Pharmacology 2060A/B Lecture Notes - Lecture 4: Prodrug, Biotransformation, Active Metabolite

• School: Western University
• Department: Pharmacology
• Course: Pharmacology 2060A/B
• Professor: Andrea Di Sebastiano

Document Summary

4. 1 drug metabolism: metabolism is the enzyme-mediated alteratio(cid:374) of a drug"s stru(cid:272)ture, metabolism is also referred to as biotransformation. Similarly, essential endogenous molecules synthesized by drug metabolizing enzymes are shown: note that even things like vegetables considered to be healthy, would be to(cid:454)i(cid:272) if (cid:449)e did(cid:374)"t ha(cid:448)e e(cid:374)z(cid:455)(cid:373)es to process them! Therapeutic consequences of drug metabolism: drug metabolism can have several different consequences. Therapeutic consequences of drug metabolism are summarized below: 1)increase water solubility of drugs to promote their excretion. In most clinical situations the concentration of drug is much lower than the metabolic capacity of the body. In these situations drug metabolism displays 1st order kinetics. In 1st order kinetics, the concentration of the drug is much lower than the lower metabolic capacity of the body zt. The top panel shows how the plasma concentration changes overtime. Notice how the concentration decreases faster when there are higher drug concentrations than at the end when the drug concentrations are low.