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10 Cards in this Set
- Front
- Back
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What are the 2 most common types of drug metabolism interactions?
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-Enzyme induction
-Enzyme inhibition |
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What is enzyme induction?
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Upregulation of an enzyme amount or activity due to exposure to its substrate drug or an environmental chemical
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What are drugs or environmental chemicals that upregulate an enzyme called?
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Inducing agents
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Which metabolism enzymes are inducible?
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Both Phase I and II
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What is usually the cause of the upregulated enzyme amt or activity?
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Increased transcription
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How does increasing the steady state concentration of an enzyme accelerate metabolism?
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By increasing the Vmax
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Upregulation of which cytochrome P450 will affect the most drug metabolisms? How much?
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Cyp 3A - 50%
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What mechanism of induction will result in slow enzyme induction? Which will result in fast?
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Slow = transcriptional increases
Fast = Translational or protein stabilization |
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How can enzyme induction effect a drug substrate?
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EITHER
-Inactivate a drug -Activate a prodrug |
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Does an inducer have to be a substrate of the enzyme it induces?
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No not necessarily
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