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Journal of Pharmacology And Experimental Therapeutics, Vol. 187, Issue 3, 575-580, 1973
Copyright © 1973 by American Society for Pharmacology and Experimental Therapeutics


DISPOSITION OF NALOXONE-7,8-3H IN NORMAL AND NARCOTIC-DEPENDENT MEN

Jack Fishman 1, Howard Roffwarg 2, and Leon Hellman 2

1 Institute for Steroid Research, Division of Psychiatry and Division on Oncology, Monteflore Hospital and Medical Center, Bronx, New York
2 Institute for Steroid Research, Division of Psychiatry and Division on Oncology, Monteforce Hospital and Medical Center, Bronx, New York

Naloxone-7,8-3H was administered intravenously and orally on separate occasions to the same normal male subject and its disposition was examined. The fate of intravenous naloxone-7,8-3H was also studied in an opiate-dependent subject both while on heroin maintenance and after withdrawal. In all cases the urinary excretioon was rapid but incomplete, nerve exceeding 70% of the dose over 72 hours. Initial plasma concentrations of naloxone were low with a rapid rate of disappearance. Oral naloxone entered plasma quickly but in metabolized form. The volume of distribution, plasma half-life and metabolic clearance rate of naloxone as calculated from the intravenous studies were about 200 liters, 90 minutes and 2500 liters/day, respectively.

Submitted on January 11, 1973
Accepted on August 3, 1973




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Copyright © 1973 by the American Society for Pharmacology and Experimental Therapeutics.