Description
Nalmefene hydrochloride has been introduced in the U.S.A. for opioid reversal
following surgery, and in the reversal of opioid overdoses and epidurally administered
narcotics. Nalmefene is an opioid antagonist that inhibits respiratory, analgesic and
subjective effects of opioids. It has a higher potency, a longer duration of action, and
superior bioavailability than the structurally related naltrexone. Nalmefene has a wide
spectrum of biological activity and is in clinical trials for the treatment of interstitial
cystitis, recalcitrant pruritus of cholestasis, stroke, rheumatoid arthritis, shock, CNS
trauma, and alcoholism. Studies indicate that nalmefene does not induce morphine-like
effects and has no apparent abuse potential.
Uses
Nalmefene Hydrochloride is a structural analog of Naltrexone (N285780) with opiate antagonist activity used in pharmaceutical treatment of alcoholism. Other pharmacological applications of this compound aim to reduce food cravings, drug abuse and pulmonary disease in affected individuals. Used as an opioid-induced tranquilizer on large animals in the veterinary industry. Narcotic antagonist
References
1) Osborn et al. (2010), In vivo characterization of the opioid antagonist nalmefene in mice; Life Sci., 86 624
2) Butelman et al. (2009), Unconditioned behavioral effects of the powerful kappa-opioid hallucinogen salvinorin A in non-human primates: fast onset and entry in cerebrospinal fluid; J. Pharmacol. Exp. Ther., 328 588
3) Butelman et al. (2008), The effects of herkinorin, the first mu-selective ligand from salvinorin A-derived scaffold, in neuroendocrine biomarker assay in nonhuman primates; J. Pharmacol. Exp. Ther., 327 154
4) Soyka and Rosner (2008), Opioid antagonists for pharmacological treatment of alcohol dependence – a critical review; Curr. Drug Abuse Rev., 1 280
