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Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents.
Gastroenterology. 1982 Jan; 82(1):89-96.G

Abstract

Cimetidine has been demonstrated to impair microsomal oxidative drug metabolism in a dose-dependent manner in an animal model. The inhibition has also been shown to be rapid, occurring after a single dose. In the present study we demonstrate that recovery from inhibition after cimetidine withdrawal is also rapid, occurring within 24 h. Furthermore, chronic dosing with cimetidine does not result in tolerance to the inhibitory effect. Other H2-antihistamines have also been studied both in vivo and in vitro. Based on spectral binding changes, in vitro enzyme assays and in vivo aminopyrine breath tests, ICI 125,211, ranitidine, and cimetidine sulfoxide are much less inhibitory than cimetidine. The ability of cimetidine to impair the elimination of aminopyrine in the mouse after acute liver damage was greater than in the normal mouse.

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Publisher Full Text

Authors

Speeg KV
No affiliation info available
Patwardhan RV
No affiliation info available
Avant GR
No affiliation info available
Mitchell MC
No affiliation info available
Schenker S
No affiliation info available

MeSH

AminopyrineAminopyrine N-DemethylaseAnimalsBreath TestsCimetidineCytochrome P-450 Enzyme SystemDose-Response Relationship, DrugFuransGuanidinesHistamine H2 AntagonistsMaleMiceMice, Inbred ICRMicrosomes, LiverRanitidineRatsRats, Inbred StrainsThiazolesTime Factors

Pub Type(s)

Comparative Study
Journal Article
Research Support, U.S. Gov't, Non-P.H.S.
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

6118315

Citation

Speeg, K V., et al. "Inhibition of Microsomal Drug Metabolism By Histamine H2-receptor Antagonists Studied in Vivo and in Vitro in Rodents." Gastroenterology, vol. 82, no. 1, 1982, pp. 89-96.
Speeg KV, Patwardhan RV, Avant GR, et al. Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents. Gastroenterology. 1982;82(1):89-96.
Speeg, K. V., Patwardhan, R. V., Avant, G. R., Mitchell, M. C., & Schenker, S. (1982). Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents. Gastroenterology, 82(1), 89-96.
Speeg KV, et al. Inhibition of Microsomal Drug Metabolism By Histamine H2-receptor Antagonists Studied in Vivo and in Vitro in Rodents. Gastroenterology. 1982;82(1):89-96. PubMed PMID: 6118315.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents. AU - Speeg,K V,Jr AU - Patwardhan,R V, AU - Avant,G R, AU - Mitchell,M C, AU - Schenker,S, PY - 1982/1/1/pubmed PY - 2001/3/28/medline PY - 1982/1/1/entrez SP - 89 EP - 96 JF - Gastroenterology JO - Gastroenterology VL - 82 IS - 1 N2 - Cimetidine has been demonstrated to impair microsomal oxidative drug metabolism in a dose-dependent manner in an animal model. The inhibition has also been shown to be rapid, occurring after a single dose. In the present study we demonstrate that recovery from inhibition after cimetidine withdrawal is also rapid, occurring within 24 h. Furthermore, chronic dosing with cimetidine does not result in tolerance to the inhibitory effect. Other H2-antihistamines have also been studied both in vivo and in vitro. Based on spectral binding changes, in vitro enzyme assays and in vivo aminopyrine breath tests, ICI 125,211, ranitidine, and cimetidine sulfoxide are much less inhibitory than cimetidine. The ability of cimetidine to impair the elimination of aminopyrine in the mouse after acute liver damage was greater than in the normal mouse. SN - 0016-5085 UR - https://www.unboundmedicine.com/medline/citation/6118315/Inhibition_of_microsomal_drug_metabolism_by_histamine_H2_receptor_antagonists_studied_in_vivo_and_in_vitro_in_rodents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0016508582000018 DB - PRIME DP - Unbound Medicine ER -