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Nefopam
Systematic (IUPAC) name
5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine
Identifiers
CAS number 13669-70-0
ATC code N02BG06
PubChem 4450
Chemical data
Formula C 17H19NO 
Mol. mass 253.34 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status POM (UK)
Routes Oral, Intravenous

Nefopam (marketed under the brandname Acupan) is a centrally-acting but non-opioid analgesic drug of the benzoxazocine chemical class, developed in the early 1970s. It is widely used, mainly in European countries, for the relief of moderate to severe pain as an alternative to opioid analgesic drugs. Animal studies have shown that nefopam has a potentiating (analgesic-sparing) effect on morphine and other opioids by broadening the antinociceptive action of the opioid and possibly other mechanisms, generally lowering the dose requirements of both when they are used concomitantly.[1]

Contents

Use

Nefopam has additional action in the prevention of shivering, which may be a side effect of other drugs used in surgery.[2]

Nefopam at a dose of 30–120 mg is significantly more effective than aspirin as an analgesic,[3] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[4][5]

Nefopam is around half the potency and slightly less effective as an analgesic compared to morphine,[6][7] or oxycodone,[8] but tends to produce less side effects, does not produce respiratory depression,[9] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[10][11]

Nefopam is also used to combat severe hiccups.[12]

Pharmacology

The mechanism of action of nefopam is not well understood, although inhibition of serotonin, dopamine and noradrenaline reuptake is thought to be involved in its analgesic effects,[13][14][15] and there may be other modes of action such as through histamine H3 receptors[16] and glutamate.[17]

Recreational use & Overdose

Recreational use of nefopam and death from overdose have both been reported,[18][19] although these events are less common with nefopam than with opioid analgesic drugs.[20][21]

References

  1. ^ Girard P, Pansart Y, Gillardin JM. Nefopam potentiates morphine antinociception in allodynia and hyperalgesia in the rat. Pharmacology, Biochemistry and Behaviour. 2004 Apr;77(4):695-703. PMID 15099914
  2. ^ Alfonsi P, Adam F, Passard A, Guignard B, Sessler DI, Chauvin M (January 2004). "Nefopam, a nonsedative benzoxazocine analgesic, selectively reduces the shivering threshold in unanesthetized subjects.". Anesthesiology 100 (1): 37–43. doi:10.1097/00000542-200401000-00010. PMID 14695722.  
  3. ^ Cohen A, Hernandez CM (1976). "Nefopam hydrochloride: new analgesic agent.". Journal of International Medical Research 4 (2): 138–43. PMID 799984.  
  4. ^ Wang RI, Waite EM (July 1979). "The clinical analgesic efficacy of oral nefopam hydrochloride.". Journal of Clinical Pharmacology 19 (7): 395–402. PMID 479385.  
  5. ^ Pillans PI, Woods DJ (September 1995). "Adverse reactions associated with nefopam.". New Zealand Medical Journal 108 (1008): 382–4. PMID 7566787.  
  6. ^ Sunshine A, Laska E (November 1975). "Nefopam and morphine in man.". Clinical Pharmacology and Therapeutics 18 ((5 Pt 1)): 530–4. PMID 1102231.  
  7. ^ Phillips G, Vickers MD (October 1979). "Nefopam in postoperative pain.". British Journal of Anaesthesia 51 (10): 961–5. doi:10.1093/bja/51.10.961. PMID 391253.  
  8. ^ Tigerstedt I, Tammisto T, Leander P (December 1979). "Comparison of the analgesic dose-effect relationships of nefopam and oxycodone in postoperative pain.". Acta Anaesthesiologica Scandinavica 23 (6): 555–60. doi:10.1111/j.1399-6576.1979.tb01486.x. PMID 397711.  
  9. ^ Gasser JC, Bellville JW (August 1975). "Respiratory effects of nefopam.". Clinical Pharmacology and Therapeutics 18 (2): 175–9. PMID 1097153.  
  10. ^ Heel RC, Brogden RN, Pakes GE, Speight TM, Avery GS (1980). "Nefopam: a review of its pharmacological properties and therapeutic efficacy.". Drugs 19 (4): 249–67. doi:10.2165/00003495-198019040-00001. PMID 6991238.  
  11. ^ Kapfer B, Alfonsi P, Guignard B, Sessler DI, Chauvin M (January 2005). "Nefopam and ketamine comparably enhance postoperative analgesia.". Anesthesia and Analgesia 100 (1): 169–74. doi:10.1213/01.ANE.0000138037.19757.ED. PMID 15616073.  
  12. ^ Bilotta F, Rosa G. Nefopam for severe hiccups. New England Journal of Medicine. 2000 Dec 28;343(26):1973-4. PMID 11186682
  13. ^ Esposito E, Romandini S, Merlo-Pich E, Mennini T, Samanin R (September 9, 1986). "Evidence of the involvement of dopamine in the analgesic effect of nefopam.". European Journal of Pharmacology 128 (3): 157–64. doi:10.1016/0014-2999(86)90762-4. PMID 3098570.  
  14. ^ Marazziti D, Rotondo A, Ambrogi F, Cassano GB (1991). "Analgesia by nefopam: does it act through serotonin?". Drugs under Experimental and Clinical Research 17 (5): 259–61. PMID 1756689.  
  15. ^ Fuller RW, Snoddy HD (October 1993). "Evaluation of nefopam as a monoamine uptake inhibitor in vivo in mice.". Neuropharmacology 32 (10): 995–9. doi:10.1016/0028-3908(93)90064-A.  
  16. ^ Girard P, Pansart Y, Coppé MC, Verniers D, Gillardin JM (October 25, 2004). "Role of the histamine system in nefopam-induced antinociception in mice.". European Journal of Pharmacology 503 (1-3): 63–9. doi:10.1016/j.ejphar.2004.09.030. PMID 15496297.  
  17. ^ Verleye M, André N, Heulard I, Gillardin JM (July 9, 2004). "Nefopam blocks voltage-sensitive sodium channels and modulates glutamatergic transmission in rodents.". Brain Research 1013 (2): 249–55. doi:10.1016/j.brainres.2004.04.035. PMID 15193535.  
  18. ^ Bismuth C, Fournier PE, Bavoux E, Husson O, Lafon D. Chronic abuse of the analgesic nefopam (Acupan). (French). Journal de Toxicologie Clinique et Experimentale. 1987 Sep-Oct;7(5):343-6.
  19. ^ Piercy DM, Cumming JA, Dawling S, Henry JA. Death due to overdose of nefopam. British Medical Journal (Clinical Research Edition). 1981 Dec 5;283(6305):1508-9.
  20. ^ Urwin SC, Smith HS. Fatal nefopam overdose. British Journal of Anaesthesia. 1999 Sep;83(3):501-2.
  21. ^ Villier C, Mallaret MP. Nefopam abuse. Annals of Pharmacotherapy. 2002 Oct;36(10):1564-6.







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