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nefopam

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Description

Nefopam is a centrally acting analgesic with a unique mechanism of action, distinct from opioids and NSAIDs. It is thought to act primarily as a serotonin-norepinephrine reuptake inhibitor (SNRI) and has also been shown to interact with opioid receptors. Nefopam is synthesized through a series of chemical reactions starting with the precursor 4-chloro-N-methyl-N-phenylbutanamide. The compound has been studied for its effectiveness in treating moderate to severe pain, particularly neuropathic pain. Its therapeutic effects include pain relief, muscle relaxation, and anti-anxiety effects. Despite its potential, nefopam has not gained widespread clinical use due to concerns regarding its adverse effects, including potential for abuse and dependency. However, research continues to explore its potential benefits and to optimize its safety profile. '

Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain. [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]

5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively. [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 CID4450
CHEMBL ID465026
CHEBI ID88318
SCHEMBL ID23646
MeSH IDM0014549

Synonyms (80)

Synonym
AC-12146
BRD-A78877355-003-03-6
5-methyl-1-phenyl-3,4,5,6-tetrahydro-1h-benzo[f][1,4]oxazocine
DIVK1C_000384
KBIO1_000384
3,4,5,6-tetrahydro-5-methyl-1-phenyl-1h-2,5-benzoxazocin
einecs 237-148-2
1h-2,5-benzoxazocine, 3,4,5,6-tetrahydro-5-methyl-1-phenyl-
nefopam [inn:ban]
nefopamum [inn-latin]
fenazoxine
SPECTRUM_001376
BSPBIO_000277
PRESTWICK3_000229
nefopam
PRESTWICK2_000229
SPECTRUM5_001349
IDI1_000384
AB00052213
NCGC00094906-01
NCGC00094906-02
KBIO3_001884
KBIOGR_001501
KBIO2_001856
KBIO2_004424
KBIO2_006992
KBIOSS_001856
SPECTRUM3_000912
NINDS_000384
SPECTRUM2_001416
SPBIO_002198
SPECTRUM4_001011
PRESTWICK0_000229
PRESTWICK1_000229
SPBIO_001492
SPECTRUM1501137
BPBIO1_000305
OPREA1_350502
NCGC00094906-03
HMS2092F11
AKOS001582723
13669-70-0
3,4,5,6-tetrahydro-5-methyl-1-phenyl-1h-2,5-benzoxazocine
nefopam (inn)
D08258
HMS501D06
CHEMBL465026
chebi:88318 ,
HMS1921J03
5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine
A807114
4up8060b7j ,
nefopamum
unii-4up8060b7j
pharmakon1600-01501137
nsc757856
CCG-38969
FT-0630408
5-methyl-1-phenyl-3,4,5,6-tetrahydro-1h-2,5-benzoxazocine
nefopam [mi]
nefopam [inn]
nefopam [who-dd]
STL483795
SCHEMBL23646
DTXSID2048535
5-methyl-1-phenyl-3,4,5,6-tetrahydro-1h-2,5-benzoxazocine #
3,4,5,6-tetrahydro-5-methyl-2-phenyl-1h-2,5-benzoxazocine
RGPDEAGGEXEMMM-UHFFFAOYSA-N
AB00052213_10
AB00052213_09
bdbm50237616
SR-01000388442-3
3-methyl-7-phenyl-6-oxa-3-azabicyclo[6.4.0]dodeca-8,10,12-triene
J-006886
SBI-0051651.P002
NCGC00094906-07
DB12293
Q599052
AKOS016842440
EN300-18537040

Research Excerpts

Overview

Nefopam is a non-opioid, non-nonsteroidal anti-imflammatory drug. It inhibits the reuptake of serotonin, norepinephrine, and dopamine. The drug has a theoretical risk of stopping lactation due to its anticholinergic and dopaminergic effects.

