Pharmacology 2060A/B Lecture Notes - Lecture 4: Prodrug, Active Metabolite, Biotransformation
20 Nov 2017
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Document Summary
Endogenous molecules synthesized by drug metabolizing enzymes are shown. Not simple and varies between drugs: drug metabolism can have several different consequences, therapeutic consequences of drug metabolism are summarized below, therefore metabolism increases water solubility of drugs to promote their excretion. Most drugs are lipophilic (fat soluble) and if not metabolized they would not eliminated from the body. This is the most important consequence of drug metabolism. Lipophilic hydrophilic: can take active drug with pharmological activity inactive the drug so that the (cid:373)eta(cid:271)olite does(cid:374)"t ha(cid:448)e a(cid:272)ti(cid:448)it(cid:455) Active inactive: can also make drugs more active increasing drug effectiveness. Example morphine, a narcotic analgesic used to relieve pain: activate prodrugs (prodrugs are inactive until metabolized in body to an active metabolite) Prodrug (inactive) active drug: less favorable can increase drug toxicity by metabolizing a non toxic drug into a metabolite that exhibits toxicity.
