The effects of heroin given to human subjects by continuous intravenous infusion are described. Progressive CNS depression eventually required reversal with levallorphan. There was no indication of development of acute tolerance to the depressant effects of heroin. Blood and urine specimens were collected for analysis of metabolites and analyzed for morphine, 6‐monoacetylmorphine, and heroin by gas‐liquid chromatography. Blood concentrations were too low to identify any heroin or metabolites, but about fifty per cent of the dose was recovered in the urine mostly as bound morphine with small amounts of 6‐monoacetylmorphine and heroin present in some specimens. Rate of excretion of total morphine indicated that man can metabolize about 6 mg. per 93 Kg. per hour of heroin.
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