ExcerptReferenceRelevance
"Nefopam is a useful agent for contemporary pain control after TKA."( Does Nefopam Provide Analgesic Effect and Reduce Morphine Consumption After Primary Total Knee Arthroplasty? A Prospective, Double-Blind, Randomized Controlled Trial.
Boontanapibul, K; Pinsornsak, P; Sukkarnkosol, S, 2022
)
1.96
"nefopam is a non-opioid, centrally-acting analgesic, frequently prescribed in France for acute pain and postoperatively. "( Nefopam prescribing preferences in French hospitals: results of a survey.
Aubrun, F; Dziadzko, M; Lalande, L; Schulz, T, 2022
)
3.61
"Nefopam is a non-opioid, non-nonsteroidal anti-imflammatory drug, analgesic drug that inhibits the reuptake of serotonin, norepinephrine, and dopamine. "( Postoperative analgesia of intraoperative nefopam in patients undergoing anterior cervical spine surgery: A prospective randomized controlled trial.
Homprasert, C; Nitising, A; Pantubtim, C; Raksakietisak, M; Rushatamukayanunt, P; Sawasdiwipachai, P; Wilaiwan, K, 2022
)
2.43
"Nefopam is a centrally acting analgesic which has a theoretical risk of stopping lactation due to its anticholinergic and dopaminergic effects. "( The effect of nefopam on lactation after caesarean section: a single-blind randomised trial.
Baka, NE; Bouaziz, H; Guerci, P; Hubert, C; Iohom, G; Rouabah, M; Vial, F, 2017
)
2.26
"Nefopam is a non-opioid, non-steroidal, central analgesic thought to act via multiple mechanisms including potent inhibition of serotonin-norepinephrine reuptake and modulation of voltage-sensitive calcium and sodium channels. "( A Simultaneous Mixed-Effects Pharmacokinetic Model for Nefopam, N-desmethylnefopam, and Nefopam N-Oxide in Human Plasma and Urine.
Mittur, A, 2018
)
2.17
"Nefopam is a nonmorphinic central analgesic, for which no recommendation exists concerning adaptation of regimen in aged patients with or without renal impairment. "( Population pharmacokinetics of nefopam in elderly, with or without renal impairment, and its link to treatment response.
Djerada, Z; Fournet-Fayard, A; Gozalo, C; Lamiable, D; Lelarge, C; Malinovsky, JM; Millart, H, 2014
)
2.13
"Nefopam is a non-opioid analgesic drug, used widely in European countries to control postoperative pain. "( Role of the 5-HT(7) receptor in the effects of intrathecal nefopam in neuropathic pain in rats.
Dam, LJ; Ha, YM; Hai, L, 2014
)
2.09
"Nefopam is a non-opiate analgesic commonly used for the treatment of moderate to severe pain. "( Nefopam Hydrochloride: A Fatal Overdose.
De Paoli, G; Drummond, G; Maskell, PD; Seetohul, LN,
)
3.02
"Nefopam is a centrally-acting non-opioid analgesic, which has no effect on bleeding time and platelet aggregation. "( A Randomized Clinical Trial of Nefopam versus Ketorolac Combined With Oxycodone in Patient-Controlled Analgesia after Gynecologic Surgery.
Hwang, BY; Kim, E; Kim, HK; Kim, TK; Kwon, JY; Lee, DW, 2015
)
2.15
"Nefopam is a non-opioid, non-steroidal, centrally acting analgesic drug used to prevent postoperative pain, primarily in the context of multimodal analgesia. "( Nefopam analgesia and its role in multimodal analgesia: A review of preclinical and clinical studies.
Chauvin, M; Girard, P; Verleye, M, 2016
)
3.32
"Nefopam is a widely available analgesic for the management of pain. "( The effect of modulated electro-hyperthermia on the pharmacokinetic properties of nefopam in healthy volunteers: A randomised, single-dose, crossover open-label study.
Kim, MG; Lee, SY, 2015
)
2.09
"Nefopam is an effective analgesic in bimaxillary osteotomy in that it can reduce the use of opioids and nonsteroidal anti-inflammatory drugs, thereby reducing the side effects of conventional analgesics. "( Analgesic effects of nefopam in patients undergoing bimaxillary osteotomy: A double-blind, randomized, placebo-controlled study.
Moon, YE; Park, HJ; Park, JU; Yoo, W, 2016
)
2.2
"Nefopam hydrochloride is a centrally acting compound that induces antinociceptive and antihyperalgesic properties in neuropathic pain models. "( The Antiallodynic Effects of Nefopam Are Mediated by the Adenosine Triphosphate-Sensitive Potassium Channel in a Neuropathic Pain Model.
Bang, JY; Kim, SG; Koh, WU; Shin, JW; Song, JG, 2016
)
2.17
"Nefopam is a centrally-acting but non-opioid analgesic drug of the benzoxazocine chemical class, developed in the early 1970s. "( Single dose oral nefopam for acute postoperative pain in adults.
Derry, S; Kakkar, M; McQuay, HJ; Moore, RA, 2009
)
2.14
"Nefopam is a potent analgesic metabolized by the liver and weakly eliminated intact in urine that may offer advantages for use in patients with ESRD because it lacks respiratory-depressive effects."( Nefopam pharmacokinetics in patients with end-stage renal disease.
Chauvet, S; Couet, W; Debaene, B; Grégoire, N; Le Guern, ME; Levy, RH; Marchand, S; Mimoz, O; Saleh, A, 2010
)
2.52
"Nefopam is a centrally acting non-opioid analgesic with a mechanism of action that is not completely understood. "( Nefopam enhances the protective activity of antiepileptics against maximal electroshock-induced convulsions in mice.
Cięszczyk, J; Czuczwar, K; Czuczwar, M; Kiś, J; Saran, T; Turski, WA; Łuszczki, JJ, 2011
)
3.25
"Nefopam is a non-opioid, non-steroidal, centrally acting analgesic which has an opioid-sparing effect. "( Compartmental pharmacokinetics of nefopam during mild hypothermia.
Bouillon, TW; Kurz, AM; Oehmke, MJ; Podranski, T; Riva, T, 2012
)
2.1
"Nefopam hyghochloride is a potent analgesic compound commercialized in most Western Europe for 20 years, which possesses a profile distinct from that of opioids or anti-inflammatory drugs. "( Nefopam, an analogue of orphenadrine, protects against both NMDA receptor-dependent and independent veratridine-induced neurotoxicity.
Biella, G; Brini, AT; Díaz-Trelles, R; Fernández-Sánchez, MT; Groppetti, A; Manfredi, B; Novelli, A; Sotgiu, ML, 2002
)
3.2
"Nefopam hydrochloride is a non-narcotic analgesic used parenterally and orally as a racemic mixture for the relief of postoperative pain. "( Effect of route of administration on the pharmacokinetic behavior of enantiomers of nefopam and desmethylnefopam.
Alquier, C; Chawla, J; Kalhorn, TF; Le Guern, ME; Levy, RH, 2003
)
1.99
"Nefopam is a central analgesic, with non-opiate action and, because of this inscribed by the WHO in the first grade, but with an analgesic capacity that corresponds to the substances of grade II analgesics."( [The management of acute pain in ambulatory patients. The place of nefopam].
Dacero, JP, 2004
)
1.28
"Nefopam hydrochloride is a potent non sedative benzoxazocine analgesic that possesses a profile distinct from that of anti-inflammatory drugs. "( Nefopam inhibits calcium influx, cGMP formation, and NMDA receptor-dependent neurotoxicity following activation of voltage sensitive calcium channels.
Díaz-Trelles, R; Fernández-Sánchez, MT; Groppetti, A; Novelli, A, 2005
)
3.21
"Nefopam (NEF) is a known analgesic that has recently been shown to be effective in controlling both neuropathic pain and convulsions in rodents. "( Nefopam is more potent than carbamazepine for neuroprotection against veratridine in vitro and has anticonvulsant properties against both electrical and chemical stimulation.
Desogus, CM; Fernández-Sánchez, MT; Ferrero-Gutiérrez, A; Groppetti, A; Manfredi, B; Novelli, A; Pérez-Gómez, A; Rossoni, G, 2007
)
3.23
"Nefopam is a centrally (but not spinally) acting analgesic with a novel activity profile."( Control of cancer pain with analgesics acting in the central nervous system.
Wörz, R, 1984
)
0.99
"Nefopam is a non-narcotic analgesic not structurally related to other analgesic drugs. "( Nefopam: a review of its pharmacological properties and therapeutic efficacy.
Avery, GS; Brogden, RN; Heel, RC; Pakes, GE; Speight, TM, 1980
)
3.15
"Nefopam is a clinically effective analgesic agent used to control mild to moderate pain, whose mechanism of action is unknown. "( The involvement of opioidergic and noradrenergic mechanisms in nefopam antinociception.
Gray, AM; Nevinson, MJ; Sewell, RD, 1999
)
1.99
"Nefopam is a non-opioid analgesic agent with a central mode of action involving activation of descending pain-modulating pathways and inhibition of synaptosomal uptake of hydroxytryptamine, norepinephrine and dopamine. "( Fatal nefopam overdose.
Smith, HS; Urwin, SC, 1999
)
2.23
"Nefopam (NEF) is a potent analgesic compound administered as a racemic mixture. "( Nefopam enantiomers: preclinical pharmacology/toxicology and pharmacokinetic characteristics in healthy subjects after intravenous administration.
Gillardin, JM; Labroo, R; Le Guern, ME; Lepage, F; Levy, RH; Mather, GG, 2000
)
3.19
"Nefopam hydrochloride is a potent analgesic compound that possesses a profile distinct from that of opiods or anti-inflammatory drugs. "( Novel effect of nefopam preventing cGMP increase, oxygen radical formation and neuronal death induced by veratridine.
Biella, G; Brini, AT; Díaz-Trelles, R; Fernández-Sánchez, MT; Groppetti, A; Manfredi, B; Novelli, A; Sotgiu, ML, 2001
)
2.1
"Nefopam is a non-opioid analgesic reported to have some stimulant properties. "( A comparative assay of nefopam, morphine and d-amphetamine.
Jasinski, DR; Preston, KL, 1987
)
2.03

