, P; Muller, K; Plant, BJ; Van Braeckel, E; Van de Steen, O; van der Ent, K; Verhulst, S, 2019
)
0.51
"Reduced doses of antibiotics, bacterial morphological alterations, efflux pump down regulation, porin over expression and beta-lactamase gene inhibition of ESBL-QR bacteria by EG alone or in combination with CTX/CIP might have reversed antibiotic resistance profile of ESBL-QR bacteria."( The use of eugenol in combination with cefotaxime and ciprofloxacin to combat ESBL-producing quinolone-resistant pathogenic Enterobacteriaceae.
Dhara, L; Tripathi, A, 2020
)
0.56
" We hypothesise that changes to gonorrhoea treatment guidelines combined with differences in country-level consumption of cephalosporins and quinolones contributed to this shift."( Gonorrhoea treatment combined with population-level general cephalosporin and quinolone consumption may select for Neisseria gonorrhoeae antimicrobial resistance at the levels of NG-MAST genogroup: An ecological study in Europe.
Abdelatti, S; De Baetselier, I; Kenyon, C; Laumen, J; Manoharan-Basil, SS; Unemo, M; Van Dijck, C, 2020
)
0.56
" Combined atorvastatin with celecoxib and tipifarnib synergistically decreased the sphere forming ability of Panc-1 cells and the drug combination also strongly inhibited cell proliferation and promoted apoptosis in the sphere-forming cells."( Effects of atorvastatin in combination with celecoxib and tipifarnib on proliferation and apoptosis in pancreatic cancer sphere-forming cells.
Chen, J; Goodin, S; Li, DL; Ma, YR; Ma, YY; Ren, X; Wang, X; Xu, XT; Zhang, K; Zhao, DG; Zheng, X; Zhou, RP, 2021
)
0.62
" The primary objective was to determine the recommended Phase 2 dose of crenigacestat in combination with other anticancer agents (taladegib, LY3023414 [dual inhibitor of phosphoinositide 3-kinase; mechanistic target of rapamycin], or abemaciclib)."( A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors.
Anderson, B; Azaro, A; Benhadji, KA; Cassier, PA; Italiano, A; Massard, C; Merchan, J; Oakley, G; Pant, S; Tap, WD; Yu, D; Yuen, E, 2021
)
0.62
"To determine the safety of tipifarnib in combination with escalating doses of bortezomib and to determine the maximum tolerated dose in patients with untreated high-risk MDS and oligoblastic acute myeloid leukemia, who were not eligible for intensive therapy."( A phase I clinical trial to study the safety of treatment with tipifarnib combined with bortezomib in patients with advanced stages of myelodysplastic syndrome and oligoblastic acute myeloid leukemia.
Blijlevens, N; de Witte, T; Langemeijer, S; Muus, P; van Bijnen, S, 2021
)
0.62
"In this case report the potential drug-drug interaction between cytochrome P450 (CYP) 3A4 substrates tezacaftor-ivacaftor and CYP3A4/5 inhibitor clofazimine is investigated in a patient with cystic fibrosis."( No drug-drug interaction between tezacaftor-ivacaftor and clofazimine: A case report.
Kemper, EM; Mathôt, RAA; Mouissie, LM; Terheggen-Lagro, SWJ; Vonk, SEM, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
"4 microM) inhibitory activities, was found to be orally bioavailable with a long duration of action and offered effective protection against mortality in a collagen-epinephrine-induced pulmonary thromboembolism model in mice."( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992
)
0.28
" At all dose levels and schedules, lomefloxacin was well absorbed and achieved peak plasma concentrations approximately 1 hour after administration."( Multiple-dose pharmacokinetics of lomefloxacin: rationale for once-a-day dosing.
Mant, TG, 1992
)
0.28
" This compound is very hydrophilic and is well absorbed by tissues such as the lung but not by tissues with tight junctions such as the gut."( [Basic research on nedocromil sodium].
Joseph, M; Rainey, DK, 1992
)
0.28
"The relative bioavailability of a single oral dose of temafloxacin given with and without enteral feeding was determined in 18 healthy male volunteers in a randomised crossover study."( The relative bioavailability of temafloxacin administered through a nasogastric tube with and without enteral feeding.
Lubowski, TJ; Nightingale, CH; Quintiliani, R; Sweeney, K, 1992
)
0.28
" The pharmacokinetics of 3 tablet formulations of temafloxacin were investigated in phase I studies in healthy adult volunteers, to determine whether the bioavailability is altered by the presence of food."( The effect of food on the bioavailability of temafloxacin. A review of 3 studies.
Granneman, GR; Mukherjee, D, 1992
)
0.28
" Comparable or greater antacid-associated reductions in relative bioavailability have been reported for other quinolones."( Effect of antacid medication on the pharmacokinetics of temafloxacin.
Birner, B; Granneman, GR; Mukherjee, D; Sörgel, F; Stephan, U, 1992
)
0.28
" The oral bioavailability of CP-74,667 was 100% in dogs and monkeys, as determined by intravenous-oral crossover experiments."( Pharmacokinetic studies of CP-74,667, a new quinolone, in laboratory animals.
Girard, D; Gootz, TD; McGuirk, PR, 1992
)
0.28
"The pharmacokinetics and bioavailability of enrofloxacin were determined after IV and IM administration of 5 mg/kg of body weight to 6 healthy adult rabbits."( Pharmacokinetics of enrofloxacin after intravenous and intramuscular injection in rabbits.
Arboix, M; Cabanes, A; Garcia Anton, JM; Reig, F, 1992
)
0.28
" The relative bioavailability of the 15-mg/kg oral dose was 48%."( Intramuscular and oral disposition of enrofloxacin in African grey parrots following single and multiple doses.
Aucoin, DP; Flammer, K; Whitt, DA, 1991
)
0.28
" Danofloxacin was rapidly absorbed following intramuscular and subcutaneous injection and bioavailability was virtually complete (101% and 94% respectively)."( Clinical pharmacokinetics of parenterally administered danofloxacin in cattle.
Giles, CJ; Grimshaw, WT; Lynch, MJ; Magonigle, RA; Rice, JR; Risk, JE; Tanner, AC, 1991
)
0.28
" Compared with IV administration, bioavailability was 77% after SC dosing and 61% for gastrointestinal absorption."( Pharmacokinetic properties of enrofloxacin in rabbits.
Babish, JG; Brooks, DL; Broome, RL; Conzelman, GM; Copeland, DD, 1991
)
0.28
" Temafloxacin has improved activity against pneumococci and its high oral bioavailability and excellent penetration into respiratory tissues now combine to provide a suitable profile for the management of a wider range of respiratory infections."( The role of temafloxacin in the community setting: an overview.
Ball, P, 1991
)
0.28
" Studies in healthy volunteers indicate that the average bioavailability of temafloxacin exceeds 90%, with little intersubject variability."( A review of the pharmacokinetic profile of temafloxacin.
Dudley, MN, 1991
)
0.28
" The absolute bioavailability of unchanged E-4441 is of 20% and the urinary excretion represents 1 to 2% of the administered oral dose."( A pharmacokinetic study of E-4441, a new quinolone, in the rat, mouse and cynomolgus monkey.
Basi, N; Dordal, A; Martinez, L; Roser, R; Sagarra, R, 1991
)
0.28
" Lomefloxacin is well absorbed after oral administration giving high blood and urine concentrations and its prolonged half-life means once daily dosing in the treatment of many types of bacterial infection may be possible."( Antibacterial activity of lomefloxacin.
Leigh, DA; Tait, S; Walsh, B, 1991
)
0.28
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" In these animals the bioavailability is equal to 60%."( A new tricyclic fluoroquinolone, rufloxacin (MF-934), with interesting antibacterial and pharmacokinetic characteristics.
Cerretani, D; Cerri, D; Moltoni, L; Segre, G, 1988
)
0.27
" The bioavailability varied considerably among the four quinolones."( Comparative single-dose pharmacokinetics of four quinolones, oxolinic acid, flumequine, sarafloxacin, and enrofloxacin, in Atlantic salmon (Salmo salar) held in seawater at 10 degrees C.
Horsberg, TE; Martinsen, B, 1995
)
0.29
" Oral bioavailability was found to be 64."( Pharmacokinetics and residues of enrofloxacin in chickens.
Anadón, A; Bringas, P; Díaz, MJ; Fernández, MC; Fernández, R; Fernàndez-Cruz, ML; Martínez, MA; Martínez-Larrañaga, MR, 1995
)
0.29
" Oral bioavailability calculated with bioassay results was more than 100% whereas availability of enrofloxacin was only 53%."( [Pharmacokinetics of baytril (enrofloxacin) in dogs].
Küng, K; Wanner, M, 1994
)
0.29
" These results confirmed that the addition of L-HPC to the cores increases not only the dissolution rate but also the bioavailability of SPFX."( Role of low-substituted hydroxypropylcellulose in dissolution and bioavailability of novel fine granule system for masking bitter taste.
Fujioka, H; Nakamura, Y; Shirai, Y; Sogo, K, 1994
)
0.29
" A slight decrease of sparfloxacin bioavailability with increasing dose was observed because AUC was 87% to 88% of the expected area when the dose was doubled."( Pharmacokinetics of sparfloxacin in humans after single oral administration at doses of 200, 400, 600, and 800 mg.
Bruno, R; Chassard, D; Ebmeier, M; Frydman, A; Guimart, C; Le Roux, Y; Montay, G; Thebault, JJ; Vergniol, JC, 1994
)
0.29
" Although 2 exhibited 25% oral bioavailability in rats, pharmacokinetic studies conducted in monkeys revealed that the parent compound was less than 5% bioavailable, the result of extensive first-pass biotransformation in the liver."( Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives.
Gamberdella, M; Goldenberg, HJ; Hewawasam, P; Meanwell, NA; Russell, JW; Seiler, SM; Thomas, JA; Wright, JJ; Zavoico, GB, 1993
)
0.29
" Bioavailability was about 80% in pregnant and lactating sows."( [The effect of pregnancy and lactation in sows on the pharmacokinetics of the gyrase inhibitor marbofloxacin].
Petracca, K; Wanner, M, 1993
)
0.29
" The bioavailability of tablet was comparable to that of capsule."( Pharmacokinetics and relative bioavailability of lomefloxacin preparations in 10 healthy Chinese volunteers.
Diao, Y; Ji, G; Li, L; Lu, J; Wang, EH; Zhu, XD, 1993
)
0.29
"The present study was designed to determine the effects of an antacid suspension containing magnesium hydroxide and aluminum hydroxide (30 ml of Maalox) on the oral bioavailability of rufloxacin (400 mg)."( Effects of magnesium-aluminum hydroxide antacid on absorption of rufloxacin.
Bargiggia, S; Bianchi Porro, G; Broccali, G; Dal Bo, L; Imbimbo, BP; Lazzaroni, M; Sangaletti, O, 1993
)
0.29
" Antacids containing aluminium hydroxide reduce the oral bioavailability of sparfloxacin by 25 to 35%."( Clinical pharmacokinetics of sparfloxacin.
Ishibashi, Y; Nogita, T; Shimada, J, 1993
)
0.29
" Bioavailability was about 80% in pregnant and lactating sows."( Pharmacokinetics of the gyrase inhibitor marbofloxacin: influence of pregnancy and lactation in sows.
Graser, T; Petracca, K; Riond, JL; Wanner, M, 1993
)
0.29
"The complexation of the fluoroquinolone antimicrobials is important because it has been implicated in reduced oral bioavailability and reduced antimicrobial activity when the drugs are co-administered with antacids or multi-vitamin preparations containing iron."( Characterization of the complexation of fluoroquinolone antimicrobials with metal ions by nuclear magnetic resonance spectroscopy.
Riley, CM; Ross, DL; Takusagawa, F; Vander Velde, D, 1993
)
0.29
" Bioavailability was 91%."( Lung tissue concentrations and plasma pharmacokinetics of danofloxacin in calves with acute pneumonia.
Apley, MD; Upson, DW, 1993
)
0.29
" These compounds are structurally related to the 1-(4-piperidyl)-2(1H)-quinolinones, including OPC-21268, an orally bioavailable AVP V1 antagonist with high V1 specificity."( Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
Chihara, T; Kondo, K; Miyamoto, H; Mori, T; Nakaya, K; Ogawa, H; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, H, 1993
)
0.29
" The bioavailability of the film-coated fine granules containing 20% SPFX and 52% L-HPC in the cores and 10% EC/HPMC (4/2) in the coating film, which masked the bitter taste of SPFX and showed the optimal release characteristics, was equivalent to that of conventional tablets containing 100 mg SPFX in beagle dogs."( A novel fine granule system for masking bitter taste.
Fujioka, H; Kojima, K; Makita, H; Nakamura, Y; Shirai, Y; Sogo, K; Yamamoto, K, 1993
)
0.29
" Results indicated that absorption rate was slow, compared with previous studies; additionally, peak concentration was lower (0."( Sustained release of liposome-encapsulated enrofloxacin after intramuscular administration in rabbits.
Antón, JM; Arboix, M; Cabanes, A; Reig, F, 1995
)
0.29
" The reduction in bioavailability of fluoroquinolones by concurrent administration of aluminium hydroxide is more striking for derivatives with fewer substituents on the essential structure and on the piperazinyl group, such as norfloxacin, ciprofloxacin and enoxacin."( Pharmacokinetic interactions related to the chemical structures of fluoroquinolones.
Fujiwara, I; Mizuki, Y; Yamaguchi, T, 1996
)
0.29
"43 hours, and the bioavailability was 57."( Pharmacokinetics of enrofloxacin in adult horses and concentration of the drug in serum, body fluids, and endometrial tissues after repeated intragastrically administered doses.
Bélanger, M; Giguère, S; Sweeney, RW, 1996
)
0.29
" When the same dose was administered IM, enrofloxacin was rapidly and almost completely absorbed, with bioavailability of 85%."( Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin after intravenous and intramuscular administrations in sheep.
Bertini, S; Intorre, L; Mengozzi, G; Soldani, G, 1996
)
0.29
" The quinolones have excellent activity against gram-negative organisms, including gonococcus, and are characterized by very high bioavailability after oral administration."( Antibiotic use in the emergency department. III. The quinolones, new beta lactams, beta lactam combination agents, and miscellaneous antibiotics.
Pollack, CV; Schmidt, J,
)
0.13
" The oral bioavailability of marbofloxacin was close to 100% for the three doses."( Pharmacokinetics of marbofloxacin in dogs after oral and parenteral administration.
Boisrame, B; Deleforge, J; Schneider, M; Thomas, V, 1996
)
0.29
" The relative bioavailability of enrofloxacin after administration directly into the crop was 68%, while the metabolic conversion of enrofloxacin to ciprofloxacin was quite low (< 10%) with both routes of administration."( The plasma kinetics and tissue distribution of enrofloxacin and its metabolite ciprofloxacin in the Muscovy duck.
Bagliacca, M; Bertini, S; Intorre, L; Luchetti, E; Mengozzi, G; Soldani, G, 1997
)
0.3
", the percent bioavailability was 90."( Pharmacokinetics of 1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1- piperazinyl)-1,4-dihydro-4-oxoquinolone-3-carboxylic acid hydrochloride (DW-116), a new quinolone antibiotic in rats.
Chung, SJ; Lee, MH; Shim, CK; Yu, IL, 1997
)
0.3
" It is usually administered orally and is well absorbed after oral ingestion."( [Urinary tract infections: risk factors and therapeutic trends].
Astorri, AL; Margariti, PA; Mastromarino, C, 1997
)
0.3
" The pharmacokinetics and bioavailability of enrofloxacin in chickens were investigated following intravenous, intramuscular, subcutaneous and oral administration of 10 mg/kg body weight."( Pharmacokinetic evaluation of enrofloxacin in chickens.
Abd el-Aziz, MI; Afify, NA; Aziz, MA; Soliman, FA, 1997
)
0.3
" The bioavailability was determined to 83 +/- 13% in fed and to 101 +/- 32% in fasted pigs."( Bioavailability of enrofloxacin after oral administration to fed and fasted pigs.
Gyrd-Hansen, N; Nielsen, P, 1997
)
0.3
" Coadministration of sucralfate leads to a 44% decrease in the bioavailability of sparfloxacin."( Pharmacokinetics of sparfloxacin and interaction with cisapride and sucralfate.
Borner, K; Geerdes-Fenge, HF; Koeppe, P; Lode, H; Rau, M; Vöckler, J; Zix, JA, 1997
)
0.3
" It is well absorbed and has excellent penetration into upper and lower respiratory tissues."( Sparfloxacin: potential clinical and economic impact in the treatment of respiratory infections.
Havlichek, DH; Stein, GE,
)
0.13
" The results of these studies indicate that neither food nor the elevation of gastric pH influence the absorption or bioavailability of grepafloxacin."( Effect of food and gastric pH on the bioavailability of grepafloxacin.
Bramer, SL; Efthymiopoulos, C; Maroli, A, 1997
)
0.3
" To increase the bioavailability of NM394, various prodrugs were synthesized and tested."( In vivo antibacterial activity of a prodrug of NM394, a thiazetoquinoline carboxylic acid derivative.
Kise, M; Kitano, M; Matsuda, M; Nishino, T; Ozaki, M; Segawa, J; Tomii, Y,
)
0.13
" Danofloxacin had an absolute bioavailability (F) of 95."( Pharmacokinetics and tissue disposition of danofloxacin in sheep.
Gibson, IF; McCormack, RZ; McKellar, QA, 1998
)
0.3
" injection but a 'flip flop' effect was clearly evident and bioavailability was > 100%."( Pharmacokinetics and penetration of danofloxacin from the blood into the milk of cows.
Glickman, A; Lavi, E; Rav-Hon, O; Saran, A; Shem-Tov, M; Ziv, G, 1998
)
0.3
" Bioavailability was 97."( Pharmacokinetics of enrofloxacin after intravenous, intramuscular and oral administration in houbara bustard (Chlamydotis undulata macqueenii).
Bailey, TA; Garner, A; Harron, DW; Samour, JH; Sheen, RS; Silvanose, C, 1998
)
0.3
" The relative bioavailability of sparfloxacin was 84."( Sparfloxacin pharmacokinetics in healthy volunteers: the influence of acidification and alkalinization.
Kamberi, M; Kotegawa, T; Nakamura, K; Nakano, S; Tsutsumi, K, 1998
)
0.3
" On the other hand, the alteration in the environmental pH in the gastrointestinal tract, produced by the concomitant ingestion of ammonium chloride or sodium bicarbonate, influences the absorption and bioavailability of sparfloxacin."( Sparfloxacin pharmacokinetics in healthy volunteers: the influence of acidification and alkalinization.
Kamberi, M; Kotegawa, T; Nakamura, K; Nakano, S; Tsutsumi, K, 1998
)
0.3
" Bioavailability by the oral route was 80."( Pharmacokinetics of enrofloxacin given by the oral, intravenous and intramuscular routes in broiler chickens.
Black, WD; Bugyei, K; McEwen, S, 1999
)
0.3
" Bioavailability (F) was high: 99% for danofloxacin and 89% for enrofloxacin."( Comparative study of the plasma pharmacokinetics and tissue concentrations of danofloxacin and enrofloxacin in broiler chickens.
Glünder, G; Kietzmann, M; Knoll, U, 1999
)
0.3
" Following intratracheal instillation of the drug solution, the lung bioavailability was found to be approximately 75% in dogs."( Pulmonary delivery of a dopamine D-1 agonist, ABT-431, in dogs and humans.
Adjei, AL; Bertz, RJ; El-Shourbagy, T; Marsh, KC; Zheng, Y, 1999
)
0.3
" In ocular kinetic studies, lomefloxacin showed nearly 10 times more ocular bioavailability in aqueous humor as compared to ciprofloxacin."( Comparative studies on topical lomefloxacin and ciprofloxacin on ocular kinetic and experimental corneal ulcer.
Agarwal, HC; Biswas, NR; Gupta, SK; Gupta, YK; Velpandian, T, 1999
)
0.3
" Bioavailability was higher in infected birds (72."( Tissue distribution and disposition kinetics of enrofloxacin in healthy and E. coli infected broilers.
Soliman, GA, 2000
)
0.31
" Bioavailability was calculated at 78."( Serum concentrations and pharmacokinetics of enrofloxacin after intravenous and intragastric administration to mares.
Brown, MP; Gronwall, RR; Haines, GR; Merritt, KA, 2000
)
0.31
"Pharmacokinetics and bioavailability of enrofloxacin were determined after single intravenous (IV) and intramuscular (IM) administrations of 5 mg/kg body weight (BW) to 5 healthy adult Angora goats."( Pharmacokinetics of enrofloxacin after intravenous and intramuscular administration in Angora goats.
Bas, AL; Elmas, M; Kaya, S; Tras, B; Yarsan, E; Yazar, E, 2001
)
0.31
" The bioavailability of an antibacterial agent depends on the target bacterial species, the site of infection and the integrity of the haemato-aqueous barrier."( Comparative review of topical ophthalmic antibacterial preparations.
Adenis, JP; Robert, PY, 2001
)
0.31
" The method was successfully applied to a bioavailability study with five different ciprofloxacin formulations."( Simple high-performance liquid chromatographic assay for the determination of ciprofloxacin in human plasma with ultraviolet detection.
Gonçalves, NJ; Maya, MT; Morais, JA; Silva, NB, 2001
)
0.31
" Non-bioequivalence of relevant pharmacokinetic values, such as Csmax and bioavailability (AUC) would facilitate development of bacterial resistance and limit the useful life span of this antibacterial agent."( Non-bioequivalence of various trademarks of enrofloxacin and Baytril in cows.
Gutiérrez, OL; Ocampo, CL; Sumano, LH, 2001
)
0.31
" These dissolution properties were clearly reflected in the oral bioavailability of TA-270 in rats."( Characterization of polymorphs of a novel quinolinone derivative, TA-270 (4-hydroxy-1-methyl-3-octyloxy-7-sinapinoylamino-2(1H)-quinolinone).
Fukui, H; Kimura, N; Takagaki, H; Terada, K; Yonemochi, E, 2001
)
0.31
" The following variables were compared: maximal plasma concentration (Cpeak), time to Cpeak, bioavailability (expressed as the area under the concentration vs."( Bioequivalence of four preparations of enrofloxacin in poultry.
Gutiérrez, OL; Sumano, LH; Zamora, MA, 2001
)
0.31
"9 h) and had high bioavailability (F=100."( Pharmacokinetic behavior of marbofloxacin after intravenous and intramuscular administrations in adult goats.
De Vicente, ML; González, F; Rodríguez, C; San Andrés, MD; San Andrés, MI; Waxman, S, 2001
)
0.31
" It may be less well absorbed and/or less effective than Clozaril, although evidence is conflicting."( Advances in atypical antipsychotics for the treatment of schizophrenia: new formulations and new agents.
Albert, MJ; Baldessarini, RJ; Centorrino, F; Kelleher, JP, 2002
)
0.31
" An open, cross-over trial was performed in 24 patients with solid tumors to compare the bioavailability of a new tablet formulation with the standard capsule formulation."( Evaluation of the bioequivalence of tablets and capsules containing the novel anticancer agent R115777 (Zarnestra) in patients with advanced solid tumors.
Beijnen, JH; Bol, CJ; Crul, M; de Klerk, GJ; Palmer, PA; Schellens, JH; Swart, M; Weiner, L,
)
0.13
"2 min) and presented high bioavailability (F = 87."( Pharmacokinetics of marbofloxacin in mature horses after single intravenous and intramuscular administration.
Carretero, M; de Lucas, JJ; Forés, P; González, F; Nieto, J; Rodríguez, C; San Andrés, MD; San Andrés, MI; Waxman, S, 2002
)
0.31
" Oral bioavailability for the oral drench, crushed tablets in grain, and enrofloxacin in grain was 4789, 98."( Pharmacokinetics after intravenous and oral administration of enrofloxacin in sheep.
Bermingham, EC; Papich, MG, 2002
)
0.31
" Oral bioavailability of marbofloxacin was 56."( Pharmacokinetic characteristics and tissue residues for marbofloxacin and its metabolite N-desmethyl-marbofloxacin in broiler chickens.
Anadón, A; Castellano, VJ; Díaz, MJ; Frejo, MT; Martínez, M; Martínez, MA; Martínez-Larrañaga, MR; Tafur, M, 2002
)
0.31
" The 4-aminopentamethylpiperidine naphthyridinone 5, which was designed to block metabolism at major 'hot spots', combined excellent inhibitory potency with good oral bioavailability in the rat."( p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.
Doherty, JB; Hop, CE; Hunt, JA; Ita, I; Kallashi, F; Kumar, S; McCormick, SX; O'Keefe, SJ; O'Neill, EA; Pivnichny, JV; Porter, G; Ruzek, RD; Sinclair, PJ; Thompson, JE; Wang, Z; Woods, A; Zaller, DM, 2003
)
0.32
" In conclusion, the combinatorial use of C12 with Tau or L-Gln could lead to a novel formulation improving the bioavailability of poorly absorbable drugs without any serious local damages."( Combinatorial use of sodium laurate with taurine or L-glutamine enhances colonic absorption of rebamipide, poorly absorbable antiulcer drug, without any serious histopathological mucosal damages.
Higaki, K; Kimura, T; Minami, T; Miyake, M; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2003
)
0.32
"R115777 is an orally bioavailable farnesyltransferase inhibitor (FTI) that has displayed encouraging activity in patients with acute myeloid leukemia."( In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.
Gray, LA; Kaufmann, SH; Mesa, RA; Reeder, T; Schroeder, G; Tefferi, A, 2003
)
0.32
" The systemic bioavailability of enrofloxacin was significantly decreased from 110."( Influence of albendazole on the disposition kinetics and milk antimicrobial equivalent activity of enrofloxacin in lactating goats.
Abo El Sooud, K, 2003
)
0.32
" Systematic modification of one of these leads produced a compound with excellent selectivity for PDE-5 over other phosphodiesterases and oral bioavailability of 15% in male rats."( Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
Bhattacharjee, S; Clancy, J; Craig, E; Fiordeliso, JJ; Haynes-Johnson, D; Jiang, W; John, TM; Kraft, P; Lanter, JC; Macielag, MJ; Qiu, Y; Sui, Z, 2004
)
0.32
" injection was well absorbed in 6- and 8-week-old kittens, but greater clearance and apparent volume of distribution resulted in lower plasma concentrations."( Pharmacokinetics of enrofloxacin in neonatal kittens.
Gibson, NM; Levy, JK; Papich, MG; Seguin, MA; Sigle, KJ, 2004
)
0.32
"To define the impact that use of different levels of hard water has on the bioavailability of the antibacterial, enrofloxacin, in poultry, an oral bioavailability-pharmacokinetic study of the drug was carried out."( Influence of hard water on the bioavailability of enrofloxacin in broilers.
Aguilera, R; Bernard, BM; Gracia, MJ; Gutierrez, OL; Rosiles, MR; Sumano, LH, 2004
)
0.32
" The mean time to peak plasma concentration is 3 hours following multiple-dose administration of aripiprazole 10 or 15 mg and the absolute oral bioavailability of the drug is 87%."( Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder.
Perry, CM; Swainston Harrison, T, 2004
)
0.32
"To develop the safe formulation that can safely improve bioavailability of poorly absorbable drugs and that is practically available, we prepared the suppositories of rebamipide, a poorly soluble and poorly absorbable antiulcer drug, by employing the combinatorial use of sodium laurate (C12), an absorption enhancer, with taurine (Tau) or L-glutamine (L-Gln), an adjuvant exerting the cytoprotective action."( Development of suppository formulation safely improving rectal absorption of rebamipide, a poorly absorbable drug, by utilizing sodium laurate and taurine.
Higaki, K; Kamada, N; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H, 2004
)
0.32
" This study was conducted to examine if the rebamipide lysinate salt form would exhibit improved solubility profiles and higher oral bioavailability compared with rebamipide free acid."( Oral absorption and pharmacokinetics of rebamipide and rebamipide lysinate in rats.
Han, HS; Jun, YS; Kim, CH; Lee, KC; Rho, JI; Shin, BS; Yoo, SD; Yoon, CH, 2004
)
0.32
"Tipifarnib, an orally bioavailable inhibitor of farnesyl transferase, has activity in hematologic malignancies, but the dose required to achieve the proposed biologic end point, inhibition of farnesylation, is unknown."( Dose-ranging pharmacodynamic study of tipifarnib (R115777) in patients with relapsed and refractory hematologic malignancies.
Berk, S; Gajewski, TF; Harlin, H; Karrison, T; Larson, RA; Odenike, OM; Ratain, MJ; Sprague, E; Stock, W; Zimmerman, TM, 2004
)
0.32
" Unfortunately, the low aqueous solubility and poor oral bioavailability rendered them undesirable development candidates."( Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
Bhattacharjee, S; Guan, J; Haynes-Johnson, D; Jiang, W; John, TM; Kraft, P; Lundeen, S; Macielag, MJ; Qiu, Y; Sui, Z; Zhang, S, 2005
)
0.33
" These agents are highly bioavailable and can facilitate the oral treatment of certain patients who otherwise might be admitted to the hospital, as outpatients."( Challenges in the management of community-acquired pneumonia: the role of quinolones and moxifloxacin.
Niederman, MS, 2005
)
0.33
" Although Tau tended to attenuate the absorption-enhancing effect of C12, several C12-Tau suppositories kept high bioavailability values, which were much higher than control."( Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide.
Higaki, K; Kamada, N; Kato, Y; Kimura, T; Minami, T; Miyake, M; Mukai, T; Odomi, M; Ogawara, K; Oka, Y; Toguchi, H; Yamazaki, H, 2006
)
0.33
" Pharmacokinetic studies showed that JNJ-10287069 had better oral bioavailability than JNJ-10280205 in several animal species."( JNJ-10280205 and JNJ-10287069: Novel PDE5 inhibitors as clinical candidates for erectile dysfunction.
Bhattacharjee, S; Haynes-Johnson, D; Jiang, W; Kraft, P; Lundeen, S; Mathew John, T; Qiu, Y; Sui, Z,
)
0.13
"316 microg/mL, and bioavailability was 90."( Pharmacokinetics of marbofloxacin in blue and gold macaws (Ara ararauna).
Carpenter, JW; Henry, H; Hunter, RP; Isaza, R; Koch, DE; Olsen, JH, 2006
)
0.33
" Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats were discovered."( Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
Ching, B; Dyck, B; Goodfellow, VS; Heise, CE; Hudson, S; Madan, A; Norton, C; Pontillo, J; Schwarz, D; Tamiya, J; Wade, W; Wen, J; Zhao, L, 2006
)
0.33
"Tipifarnib oral bioavailability (26."( Population pharmacokinetics of tipifarnib in healthy subjects and adult cancer patients.
De Porre, P; Hayes, S; Perez-Ruixo, JJ; Piotrovskij, V; Zannikos, P; Zhang, S, 2006
)
0.33
" A repeated measures study has been designed to compare their pharmacokinetic parameters, to investigate their bioavailability and to estimate their absorbed fraction and first-pass effect by using plasma, urinary and metabolite data collected from five healthy mares."( Enrofloxacin and marbofloxacin in horses: comparison of pharmacokinetic parameters, use of urinary and metabolite data to estimate first-pass effect and absorbed fraction.
Bousquet-Melou, A; Doucet, MY; Laroute, V; Peyrou, M; Vrins, A, 2006
)
0.33
" Due to the poor oral bioavailability of many drugs in the horse, this method may be useful for screening drugs before development to determine if they warrant further study."( Mucosal permeability of water-soluble drugs in the equine jejunum: a preliminary investigation.
Blikslager, AT; Davis, JL; Little, D; Papich, MG, 2006
)
0.33
"5 h, and an absolute bioavailability (F %) of 86."( Single-dose pharmacokinetics of marbofloxacin in Egyptian buffalo (Bubalus bubalis L.) steers.
