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Chemical Compound Review

nefopam     6-methyl-2-phenyl-3-oxa-6...

Synonyms: Nefopamum, Sinalgico, Fenazoxine, SureCN23646, Nefopam (INN), ...
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Disease relevance of Fenazoxine


Psychiatry related information on Fenazoxine

  • Nefopam displaced 3H-batrachotoxinin and inhibited the uptake of 22Na in the micromolar range and it protected mice against electroshock induced seizures [6].
  • She now obtains nefopam by prescription forgery and self-administers intramuscular nefopam 300 mg/d. She experiences anticholinergic effects of nefopam and, when attempting withdrawal, depressive symptoms [7].
  • RESULTS: There were 70 reports of adverse reactions thought to be causally related to nefopam, most of which appear to be predictable extensions of the pharmacological effect of nefopam, and included confusion, hallucinations, convulsions, dizziness, headache, sweating, urinary retention, nausea, vomiting, tachycardia and palpitations [8].

High impact information on Fenazoxine

  • Relative efficacy, based on summed pain intensity differences, showed measurable but modest dose-dependent analgesia with nefopam, suggesting that the effectiveness of 65 mg propoxyphene lay between 45 mg nefopam and placebo [2].
  • Estimated relative potency of nefopam to aspirin was 10.4 with a 95% confidence interval of 6.3 to 20.8 for SPID, indicating that the analgesic potency of nefopam, 60 mg, was equivalent to that of aspirin, 650 mg [9].
  • A comparison was made of morphine and nefopam in 74 patients who required parenteral analgesia for moderate to severe postoperative and somatic pain, using a single administration, 2-dose level, double-blind design [10].
  • However, when 'higher' dose ratios were compared, morphine and pethidine were usually more effective than nefopam, possibly due to a 'ceiling effect' for analgesia which may occur with higher doses of nefopam, as with other simple analgesics [11].
  • RESULTS: The median effective analgesic dose (median value and 95% confidence interval) of nefopam and ketoprofen were, respectively, 28 mg (17-39 mg) and 30 mg (14-46 mg) [12].

Chemical compound and disease context of Fenazoxine


Biological context of Fenazoxine

  • The authors evaluated the effects of nefopam on the major thermoregulatory responses in humans: sweating, vasoconstriction, and shivering [17].
  • However, no information is presently available on the oral kinetics of (+) and (-) nefopam in humans [18].
  • For the entire study period (loading dose and PCA), morphine use was less for the nefopam group (34.5 (19.6) vs 42.7 (23.6) mg; P=0.01) [19].
  • Following oral administration, (+) and (-) nefopam were rapidly absorbed with bioavailabilities of 44% and 42%, respectively, probably due to a first-pass effect [18].
  • Both left ventricular systolic work index and oxygen consumption index were similar in the two groups before extubation, increased after extubation, and further increased in control patients showing a statistical difference compared to patients treated with nefopam [20].

Anatomical context of Fenazoxine


Associations of Fenazoxine with other chemical compounds


Gene context of Fenazoxine

  • In vitro binding assays revealed that nefopam possesses moderate affinity for histamine H1 and H2 receptor subtypes, with IC50 of 0.8 and 6.9 microM, respectively, but no affinity for histamine H(3) receptor subtype until 100 microM [31].
  • Nefopam (100 microM) effectively prevented NMDA receptor-mediated early appearance (30 min) of toxicity signs induced by the VSSC activator veratridine [4].
  • After I.V. administration, the enantiomers of desmethylnefopam exhibited lower concentrations and longer half-lives (20.0 h for DES1 and 25.3 h for DES2) relative to nefopam enantiomers [18].
  • Although nefopam also bound to the ED site in cockroach AChE, it did not inhibit the enzyme [32].
  • The possible involvement of central serotonergic pathways in the mechanism of action of nefopam was investigated in male albino mice [33].