Effects

Nefopam hydrochloride has been commercialized as an analgesic drug in most Western European countries for 20 years. The use of nefopam can lead to nausea and vomiting.

ExcerptReferenceRelevance
"Nefopam has a pharmacologic profile distinct from that of opioids or other anti-inflammatory drugs. "( Mechanical Antiallodynic Effect of Intrathecal Nefopam in a Rat Neuropathic Pain Model.
Baek, SH; Byeon, GJ; Kim, HY; Kim, KH; Koo, ST; Shin, SW, 2015
)
2.12
"Nefopam has been reported to be effective in postoperative pain control with an opioid-sparing effect, but the use of nefopam can lead to nausea and vomiting. "( Physicochemical stability of nefopam and nefopam/droperidol solutions in polypropylene syringes for intensive care units.
Clarot, I; D'Huart, E; Demoré, B; Vigneron, J, 2020
)
2.29
"Nefopam has been considered as a good candidate for inclusion in multimodal analgesia because of its opioid sparing effect, but it can be emetic."( Association of nefopam use with postoperative nausea and vomiting in gynecological patients receiving prophylactic ramosetron: A retrospective study.
Bahk, JH; Kim, JT; Kim, WH; Lim, YJ; Park, SK; Yoo, S, 2018
)
1.56
"Nefopam has shown potential for reducing neuropathic pain, but the underlying mechanisms are unknown."( Nefopam downregulates autophagy and c-Jun N-terminal kinase activity in the regulation of neuropathic pain development following spinal nerve ligation.
Jee, IG; Jung, KT; Lim, KJ; Oh, SH; Yoon, MH; Yu, BS, 2018
)
2.64
"Nefopam has been used as an adjuvant to opioid analgesia after operation. "( Nefopam as an adjunct to intravenous patient-controlled analgesia after renal transplantation: a randomised trial.
Choi, YS; Huh, KH; Kim, SY; Oh, YJ; Park, J; Roh, YH, 2015
)
3.3
"Nefopam has no influence on the extubation time (WMD 0.92; 95% CI -0.15-1.99)."( Nefopam for the prevention of perioperative shivering: a meta-analysis of randomized controlled trials.
Liu, M; Lv, M; Qu, W; Wang, X; Wang, Y, 2015
)
2.58
"Nefopam has a pharmacologic profile distinct from that of opioids or other anti-inflammatory drugs. "( Mechanical Antiallodynic Effect of Intrathecal Nefopam in a Rat Neuropathic Pain Model.
Baek, SH; Byeon, GJ; Kim, HY; Kim, KH; Koo, ST; Shin, SW, 2015
)
2.12
"Nefopam hydrochloride has been commercialized as an analgesic drug in most Western European countries for 20 years. "( Nefopam strongly depresses the nociceptive flexion (R(III)) reflex in humans.
Bouhassira, D; Brasseur, L; Chauvin, M; Dupont, X; Guirimand, F, 1999
)
3.19

