Nefopam

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Nefopam
File:Nefopam.svg
Systematic (IUPAC) name
5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine
Clinical data
Routes of
administration
Oral, Intravenous
Legal status
Legal status
  • Uncontrolled
Identifiers
CAS Number 13669-70-0
ATC code N02BG06 (WHO)
PubChem CID 4450
Chemical data
Formula C17H19NO
Molar mass 253.34 g/mol[[Script error: No such module "String".]]
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Nefopam (Acupan) is a centrally-acting but non-opioid analgesic drug of the benzoxazocine chemical class which was 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]

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] Recently, like its analogue orphenadrine which also has analgesic effects, nefopam has been found to act as a voltage-gated sodium channel blocker, and this may in part or fully mediate its antinociceptive effects.[18]

Recreational Use/Overdose

Recreational use of nefopam and death from overdose have both been reported,[19][20] although these events are less common with nefopam than with opioid analgesic drugs.[21][22]

See also

References

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fr:Néfopam
  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
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  3. Cohen A, Hernandez CM (1976). "Nefopam hydrochloride: new analgesic agent". Journal of International Medical Research. 4 (2): 138–43. PMID 799984. 
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  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. 
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  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. 
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  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. 
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  19. 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.
  20. 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.
  21. Urwin SC, Smith HS. Fatal nefopam overdose. British Journal of Anaesthesia. 1999 Sep;83(3):501-2.
  22. Villier C, Mallaret MP. Nefopam abuse. Annals of Pharmacotherapy. 2002 Oct;36(10):1564-6.