Abd El-Aty, AM; Goudah, A; Regmi, NL; Shim, JH; Shimoda, M; Shin, HC,
)
0.13
"The tolerability and efficacy of the combination of tipifarnib, an orally bioavailable nonpeptidomimetic farnesyl transferase inhibitor, and imatinib was investigated in patients with chronic myelogenous leukemia in chronic phase who had failed imatinib."( Phase 1 study of tipifarnib in combination with imatinib for patients with chronic myelogenous leukemia in chronic phase after imatinib failure.
Cortes, J; Ebarb, T; Faderl, S; Garcia-Manero, G; Giles, F; Jones, D; Kantarjian, H; O'Brien, S; Quintás-Cardama, A; Thomas, D, 2007
)
0.34
"Study 1 was an open-label, randomized, three-treatment crossover study in healthy subjects (n = 18) to assess the bioavailability and pharmacokinetics of intramuscular aripiprazole 5 mg and oral aripiprazole 5 mg relative to intravenous aripiprazole 2 mg."( Pharmacokinetics and tolerability of intramuscular, oral and intravenous aripiprazole in healthy subjects and in patients with schizophrenia.
Boulton, DW; Kollia, G; Komoroski, B; Kovalick, LJ; Mallikaarjun, S; Reeves, RA; Sharma, A, 2008
)
0.35
", 12 with a peroral bioavailability of 71%)."( In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Birk, B; Hartmann, RW; Heim, R; Lucas, S; Ries, C; Schewe, KE, 2008
)
0.35
" Tipifarnib plus etoposide is a promising orally bioavailable regimen that warrants further evaluation in elderly adults who are not candidates for conventional induction chemotherapy."( Active oral regimen for elderly adults with newly diagnosed acute myelogenous leukemia: a preclinical and phase 1 trial of the farnesyltransferase inhibitor tipifarnib (R115777, Zarnestra) combined with etoposide.
Adjei, AA; Dai, NT; Feldman, EJ; Flatten, K; Garrett-Mayer, E; Gore, SD; Greer, JM; Ironside, V; Karp, JE; Kaufmann, SH; Le, SB; Levis, MJ; Loegering, DA; Meng, XW; Morris, LE; Ricklis, RM; Ritchie, E; Roboz, G; Schneider, PA; Smith, BD; Talbott, T; Wright, JJ, 2009
)
0.35
" Consequently, the coadministration of elvitegravir with the protease inhibitor ritonavir (a substantial CYP3A4 inhibitor) results in significantly enhanced bioavailability and a longer half-life than with elvitegravir alone, allowing for the once-daily dosing of elvitegravir."( Elvitegravir, an oral HIV integrase inhibitor, for the potential treatment of HIV infection.
Klibanov, OM, 2009
)
0.35
" Compound 2j was identified as a lead compound for future investigation due to its: (i) high activity against HIV-1, (ii) low cytotoxicity in PBMC, (iii) low toxic risks based on in silico evaluation, (iv) a good theoretical oral bioavailability according to Lipinski 'rule of five', (v) higher druglikeness and drug-score values than current antivirals AZT and efavirenz."( Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives.
Abreu, P; Barbosa, JE; Batalha, PN; Bou-Habib, DC; Castro, HC; Cirne-Santos, CC; Cunha, AC; de Souza, MC; Ferreira, VF; Garrido, V; Giongo, V; Nogueira, CM; Paixão, IC; Rodrigues, CR; Santos, Fda C; Silva, Dde O; Simonetti, BR; Souza, TM; Temerozo, JR, 2009
)
0.35
" Here we describe the in vitro pharmacology of VX-770, an orally bioavailable CFTR potentiator in clinical development for the treatment of CF."( Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770.
Arumugam, V; Ashlock, M; Burton, B; Cao, D; Decker, C; Frizzell, RA; Grootenhuis, PD; Hadida, S; Hazlewood, A; Joubran, J; McCartney, J; Negulescu, P; Neuberger, T; Olson, ER; Singh, A; Turnbull, A; Van Goor, F; Wine, JJ; Yang, J; Young, C; Zhou, J, 2009
)
0.35
" Since tipifarnib displays high oral bioavailability and acceptable pharmacokinetic properties, the newly discovered tipifarnib analogues are ideal leads for the development of drugs to treat Chagas disease."( Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.
Arif, J; Buckner, FS; Chennamaneni, NK; Gelb, MH; Karimi, M; Kraus, JM; McGuffin, SA; Tatipaka, HB; Verlinde, CL, 2010
)
0.36
"This study evaluated the relative bioavailability and pharmacokinetics of elvitegravir (EVG), emtricitabine (FTC), tenofovir disoproxil fumarate (TDF), and a investigational pharmacoenhancer, cobicistat (GS-9350, COBI) coformulated as a fixed-dose combination tablet (FDC) compared with ritonavir-boosted EVG and FTC + TDF in healthy subjects."( Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV.
German, P; Hui, J; Kearney, BP; Warren, D; West, S, 2010
)
0.36
" MRZ-8676 (6,6-dimethyl-2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one) is a novel proprietary, selective, orally bioavailable mGluR5 NAM."( Pharmacological characterization of MRZ-8676, a novel negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5): focus on L: -DOPA-induced dyskinesia.
Danysz, W; Dekundy, A; Gravius, A; Hechenberger, M; Mela, F; Nagel, J; Parsons, CG; Pietraszek, M; Tober, C; van der Elst, M, 2011
)
0.37
"P-glycoprotein (Pgp or ABCB1) is an ABC transporter protein involved in intestinal absorption, drug metabolism, and brain penetration, and its inhibition can seriously alter a drug's bioavailability and safety."( A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
Broccatelli, F; Carosati, E; Cruciani, G; Frosini, M; Goracci, L; Neri, A; Oprea, TI, 2011
)
0.37
" They are used worldwide due to their broad spectrum of activity, high bioavailability and good safety profile."( Quinolones: review of psychiatric and neurological adverse reactions.
Filipe, A; Tomé, AM, 2011
)
0.37
" AS1928370 showed good oral bioavailability and high penetration into the brain and spinal cord in mice."( Intrathecal administration of AS1928370, a transient receptor potential vanilloid 1 antagonist, attenuates mechanical allodynia in a mouse model of neuropathic pain.
Aoki, T; Kiso, T; Matsuoka, N; Tsukamoto, M; Watabiki, T, 2011
)
0.37
" Among the compounds designed in this study, we identified 2-[(3-aminomethyl-2-(2-methylpropyl)-1-oxo-4-phenyl-1,2-dihydro-6-isoquinolinyl)oxy]acetamide (35a) as a potent, selective, and orally bioavailable DPP-4 inhibitor, which exhibited in vivo efficacy in diabetic model rats."( Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Aertgeerts, K; Asakawa, T; Banno, Y; Funami, M; Ikedo, K; Kataoka, O; Kosaka, T; Maezaki, H; Miyamoto, Y; Oi, S; Sasaki, M; Suzuki, N; Takeuchi, K; Tani, A; Tawada, M; Tsubotani, S; Yamamoto, Y; Yano, J, 2011
)
0.37
" Consequently, the bioavailability of rebamipide is under 10% in humans."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" The bioavailability and efficacy of RBM solid dispersion were evaluated in a rat model."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" Bioavailability and efficacy of rebamipide were increased significantly by solubility enhancement of the drug."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" PK and PD studies in Sprague-Dawley rats revealed that the bioavailability of the drug using optimal SD was about twofold higher than that of reference product, and the irritation area of stomach was significantly reduced in the ulcer-induced rat model using optimal SD as compared to the reference product."( Physicochemical, pharmacokinetic and pharmacodynamic evaluations of novel ternary solid dispersion of rebamipide with poloxamer 407.
Chi, SC; Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2013
)
0.39
" A pediatric formulation of raltegravir with less variable pharmacokinetics and greater bioavailability was US Food and Drug Administration (US FDA)-approved in December 2011."( Pharmacology of HIV integrase inhibitors.
Adams, JL; Greener, BN; Kashuba, AD, 2012
)
0.38
" APZ nanosuspensions got maximum absorption rate and extent comparing with APZ commercial tablet and suspensions with relative bioavailability of 123."( Enhanced dissolution and oral bioavailability of aripiprazole nanosuspensions prepared by nanoprecipitation/homogenization based on acid-base neutralization.
Lian, R; Liu, X; Lu, Y; Wu, W; Xu, Y; Yin, Z; Zheng, S, 2012
)
0.38
"The oral (po) bioavailability of gemifloxacin mesylate in rats and its possible association with efflux transporters was investigated."( Transport of gemifloxacin, a 4th generation quinolone antibiotic, in the Caco-2 and engineered MDCKII cells, and potential involvement of efflux transporters in the intestinal absorption of the drug.
Chong, S; Chung, SJ; Jin, HE; Kim, DD; Kim, SB; Shim, CK; Shim, WS; Song, B, 2013
)
0.39
"98-fold) and bioavailability (3."( Aripiprazole in an animal model of chronic alcohol consumption and dopamine D₂ receptor occupancy in rats.
Abraham, R; Bhyrapuneni, G; Jayarajan, P; Kandikere, V; Muddana, N; Nirogi, R; Saralaya, R, 2013
)
0.39
"Poor aqueous solubility and the unpleasant taste of aripiprazole (APZ) have been recurring problems, owing to its low bioavailability and low patient tolerance, respectively."( Aripiprazole-montmorillonite: a new organic-inorganic nanohybrid material for biomedical applications.
Chang, HC; Choi, G; Choy, JH; Choy, YB; Lee, HJ; Oh, YJ; Park, JH; Park, JW; Yoon, YJ, 2013
)
0.39
" Selected as a preclinical candidate, ELQ-300 has good oral bioavailability at efficacious doses in mice, is metabolically stable, and is highly active in blocking transmission in rodent models of malaria."( Quinolone-3-diarylethers: a new class of antimalarial drug.
Angulo-Barturen, I; Avery, VM; Bathurst, I; Burrows, JN; Charman, SA; Cross, RM; Delves, MJ; Duffy, S; Ferrer, S; Forquer, IP; Gamo, FJ; Guy, RK; Herreros, E; Jiménez-Díaz, MB; Kelly, JX; Kocken, CHM; Kyle, DE; LaCrue, AN; Li, Y; Manetsch, R; Marfurt, J; Mather, MW; Morrisey, JM; Mutka, T; Nilsen, A; Noviyanti, R; Price, RN; Riscoe, MK; Ryan, E; Saenz, FE; Sanz, LM; Sebayang, BF; Shackleford, DM; Siegl, P; Sinden, RE; Steuten, J; Vaidya, AB; White, KL; Winter, RW; Wirjanata, G; Zeeman, AM, 2013
)
0.39
" The values of the bioavailability for the compound ranged from 10."( Disposition of the new potent acetylcholinesterase inhibitor 8-[3-[1-[(3-fluorophenyl)methyl]-4-piperidiny]-1-oxopropyl]-1, 2, 5, 6-tetrahydro-4H-pyrrolo [3, 2, 1-ij] quinolin-4-one (TAK-802) in rats, dogs and monkeys.
Asahi, S; Kakehi, M; Kondo, T; Tagawa, Y, 2013
)
0.39
" BMS-742413 has good intranasal bioavailability in the rabbit and shows a robust, dose-dependent inhibition of CGRP-induced increases in marmoset facial blood flow."( Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr
Cantor, GH; Chaturvedula, PV; Conway, CM; Davis, C; Denton, R; Dubowchik, GM; Keavy, D; Macci, R; Macor, JE; Mathias, N; Mercer, SE; Moench, P; Pin, SS; Schartman, R; Signor, L; Thalody, G; Whiterock, V; Xu, C, 2013
)
0.39
" Bioavailability studies of the polymorphs of aripiprazole and their pharmaceutical preparations are very important to optimize the formulations of the dosage forms."( Aripiprazole.
Ardiana, F; Indrayanto, G; Lestari, ML, 2013
)
0.39
"  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
)
0.4
" Interaction with metal ions has some important consequences for the solubility, pharmacokinetics and bioavailability of quinolones, and is also involved in the mechanism of action of these bactericidal agents."( Metal complexes of quinolone antibiotics and their applications: an update.
Uivarosi, V, 2013
)
0.39
"Dovitinib (TKI258; formerly CHIR-258) is an orally bioavailable inhibitor of multiple receptor tyrosine kinases."( Dovitinib induces mitotic defects and activates the G2 DNA damage checkpoint.
Mak, JP; Man, WY; Poon, RY, 2014
)
0.4
" This compound had good in vitro and in vivo potency, low rates of metabolism, moderate permeability, and good oral bioavailability in rodents."( Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Fish, S; Follows, B; Huang, A; Hubeau, C; Janz, K; Kaila, N; Leung, L; Lowe, M; Mansour, TS; Moretto, A; Morgan, P; Page, K; Saiah, E; Thomason, J; Williams, C; Xu, X, 2014
)
0.4
" These findings suggest that elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate should be administered with food, and that the bioavailability of elvitegravir and tenofovir is not affected by the type of meal ingested."( Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Matsuki, S; Nishino, N; Shiomi, M, 2014
)
0.4
"The purpose of this study was to improve the gastric solubility and bioavailability of rebamipide (RBM) by preparing the RBM solid dispersion tablet (RBM-SDT) from solid dispersion powder prepared by spray-drying technique."( Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability.
Choi, HG; Choi, IS; Choi, JY; Kim, JO; Pradhan, R; Tran, TH; Yong, CS, 2015
)
0.42
"This 2-arm, phase 1, crossover study compared the relative bioavailability of two dovitinib (TKI258) capsule formulations [anhydrate clinical service form (CSF) and monohydrate final market image (FMI); Arm 1] and determined the effect of food on dovitinib exposure (Arm 2)."( The effect of formulation and food consumption on the bioavailability of dovitinib (TKI258) in patients with advanced solid tumors.
Britten, CD; George, D; Kulkarni, S; Liu, A; Mortimer, J; Quinlan, M; Scott, JW; Sharma, S, 2014
)
0.4
"A series of Phase I studies was conducted in healthy volunteers to examine the systemic bioavailability and safety of topical ozenoxacin."( Systemic bioavailability, safety and tolerability of topical ozenoxacin in healthy adult volunteers.
Albareda, N; Febbraro, S; Gropper, S; Santos, B, 2014
)
0.4
" The validated methods were successfully applied to an absolute bioavailability clinical study of nemonoxacin malate capsule."( Determination of a novel nonfluorinated quinolone, nemonoxacin, in human feces and its glucuronide conjugate in human urine and feces by high-performance liquid chromatography-triple quadrupole mass spectrometry.
Cao, G; Guo, B; He, G; Shi, Y; Tsai, CY; Wu, X; Yu, J; Zhang, J, 2015
)
0.42
"This 2-arm crossover study compared the relative bioavailability of two dovitinib (TKI258) formulations [anhydrate clinical service form (CSF) capsule and monohydrate final market image (FMI) tablet; Arm 1] and determined the effect of food on dovitinib exposure (Arm 2)."( A randomized, crossover phase 1 study to assess the effects of formulation (capsule vs tablet) and meal consumption on the bioavailability of dovitinib (TKI258).
George, D; Infante, JR; Liu, A; Quinlan, M; Ramanathan, RK; Scott, JW; Sharma, S; Tan, E, 2015
)
0.42
" The oral bioavailability of Phe-Ψ-Ala in the presence and absence of MFLX was 41."( Possible interaction of quinolone antibiotics with peptide transporter 1 in oral absorption of peptide-mimetic drugs.
Arakawa, H; Hatano, Y; Idota, Y; Kamioka, H; Kanagawa, M; Morimoto, K; Ogihara, T; Yano, K, 2016
)
0.43
" Here, we described ZLD1039 a potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2, which inhibited breast tumor growth and metastasis."( Selective inhibition of EZH2 by ZLD1039 blocks H3K27 methylation and leads to potent anti-tumor activity in breast cancer.
Feng, Q; Gao, T; Lei, Q; Shi, Y; Song, X; Wang, N; Wei, Y; Xia, Y; Xiong, M; Yang, F; Ye, T; You, X; Yu, L; Zhang, L; Zhu, Y, 2016
)
0.43
" Much progress has been made over the past decade with the development of orally bioavailable small molecule drugs that target defective CFTR proteins caused by specific mutations."( New and emerging targeted therapies for cystic fibrosis.
Quon, BS; Rowe, SM, 2016
)
0.43
"This randomized, two-way crossover study evaluated the bioavailability of elvitegravir administered as the new individual tablet containing 150 mg and a cobicistat 150 mg tablet, concomitantly with a fixed-dose combination tablet containing 200 mg of emtricitabine and 300 mg of tenofovir disoproxil fumarate (EVG + COBI + FTC/TDF), in comparison with a single-tablet regimen containing the same dose of each component (EVG/COBI/FTC/TDF)."( Pharmacokinetic and bioequivalence evaluation of single-tablet and separate-tablet regimens for once-daily cobicistat-boosted elvitegravir in healthy Japanese male subjects: A randomized, two-way crossover study.
Ikeda, A; Irie, S; Ishikawa, T; Kimura, M; Kumagai, Y; Matsuki, S; Nishino, N; Shiomi, M,
)
0.13
"Cavosonstat (N91115), an orally bioavailable inhibitor of S-nitrosoglutathione reductase, promotes cystic fibrosis transmembrane conductance regulator (CFTR) maturation and plasma membrane stability, with a mechanism of action complementary to CFTR correctors and potentiators."( Pharmacokinetics and safety of cavosonstat (N91115) in healthy and cystic fibrosis adults homozygous for F508DEL-CFTR.
Casey, A; Chmiel, JF; Donaldson, SH; Flume, PA; Mandagere, A; McCoy, K; Shoemaker, SA; Solomon, GM; Taylor-Cousar, JL; Troha, JM; Zeitlin, PL; Zemanick, ET, 2017
)
0.46
" There is evidence that the bioavailability of ivacaftor in the body may be influenced by the multi-drug exporter P-glycoprotein."( Investigation of the effects of the CFTR potentiator ivacaftor on human P-glycoprotein (ABCB1).
Ford, RC; Lingam, S; Thonghin, N, 2017
)
0.46
"Rebamipide (RBP) is a potent anti-ulcer and anti-oxidative agent, which is a BCS class IV drug with a low oral bioavailability of less than 10%."( Capmul MCM/Solutol HS15-Based Microemulsion for Enhanced Oral Bioavailability of Rebamipide.
Cho, HJ; Kim, DD; Kim, KT; Lee, JY; Park, JH; Yoon, IS, 2017
)
0.46
" A prodrug strategy was also investigated to address the problem of low aqueous solubility and low bioavailability of the antitumor agent CHM-1."( CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells.
Ho, CT; Hung, CH; Hung, CM; Kuo, SC; Lin, YC; Liu, BL; Liu, CW; Way, TD, 2018
)
0.48
"Rebamipide has low oral bioavailability (10%) due to its low solubility and permeability."( Lipid Nanoemulsions of Rebamipide: Formulation, Characterization, and In Vivo Evaluation of Pharmacokinetic and Pharmacodynamic Effects.
Guda, S; Narala, A; Veerabrahma, K, 2019
)
0.51
" To improve solubility and bioavailability of highly potent anti-retroviral drugs, we explored the use of a nanoparticle (NP) for formulating a combination of two water-insoluble HIV inhibitors."( Antiretroviral Hydrophobic Core Graft-Copolymer Nanoparticles: The Effectiveness against Mutant HIV-1 Strains and in Vivo Distribution after Topical Application.
Alfaro, J; Bogdanov, AA; Bolotin, E; Castillo, G; Gottikh, MB; Gupta, S; Leporati, A, 2019
)
0.51
" Structure guided optimization of an imidazo-quinolinones based pan-PI3K/m-TOR inhibitor (Dactolisib) led to the discovery of a potent and orally bioavailable PI3Kδ isoform selective inhibitor (10h), with an improved efficacy in the animal models."( Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.
Bahekar, R; Bandyopadhyay, D; Chatterjee, A; Chopade, R; Dave, B; Desai, RC; Funde, R; Ghoshdastidar, K; Giri, P; Kumar, J; Mahapatra, J; Patel, D; Sachchidanand, S; Soman, S; Vyas, P, 2019
)
0.51
" Herein, we report the discovery and optimization of a series of quinolinones to provide potent and orally bioavailable mIDH1 inhibitors with selectivity over wild-type IDH1."( Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Ashwell, S; Bair, KW; Barr, KJ; Campbell, AM; Caravella, JA; Castro, J; Clarke, A; Diebold, RB; Diep, H; Dinsmore, C; Ericsson, A; Fritzen, E; Gotur, D; Gustafson, GR; Hubbs, SE; Josephine, HR; Katz, M; Kauffman, G; Kershaw, M; Lancia, DR; Lin, J; Lu, W; Luke, GP; Shelekhin, T; Toms, AV; Walker, D; Wang, L; Wang, Z; Yao, L, 2019
)
0.51
"To improve the solubility and oral bioavailability of a novel antimalarial agent ELQ-331(a prodrug of ELQ-300), spray-dried dispersions (SDD) and a self-emulsifying drug delivery system (SEDDS) were developed."( Improving solubility and oral bioavailability of a novel antimalarial prodrug: comparing spray-dried dispersions with self-emulsifying drug delivery systems.
Frueh, L; Green, C; Liu, M; Mutyam, SK; Nilsen, A; Potharaju, S; Pou, S; Riscoe, MK; Shankar, G; Winter, R, 2020
)
0.56
" In addition, 20f demonstrated good bioavailability (F = 41."( Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway.
Chen, L; Chen, Y; Deng, D; Liu, K; Pei, H; Tang, M; Xue, L; Yang, T; Yang, Z; Ye, H; Zheng, S, 2020
)
0.56
" However, its poor water solubility and weak cellular bioavailability hinder its use as a therapeutic agent for cancer."( Antitumor Efficacy of Ceranib-2 with Nano-Formulation of PEG and Rosin Esters.
Ben Taleb, A; Gözüaçık, D; Ilgar, M; Karakuş, S; Kilislioğlu, A; Kutlu, HM; Kutlu, Ö; Tan, E, 2021
)
0.62
" Compound 34 is orally bioavailable and displayed favorable pharmacokinetic (PK) properties."( Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.
Ahirrao, P; Bakhle, D; Bernstein, PR; Bhat, T; Bhonde, M; Bommakanti, A; Bora, P; Francis, A; George, KS; Gole, G; Goyal, H; Gundu, J; Gupta, NR; Gupta, R; Hajare, AK; Jadhav, GR; Jagdale, AR; Jana, G; Kale, R; Kamalakannan, P; Kamble, N; Kamboj, RK; Karche, NP; Khanwalkar, H; Khedkar, N; Kukreja, G; Kumar, P; Kumar, R; Kurhade, SP; Limaye, R; Mallurwar, S; Modi, D; Naidu, S; Naik, KR; Narasimham, L; Nemmani, K; Nigade, PB; Pagdala, V; Palle, VP; Patil, V; Pawar, S; Pawar, Y; Phukan, S; Powar, RG; Praveen Kumar, VR; Rao Irlapati, N; Shaikh, JS; Shankar, RB; Sharma, S; Singh, M; Sinha, N; Thube, BR; Tilekar, AR; Volam, H; Wahid, S, 2020
)
0.56
" Rebamipide, classified into BCS class IV, is one of those drugs which provide very low bioavailability and/or the difficulty of formulation for oral administration."( Improvement of lipid solubility and oral bioavailability of a poorly water- and poorly lipid-soluble drug, rebamipide, by utilizing its counter ion and SNEDDS preparation.
Higaki, K; Maruyama, M; Masuda, K; Ogawara, KI; Okawa, S; Sumimoto, Y, 2021
)
0.62
"In this study, a novel rebamipide-loaded spray-dried microsphere (RSM) with enhanced drug solubility and oral bioavailability has been developed utilizing meglumine, an alkalizing agent."( Development of rebamipide-loaded spray-dried microsphere using distilled water and meglumine: physicochemical characterization and pharmacokinetics in rats.
Cho, JH; Choi, HG; Ko, DW, 2021
)
0.62
"Broad antibacterial spectrum, high oral bioavailability and excellent tissue penetration combined with safety and few, yet rare, unwanted effects, have made the quinolones class of antimicrobials one of the most used in inpatients and outpatients."( Biological Effects of Quinolones: A Family of Broad-Spectrum Antimicrobial Agents.
Bucarey, SA; Hidalgo, AA; Millanao, AR; Mora, AY; Villagra, NA, 2021
)
0.62
"Rebamipide (REB) a potent anti-ulcer agent, has not been exploited to its full potential, owing to it extremely poor solubility, leading to highly diminutive bioavailability (<10%)."( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies.
Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021
)
0.62
"5 folds enhancement in relative bioavailability and remarkable amplification in anti-ulcer, anti-inflammatory and the antioxidant potential of these cocrystals were observed."( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies.
Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021
)
0.62
" Unexpectedly, despite enhanced dissolution rate in a controlled manner, a designed bilayer tablet had no dose- and dosage form dependent in vivo bioavailability in beagle dogs as compared with IR 100 mg RBM reference tablet."( Design and evaluation of in vivo bioavailability in beagle dogs of bilayer tablet consisting of immediate release nanosuspension and sustained release layers of rebamipide.
Cao, QR; Cui, JH; Jin, G; Jung, M; Lee, BJ; Ngo, HV; Park, C; Wang, J, 2022
)
0.72
" In vivo, using IVA-suspension (Fed) as a reference, the relative oral bioavailability of IVA-suspension (Fasted), IVA-SNEDDS (Fasted), and IVA-SNEDDS (Fed) were 23."( Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase.
Miao, Y; Sun, J; Wang, J; Zhao, S; Zuo, J, 2022
)
0.72
" Moreover, ADME studies were conducted, disclosing an eligible bioavailability score of >0."( Structure based design and synthesis of 3-(7-nitro-3-oxo-3,4-dihydroquinoxalin-2-yl)propanehydrazide derivatives as novel bacterial DNA-gyrase inhibitors: In-vitro, In-vivo, In-silico and SAR studies.
El Saeed, HS; Elmaaty, AA; Ezz Eldin, RR; Salah, M; Saleh, MA; Saleh, MM, 2022
)
0.72
" These include cannabinoids and drug combinations that inhibit dextromethorphan metabolism peripherally, thereby increasing its bioavailability in the brain."( Management of neuropsychiatric symptoms in dementia.
Devanand, DP, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" The emergence of the newer antibiotic classes, including the second and third-generation cephalosporins and the fluoroquinolones, has provided the clinician with agents that offer a broad spectrum of activity, good patient acceptance, a well-tolerated safety profile, and convenient dosage regimens due to their unique pharmacokinetic profiles."( New considerations in treatment of urinary tract infections in adults.
Faro, S, 1992
)
0.28
" The results suggest that nedocromil sodium may permit a reduction in theophylline dosage and possibly substitute for theophylline in previously dependent patients."( Effects of the addition of nedocromil sodium to maintenance bronchodilator therapy in the management of chronic asthma.
Callaghan, B; Clancy, L; Teo, NC, 1992
)
0.28
" 7e, 9e, 13a, 13d, 18, 20, 21, and 23, when dosed orally in conscious spontaneously hypertensive rats."( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992
)
0.28
" At 110 min after dosing, subjects took a slow, full inspiration with a 30 s breath-hold, and at 150 min after dosing the subjects performed one single forced expiration."( The effect of respiratory manoeuvres and pharmacological agents on the pharmacokinetics of nedocromil sodium after inhalation.
Holgate, ST; Honeywell, RG; Renwick, AG; Singh, S; Summers, QA, 1992
)
0.28
" These results attest to the value of the convenience and simplicity of the oral dosing regimen for lomefloxacin."( The U.S. clinical experience with lomefloxacin, a new once-daily fluoroquinolone.
Rizk, E, 1992
)
0.28
" Both total clearance and renal clearance significantly correlate with creatinine clearance for these fluoroquinolones, and creatinine clearance is a useful clinical marker on which to base dosage adjustments."( Influence of renal function on the pharmacokinetics of lomefloxacin compared with other fluoroquinolones.
Blum, RA, 1992
)
0.28
"Six dosage regimens of oral lomefloxacin, a new difluorinated quinolone, were given to healthy volunteer subjects for 7 days in a randomized, placebo-controlled trial to evaluate pharmacokinetics and tolerability and to determine the optimum dosage schedule."( Multiple-dose pharmacokinetics of lomefloxacin: rationale for once-a-day dosing.
Mant, TG, 1992
)
0.28
" Dosage adjustments should not be necessary in elderly patients with only minor changes in renal function caused by age-related changes in physiology."( Quinolone pharmacokinetics in the elderly.
Goss, TF; Schentag, JJ, 1992
)
0.28
" The pharmacokinetics of lomefloxacin are dependent on renal function, and appropriate dosage adjustment is necessary when creatinine clearance is less than 30 mL/min/1."( Single-dose pharmacokinetics of lomefloxacin in patients with normal and impaired renal function.
Marstein, S; Nilsen, OG; Saltvedt, E; Walstad, RA, 1992
)
0.28
" The results of this study demonstrate that once-daily treatment with 400 mg lomefloxacin is as effective as twice-daily dosing with 400 mg in patients with acute bacterial exacerbations of chronic bronchitis."( A double-blind study of two dosage regimens of lomefloxacin in bacteriologically proven exacerbations of chronic bronchitis of gram-negative etiology.
Kemper, P; Köhler, D, 1992
)
0.28
" Analyses of variance found no significant differences among the dosage groups in total apparent clearances (CLT/F), renal clearances (CLR), or nonrenal clearances, which averaged 197, 119, and 78 ml/min, respectively."( Pharmacokinetics of temafloxacin in humans after multiple oral doses.
Carpentier, P; Granneman, GR; Morrison, PJ; Pernet, AG, 1992
)
0.28
" Because the altered temafloxacin pharmacokinetics appear to be primarily due to impaired renal function, this should be the main determinant of temafloxacin dosage in patients with liver disease."( Pharmacokinetics of temafloxacin in patients with liver impairment.
Fabian, W; Granneman, GR; Kinzig, M; Kirch, W; Locke, C; Mahr, G; Naber, KG; Nickel, P; Sörgel, F, 1992
)
0.28
" This may partly be explained by intertrial differences in dosage and study design."( Effects of temafloxacin and ciprofloxacin on the pharmacokinetics of caffeine.
Fuhr, U; Granneman, GR; Kinzig, M; Mahr, G; Muth, P; Nickel, P; Patterson, K; Sörgel, F; Stephan, U, 1992
)
0.28
" A serum concentration-time data analysis was performed to evaluate the oral enrofloxacin dose and dosing interval for nonfasted macaques."( Enrofloxacin treatment of long-tailed macaques with acute bacillary dysentery due to multiresistant Shigella flexneri IV.
Aucoin, DP; Hirsh, DC; Line, AS; Paul-Murphy, J, 1992
)
0.28
" Twenty-seven atopic asthmatic adults (21-39 years), with a measurable maximal-response plateau on the dose-response curve (20-55% fall in FEV1), were randomly allocated into two parallel treatment groups."( The long-term effect of nedocromil sodium on the maximal degree of airway narrowing to methacholine in atopic asthmatic subjects.
Bel, EH; Dijkman, JH; Sont, JK; Sterk, PJ, 1992
)
0.28
" In the rat 4f inhibited LTB4 synthesis in blood ex vivo and in zymosan-inflamed air pouch exudate with an ED50 3 h after oral dosing of 10 mg/kg in each system."( Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.
Bird, TG; Bruneau, P; Crawley, GC; Dowell, RI; Edwards, PN; Foster, SJ; Giroaeau, JM; McMillan, RM; Walker, ER; Waterson, D, 1992
)
0.28
" Ester 11b, acid 12b, amide 13d, and sulfone 29c protected against thrombus formation in two different animal models following oral dosing and were found to be superior to anagrelide (2) and BMY 20844 (5)."( Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.