Actions

Nefopam can cause unpleasant adverse effects and there are important cautions and contraindications with this analgesic. NefopAm led to a 30% increase in heart rate for one hour (p less than 0.01).

ExcerptReferenceRelevance
"Nefopam can cause unpleasant adverse effects and there are important cautions and contraindications with this analgesic. "( Adverse reactions associated with nefopam.
Pillans, PI; Woods, DJ, 1995
)
2.01
"Nefopam led to a 30% increase in heart rate for one hour (p less than 0.01)."( [Analgesic and respiratory effects of nalbuphine during the immediate postoperative period in thoracotomy].
Boileau, S; Boulanger, G; Laxenaire, MC; Louppe, B; Manel, J, 1990
)
1

Treatment

Nefopam HCl treated subjects had an insignificant change from a control mean of 0.55 ml per 24 hours to 0.60 ml per24 hours. A third of this group actually had a decrease in measurable blood loss.

ExcerptReferenceRelevance
"Nefopam HCl treated subjects had an insignificant change from a control mean of 0.55 ml per 24 hours to 0.60 ml per 24 hours; a third of this group actually had a decrease in measurable blood loss."( Gastrointestinal blood loss study with a new analgesic compound: nefopam hydrochloride.
Baltes, BJ,
)
1.09
"Pretreatment with nefopam could be useful to prevent pain sensitization induced by opioids."( The effect of nefopam on morphine overconsumption induced by large-dose remifentanil during propofol anesthesia for major abdominal surgery.
Clevenot, D; Debaene, B; Derrode, N; Fletcher, D; Rolland, D; Tirault, M, 2006
)
1.02

Toxicity

Intravenous nefopam infusion resulted in significant reduction in postoperative pain scores and opioid requirements. There was a decreased risk of opioid-related adverse effects in the ne fopam groups.

ExcerptReferenceRelevance
" Adverse effects were comparable in the three groups, except for significantly more nausea in the control group (39% vs."( Analgesic efficacy and safety of nefopam vs. propacetamol following hepatic resection.
Fletcher, D; Gillon, MC; Incagnoli, P; Josse, C; Kuhlman, L; Mimoz, O; Mirand, A; Soilleux, H, 2001
)
0.59
" Primary outcomes of interest were patient-reported pain relief of 30% or greater and withdrawals due to adverse events."( Efficacy and safety of neuromodulators in inflammatory arthritis: a Cochrane systematic review.
Buchbinder, R; Richards, BL; van der Heijde, DM; Whittle, SL, 2012
)
0.38
"Based on 3 small trials, which were all at high risk of bias, there is weak evidence that nefopam and capsaicin are superior to placebo in reducing pain in patients with RA, but both are associated with a significant side effect profile."( Efficacy and safety of neuromodulators in inflammatory arthritis: a Cochrane systematic review.
Buchbinder, R; Richards, BL; van der Heijde, DM; Whittle, SL, 2012
)
0.6
" The incidence of adverse effects was noted at 48 h postoperatively."( The analgesic efficacy and safety of nefopam in patient-controlled analgesia after cardiac surgery: A randomized, double-blind, prospective study.
Choi, DK; Choi, IC; Kim, K; Kim, WJ; Lee, YK; Sim, JY, 2014
)
0.68
" There were no other statistically significant between-group differences in the incidence of adverse events."( Opioid sparing effect and safety of nefopam in patient controlled analgesia after laparotomy: A randomized, double blind study.
Cho, CW; Jin, HS; Kim, WJ; Kim, YC; Lee, C; Yoo, Y, 2016
)
0.71
"Intravenous PCA using nefopam + fentanyl following laparotomy has an opioid sparing effect and is associated with a low incidence of some of the typical opioid related adverse events."( Opioid sparing effect and safety of nefopam in patient controlled analgesia after laparotomy: A randomized, double blind study.
Cho, CW; Jin, HS; Kim, WJ; Kim, YC; Lee, C; Yoo, Y, 2016
)
1.02
" Secondary outcomes were length of hospital stay, opioid-related adverse effects, and postoperative complications."( The efficacy and safety of nefopam for pain relief during laparoscopic cholecystectomy: A meta-analysis.
Shen, Z; Sheng, S; Zhao, T, 2018
)
0.78
" Moreover, there was a decreased risk of opioid-related adverse effects in the nefopam groups."( The efficacy and safety of nefopam for pain relief during laparoscopic cholecystectomy: A meta-analysis.
Shen, Z; Sheng, S; Zhao, T, 2018
)
1.01
"Intravenous nefopam infusion resulted in significant reduction in postoperative pain scores and opioid requirements while decreasing opioid-related adverse effects."( The efficacy and safety of nefopam for pain relief during laparoscopic cholecystectomy: A meta-analysis.
Shen, Z; Sheng, S; Zhao, T, 2018
)
1.16

Pharmacokinetics

We identified the nefopam pharmacokinetic predictors for morphine requirement and side-effects, such as tachycardia and postoperative nausea and vomiting. This validated LC/MS method was applied to a study in 12 fasting healthy Pakistani male subjects.

