Pharmacology 2060A/B Lecture Notes - Lecture 4: Cytochrome P450, Drug Metabolism, Prodrug

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Objectives: why drug metabolism is important to drug therapy, important sites of drug metabolism, concept and relevance of first pass metabolism, importance of genetic polymorphisms in drug metabolism enzymes to therapeutic drug response. Metabolism is also referred to as biotransformation. Drug metabolism is important in humans to protect us from a number of environmental toxins as well as synthesize essential endogenous molecules. Exogenous toxins (dm protects from) alcohol, red meat, cigarettes, coffee, drugs, vegetables. Endogenous (essential molecules) vitamin d synthesis, bile acid synthesis, Note that even things like vegetables considered to be healthy would by toxic if we cholesterol metabolism, steroid hormones, bilirubin didn"t have enzymes to process them. Drug metabolism can have several different consequences. When the concentration of drug is much lower than the metabolic capacity of the body. Drug metabolism is directly proportional to the concentration of free drug. Constant fraction of drug is metabolized per unit time.

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