Naltrexone

BeschreibungThis drug does not have agonistic properties. It is similar to naloxone in terms of pharmacological characteristics; however, it differs in two important ways—long-lasting action and that its metabolite 6-β-naltrexol is also a strong antagonist. Naltrexone is potentially hepatotoxic. Naltrexone is used for blocking pharmacological effects of opioids upon their overdose.

HistoryNaloxone was discovered by Drs. Jack Fischman and Mozez Lewenstein of the Memorial Sloan Kettering Institute for Cancer Research in 1961, based on a theory proposed by their colleague, Dr. Harold Blumberg at the Long Island-based Endo Laboratories. Intravenous naloxone (Envizio) was approved by the Food and Drug Administration (FDA) for opioid overdose reversal in 1971 and was shortly adopted as a standard emergency treatment at many of the nation’s premier academic medical centers.

HistoryNaltrexone was first synthesized in 1963 by Endo Laboratories, which was patented by Endo Laboratories in 1967 under the developmental code name EN-1639A. Naltrexone was later purchased in 1969 by DuPont Pharmaceuticals. It was developed by the National Institute on Drug Abuse in the 1970s and early 1980s . In 1984, it was approved by the Food and Drug Administration (FDA) for the treatment of heroin addiction . In 1995, Naltrexone was approved by the FDA for the treatment of alcoholism, when the brand name was changed by DuPont to Revia. A new extended-release formulation of naltrexone has been developed and was approved by the FDA in 2006 for use in the treatment of alcohol dependence.

VerwendenLabeled Naltrexone, intended for use as an internal standard for the quantification of Naltrexone by GC- or LC-mass spectrometry.