Chapter 21. Drug Metabolism

作者: Hugh M. McIlhenny

DOI: 10.1016/S0065-7743(08)61559-6

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摘要: Publisher Summary The influence of the structural alterations on drug disposition, metabolic events that lead to pharmacologically active or toxic substances, advances in novel little studied biotransformations, and species differences metabolism are discussed this chapter. hydroxylation amobarbital breath analysis aminopyrine demethylation is proving be useful tests determine a patient's capacity for hepatic oxidation. increased use hepatocyte preparations demonstrates their utility as models studies. simplicity, sensitivity, specificity radioimmunoassays have led development number practical assays biological fluids. Numerous publications appeared subject biotransformation drugs metabolites reactive intermediates manifest toxicity. Acetylhydrazine isopropylhydrazine, isoniazid, iproniazid initiate hepatotoxicity through covalent binding an electrophilic intermediate. A intermediate involving furan ring furosemide responsible necrosis produced by diuretic agent. Covalent isoproterenol rifampicin macromolecules occur following phenol oxidation adrenochrome quinone, respectively. Methylmercapto replacement chloro substituent antiviral agent acluraci sulfoxidation pyridyl moiety bromazepine involve mercapturic cysteine conjugation. Clonidine metabolized rats dogs cleavage 2,6-dichlorophenylguanidine.

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