Pharmacology 2060A/B Lecture Notes - Lecture 4: Thiopurine Methyltransferase, Cytochrome P450, Glutathione
15 Feb 2016
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Document Summary
To understand why drug metabolism is important in drug therapy. To appreciate the concept and relevance of first pass metabolism. To understand the importance of genetic polymorphisms in drug metabolizing enzymes to therapeutic drug response. Metabolism is the enzyme mediated alteration of a drug"s structure. Metabolism is also referred to as biotransformation. Drug metabolism is important in humans to protect us from a number of environmental exogenous toxins as well as synthesize essential endogenous molecules. Therapeutic consequences of drug metabolism are summarized below: increase water solubility of drugs to promote their excretion. Active more active: activate prodrugs (prodrugs are inactive until metabolized) Prodrug (inactive) active drug: increase drug toxicity. First order kinetics: in most clinical situations, the concentration of drug is much lower of the body. Notice how the concentration decreases faster when there are higher drug concentrations than at the end when the drug concentrations are low. Notice how there is much more enzyme than there is drug.