ExcerptReferenceRelevance
" Additionally, a pharmacokinetic study was conducted in human volunteers."( Nefopam enantiomers: preclinical pharmacology/toxicology and pharmacokinetic characteristics in healthy subjects after intravenous administration.
Gillardin, JM; Labroo, R; Le Guern, ME; Lepage, F; Levy, RH; Mather, GG, 2000
)
1.75
" and oral administration, desmethylnefopam enantiomers showed stereoselectivity in AUC and Cmax values."( Effect of route of administration on the pharmacokinetic behavior of enantiomers of nefopam and desmethylnefopam.
Alquier, C; Chawla, J; Kalhorn, TF; Le Guern, ME; Levy, RH, 2003
)
0.82
" The half-life of nefopam was similar whether administered orally (5."( Comparative pharmacokinetics and pharmacodynamics of intravenous and oral nefopam in healthy volunteers.
Alquier, C; Aymard, G; Démolis, P; Diquet, B; Giudicelli, JF; Le Guern, ME; Lechat, P; Warot, D, 2003
)
0.88
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The pharmacokinetic parameter values obtained were compared with those of 12 healthy 50- to 60-year-old volunteers who also received a single 20-mg nefopam infusion over 30 minutes using a population pharmacokinetic approach."( Nefopam pharmacokinetics in patients with end-stage renal disease.
Chauvet, S; Couet, W; Debaene, B; Grégoire, N; Le Guern, ME; Levy, RH; Marchand, S; Mimoz, O; Saleh, A, 2010
)
2
"001), resulting in higher mean nefopam peak concentration (121 and 223 ng/mL vs."( Nefopam pharmacokinetics in patients with end-stage renal disease.
Chauvet, S; Couet, W; Debaene, B; Grégoire, N; Le Guern, ME; Levy, RH; Marchand, S; Mimoz, O; Saleh, A, 2010
)
2.09
" This validated LC/MS method was applied to a pharmacokinetic and bioavailability study in 12 fasting healthy Pakistani male subjects from the blood samples taken up to 24 h after an oral dose of one tablet of 30 mg nefopam in a double-blind, randomized, cross-over design."( Study of pharmacokinetics and comparative bioavailability of nefopam 30 mg tablets in twelve fasting healthy Pakistani male young subjects: single-dose, randomized, two-period, two-treatment and two-way cross-over design.
Ahmad, M; Murtaza, G; Yaqoob, M, 2012
)
0.81
"The results showed that both formulations possessed almost the same relative bioavailability and pharmacokinetic parameters."( Study of pharmacokinetics and comparative bioavailability of nefopam 30 mg tablets in twelve fasting healthy Pakistani male young subjects: single-dose, randomized, two-period, two-treatment and two-way cross-over design.
Ahmad, M; Murtaza, G; Yaqoob, M, 2012
)
0.62
" The association between pharmacokinetic parameters and treatment response was assessed using logistic regression."( Population pharmacokinetics of nefopam in elderly, with or without renal impairment, and its link to treatment response.
Djerada, Z; Fournet-Fayard, A; Gozalo, C; Lamiable, D; Lelarge, C; Malinovsky, JM; Millart, H, 2014
)
0.69
"We identified the nefopam pharmacokinetic predictors for morphine requirement and side-effects, such as tachycardia and postoperative nausea and vomiting."( Population pharmacokinetics of nefopam in elderly, with or without renal impairment, and its link to treatment response.
Djerada, Z; Fournet-Fayard, A; Gozalo, C; Lamiable, D; Lelarge, C; Malinovsky, JM; Millart, H, 2014
)
1.02
" The noncompartmental approach was used to calculate pharmacokinetic parameters."( Pharmacokinetics of dexamethasone and nefopam administered alone or in combination using a newly developed prefilled multi-drug injector in rats.
Fan, K; Gu, J; Ma, J; Yang, T; Yin, G; Zhang, J, 2014
)
0.67
" The co-administration exhibited no significant influence on the pharmacokinetic parameters of DXM."( Pharmacokinetics of dexamethasone and nefopam administered alone or in combination using a newly developed prefilled multi-drug injector in rats.
Fan, K; Gu, J; Ma, J; Yang, T; Yin, G; Zhang, J, 2014
)
0.67
"These results indicate that the co-administration of DXM and nefopam using the prefilled multi-drug injector significantly alters some pharmacokinetic parameters of nefopam and has a minor effect on DXM pharmacokinetics."( Pharmacokinetics of dexamethasone and nefopam administered alone or in combination using a newly developed prefilled multi-drug injector in rats.
Fan, K; Gu, J; Ma, J; Yang, T; Yin, G; Zhang, J, 2014
)
0.91
" The pharmacokinetic profiles of total radioactivity and nefopam were similar in male and female rats."( Pharmacokinetics, distribution, metabolism, and excretion of the dual reuptake inhibitor [(14)C]-nefopam in rats.
Mittur, A; Modi, NB; Shen, H; Solon, E; Yu, J, 2016
)
0.9

Compound-Compound Interactions

Nefopam's morphine-sparing is debated when combined with paracetamol. This study aimed to assess pain relief by IV nefopam in combination with par acetamol after major abdominal surgery.

