Long-Term Pharmacotherapy for Opiate (Primarily Heroin) Addiction: Opioid Antagonists and Partial Agonists

摘要: The action of a specific opioid antagonist is to bind receptors and thus prevent the exogenous opioids. Use such an will normal physiological endogenous opioids at their receptors. first pure which was successfully synthesized, characterized, patented in 1960 by Dr. J. Fishman with M.J. Lewenstein naloxone, alkyl derivative nor-oxymorphone (BLUMBERG et al. 1961; BLUMBERG DAYTON 1974). Naloxone used clinically remains extremely useful management accidental or medical overdose. has very limited systemic bioavailability, less than 3% reaching circulation after oral administration; when it for narcotic overdose (or attempt made use more chronic opiate dependency) direct receptor blockade agonist central nervous system, naloxone must be administered parenterally, ideally, intravenously (KREEK 1973c; KREEK 1983a,b,c, 1984). Although brief sporadic attempts were maintenance treatment addiction, clear that this would not suitable because need parenteral route administration. However, studies using showed could block all effects, moreover, reverse effects both (KOSTERLITZ WATT 1968; VEREBEY MULE 1975; VOLAVKA 1979a,b; MENDELSON 1980; NABER 1981; HARTMAN 1982; 1984; COHEN 1983; CULPEPPER-MORGAN 1991.