Baryla, UM; Buchanan, JO; Gamberdella, M; Gillespie, E; Meanwell, NA; Pearce, BC; Roth, HR; Smith, EC; Wedding, DL; Wright, JJ, 1992
)
0.28
" By serial dosing (once a day, 5 or 6 times per week, during the 3rd-5th months postinoculation), 10 mg/kg of sparfloxacin displayed bactericidal-type activity and bacteriostatic activity was present at daily doses of 5 and 2 mg/kg."( Activity of sparfloxacin against Mycobacterium leprae inoculated into footpads of nude mice.
Gidoh, M; Tsutsumi, S, 1992
)
0.28
" Rufloxacin was administered orally at the dosage of 400 mg/die the first day; 200 mg/die the following 6 days or more."( [Treatment with rufloxacin of complicated urinary tract infections].
Caglio, G; Cantoni, L; Carmignani, G; Gusmitta, A; Maffezzini, M; Monti Bragadin, C; Samer, L, 1992
)
0.28
"The chemistry, mechanism of action, antimicrobial spectrum, pharmacokinetics, clinical efficacy, safety, drug interactions, and dosage and administration of lomefloxacin and temafloxacin, two new antimicrobials, are presented."( Lomefloxacin and temafloxacin: two new fluoroquinolone antimicrobials.
Nix, DE; Symonds, WT, 1992
)
0.28
" The observation that serum (and tissue) concentrations of temafloxacin exceeded the minimal inhibitory concentration of the test organism over the whole dosing interval (12 hr), could account for its efficacy in severe pneumococcal disease."( Kinetic disposition of temafloxacin and ciprofloxacin in a murine model of pneumococcal pneumonia. Relevance for drug efficacy.
Azoulay-Dupuis, E; Bauchet, J; Pocidalo, JJ; Vallée, E, 1992
)
0.28
" The dose-response curve for AVP was shifted to the right in parallel by OPC-31260 but not by OPC-21268."( Potent antagonistic action of OPC-31260, a vasopressin V2 receptor antagonist, on [Arg8]vasopressin-induced vasoconstriction in isolated simian femoral arteries.
Chiba, S; Tsukada, M, 1992
)
0.28
" dosage but without statistical significance."( Comparison of nedocromil sodium at two dosage frequencies with placebo in the management of chronic asthma.
Drennan, C; Holst, P; Jones, D; Rea, H; Thornley, P; Wells, A, 1992
)
0.28
"5, and 11 mg/kg of body weight, every 12 hours for 4 days, with a 4-week interval between dosage regimens."( Pharmacokinetic evaluation of enrofloxacin administered orally to healthy dogs.
Hauptman, JG; MacDonald, KH; Stein, GE; Walker, RD, 1992
)
0.28
" A dose-response experiment was performed with clarithromycin at 50, 100, 200, or 300 mg/kg of body weight administered daily by gavage to mice infected with approximately 10(7) viable MAC."( Activity of clarithromycin against Mycobacterium avium complex infection in beige mice.
Cynamon, MH; DeStefano, MS; Klemens, SP, 1992
)
0.28
" Our results indicate that a once-daily dosage of sparfloxacin should be adequate to treat systemic infections caused by most common bacterial pathogens."( Pharmacokinetics and inflammatory fluid penetration of sparfloxacin.
Andrews, JM; Cooper, MA; Johnson, JH; Wise, R, 1992
)
0.28
" Serial plasma and sputum samples and fractional urine samples were obtained over a steady-state dosing interval."( Steady-state pharmacokinetics and sputum penetration of lomefloxacin in patients with chronic obstructive pulmonary disease and acute respiratory tract infections.
Glerum, JH; Hoepelman, AI; Kovarik, JM; Rozenberg-Arska, M; Sips, PA; Smit, JM; Verhoef, J, 1992
)
0.28
" leprae; temafloxacin and sparfloxacin were the most active, being fully bactericidal at all three dosage schedules."( Activities of various quinolone antibiotics against Mycobacterium leprae in infected mice.
Gelber, RH; Iranmanesh, A; Murray, L; Siu, P; Tsang, M, 1992
)
0.28
" In conclusion, once-daily oral dosing with lomefloxacin is a safe and efficacious alternative to twice-daily dosing with TMP/SMX in the treatment of uncomplicated urinary tract infections."( Uncomplicated urinary tract infections: lomefloxacin versus trimethoprim/sulphamethoxazole.
Capron, MH; Guibert, J, 1992
)
0.28
" The trough SBAs of the 4 fluoroquinolones suggest that the time interval of administration of CPLX and OFLX should be more than 8 hours, but increase of the dosage or shortening of the time interval between the administrations is recommended for ENX and NFLX."( Comparison of serum bactericidal activity of 4 fluoroquinolones in healthy volunteers.
Liu, YN; Sun, XD; Wang, R; Zhao, HZ, 1992
)
0.28
" Based on an evaluation of adverse events among elderly patients with varying degrees of renal impairment, dosage adjustment of temafloxacin is necessary only for elderly patients with severe renal impairment."( Temafloxacin: a safe antibiotic for the elderly, patients with comorbidities, and other special populations.
Pernet, AG, 1991
)
0.28
" Evidence of cartilaginous joint damage was observed in puppies receiving oral temafloxacin, in young dogs receiving intravenous temafloxacin, and in a single dog receiving a lethal dosage in a dose range-finding study."( Comparison of organ-specific toxicity of temafloxacin in animals and humans.
Krasula, RW; Pernet, AG, 1991
)
0.28
" The longer half-life of temafloxacin enables a once-daily dose regimen, whereas the usual recommended dosage of ciprofloxacin is twice daily."( Comparative pharmacokinetics of ciprofloxacin and temafloxacin in humans: a review.
Kinzig, M; Mahr, G; Muth, P; Naber, KG; Sorgel, F, 1991
)
0.28
" As the difference in elimination half-life was small, alteration of the usual twice-daily dosage regimen is not necessary in the elderly."( The influence of age on the pharmacokinetics of temafloxacin.
Granneman, GR; Guay, DR, 1991
)
0.28
" Twelve healthy subjects (8 males, 4 females; average age and weight 34 years and 62 kg, respectively) were given oral controlled-release theophylline in an individualized dosage to achieve a target plasma level of 10 mg/L."( Effect of temafloxacin on the pharmacokinetics of theophylline.
Callens, E; Chauvin, JP; Hazebroucq, J; Ruff, F; Santais, MC, 1991
)
0.28
" It is suggested that a once daily dose of 400 mg lomefloxacin is suitable for the elderly and that no dosage modification is needed in this patient group."( The pharmacokinetics of lomefloxacin in elderly patients with urinary tract infection following daily dosing with 400 mg.
Cowling, P; Lovering, AM; MacGowan, AP; McMullin, CM; Reeves, DS; Rogers, S; White, LO, 1991
)
0.28
" tuberculosis H37Rv strain, the minimal effective dosage of sparfloxacin, as assessed by survival rate, spleen enlargement and gross lung lesions, was 12."( In vitro and in vivo activities of sparfloxacin (AT-4140) against Mycobacterium tuberculosis.
Grosset, J; Ji, B; Truffot-Pernot, C, 1991
)
0.28
" Within 48 h, about half of the dosed radioactivity was excreted in the bile, and part of which was re-absorbed."( Disposition and metabolism of [14C]sparfloxacin in the rat.
Furukawa, H; Hashimoto, M; Matsunaga, Y; Miyazaki, H; Nambu, K; Oh-e, Y; Yoshida, K, 1991
)
0.28
" Four rabbits were each given enrofloxacin as a single 5 mg/kg of body weight dosage by IV, SC, and oral routes over 4 weeks."( Pharmacokinetic properties of enrofloxacin in rabbits.
Babish, JG; Brooks, DL; Broome, RL; Conzelman, GM; Copeland, DD, 1991
)
0.28
" Steady-state peak serum levels are approximately 1 mg/L per 100 mg oral dose administered; thus, the steady-state peak serum level after 600 mg bd oral dosing is approximately 6 mg/L."( A review of the pharmacokinetic profile of temafloxacin.
Dudley, MN, 1991
)
0.28
" Pharmacokinetics of evocarpine after intravenous injection was expressed in a one-compartment model, showing a linear elimination of plasma evocarpine up to a dosage of 75 mg/kg."( Pharmacological properties of galenical preparation. XV. Pharmacokinetics study of evocarpine and its metabolite in rats.
Chen, XF; Kanemaki, S; Kano, Y; Komatsu, K; Zong, Q, 1991
)
0.28
" Compared with the CLT/F in the subjects with normal renal function, CLT/F was reduced 60% in subjects with a CLCR of less than 40 ml/min, indicating that the dosage should be reduced by at least one-half for patients with comparable impairment."( Temafloxacin pharmacokinetics in subjects with normal and impaired renal function.
Braeckman, R; Craft, JC; Granneman, GR; Kraut, J; Shupien, S, 1991
)
0.28
" Lomefloxacin offers certain advantages compared with other quinolone antibacterial drugs in that it may be conveniently administered once daily and theophylline dosage adjustment does not appear to be necessary in patients receiving this bronchodilator concomitantly."( Lomefloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
Goa, KL; Wadworth, AN, 1991
)
0.28
" Some of the more resistant strains of Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, and Pseudomonas aeruginosa were studied in a dynamic in-vitro model in order to study dosing strategies."( Antimicrobial effects of lomefloxacin in vitro.
Begg, EJ; Boswell, DR; Chambers, ST; Peddie, BA; Robson, RA, 1991
)
0.28
" Lomefloxacin is well absorbed after oral administration giving high blood and urine concentrations and its prolonged half-life means once daily dosing in the treatment of many types of bacterial infection may be possible."( Antibacterial activity of lomefloxacin.
Leigh, DA; Tait, S; Walsh, B, 1991
)
0.28
"0 hours after dosing with their OCS on days 5, 6, 7 and 8 of their contraceptive cycle, for measurement of EE2, Ng, FSH and LH by radioimmunoassay."( The lack of interaction between temafloxacin and combined oral contraceptive steroids.
Back, DJ; Mant, T; Martin, C; Millar, E; Morrison, P; Orme, M; Tjia, J, 1991
)
0.28
"0 hours after dosing with OCs on days 5, 6, 7, and 8 of their contraceptive cycle, for measurement of EE2, Ng, FSH, and LH by radioimmunoassay."( The lack of interaction between temafloxacin and combined oral contraceptive steroids.
Back, DJ; Mant, T; Martin, C; Millar, E; Morrison, P; Orme, M; Tjia, J, 1991
)
0.28
" Familiarity with commonly encountered adverse antibiotic reactions, dosage guidelines, and special situations (pregnancy, pediatric patients) will help avoid problems associated with antibiotic use."( Antibiotics and infectious diseases.
Liu, HH, 1990
)
0.28
" Since intravenously dosed dogs eliminated 50% of the dose by nonrenal processes, urinary recoveries approaching two-thirds of the dose in humans were consistent with high, if not quantitative, absorption."( Pharmacokinetics of temafloxacin in humans after single oral doses.
Carpentier, P; Granneman, GR; Morrison, PJ; Pernet, AG, 1991
)
0.28
" No additional dosage adjustments appear to be necessary for hemodialysis patients."( Pharmacokinetics of lomefloxacin in renally compromised patients.
Blum, RA; Schentag, JJ; Schultz, RW, 1990
)
0.28
"5 microgram/ml were inhibited with both dosing schedules."( Antibacterial activity of lomefloxacin in a pharmacokinetic in vitro model.
Rustige, C; Wiedemann, B, 1990
)
0.28
" The eradication rate on each observation day was 100% in both dosage groups."( [Epidemiological and therapeutic study on gonorrheal infection--study on NY-198 (lomefloxacin) single administration therapy. Sapporo Clinical Research Group for STD].
Gohro, T; Hayashi, K; Henmi, I; Kato, S; Kumamoto, Y; Sakai, S; Tabata, S; Tanda, H; Tsunekawa, T; Yoshio, H, 1990
)
0.28
" Dosage adjustments are required, particularly in severe renal failure and for the drugs almost exclusively excreted, in unchanged form, via the renal route."( Pharmacokinetics of quinolones in renal insufficiency.
Borsa-Lebas, F; Dhib, M; Fillastre, JP; Humbert, G; Leroy, A; Moulin, B, 1990
)
0.28
" Specific lung resistance (SRL) was measured to assess bronchial responses to PAF, and airway responsiveness was determined by deriving a provocative dose of carbachol in breath units causing an increase in SRL to 4 L times centimeters of H2O per liters per second (PD4) from carbachol dose-response curves."( PAF-induced airway responses in sheep: effects of a PAF antagonist and nedocromil sodium.
Abraham, WM; Ahmed, T; D'Brot, J; Fernandez, A; Mansour, E; Soler, M, 1990
)
0.28
"1 X 10(-6) M) and matched placebo were administered by identical metered dose inhalers 30 min before a dose-response to sodium metabisulphite (5-100 mg ml-1) was performed."( Inhaled sodium metabisulphite induced bronchoconstriction: inhibition by nedocromil sodium and sodium cromoglycate.
Dixon, CM; Ind, PW, 1990
)
0.28
"The fluoroquinolones, temafloxacin, sarafloxacin, and difloxacin, are determined in the bulk drug substances and in a variety of dosage form using high-performance liquid chromatography (HPLC)."( Determination of temafloxacin, sarafloxacin, and difloxacin in bulk drug and dosage forms by high-performance liquid chromatography.
Bauer, JF; Elrod, L; Fornnarino, JR; Heathcote, DE; Krogh, SK; Linton, CL; Norris, BJ; Quick, JE, 1990
)
0.28
" Dosage adjustments are necessary in uremic patients."( Lomefloxacin pharmacokinetics in subjects with normal and impaired renal function.
Fillastre, JP; Humbert, G; Leroy, A, 1990
)
0.28
" The dose-response curves for NKA after nedocromil sodium treatment were significantly shifted to the right compared to the curve after placebo-treatment."( The effect of nedocromil sodium on the bronchoconstrictor effect of neurokinin A in subjects with asthma.
Joos, GF; Pauwels, RA; Van der Straeten, ME, 1989
)
0.28
" Given intraperitoneally at the single dosing range of 10-100 mg/kg, OPC-12759 inhibited the formation of these acute gastric ulcer models."( Effect of OPC-12759, a novel antiulcer agent, on chronic and acute experimental gastric ulcer, and gastric secretion in rats.
Imaizumi, T; Ishiyama, H; Kanbe, T; Yabuuchi, Y; Yamasaki, K, 1989
)
0.28
" In guinea-pig airway, microvascular leakage induced by allergen was significantly inhibited by prior treatment with nedocromil sodium (100 micrograms/kg IV), but this had no effect on histamine-induced leakage and reduced PAF-induced leakage only at a dosage of 5 mg/kg."( Effects of nedocromil sodium on airway microvascular leakage and neural reflexes.
Barnes, PJ, 1989
)
0.28
" Azithromycin was more potent than the other macrolides in experimental animal infection, eradicating the organism in all animals tested at a dosage of 8 mg/kg."( Comparative antimicrobial activity of the new macrolides against Borrelia burgdorferi.
Gross, B; Preac-Mursic, V; Schierz, G; Süss, E; Wilske, B, 1989
)
0.28
" These results suggest that asthmatic patients who require inhaled steroids show better control of their asthma with the addition of nedocromil sodium than of placebo over a four week period after reduction of the dosage of their inhaled steroids."( Nedocromil sodium in adults with asthma dependent on inhaled corticosteroids: a double blind, placebo controlled study.
Allan, GW; Bone, MF; Burge, PS; Connolly, CK; Dent, RG; Keaney, NP; Kubik, MM; Summers, GD, 1989
)
0.28
" The experimental application of enrofloxacin (Baytril) at a dosage of 100 mg/l drinking water for 10 days resulted in a stop of the mortality rate, increment of egg production and reduction of Salmonella excretion."( [Therapy trials with enrofloxacin (Baytril) in a laying hen flock with Salmonella pullorum infections].
Glünder, G; Göbel, T; Kaleta, EF; Redmann, T; Schildger, B, 1989
)
0.28
" Daily dosage of LFLX and PPA was 600 mg and 2000 mg, respectively administered orally divided into 4 doses."( [Comparison of clinical efficacy of lomefloxacin (LFLX, NY-198) and pipemidic acid (PPA) in the treatment of infectious enteritis by a double-blind method. The Japan Research Committee of Lomefloxacin Research Group Enteritis].
Aoki, T; Kanehisa, N; Matsubara, Y; Murata, M; Nitta, Y; Sagara, H; Seo, T; Shimizu, N; Takizawa, Y; Tomizawa, I, 1989
)
0.28
" This dose, interval, and duration of dosing were chosen to be identical to the highest anticipated clinical dose for the longest anticipated clinical duration."( Pharmacokinetics and safety of lomefloxacin following multiple doses.
Adams, MA; Hunt, TL,
)
0.13
" Serum and blister fluid levels in excess of 1 mg/l were present for at least 8 h post dose, suggesting that a once or twice daily dosing regimen would be suitable for the treatment of infections caused by susceptible organisms."( The in-vitro activity, pharmacokinetics and tissue penetration of temafloxacin.
Andrews, JM; Ashby, JP; Nye, K; Shi, YG; Wise, R, 1989
)
0.28
" Airway responsiveness was assessed by determining from dose-response curves the carbachol concentration (in % wt/vol) that increased sRL to 5 cmH2O/s."( Nedocromil sodium in allergen-induced bronchial responses and airway hyperresponsiveness in allergic sheep.
Abraham, WM; Eldridge, M; Garrido, R; Nieves, L; Stevenson, JS, 1988
)
0.27
"The safety, acceptability and efficacy of nedocromil sodium, given by metered dose inhaler at a dosage of 4 mg four times daily, were investigated in a 52-week open assessment study of 79 perennial bronchial asthmatic patients maintained on oral bronchodilator therapy."( The acceptability, safety and efficacy of nedocromil sodium in long-term clinical use in patients with perennial asthma.
Carrasco, E; Sepulveda, R,
)
0.13
" The severity of these symptoms increased dose-dependently, and the upper limit dosage of OPC was considered to be 5 mg for the healthy volunteers."( Phase 1 study of a new antipsychotic drug, OPC-4392.
Fukuyama, Y; Ishigooka, J; Ishii, Y; Miura, S; Murasaki, M; Takahashi, A, 1988
)
0.27
" The high efficacy of the low dosage of enrofloxacin in this clinical syndrome may be explained by its antibacterial activity against Pasteurella species and Mycoplasma species."( Effect of enrofloxacin therapy on shipping fever pneumonia in feedlot cattle.
Art, T; Lekeux, P, 1988
)
0.27
" MY-1250 had no effect on the norepinephrine-induced dose-response curve in isolated rat aorta."( [Cardiovascular effects of MY-5116 and MY-1250].
Hanazuka, M; Hara, Y; Horii, D; Nishi, H, 1986
)
0.27
" This study suggests that either once-daily or twice-daily dosage of lomefloxacin should be sufficient to treat urinary or systemic infections, respectively, caused by susceptible pathogens."( Pharmacokinetics and tissue penetration of orally administered lomefloxacin.
Andrews, JM; Ashby, JP; Griggs, D; Stone, JW; Wise, R, 1988
)
0.27
" Males were dosed for 71 days before pairing and then until termination, and females were dosed for 15 days before pairing, throughout mating and until Day 7 of gestation."( Reproductive studies of NY-198 in rats. I. Fertility study.
Higgins, C; McAnulty, PA; Tesh, JM; Tesh, SA; Wilby, OK; Willoughby, CR, 1988
)
0.27
" At the highest dosage (300 mg/kg/day), there was a small reduction in maternal weight gain and a transient reduction in food intake during the treatment period."( Reproductive studies of NY-198 in rats. II. Teratology study.
McAnulty, PA; Tesh, JM; Tesh, SA; Wilby, OK; Willoughby, CR, 1988
)
0.27
" There was a slight maternal response at the highest dosage (300 mg/kg/day), including increased salivation after dosing, reduced food intake in the treated period of gestation and increased water intake during the lactation period."( Reproductive studies of NY-198 in rats. III. Perinatal and postnatal study.
Higgins, C; McAnulty, PA; Tesh, JM; Tesh, SA; Wilby, OK; Willoughby, CR, 1988
)
0.27
" Ciprofloxacin is effective in single dosage against urogenital gonococcal infections, and probably also against rectal and pharyngeal infections."( Ciprofloxacin in the treatment of gonorrhoea and non-gonococcal urethritis.
Oriel, JD, 1986
)
0.27
" We concluded that rosoxacin at a dosage of 300 mg administered orally was fairly effective in the treatment of gonococcal urethritis in men caused by both PPNG and non-PPNG strains."( Rosoxacin in the treatment of uncomplicated gonorrhoea in men.
Ariyarit, C; Chitwarakorn, A; Panikabutra, K; Saensanoh, C, 1984
)
0.27
" In the retinas of controls, dosage with ICI 105552 reduced the concentration of sorbitol by 36% without other effects."( The effects of an aldose reductase inhibitor upon the sorbitol pathway, fructose-1-phosphate and lactate in the retina and nerve of streptozotocin-diabetic rats.
Earl, DC; Heath, H; Mirrlees, DJ; Poulsom, R, 1983
)
0.27
"To test the possible involvement of the sorbitol pathway in the pathogenesis of retinopathy in long-term experimentally-diabetic rats, streptozotocin-diabetic and normal rats were dosed orally (50 mg/kg body weight daily) for up to 373 days with an aldose reductase inhibitor (ICI 105552) or a placebo."( The effects of long-term treatment of streptozotocin-diabetic rats with an aldose reductase inhibitor.
Boot-Handford, RP; Heath, H; Poulsom, R, 1983
)
0.27
" produced a rightward parallel shift of the dose-response curves for AVP in a dose-dependent manner."( OPC-21268 antagonizes arginine vasopressin-induced vasoconstrictor response in the spinally-anesthetized dog.
Chihara, T; Mori, T; Nakamura, S; Onogawa, T; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, T, 1995
)
0.29
" In each 24-hour dosage trial, enrofloxacin was administered SC as a single dose or in divided doses given every 3, 6, or 12 hours."( Pharmacokinetics of enrofloxacin in clinically normal dogs and mice and drug pharmacodynamics in neutropenic mice with Escherichia coli and staphylococcal infections.
McClure, JT; Meinen, JB; Rosin, E, 1995
)
0.29
" This study was designed to evaluate two dosage regimens of a new difluoroquinolone, lomefloxacin, for prevention of postoperative bacteriuria following VLAP."( Lomefloxacin prophylaxis in visual laser ablation of the prostate.
Costa, FJ, 1994
)
0.29
" Both dosage regimens were well tolerated."( Lomefloxacin prophylaxis in visual laser ablation of the prostate.
Costa, FJ, 1994
)
0.29
" There was no clinically significant difference between the two dosage regimens."( Lomefloxacin prophylaxis in visual laser ablation of the prostate.
Costa, FJ, 1994
)
0.29
" It seems, therefore, that the in vivo activity of LVFX is comparable to that produced by a twofold-greater dosage of OFLO."( In vitro and in vivo activities of levofloxacin against Mycobacterium tuberculosis.
Grosset, J; JI, B; Lounis, N; Truffot-Pernot, C, 1995
)
0.29
"62 mumol/L) and the theophylline dosage was increased to 300 mg tid."( Clinafloxacin-theophylline drug interaction.
Matuschka, PR; Vissing, RS, 1995
)
0.29
" In our patient, careful monitoring of theophylline concentrations and dosage adjustments resulted in the restoration of therapeutic serum concentrations."( Clinafloxacin-theophylline drug interaction.
Matuschka, PR; Vissing, RS, 1995
)
0.29
" Dosage adjustments may be warranted when this combination of medications is used."( Clinafloxacin-theophylline drug interaction.
Matuschka, PR; Vissing, RS, 1995
)
0.29
" Our results indicate that a once- or twice-daily dosage of grepafloxacin should be adequate to treat systemic infections caused by most bacterial pathogens."( Pharmacokinetics and tissue penetration of the new fluoroquinolone grepafloxacin.
Andrews, JM; Child, J; Wise, R, 1995
)
0.29
" Although there were no statistically significant differences between the two LFLX dosage groups for these parameters at either of the evaluation times, the rates for the 300-mg LFLX dose were slightly superior."( [Clinical efficacy of lomefloxacin (100 mg or 300 mg) single-dose therapy in female acute uncomplicated cystitis].
Aoki, M; Hirose, T; Kumamoto, Y; Miyake, M; Sakai, S; Shibuya, A; Shimamura, S; Takatsuka, K; Umehara, T; Yamazaki, K, 1995
)
0.29
" Enrofloxacin, a fluoroquinolone antimicrobial agent, was administered orally to all dogs during the third or fourth week after surgery, at a dosage of approximately 5 mg/kg of body weight, every 12 hours for 7 days."( Enrofloxacin concentrations in dogs with normal prostate and dogs with chronic bacterial prostatitis.
Barsanti, J; Budsberg, SC; Dorfman, M, 1995
)
0.29
" Duration of treatment with appropriate dosage should be at least 10 days."( [The therapy of urinary tract infections in sows].
Sobestiansky, J; Wendt, M, 1995
)
0.29
" Antitumor efficacy was little effected by treatment schedule, although multiple divided dosing was generally more effective than single dose treatment."( Biological characterization of a novel antitumor quinolone.
Alder, J; Burres, N; Chu, DT; Clement, JJ; Jarvis, K; Swiniarski, J, 1995
)
0.29
" In a dose-response study, treatment with LEV at 100, 200, and 400 mg/kg of body weight was started 1 day after infection and was given daily for 28 days."( Activity of levofloxacin in a murine model of tuberculosis.
Cynamon, MH; Klemens, SP; Rogge, MC; Sharpe, CA, 1994
)
0.29
"2%, respectively within 72 hours after dosing of 400 mg."( Pharmacokinetics and safety of NM441, a new quinolone, in healthy male volunteers.
Kosuge, K; Morino, A; Nakashima, M; Okuyama, Y; Ozaki, M; Takebe, Y; Uematsu, T, 1994
)
0.29
" Sparfloxacin was more effective than levofloxacin and ofloxacin in both dosing regimens."( In vitro and in vivo activities of sparfloxacin against Mycoplasma pneumoniae.
Irifune, K; Ishida, K; Kaku, M; Mizukane, R; Suyama, N; Takemura, H; Tanaka, H; Tomono, K; Usui, T; Yoshida, R, 1994
)
0.29
" Allergen inhalation challenge was performed four hours after dosing and FEV1 was measured for eight hours."( Effect of the 5-lipoxygenase inhibitor ZD2138 on allergen-induced early and late asthmatic responses.
Arm, JP; Bell, GS; Hawksworth, RJ; Lee, TH; MacMillan, R; Nasser, SM; Spruce, KE; Williams, AJ, 1994
)
0.29
" A single dose of aspirin was administered four hours after dosing and FEV1 was measured for six hours."( Effect of the 5-lipoxygenase inhibitor ZD2138 on aspirin-induced asthma.
Arm, JP; Bell, GS; Foster, S; Lee, TH; MacMillan, R; Nasser, SM; Spruce, KE; Williams, AJ, 1994
)
0.29
" One of five new quinolones was orally administered, before transurethral resection of the prostate, at the dosage of 200 mg three times daily for 3 consecutive days."( Accumulation of new quinolones in the blood of elderly patients.
Abe, Y; Hasuda, A; Morita, M; Nakagawa, H; Suzuki, K,
)
0.13
" These findings indicate that sub-inhibitory concentrations of rufloxacin, which may be present in vivo in the mucosae in the troughs of the dosage cycle, significantly inhibit the adhesive properties of bacteria involved in mucosal colonization."( Favourable effects of sub-MIC rufloxacin concentrations in decreasing the pathogen-host cell adhesion.
Braga, PC; Piatti, G,
)
0.13
" When mice were dosed orally with 800 mg of Q-35 (8-OCH3) per kg of body weight, the maximum dose given, and exposed to the UVA light, no inflammatory lesions were observed in their ears."( Reduced phototoxicity of a fluoroquinolone antibacterial agent with a methoxy group at the 8 position in mice irradiated with long-wavelength UV light.
Hasegawa, T; Kamide, R; Marutani, K; Matsubara, S; Matsumoto, M; Miyoshi, A; Nagamuta, M; Nagano, H; Otabe, Y; Tanaka, K, 1993
)
0.29
"In a double-blind, randomized, multicenter study, the efficacy and safety of two dosage schedules of rufloxacin once daily were compared with those of amoxicillin three times a day in the treatment of 192 outpatients with exacerbations of chronic bronchitis."( Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis.
Cesana, M; Focht, J; Klietmann, W; Rondel, RK, 1993
)
0.29
" There were no differences in the background factors of the patients between the 2 dosage groups."( [A clinical study on lomefloxacin to find appropriate dose levels in the treatment of respiratory tract infections].
Hasegawa, Y; Ichiyama, S; Ikeda, T; Nakanishi, K; Nishiwaki, K; Saka, H; Shimokata, K; Taniguchi, K; Totani, Y; Yamada, Y, 1993
)
0.29
" Early asthmatic response was analyzed using three indices: dose producing a 20% decrease in FEV1 (PD20), the slope of and area under the dose-response curve."( Protective effect of nedocromil sodium on the dual asthmatic response to bronchial antigen challenge.
Bessot, JC; Bigot, H; Hutt, N; Kopferschmitt-Kubler, MC; Pauli, G, 1993
)
0.29
"Nedocromil significantly relieved preexisting seasonal allergic rhinitis symptoms during peak pollen exposures within 2 hours of the first dose, and the therapeutic benefits were maintained on a dosing regimen of four times a day."( Nedocromil sodium is rapidly effective in the therapy of seasonal allergic rhinitis.
Casale, TB; Donnelly, A, 1993
)
0.29
" In patients with moderate renal failure, dosage adjustment of rufloxacin is not needed."( Pharmacokinetics of rufloxacin in patients with impaired renal function.
Imbimbo, BP; Mant, TG; Morrison, PJ; Perry, G; Sacks, S; Wise, R; Woodcook, J, 1993
)
0.29
" These results, together with pharmacokinetic and toxicological data in mice and man, suggest that sparfloxacin may have a higher therapeutic index than ofloxacin in leprosy, and that the tentative standard dosage of 200 mg sparfloxacin daily should be appropriate for a clinical trial."( Sparfloxacin is more bactericidal than ofloxacin against Mycobacterium leprae in mice.
Chan, GP; Franzblau, SG; Parrilla, ML, 1993
)
0.29
" On the first of 5 days, each subject had a history taken and physical examination, SO2 baseline test, laboratory testing, and a methacoline dose-response test."( Effects of nedocromil sodium on the bronchomotor response to sulfur dioxide in asthmatic patients.
Bigby, B; Boushey, H, 1993
)
0.29
" As compared with baseline control (regular dose of inhaled steroids), patients treated with nedocromil plus the 50 percent reduced dosage of inhaled corticosteroid consistently demonstrated comparable or better symptom control."( Nedocromil sodium is more effective than cromolyn sodium for the treatment of chronic reversible obstructive airway disease.
Chatterjee, SS; Dorow, PD; Lal, S; Venho, KK, 1993
)
0.29
" The dose-response relationship of indomethacin for inhibition of prostaglandin formation and rebamipide-induced protection correlated well and 5 mg/kg indomethacin completely prevented the protective effect of rebamipide."( Stimulation of prostaglandin biosynthesis mediates gastroprotective effect of rebamipide in rats.
Kleine, A; Kluge, S; Peskar, BM, 1993
)
0.29
" Dosage adjustments are required in patients with renal dysfunction."( Lomefloxacin clinical pharmacokinetics.
Belliveau, PP; Freeman, CD; Nicolau, DP; Nightingale, CH, 1993
)
0.29
"A review of the literature on quinolones reveals numerous clinically relevant points regarding indications, dosing considerations, and drug interactions."( Quinolones: a practical review of clinical uses, dosing considerations, and drug interactions.
