Nizatidine, an H2-blocker. Its metabolism and disposition in man

M. P. Knadler, R. F. Bergstrom, J. T. Callaghan, A. Rubin

Research output: Contribution to journalArticle

73 Scopus citations

Abstract

The disposition of a single oral dose of about 150 mg of nizatidine, an H2-blocker, was studied in five men. Plasma levels of both parent drug and radioactivity peaked in 1-3 hr. Nizatidine accounted for about 60% of the plasma radioactivity. The T 1/2 of nizatidine was 1.6 hr. About 35% of nizatidine became bound to plasma proteins in vitro, particularly to α-1-glycoprotein. Warfarin, acetaminophen, phenobarbital, propantheline, diazepam, and propranolol did not notably affect the amount of niztidine bound. Two to 3 times more radioactivity was in plasma than in blood cells or saliva. Greater than 90% of the dose of nizatidine was excreted in urine, probably by glomerular filtration and active tubular secretion. Nizatidine accounted for about 65% of the urinary radioactivity. The major metabolite of nizatidine was N2-monodesmethylnizatidine; it represented about 7% of the nizatidine dosage. Another metabolite, constituting about 5% of the dose, is proposed to be nizatidine N2-oxide. Nizatidine sulfoxide also may be a minor metabolite of nizatidine.

Original languageEnglish (US)
Pages (from-to)175-182
Number of pages8
JournalDrug Metabolism and Disposition
Volume14
Issue number2
StatePublished - Jan 1 1986

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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