ExcerptReferenceRelevance
"Because nefopam's morphine-sparing is debated when combined with paracetamol, this study aimed to assess pain relief by IV nefopam in combination with paracetamol after major abdominal surgery."( Opioid-sparing effect of nefopam in combination with paracetamol after major abdominal surgery: a randomized double-blind study.
Alonso, S; Casano, F; Cuvillon, P; Demattei, C; L'hermite, J; Lefrant, JY; Muller, L; Ripart, J; Zoric, L, 2017
)
1.19
"This prospective randomized study suggested that nefopam in combination with paracetamol has no benefit after open abdominal surgery."( Opioid-sparing effect of nefopam in combination with paracetamol after major abdominal surgery: a randomized double-blind study.
Alonso, S; Casano, F; Cuvillon, P; Demattei, C; L'hermite, J; Lefrant, JY; Muller, L; Ripart, J; Zoric, L, 2017
)
1.01

Bioavailability

This study shows a rather low bioavailability of nefopam given in intravenous solution when administered orally. This validated LC/MS method was applied to a pharmacokinetic and bioavailability study in 12 fasting healthy Pakistani male subjects.

ExcerptReferenceRelevance
" Possible drug interactions were detected by the occurrence of side-effects and interference with bioavailability of the new analgesic, also by changes in vital signs or in various laboratory tests."( Nefopam HCl interaction study with eight other drugs.
Back, EL; Cohen, A; Lasseter, KC, 1976
)
1.7
" This study shows a rather low bioavailability of nefopam given in intravenous solution when administered orally."( Comparative pharmacokinetics and pharmacodynamics of intravenous and oral nefopam in healthy volunteers.
Alquier, C; Aymard, G; Démolis, P; Diquet, B; Giudicelli, JF; Le Guern, ME; Lechat, P; Warot, D, 2003
)
0.8
"To study the pharmacokinetics and comparative bioavailability of nefopam tablets (Acupan®)."( Study of pharmacokinetics and comparative bioavailability of nefopam 30 mg tablets in twelve fasting healthy Pakistani male young subjects: single-dose, randomized, two-period, two-treatment and two-way cross-over design.
Ahmad, M; Murtaza, G; Yaqoob, M, 2012
)
0.86
" This validated LC/MS method was applied to a pharmacokinetic and bioavailability study in 12 fasting healthy Pakistani male subjects from the blood samples taken up to 24 h after an oral dose of one tablet of 30 mg nefopam in a double-blind, randomized, cross-over design."( Study of pharmacokinetics and comparative bioavailability of nefopam 30 mg tablets in twelve fasting healthy Pakistani male young subjects: single-dose, randomized, two-period, two-treatment and two-way cross-over design.
Ahmad, M; Murtaza, G; Yaqoob, M, 2012
)
0.81
"The results showed that both formulations possessed almost the same relative bioavailability and pharmacokinetic parameters."( Study of pharmacokinetics and comparative bioavailability of nefopam 30 mg tablets in twelve fasting healthy Pakistani male young subjects: single-dose, randomized, two-period, two-treatment and two-way cross-over design.
Ahmad, M; Murtaza, G; Yaqoob, M, 2012
)
0.62
"One of the greatest challenges drug formulation is facing is poor bioavailability via oral route."( Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation.
Abdel-Aleem, JA; Abou-Taleb, HA; Khallaf, RA, 2018
)
0.79
"77-fold increase in bioavailability of optimized nasal niosomes compared with oral solution of drug."( Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation.
Abdel-Aleem, JA; Abou-Taleb, HA; Khallaf, RA, 2018
)
0.79
"The obtained results revealed the great ability of the produced NF-loaded nio-somes to enhance drug penetration through nasal mucosa and improve its relative bioavailability compared with NF oral solution."( Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation.
Abdel-Aleem, JA; Abou-Taleb, HA; Khallaf, RA, 2018
)
0.79
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management. Morphine was a potent respiratory depressant at therapeutic dosage while neFopam was not.

