Pharmacology 2060A/B Lecture Notes - Lecture 4: Irinotecan, Critical Role, Hydrolysis

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Module 4 pharmacokinetics - metabolism. Therapeutic consequences of drug metabolism. Increase water solubility of drugs to promote their enzyme mediated alteration of a drugs structure. Liver primary site of drug metabolism. Intestine enterocytes that line the gut are able to metabolize drugs. Stomach a site for the metabolism of alcohol: kidney underappreciated as metabolic organ. Intestinal bacteria normal flora. Protection from a number of environmental toxins as well as synthesize essential endogenous molecules. Exogenous toxins wine, cigarettes, coffee, vegetables, red meat. Many consequences: excretion: lipophilic hydrophilic. Inactive drugs: active inactive. Increased drug effectiveness: active more active: activate prodrugs (prodrugs are inactive until metabolized): prodrug (inactive) active drug. Increase drug toxicity: non- toxic toxic. = concentration of drug is much lower than the metabolic capacity of the body. Concentration decreases faster when there are higher drug concentrations than at the end when the drug concentrations are low. Much more enzyme than there is drug, typical of 1st order.

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