Borcherding, SM; Corley, CR; Nicholas, RA; Self, T; Stevens, R, 1996
)
0.29
" In addition, dose-response curves were constructed for erythema as measured by a reflectance device."( The UVR wavelength dependence for lomefloxacin photosensitization of human skin.
Fakouhi, TD; Harrison, GI; Hawk, JL; Roniker, B; Swabb, EA; Young, AR, 1996
)
0.29
" No effects caused by the repeated dosing were seen in the plasma concentrations."( [A 4-week intravenous toxicity study of the active metabolite (NM394) of prulifloxacin (NM441) in rats followed by a 4-week recovery test].
Iketani, M; Ishida, S; Iwakura, K; Shindo, Y; Sumi, N; Tamura, K; Yamazaki, S, 1996
)
0.29
" At 500 mg/kg, vomiting was observed every day or intermittently throughout the dosing period and salivation was observed almost every day from day 6 to the end of the dosing onward."( [Single and 4-week oral toxicity studies of prulifloxacin (NM441) in aged dogs].
Akune, A; Asaoka, H; Chihaya, Y; Ihara, T; Nagata, R; Nakama, K; Shindo, Y; Sumi, N, 1996
)
0.29
" No effects caused by the repeated dosing were seen in the plasma concentrations."( [A 4-week oral toxicity study of prulifloxacin (NM441) in rats followed by a 4-week recovery test].
Fukuda, K; Iwakura, K; Nishimura, N; Shindo, Y; Sumi, N; Tamura, K; Yamazaki, S, 1996
)
0.29
" No effects caused by the repeated dosing were seen in the plasma concentrations."( [A 4-week oral toxicity study of prulifloxacin (NM441) in dogs followed by a 4-week recovery test].
Ide, M; Iwakura, K; Nagatani, M; Oda, S; Shindo, Y; Sumi, N; Tamura, K, 1996
)
0.29
" The mutated grlA genes responsible for quinolone resistance were dominant over the wild-type allele, irrespective of gene dosage in a transformation experiment with the grlA gene alone."( Alterations in the DNA topoisomerase IV grlA gene responsible for quinolone resistance in Staphylococcus aureus.
Fujimoto, K; Hattori, H; Inoue, M; Kojima, T; Nakamura, S; Oyamada, Y; Yamagishi, J, 1996
)
0.29
" Studies in patients show that the pharmacokinetics of sparfloxacin were not influenced by age but severe renal failure markedly impaired elimination of the parent drug (the T1/2 was approximately doubled in patients with renal failure), and glucuronide, requiring adjustment of the dosage regimen."( Pharmacokinetics of sparfloxacin in healthy volunteers and patients: a review.
Montay, G, 1996
)
0.29
" Pharmacokinetic values for enrofloxacin and its metabolite ciprofloxacin are given separately for serum and milk whey following three intravascular dosing routes."( Disposition of enrofloxacin (Baytril) into the udder after intravenous and intra-arterial injections into dairy cows.
Fang, W; Jalakas, M; Klaassen, M; Malbe, M; Oöpik, T; Salonen, M; Sandholm, M, 1996
)
0.29
" Monkeys (n = 6 each group) were dosed with vehicle, 3 or 10 mg/kg ZD2138, or 30 mg/kg Zileuton (p."( The effect of 5-lipoxygenase inhibition on Ascaris antigen (Ag)-induced responses in atopic monkeys.
Andresen, CJ; Eggler, JF; Smith, WB; Turner, CR; Watson, JW, 1996
)
0.29
" Due to automated intermittent dosing and on-line LC analysis, the system operates unattended."( Automated analytical systems for drug development studies. Part IV. A microdialysis system to study the partitioning of lomefloxacin across an erythrocyte membrane in vitro.
Chang, MF; Knaub, SR; Lunte, CE; Riley, CM; Topp, EM, 1995
)
0.29
" In addition, dosing at 800 mg/kg induced decrease in body weight gain and increased levels of serum alkaline phosphatase (ALP), cholinesterase, leucine aminopeptidase and total cholesterol."( One-month oral toxicity study of the new quinolone antibacterial agent (S)-10-[(S)-(8-amino-6-azaspiro[3,4]octan-6-yl)-9-fluoro-2,3-dihydro-3- methyl-7-oxo-7H-pyrido [1,2,3-de] [1,4] benzoxazine-6-carboxylic acid hemihydrate in rats and cynomolgus monkeys
Kato, M; Miyamoto, M; Nomura, M; Shimoda, K; Sugawara, T; Takada, S; Yoshida, M, 1996
)
0.29
" This finding may be due to the somewhat lower initial degree of corneal inflammation in this group and suggests that the course of corneal recovery is predominately dependent on the initial degree of infection with both dosage regimens of lomefloxacin capable of eradicating corneal organisms."( Bacterial keratitis therapy in guinea pigs with lomefloxacin by initially high-followed by low-dosage regimen.
Abalain, ML; Colin, J; Jauch, A; Malet, F, 1995
)
0.29
"Multifactor analysis of the lomefloxacin effect on the primary immune response to T-independent bacterial antigen (vaccine EV fraction 1) and to T-dependent cellular antigen (SRBC) in mice was performed with the use of a wide range of the antibiotic concentrations and the dosage time."( [Effect of lomefloxacin on the synthesis of antibodies to vaccine EV fraction I and hemagglutinins].
Iordanova, AI; Navashin, PS; Nikitin, AV; Smolkina, TV, 1996
)
0.29
" bolus dosing were determined by reverse phase HPLC."( The disposition of five therapeutically important antimicrobial agents in llamas.
Christensen, JM; Hollingshead, N; Murdane, SB; Smith, BB, 1996
)
0.29
" Its long elimination half-life permits once-daily dosage regimens."( Sparfloxacin. A review of its antibacterial activity, pharmacokinetic properties, clinical efficacy and tolerability in lower respiratory tract infections.
Bryson, HM; Goa, KL; Markham, A, 1997
)
0.3
" Clinafloxacin at higher dosage (45 mg/kg/d) resulted in a decrease in myeloid progenitors in BM."( Enhanced hematopoiesis in sublethally irradiated mice treated with various quinolones.
Fabian, I; Gruss, T; Kletter, Y; Shalit, I; Weiss, K, 1997
)
0.3
"0 mg/kg dosing easily exceeds the in vitro minimum inhibitory concentration (MIC) for 20 bacterial organisms known to infect fish."( Pharmacokinetics of enrofloxacin in the red pacu (Colossoma brachypomum) after intramuscular, oral and bath administration.
Deen, J; Doi, A; Flammer, K; Lewbart, G; Manaugh, C; Smith, T; Vaden, S; Whitt, D, 1997
)
0.3
" Inaccurate estimations of ex vivo antibacterial activity of a suspected active metabolite (as with rufloxacin) when an adequate cutoff is not established may have dosing implications."( Suspicion of quinolone active metabolite following discrepancy between predicted and experimental urine bactericidal activities.
Aguilar, L; Costa, J; Dal-Ré, R; Giménez, MJ; Prieto, J, 1997
)
0.3
" After intravenous dosing of 10 mg/kg [14C]toborinone, fecal and urinary recoveries of the 14C dose were approximately 70% and 26-30%, respectively, in both rats and dogs."( Biotransformation of the novel inotropic agent toborinone (OPC-18790) in rats and dogs. Evidence for the formation of novel glutathione and two cysteine conjugates.
Kitani, M; Matsubara, J; Miyamoto, G; Nagasawa, M; Odomi, M; Uchida, M; Yamada, T, 1997
)
0.3
" In addition, a constant dosage of SPFX and SYN 1193, in combination with varying dosages of erythromycin, was tested under similar experimental conditions."( The effects of macrolide and quinolone antibiotics in methicillin-resistant Staphylococcus aureus biofilm growth.
Dasgupta, MK; Larabie, M; Micetich, RG; Salama, S; Shishido, H; Singh, R, 1997
)
0.3
" We conclude that the dosage of enrofloxacin should be adjusted according to age when administered to very young calves."( Pharmacokinetics of enrofloxacin in newborn and one-week-old calves.
Kaartinen, L; Moilanen, M; Pyörälä, S; Räisänen, S, 1997
)
0.3
" These features, together with the excellent bactericidal activity of grepafloxacin, support the recommended dosage regimen of grepafloxacin for the treatment of respiratory tract infections and sexually transmitted diseases."( Pharmacokinetics of grepafloxacin after oral administration of single and repeat doses in healthy young males.
Bramer, SL; Efthymiopoulos, C; Maroli, A, 1997
)
0.3
" The study group included 76 patients (43 male, 33 female) between 23 and 81 years of age, who were part of a multicentre, randomized, double-blind, dose-response study."( Pharmacokinetics and pharmacodynamics of oral grepafloxacin in patients with acute bacterial exacerbations of chronic bronchitis.
Amantea, MA; Chodosh, S; Collins, DA; Forrest, A; Schentag, JJ, 1997
)
0.3
" Intravenous injection of grepafloxacin caused transient dysrhythmias in rabbits at a dosage of 10 mg/kg and ventricular tachycardia at 30 mg/kg iv."( Safety profile of grepafloxacin compared with other fluoroquinolones.
Schwabe, R; Stahlmann, R, 1997
)
0.3
" Patient compliance is essential for successful therapy but diminishes with inconvenient dosing schedules and with poorly tolerated medicines."( What new antibiotics to offer in the outpatient setting.
Fraser, KL; Grossman, RF, 1998
)
0.3
" The same dosage regimen resulted in complete bacterial eradication in 88% of the kidneys."( Comparative therapeutic efficacy of clinafloxacin in a Pseudomonas aeruginosa mouse renal abscess model.
Desaty, TM; Griffin, TJ; Heifetz, CL; Sesnie, JC; Shapiro, MA, 1998
)
0.3
" Both fleroxacin and lomefloxacin were given orally, the dosage was 200 mg every 12 hours or 400 mg every 24 hours for 7-14 days."( [A clinical study in the treatment of acute bacterial infections with fleroxacin].
Cui, H; Hou, J; Li, J, 1996
)
0.29
" The activity of moxifloxacin could be described by a sigmoid dose-response curve with a maximum effect of -0."( Moxifloxacin in the therapy of experimental pneumococcal meningitis.
Brück, W; Chen, V; Dalhoff, A; Kohlsdorfer, C; Nau, R; Schmidt, H; Schneider, O; Stuertz, K; Trostdorf, F, 1998
)
0.3
" DCITC attenuated the maximal (-)-isoprenaline-mediated relaxation of a phenylephrine contracted aorta in a concentration-dependent manner and shifted the dose-response curves for (-)-isoprenaline to the right."( Irreversible binding of a carbostyril-based agonist and antagonist to the beta-adrenoceptor in DDT1 MF-2 cells and rat aorta.
Baker, SP; Dennis, DM; Deyrup, MD; Gelband, CH; Greco, PG; Otero, DH, 1998
)
0.6
"The objective of this randomized, double-blind, multicenter study of 329 adult patients requiring hospitalization was to compare the safety and efficacy of sparfloxacin at a dosage of 200 mg once daily (following a 400-mg loading dose on day 1) with those of amoxicillin given as a 1-g oral dose three times daily for treatment of community-acquired pneumonia suspected to be due to Streptococcus pneumoniae."( Once-daily sparfloxacin versus high-dosage amoxicillin in the treatment of community-acquired, suspected pneumococcal pneumonia in adults. Sparfloxacin European Study Group.
Aubier, M; Geslin, P; Regamey, C; Vercken, JB; Verster, R, 1998
)
0.3
" The impact of the dosing interval on the antimicrobial dose response was evaluated based on the survival of mice treated for 3 days with CPFX (25-200 mg/kg) or SPFX (6."( Pharmacodynamic activities of ciprofloxacin and sparfloxacin in a murine pneumococcal pneumonia model: relevance for drug efficacy.
Azoulay-Dupuis, E; Bédos, JP; Moine, P; Muffat-Joly, M; Pocidalo, JJ; Vallée, E; Veber, B, 1998
)
0.3
" It appears that although DU-6859a has a weak inhibitory effect on TP metabolism in vitro, its concomitant use with TP at clinical dosage levels does not cause any adverse effects, showing only a slight increase in blood TP concentrations and a decrease in urinary metabolites."( Effects of DU-6859a, a new quinolone antimicrobial, on theophylline metabolism in in vitro and in vivo studies.
Itokawa, K; Niki, Y; Okazaki, O, 1998
)
0.3
" Each cat underwent a bacteriological examination before treatment (day 0) and received either marbofloxacin, at a dosage of 2 mg/kg once daily for five days, or amoxycillin-clavulanic acid (ACA) at a dosage of 12."( Comparative field evaluation of marbofloxacin tablets in the treatment of feline upper respiratory infections.
Dossin, O; Gruet, P; Thomas, E, 1998
)
0.3
" tuberculosis, whereas both SPFX and MXFX were effective; administration six times weekly of either of the latter two drugs demonstrated dosage-dependent bactericidal effects, as measured by enumeration of CFU in the spleens, and MXFX appeared more bactericidal than the same dosage of SPFX."( In vitro and in vivo activities of moxifloxacin and clinafloxacin against Mycobacterium tuberculosis.
Bonnafous, P; Grosset, J; Ji, B; Lounis, N; Maslo, C; Truffot-Pernot, C, 1998
)
0.3
" Sixty patients received 40 mg of omeprazole twice a day, 1500 mg of amoxicillin three times a day, and 300 mg of rebamipide three times a day (group OAR); the other 60 patients received the same dosage of omeprazole and amoxicillin but no rebamipide for two weeks (group OA)."( Effect of rebamipide on Helicobacter pylori infection in patients with peptic ulcer.
Ando, K; Arakawa, T; Harihara, S; Higuchi, K; Ito, H; Kobayashi, K; Kuroki, T; Nebiki, H; Uchida, T, 1998
)
0.3
" Grepafloxacin's once-daily dosing regimen may offer advantages in terms of patient compliance."( Daily oral grepafloxacin vs. twice daily oral doxycycline in the treatment of Chlamydia trachomatis endocervical infection.
Hook, EW; Jones, RB; Martin, DH; McCormack, WM, 1998
)
0.3
" Its pharmacokinetics indicate that once-daily dosing may be possible."( Safety, tolerability and pharmacokinetics of the new long-acting quinolone DW-116 after single and multiple dosing in healthy subjects.
Choi, MS; Chung, YH; Dilger, C; Lee, CW; Lee, DK; Meyerhoff, C; Pabst, G; Reh, C; Ryu, JM; Yoon, SJ, 1998
)
0.3
" Multiple dosing and long-term treatment with sparfloxacin seems to induce a mutation in ParC and an alteration leading to reduced drug accumulation that contribute to increasing the fluoroquinolone resistance level."( Analysis of quinolone resistance mechanisms in a sparfloxacin-resistant clinical isolate of Neisseria gonorrhoeae.
Haraoka, M; Kobayashi, I; Nagafuji, T; Nakayama, H; Saika, T; Tanaka, M, 1998
)
0.3
"), treatment factors (daily dosage of LFLX, duration of treatment, total dose, concomitant drugs, and previous medication, etc."( Photosensitivity reactions caused by lomefloxacin hydrochloride: a multicenter survey.
Arata, J; Horio, T; Ohara, K; Soejima, R, 1998
)
0.3
"At mean dosage of 5 mg/kg once daily, enrofloxacin tissue concentrations were significantly greater in dogs with pyoderma at 3 hours after pill administration."( Determination of skin concentrations of enrofloxacin in dogs with pyoderma.
Brandt, CM; DeManuelle, TC; Ihrke, PJ; Kass, PH; Vulliet, PR, 1998
)
0.3
" In conclusion, renal impairment has no biologically relevant influence on marbofloxacin disposition and there is no need for dosage adjustment of marbofloxacin in dogs with mild renal impairment."( Effect of experimental renal impairment on disposition of marbofloxacin and its metabolites in the dog.
Costes, G; Delesalle, L; Dupouy, V; Laroute, V; Lefebvre, HP; Schneider, M; Toutain, PL, 1998
)
0.3
" Brain tissue sodium content was significantly reduced at the dosage of 300 mg/kg (P<0."( Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats.
Bemana, I; Nagao, S, 1999
)
0.3
" This study was undertaken to determine an optimal time for dosing antacids in relation to sparfloxacin administration to minimize antacid-induced reduction in sparfloxacin bioavailability."( Effect of Maalox on the oral absorption of sparfloxacin.
Caille, G; Dorr, MB; Johnson, RD; Talbot, GH,
)
0.13
" Groups of eight male Sprague-Dawley rats received either control material or grepafloxacin, enoxacin, lomefloxacin, ofloxacin or ciprofloxacin at an oral dosage of 300 mg/kg/day for 4 consecutive weeks."( A comparative study of the repeat dose toxicity of grepafloxacin and a number of other fluoroquinolones in rats.
Hasimoto, K; Itoh, N; Owen, K; Takizawa, T; Yamashita, S, 1999
)
0.3
"A stability indicating, reversed phase high-performance liquid chromatographic method utilizing a smallbore HPLC column has been developed for the determination of clonazepam in a commercial tablet dosage form."( Analysis of clonazepam in a tablet dosage form using smallbore HPLC.
Spell, JC; Stewart, JT, 1998
)
0.3
" Emesis induced by RS14203 exhibited a dose-response relationship but no such relationship was seen for R-rolipram or CT-2450."( Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret.
Choudhury, I; Robichaud, A; Rodger, IW; Tattersall, FD, 1999
)
0.3
" The concentration of theophylline in serum and the urinary excretion rates of theophylline on day 5 of concomitant dosing with HSR-903 tended to increase compared to those on day 4, when theophylline was given alone; however, the urinary excretion rates of 1-methyluric acid and 3-methylxanthine on day 5 of concomitant dosing with HSR-903 tended to decrease in comparison to those on day 4, when theophylline was given alone."( Effect of HSR-903, a new fluoroquinolone, on the concentration of theophylline in serum.
Matsuoka, O; Matsushima, T; Miyashita, N; Nakajima, M; Niki, Y; Sekino, H; Tamada, S; Watanabe, S; Yoshida, K, 1999
)
0.3
"Lomefloxacin eye drops used with a loading dosage followed by a twice daily regimen proved as effective, safe and well tolerated as five established standard treatments used at a 2, 4 or 5 times daily regimen, caused less discomfort upon instillation, and showed a lower risk to generate or select new resistant strains."( Meta-analysis of six clinical phase III studies comparing lomefloxacin 0.3% eye drops twice daily to five standard antibiotics in patients with acute bacterial conjunctivitis.
Fsadni, M; Gamba, G; Jauch, A, 1999
)
0.3
"Eight adult bottlenose dolphins Tursiops truncatus (six male, two female) were employed in a single-dose study of orally administered enrofloxacin dosed at 5 mg/kg body weight."( Enrofloxacin serum bioactivity in bottlenose dolphins, Tursiops truncatus, following oral administration of 5 mg/kg in whole fish.
Linnehan, RM; Ridgway, S; Ulrich, RW, 1999
)
0.3
"The disposition kinetics and dosage regimen of enrofloxacin were investigated in breeding buffalo bulls following a single intramuscular administration of 5 mg/kg."( Pharmacokinetics and dosage regimen of enrofloxacin in buffalo bulls after intramuscular administration.
Chaudhary, RK; Pangawkar, GR; Srivastava, AK; Verma, HK, 1999
)
0.3
" Studies of continuous dosing and studies of R115777 in combination with chemotherapy are ongoing."( Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer.
Belly, RT; Bol, CJ; Bowden, C; Chiao, J; Chow, C; Cowan, KH; End, DW; Gress, RE; Hakim, FT; Horak, ID; Kohler, DR; Kopp, WC; Kremer, AB; Larkin, G; Noone, M; Nussenblatt, RB; Piotrovsky, VK; Todd, A; Woestenborghs, R; Zujewski, J, 2000
)
0.31
" Combination tests of glycineB ligands demonstrated that injection of a fixed dose of ACPC (200 mg/kg) or L-701,324 (3 mg/kg) together with different doses of AMPH or COC practically did not modify dose-response curves of the psychostimulants, nor did it affect their ED50 values."( Lack of effects of glycineB receptor ligands on the psychostimulant-induced discriminative stimuli in rats.
Filip, M; Papp, M; Przegaliński, E, 2000
)
0.31
" Plasma enrofloxacin concentrations after intravenous dosing to healthy and infected birds were best described by a two-compartments model."( Tissue distribution and disposition kinetics of enrofloxacin in healthy and E. coli infected broilers.
Soliman, GA, 2000
)
0.31
" This article proposes that dosage schedules should be developed to provide a basis for the rational use of antimicrobial drugs."( Antibiotic treatment for animals: effect on bacterial population and dosage regimen optimisation.
AliAbadi, FS; Lees, P, 2000
)
0.31
"A highly sensitive spectrofluorimetric procedure is developed for the analysis of certain 4-quinolone antibiotics: sparfloxacin (I), oxolonic acid (II), flumequine (III) and enrofloxacin (IV) in their pharmaceutical dosage forms or in biological fluids."( Spectrofluorimetric analysis of certain 4-quinolone in pharmaceuticals and biological fluids.
Ahmed, S; Belal, F; el-Enany, N; Ibrahim, F; Rizk, M, 2000
)
0.31
" Cultures grown in sucrose-peptone broth were dosed with enrofloxacin."( Microbiological transformation of enrofloxacin by the fungus Mucor ramannianus.
Beger, RD; Freeman, JP; Lay, JO; Parshikov, IA; Sutherland, JB; Williams, AJ, 2000
)
0.31
" Results of the present study show that single dose oral rufloxacin may be used in routine clinical practice as a preoperative prophylactic antibiotic due to its low cost, its documented efficacy and its simple once daily dosage regimen."( Comparison of single preoperative oral rufloxacin versus perioperative ciprofloxacin as prophylactic agents in transurethral surgery.
Belgrano, E; Buttazzi, L; Ciampalini, S; Lissiani, A; Plaino, F; Raber, M; Savoca, G, 2000
)
0.31
" The stability of the DPC 961 and 963 in the dosing formulation was followed over a 24-h period using a stability indicating HPLC method."( In-use testing of extemporaneously prepared suspensions of second generation non-nucleoside reversed transcriptase inhibitors in support of phase I clinical studies.
Aubry, AF; Gray, V; Hobson, T; Rabel, S; Sebastian, D; Xie, M; Xu, JQ, 2000
)
0.31
" JTE-907 dosed orally inhibited carrageenin-induced mouse paw edema dose dependently."( In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.
Inaba, T; Iwamura, H; Kaya, T; Suzuki, H; Ueda, Y, 2001
)
0.31
" The competitive antagonistic action was further confirmed by the finding that rebamipide caused a parallel shift to the right in the dose-response curve of O2 production induced by fMLP."( Rebamipide suppresses formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide production by inhibiting fMLP-receptor binding in human neutrophils.
Azuma, A; Imagawa, K; Ishiyama, H; Kikuchi, M; Nagano, C; Sekiguchi, K, 2001
)
0.31
" Marbofloxacin was safe and effective for the treatment of superficial and deep pyoderma in dogs at the dosage used in this study."( Evaluation of the clinical efficacy of marbofloxacin (Zeniquin) tablets for the treatment of canine pyoderma: an open clinical trial.
Abbey, L; Baker, B; Coyne, M; Hannigan, M; Joffe, D; Paradis, M; Pukay, B; Trettien, A; Waisglass, S; Wellington, J, 2001
)
0.31
" Parameters recorded included breed, age, sex, enrofloxacin dosage (daily dose and number of days administered), medical condition for which the antibiotic had been prescribed, ophthalmic signs, examination results, and the visual outcome."( Enrofloxacin-associated retinal degeneration in cats.
Andrew, SE; Biros, DJ; Brooks, DE; Cutler, TJ; Denis, HM; Gelatt, KN; Ketring, KL; van der Woerdt, A, 2001
)
0.31
" The daily and total dosage of enrofloxacin and number of days of administration were also highly variable."( Enrofloxacin-associated retinal degeneration in cats.
Andrew, SE; Biros, DJ; Brooks, DE; Cutler, TJ; Denis, HM; Gelatt, KN; Ketring, KL; van der Woerdt, A, 2001
)
0.31
" Practitioners should adhere closely to the manufacturer's current enrofloxacin dosage recommendation (5 mg/kg q 24 h), and continue clinical observations for this drug toxicity in cats."( Enrofloxacin-associated retinal degeneration in cats.
Andrew, SE; Biros, DJ; Brooks, DE; Cutler, TJ; Denis, HM; Gelatt, KN; Ketring, KL; van der Woerdt, A, 2001
)
0.31
" In contrast, fluoxetine and imipramine each required at least four days of repeated dosing to show this activity."( Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523.
Altar, CA; Kikuchi, T; Miwa, T; Nakai, M; Oshiro, Y; Tottori, K; Uwahodo, Y; Yamada, S, 2001
)
0.31
" This open, cross-sectional, multicenter study has evaluated the efficacy and safety of a once-daily dosage of 400 mg lomefloxacin in patients with AECB chronically treated with theophylline."( Safety and effectiveness of lomefloxacin in patients with acute exacerbation of chronic bronchitis (AECB) chronically treated with oral theophyllines.
Cantoni, V; Melani, AS; Pirrelli, M; Sarlo, F, 2001
)
0.31
" In conclusion, a dosage of 10 mg/kg enrofloxacin is sufficient to exceed the minimal inhibitory concentrations in osteomyelitic bone against most pathogens that are sensitive in vitro, but clinical efficacy remains to be evaluated."( Concentration of enrofloxacin and its metabolite ciprofloxacin in canine matrices of the locomotor system.
Ehinger, AM; Kietzmann, M; Meyer-Lindenberg, A; Nolte, I; Vick, M, 2002
)
0.31
" Both dosage forms were administered once daily in doses of 300 or 400 mg."( Evaluation of the bioequivalence of tablets and capsules containing the novel anticancer agent R115777 (Zarnestra) in patients with advanced solid tumors.
Beijnen, JH; Bol, CJ; Crul, M; de Klerk, GJ; Palmer, PA; Schellens, JH; Swart, M; Weiner, L,
)
0.13
"Continuous dosing of R115777 is feasible with an acceptable toxicity profile at a dose of 300 mg bid."( Phase I clinical and pharmacologic study of chronic oral administration of the farnesyl protein transferase inhibitor R115777 in advanced cancer.
Beijnen, JH; Boerrigter, L; Bol, CJ; Crul, M; de Gast, GC; de Jong, D; de Klerk, GJ; Palmer, PA; Schellens, JH; Swart, M; Tan, H; van't Veer, LJ, 2002
)
0.31
" Eight subjects were assigned to each of five dose panels (100, 200, 400, 800 and 1200 mg BMS-284756) and received daily oral dosing with either BMS-284756 (n = 6) or placebo (n = 2) for 14 days."( Ecological impact of the des-F(6)-quinolone, BMS-284756, on the normal intestinal microflora.
Gajjar, DA; Grasela, DM; Nord, CE, 2002
)
0.31
" In this investigation the pharmacokinetics (PK) of marbofloxacin were determined after intravenous and intramuscular dosing at a dosage of 2 mg/kg."( Pharmacokinetics and pharmacokinetic/pharmacodynamic integration of marbofloxacin in calf serum, exudate and transudate.
Aliabadi, FS; Lees, P, 2002
)
0.31
" Its spectrum remains equivalent only if dosing schedules substantiate a proposed susceptible breakpoint of < or =4 mg/L."( Comparative antimicrobial spectrum and activity of the desfluoroquinolone BMS284756 (T-3811) tested against non-fermentative Gram-negative bacilli.
Biedenbach, DJ; Howard, W; Jones, RN, 2002
)
0.31
" Many of the fluoroquinolone agents have once-daily dosing regimens, enhancing patient adherence."( The expanding role of fluoroquinolones.
Schaeffer, AJ, 2002
)
0.31
" In addition, concurrent dosing of BPAA (1 microgram/body) did not reduce the convulsion-inducing dose of PZFX mesilate."( [Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration].
Fukuda, H; Kawamura, Y, 2002
)
0.31
" Owing to the high variations in MIC (minimal inhibitory concentration) of sensitive veterinary pathogens, it is recommended that enrofloxacin dosage regimens be calculated according to the sensitivity of the individual pathogen, site of infection and clinical response, than by following a preset dosage regimen."( Disposition kinetics of enrofloxacin (Baytril 5%) in sheep and goats following intravenous and intramuscular injection using a microbiological assay.
Elsheikh, HA; Khalafallah, AI; Osman, IA; Taha, AA, 2002
)
0.31
" Contaminated mice, maintained within 4 animal rooms, were administered Enrofloxacin in drinking water at a daily dosage of 25."( Elimination of Pasteurella pneumotropica from a contaminated mouse colony by oral administration of Enrofloxacin.
Itoh, T; Nozu, R; Shimizu, R; Sugiyama, F; Takahashi, S; Takakura, A; Ueno, Y; Yagami, K; Yamamoto, M, 2002
)
0.31
" Animals were killed on Days 2, 3, 4, 5 or 8 (the dosing day was designated as Day 1), and the incidence of micronucleus in the epidermis was determined."( In vivo photochemical micronucleus induction due to certain quinolone antimicrobial agents in the skin of hairless mice.
Furuhama, K; Itoh, S; Katoh, M, 2002
)
0.31
" Endometrial tissue concentrations taken from the mares after dosing showed that enrofloxacin and ciprofloxacin both penetrate this tissue adequately after systemic administration and would attain concentrations high enough in the tissue fluids to treat infections of the endometrium caused by susceptible bacteria."( Pharmacokinetics and endometrial tissue concentrations of enrofloxacin and the metabolite ciprofloxacin after i.v. administration of enrofloxacin to mares.
Cole, JA; Papich, MG; Van Camp, SD; Whitacre, MD, 2002
)
0.31
" Dosing on renal impairment."( Fluoroquinolone-induced retinal degeneration in cats.
Hamilton, P; Wiebe, V, 2002
)
0.31
" Electrospray ionization-liquid chromatography/mass spectrometry analyses of urine from subjects dosed with DPC 963 also revealed the presence of other minor metabolites including glucuronide conjugate of 6-OH DPC 963 (M7)."( Metabolism of (S)-5,6-difluoro-4-cyclopropylethynyl-4-trifluoromethyl-3, 4-dihydro-2(1H)-quinazolinone, a non-nucleoside reverse transcriptase inhibitor, in human liver microsomes. Metabolic activation and enzyme kinetics.
Chen, H; Chen, W; Gan, LS; Mutlib, AE, 2003
)
0.32
" Sixteen hours after inoculation, therapy was given by intravenous administration of BMS at 20 mg/kg of body weight, followed 5 h later by administration at a dosage of 10 mg/kg (n = 9 animals) or MOX as two doses of 20 mg/kg every 5 h (n = 8 animals)."( Garenoxacin (BMS-284756) and moxifloxacin in experimental meningitis caused by vancomycin-tolerant pneumococci.
Barton, T; Bowlware, K; Hardy, RD; Iglehart, J; Katz, K; McCoig, CC; McCracken, GH; Michelow, IC; Rodriguez-Cerrato, V; Saavedra, J, 2003
)
0.32
" Descriptive statistics were determined for each dosage, and comparisons were made among dosage groups for selected pharmacokinetic parameters."( Plasma concentrations of enrofloxacin and its active metabolite ciprofloxacin in dogs following single oral administration of enrofloxacin at 7.5, 10, or 20 mg/kg.
Boeckh, A; Boothe, DM; Boothe, HW; Jones, S; Wilkie, S, 2002
)
0.31
"To investigate the efficacy, safety and tolerability of three dosing strategies for switching chronic, stable patients with schizophrenia from current oral antipsychotic monotherapy to once-daily oral aripiprazole monotherapy."( Switching patients to aripiprazole from other antipsychotic agents: a multicenter randomized study.
