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BIOLOGICAL INFO
Form:
HCl salt
REVIEW Nefopam (Acupan®, Silentan®, Nefadol®, Ajan®) is a centrally-acting but non-opioid analgesic drug of the benzoxazocine chemical class which was developed by Riker Laboratories in the 1960s. It is widely used, mainly in European countries, for the relief of moderate to severe pain as an alternative to opioid analgesic drugs. The mechanism of action of nefopam is not well understood, although inhibition of serotonin, dopamine and noradrenaline reuptake is believed to be involved in its analgesic effects,and there may be other modes of action such as through histamine H3 receptors and glutamate. Recently, nefopam has been found to act as a voltage-gated sodium channel blocker, and this may in part or fully mediate its antinociceptive effects.
REFERENCES
[1]
Heel RC, Brogden RN, Pakes GE, Speight TM, Avery GS. Nefopam: a review of its pharmacological properties and therapeutic efficacy. Drugs. 1980 Apr;19(4):249-67.
[2]
Evans MS, Lysakowski C, Tram?r MR. Nefopam for the prevention of postoperative pain: quantitative systematic review. Br J Anaesth. 2008 Nov;101(5):610-7.
[3]
Esposito E, Romandini S, Merlo-Pich E, Mennini T, Samanin R. Evidence of the involvement of dopamine in the analgesic effect of nefopam. Eur J Pharmacol. 1986 Sep 9;128(3):157-64.
[4]
Marazziti D, Rotondo A, Ambrogi F, Cassano GB, Analgesia by nefopam: does it act through serotonin? Drugs Exp Clin Res. 1991;17(5):259-61.
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