Cimetidine impairs nitrazepam clearance

Hermann R. Ochs, David J. Greenblatt, Roland Gugler, Gerrit Müntefering, Ann Locniskar, Darrell R. Abernethy

Research output: Contribution to journalArticle

Abstract

The effect of cimetidine on hepatic clearance of the benzodiazepine derivative nitrazepam was evaluated in healthy subjects. Six received a single 5- or 10-mg oral nitrazepam dose in the drug-free state and again with therapeutic cimetidine doses. Nitrazepam kinetics were determined from multiple serum concentrations measured during the 72 hr after each dose. Cimetidine had no effect on nitrazepam absorption kinetics, since peak serum nitrazepam concentration and time of peak concentration were not altered. Cimetidine did not alter nitrazepam volume of distribution, but cimetidine consistently reduced nitrazepam clearance, from a mean of 1.41 ml/min/kg in the control state to 1.17 mllminlkg during cimetidine treatment. This resulted in prolongation of nitrazepam elimination t 1 2 from 22.2 to 27.8 hr. Thus the ability of cimetidine to impair drug oxidation in man extends to the capacity for clearance of nitrazepam, a compound biotransformed mainly by nitroreduction.

Original languageEnglish (US)
Pages (from-to)227-230
Number of pages4
JournalClinical pharmacology and therapeutics
Volume34
Issue number2
DOIs
StatePublished - Aug 1983

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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    Ochs, H. R., Greenblatt, D. J., Gugler, R., Müntefering, G., Locniskar, A., & Abernethy, D. R. (1983). Cimetidine impairs nitrazepam clearance. Clinical pharmacology and therapeutics, 34(2), 227-230. https://doi.org/10.1038/clpt.1983.157