Dantrolene sodium: urinary metabolites and hepatotoxicity.

T H, Arnold; J M, Epps; H R, Cook; M E, Hamrick

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Article . 1983

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Dantrolene sodium: urinary metabolites and hepatotoxicity.

descriptionPublicationkeyboard_double_arrow_right Article 08 Jul 1983 English Journal:Research communications in chemical pathology and pharmacology, volume 39 (issn: 0034-5164,

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Authors: T H, Arnold; J M, Epps; H R, Cook; M E, Hamrick;

pmid: 6856946

Dantrolene sodium: urinary metabolites and hepatotoxicity.

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Abstract

Dantrolene is metabolized by the hepatic MFO system to hydroxydantrolene which is conjugated with glucuronic acid or with sulfate. Dantrolene is also metabolized by nitroreductase to aminodantrolene. The aminodantrolene inhibits the hepatic MFO system. Acetylation of aminodantrolene blocks the inhibitory effects of aminodantrolene on the hepatic MFO system. Intermediates in the nitroreductase pathway form glucuronide and mercapturic acid conjugates. The mercapturic acid conjugation reaction is a detoxification mechanism for an electrophilic metabolite of dantrolene.

Keywords

Male, Mesocricetus, Rats, Inbred Strains, Glutathione, Dantrolene, Acetylcysteine, Mixed Function Oxygenases, Rats, Kinetics, Mice, Cytochrome P-450 Enzyme System, Species Specificity, Cricetinae, Animals, Ethylmorphine, Chemical and Drug Induced Liver Injury, Biotransformation

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