The effect of chronic oral ketoconazole on in vivo drug metabolism in the rat. 1986

L Jiritano, and A Bortolotti, and M Bonati

To verify the potential in vivo effects of ketoconazole, an antifungal agent with a wide spectrum of activity, on liver function, caffeine and phenytoin were chosen as probes for hepatic oxidative drug metabolism. Chronic treatment with ketoconazole (80 mg/kg oral) in the rat did not affect both pharmacokinetic profile of probes and a few biochemical parameters related to liver functions. These results indicate that further specific hepatic drug-metabolizing monoxygenase activities responsible to ketoconazole are to be identified to explain ketoconazole-drug interactions reported in vivo.

UI MeSH Term Description Entries
D007654 Ketoconazole Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. Nizoral,R-41400,R41,400,R41400,R 41400
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D010672 Phenytoin An anticonvulsant that is used to treat a wide variety of seizures. It is also an anti-arrhythmic and a muscle relaxant. The mechanism of therapeutic action is not clear, although several cellular actions have been described including effects on ion channels, active transport, and general membrane stabilization. The mechanism of its muscle relaxant effect appears to involve a reduction in the sensitivity of muscle spindles to stretch. Phenytoin has been proposed for several other therapeutic uses, but its use has been limited by its many adverse effects and interactions with other drugs. Diphenylhydantoin,Fenitoin,Phenhydan,5,5-Diphenylhydantoin,5,5-diphenylimidazolidine-2,4-dione,Antisacer,Difenin,Dihydan,Dilantin,Epamin,Epanutin,Hydantol,Phenytoin Sodium,Sodium Diphenylhydantoinate,Diphenylhydantoinate, Sodium
D002110 Caffeine A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling. 1,3,7-Trimethylxanthine,Caffedrine,Coffeinum N,Coffeinum Purrum,Dexitac,Durvitan,No Doz,Percoffedrinol N,Percutaféine,Quick-Pep,Vivarin,Quick Pep,QuickPep
D004364 Pharmaceutical Preparations Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form. Drug,Drugs,Pharmaceutical,Pharmaceutical Preparation,Pharmaceutical Product,Pharmaceutic Preparations,Pharmaceutical Products,Pharmaceuticals,Preparations, Pharmaceutical,Preparation, Pharmaceutical,Preparations, Pharmaceutic,Product, Pharmaceutical,Products, Pharmaceutical
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

Related Publications

L Jiritano, and A Bortolotti, and M Bonati
January 1985, Drug metabolism and disposition: the biological fate of chemicals,
L Jiritano, and A Bortolotti, and M Bonati
March 1985, Clinical pharmacology and therapeutics,
L Jiritano, and A Bortolotti, and M Bonati
May 1987, Research communications in chemical pathology and pharmacology,
L Jiritano, and A Bortolotti, and M Bonati
November 2011, Journal of pharmaceutical sciences,
L Jiritano, and A Bortolotti, and M Bonati
November 1987, Research communications in chemical pathology and pharmacology,
L Jiritano, and A Bortolotti, and M Bonati
December 1971, The Journal of pharmacology and experimental therapeutics,
L Jiritano, and A Bortolotti, and M Bonati
January 1990, Research communications in chemical pathology and pharmacology,
L Jiritano, and A Bortolotti, and M Bonati
February 1980, Life sciences,
L Jiritano, and A Bortolotti, and M Bonati
December 1985, British journal of experimental pathology,
L Jiritano, and A Bortolotti, and M Bonati
January 1974, Clinical pharmacology and therapeutics,
Copied contents to your clipboard!