Ali, MW; Carson, WH; Casey, DE; Ingenito, GG; Jody, D; Liebeskind, A; Saha, AR, 2003
)
0.32
"Aripiprazole is a dopamine partial agonist and a serotonin-2A antagonist; it is dosed 10-30 mg/d, with no initial titration necessary."( Aripiprazole: a new atypical antipsychotic drug.
Bowles, TM; Levin, GM, 2003
)
0.32
" The corresponding values for the geometric mean area under the concentration-time curve over the dosing interval (AUC(tau)) for garenoxacin in plasma at the 100- and 1200-mg doses were within the ranges of 11."( Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects.
Bello, A; Christopher, L; Gajjar, DA; Ge, Z; Grasela, DM, 2003
)
0.32
" The first cohort (n = 41) received a continuous dosing [CD] regimen of R115777 400 or 300 mg bid."( Phase II study of the efficacy and tolerability of two dosing regimens of the farnesyl transferase inhibitor, R115777, in advanced breast cancer.
Dowsett, M; Ellis, P; Hickish, T; Houston, S; Howes, A; Johnston, SR; Kelland, L; Michiels, B; Palmer, P; Perez-Ruixo, JJ; Salter, J, 2003
)
0.32
" Dosing regimens and consequent drug exposures that amplify or suppress the emergence of resistant bacterial subpopulations were identified and prospectively validated."( Application of a mathematical model to prevent in vivo amplification of antibiotic-resistant bacterial populations during therapy.
Bachhawat, R; Bush, K; Deziel, MR; Drusano, GL; Dudley, MN; Freeman, C; Jumbe, N; Kahn, JB; Leary, R; Liu, W; Louie, A; Miller, MH; Tam, VH, 2003
)
0.32
" The 26% reduction in theophylline clearance is probably not clinically significant in healthy dogs, but for dogs with renal impairment, there might be a chance of theophylline accumulation when dosed concomitantly with marbofloxacin."( The effect of orally administered marbofloxacin on the pharmacokinetics of theophylline.
Dederichs, D; Hirt, RA; Teinfalt, M; van den Hoven, R, 2003
)
0.32
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and dosage and administration of aripiprazole are discussed."( Aripiprazole.
Winans, E, 2003
)
0.32
" This compound also displayed in vivo efficacy in an anesthetized canine model of erection when dosed intravenously."( Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
Bhattacharjee, S; Clancy, J; Craig, E; Fiordeliso, JJ; Haynes-Johnson, D; Jiang, W; John, TM; Kraft, P; Lanter, JC; Macielag, MJ; Qiu, Y; Sui, Z, 2004
)
0.32
"At the conclusion of this learning activity, participants should be familiar with the modes of action, clinical indications, dosage regimens, and contraindications and cautions for several novel antibacterial agents for skin and skin structure infections."( Novel antibacterial agents for skin and skin structure infections.
Schweiger, ES; Weinberg, JM, 2004
)
0.32
" Patients were treated with escalating doses of irinotecan with interval-modulated dosing of R115777 (continuously or on days 1-14, and repeated every 21 days)."( Phase I and pharmacokinetic study of irinotecan in combination with R115777, a farnesyl protein transferase inhibitor.
de Bruijn, P; de Heus, G; de Jonge, MJ; Eskens, FA; Kehrer, DF; Klaren, A; Mathijssen, RH; Palmer, PA; Planting, AS; Sparreboom, A; Verhaeghe, T; Verheij, C; Verweij, J; Xie, R; Zhang, S, 2004
)
0.32
" Although a recent dose-finding study in 22 pediatric patients (> or = 6 yrs old) described weight-based dosages that were safe and well tolerated, dosing of aripiprazole in children has not been well established."( Excessive somnolence from aripiprazole in a child.
Buck, ML; Davenport, JD; McCarthy, MW, 2004
)
0.32
"33 mM in the ST cross only and without a clear dose-response effect."( Genotoxicity of tamoxifen citrate and 4-nitroquinoline-1-oxide in the wing spot test of Drosophila melanogaster.
Castañeda-Partida, L; Contreras-Sousa, M; Dueñas-García, I; Durán-Díaz, A; Graf, U; Heres-Pulido, ME; Sánchez-García, A, 2004
)
0.32
" To produce incurred enrofloxacin (ENRO) tissues (where ENRO is incorporated into complex tissue matrices) for the method comparison, 40-d-old broilers (mixed sex) were orally dosed through drinking water for 3 d at the FDA-approved dose of ENRO (50 ppm)."( Comparison of a bioassay and a liquid chromatography-fluorescence-mass spectrometry(n) method for the detection of incurred enrofloxacin residues in chicken tissues.
Donoghue, DJ; Schneider, MJ, 2004
)
0.32
"Dogs with superficial or deep pyoderma (n = 228) presented to first opinion veterinarians (n = 20) were treated orally with either ibafloxacin, at a dosage of 15 mg/kg, or marbofloxacin, at a dosage of 2 mg/kg, once daily for 3-16 weeks."( Treatment of canine pyoderma with ibafloxacin and marbofloxacin--fluoroquinolones with different pharmacokinetic profiles.
Horspool, LJ; Mawhinney, I; van den Bos, R; van Laar, P, 2004
)
0.32
" Areas between the control growth and the time--kill curves (ABBC in single dose simulations and the sum of ABBCs determined after the first, second and third dosing in multiple dose simulations--ABBC(1+2+3)) were higher with ABT492 than levofloxacin."( ABT492 and levofloxacin: comparison of their pharmacodynamics and their abilities to prevent the selection of resistant Staphylococcus aureus in an in vitro dynamic model.
Arzamastsev, AP; Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2004
)
0.32
" It is suggested that these MPC values will be useful when considering dosing strategies."( Mutant prevention concentrations of ciprofloxacin and enrofloxacin for Salmonella enterica.
Cooles, SW; Piddock, LJ; Randall, LP; Woodward, MJ, 2004
)
0.32
" Dosage titration is not necessary and the drug is effective in the first few weeks of treatment."( Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder.
Perry, CM; Swainston Harrison, T, 2004
)
0.32
"5 h after oral dosing and no significant drug accumulation."( Phase II study of the farnesyl transferase inhibitor R115777 in patients with sensitive relapse small-cell lung cancer.
De Porre, PM; DeVore, RF; Heymach, JV; Jia, X; Johnson, BE; Johnson, DH; Khuri, FR; Richards, HM; Safran, H; Schlabach, LL; Yunus, F; Zhang, S, 2004
)
0.32
" This is one of the first studies to demonstrate a significant effect of a computerized intervention on dosing route within an antibiotic class."( Oral quinolones in hospitalized patients: an evaluation of a computerized decision support intervention.
Arbogast, PG; Bansal, P; Hargrove, F; Hulgan, T; Kernodle, DS; Miller, RA; Rosenbloom, ST; Talbert, DA, 2004
)
0.32
" Among them, using antibiotic dosing regimens that may be less likely to promote resistance is one measure which could be beneficial, and this will be the focus of this review."( Optimization of antibiotic dosing schedules in the light of increasing antibiotic resistance.
Gould, IM; Smith, SV, 2004
)
0.32
" There is only limited information available on the use of aripiprazole in children and adolescents, and pilot data suggest that a revised dosing strategy, based on weight, is indicated in this population."( Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology.
Davies, MA; Roth, BL; Sheffler, DJ, 2004
)
0.32
" We conducted a National Cancer Institute-sponsored phase I trial to determine the feasibility of an intermittent dosing schedule of R115777 given orally twice daily on weeks 1 and 3 of a 28-day cycle in patients with malignant solid tumors."( Intermittent dosing of the farnesyl transferase inhibitor tipifarnib (R115777) in advanced malignant solid tumors: a phase I California Cancer Consortium Trial.
Doroshow, JH; Frankel, P; Gandara, DR; Gumerlock, PH; Kawaguchi, T; Lara, PN; Lau, DH; Law, LY; Lenz, HJ; Twardowski, P; Wright, JJ, 2005
)
0.33
" Immunohistochemical analysis showed a reduction of phosphorylated PDGFRbeta and phosphorylated ERK in tumor cells after oral dosing with CHIR-258 compared with control tumors."( In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models.
Aukerman, SL; Garrett, E; Gelb, AB; Harris, A; Heise, C; Lee, SH; Lopes de Menezes, D; Nordahl, L; Samara, E; Vora, J; Ye, H, 2005
)
0.33
" Current anti-VEGF therapies in late-stage development, while efficacious, require dosing by frequent intravitreal injections that are inconvenient to patients."( Inhibition of retinal and choroidal neovascularization by a novel KDR kinase inhibitor.
Anderson, KD; Bonelli, F; Ciliberto, G; Holder, DJ; Kinose, F; Lamartina, S; Roscilli, G; Spence, SG; Thut, CJ; Toniatti, C; Vogt, TF, 2005
)
0.33
"A novel KDR kinase inhibitor was dosed by oral gavage for 12 days at 0, 10, 30, or 100 mg/kg in an adult male Brown Norway rat laser induced choroidal neovascularization (CNV) model."( Inhibition of retinal and choroidal neovascularization by a novel KDR kinase inhibitor.
Anderson, KD; Bonelli, F; Ciliberto, G; Holder, DJ; Kinose, F; Lamartina, S; Roscilli, G; Spence, SG; Thut, CJ; Toniatti, C; Vogt, TF, 2005
)
0.33
"Oral dosing of the described KDR kinase inhibitor effectively inhibits neovascularization in two well-established animal models of ocular neovascularization."( Inhibition of retinal and choroidal neovascularization by a novel KDR kinase inhibitor.
Anderson, KD; Bonelli, F; Ciliberto, G; Holder, DJ; Kinose, F; Lamartina, S; Roscilli, G; Spence, SG; Thut, CJ; Toniatti, C; Vogt, TF, 2005
)
0.33
" From the pharmacokinetic and eicosanoid inhibition data for TA, pharmacodynamic parameters after dosing with TA alone for serum TxB2 and exudate PGE2 expressing efficacy (Emax=69."( Pharmacokinetic and pharmacodynamic interactions of tolfenamic acid and marbofloxacin in goats.
Landoni, MF; Lees, P; Sidhu, PK, 2006
)
0.33
" The dosing of the drugs were scheduled for both treatment groups as follows: 1 drop of each solution was alternately instilled every 5 minutes for the first 30 minutes (as loading dose), then 1 drop with 5-minute interval between 2 bottles instilled hourly for day 1-3, tapering to every 2 hours on day 4-6, and every 4 hours on day 7-14."( Clinical evaluation of ophthalmic lomefloxacin 0.3% in comparison with fortified cefazolin and gentamicin ophthalmic solutions in the treatment of presumed bacterial keratitis.
Erjongmanee, S; Kasetsuwan, N; Pariyakanok, L; Phusitphoykai, N; Puangsricharern, V, 2004
)
0.32
" Serum marbofloxacin disposition was best described by bicompartmental and mono-compartmental open models with first-order elimination after IV and oral dosing respectively."( Pharmacokinetics of marbofloxacin after single intravenous and repeat oral administration to cats.
Albarellos, GA; Landoni, MF; Montoya, L, 2005
)
0.33
" acutatum, Botrytis cinerea, Fusarium oxysporum, and Phomopsis obscurans in a dose-response growth-inhibitory bioassay at 50."( Isolation and identification of antifungal and antialgal alkaloids from Haplophyllum sieversii.
Cantrell, CL; Dunbar, C; Kustova, TS; Mamonov, LK; Schrader, KK; Sitpaeva, GT; Wedge, DE, 2005
)
0.33
" The method was applied to the determination of LFX, SFX and GFX in dilute urine samples and dosage forms, and compared with the HPLC method."( Electrochemical adsorptive behavior of some fluoroquinolones at carbon paste electrode.
Abdel Ghani, NT; El Ries, MA; El-Shall, MA; Wassel, AA, 2005
)
0.33
" (3) Five double-blind placebo-controlled trials lasting 4 to 6 weeks showed that aripiprazole was a little more effective than placebo at daily doses of 10 mg to 30 mg, without a clear dose-response relationship."( Aripiprazole: new drug. Just another neuroleptic.
, 2005
)
0.33
" Steady-state concentrations are attained within 14 days of dosing for both active moieties."( Aripiprazole: an overview of a novel antipsychotic.
Folnegović-Smalc, V; Kozumplik, O; Mimica, N; Uzun, S, 2005
)
0.33
" Dosing could be reduced to 15 mg/day for tolerability and, subsequently, increased to 30 mg/day based on clinical response."( Aripiprazole in the treatment of acute manic or mixed episodes in patients with bipolar I disorder: a 3-week placebo-controlled study.
Abou-Gharbia, N; Carson, W; Impellizzeri, C; Iwamoto, T; Kaplita, S; Marcus, R; McQuade, R; Rollin, L; Sachs, G; Sanchez, R; Stock, E, 2006
)
0.33
" The MTD was also evaluated on a chronic continuous dosing schedule (n = 6)."( Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Arceci, RJ; Balis, FM; Blaney, SM; End, D; Fox, E; Gillespie, A; Jayaprakash, N; Palumbo, JS; Pitney, A; Salzer, WL; Whitcomb, P; Widemann, BC; Zannikos, P, 2006
)
0.33
" The 200 mg/m2/dose was also tolerable on the continuous dosing schedule."( Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Arceci, RJ; Balis, FM; Blaney, SM; End, D; Fox, E; Gillespie, A; Jayaprakash, N; Palumbo, JS; Pitney, A; Salzer, WL; Whitcomb, P; Widemann, BC; Zannikos, P, 2006
)
0.33
"Oral tipifarnib is well tolerated in children receiving the drug twice daily for 21 days and a continuous dosing schedule at 200 mg/m2/dose, which is equivalent to the MTD in adults."( Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Arceci, RJ; Balis, FM; Blaney, SM; End, D; Fox, E; Gillespie, A; Jayaprakash, N; Palumbo, JS; Pitney, A; Salzer, WL; Whitcomb, P; Widemann, BC; Zannikos, P, 2006
)
0.33
" In conclusion, the preclinical profile of indacaterol suggests that this compound has a superior duration of action compatible with once-daily dosing in human, together with a fast onset of action and an improved cardiovascular safety profile over marketed inhaled beta(2) adrenoceptor agonists."( In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action.
Battram, C; Charlton, SJ; Cuenoud, B; Dowling, MR; Fairhurst, RA; Farr, D; Fozard, JR; Leighton-Davies, JR; Lewis, CA; McEvoy, L; Trifilieff, A; Turner, RJ, 2006
)
0.33
" The SC medication was specifically selected for each patient by the clinician and dosed according to prescribing guidelines for that medication."( A prospective, multicenter, randomized, parallel-group, open-label study of aripiprazole in the management of patients with schizophrenia or schizoaffective disorder in general psychiatric practice: Broad Effectiveness Trial With Aripiprazole (BETA).
Crandall, DT; Iwamoto, T; Kostic, D; Marcus, RN; McQuade, RD; Nyilas, M; Pans, M; Riera, LC; Stock, EG; Tandon, R, 2006
)
0.33
" All molecules except the macrolides caused a net reduction in bacterial counts that was time and concentration/MIC ratio dependent (four molecules tested in detail [gentamicin, oxacillin, moxifloxacin, and oritavancin] showed typical sigmoidal dose-response curves at 24 h)."( Pharmacodynamic evaluation of the intracellular activities of antibiotics against Staphylococcus aureus in a model of THP-1 macrophages.
Barcia-Macay, M; Mingeot-Leclercq, MP; Seral, C; Tulkens, PM; Van Bambeke, F, 2006
)
0.33
" Subsequent trials demonstrated that pauses in therapy (with staccato dosing schedules) seem to increase tolerability without a clear decrease in efficacy."( Tipifarnib: farnesyl transferase inhibition at a crossroads.
Mesa, RA, 2006
)
0.33
" The proposed method was successfully applied to the analysis of the investigated drugs in pure and pharmaceutical dosage forms with good accuracy and precision; the percentages of label claim ranged from 97."( Generic nonextractive spectrophotometric method for determination of 4-quinolone antibiotics by formation of ion-pair complexes with beta-naphthol.
Askal, HF; Darwish, IA; Marzouq, MA; Refaat, IH,
)
0.13
"A phase II study was undertaken in patients with recurrent malignant glioma to determine the efficacy and safety of tipifarnib, a farnesyltransferase inhibitor, dosed at the respective maximum-tolerated dose (MTD) for patients receiving and not receiving enzyme-inducing antiepileptic drugs (EIAEDs)."( Phase II trial of tipifarnib in patients with recurrent malignant glioma either receiving or not receiving enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Abrey, L; Aldape, K; Chang, SM; Cloughesy, TF; DeAngelis, LM; Fink, KL; Gilbert, MR; Groves, MD; Junck, L; Kuhn, J; Lamborn, KR; Lieberman, F; Mehta, M; Prados, MD; Raizer, JJ; Robins, HI; Schiff, D; Wen, PY; Wright, J; Yung, WK, 2006
)
0.33
" GS-9137 or matching placebo was administered with food for 10 days at 5 dosage regimens (200, 400, or 800 mg BID, 800 mg QD, or 50 mg+100 mg ritonavir QD; 6 active, 2 placebo per dose level)."( Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients.
Berger, D; Cheng, AK; Cohen, C; DeJesus, E; Elion, R; Farthing, C; Hawkins, T; Kearney, BP; Markowitz, M; McColl, D; Ruane, P; Zhong, L, 2006
)
0.33
" Each GS-9137 dosing regimen exhibited significant, exposure-dependent (mean reductions, -0."( Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients.
Berger, D; Cheng, AK; Cohen, C; DeJesus, E; Elion, R; Farthing, C; Hawkins, T; Kearney, BP; Markowitz, M; McColl, D; Ruane, P; Zhong, L, 2006
)
0.33
", 30- to 60-fold more potent than linomide) in these assays and its lack of a proinflammation in the Beagle-dog, ABR-215050 (tasquinimod), Figure 1, was characterized for dose-response ability to inhibit the growth of a series of four additional human and rodent prostate cancer models in mice."( Identification of ABR-215050 as lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer.
Björk, A; Dalrymple, SL; Garrison, JB; Isaacs, JT; Kyprianou, N; Leanderson, T; Olsson, A; Pili, R; Qian, DZ, 2006
)
0.33
" doses of tipifarnib, without a dose-response relationship."( A phase I safety, pharmacological and biological study of the farnesyl protein transferase inhibitor, tipifarnib and capecitabine in advanced solid tumors.
Cohen, RB; Eckhardt, SG; Gore, L; Gustafson, D; Holden, SN; Mikule, C; Morrow, M; O'Bryant, CL; Palmer, PA; Persky, M; Pierson, AS; Zhang, S, 2006
)
0.33
"The aim of this study was to verify an approach for calculating pharmacokinetic parameters suitable for adjusting dosage regimens in patients with renal dysfunction."( Dosage adjustment of quinolone antibiotics and angiotensin-converting enzyme inhibitors in patients with renal dysfunction.
Kinoshita, Y; Miki, A; Nagasaki, Y; Ohtani, H; Sata, H; Sawada, Y; Tsujimoto, M, 2006
)
0.33
" Also discussed are findings concerning the continuation of acute treatments, including antidepressants, into the maintenance phase; dosage adjustments for maintenance treatment; the rationale for combination treatments; and implications of comorbid substance abuse and strategies for its management."( Maintenance treatment of bipolar disorder: Applying research to clinical practice.
Chou, JC; Fazzio, L, 2006
)
0.33
" Further dosing was based on the individual day 5 pharmacokinetic data and absolute neutrophil count."( Clinical and pharmacologic study of the farnesyltransferase inhibitor tipifarnib in cancer patients with normal or mildly or moderately impaired hepatic function.
Beijnen, JH; Boot, H; Chang, I; Crul, M; De Porre, P; Schellens, JH; Siegel-Lakhai, WS; Zhang, S, 2006
)
0.33
"A 57-year-old man with a 30 year history of schizophrenia had been taking olanzapine for 4 years, with the dosage titrated to 20 mg/day, to control the psychosis."( Efficacy with high-dose aripiprazole after olanzapine-related metabolic disturbances.
Chavez, B; Poveda, RA, 2006
)
0.33
" Our recommendations for dosage and administration of aripiprazole are in agreement with the manufacturer's prescribing information."( Aripiprazole in the treatment of schizophrenia: a consensus report produced by schizophrenia experts in Italy.
Cassano, GB; Fagiolini, A; Lattanzi, L; Monteleone, P; Niolu, C; Sacchetti, E; Siracusano, A; Vita, A, 2007
)
0.34
" Steroids should be administered at a low dose and tapered off slowly, whereas antibiotics should be applied at a high dosage and discontinued abruptly."( [Therapy and prognosis of bacterial keratitis].
Behrens-Baumann, W; Pleyer, U, 2007
)
0.34
" Plasma concentrations attained with a dosage of 5 mg/kg every 24 hours would be expected to be efficacious for treatment of infections caused by susceptible bacteria (excluding Pseudomonas aeruginosa)."( Naïve averaged, naïve pooled, and population pharmacokinetics of orally administered marbofloxacin in juvenile harbor seals.
Huff, D; KuKanich, B; Papich, MG; Riviere, JE, 2007
)
0.34
"Twenty patients with the active distal type of UC in whom corticosteroid treatment had been unsuccessful were treated with rectal administration of Rebamipide twice a day for 3 weeks, during which corticosteroid dosage was kept constant."( Rebamipide enema therapy as a treatment for patients with active distal ulcerative colitis.
Ando, T; Furuta, R; Goto, H; Ina, K; Ishiguro, K; Kusugami, K; Maeda, O; Watanabe, O, 2007
)
0.34
" After 15 sessions, the dose-response function of methamphetamine was determined under either a progressive- or a fixed-ratio schedule."( Effect of aripiprazole, a partial dopamine D2 receptor agonist, on increased rate of methamphetamine self-administration in rats with prolonged session duration.
Koob, GF; Pulvirenti, L; Wang, Z; Wee, S; Woolverton, WL, 2007
)
0.34
"Quinolones, an expanding class of clinically established potent antibiotics, is not freely soluble in water which prevents the design of liquid dosage forms and restricts their use in topical applications."( Polyamidoamine (PAMAM) dendrimers as biocompatible carriers of quinolone antimicrobials: an in vitro study.
Cheng, Y; Fang, Y; Ma, M; Qu, H; Xu, P; Xu, T; Xu, Z, 2007
)
0.34
" However, an exposure-guided approach to dosage adjustment to limit haematological and nonhaematological toxicity is not warranted."( Exposure-toxicity relationships for tipifarnib in cancer patients.
Chen, W; Chow, A; Hayes, S; Perez-Ruixo, JJ; Zhang, S, 2007
)
0.34
" Lack of PK alteration for FTC, tenofovir (TFV), and GS-9137 was defined as a 90% confidence interval (CI) for the estimated ratio of geometric least squares means (coadministration/alone) between 70% and 143% for the primary PK parameters: maximum observed plasma concentration (Cmax), area under the plasma concentration-time curve over dosing interval (AUCtau), and trough concentration (Ctau)."( Pharmacokinetics of emtricitabine, tenofovir, and GS-9137 following coadministration of emtricitabine/tenofovir disoproxil fumarate and ritonavir-boosted GS-9137.
Cheng, A; Kearney, BP; Ramanathan, S; Shen, G, 2007
)
0.34
" The dosage was increased to 10 mg daily two weeks later."( Potential aripiprazole-mediated extrapyramidal symptoms in an adult with developmental disabilities.
Brahm, NC; Brown, RC; McElwain, DL, 2007
)
0.34
"0 mg/kg body weight dosage to five healthy Egyptian buffalo steers."( Single-dose pharmacokinetics of marbofloxacin in Egyptian buffalo (Bubalus bubalis L.) steers.
Abd El-Aty, AM; Goudah, A; Regmi, NL; Shim, JH; Shimoda, M; Shin, HC,
)
0.13
"Twenty-four outpatients aged 7 to 18 years with DSM-IV-diagnosed tic disorders were treated with aripiprazole using an open-label, flexible dosing schedule for 8 weeks from January 2005 to August 2006."( An open-label study of the efficacy and tolerability of aripiprazole for children and adolescents with tic disorders.
Choi, SH; Hong, JP; Kim, CY; Park, S; Wang, HR; Yoo, HK, 2007
)
0.34
" For example, a low dosage of cefotaxime, a cephalosporin, increased an uropathogenic Escherichia coli strain's production of the phage PhiMFP by more than 7-fold."( Phage-Antibiotic Synergy (PAS): beta-lactam and quinolone antibiotics stimulate virulent phage growth.
Comeau, AM; Krisch, HM; Prère, MF; Tétart, F; Trojet, SN, 2007
)
0.34
" Haloperidol dose was fixed; aripiprazole was dosed at 15 mg/day for the first 4 weeks, then 30 mg/day for the following 4 weeks."( Adjunctive treatment with a dopamine partial agonist, aripiprazole, for antipsychotic-induced hyperprolactinemia: a placebo-controlled trial.
Conley, RR; Jung, DU; Kelly, DL; Liu, KH; Seo, YS; Shim, JC; Shin, JG; Shon, JH, 2007
)
0.34
"Four quinolones were tested against the GrlA mutant, and a resistant population emerged after treatment with 250 mg pazufloxacin intravenous drip infusion, 600 mg ciprofloxacin intravenous drip infusion, 200 mg levofloxacin oral dosing and 150 mg tosufloxacin oral dosing."( Effect of GrlA mutation on the development of quinolone resistance in Staphylococcus aureus in an in vitro pharmacokinetic model.
Mitsuyama, J; Oonishi, Y; Yamaguchi, K, 2007
)
0.34
" The standard of care for treating schizophrenia is to first use monotherapy of adequate dosage and duration, including a trial of clozapine before adding a second agent."( Augmentation of aripiprazole with low-dose clozapine.
Berges, A; Dahmen, MM; Petry, WM; Stoner, SC, 2007
)
0.34
"Once-daily dosing with indacaterol provided sustained 24-h bronchodilation in patients with moderate-to-severe asthma, with a satisfactory overall safety profile."( Indacaterol provides sustained 24 h bronchodilation on once-daily dosing in asthma: a 7-day dose-ranging study.
Aisanov, Z; Alexander, M; Cameron, R; Deckelmann, R; Fabbri, LM; Higgins, M; LaForce, C; Owen, R, 2008
)
0.35
"5) enrolled in an open-label, single-site trial with fixed-flexible dosing of aripiprazole (5-30 mg/day) for 8 weeks."( Aripiprazole in the treatment of the psychosis prodrome: an open-label pilot study.
Callahan, JL; Cohen, SJ; Hawkins, KA; Mathalon, DH; McGlashan, TH; Miller, TJ; Tully, EM; Walsh, BC; Woods, SW, 2007
)
0.34
" Patients were randomized to placebo or aripiprazole (initiated at 10 mg/d, then flexibly dosed at 5-30 mg/d based on clinical effect and tolerability)."( Aripiprazole monotherapy in nonpsychotic bipolar I depression: results of 2 randomized, placebo-controlled studies.
Bowden, CL; Carson, WH; Jonas, A; Khan, A; Marcus, RN; McQuade, RD; Owen, R; Thase, ME; Wu, X, 2008
)
0.35
" Safety assessments were performed before and after dosing on days 1, 14, and 28, with particular attention to key beta2-agonist safety variables."( Tolerability of indacaterol, a novel once-daily beta2-agonist, in patients with asthma: a randomized, placebo-controlled, 28-day safety study.
Beier, J; Cameron, R; Higgins, M; Magula, D; Martinot, JB; Owen, R; Pohunek, P; Yang, WH, 2007
)
0.34
" There was no dose-response relationship between indacaterol and the incidence of AEs (400 microg, 40."( Tolerability of indacaterol, a novel once-daily beta2-agonist, in patients with asthma: a randomized, placebo-controlled, 28-day safety study.
Beier, J; Cameron, R; Higgins, M; Magula, D; Martinot, JB; Owen, R; Pohunek, P; Yang, WH, 2007
)
0.34
" There was no obvious dose-response relationship."( Phase I study of alternate-week administration of tipifarnib in patients with myelodysplastic syndrome.
Beran, M; Blascovich, MA; Bucher, C; Cortes, JE; Estey, EH; Giles, FJ; Kantarjian, HM; Kurzrock, R; Pilat, SR; Sebti, SM; Verstovsek, S; Wright, JJ, 2008
)
0.35
" Aripiprazole was dosed flexibly up to a maximum of 30 mg daily, based on tolerability and efficacy."( A prospective, open-label study of Aripiprazole mono- and adjunctive treatment in acute bipolar depression.
Chriki, LS; Dunn, RT; Filkowski, MM; Ghaemi, SN; Stan, VA, 2008
)
0.35
" Enemas containing 150 mg rebamipide per dosing were administered after morning bowel movement, and always prior to bedtime, twice daily for 4 weeks."( Rebampide enema therapy as a treatment for patients with chronic radiation proctitis: initial treatment or when other methods of conservative management have failed.
Cho, M; Heo, J; Kang, DH; Kim, GH; Kim, TO; Lee, SM; Song, GA, 2008
)
0.35
"Thirty-five patients were treated in four intermittent (25-100 mg/d) and three continuous (100-175 mg/d) dosing cohorts."( A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors.
Aziz, N; Braendle, E; Butzberger-Zimmerli, P; de Bono, JS; Evans, TR; Fox, JA; Garzon, F; Hardie, M; Heise, C; Jadayel, D; Judson, IR; Louie, S; Marriott, C; Michelson, G; Molife, R; Morrison, R; Sarker, D, 2008
)
0.35
" At a mean dosage of 20."( Combined antipsychotic treatment involving clozapine and aripiprazole.
Englisch, S; Zink, M, 2008
)
0.35
" We measured regional occupancy attained across a range of clinical dosing by the partial D(2) agonist aripiprazole using these methods."( Dose-occupancy study of striatal and extrastriatal dopamine D2 receptors by aripiprazole in schizophrenia with PET and [18F]fallypride.
Abi-Dargham, A; Alvarez, B; Bae, SA; Frankle, WG; Gil, R; Gonzales, R; Hackett, E; Kegeles, LS; Kim, JH; Laruelle, M; Slifstein, M; Xu, X, 2008
)
0.35
"A 12-week, open-label trial with flexible dosing strategy of aripiprazole was performed with 15 participants, aged 7-19 years."( Aripiprazole treatment of children and adolescents with Tourette disorder or chronic tic disorder.
Bai, DS; Sea, HS; Seo, WS; Sung, HM, 2008
)
0.35
"We performed a meta-analysis of randomized controlled trials (RCTs) comparing regimens of the same antibiotic (same dosage and same route of administration) administered for a different time period."( Short- versus long-duration antimicrobial treatment for exacerbations of chronic bronchitis: a meta-analysis.
Avgeri, SG; Dimopoulos, G; Falagas, ME; Matthaiou, DK; Siempos, II, 2008
)
0.35
" Despite its potential clinical benefits, the management of aripiprazole-treated patients can be challenging due to the lack of a simple dosing strategy and guidelines for preventing and managing potential adverse effects."( Proposed strategies for successful clinical management with aripiprazole.
Mago, R, 2008
)
0.35
"The dosing strategy recommendations are based on clinical experience and a PubMed database search conducted with no date restrictions for English-language literature."( Proposed strategies for successful clinical management with aripiprazole.
Mago, R, 2008
)
0.35
"4 mg/kg, aripiprazole decreased rates of cocaine self-administration without shifting the peak of the dose-response function."( Aripiprazole blocks acute self-administration of cocaine and is not self-administered in mice.
