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

M. P. Knadler, R. F. Bergstrom, John Callaghan, A. Rubin

Research output: Contribution to journalArticle

70 Citations (Scopus)

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 - 1986

Fingerprint

Nizatidine
Metabolism
Radioactivity
Metabolites
Plasmas
Propantheline
Warfarin
Phenobarbital
Acetaminophen
Diazepam
Saliva
Propranolol
Oxides
Blood Proteins
Blood Cells
Glycoproteins
Blood

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Cite this

Knadler, M. P., Bergstrom, R. F., Callaghan, J., & Rubin, A. (1986). Nizatidine, an H2-blocker. Its metabolism and disposition in man. Drug Metabolism and Disposition, 14(2), 175-182.

Nizatidine, an H2-blocker. Its metabolism and disposition in man. / Knadler, M. P.; Bergstrom, R. F.; Callaghan, John; Rubin, A.

In: Drug Metabolism and Disposition, Vol. 14, No. 2, 1986, p. 175-182.

Research output: Contribution to journalArticle

Knadler, MP, Bergstrom, RF, Callaghan, J & Rubin, A 1986, 'Nizatidine, an H2-blocker. Its metabolism and disposition in man', Drug Metabolism and Disposition, vol. 14, no. 2, pp. 175-182.
Knadler, M. P. ; Bergstrom, R. F. ; Callaghan, John ; Rubin, A. / Nizatidine, an H2-blocker. Its metabolism and disposition in man. In: Drug Metabolism and Disposition. 1986 ; Vol. 14, No. 2. pp. 175-182.
@article{f88e9ff2bafd474bb7e8cc0ee0450bfd,
title = "Nizatidine, an H2-blocker. Its metabolism and disposition in man",
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.",
author = "Knadler, {M. P.} and Bergstrom, {R. F.} and John Callaghan and A. Rubin",
year = "1986",
language = "English (US)",
volume = "14",
pages = "175--182",
journal = "Drug Metabolism and Disposition",
issn = "0090-9556",
publisher = "American Society for Pharmacology and Experimental Therapeutics",
number = "2",

}

TY - JOUR

T1 - Nizatidine, an H2-blocker. Its metabolism and disposition in man

AU - Knadler, M. P.

AU - Bergstrom, R. F.

AU - Callaghan, John

AU - Rubin, A.

PY - 1986

Y1 - 1986

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0022560113&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0022560113&partnerID=8YFLogxK

M3 - Article

VL - 14

SP - 175

EP - 182

JO - Drug Metabolism and Disposition

JF - Drug Metabolism and Disposition

SN - 0090-9556

IS - 2

ER -