Term
| What are the three CYP (P450) families involved in drug (xenobiotic) metabolism? |
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Definition
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Term
| Which P450 enzyme metabolizes the largest percentage of marketed drugs? |
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Definition
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Term
| What will induce the CYP1 family? |
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Definition
Cigarette smoke, polycyclic aromatic hydrocarbons, charred meats, omeprazole
(think burnt) |
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Term
| What will induce the CYP2D subfamily? |
|
Definition
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Term
| What will induce the CYP2A,CYP2B,or CYP2C subfamilies? |
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Definition
| Barbiturates (phenobarbitol), Rifampin |
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Term
| What will induce the CYP2E subfamily? |
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Definition
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Term
| What will induce the CYP3A subfamily? |
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Definition
| Barbiturates, Rifampin, Carbamazepine, St. John’s Wort, Efavirenz |
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Term
| What happens during enzyme induction? |
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Definition
Increased enzymatic activity (metabolism) which leads to:
- Increased transcription
- Increased translation
- Decreased protein degradation
And in the case of our drugs, a decrease in drug concentration and bioavailability. |
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Term
| Which CYPs have polymorphism? |
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Definition
CYP2D6
and also:
CYP2C9
CYP2C19
CYP2A6 |
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Term
| What is the effect of an INHIBITOR on the drug? |
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Definition
| Increases bioavailability |
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Term
| What is the effect of an INDUCER on the drug? |
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Definition
| Decreases bioavailability |
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