Pharmacokinetics and metabolism of premazepam, a new potential anxiolytic, in humans

B. Vitiello, G. Buniva, A. Bernareggi, A. Assandri, A. Perazzi, L. M. Fuccella, R. Palumbo

Research output: Contribution to journalArticlepeer-review

Abstract

Premazepam, a pyrrolodiazepine with potential anxiolytic properties, behaves as a partial antagonist to diazepam in animal tests. Its pharmacokinetics and metabolism were studied in four healthy volunteers. After oral administration of 30 mg [6-14C] premazepam, the plasma levels of total radioactivity reached maximum concentrations 1-4 h (mean 2 h) following administration. The plasma curve was described by an open one-compartment model, and half-life was 11.5 ± 1.3 h. Levels of the unchanged compound accounted for about 80% of the total radioactivity up to 24 h. Half-life of the unchanged compound was 7.9 ± 1.2 h. On the average, 89.6% of the administered radioactivity was recovered in the urine and 2.3% in the feces during the 5 days following administration. Unchanged premazepam accounted for 70% of the total radioactivity excreted in the urine. Of the three metabolites identified in the urine, none was active in vitro in displacing 3H-diazepam from its forebrain receptors in the rat, indicating that only the parent compound has definite pharmacologic activity.

Original languageEnglish (US)
Pages (from-to)273-277
Number of pages5
JournalInternational Journal of Clinical Pharmacology Therapy and Toxicology
Volume22
Issue number5
StatePublished - Jul 5 1984

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology (medical)

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