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General Drug Metabolism-Exam II review

General Drug Metabolism-Exam II review - reversing...

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General Drug Metabolism : major functional groups that undergo phase I and II metabolism and enzymes involved modulating factors---host, environmental • Consequences: - inactivation excretion - bioactivation pharmacologically active drugs (enzymes involved): cyclophosphamide, codeine, morphine, ironotecan, minoxidil, etc. First pass effects: - causes - implications for drug bioavailability/plasma levels/duration and intensity of pharmacological effects • Enzyme induction/inhibition and sample therapeutic/adverse responses implications: - ethanol/rifampin/St. John’s wort/tobacco smoke smoke; grape fruit juice) - representative mechanisms of enzyme induction (including receptors) and enzyme repression (negative gene regulators, gene methylation, gene demethylation, etc) P-glycoprotein , MRP2, OATs, OCTs: representative functions
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Unformatted text preview: - reversing agents/chemosensitizers SNPs : definition, consequences and pharmacotherapeutic relevance? Polymorphisms : ethnic distribution (Caucasians vs Asians vs Blacks) of CYP2D6 (debrisoquine), CYP2C9 (warfarin), CYP2C19 (omeprazole), ADH (ethanol) and ALDH (acetaldehyde) poor/rapid/ultra-rapid metabolizers; primaquine sensitivity Glutathione conjugations -conjugate processing → mercapturic acids → β-lyase → ? Glucuronidation - congenital deficiency states and forms of hyperbilirubinemia -β-glucuronidase and drug bioavailability Acetylation -isoniazid (peripheral neuropathy), aromatic amines (kidney toxicity), lupus-inducing therapeutic drugs Methylation - thiopurine/polymorphism Aspirin metabolism Acetaminophen - mechanisms and modulators of hepatotoxicity...
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General Drug Metabolism-Exam II review - reversing...

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