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Heroin, α- l -acetylmethadol (LAAM), morphine, and methadone each maintained self-administration in rhesus monkeys. The order of relative potency was heroin ≥ LAAM > morphine ≥ methadone. Total daily drug intake increased as dose per injection increased; maximum daily intake was inversely related to relative potency. At high doses, self-injection of methadone and LAAM caused stupor and/or respiratory failure in some monkeys. These toxic effects were partly or completely reversible by naloxone.

Both the release and the metabolism of naltrexone have been evaluated after intramuscular administration of a sustained release [15,16-3H2]naltrexone aluminium tannate complex in guinea-pigs and rhesus monkeys. In both species, measurable excretion of radioactivity was obtained for < 50 days and complete recovery of the dose was obtained in the guinea-pig. The radioactivity excretion rate-time profile differed in the two species with guinea-pig yielding a continuously declining rate and monkey yielding a peak at 5 days. In selected monkey urine samples (days 4,17–20 and 49–52) subjected to t.l.c., evidence was obtained for the presence of naltrexone, β-naltrexol and 2-hydroxy-3-O-methyl-β-naltrexol, mostly as glucuronide and/or sulphate conjugates. The t.l.c. data also suggest that in monkey a naltrexone metabolite builds up relative to naltrexone over the 52 day release period.