Brennum, LT; Fink-Jensen, A; Hee Bengtsen, C; Petersen, JH; Sager, TN; Sørensen, G; Thomsen, M; Thøgersen, P; Woldbye, DP; Wörtwein, G, 2008
)
0.35
" Future studies are warranted to examine alternative tipifarnib dosing and continuation beyond 16 cycles."( Phase II trial of tipifarnib as maintenance therapy in first complete remission in adults with acute myelogenous leukemia and poor-risk features.
Garrett-Mayer, E; Gojo, I; Gore, SD; Greer, J; Karp, JE; Klein, M; Lancet, JE; Levis, MJ; Morris, L; Smith, BD; Wright, JJ, 2008
)
0.35
" The interaction was observed after administration of DHQ and 3M-GBP combination at fixed dose ratios of 1:10 and 1:30 and the dose-response curves shifted approximately 13- and 17-fold leftward, respectively, from the theoretical additive values."( Synergy between a NR2B receptor antagonist DHQ and 3-methyl-gabapentin in mice with neuropathic pain.
Hizue, M; Imai, A; Toide, K, 2008
)
0.35
" The main objective of the two clinical pharmacology studies reported here was to evaluate the pharmacokinetics of aripiprazole after intramuscular dosing in healthy subjects and in patients with schizophrenia, and after intravenous and oral dosing in healthy subjects."( Pharmacokinetics and tolerability of intramuscular, oral and intravenous aripiprazole in healthy subjects and in patients with schizophrenia.
Boulton, DW; Kollia, G; Komoroski, B; Kovalick, LJ; Mallikaarjun, S; Reeves, RA; Sharma, A, 2008
)
0.35
" The results have confirmed that the D-optimal experimental design technique can be successfully employed for designing the long acting microsphere dosage form."( D-optimal designing and optimization of long acting microsphere-based injectable formulation of aripiprazole.
Nahata, T; Saini, TR, 2008
)
0.35
" Following baseline Meth dosing (15 mg and 30 mg), participants received 2 wk treatment with aripiprazole (n=8) or placebo (n=8)."( Evaluation of subjective effects of aripiprazole and methamphetamine in methamphetamine-dependent volunteers.
Abad, A; Anderson, A; Condos, R; De La Garza, R; Elkashef, A; Halkitis, PN; Li, SH; Mahoney, JJ; Mojisak, J; Newton, TF; Palamar, J; Reid, MS, 2008
)
0.35
" The methods developed were applied successfully to the determination of the subject drugs in their pharmaceutical dosage forms with good precision and accuracy compared to official and reported methods as revealed by t- and F-tests."( Study of fluorescence characteristics of the charge-transfer reaction of quinolone agents with bromanil.
Chen, XF; Li, WY; Xuan, CS, 2009
)
0.35
" The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms."( Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier.
Akira, Y; Duan, L; Huang, BB; Li, GF; Luo, JH; Nobuaki, K, 2008
)
0.35
"This study joins several others in demonstrating the utility of subacute dosing laboratory paradigms for evaluating medication effects in alcoholics."( Aripiprazole effects on alcohol consumption and subjective reports in a clinical laboratory paradigm--possible influence of self-control.
Anton, R; Myrick, H; Randall, P; Voronin, K, 2008
)
0.35
" This study systematically evaluated the ritonavir dose-response relationship on presystemic and systemic CYP3A metabolism using the human immunodeficiency virus integrase inhibitor elvitegravir and midazolam as probe substrates."( Dose-response of ritonavir on hepatic CYP3A activity and elvitegravir oral exposure.
Hui, J; Kearney, BP; Mathias, AA; West, S, 2009
)
0.35
" Adverse effects were evaluated using the Dosage Record and Treatment Emergent Symptom Scale (DOTES)."( Efficacy and tolerability of aripiprazole augmentation in sertraline-resistant patients with borderline personality disorder.
Bellino, S; Bogetto, F; Paradiso, E, 2008
)
0.35
" Clinical factors such as gender, age, illness duration, education level, diagnostic subtype, and medication dosage were also recorded."( Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients.
Chen, CH; Chen, SF; Chen, SJ; Chen, YJ; Lin, CC; Luu, SU; Shen, YC, 2009
)
0.35
" Serotonergic antidepressants, used both continuously and with increased dosage in the late luteal phase, are believed to be effective for major depressive disorder with premenstrual exacerbation."( Effective treatment of premenstrual violence in major depression: augmentation with aripiprazole.
Chiang, PH; Hsiao, MC; Liu, CY; Yao, YC,
)
0.13
" A high kinetic stability was observed for three metastable polymorphs which can be categorized as suitable candidates for the development of solid dosage forms."( Conformational polymorphism in aripiprazole: Preparation, stability and structure of five modifications.
Braun, DE; Gelbrich, T; Griesser, UJ; Kahlenberg, V; Tessadri, R; Wieser, J, 2009
)
0.35
" Some principles for dosing and switching are provided to assist with a successful treatment outcome with aripiprazole in mania."( A UK consensus on the administration of aripiprazole for the treatment of mania.
Aitchison, KJ; Bienroth, M; Cookson, J; Goodwin, GM; Gray, R; Haddad, PM; Moore, B; Ratna, L; Sullivan, G; Taylor, D; Taylor, M, 2009
)
0.35
" This 5-day, randomized, double-blind trial evaluated relative improvements in agitation in hospitalized patients who received orally dosed olanzapine (n = 306, 20 mg/d) or aripiprazole (n = 298, 15 mg/d, increasing to 30 mg/d as needed)."( Olanzapine versus aripiprazole for the treatment of agitation in acutely ill patients with schizophrenia.
Chen, L; Kinon, BJ; Kollack-Walker, S; Sniadecki, J; Stauffer, VL, 2008
)
0.35
" Tissue-selective activity was maintained when LGD-3303 was dosed orally or by continuous infusion, two routes of administration with markedly different time versus exposure profiles."( Pharmacokinetics and pharmacodynamics of LGD-3303 [9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator.
Chang, WY; Chen, Y; Hill, R; Lee, KJ; Lee, YH; López, FJ; Meglasson, MD; O'Brien, Z; Rix, P; Vajda, EG, 2009
)
0.35
" No dosage adjustment of lamotrigine is required and the combination was generally safe and well tolerated."( A non-randomized study to investigate the effects of the atypical antipsychotic aripiprazole on the steady-state pharmacokinetics of lamotrigine in patients with bipolar I disorder.
Balch, AH; Benson, J; Boulton, DW; Carlson, BX; Croop, R; Mallikaarjun, S; Schieber, FC, 2009
)
0.35
" Escitalopram and aripiprazole were flexibly dosed for 7 weeks, with maximum dosages of 20 and 30 mg/d, respectively."( An open study of aripiprazole and escitalopram for psychotic major depressive disorder.
Denninger, JW; Dording, C; Fava, M; Hilliker, S; Homberger, C; Matthews, JD; Park, L; Rooney, K; Siefert, C; Sklarsky, K; van Nieuwenhuizen, AO, 2009
)
0.35
" Group 1 (n = 20) followed a sequence of 10-day dosing of elvitegravir/r (150/100 mg once daily) and elvitegravir/r plus etravirine (200 mg twice daily) or the reverse (n = 10 per sequence)."( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine.
Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008
)
0.35
" Elvitegravir pharmacokinetic GMR was 6-7% higher following elvitegravir/r plus etravirine dosing versus elvitegravir/r."( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine.
Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008
)
0.35
" Consequently, the coadministration of elvitegravir with the protease inhibitor ritonavir (a substantial CYP3A4 inhibitor) results in significantly enhanced bioavailability and a longer half-life than with elvitegravir alone, allowing for the once-daily dosing of elvitegravir."( Elvitegravir, an oral HIV integrase inhibitor, for the potential treatment of HIV infection.
Klibanov, OM, 2009
)
0.35
" To evaluate the role of P-glycoprotein (P-gp) in aripiprazole tissue distribution and penetration across the blood-brain barrier, mice deficient in the P-gp gene (Abcb1a/b-/-) were dosed intraperitoneally with 2 microg/g mouse of the antipsychotic drug aripiprazole."( Aripiprazole brain concentration is altered in P-glycoprotein deficient mice.
Devane, CL; Donovan, JL; Geesey, ME; Markowitz, JS; Wang, JS; Yuan, HJ; Zhu, HJ, 2009
)
0.35
" Clinical factors such as gender, age, duration of illness, education level, diagnostic subtype and medication dosage were recorded."( Effects of the DRD3 Ser9Gly polymorphism on aripiprazole efficacy in schizophrenic patients as modified by clinical factors.
Chen, CH; Chen, SF; Shen, YC, 2009
)
0.35
"This analysis examined dosing patterns and safety of aripiprazole in elderly inpatients."( Aripiprazole prescribing patterns and side effects in elderly psychiatric inpatients.
Coley, KC; Fabian, TJ; Lenze, EJ; Ruby, C; Scipio, TM, 2009
)
0.35
"A total of 52 elderly inpatients treated with aripiprazole over 3 years were retrospectively identified to examine dosing patterns and side effects associated with use of aripiprazole."( Aripiprazole prescribing patterns and side effects in elderly psychiatric inpatients.
Coley, KC; Fabian, TJ; Lenze, EJ; Ruby, C; Scipio, TM, 2009
)
0.35
" Clinical factors such as gender, age, duration of illness, education level, diagnostic subtype, and medication dosage were noted as well."( HTR2A A-1438G/T102C polymorphisms predict negative symptoms performance upon aripiprazole treatment in schizophrenic patients.
Chen, CH; Chen, SF; Shen, YC, 2009
)
0.35
" In addition, the clinical factors, including dosage of aripiprazole, age, duration of illness, and diagnostic subtype, were found to influence PANSS performance after aripiprazole treatment."( HTR2A A-1438G/T102C polymorphisms predict negative symptoms performance upon aripiprazole treatment in schizophrenic patients.
Chen, CH; Chen, SF; Shen, YC, 2009
)
0.35
" In such situations, clinicians may want to consider prescribing a different antipsychotic or adding another antipsychotic and decreasing the dosage of clozapine."( Aripiprazole in treatment-refractory schizophrenia.
Chiu, NY; Hsu, WY; Kahn, DA; Lee, CI, 2009
)
0.35
" Dosing was determined by clinical judgment."( Efficacy and tolerability of aripiprazole in first-episode drug-naive patients with schizophrenia: an open-label trial.
Ishigooka, J; Oshimo, T; Takahashi, H,
)
0.13
" The mean dosage of aripiprazole was 17."( Efficacy and tolerability of aripiprazole in first-episode drug-naive patients with schizophrenia: an open-label trial.
Ishigooka, J; Oshimo, T; Takahashi, H,
)
0.13
" Phase II studies in relapsing MS demonstrate a dose-response effect on disease activity, measured by number of active lesions on brain magnetic resonance imaging, and show favorable tolerability and safety based on clinical and laboratory indicators."( Oral laquinimod therapy in relapsing multiple sclerosis.
Preiningerova, J, 2009
)
0.35
" The mean daily dosage of aripiprazole in completers was 11."( Aripiprazole augmentation of serotonin reuptake inhibitors in treatment-resistant obsessive-compulsive disorder: a 12-week open-label preliminary study.
Albert, U; Bogetto, F; Maina, G; Pessina, E, 2009
)
0.35
" The reasons for the change, course of illness, and types and dosage of antipsychotics previously used were collected."( Switching of antipsychotics to aripiprazole in the treatment of schizophrenia.
Chong, MY; Lee, Y; Lin, HC; Lin, PY; Yeh, WC,
)
0.13
" In this review we examined the efficacy data from short-term studies of aripiprazole in relapsed schizophrenia or schizoaffective disorder, in order to establish a dose-response relationship for aripiprazole."( Aripiprazole: dose-response relationship in schizophrenia and schizoaffective disorder.
Mace, S; Taylor, D, 2009
)
0.35
" The maximum plasma concentration and the area under the plasma concentration-time curve were dose proportional over the dosing range."( Multiple-dose safety, tolerability, and pharmacokinetics of oral nemonoxacin (TG-873870) in healthy volunteers.
Chang, LW; Chang, YT; Chen, SJ; Chiu, KM; Chung, DT; Hsu, CH; Hsu, MC; King, CH; Tan, HC; Tsai, CY, 2010
)
0.36
" Patients were randomly assigned (1:1) to flexibly dosed aripiprazole (target dosage: 5, 10, or 15 mg/day) or placebo."( Aripiprazole in the treatment of irritability in children and adolescents with autistic disorder.
Carson, WH; Corey-Lisle, P; Findling, RL; Manos, G; Marcus, RN; McQuade, RD; Owen, R; Sikich, L, 2009
)
0.35
" Vital signs (temperature, blood pressure, and heart rate) were measured before and after dosing in both periods."( Pharmacokinetics and bioequivalence of two formulations of rebamipide 100-mg tablets: a randomized, single-dose, two-period, two-sequence crossover study in healthy Korean male volunteers.
Cho, HY; Lee, YB; Park, GK; Yoon, H, 2009
)
0.35
" There was no relationship between elvitegravir dosage and adverse events."( Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV Type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial.
Berger, DS; Cheng, AK; Chuck, SL; Enejosa, JV; Kearney, BP; Lampiris, H; Zhong, L; Zolopa, AR, 2010
)
0.36
" Medication and dosing decisions were made by treating psychiatrists, constrained to once-a-day dosing, low initial doses and no clozapine."( Early intervention with second-generation antipsychotics in first-episode psychosis: results of an 8-week naturalistic study.
Audino, B; Curtis, J; Donohue, AM; Filymer, DM; Finkel, N; Josiassen, RC; Kacso, M; Shaughnessy, RA; Skuban, N, 2010
)
0.36
" Outpatients who met DSM-IV-TR criteria for schizophrenia, who were not optimally controlled while on stable dosage of clozapine for > or =3 months and had experienced weight gain of > or =2."( Effects of adjunctive treatment with aripiprazole on body weight and clinical efficacy in schizophrenia patients treated with clozapine: a randomized, double-blind, placebo-controlled trial.
Dewaele, P; Fleischhacker, WW; Heikkinen, ME; Hennicken, D; Kerselaers, W; Landsberg, W; Loze, JY; McQuade, RD; Olié, JP, 2010
)
0.36
" In previous studies, indacaterol provided 24 h bronchodilation on once-daily dosing with a fast onset of action."( Efficacy of a new once-daily long-acting inhaled beta2-agonist indacaterol versus twice-daily formoterol in COPD.
Bleasdale, P; Buhl, R; Chung, KF; Dahl, R; Higgins, M; Jack, D; Kramer, B; Magnussen, H; Nonikov, V; Owen, R, 2010
)
0.36
" Dopamine receptor occupancy appears to reach a plateau at doses above 10 mg, supporting the observation found in dose-response studies that 10 mg/d is the optimal dose for aripiprazole."( A systematic review of aripiprazole--dose, plasma concentration, receptor occupancy, and response: implications for therapeutic drug monitoring.
Kapur, S; Patel, MX; Sparshatt, A; Taylor, D, 2010
)
0.36
" Mean effective dosage was 14."( [Aripiprazole - a medical treatment alternative for Tourette Syndrome in childhood and adolescence].
Banaschewski, T; Frölich, J; Lehmkuhl, G; Starck, M, 2010
)
0.36
" Relative to ritonavir-boosted EVG, the geometric least-squares means ratios (GMR) [90% confidence interval (CI)] for EVG area under plasma concentration-time curve from time zero until the end of the dosing interval (AUC)tau, maximum concentration (Cmax), and trough concentration (Ctau) were 118 (110 to 126), 108 (100 to 116), and 110 (95."( Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV.
German, P; Hui, J; Kearney, BP; Warren, D; West, S, 2010
)
0.36
"This was an 8-week, open-label trial with flexible dosing strategy of aripiprazole in children and adolescents with TD."( Effectiveness and tolerability of aripiprazole in children and adolescents with Tourette's disorder: a pilot study in China.
Cui, YH; Li, J; Liu, J; Yang, YP; Zheng, Y, 2010
)
0.36
" The effect occurs even when a low dosage (3 mg/d) of aripiprazole was used and achieves a plateau at dosages beyond 6 mg/d."( Dose-dependent effects of adjunctive treatment with aripiprazole on hyperprolactinemia induced by risperidone in female patients with schizophrenia.
Fujii, A; Furukori, H; Kaneko, S; Sugawara, N; Yasui-Furukori, N, 2010
)
0.36
") dosing in patients with COPD."( Indacaterol once-daily is equally effective dosed in the evening or morning in COPD.
Henley, M; Higgins, M; Jack, D; Jadayel, D; Kramer, B; Magnussen, H; Verkindre, C; Woessner, R, 2010
)
0.36
"After diagnostic surgery or biopsy, treatment with tipifarnib started 5 to 9 days before initiating radiotherapy, twice daily, in 4-week cycles using discontinuous dosing (21 out of 28 days), until toxicity or progression."( A phase I trial of tipifarnib with radiation therapy, with and without temozolomide, for patients with newly diagnosed glioblastoma.
Abrey, L; Chang, SM; Cloughesy, TF; DeAngelis, LM; Demopoulos, A; Drappatz, J; Fine, HA; Fink, K; Kesari, S; Lamborn, KR; Lassman, AB; Lieberman, FS; Malkin, MG; Mehta, MP; Nghiemphu, PL; Prados, MD; Robins, HI; Torres-Trejo, A; Wen, PY, 2011
)
0.37
" However, excessive dosing of the antipsychotic medications, in particular haloperidol, may have played an important role in accounting for the differences between aripiprazole and haloperidol in this study."( Aripiprazole versus haloperidol treatment in early-stage schizophrenia.
Girgis, RR; Lieberman, JA; Merrill, DB; Pikalov, A; Vorel, SR; Whitehead, R; You, M, 2011
)
0.37
"Despite the growing epidemic of obesity in the United States, dosing medications in such patients remains poorly studied and understood."( Pharmacotherapy in the critically ill obese patient.
Medico, CJ; Walsh, P, 2010
)
0.36
"This was a post hoc analysis of data from two 8-week, randomized, double-blind, multicenter trials to evaluate the efficacy of aripiprazole dosed flexibly (2-15 mg/day, n=47) or fixed (5, 10, or 15 mg/day, n = 166) versus placebo (flexibly dosed, n = 51; fixed dose, n = 52)."( Line-item analysis of the Aberrant Behavior Checklist: results from two studies of aripiprazole in the treatment of irritability associated with autistic disorder.
Aman, MG; Kasper, W; Mankoski, R; Manos, G; Marcus, R; Mathew, S; Owen, R, 2010
)
0.36
" A month after the aripiprazole dosage was increased to 50 mg daily, the patient developed confusion and loss of coordination."( Increased aripiprazole concentrations in an HIV-positive male concurrently taking duloxetine, darunavir, and ritonavir.
Aung, GL; Kawamoto, LS; O'Brien, JG; Tien, PG, 2010
)
0.36
" Dosing regimens requiring less frequent dosing also provide improved treatment compliance."( An update on the use of indacaterol in patients with COPD.
Amor-Carro, O; Brienza, NS; Ramos-Barbón, D, 2011
)
0.37
" The mean final aripiprazole dosage was 12."( Aripiprazole augmentation in 39 adolescents with medication-resistant obsessive-compulsive disorder.
Berloffa, S; Masi, G; Millepiedi, S; Pfanner, C, 2010
)
0.36
" Phase II studies in RRMS demonstrate a dose-response effect on disease activity, measured by the number of active lesions on brain magnetic resonance imaging, and show favourable tolerability and safety based on clinical and laboratory indicators."( Oral laquinimod treatment in multiple sclerosis.
Fernández, O, 2011
)
0.37
" In addition, specific issues associated with the use of aripiprazole as an adjunctive therapy in patients with MDD, including possible early treatment effect, appropriate timing of therapy initiation, appropriate dosing and duration of treatment, possible differential effect on depressive subgroups and long-term tolerability, are also discussed."( Aripiprazole as adjunctive therapy for patients with major depressive disorder: overview and implications of clinical trial data.
Forbes, A; Pae, CU; Patkar, AA, 2011
)
0.37
" Choosing the appropriate dosing and tapering strategy, addressing the side effects, controlling withdrawal symptoms from previous medications and using adjunctive medications when necessary are key to successful treatment with aripiprazole."( Aripiprazole for the treatment of bipolar disorder: a review of current evidence.
Casamassima, F; Fagiolini, A; Forgione, RN; Marra, FS; Nitti, M, 2011
)
0.37
"Indacaterol is an inhaled, long-acting β(2)-agonist providing 24-h bronchodilation with once-daily dosing in patients with COPD."( Long-term safety and efficacy of indacaterol, a long-acting β₂-agonist, in subjects with COPD: a randomized, placebo-controlled study.
Chapman, KR; Dogra, A; Kramer, B; Lassen, C; Owen, R; Rennard, SI, 2011
)
0.37
" A smoked cocaine dose-response curve (0, 12, 25, 50 mg) was determined twice under placebo and aripiprazole maintenance."( Aripiprazole maintenance increases smoked cocaine self-administration in humans.
Foltin, RW; Haney, M; Rubin, E, 2011
)
0.37
" Decreases in estimated glomerular filtration rate occurred within the first few weeks of dosing in participants receiving EVG/COBI/FTC/TDF, remained within the normal range and did not progress at week 24 or 48; no participant experienced a clinical adverse event or discontinued study drug due to changes in serum creatinine or renal function."( Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection.
Chuck, SL; Cohen, C; DeJesus, E; Elion, R; Kearney, BP; Liu, HC; Ramanathan, S; Rashbaum, B; Ruane, P; Shamblaw, D; Warren, DR; Yale, K, 2011
)
0.37
"OCS were significantly more prevalent and severe in group I, in which OCS severity correlated with dosage of clozapine and duration of treatment."( Antiserotonergic antipsychotics are associated with obsessive-compulsive symptoms in schizophrenia.
Englisch, S; Esslinger, C; Meyer-Lindenberg, A; Rausch, F; Schirmbeck, F; Zink, M, 2011
)
0.37
" Indacaterol with 24 hours duration and fast onset of bronchodilation is the first once daily dosing LABA."( [New drugs in chronic obstructive pulmonary disease].
Chazan, RC, 2011
)
0.37
" One patient required a dosage reduction of ropinirole because of sleepiness and one patient assigned to aripiprazole who reported moderate akathysia had the dosage reduced to 5 mg/day."( Aripiprazole and ropinirole treatment for cocaine dependence: evidence from a pilot study.
Ameglio, M; Biasci, L; Cecconi, D; Cellesi, V; Forgione, RN; Meini, M; Moncini, M; Pellegrini, M; Rucci, P; Simoni, G, 2011
)
0.37
" A reduction of the histone gene dosage in the rad53 mutant restores Ixr1 levels."( Ixr1 is required for the expression of the ribonucleotide reductase Rnr1 and maintenance of dNTP pools.
Aström, SU; Barsoum, E; Chabes, A; Tsaponina, O, 2011
)
0.37
"Indacaterol is a novel, inhaled, ultra-long-acting β(2)-agonist providing 24-h bronchodilation with once-daily (od) dosing for maintenance use in patients with chronic obstructive pulmonary disease (COPD)."( Profiling the bronchodilator effects of the novel ultra-long-acting β2-agonist indacaterol against established treatments in chronic obstructive pulmonary disease.
Kramer, B; LaForce, C; Magnussen, H; Owen, R; Vogelmeier, C, 2011
)
0.37
"Patients with schizophrenia or schizoaffective disorder with a body mass index ≥ 27 and non-high-density lipoprotein (non-HDL) cholesterol ≥ 130 mg/dl who were on a stable treatment dosage of olanzapine, quetiapine, or risperidone were randomly assigned to switch to ari-piprazole (N=109) for 24 weeks or stay on their current medication (N=106)."( A randomized trial examining the effectiveness of switching from olanzapine, quetiapine, or risperidone to aripiprazole to reduce metabolic risk: comparison of antipsychotics for metabolic problems (CAMP).
Hamer, RH; LaVange, LM; Lieberman, JA; McEvoy, JP; Nussbaum, AM; Perkins, DO; Ring, KD; Rosenheck, RA; Stroup, TS; Swartz, MS, 2011
)
0.37
"A 52-week, open-label, flexibly dosed (2-15 mg/d) study of the safety and tolerability of aripiprazole in outpatients with a DSM-IV-TR diagnosis of autistic disorder who either had completed 1 of 2 antecedent, 8-week randomized trials or were enrolled de novo (ie, not treated in the randomized trials)."( Safety and tolerability of aripiprazole for irritability in pediatric patients with autistic disorder: a 52-week, open-label, multicenter study.
Carson, WH; Findling, RL; Kamen, L; Mankoski, R; Manos, G; Marcus, RN; McQuade, RD; Owen, R, 2011
)
0.37
" The recent therapeutic developments in COPD underscore a shift from short-acting bronchodilators with multiple dosings per day to reduced dosing frequency and prolonged duration of action, including once-daily treatment, with more consistent effects on various clinical outcomes."( Long-acting β-adrenoceptor agonists in the management of COPD: focus on indacaterol.
Beeh, KM; Beier, J, 2011
)
0.37
" There was no difference in baseline PANSS scores or the daily dosage used between responders (n = 28) and nonresponders (n = 17) (15."( Aripiprazole and dehydroaripiprazole plasma concentrations and clinical responses in patients with schizophrenia.
Chen, CK; Lin, SK; Liu, YL, 2011
)
0.37
"After taking into account the physiochemical properties of RBM (solubility, melting point, dosage etc."( Formulation of solid dispersion of rebamipide evaluated in a rat model for improved bioavailability and efficacy.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Tung, NT, 2011
)
0.37
" He was started on aripiprazole 15 mg po daily for 4 days; the dosage was then increased to 30 mg po daily, with Valproic Acid 500 mg po tid."( Pituitary microadenoma treated with antipsychotic drug aripiprazole.
Capote, E; Ezequiel, U; Paez, R; Wix-Ramos, RJ, 2011
)
0.37
" The patients were assigned to two groups: aripiprazole group (n=98) and tiapride group (n=97), with the treatment dosage of 5-25 mg/d and 100-500 mg/d, respectively."( [A multicenter controlled study on aripiprazole treatment for children with Tourette syndrome in China].
Chen, YH; Liao, JX; Liu, ZS; Sun, D; Wang, DB; Wang, H; Zhong, YQ; Zou, LP, 2011
)
0.37
" The mean dosage of aripiprazole required was 18."( An open trial of aripiprazole for the treatment of delirium in hospitalized cancer patients.
Boettger, S; Breitbart, W, 2011
)
0.37
"The mean maximum daily dosage of aripiprazole in the completers was 10."( A case series of aripiprazole augmentation of selective serotonin reuptake inhibitors in treatment-refractory obsessive compulsive disorder.
Hayashida, K; Kiriike, N; Maebayashi, K; Matsunaga, H; Mito, H, 2011
)
0.37
" The dose-response relationships of these derivatives were established in a primary cell model."( Novel structurally related compounds reactivate latent HIV-1 in a bcl-2-transduced primary CD4+ T cell model without inducing global T cell activation.
Bhat, S; Liu, JO; Lopez, JA; Margolick, JB; Shroff, NS; Siliciano, RF; Xing, S; Zhang, H, 2012
)
0.38
" SAR studies led to identification of piperazine 22 and pyrimidine 32, both of which reduced plasma nitrates following oral dosing in a mouse lipopolysaccharide challenge assay."( Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.
Bonnefous, C; Chen, X; Durón, SG; Hassig, CA; Lindstrom, A; Noble, SA; Rao, TS; Rix, P; Rozenkrants, N; Sablad, M; Shiau, AK; Smith, ND; Symons, KT; Wang, L; Yazdani, N; Zhang, H; Zhang, Y, 2012
)
0.38
"Positron emission tomography (PET) studies of dopamine receptor occupancy can be used to assess dosing of antipsychotics."( Predicting brain occupancy from plasma levels using PET: superiority of combining pharmacokinetics with pharmacodynamics while modeling the relationship.
Howes, OD; Jang, IJ; Jeong, JM; Kapur, S; Kim, BH; Kim, E; Kwon, JS; Lee, JS; Shin, SG; Turkheimer, FE, 2012
)
0.38
" We conducted a prospective, open-label nonrandomized, 4-week flexibly dosed (2."( The effectiveness and safety of adjunctive aripiprazole in Taiwanese patients with antidepressant-refractory major depressive disorder: a prospective, open-label trial.
Chen, SJ; Chen, ST; Hsiao, YL; Shen, TW, 2012
)
0.38
" Using a similar dosing selection pressure, the emergence of levofloxacin resistance was delayed in a strain with acrAB deleted compared to the isogenic parent."( Temporal interplay between efflux pumps and target mutations in development of antibiotic resistance in Escherichia coli.
Hu, M; Ledesma, KR; Singh, R; Swick, MC; Tam, VH; Yang, Z; Zechiedrich, L, 2012
)
0.38
" Once-daily dosing offers an advantage over raltegravir, but the requirement for pharmacologic boosting increases regimen complexity."( Elvitegravir: a once-daily inhibitor of HIV-1 integrase.
Vega, V; Wills, T, 2012
)
0.38
" It is likely that once-daily dosing of a bronchodilator would be a significant convenience and probably a compliance-enhancing advantage, leading to improved overall clinical outcomes in patients with COPD."( Comparative efficacy of indacaterol in chronic obstructive pulmonary disease.
Chapman, KR; Ribeiro, M, 2012
)
0.38
"We investigated the effects of the atypical antipsychotics risperidone, olanzapine, and aripiprazole on the cognitive functions of Japanese patients with schizophrenia with respect to dosage amounts and dosing schedules."( The cognitive profile of aripiprazole differs from that of other atypical antipsychotics in schizophrenia patients.
Hayashi, K; Hori, H; Ikenouchi-Sugita, A; Katsuki, A; Nakamura, J; Umene-Nakano, W; Yoshimura, R, 2012
)
0.38
", PTSD criteria participated in this 12-week, open-label, flexibly dosed monotherapy trial."( An open-label pilot study of aripiprazole for male and female veterans with chronic post-traumatic stress disorder who respond suboptimally to antidepressants.
Bradford, DW; Butterfield, MI; Hertzberg, MA; Kilts, JD; Marx, CE; Naylor, JC; Strauss, JL; Youssef, NA; Zinn, S, 2012
)
0.38
"4 weeks with a mean final aripiprazole dosage of 10."( A retrospective review of the effectiveness of aripiprazole in the treatment of sensory abnormalities in autism.
Bivas, R; Chahal, L; Fung, LK; Hardan, AY; Libove, RA, 2012
)
0.38
" In conclusion, our results suggest that abediterol has a preclinical profile for once-daily dosing in humans together with a fast onset of action and a favorable cardiovascular safety profile."( Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models.
Aparici, M; Beleta, J; Carcasona, C; Cortijo, J; De Alba, J; Gavaldà, A; Gómez-Angelats, M; Gras, J; Miralpeix, M; Morcillo, E; Otal, R; Puig, C; Ramos, I; Ryder, H; Vilella, D; Viñals, M, 2012
)
0.38
" The PK and safety profiles of nemonoxacin in Chinese subjects support evaluation of once-daily dosing in the future development of this agent."( Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses.
Cao, G; Guo, B; Shi, Y; Wu, X; Yu, J; Zhang, J; Zhang, Y, 2012
)
0.38
" Ataluren requires 3 times a day dosing and is currently in a Phase 3 placebo-controlled study."( Cystic fibrosis transmembrane conductance regulator-modifying medications: the future of cystic fibrosis treatment.
Pettit, RS,
)
0.13
" The development of resistance and the need for a once-daily dosing option has led to the development of new INSTIs, including elvitegravir and dolutegravir."( Update on raltegravir and the development of new integrase strand transfer inhibitors.
Bookstaver, PB; Rokas, KE; Shamroe, CL; Weissman, SB, 2012
)
0.38
" The plasma exposure profiles for each compound following a single oral dose in mice and estimated exposure parameters after repeated twice-daily dosing for 20 days are also presented."( Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.
