PHA 4107 Lecture Notes - Lecture 2: Drug Metabolism, Glucuronidation, Biotransformation
12 Jul 2018
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Metabolism: goal: to increase size and polarity of compounds (more easily excreted, drugs are mostly metabolized in the liver, also gi tract, kidneys, lungs, placenta, skin, etc, phase i, addition of a reactive group (-oh, -nh2, -sh). Increase therapeutic action of some drugs, e. g. codeine -> morphine: decrease toxicity (usually, occasionally can increase toxicity, ex. conversion of acetaminophen (tylenol) into a hepatotoxic substance. Cytochrom p450: contain a heme (fe) group, absorb light at 450 nm, many cyp: polymorphic distribution of activity. Cyp- polymorphic distribution: a trait that demonstrates a different distribution in >1% of the population, poor metabolizers (pm) have severely reduced or no functional capacity to metabolize substrate medications. Poor metabolizers are at risk for side effects due to toxic drug accumulation and may require lower doses: extensive metabolizers (em) carry. 2 functional genes and have normal enzyme activity.
