Pharmacology 2060A/B Lecture Notes - Lecture 4: Biotransformation, Bilirubin, Cholesterol
22 Feb 2019
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Notice how there is much more enzyme than there is drug. This is typical in drugs that display zero order metabolism: first pass metabolism, po drugs may undergo significant metabolism prior to entering the systemic circulation. After drug becomes more water soluble, it can be eliminated, and excreted into urine. Drug + acetyl coa acetylated drug + coa: thiopurine methyltransferase (tpmt, are cytosolic phase ii drug metabolizing enzymes, catalyze the transfer of a methyl group from s- adenosylmethionine to a drug, subject to genetic polymorphisms. Although rare, these polymorphisms have dramatic effect on drug safety (more later) Extensive metabolizer (em), intermediate metabolizer (im) and poor metabolizer (pm: extensive metabolizers are considered have normal enzymatic activity, intermediate metabolizers have reduced metabolic activity whereas poor metabolizers have almost no metabolic activity, ultra-rapid metabolizers have significantly increased. Cyp2d6 activity: ultra-rapid metabolizers possess multiple copies of the.