ExcerptRelevanceReference
" In the oxycodone group, only two patients (12%) needed maximal dosage (6 x 4 mg), one of them requiring 32 mg of oxycodone."( Comparison of the analgesic dose-effect relationships of nefopam and oxycodone in postoperative pain.
Leander, P; Tammisto, T; Tigerstedt, I, 1979
)
0.5
" Morphine was a potent respiratory depressant at therapeutic dosage while nefopam was not."( Respiratory effects of nefopam.
Bellville, JW; Gasser, JC, 1975
)
0.8
" A significant dose-response curve was obtained with nefopam and with morphine, and there was no significant deviation from parallelism."( Nefopam and morphine in man.
Laska, E; Sunshine, A, 1975
)
1.95
" ED50 values were derived from the dose-response lines."( Intrathecal injection of codeine, buprenorphine, tilidine, tramadol and nefopam depresses the tail-flick response in rats.
Bernatzky, G; Jurna, I, 1986
)
0.5
" In the presence of the opioid receptor antagonists, naloxone or naltrindole, the resulting nefopam dose-response relationships were shifted to the right."( The involvement of opioidergic and noradrenergic mechanisms in nefopam antinociception.
Gray, AM; Nevinson, MJ; Sewell, RD, 1999
)
0.76
"Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management."( Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation.
Arora, S; Madan, J; Sharma, N, 2018
)
2.22
" Dosing route-dependent metabolism and clinical effects have been described following intravenous and oral nefopam."( A Simultaneous Mixed-Effects Pharmacokinetic Model for Nefopam, N-desmethylnefopam, and Nefopam N-Oxide in Human Plasma and Urine.
Mittur, A, 2018
)
0.94
" The primary outcome was the dosage of fentanyl-nefopam IV-PCA infused over 24 h postoperatively."( Effect of remifentanil on post-operative analgesic consumption in patients undergoing shoulder arthroplasty after interscalene brachial plexus block: a randomized controlled trial.
Bae, H; Kim, JT; Kim, Y; Lim, YJ; Park, SK; Sakura, S; Yoo, S, 2022
)
0.98
"The dosage of fentanyl-nefopam IV-PCA was significantly less in C group than R group for postoperative 24 h."( Effect of remifentanil on post-operative analgesic consumption in patients undergoing shoulder arthroplasty after interscalene brachial plexus block: a randomized controlled trial.
Bae, H; Kim, JT; Kim, Y; Lim, YJ; Park, SK; Sakura, S; Yoo, S, 2022
)
1.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
benzoxazocineAn organonitrogen heterocyclic compound that consists of a benzene ring ortho-fused at any position to an oxazocine ring.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency1.12200.004023.8416100.0000AID485290
TDP1 proteinHomo sapiens (human)Potency18.35640.000811.382244.6684AID686978; AID686979
survival motor neuron protein isoform dHomo sapiens (human)Potency25.11890.125912.234435.4813AID1458
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (283)

TimeframeStudies, This Drug (%)All Drugs %
pre-199081 (28.62)18.7374
1990's31 (10.95)18.2507
2000's68 (24.03)29.6817
2010's84 (29.68)24.3611
2020's19 (6.71)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.27

