Depot naltrexone: long-lasting antagonism of the effects of heroin in humans

摘要: Rationale: Naltrexone, an opioid antagonist, is currently approved as a treatment for heroin dependence. However, naltrexone generally not well accepted by patients, and medication non-compliance difficult obstacle to treatment. A sustained-release form of may improve compliance. Objective: The present study was designed evaluate the time course, safety, effectiveness depot formulation (Depotrex®). Methods: Twelve heroin-dependent individuals participated in 8-week inpatient study. After 1-week detoxification period, six participants received 192 mg base 384 base. For low dose tested before high dose. effects (0, 6.25, 12.5, 18.75, 25 mg, IV) were evaluated next 6 weeks. One per day on Mondays through Fridays, entire range each week. Active doses administered ascending order during week, while placebo could be any day. Subjective, performance, physiological measured both after administration. hypotheses that would antagonize heroin, produce more effective longer-lasting antagonism than Results: antagonized heroin-induced subjective ratings 3 5 weeks, respectively. Plasma levels remained above 1 ng/ml approximately 4 weeks administration naltrexone. Other initial discomfort associated with injection naltrexone, there no untoward side-effects. Conclusions: These results suggest this provides safe, effective, long-lasting heroin.