Nefopam
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nefopam
An analgesic used for the relief of persistent pain that has not responded to other non-opioid analgesics; the way in which it works is not completely understood. Nefopam is used to treat moderate pain, including that occurring after operations or dental procedures or associated with cancer; it does not reduce fever or inflammation. Nefopam is available as tablets on prescription only.
Side effects:
include nausea, nervousness, dry mouth, urinary retention, and dizziness.
Precautions:
nefopam should not be used to relieve the pain of a heart attack and should not be taken by people with epilepsy or other convulsive disorders. It should be used with caution in people with liver or kidney disease or urinary retention, in elderly people, and in women who are pregnant or breastfeeding.
Interactions with other drugs:
monoamine oxidase inhibitors should not be taken with nefopam.
Tricyclic antidepressants may increase the side effects of nefopam.
Proprietary preparation:
Acupan.
| nedocromil sodium, nebulizer, nebivolol | |
| nelarabine, nelfinavir, neomycin sulphate |
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Nefopam
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Nefopam
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| Systematic (IUPAC) name | |
| 5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| Pregnancy cat. | ? |
| Legal status | Uncontrolled |
| Routes | Oral, Intravenous |
| Identifiers | |
| CAS number | 13669-70-0  |
| ATC code | N02BG06 |
| PubChem | CID 4450 |
| UNII | 4UP8060B7J |
| KEGG | D08258 |
| Chemical data | |
| Formula | C17H19NO |
| Mol. mass | 253.34 g/mol |
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Nefopam (Acupan) is a centrally-acting but non-opioid analgesic drug of the benzoxazocine chemical class which was developed by Riker Laboratories in the 1960s[1]. 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.[2]
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Use
Nefopam has additional action in the prevention of shivering, which may be a side effect of other drugs used in surgery.[3]
Nefopam at a dose of 30–120 mg is significantly more effective than aspirin as an analgesic,[4] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[5][6]
Nefopam is around half the potency and slightly less effective as an analgesic compared to morphine,[7][8] or oxycodone,[9] but tends to produce fewer side effects, does not produce respiratory depression,[10] 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.[11][12]
Nefopam is also used to combat severe hiccups.[13]
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,[14][15][16] and there may be other modes of action such as through histamine H3 receptors[17] and glutamate.[18] 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.[19]
Recreational Use/Overdose
Recreational use of nefopam and death from overdose have both been reported,[20][21] although these events are less common with nefopam than with opioid analgesic drugs.[22][23]
See also
References
- ^ US Patent 3830803
- ^ 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
- ^ Alfonsi P, Adam F, Passard A, Guignard B, Sessler DI, Chauvin M (January 2004). "Nefopam, a Non-sedative Benzoxazocine Analgesic, Selectively Reduces the Shivering Threshold". Anesthesiology 100 (1): 37–43. doi:10.1097/00000542-200401000-00010. PMC 1283107. PMID 14695722. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1283107.
- ^ Cohen A, Hernandez CM (1976). "Nefopam hydrochloride: new analgesic agent". Journal of International Medical Research 4 (2): 138–43. PMID 799984.
- ^ Wang RI, Waite EM (July 1979). "The clinical analgesic efficacy of oral nefopam hydrochloride". Journal of Clinical Pharmacology 19 (7): 395–402. PMID 479385.
- ^ Pillans PI, Woods DJ (September 1995). "Adverse reactions associated with nefopam". New Zealand Medical Journal 108 (1008): 382–4. PMID 7566787.
- ^ Sunshine A, Laska E (November 1975). "Nefopam and morphine in man". Clinical Pharmacology and Therapeutics 18 ((5 Pt 1)): 530–4. PMID 1102231.
- ^ 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.
- ^ 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.
- ^ Gasser JC, Bellville JW (August 1975). "Respiratory effects of nefopam". Clinical Pharmacology and Therapeutics 18 (2): 175–9. PMID 1097153.
- ^ 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.
- ^ 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. PMC 1283103. PMID 15616073. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1283103.
- ^ Bilotta F, Rosa G. Nefopam for severe hiccups. New England Journal of Medicine. 2000 Dec 28;343(26):1973-4. PMID 11186682
- ^ 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.
- ^ 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.
- ^ 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. PMID 7507578.
- ^ 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.
- ^ 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.
- ^ Verleye M, André N, Heulard I, Gillardin JM (July 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. http://linkinghub.elsevier.com/retrieve/pii/S0006899304006444.
- ^ 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.
- ^ 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.
- ^ Urwin SC, Smith HS. Fatal nefopam overdose. British Journal of Anaesthesia. 1999 Sep;83(3):501-2.
- ^ Villier C, Mallaret MP. Nefopam abuse. Annals of Pharmacotherapy. 2002 Oct;36(10):1564-6.
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