Analytical, diagnostic and therapeutic context of Fenazoxine

  • Analgesia through nefopam (30 mg, 60 mg, 90 mg), aspirin (325 mg, 650 mg), and placebo were compared in 122 hospitalized patients with moderate to severe postoperative, fracture, or other somatic pain [9].
  • On each experimental day, four recruitment (intensity-response) curves of the R(III) reflex were constructed: before (control period) and then 30, 60 and 90 min after the intravenous injection of nefopam (20 mg) or a placebo [34].
  • Patients receiving nefopam had a mean (+/- s.e.m.) cumulative morphine consumption of 4.1 +/- 0.8 mg in the first hour, compared with 8.5 +/- 0.8 mg in the control group (P less than 0.01) [26].
  • Nefopam injected after constriction was ineffective [21].
  • Determination of plasma nefopam by liquid chromatography and electrochemical detection [35].


  1. Nefopam for severe hiccups. Bilotta, F., Rosa, G. N. Engl. J. Med. (2000) [Pubmed]
  2. Nefopam and propoxyphene in episiotomy pain. Bloomfield, S.S., Barden, T.P., Mitchell, J. Clin. Pharmacol. Ther. (1980) [Pubmed]
  3. Double-blind evaluation of analgesic efficacy of orally administered diclofenac, nefopam, and acetylsalicylic acid (ASA) plus codeine in chronic cancer pain. Minotti, V., Patoia, L., Roila, F., Basurto, C., Tonato, M., Pasqualucci, V., Maresca, V., Del Favero, A. Pain (1989) [Pubmed]
  4. Novel effect of nefopam preventing cGMP increase, oxygen radical formation and neuronal death induced by veratridine. Fernández-Sánchez, M.T., Díaz-Trelles, R., Groppetti, A., Manfredi, B., Brini, A.T., Biella, G., Sotgiu, M.L., Novelli, A. Neuropharmacology (2001) [Pubmed]
  5. Nefopam in postoperative pain. Phillips, G., Vickers, M.D. British journal of anaesthesia. (1979) [Pubmed]
  6. Nefopam blocks voltage-sensitive sodium channels and modulates glutamatergic transmission in rodents. Verleye, M., André, N., Heulard, I., Gillardin, J.M. Brain Res. (2004) [Pubmed]
  7. Nefopam abuse. Villier, C., Mallaret, M.P. The Annals of pharmacotherapy. (2002) [Pubmed]
  8. Adverse reactions associated with nefopam. Pillans, P.I., Woods, D.J. N. Z. Med. J. (1995) [Pubmed]
  9. Oral nefopam and aspirin. Sunshine, A., Laska, E., Slafta, J. Clin. Pharmacol. Ther. (1978) [Pubmed]
  10. Nefopam and morphine in man. Sunshine, A., Laska, E. Clin. Pharmacol. Ther. (1975) [Pubmed]
  11. Nefopam: a review of its pharmacological properties and therapeutic efficacy. Heel, R.C., Brogden, R.N., Pakes, G.E., Speight, T.M., Avery, G.S. Drugs (1980) [Pubmed]
  12. Median effective dose (ED50) of nefopam and ketoprofen in postoperative patients: a study of interaction using sequential analysis and isobolographic analysis. Delage, N., Maaliki, H., Beloeil, H., Benhamou, D., Mazoit, J.X. Anesthesiology (2005) [Pubmed]
  13. Comparison of nefopam and pethidine in postoperative pain. Tigerstedt, I., Sipponen, J., Tammisto, T., Turunen, M. British journal of anaesthesia. (1977) [Pubmed]
  14. Nefopam and clonidine in the prevention of postanaesthetic shivering. Piper, S.N., Suttner, S.W., Schmidt, C.C., Maleck, W.H., Kumle, B., Boldt, J. Anaesthesia. (1999) [Pubmed]
  15. Effect of ketorolac, ketoprofen and nefopam on platelet function. Dordoni, P.L., Della Ventura, M., Stefanelli, A., Iannace, E., Paparella, P., Rocca, B., Accorra, F. Anaesthesia. (1994) [Pubmed]
  16. Effect of a non-opiate analgesic, nefopam hydrochloride, on stress gastric ulcer in rats. Michael, R., Younan, N., Aziz, M., Mostafa, N., Ghobriel, A., Gintautas, J. Proc. West. Pharmacol. Soc. (2001) [Pubmed]
  17. Nefopam, a nonsedative benzoxazocine analgesic, selectively reduces the shivering threshold in unanesthetized subjects. Alfonsi, P., Adam, F., Passard, A., Guignard, B., Sessler, D.I., Chauvin, M. Anesthesiology (2004) [Pubmed]
