Serum naltrexone and 6-beta-naltrexol levels from naltrexone implants can block very large amounts of heroin: a report of two cases.
The maximum dose of heroin that is blocked by customary doses of oral naltrexone (NTX) and its active metabolite 6-beta-naltrexol (6BNT) is unknown, particularly at trough serum levels which show much interindividual variation and can be low. NTX has only once been tested formally against opiate equivalents of more than 25 mg of diamorphine. Increasing interest in long-acting implantable NTX preparations makes it important to have objective information about blocking activity at various blood levels of NTX and 6BNT. Two cases are described in which NTX and 6BNT levels as low as 2.8 and 9.0 ng/ml, respectively, were sufficient to block doses of pure diamorphine as high as 500 mg.
The Stapleford Centre, London, UK. cb@stap-cen.demon.co.uk
Colin
C
Brewer
D000328:Adult; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D004343:Drug Implants; D006207:Half-Life; D003932:Heroin / Q000008:administration & dosage / Q000037:antagonists & inhibitors*; D006556:Heroin Dependence / Q000097:blood / Q000534:rehabilitation*; D006801:Humans; D008297:Male; D009020:Morphine / Q000493:pharmacokinetics; D009022:Morphine Derivatives / Q000493:pharmacokinetics; D009271:Naltrexone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D009292:Narcotic Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010352:Patient Dropouts
D003692:Delayed-Action Preparations; D004343:Drug Implants; D009022:Morphine Derivatives; D009292:Narcotic Antagonists; C010410:6 beta-hydroxynaltrexone; D009271:Naltrexone; D003932:Heroin; D009020:Morphine; C026979:6-O-monoacetylmorphine