The metabolism and excretion of buprenorphine in humans

E. J. Cone, C. W. Gorodetzky, D. Yousefnejad, W. F. Buchwald, R. E. Johnson

Research output: Contribution to journalArticle

Abstract

Buprenorphine, a powerful mixed agonist-antagonist analgesic which shows promise of providing maintenance pharmacotherapy for heroin addicts, is metabolized in male human subjects to norbuprenorphine and to conjugated buprenorphine and norbuprenorphin. Following subcutaneous, sublingual, and oral buprenorphine administration to a single subject, total metabolite excretion in urine was 2, 13.4, and 12.1%, respectively. No free parent drug was detected in urine. The amount of norbuprenorphine metabolite excreted in urine generally exceeded that of conjugated buprenorphine. In contrast, free and conjugated buprenorphine equaled or greatly exceeded total norbuprenorphine content in fecal samples following oral or sublingual administration. The greatest amount of drug and metabolite eliminated in feces occurred at 4 to 6 days following buprenorphine administration at times when there was very little urinary excretion of conjugated buprenorphine. This latter evidence indicates an enterohepatic circulation of buprenorphine in humans.

Original languageEnglish (US)
Pages (from-to)577-581
Number of pages5
JournalDrug Metabolism and Disposition
Volume12
Issue number5
StatePublished - Dec 13 1984

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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    Cone, E. J., Gorodetzky, C. W., Yousefnejad, D., Buchwald, W. F., & Johnson, R. E. (1984). The metabolism and excretion of buprenorphine in humans. Drug Metabolism and Disposition, 12(5), 577-581.