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

MetricThis Compound (vs All)
Research Demand Index91.27 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index4.67 (4.65)
Search Engine Demand Index164.38 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (91.27)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials120 (37.74%)5.53%
Reviews25 (7.86%)6.00%
Case Studies21 (6.60%)4.05%
Observational0 (0.00%)0.25%
Other152 (47.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (40)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Effect of Intraoperative Nefopam, Ketoprofen and Paracetamol Combination vs Ketoprofen and Paracetamol Combination on Postoperative Morphine Requirements After Laparoscopic Cholecystectomy: A Randomized, Controlled Trial [NCT04622813]Phase 390 participants (Actual)Interventional2021-04-08Completed
Interest of the Nefopam and PCA Morphine Combination for Postoperative Analgesia in Patients Undergoing Colon Surgery [NCT03619538]80 participants (Actual)Interventional2011-07-31Completed
A MULTICENTER, RANDOMIZED, CONTROLLED STUDY OF EPIDURAL ANALGESIA FOR SEVERE ACUTE PANCREATITIS [NCT02126332]Phase 3148 participants (Actual)Interventional2014-06-06Completed
A Randomized, Placebo Controlled, Double-Blind, Single Dose Study To Evaluate The Safety And Tolerability Of Cream In Burn Patients With Induced Dermal Incisions [NCT04685577]Phase 260 participants (Anticipated)Interventional2022-07-10Recruiting
Comparison of Two Routes of Administration of a Multimodal Analgesic Protocol in Postoperative Cesarean Section Oral vs Intravenous [NCT03626753]Phase 2/Phase 3200 participants (Actual)Interventional2015-01-01Completed
The Effect of Nefopam on Catheter-related Bladder Discomfort: A Double-blind, Randomized, Controlled, Parallel Design Study [NCT03130010]110 participants (Actual)Interventional2017-03-31Completed
A Pharmacokinetic Drug Interaction and Tolerance Study of Paracetamol and Nefopam [NCT02174068]Phase 112 participants (Actual)Interventional2014-07-31Completed
[NCT02493231]Phase 460 participants (Anticipated)Interventional2015-03-31Recruiting
Nefopam vs Tramadol in the Prevention of Post Anaesthetic Shivering Following Subarachnoid Block [NCT02441673]Phase 2130 participants (Anticipated)Interventional2018-10-12Not yet recruiting
Analgesic Effectiveness of Nefopam in Patients Undergoing Anterior Cervical Spine Surgery [NCT03955705]50 participants (Anticipated)Interventional2019-05-15Enrolling by invitation
Comparison of Patient-controlled Analgesia With Background Opioid Versus Non-opioid Infusion for Postoperative Pain in Patients Undergoing Total Knee Arthroplasty: a Randomized, Non-inferiority Study [NCT05861791]98 participants (Anticipated)Interventional2023-02-07Recruiting
[NCT02561494]78 participants (Actual)Interventional2015-06-30Completed
A Randomized Controlled Trial on the Effect and Safety of Intravenous Nefopam/Fentanyl Postoperative Patient-Controlled-Analgesia in Patients Undergoing Laparotomy [NCT02596269]Phase 2/Phase 373 participants (Actual)Interventional2012-10-31Completed
[NCT02577068]84 participants (Actual)Interventional2015-11-15Completed
Postoperative Analgesic Effect of Orally Administrated Nefopam After a Total Knee Arthroplasty: a Randomized Controlled Trial [NCT04576078]Phase 240 participants (Anticipated)Interventional2021-06-29Recruiting
[NCT02561468]94 participants (Actual)Interventional2015-04-30Completed
[NCT02949310]88 participants (Anticipated)Interventional2016-10-31Recruiting
Prospective, Controlled Versus Placebo, Randomized, Double-blind Study, Evaluating the Value of Non-opioid Analgesic Combination (Based on Paracetamol, Nefopam, Ketoprofen) for Postoperative Analgesia. [NCT01882530]Phase 4223 participants (Actual)Interventional2013-07-23Terminated(stopped due to Practice on postoperative pain management changed)
Evaluation of Multimodal Oral Strategies Using Sequential Analysis (Tramadol, Opioid) After Shoulder Ambulatory Surgery [NCT04110665]Phase 4200 participants (Anticipated)Interventional2017-09-01Recruiting
Interest of Néfopam in the Treatment of Pain During the Intense Ureteral Calculi Uncomplicated in Adults in Emergencies Unit. [NCT00639574]Phase 452 participants (Anticipated)Interventional2008-03-31Completed
Nefopam as a Multimodal Analgesia for Video-assisted Thoracoscopic Surgery [NCT05173337]46 participants (Actual)Interventional2021-12-08Completed
A Single Center, Prospective Randomized Double-blind Trial: Efficacy of Nefopam and Morphine in Balanced Analgesia for Acute Ureteric Colic [NCT01543165]Phase 4111 participants (Anticipated)Interventional2012-12-31Recruiting
Study of the Effects of Nefopam on Hyperalgesia Following Sternotomy in Cardiac Surgery [NCT00413257]Phase 2/Phase 390 participants (Actual)Interventional2006-12-31Completed
Analgesic Efficacy of Nefopam in Patients Undergoing Kidney Transplantation : Randomized Controlled Study [NCT01622881]98 participants (Actual)Interventional2012-06-30Completed
Comparative Study Between Nefopam and Ondansteron for Prevention of Post Spinal Shivering. A Randomized Controlled Trial. [NCT04870541]Phase 4150 participants (Anticipated)Interventional2020-12-01Recruiting
Pharmacokinetic Study of a Fixed Dose Combination Nefopam Hydrochloride (30 mg) / Paracetamol (500 mg) and Individual Nefopam Hydrochloride and Paracetamol Taken Alone or Concomitantly After Oral Single Dose [NCT05129137]Phase 131 participants (Actual)Interventional2021-11-29Completed
[NCT01732666]25 participants (Actual)Interventional2012-05-31Completed
[NCT01808014]54 participants (Anticipated)Interventional2013-02-28Recruiting
Effect of Nefopam on Acute Postoperative Pain in Patients Undergoing Orthognathic Surgery [NCT01461031]40 participants (Actual)Interventional2011-10-31Completed
A Comparative, Randomized, Double-blind, 3-arm Parallel, Phase III Study to Evaluate the Efficacy and Safety of a Fixed Dose Combination of Nefopam/Paracetamol Taken Orally in Moderate to Severe Pain After Impacted Third Molar Extraction [NCT04622735]Phase 3321 participants (Actual)Interventional2020-02-22Completed
Non Opioid Treatment for Experimental Dyspnea [NCT01577407]Phase 315 participants (Actual)Interventional2011-09-30Completed
Effects of Continuous Infusion of Intravenous Nefopam on Postoperative Pain and Opioid Consumption After Video Assisted Thoracic Surgery: A Double Blind Randomized Controlled Trial [NCT04450355]90 participants (Actual)Interventional2020-07-30Completed
Adjuvant Continuous Infusion of Nefopam Versus Standard of Care in Mechanically Ventilated Critically Ill Patients: Randomized Double-blind Controlled Study [NCT05071352]Phase 360 participants (Anticipated)Interventional2021-10-01Recruiting
Role of Nefopam in Rituximab Transfusion Reaction [NCT05648058]Phase 3100 participants (Anticipated)Interventional2022-12-20Not yet recruiting
The Comparison Between Epidural and Intravenous Patient-controlled Analgesia for Laparoscopic Gastrectomy [NCT02444897]Phase 360 participants (Actual)Interventional2013-09-30Completed
Nefopam for Post Video-Assisted Thoracoscopic Lobectomy Pain Management and the Improvement of Enhanced Recovery After Surgery (ERAS): A Randomized Controlled Trial [NCT04241640]Phase 472 participants (Actual)Interventional2020-09-01Completed
[NCT01833728]16 participants (Actual)Interventional2013-04-30Completed
Department of Anaesthesiology [NCT04491786]60 participants (Actual)Interventional2020-08-01Completed
A Randomised, Open-label, Single Dose, Crossover Study Investigating the Bioequivalence of Nefopam Hydrochloride 30mg Tablets With Acupan® 30mg Tablets in Healthy Subjects Under Fasting Conditions. [NCT03311022]Phase 129 participants (Actual)Interventional2015-11-06Completed
Effectiveness of Nefopam for Thermoregulation During Surgery [NCT03122665]8 participants (Actual)Interventional2004-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]