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19 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What 7 enzymes are responsible for the majority of drug metabolism? |
CPY:
1A2 2C8, 2C9, 2C19, 2D6, 2E1 3A4 |
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CYP1 Family |
found in liver
drug metabolism, steroid & heme metabolism induced by polycyclic aromatic hydrocarbons, aromatic amines, & nitroamines |
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CYP2 Family
- where found - what metabolized - induced by |
found in liver
drug metabolism induced by ethanol & acetone |
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CYP3 Family
- where found - induced by |
found in liver, GI, kidneys, placenta
induced by glucocorticoids & phenobarb |
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CYP4 Family
- where found - what metabolized |
found in liver & kidney
FFA metabolism |
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CYP7 Family
-where found - what synthesized |
found in liver & brain
synthesis of bile acid, sex hormones |
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Where is the concentration of enzymes the highest?
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upper small intestine
duodenum & jejunum > ileum & colon |
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What are the main inhibitors of 3A4?
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V I K E G
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Verapamil
Itraconazole Ketaconazole Erythromycin, Clarythromycin Grapefruit Juice |
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What are the main inducers of 3A4?
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C R (a) P S
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Carbamazepine
Rifampin Phenytin St. John's Wort |
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What are the main broad spectrum Inducers?
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C R P P
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Carbamazapine
Rifampin Phenytoin Phenobarb |
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What are the main 2D6 Inhibitors?
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a c d q p f r
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amiodarone
chloraquine diphenhydramine quinine paroxetine fluoxetine ritonavir |
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What are the selective 3A4 Inducers?
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F G T O N S
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Felbamate
Griseofuluin Topiramate Oxcarbazapine Nevirapine St. John's Wort |
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What is the selective 1A2 Inducer?
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smoking
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What is the selective 2E1 Inducer?
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alcohol
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What are the UGT inducers? |
LOOC
Lamotrigine Oxcarbazepine Oral Contraceptives |
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What are the four types of transporters? |
1. P-glycoprotein (PgP) 2. Multi-drug resistance (MDR) 3. Organic Anion Transporter (OAT) 4. Organic Cation Transporter (OCT) |
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Why does enzyme induction occur?
What is the time course? |
Occurs due to increase in enzyme activity usually due to increased concentration of enzyme protein.
1-2 weeks for induction, 1-2 weeks for de-induction; dependent on time to reach Css of inducing agent and rate of synthesis/destruction of enzymes |
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Is enzyme induction dose-dependent?
Is enzyme induction additive with multiple inducers? |
Enzyme induction is dose-dependent,
is not additive |
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What are the clinical results of inhibition?
What is the time course for inhibition? |
Inhibition can be associate with increased plasma concentration and pharmacologic response due to decrease in the rate of metabolism of the drug
Onset is usually rapid, w/in 24 hours. Time to max inhibition depends on elimination half life
Inhibition is generally dose-dependent
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