Problemset3 TA John

Problemset3 TA John - Bimm118 Worksheet #3 (REVISED) TA:...

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Bimm118 Worksheet #3 (REVISED) TA: John Diep 1. What generally happens to a drug in Phase I reactions? Drug is usually converted into a more hydrophilic metabolite by adding or unmasking functional groups. 2. List some examples of Cytochrome P450 enzyme inducers and inhibitors. Barbiturates – induces CYP2B Ethanol – induces CYP2E Cigarette smoke/Charred foods – induces CYP1 Grapefruit juice – inhibits CYP3A4 Ketoconazole (antifungal) – inhibits CYP3A4 3. Explain the mechanism behind the “cheese reaction”. Tyramine (in old cheese) is structurally similar to norepinephrine and is metabolized by peripheral MAO (monoamine oxidase). 1. MAOi (monoamine oxidase inhibitor) causes an accumulation of tyramine and increased absorption from the GI into the blood 2. High levels of tyramine will displace norepinephrine (NE) from storage vesicles 3. Displaced NE will trigger a sympathetic response and cause a hypertensive crisis Note: MAOi also inhibits the metabolism of the displaced NE 4. What are the two major Phase II conjugation reactions? Which reaction occurs at high substrate concentration? Glucuronidation and Sulfation. Predominantly glucuronidation at high substrate concentrations. 5. Name the functional groups that are susceptible to the addition of glucuronic acid.
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Problemset3 TA John - Bimm118 Worksheet #3 (REVISED) TA:...

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