URINARY-EXCRETION OF HEROIN AND ITS METABOLITES IN MAN

Abstract

The kinetics of urinary excretion of heroin and its metabolites in human subjects was investigated. Heroin and its metabolites were determined with GLC. Two studies were conducted, each using 10 subjects. After i.v. administration of heroin hydrochloride (10 mg/70 kg) urine was collected every 8 h and ad lib for 1 wk in the 1st study and every 2 h in the first 8 h and then at less frequent intervals for 24 h in the 2nd study. Heroin, 6-acetylmorphine, morphine, the sum of conjugates (morphine plus 6-acetylmorphine) and total normorphine were determined in the first 24-h urine and accounted for 0.5, 1.5, 7.2, 52 and 4%, respectively, of the administered dose. Conjugated morphine was detected in the urine 96 h after drug administration. Eighty-eight percent of the free morphine and 84% of the total morphine found in the urine were excreted in the first 8 h. The half-lives of urinary excretion of free morphine, 6-acetylmorphine, the sum of conjugates (morphine plus 6-acetylmorphine) and total normorphine were 1.28, 1.31, 2.76 and 2.72 h, respectively. Heroin in the body was rapidly metabolized, and its metabolites were rapidly excreted in the urine.