  18. Effect of route of administration on the pharmacokinetic behavior of enantiomers of nefopam and desmethylnefopam. Chawla, J., Le Guern, M.E., Alquier, C., Kalhorn, T.F., Levy, R.H. Therapeutic drug monitoring. (2003) [Pubmed]
  19. Randomized prospective study of the analgesic effect of nefopam after orthopaedic surgery. Du Manoir, B., Aubrun, F., Langlois, M., Le Guern, M.E., Alquier, C., Chauvin, M., Fletcher, D. British journal of anaesthesia. (2003) [Pubmed]
  20. Effects of shivering prevention on haemodynamic and metabolic demands in hypothermic postoperative neurosurgical patients. Bilotta, F., Pietropaoli, P., La Rosa, I., Spinelli, F., Rosa, G. Anaesthesia. (2001) [Pubmed]
  21. Neuronal sensitization and its behavioral correlates in a rat model of neuropathy are prevented by a cyclic analog of orphenadrine. Biella, G.E., Groppetti, A., Novelli, A., Fernández-Sánchez, M.T., Manfredi, B., Sotgiu, M.L. J. Neurotrauma (2003) [Pubmed]
  22. Quantitative determination of nefopam in human plasma, saliva and cerebrospinal fluid by gas-liquid chromatography using a nitrogen-selective detector. Chang, S.F., Hansen, C.S., Fox, J.M., Ober, R.E. J. Chromatogr. (1981) [Pubmed]
  23. Nefopam excretion in human milk. Liu, D.T., Savage, J.M., Donnell, D. British journal of clinical pharmacology. (1987) [Pubmed]
  24. Modulation of nitric oxide effects by flurbiprofen enantiomers and nefopam and its relation to antinociception. Pallapies, D., Peskar, B.A., Brune, K., Zeilhofer, H.U. Eur. J. Pharmacol. (1994) [Pubmed]
  25. Fatal nefopam overdose. Urwin, S.C., Smith, H.S. British journal of anaesthesia. (1999) [Pubmed]
  26. Assessment of the analgesic efficacy of nefopam hydrochloride after upper abdominal surgery: a study using patient controlled analgesia. McLintock, T.T., Kenny, G.N., Howie, J.C., McArdle, C.S., Lawrie, S., Aitken, H. The British journal of surgery. (1988) [Pubmed]
  27. Analgesic efficacy and safety of nefopam vs. propacetamol following hepatic resection. Mimoz, O., Incagnoli, P., Josse, C., Gillon, M.C., Kuhlman, L., Mirand, A., Soilleux, H., Fletcher, D. Anaesthesia. (2001) [Pubmed]
  28. Molecular properties and inhibition kinetics of acetylcholinesterase obtained from rat brain and cockroach ganglion. Singh, A.K. Toxicology and industrial health. (1990) [Pubmed]
  29. Intrathecal injection of codeine, buprenorphine, tilidine, tramadol and nefopam depresses the tail-flick response in rats. Bernatzky, G., Jurna, I. Eur. J. Pharmacol. (1986) [Pubmed]
  30. Effect of premedication on drug absorption and gastric emptying. Todd, J.G., Nimmo, W.S. British journal of anaesthesia. (1983) [Pubmed]
  31. Role of the histamine system in nefopam-induced antinociception in mice. Girard, P., Pansart, Y., Coppé, M.C., Verniers, D., Gillardin, J.M. Eur. J. Pharmacol. (2004) [Pubmed]
  32. Molecular properties and inhibition kinetics of acetylcholinesterase obtained from rat brain and cockroach ganglion. Singh, A.K. Toxicology and industrial health. (1990) [Pubmed]
  33. Involvement of central serotonergic pathways in nefopam-induced antinociception. Hunskaar, S., Fasmer, O.B., Broch, O.J., Hole, K. Eur. J. Pharmacol. (1987) [Pubmed]
  34. Nefopam strongly depresses the nociceptive flexion (R(III)) reflex in humans. Guirimand, F., Dupont, X., Bouhassira, D., Brasseur, L., Chauvin, M. Pain (1999) [Pubmed]
  35. Determination of plasma nefopam by liquid chromatography and electrochemical detection. Burton, L.C., Loftus, N.J., Vere, D.W., Whelpton, R. J. Chromatogr. (1990) [Pubmed]
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