Bahia, MT; Buckner, FS; Charman, SA; Chatelain, E; Chennamaneni, NK; Gelb, MH; Hulverson, MA; Laydbak, JU; Lepesheva, GI; Scandale, I; Shackleford, DM; Suryadevara, PK; Verlinde, CL; White, KL, 2012
)
0.38
" Once daily dosing of raltegravir is virologically inferior to raltegravir taken twice daily."( The use of HIV-1 integrase inhibitors in antiretroviral naive patients.
Lennox, JL, 2012
)
0.38
" These data better characterized integrase inhibitor pharmacokinetics, assessed dosing regimens, and investigated previously undescribed drug-drug interactions."( Pharmacology of HIV integrase inhibitors.
Adams, JL; Greener, BN; Kashuba, AD, 2012
)
0.38
" Pharmacokinetic data in special populations (pregnancy, pediatrics) to optimize dosing are still required."( Pharmacology of HIV integrase inhibitors.
Adams, JL; Greener, BN; Kashuba, AD, 2012
)
0.38
"The panel agreed that aripiprazole is effective in treating bipolar mania when prescribed and dosed appropriately, in both the short and long term, as monotherapy or in combination with a mood stabilizer."( A UK panel consensus on the initiation of aripiprazole for the treatment of bipolar mania.
Bobmanuel, S; Davies, W; Dratcu, L; Farmer, A; George, M; Rana, T; Singh, M; Turner, M, 2012
)
0.38
" Despite the lack of evidence, experts recommend an overlap strategy that includes maintaining the current antipsychotic dosage while titrating to a therapeutic dose of aripiprazole."( Strategies for transitioning therapy to aripiprazole from other antipsychotics in schizophrenia.
Robert, S; Wisniewski, CS,
)
0.13
"A randomized, double-masked, multicenter, placebo-controlled, parallel-group, dose-response phase II study."( Rebamipide (OPC-12759) in the treatment of dry eye: a randomized, double-masked, multicenter, placebo-controlled phase II study.
Awamura, S; Kinoshita, S; Nakamichi, N; Oshiden, K; Suzuki, H; Yokoi, N, 2012
)
0.38
"Patients were treated with aripiprazole monotherapy at a dosage of 10-30 mg/day."( Effect of aripiprazole on verbal memory and fluency in schizophrenic patients : results from the ESCAPE study.
Bervoets, C; Constant, E; de Patoul, A; Halkin, V; Kok, F; Morrens, M; Peuskens, J; Pitsi, D; Sabbe, B; Vansteelandt, K, 2012
)
0.38
" The dosage of pre-existing atypical antipsychotics was fixed, while the dosage of aripiprazole ranged from 5 to 20 mg/day during the study period."( Adjunctive effects of aripiprazole on metabolic profiles: comparison of patients treated with olanzapine to patients treated with other atypical antipsychotic drugs.
Chen, CK; Hsiao, CC; Huang, YS; Ree, SC; Wang, LJ, 2013
)
0.39
"All trials were industry supported, with some variability in dosage of haloperidol."( Lower rate of depressive switch following antimanic treatment with second-generation antipsychotics versus haloperidol.
Capapey, J; Colom, F; Goikolea, JM; Grande, I; Sanchez-Moreno, J; Torres, I; Undurraga, J; Valentí, M; Vieta, E, 2013
)
0.39
"The aim of this study was to investigate the dosing patterns of adjunctive quetiapine or adjunctive aripiprazole in the treatment of major depressive disorder from 2006 to 2010, and to evaluate the impact of Food and Drug Administration (FDA) approval on these dosing patterns."( Dosing patterns of aripiprazole and quetiapine for adjunctive treatment of major depressive disorder (2006-2010).
Forbes, RA; Guo, Z; Hebden, T; Jing, Y; Kalsekar, I; Thase, ME, 2013
)
0.39
" A clinical trial performed to support ivacaftor dose selection demonstrated a dose-response relationship between improvement in FEV(1) and decrease in sweat chloride, a measure of CFTR function."( Change in sweat chloride as a clinical end point in cystic fibrosis clinical trials: the ivacaftor experience.
Chowdhury, BA; Durmowicz, AG; Rosebraugh, CJ; Witzmann, KA, 2013
)
0.39
" A flexible dosing strategy based on clinical improvement and tolerability with a target dose 15 mg/d by the end of the fourth week."( Aripiprazole for drug-naive or antipsychotic-short-exposure subjects with ultra-high risk state and first-episode psychosis: an open-label study.
Chien, YL; Hsieh, MH; Hwang, TJ; Hwu, HG; Liu, CC; Liu, CM, 2013
)
0.39
" Rapid displacement in the caudate and putamen, but not in the cerebellum, was observed after injection of the dopamine D2/3 receptor nonselective ligand S(-)-eticlopride at a low dosage (0."( Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist.
Chu, W; Cui, J; Fan, J; Jones, LA; Li, S; Mach, RH; Perlmutter, JS; Tu, Z; Vangveravong, S; Wang, R; Xu, J, 2013
)
0.39
" They responded well to the reduction in dosage or to withdrawal of the apparent causing agent."( [Medication-related oculogyric crises: a description of four cases and a review of the literature].
Campistol, J; Darling, A; Perez-Duenas, B; Poo, P, 2013
)
0.39
" Initial phase 1 to 2 studies of dovitinib using a continuous daily dosing schedule has shown that dovitinib exhibits a prolonged and overproportional increase in dose and exposure relationship above 400 mg/d."( Population pharmacokinetic/pharmacodynamic modeling to assist dosing schedule selection for dovitinib.
Anak, O; Angevin, E; Dugan, M; Escudier, B; Feng, Y; Kay, A; Schran, H; Wang, X; Zhou, W, 2013
)
0.39
" However, it has the limitations of twice-daily dosing and a relatively modest genetic barrier to the development of resistance."( Next-generation integrase inhibitors : where to after raltegravir?
Karmon, SL; Markowitz, M, 2013
)
0.39
" No effects were observed on glucose, potassium, heart rate, blood pressure and no dose-response effect was seen on corrected QT elongation."( A new class of bronchodilator improves lung function in COPD: a trial with GSK961081.
Baggen, S; Chan, R; Locantore, N; Ludwig-Sengpiel, A; Riley, JH; Wielders, PL, 2013
)
0.39
" Assumed the importance of this topic and the lack of a clinical evaluation specifically designed to assess the impact of chronic administration of indacaterol on the response to salbutamol, we sought to compare the effect of 4-week treatment with indacaterol 150 μg once-daily versus formoterol 12 μg twice-daily on the dose-response curve to inhaled salbutamol (total cumulative dose of 800 μg) in a non-double-blinded, crossover, randomised, and controlled pilot trial that enrolled 20 outpatients with moderate to severe COPD."( Chronic treatment with indacaterol and airway response to salbutamol in stable COPD.
Cazzola, M; Matera, MG; Picciolo, S; Proietto, A; Rogliani, P; Ruggeri, P; Segreti, A, 2013
)
0.39
" After oral dosing, the dosed 14C was predominantly excreted into the feces of the test animals and the hepato-biliary route mainly contributed to the excretion of 14C in rats."( Disposition of the new potent acetylcholinesterase inhibitor 8-[3-[1-[(3-fluorophenyl)methyl]-4-piperidiny]-1-oxopropyl]-1, 2, 5, 6-tetrahydro-4H-pyrrolo [3, 2, 1-ij] quinolin-4-one (TAK-802) in rats, dogs and monkeys.
Asahi, S; Kakehi, M; Kondo, T; Tagawa, Y, 2013
)
0.39
" Bioavailability studies of the polymorphs of aripiprazole and their pharmaceutical preparations are very important to optimize the formulations of the dosage forms."( Aripiprazole.
Ardiana, F; Indrayanto, G; Lestari, ML, 2013
)
0.39
"EVG exposures were 40%-50% lower upon simultaneous dosing of EVG/r and antacids, probably due to local complexation with cations in gastrointestinal tract, and were unaffected with ≥2 hours staggered dosing."( Pharmacokinetics of once-daily boosted elvitegravir when administered in combination with acid-reducing agents.
Cheng, A; Kearney, BP; Koziara, J; Mathias, A; Ramanathan, S; Shen, G; Wei, X, 2013
)
0.39
" The performance of this screening is currently based on the dosage of trypsin immuno reactive, followed in case of exceeding the threshold of a search of the 30 most common mutations, can detect around 96% of 150 to 200 CF cases every year."( [News in cystic fibrosis].
Delaisi, B, 2013
)
0.39
" This was the first 12-week prospective, multicentre, open-label study of the effectiveness and tolerability of flexibly dosed aripiprazole as an augmentation to ongoing antidepressant treatment in patients with chronic or recurrent MDD."( Aripiprazole augmentation for treatment of patients with chronic or recurrent major depressive disorder: a 12-week prospective open-label multicentre study.
Cho, SJ; Choi, JH; Hahn, SW; Han, C; Jeon, HJ; Jon, DI; Jun, TY; Kim, SG; Kim, W; Kwak, KP; Lee, BC; Pae, CU; Park, EJ; Seo, HJ, 2013
)
0.39
" Available experimental evidences and published patents are indicative of broadening the circle of the applications in point of both technological advantages and dosage forms."( [Pharmaceutical applications of sulfobuthylether-beta-cyclodextrin].
Sebestyén, Z; Szabó, B; Szepesi, K, 2013
)
0.39
" Lowering the dosage of aripiprazole or changing the antipsychotic medication might be helpful in this situation."( Aripiprazole associated urine retention in a male schizophrenia patient.
Chang, TG; Chiu, NY; Hsu, WY,
)
0.13
"Indacaterol is safe and beneficial for patients with COPD at dosage ≤150 ug."( Indacaterol for chronic obstructive pulmonary disease: systematic review and meta-analysis.
Chung, VC; Hui, DS; Ma, PH; Tam, WW; Tang, JL, 2013
)
0.39
" As a fixed-dose combination tablet given once daily, EFV/FTC/TDF was the first available STR combining efficacy, tolerability and convenience, with the simplest dosing schedule and smallest numbers of pills of any ART combination therapy."( Single-tablet regimens in HIV: does it really make a difference?
Aldir, I; Horta, A; Serrado, M, 2014
)
0.4
"This was a 6-week prospective, multicenter, open-label study with flexibly dosed adjunctive aripiprazole."( Augmentation of aripiprazole for depressed patients with an inadequate response to antidepressant treatment: a 6-week prospective, open-label, multicenter study.
Bahk, WM; Jon, DI; Kim, DH; Kim, MD; Kwon, YJ; Min, KJ; Pae, CU; Seo, HJ; Suh, HS; Yang, JC,
)
0.13
" Compared to baseline values, the R-methadone mean area under the concentration-time curve to the end of the dosing period (AUCtau) (5,550 versus 6,210 h · ng/ml) and mean maximum concentration of drug in serum (Cmax) (316 versus 337 ng/ml) did not significantly increase in the presence of EVG/COBI."( Investigation of the interactions between methadone and elvitegravir-cobicistat in subjects receiving chronic methadone maintenance.
Bruce, RD; Custodio, JM; Friedland, GH; Kearney, BP; Ramanathan, S; Rhee, MS; Wei, X; Winkle, P, 2013
)
0.39
" Concerning adherence with drug treatment and real-life management in respect to long-acting β2-agonists, once-daily dosing makes indacaterol more convenient for COPD patients and is likely to enhance patient adherence."( Role of indacaterol and the newer very long-acting β2-agonists in patients with stable COPD: a review.
Incorvaia, C; Montagni, M; Olivieri, E; Riario-Sforza, GG; Ridolo, E, 2013
)
0.39
"This study investigated the dosing patterns for aripiprazole augmentation for major depressive disorder (MDD) in a naturalistic treatment setting."( Aripiprazole augmentation for major depressive disorder: dosing patterns in a naturalistic treatment setting.
Han, C; Lee, SJ; Masand, PS; Pae, CU; Patkar, AA; Wang, SM, 2014
)
0.4
" Further studies are necessary to evaluate both neuroprotective efficacy and optimal dosage of laquinimod in more detail."( Review of laquinimod and its therapeutic potential in multiple sclerosis.
Gold, R; Thöne, J, 2013
)
0.39
"A 65-year-old man developed severe hyponatremia after an aripiprazole dosage increase."( Syndrome of inappropriate antidiuretic hormone associated with aripiprazole.
Jackson, EA; Kwan, BK; Yam, FK, 2013
)
0.39
" Indacaterol is a novel, inhaled, long-acting β2-agonist, with rapid onset of action and once-daily dosing providing 24-hour bronchodilation."( New developments in the management of COPD: clinical utility of indacaterol 75 μg.
Archontogeorgis, K; Bouros, D; Nena, E; Steiropoulos, P, 2014
)
0.4
" Ancillary analyses indicated that tolerability was less favourable in younger (10-12 years) than in older (≥13 years) subjects, and less favourable with the higher (30 mg/day) than the lower dosage (10 mg/day)."( Aripiprazole: a review of its use in the treatment of manic episodes in adolescents with bipolar I disorder.
McKeage, K, 2014
)
0.4
", self-administration) sessions and 1 dose-response session, were conducted (once during the lead-in and twice after randomization)."( Aripiprazole effects on self-administration and pharmacodynamics of intravenous cocaine and cigarette smoking in humans.
Campbell, C; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2014
)
0.4
"Human colon cancer cells with different RAS-RAF mutation status (HCT-116, HT-29, SW-480, CaCO2 and LS174T) were treated with a combination of Dovitinib and Oxaliplatin at low dosage followed by assays to investigate the effect of the combination on cell proliferation, cell migration, cell apoptosis and signaling pathways involved in molecular mechanism of drug(s)."( Dovitinib synergizes with oxaliplatin in suppressing cell proliferation and inducing apoptosis in colorectal cancer cells regardless of RAS-RAF mutation status.
Ann, V; Chang, VH; Chen, L; Gaur, S; Hsu, NY; Lin, WC; Shia, HS; Wang, Y; Yen, Y, 2014
)
0.4
" In phase 1, single-blind aripiprazole was flexibly dosed (2-15 mg/d) for 13-26 weeks."( A randomized controlled trial investigating the safety and efficacy of aripiprazole in the long-term maintenance treatment of pediatric patients with irritability associated with autistic disorder.
Amatniek, J; Eudicone, JM; Findling, RL; Lears, K; Mankoski, R; Marcus, RN; McCartney, T; McQuade, RD; Sheehan, JJ; Timko, K, 2014
)
0.4
"To determine if oral dosing with the CFTR-potentiator ivacaftor (VX-770, Kalydeco) improves CFTR-dependent sweating in CF subjects carrying G551D or R117H-5T mutations, we optically measured sweat secretion from 32-143 individually identified glands in each of 8 CF subjects; 6 F508del/G551D, one G551D/R117H-5T, and one I507del/R117H-5T."( A little CFTR goes a long way: CFTR-dependent sweat secretion from G551D and R117H-5T cystic fibrosis subjects taking ivacaftor.
Char, JE; Cho, HJ; Davies, Z; Dunn, C; Frisbee, E; Jeong, JH; Milla, C; Moss, RB; Park, IH; Thomas, EA; Wine, JJ; Wolfe, MH, 2014
)
0.4
" All patients were titrated on iloperidone to 6mg BID by Day 4, then flexibly dosing between 6 and 12mg BID, as needed."( A trial evaluating gradual- or immediate-switch strategies from risperidone, olanzapine, or aripiprazole to iloperidone in patients with schizophrenia.
Alva, G; Brams, M; Citrome, L; Glick, ID; Hochfeld, M; Jackson, R; Kianifard, F; Mattingly, G; Meng, X; Pestreich, L; Weiden, PJ; Winseck, A, 2014
)
0.4
" The geometric mean ratio (90% confidence interval [CI]) for EVG area under the concentration-time curve over the dosing interval (AUCtau) and maximum observed plasma concentration (Cmax) were 135% (103%, 177%) and 141% (109%, 183%), respectively."( Pharmacokinetics and safety of boosted elvitegravir in subjects with hepatic impairment.
Custodio, JM; Kearney, BP; Ling, KH; Ramanathan, S; Rhee, M; Shen, G, 2014
)
0.4
" In the quinolone allergic population, ofloxacin elicited inhibition of the 4 positive QA-specific IgE sera tested, in a dose-response manner."( Immediate allergic hypersensitivity to quinolones associates with neuromuscular blocking agent sensitization.
Bérard, F; Bienvenu, F; Bienvenu, J; Diot, N; Dubost, R; Guilloux, L; Mullet, C; Nosbaum, A; Piriou, V; Rouzaire, P,
)
0.13
" When dual bronchodilation is indicated, QVA149 offers the convenience of two bronchodilators in a single inhaler coupled with a simple, once-daily dosing regimen that may encourage better treatment adherence."( QVA149 (indacaterol/glycopyrronium fixed-dose combination): a review of its use in patients with chronic obstructive pulmonary disease.
Frampton, JE, 2014
)
0.4
" A low dosage of phenobarbital caused a significant increase of the generalized seizure threshold in the L-701,324 pre-treated group, whereas it did not exert a comparable effect in animals that received vehicle during the massive kindling phase."( Pre-treatment with the NMDA receptor glycine-binding site antagonist L-701,324 improves pharmacosensitivity in a mouse kindling model.
Aronica, E; Gorter, J; Potschka, H; Salvamoser, JD; Soerensen, J; van Vliet, EA; Zellinger, C, 2014
)
0.4
" The grade of gastric mucosal injuries was evaluated by esophagogastroduodenoscopy before and after dosing (on day 0 and day 14), and the grade of gastric mucosal injury was assessed according to the modified Lanza score."( A randomized, double-blind, placebo-controlled study of rebamipide for gastric mucosal injury taking aspirin with or without clopidogrel.
Fukui, H; Hida, N; Hori, K; Miwa, H; Nakamura, S; Ogawa, T; Ohda, Y; Okugawa, T; Oshima, T; Tomita, T; Tozawa, K; Watari, J, 2014
)
0.4
" The proposed methods have been successfully applied to the analysis of REB in pharmaceutical dosage forms without interference from other dosage form excipients."( Stability-indicating determination of rebamipide in the presence of its acid degradation products.
Abbas, SS; El-Bardicy, MG; Essam, HA; Zaazaa, HE,
)
0.13
" Once-a-day dolutegravir dosing also does not require a pharmacokinetic booster like elvitegravir which minimizes the drug-drug interaction potential of dolutegravir."( Dolutegravir for the treatment of adult patients with HIV-1 infection.
Abraham, T; Saad, N; Wu, G, 2014
)
0.4
" As a stand-alone agent, elvitegravir will require twice-daily dosing to achieve effective viral reductions."( Elvitegravir for the treatment of HIV infection.
Reviriego, C, 2014
)
0.4
"Indacaterol is an inhaled, ultra-long-acting β2-agonist that provides 24-h bronchodilation with once-daily dosing in patients with chronic obstructive pulmonary disorder."( Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteers.
Emotte, C; Jiang, J; Khindri, S; Li, L; Li, R; Pei, H; Woessner, R; Yin, H, 2015
)
0.42
"Pill burden, dosing frequency, and concerns about safety and tolerability are important obstacles to maintaining adequate medication adherence."( Switching from twice-daily raltegravir plus tenofovir disoproxil fumarate/emtricitabine to once-daily elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate in virologically suppressed, HIV-1-infected subjects: 48 weeks data.
Brinson, C; Cao, H; Cheng, A; Crofoot, G; Ebrahimi, R; Garner, W; Kulkarni, R; Mills, A; Ortiz, R; Rashbaum, B; Szwarcberg, J; Towner, W; Ward, D,
)
0.13
" Analyses were performed assuming dosing of clinical trials, real-world practice, PIs, and highest therapeutic dose available, because of variation in practice settings."( Cost-effectiveness of aripiprazole once-monthly compared with paliperidone palmitate once-monthly injectable for the treatment of schizophrenia in the United States.
Baker, RA; Bentley, TG; Citrome, L; Eramo, A; Gutierrez, B; Hansen, K; Kamat, SA; Ortendahl, J; Sapin, C, 2014
)
0.4
" When PI dosing was assumed, this ICER increased to US$19,968/relapse averted."( Cost-effectiveness of aripiprazole once-monthly compared with paliperidone palmitate once-monthly injectable for the treatment of schizophrenia in the United States.
Baker, RA; Bentley, TG; Citrome, L; Eramo, A; Gutierrez, B; Hansen, K; Kamat, SA; Ortendahl, J; Sapin, C, 2014
)
0.4
" Under various dosing scenarios, AOM results indicated fewer relapses at lower overall costs or a reasonable cost-effectiveness threshold (i."( Cost-effectiveness of aripiprazole once-monthly compared with paliperidone palmitate once-monthly injectable for the treatment of schizophrenia in the United States.
Baker, RA; Bentley, TG; Citrome, L; Eramo, A; Gutierrez, B; Hansen, K; Kamat, SA; Ortendahl, J; Sapin, C, 2014
)
0.4
" Concerning the real-life management, in respect to LABA, the OD dosing makes indacaterol more convenient for COPD patients and is likely to positively influence the patient's adherence."( Indacaterol in the Treatment of Chronic Obstructive Pulmonary Disease: From Clinical Trials to Daily Practice.
Incorvaia, C; Montagni, M; Riario-Sforza, E; Riario-Sforza, GG; Ridolo, E, 2014
)
0.4
" The optimized RBM-SD was formulated in tablet dosage form, containing approximately 2 % sodium lauryl sulphate and poloxamer F68 as wetting agents."( Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability.
Choi, HG; Choi, IS; Choi, JY; Kim, JO; Pradhan, R; Tran, TH; Yong, CS, 2015
)
0.42
"Patients with HIV on antiretroviral therapy might benefit from regimen simplification to reduce pill burden and dosing frequency."( Simplification to coformulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus continuation of ritonavir-boosted protease inhibitor with emtricitabine and tenofovir in adults with virologically suppressed HIV (STRATEGY-PI): 48 week results o
Arribas, JR; Di Perri, G; Ebrahimi, R; Gathe, J; Nguyen, T; Pialoux, G; Piontkowsky, D; Reynes, J; Tebas, P; White, K, 2014
)
0.4
" Volunteers treated with 250 to 750 mg nemonoxacin exhibited a linear dose-response relationship between the AUC0-72 h and AUC0-∞."( Safety, tolerability, and pharmacokinetics of intravenous nemonoxacin in healthy chinese volunteers.
Cao, GY; Chen, YC; Guo, BN; Shi, YG; Wu, JF; Wu, XJ; Yu, JC; Zhang, J; Zhang, YY, 2014
)
0.4
" Combining these drugs to maximize rescue of ΔF508 CFTR may require changes in dosing and/or development of new potentiator compounds that do not interfere with CFTR stability."( Potentiator ivacaftor abrogates pharmacological correction of ΔF508 CFTR in cystic fibrosis.
Boucher, RC; Cholon, DM; Das, J; Dokholyan, NV; Esther, CR; Fulcher, ML; Gentzsch, M; Quinney, NL; Randell, SH, 2014
)
0.4
" This finding suggests the need to increase the dosage during pregnancy in order to maintain stable PLs."( A safety evaluation of aripiprazole for treating schizophrenia during pregnancy and puerperium.
Gentile, S, 2014
)
0.4
" His TD always improved immediately after the dosage was shifted to aripiprazole."( Suppression of antipsychotic-induced tardive dyskinesia with aripiprazole in an elderly patient with bipolar I disorder.
Chan, HY; Tan, HK; Wu, WY, 2014
)
0.4
" Indacaterol was developed using a combination of informed drug design and molecular chemistry to generate a β2-adrenergic agonist with a fast onset and long duration of action, enabling once-daily dosing with an acceptable safety profile."( Turning a molecule into a medicine: the development of indacaterol as a novel once-daily bronchodilator treatment for patients with COPD.
Beeh, KM; Dahl, R; Dederichs, J; Donohue, J; Fülle, HJ; Higgins, M; Molimard, M; Murphy, L; Rennard, S; Young, D, 2014
)
0.4
" Following optimization of the propranolol dosing regimen (study 1), we conducted a five-period crossover study (study 2) in which subjects received the following treatments: dry powder inhaler (DPI) GSK961081 400 µg + oral placebo, DPI GSK961081 1,200 µg + oral placebo, DPI GSK961081 400 µg + oral propranolol 80 mg, DPI GSK961081 1,200 µg + oral propranolol 80 mg and DPI and oral placebo."( Use of propranolol blockade to explore the pharmacology of GSK961081, a bi-functional bronchodilator, in healthy volunteers: results from two randomized trials.
Ambery, C; Norris, V, 2014
)
0.4
" RESULTS were adjusted for initial prescriber, initial medication, dosing regimen and relevant comorbidities."( Impact of multiple-dose versus single-dose inhaler devices on COPD patients' persistence with long-acting β₂-agonists: a dispensing database analysis.
Dekhuijzen, PN; Postma, MJ; van Boven, JF; van der Galiën, R; van der Molen, T; van Raaij, JJ; Vegter, S, 2014
)
0.4
"The aim of this study is to assess urine levels of aripiprazole and metabolites among patients receiving steady-state dosing of aripiprazole."( Quantitative levels of aripiprazole parent drug and metabolites in urine.
Buckley, P; Corwin, MJ; Dretchen, K; McEvoy, J; Millet, RA; Morris, AA, 2014
)
0.4
"One hundred fifty adults, judged compliant with a stable aripiprazole regimen, had observed dosing for 5 consecutive days."( Quantitative levels of aripiprazole parent drug and metabolites in urine.
Buckley, P; Corwin, MJ; Dretchen, K; McEvoy, J; Millet, RA; Morris, AA, 2014
)
0.4
" This study aimed to determine abediterol doses with similar peak bronchodilatory effect to salbutamol 400 μg, and duration of action compatible with once-daily dosing in patients with persistent, stable asthma."( A dose-ranging study of the bronchodilator effects of abediterol (LAS100977), a long-acting β2-adrenergic agonist, in asthma; a Phase II, randomized study.
Astbury, C; de Miquel, G; Massana, E; Pujol, H; Ribera, A; Ruiz, S; Seoane, B; Singh, D, 2014
)
0.4
" After multiple oral doses, steady state was achieved after 7 days of dosing (400 or 800 mg QD and 600 mg BID) and accumulation was dose-independent."( Pharmacokinetics and pharmacodynamics of setrobuvir, an orally administered hepatitis C virus non-nucleoside analogue inhibitor.
Appleman, JR; Crowley, CA; Freddo, JL; Mallalieu, NL; Rahimy, MH; Smith, PF, 2014
)
0.4
" A Monte Carlo simulation indicated that the cumulative fraction of response of any dosing regimen was nearly 100% against Streptococcus pneumoniae."( Pharmacokinetics and pharmacodynamics of multiple-dose intravenous nemonoxacin in healthy Chinese volunteers.
Cao, GY; Chang, LW; Chang, YT; Chen, YC; Guo, BN; Shi, YG; Tsai, CY; Wu, JF; Wu, XJ; Ye, XY; Yu, JC; Zhang, J; Zhang, YY; Zhu, DM, 2015
)
0.42
" Dosing with dizocilpine (0."( Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator.
Futamura, T; Hashimoto, K; Yoshimi, N, 2015
)
0.42
" Our results indicated that IV dosage of MTX-DOX is more effective than free DOX (12 fold) in inhibiting the activity of MMP-2 in OSCCs (P<0."( Oral and IV dosages of doxorubicin-methotrexate loaded- nanoparticles inhibit progression of oral cancer by down- regulation of matrix Methaloproteinase 2 expression in vivo.
Abbasi, MM; Hamishehkar, H; Jahanban-Esfahlan, R; Khiavi, MM; Monfaredan, A; Seidi, K, 2014
)
0.4
" In a phase 2b trial, batefenterol produced statistical and clinically significant differences compared to placebo and numerically greater improvements in the primary end point of trough FEV1 compared to salmeterol after 4 weeks of dosing in patients with moderate to severe chronic obstructive pulmonary disease (COPD)."( Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmac
Chen, Y; Hegde, SS; Hughes, AD; Jasper, JR; Jaw-Tsai, S; Lee, TW; Mammen, M; McNamara, A; Pulido-Rios, MT; Steinfeld, T, 2015
)
0.42
" To constitute morphine tolerance, we used a 3 day cumulative dosing regimen."( Attenuation of morphine antinociceptive tolerance by cannabinoid CB1 and CB2 receptor antagonists.
Altun, A; Bagcivan, I; Durmus, N; Gursoy, S; Ozdemir, E; Yildirim, K, 2015
)
0.42
"Escalating dose cohorts of daily erlotinib and dovitinib dosed 5 days on/2 days off, starting after a 2-week lead-in of erlotinib alone, were planned."( Dovitinib and erlotinib in patients with metastatic non-small cell lung cancer: A drug-drug interaction.
Das, M; Frymoyer, A; Neal, JW; Padda, SK; Riess, JW; Wakelee, HA; Zhou, L, 2015
)
0.42
" We evaluated the effect of daily dosing with armodafinil on the pharmacokinetics and safety of the CYP3A4 substrate aripiprazole, an atypical antipsychotic used to treat bipolar I disorder."( Evaluation of Potential Pharmacokinetic Drug-Drug Interaction between Armodafinil and Aripiprazole in Healthy Adults.
Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015
)
0.42
"This article reviews the clinical pharmacology, pharmacodynamic and pharmacokinetic (PK) properties, clinical efficacy and tolerability, drug interactions, and dosing and administration of cobicistat."( Cobicistat: Review of a Pharmacokinetic Enhancer for HIV Infection.
Gauthier, TP; Schafer, JJ; Sherman, EM; Unger, NR; Worley, MV, 2015
)
0.42
"With potent durability through 48 weeks, a tolerability profile comparable to other first- and second-line antiretroviral therapies, and a convenient dosing schedule with low daily pill burden in fixed-dose combination tablets, cobicistat is a potential addition to the management of HIV infection as a PK enhancer."( Cobicistat: Review of a Pharmacokinetic Enhancer for HIV Infection.
Gauthier, TP; Schafer, JJ; Sherman, EM; Unger, NR; Worley, MV, 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
)
0.42
" For dolutegravir, plasma terminal elimination t1/2 to the last measurable concentration (within 216 h) was longer than its t1/2 within the dosing interval (0-24 h): 14."( Dolutegravir and elvitegravir plasma concentrations following cessation of drug intake.
Amara, A; Back, D; Boffito, M; Elliot, E; Else, L; Jackson, A; Khoo, S; Moyle, G; Owen, A, 2016
)
0.43
"Three spectrophotometric methods have been developed and validated for determination of indacaterol (IND) and glycopyrronium (GLY) in their binary mixtures and novel pharmaceutical dosage form."( Simultaneous spectrophotometric determination of indacaterol and glycopyrronium in a newly approved pharmaceutical formulation using different signal processing techniques of ratio spectra.
Abdel Ghany, MF; Hussein, LA; Magdy, N; Yamani, HZ, 2016
)
0.43
" Simulations based on the final model served to compare expected drug concentrations under standard and alternative dosage regimens."( Population pharmacokinetic analysis of elvitegravir and cobicistat in HIV-1-infected individuals.
Aouri, M; Barceló, C; Buclin, T; Cavassini, M; Csajka, C; Decosterd, LA; Gaspar, F; Guidi, M; Panchaud, A; Rotger, M, 2016
)
0.43
" New information about cardiovascular events is prompting the discontinuation of higher dosing regimens in both ongoing trials."( Laquinimod in the treatment of relapsing remitting multiple sclerosis.
Hainke, U; Thomas, K; Ziemssen, T, 2016
)
0.43
"Cobicistat and ritonavir are structurally distinct compounds that both potently inhibit cytochrome P450 (CYP) 3A, the metabolizing enzyme primarily responsible for the elimination of several antiretroviral medications, and, as such, are pharmacokinetic boosters for antiretroviral agents that require longer dosing intervals."( Drug Interactions with Cobicistat- or Ritonavir-Boosted Elvitegravir.
Custodio, JM; McNicholl, I; Nguyen, T; Piontkowsky, D; Szwarcberg, J,
)
0.13
" In our monotherapy assessments, we found that ATV functioned as a single-dose curative compound in suppressive tests whereas ELQ-300 demonstrated a unique cumulative dosing effect that successfully blocked recrudescence even in a high-parasitemia acute infection model."( Atovaquone and ELQ-300 Combination Therapy as a Novel Dual-Site Cytochrome bc1 Inhibition Strategy for Malaria.
Forquer, IP; Kelly, JX; Li, Y; Morrisey, JM; Nilsen, A; Pou, S; Riscoe, MK; Smilkstein, MJ; Stickles, AM; Vaidya, AB; Winter, RW, 2016
)
0.43
"The aim of this study was to evaluate flexibly dosed brexpiprazole for early-episode schizophrenia through the assessment of efficacy, social functioning, and tolerability."( The effect of brexpiprazole in adult outpatients with early-episode schizophrenia: an exploratory study.
Baker, RA; Malla, A; Nagamizu, K; Ota, A; Perry, P; Weiller, E, 2016
)
0.43
" Patients could continue to receive dovitinib capsules on the same dosing schedule during the post-bioequivalence phase."( Randomized phase 1 crossover study assessing the bioequivalence of capsule and tablet formulations of dovitinib (TKI258) in patients with advanced solid tumors.
Becerra, C; Bruce, J; Carlson, G; Chung, V; Goel, S; Infante, J; Kabbinavar, F; Lockhart, AC; Munster, P; Pant, S; Patel, MR; Sarantopoulos, J; Scott, JW; Sharma, S; Tan, E; Tawbi, H; Yang, S, 2016
)
0.43
" Elvitegravir, cobicistat and darunavir concentrations at the end of the dosing interval ( C 24 ) were quantified using a validated LC with tandem MS method."( Pharmacokinetic interactions between cobicistat-boosted elvitegravir and darunavir in HIV-infected patients.
Benmarzouk-Hidalgo, OJ; Espinosa, N; Fernandez-Magdaleno, T; Gutierrez-Valencia, A; Llaves, S; Lopez-Cortes, LF; Viciana, P, 2017
)
0.46
"The results provide evidence of similar elvitegravir and darunavir C 24 concentrations when these drugs are co-administered as co-formulated elvitegravir, cobicistat, emtricitabine and tenofovir disoproxil fumarate plus 800 mg darunavir or dosed separately."( Pharmacokinetic interactions between cobicistat-boosted elvitegravir and darunavir in HIV-infected patients.
Benmarzouk-Hidalgo, OJ; Espinosa, N; Fernandez-Magdaleno, T; Gutierrez-Valencia, A; Llaves, S; Lopez-Cortes, LF; Viciana, P, 2017
)
0.46
" The pretreatment period, dosing frequency, and dose dependency of rebamipide were examined."( Intra-oral administration of rebamipide liquid prevents tongue injuries induced by X-ray irradiation in rats.
Nakashima, T; Sakurai, K; Uematsu, N, 2017
)
0.46
"Brexpiprazole showed efficacy for the treatment of schizophrenia in the range of 2 to 4 mg/d and as an adjunct to antidepressant therapy in MDD when dosed at 2 to 3 mg/d."( Brexpiprazole.
Gallipani, A; Markovic, M; Maroney, M; Patel, KH, 2017
)
0.46
" The pharmacokinetics (PK) and pharmacodynamics (PD) of antimicrobials in these patients differ significantly from the patient groups from whose data the conventional dosing regimens were developed."( The role of infection models and PK/PD modelling for optimising care of critically ill patients with severe infections.
Bassetti, M; Brüggemann, RJ; Bulitta, JB; De Waele, JJ; Felton, TW; Friberg, LE; Marchand, S; Nielsen, EI; Ramos Martín, V; Roberts, JA; Tam, VH; Tängdén, T; Theuretzbacher, U; Tsuji, BT; Wareham, DW, 2017
)
0.46
"5mg/kg) and 5-day repeated dosing at the highest doses achievable (IMA-08401: 100mg/kg/day; and IMA-07101: 75mg/kg/day)."( Toxicological characterisation of two novel selective aryl hydrocarbon receptor modulators in Sprague-Dawley rats.
Esteban, J; Håkansson, H; Lindén, J; Mahiout, S; Pettersson, L; Pohjanvirta, R; Sánchez-Pérez, I; Sankari, S, 2017
)
0.46
"Methacholine dose-response curves illustrate pharmacologic bronchoprotection against methacholine-induced airway hyperresponsiveness and can be used to quantitate changes in airway sensitivity (position), reactivity (slope), and maximal responsiveness following drug administration."( The effect of glycopyrronium and indacaterol, as monotherapy and in combination, on the methacholine dose-response curve of mild asthmatics: a randomized three-way crossover study.
Blais, CM; Cockcroft, DW; Davis, BE, 2017
)
0.46
"Methacholine dose-response curves differentiate the bronchoprotective mechanisms triggered by different classes of asthma medications."( The effect of glycopyrronium and indacaterol, as monotherapy and in combination, on the methacholine dose-response curve of mild asthmatics: a randomized three-way crossover study.
Blais, CM; Cockcroft, DW; Davis, BE, 2017
)
0.46
"Standard elvitegravir and cobicistat dosing during pregnancy results in significantly lower exposure which may increase the risk of virologic failure and mother-to-child transmission."( Elvitegravir/cobicistat pharmacokinetics in pregnant and postpartum women with HIV.
Acosta, EP; Badell, ML; Barr, E; Best, BM; Burchett, S; Capparelli, EV; Chakhtoura, N; Mirochnick, M; Momper, JD; Park, K; Purswani, M; Shapiro, DE; Smith, E; Stek, A; Wang, J, 2018
)
0.48
"Laquinimod is an orally dosed immuno-modulator currently under development for Huntington's disease (HD)."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
0.51
" At baseline (pre-switch) and at 12 weeks post-switch, we measured HIV-1 RNA in seminal plasma (SP) and blood plasma (BP), tenofovir (TFV) in SP and BP, and TFV-diphosphate (dp) in peripheral blood mononuclear cells (PBMCs) and seminal mononuclear cells (SMCs) at the end of the dosing interval (C24h)."( Seminal Tenofovir Concentrations, Viral Suppression, and Semen Quality With Tenofovir Alafenamide, Compared With Tenofovir Disoproxil Fumarate (Spanish HIV/AIDS Research Network, PreEC/RIS 40).
Cottrell, ML; Garcia, B; Imaz, A; Kashuba, ADM; Morenilla, S; Niubó, J; Perez, E; Podzamczer, D; Tiraboschi, JM, 2019
)
0.51
"A sensitive, selective and precise high performance thin layer chromatographic method has been developed and validated for the quantification of Brexpiprazole in bulk drug and in pharmaceutical dosage form."( Stability Indicating TLC Method for Quantification of Brexpiprazole in Bulk and Its Pharmaceutical Dosage Form and Determination of Content Uniformity.
Chhalotiya, UK; Desai, JV; Parekh, N; Shah, DA; Thakkar, AM, 2019
)
0.51
" Combined with its favorable features, such as a low dosing frequency and a 5 days treatment regimen, ozenoxacin 1% cream is an important option for the treatment of impetigo for pediatric and adult populations."( Topical Ozenoxacin Cream 1% for Impetigo: A Review
Andriessen, A; Bhatia, N; Grada, A; Patele, D; Schachner, L, 2019
)
0.51
"High urine FTC and TFV concentrations could provide an indication of adherence to daily oral dosing with TDF or TAF-based regimens used for treatment and prevention."( Brief Report: Urine Emtricitabine and Tenofovir Concentrations Provide Markers of Recent Antiretroviral Drug Exposure Among HIV-Negative Men Who Have Sex With Men.
Conway-Washington, C; Dinh, C; Fountain, J; Haaland, RE; Hall, L; Holder, A; Kelley, CF; Livermont, T; Lupo, LD; Martin, A, 2019
)
0.51
" Cilostamide at the high dosage (20 μM) also upregulated GJA1 expression."( Cilostamide and forskolin maintain gap junction function of incubated dog follicles.
Brown, M; Chansaenroj, A; Doriguzzi, N; Nagashima, J; Songsasen, N; Thongkittidilok, C, 2020
)
0.56
"Tailoring medication dosing for the individual patient is complex, and many factors can influence drug exposure."( Impact of age and CYP2D6 genetics on exposure of aripiprazole and dehydroaripiprazole in patients using long-acting injectable versus oral formulation: relevance of poor and intermediate metabolizer status.
Correll, CU; Høiseth, G; Molden, E; Smith, RL; Tveito, M, 2020
)
0.56
" Due to its extremely low solubility in water, it was difficult to develop an injectable liquid dosage form."( Injected laquinimod D-α-tocopheryl polyethylene glycol-1000 succinate polymeric micelles for the treatment of inflammatory bowel disease.
Chen, R; Tong, M; Wang, L; Xu, H; Xue, P; Yang, W; Yao, Q; Yuan, J; Zhao, Y; ZhuGe, D, 2020
)
0.56
"The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
"A simple and precise novel stability-indicating method for the simultaneous estimation of tezacaftor and ivacaftor in combined tablet dosage form was developed and validated using reversed-phase high-performance liquid chromatography (RP-HPLC)."( Development and Validation of a Novel Stability-Indicating RP-HPLC Method for Simultaneous Determination of Tezacaftor and Ivacaftor in Fixed Dose Combination.
Bansal, P; Chauhan, Y; Maithani, M; Singh, N, 2020
)
0.56
" To determine the drug-drug interaction potential of laquinimod with CYP3A inhibitors and inducers, interaction assessments were conducted in healthy volunteers using single-dose administration of laquinimod before and after multiple dosing of CYP3A inhibitors (ketoconazole, fluconazole, and cimetidine) or a CYP3A4 inducer (rifampin)."( The Effect of CYP3A Induction and Inhibition on the Pharmacokinetics of Laquinimod, a Novel Neuroimmunomodulator.
Elgart, A; Greenblatt, DJ; Loupe, PS; Mimrod, D; Spiegelstein, O; Weiss, S; Zur, AA, 2020
)
0.56
" The results support the recommendation against elvitegravir/cobicistat use during pregnancy, as the elvitegravir concentration at the end of the dosing interval (Ctrough) was reduced by 77%, with 85% of pregnant women having a Ctrough below the effective concentration (EC90)."( Clinically Significant Lower Elvitegravir Exposure During the Third Trimester of Pregnant Patients Living With Human Immunodeficiency Virus: Data From the Pharmacokinetics of ANtiretroviral agents in HIV-infected pregNAnt women (PANNA) Network.
Bukkems, V; Burger, D; Colbers, A; Garcia, C; Konopnicki, D; Lambert, JS; Necsoi, C; Rockstroh, J; Schwarze-Zander, C; Tenorio, CH, 2020
)
0.56
"Current dosing strategies of CFTR modulators are based on serum pharmacokinetics, but drug concentrations in target tissues such as airway epithelia are not known."( Accumulation and persistence of ivacaftor in airway epithelia with prolonged treatment.
Cholon, DM; Esther, CR; Gentzsch, M; Guhr Lee, TN; Quinney, NL, 2020
)
0.56
" Direct measurement of drugs in target tissues may be needed to optimize dosing strategies, and the persistence of CFTR modulators after treatment cessation has implications for personalized medicine approaches."( Accumulation and persistence of ivacaftor in airway epithelia with prolonged treatment.
Cholon, DM; Esther, CR; Gentzsch, M; Guhr Lee, TN; Quinney, NL, 2020
)
0.56
" Tipifarnib was dosed orally twice daily."( Tipifarnib in recurrent, metastatic HRAS-mutant salivary gland cancer.
Aggarwal, R; Brose, M; Chau, NG; Cohen, EEW; Gualberto, A; Guenette, JP; Hanna, GJ; Ho, AL; Metcalf, R; Pérez-Ruiz, E; Razaq, M; Sayehli, CM; Scholz, C; Wilhelm, C; Wong, DJ, 2020
)
0.56
" We report results of a 3 + 3 dose-escalation Phase 1 study for twice-daily (BID) dosing of LY3023414 monotherapy in Japanese patients with advanced malignancies."( Phase 1 dose-escalation study of a novel oral PI3K/mTOR dual inhibitor, LY3023414, in patients with cancer.
Asou, H; Doi, T; Funai, T; Inoue, K; Kondo, S; Ranka, VK; Tajimi, M; Wacheck, V, 2020
)
0.56
" Here, we describe a computational model (COMBAT-COmputational Model of Bacterial Antibiotic Target-binding) that can quantitatively predict antibiotic dose-response relationships."( Drug-target binding quantitatively predicts optimal antibiotic dose levels in quinolones.
Abel Zur Wiesch, P; Abel, S; Clarelli, F; Cohen, T; Lauksund, S; Palmer, A; Singh, B; Storflor, M, 2020
)
0.56
" The observed differences may be caused by the difference in dosing between the two regimens."( Long-acting dual bronchodilator therapy (indacaterol/glycopyrronium) versus nebulized short-acting dual bronchodilator (salbutamol/ipratropium) in chronic obstructive pulmonary disease: A double-blind, randomized, placebo-controlled trial.
Carpaij, OA; Kerstjens, HAM; Niemeijer, A; Seigers, D; van Geffen, WH; Vonk, JM; Westbroek, LF, 2020
)
0.56
" Correlations between CIP and ENR with TP were significant, while OFX was positively associated with total nitrogen (TN) which mainly originated from urban sewage as well as directly dosed drugs in fish farms."( Occurrence, distribution, and health risk assessment of quinolone antibiotics in water, sediment, and fish species of Qingshitan reservoir, South China.
Bashir, S; Chen, Z; Huang, L; Kang, B; Mo, Y; Rad, S; Song, X; Wu, Z; Zeng, H, 2020
)
0.56
" This study demonstrated that crenigacestat combined with different anticancer agents (taladegib, LY3023414, or abemaciclib) was poorly tolerated, leading to lowered dosing and disappointing clinical activity in patients with advanced or metastatic solid tumors."( A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors.
Anderson, B; Azaro, A; Benhadji, KA; Cassier, PA; Italiano, A; Massard, C; Merchan, J; Oakley, G; Pant, S; Tap, WD; Yu, D; Yuen, E, 2021
)
0.62
"To optimize the dosing regimen in patients with severe renal impairment based on population pharmacokinetic (PPK)/pharmacodynamic analysis."( Nemonoxacin dosage adjustment in patients with severe renal impairment based on population pharmacokinetic and pharmacodynamic analysis.
Chen, Y; Fan, Y; Guo, B; Hu, J; Kang, Y; Li, X; Li, Y; Liu, X; Lu, J; Wang, K; Wang, Y; Wu, H; Wu, J; Xu, X; Xue, J; Yu, J; Zeng, X; Zhang, J; Zhang, Y; Zhao, M, 2021
)
0.62
"An extended dosing interval (0."( Nemonoxacin dosage adjustment in patients with severe renal impairment based on population pharmacokinetic and pharmacodynamic analysis.
Chen, Y; Fan, Y; Guo, B; Hu, J; Kang, Y; Li, X; Li, Y; Liu, X; Lu, J; Wang, K; Wang, Y; Wu, H; Wu, J; Xu, X; Xue, J; Yu, J; Zeng, X; Zhang, J; Zhang, Y; Zhao, M, 2021
)
0.62
" This might indicate that the current recommended dose of ivacaftor is at the top of the dose-response curve and that some patients can be treated with lower doses of ivacaftor with similar clinical effect."( Breast development in a 7 year old girl with CF treated with ivacaftor: An indication for personalized dosing?
Beekman, JM; Berkers, G; Heijerman, HG; Jeyaratnam, J; van der Ent, CK; van der Meer, R, 2021
)
0.62
" Additionally, these simulations suggest that CYP2D6 PMs consistently achieve lower minimum concentrations during the dosing interval than CYP2D6 EMs."( Brexpiprazole Pharmacokinetics in CYP2D6 Poor Metabolizers: Using Physiologically Based Pharmacokinetic Modeling to Optimize Time to Effective Concentrations.
Bruno, CD; Chow, CR; Elmokadem, A; Greenblatt, DJ; Housand, C; Jordie, EB; Lesko, LJ, 2022
)
0.72
" These methods are useful for analysis of REB in pharmaceutical dosage form."( Development and Validation of Four Spectrophotometric Methods for Assay of Rebamipide and its Impurity: Application to Tablet Dosage Form.
Alqarni, MA; El Ghobashy, MR; Farid, NF; Moatamed, RS; Naguib, IA, 2022
)
0.72
" The assay is suitable for state-of-the-art pharmacovigilance of CFTR modulator therapy in CF patients, in order to maximize safety and efficacy, and also to establish dose-response relationships in clinical trials."( Isotope dilution LC-MS/MS quantification of the cystic fibrosis transmembrane conductance regulator (CFTR) modulators ivacaftor, lumacaftor, tezacaftor, elexacaftor, and their major metabolites in human serum.
Bruegel, M; Habler, K; Kalla, AS; Nährig, S; Paal, M; Rychlik, M; Teupser, D; Vogeser, M, 2022
)
0.72
" In repeat-dose toxicity studies, except for IV bolus dosing related effects in rat (hyperactivity, mild convulsion, polypnoea and injection site irritation) and dog (emesis and salivation), no other adverse findings limiting the dosing duration were observed."( Preclinical safety evaluation of levonadifloxacin, a novel anti-methicillin-resistant Staphyloccocus aureus benzoquinolizine fluoroquinolone by intravenous and oral administration.
Gupta, S; Kansagara, A; Nandanwar, M; Patel, A; Patel, M; Patel, MA; Thorve, D; Yeole, R, 2022
)
0.72
" Unexpectedly, despite enhanced dissolution rate in a controlled manner, a designed bilayer tablet had no dose- and dosage form dependent in vivo bioavailability in beagle dogs as compared with IR 100 mg RBM reference tablet."( Design and evaluation of in vivo bioavailability in beagle dogs of bilayer tablet consisting of immediate release nanosuspension and sustained release layers of rebamipide.
Cao, QR; Cui, JH; Jin, G; Jung, M; Lee, BJ; Ngo, HV; Park, C; Wang, J, 2022
)
0.72
" Moreover, the enhancement of potential DAMO rates is positively correlated with the dosage of QNs."( Quinolone antibiotics enhance denitrifying anaerobic methane oxidation in Wetland sediments: Counterintuitive results.
Jiang, H; Liu, C; Wang, X; Yang, Y; Zhao, Y, 2022
)
0.72
"Brexpiprazole augmentation is an effective treatment strategy for antidepressant-refractory depression, but its optimal dosage remains unclear."( Optimal dose of brexpiprazole for augmentation therapy of antidepressant-refractory depression: A systematic review and dose-effect meta-analysis.
Furukawa, Y; Hamza, T; Kasai, K; Obata, S; Oguro, S; Ostinelli, EG, 2022
)
0.72
"To find the optimal dosage of brexpiprazole as augmentation of other antidepressants."( Optimal dose of brexpiprazole for augmentation therapy of antidepressant-refractory depression: A systematic review and dose-effect meta-analysis.
Furukawa, Y; Hamza, T; Kasai, K; Obata, S; Oguro, S; Ostinelli, EG, 2022
)
0.72
" We found that patients on ivacaftor monotherapy have variable concentrations well above the maximal effective concentration and may maintain concentrations necessary for the clinical benefit even if dosing is reduced."( Plasma and cellular ivacaftor concentrations in patients with cystic fibrosis.
Acosta, EP; Anderson, JD; Guimbellot, JS; Parker, KL; Rowe, SM; Ryan, KJ; Victoria Odom, L, 2022
)
0.72
"Due to the customary delay between medication approvals in adult and adolescent populations, adolescents with schizophrenia may receive off-label antipsychotic treatment, without empirically justified dosing recommendations."( Population Pharmacokinetic Analysis of Brexpiprazole to Support its Indication and Dose Selection in Adolescents With Schizophrenia.
Cahill, D; Kohegyi, E; Larsen, F; Raoufinia, A; Wang, X; Wang, Y; Ward, C; Zoubroulis, A, 2023
)
0.91
" Focusing on another indication, the ongoing RISE trial investigates the optimal dosage of mitapivat in sickle cell disease."( Mitapivat: A Quinolone Sulfonamide to Manage Hemolytic Anemia in Adults With Pyruvate Kinase Deficiency.
Dima, L; Horenstein, M; Kim, A; Silva, MA; Wills, J,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
bacterial xenobiotic metaboliteAny bacterial metabolite produced by metabolism of a xenobiotic compound in bacteria.
[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 (2)

ClassDescription
monohydroxyquinolineA hydroxyquinoline carrying a single hydroxy substituent.
quinolone
[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]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.81140.140911.194039.8107AID2451
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency9.44950.00798.23321,122.0200AID2546; AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency8.43680.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, serum paraoxonaseOryctolagus cuniculus (rabbit)Ki2.00002.00002.00002.0000AID977610
Carbonic anhydrase 12Homo sapiens (human)Ki0.09300.00021.10439.9000AID1387634; AID649870; AID649882
Carbonic anhydrase 1Homo sapiens (human)Ki7.48670.00001.372610.0000AID1387631; AID649879; AID649891
Carbonic anhydrase 2Homo sapiens (human)Ki136.66670.00000.72369.9200AID1387632; AID649878; AID649890
Carbonic anhydrase 3Homo sapiens (human)Ki0.57000.00022.010210.0000AID649877; AID649889
Carbonic anhydrase 4Homo sapiens (human)Ki0.36000.00021.97209.9200AID649876; AID649888
Carbonic anhydrase 6Homo sapiens (human)Ki0.03300.00011.47109.9200AID649873; AID649885
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.41000.00001.27259.9000AID649875; AID649887
Carbonic anhydrase 7Homo sapiens (human)Ki0.42000.00021.37379.9000AID649872; AID649884
Carbonic anhydrase 9Homo sapiens (human)Ki0.08200.00010.78749.9000AID1387633; AID649871; AID649883
Carbonic anhydrase 13Homo sapiens (human)Ki0.06500.00031.23099.8000AID649869; AID649881
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)IC50 (µMol)20.00000.00210.67505.1300AID748132
Carbonic anhydrase 14Homo sapiens (human)Ki0.03600.00021.50999.9000AID649868; AID649880
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.75000.00001.34129.9700AID649874; AID649886
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo 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)
response to bacteriumCarbonic anhydrase 3Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 3Homo sapiens (human)
superoxide anion generationNeutrophil cytosol factor 1Homo sapiens (human)
protein targeting to membraneNeutrophil cytosol factor 1Homo sapiens (human)
superoxide metabolic processNeutrophil cytosol factor 1Homo sapiens (human)
cellular defense responseNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to reactive oxygen speciesNeutrophil cytosol factor 1Homo sapiens (human)
superoxide anion generationNeutrophil cytosol factor 1Homo sapiens (human)
innate immune responseNeutrophil cytosol factor 1Homo sapiens (human)
respiratory burstNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of JNK cascadeNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionNeutrophil cytosol factor 1Homo sapiens (human)
regulation of respiratory burst involved in inflammatory responseNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to cadmium ionNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to glucose stimulusNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to testosterone stimulusNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of p38MAPK cascadeNeutrophil cytosol factor 1Homo sapiens (human)
reactive oxygen species biosynthetic processNeutrophil cytosol factor 1Homo sapiens (human)
bicarbonate transportCarbonic anhydrase 4Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 4Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 6Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 7Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 7Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 7Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 7Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 7Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 7Homo 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)
one-carbon metabolic processCarbonic anhydrase 13Homo sapiens (human)
protein polyubiquitinationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of telomere maintenance via telomerasePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein localization to chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein poly-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein auto-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of telomere cappingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
negative regulation of telomere maintenance via telomere lengtheningPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 14Homo sapiens (human)
response to bacteriumCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo 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)
carbonate dehydratase activityCarbonic anhydrase 3Homo sapiens (human)
protein bindingCarbonic anhydrase 3Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 3Homo sapiens (human)
nickel cation bindingCarbonic anhydrase 3Homo sapiens (human)
protein bindingNeutrophil cytosol factor 1Homo sapiens (human)
electron transfer activityNeutrophil cytosol factor 1Homo sapiens (human)
superoxide-generating NAD(P)H oxidase activityNeutrophil cytosol factor 1Homo sapiens (human)
SH3 domain bindingNeutrophil cytosol factor 1Homo sapiens (human)
phosphatidylinositol bindingNeutrophil cytosol factor 1Homo sapiens (human)
phosphatidylinositol-3,4-bisphosphate bindingNeutrophil cytosol factor 1Homo sapiens (human)
superoxide-generating NADPH oxidase activator activityNeutrophil cytosol factor 1Homo sapiens (human)
protein bindingCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 4Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 7Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 7Homo 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)
protein bindingCarbonic anhydrase 13Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 13Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 13Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleotidyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
enzyme bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
metal ion bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 14Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
zinc ion bindingCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo 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)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytosolCarbonic anhydrase 3Homo sapiens (human)
cytoplasmCarbonic anhydrase 3Homo sapiens (human)
cytosolNeutrophil cytosol factor 1Homo sapiens (human)
plasma membraneNeutrophil cytosol factor 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeutrophil cytosol factor 1Homo sapiens (human)
membraneNeutrophil cytosol factor 1Homo sapiens (human)
dendriteNeutrophil cytosol factor 1Homo sapiens (human)
phagolysosomeNeutrophil cytosol factor 1Homo sapiens (human)
NADPH oxidase complexNeutrophil cytosol factor 1Homo sapiens (human)
neuronal cell bodyNeutrophil cytosol factor 1Homo sapiens (human)
cytoplasmNeutrophil cytosol factor 1Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 4Homo sapiens (human)
rough endoplasmic reticulumCarbonic anhydrase 4Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentCarbonic anhydrase 4Homo sapiens (human)
Golgi apparatusCarbonic anhydrase 4Homo sapiens (human)
trans-Golgi networkCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
external side of plasma membraneCarbonic anhydrase 4Homo sapiens (human)
cell surfaceCarbonic anhydrase 4Homo sapiens (human)
membraneCarbonic anhydrase 4Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 4Homo sapiens (human)
transport vesicle membraneCarbonic anhydrase 4Homo sapiens (human)
secretory granule membraneCarbonic anhydrase 4Homo sapiens (human)
brush border membraneCarbonic anhydrase 4Homo sapiens (human)
perinuclear region of cytoplasmCarbonic anhydrase 4Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 4Homo sapiens (human)
extracellular regionCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
cytosolCarbonic anhydrase 6Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 6Homo sapiens (human)
extracellular spaceCarbonic anhydrase 6Homo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5A, mitochondrialHomo sapiens (human)
cytosolCarbonic anhydrase 7Homo sapiens (human)
cytoplasmCarbonic anhydrase 7Homo 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)
cytosolCarbonic anhydrase 13Homo sapiens (human)
myelin sheathCarbonic anhydrase 13Homo sapiens (human)
intracellular membrane-bounded organelleCarbonic anhydrase 13Homo sapiens (human)
cytoplasmCarbonic anhydrase 13Homo sapiens (human)
cytosolCarbonic anhydrase 13Homo sapiens (human)
Golgi membranePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
pericentriolar materialPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nuclear envelopePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytosolPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
perinuclear region of cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
membraneCarbonic anhydrase 14Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 14Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 14Homo sapiens (human)
plasma membraneCarbonic anhydrase 14Homo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrial matrixCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
mitochondrionCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
cytoplasmCarbonic anhydrase 5B, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID566699Inhibition of mushroom tyrosinase at 1 mM after 10 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566705Inhibition of human recombinant MMP8 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649882Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649878Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID748132Inhibition of auto-PARsylation of GST-tagged TNKS2 PARP domain (947 to 1162) (unknown origin) expressed in Escherichia coli BL21(DE3) after 2 hrs by LC/MS analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Fragment-based ligand design of novel potent inhibitors of tankyrases.
AID649872Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649887Inhibition of human recombinant carbonic anhydrase 5A preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649886Inhibition of human recombinant carbonic anhydrase 5B preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID238164Displacement of PRP-1 peptide from mouse Tec kinase SH3 domain by fluorescence polarization; No binding2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Identification and specificity studies of small-molecule ligands for SH3 protein domains.
AID566703Inhibition of human recombinant MMP2 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649873Inhibition of human recombinant carbonic anhydrase 6 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1387634Inhibition of recombinant human carbonic anhydrase 12 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines.
AID566702Inhibition of human recombinant MMP1 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649870Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649871Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649879Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID566700Inhibition of human recombinant 5-lipoxygenase at 1 mM after 10 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649883Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1582668Covalent inhibition of recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells interaction with Cy5-p22phox149-162 incubated for 10 mins by fluorescence polarization competition assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery.
AID1387633Inhibition of recombinant human carbonic anhydrase 9 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines.
AID1387631Inhibition of recombinant human carbonic anhydrase 1 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines.
AID668288Cytotoxicity against mouse J774A1 cells after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery of a new antileishmanial hit in 8-nitroquinoline series.
AID649889Inhibition of human recombinant carbonic anhydrase 3 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1360418Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei brucei AnTat 1.9 assessed as decrease in parasite viability after 69 hrs by Alamar Blue assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID566706Inhibition of human recombinant MMP9 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID1360417Antileishmanial activity against axenic amastigote stage of Leishmania infantum MHOM/MA/67/ITMAP-263 assessed as inhibition of parasite metabolic activity after 48 hrs by luciferase reporter assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID649875Inhibition of human recombinant carbonic anhydrase 5A preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649885Inhibition of human recombinant carbonic anhydrase 6 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1387632Inhibition of recombinant human carbonic anhydrase 2 incubated 15 mins prior to testing by CO2 hydration based stopped-flow assay2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines.
AID649884Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID668283Antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery of a new antileishmanial hit in 8-nitroquinoline series.
AID1467207Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Alkaloids from aerial parts of Houttuynia cordata and their anti-inflammatory activity.
AID1360416Electrochemical behavior of the compound assessed as redox potential corrected toward normal hydrogen electrode at 10'-3 mol/L by cyclic voltammetry2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID649877Inhibition of human recombinant carbonic anhydrase 3 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649891Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649868Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1582677Binding affinity to immobilized recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as maximal response by SPR assay relative to quinolin-2-amine2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery.
AID668289Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery of a new antileishmanial hit in 8-nitroquinoline series.
AID649890Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649876Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649888Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID566701Inhibition of recombinant anthrax lethal factor at 1 mM after 30 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649881Inhibition of human recombinant carbonic anhydrase 13 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID649869Inhibition of human recombinant carbonic anhydrase 13 preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID1360419Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID649874Inhibition of human recombinant carbonic anhydrase 5B preincubated for 15 mins to 72 hrs measured after 15 mins by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID566704Inhibition of human recombinant MMP3 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID649880Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins to 72 hrs measured after 6 hrs by stopped flow CO2 hydration method2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II.
AID566707Inhibition of mouse recombinant iNOS at 1 mM after 40 mins by colorimetric assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2012Journal of molecular biology, May-04, Volume: 418, Issue:3-4
Catalytic versatility and backups in enzyme active sites: the case of serum paraoxonase 1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12,309)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990433 (3.52)18.7374
1990's2455 (19.94)18.2507
2000's3378 (27.44)29.6817
2010's4806 (39.04)24.3611
2020's1237 (10.05)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.75

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.75 (24.57)
Research Supply Index9.56 (2.92)
Research Growth Index5.24 (4.65)
Search Engine Demand Index61.82 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,323 (10.29%)5.53%
Reviews1,396 (10.86%)6.00%
Case Studies807 (6.28%)4.05%
Observational80 (0.62%)0.25%
Other9,249 (71.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]