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22 Cards in this Set
- Front
- Back
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What do the different letters/numbers in CYP 3A4 represent?
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C - gene for cytrochrome 3 - family A - subfamily 4 - specific enzyme
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What type of metabolism reaction are CYP P450 responsible for?
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Phase 1 reactions (oxidation, reduction, hydrolysis)
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Where are CYP P450 enzyme systems located?
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- primarily located in the membranes of the smooth endoplastic reticulum - located in the liver, small intestines, brain
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What type of metabolism do elderly patients lose?
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Phase I
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What type of reactions are Phase II reactions?
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synthesis and oxidation
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What is induction?
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- a substance that stimulates the synthesis of the enzyme and the metabolic capacity of that substance is increased - inducing the metabolism of a drug increases the rate of elimination of that drug
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What is inhibition?
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- competitive binding at an enzyme site - will slow metabolism of a drug (increases drug level in the body because drug is not being eliminated)
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Which CYP-450 isoenzyme is most abundant?
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CYP 3A4
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Name some drugs that are metabolized by 3A4
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1. macrolides - clarithromycin 2. Fluoxetine (Prozac) 3. Indanivir - protease inhibitor in HIV 4. Itraconazole (Sporanox) 5. Ketonazole (or Nizoral)- antifungal 6. Ritonavir - protease inhibitor
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Name some CYP-450 1A2 inhibitors
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- Cimetidine (Tagemet) - quinolones (Levaquin)
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Name some inhibitors of CYP 450 2C10
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- Fluoxetine (Prozac) - Ketocanazole - Lansoprazole
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Name some inhibitors of CYP 450 2C9
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- Amiodarone (Cordarone) - Fluconazole (Diflucan) - Isoniazid (INH)
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Name some inhibitors of the CYP450 2D6
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- Amiodarone - Cimetidine (Tagmet) - Clomipramine (Anafranil): a tricyclic antidepressant - Paroxetine (Paxil): SSRI - Ritonavir (a very potent inhibitor used to keep other antiviral drugs in the system)
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Name some CYP450 3A4 inhibitors
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- protease inhibitors - Amiodarone (Cordarone) - Clarithromycin - Erythromycin
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What dosage adjustment need to be made if a patient is given Amiodarone and Coumadin?
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- decrease dosage of Coumadin (Warfarin) by 25% because Amiodarone is an inhibitor of Coumadin
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What is the safest macrolide to use to avoid drug interactions?
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Azithromycin (Zithromax)
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Name an inducer of CYP 450 1A2
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tobacco
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Name an inducer of CYP 450 2C9
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Rifampin (potent inducer) - a antimicrobial agent
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Name some inducers of CYP-450 2E1
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- ethanol (acute) - isoniazid (chronic)
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Name an inducer of CYP-450 3A4
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- Carbamazipine - Barbituates (phenobarbital) - Rifampin
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What is the pneumonic for remembering inducers?
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Barbie's Car Goes Real F(Ph)ast Barbituates Carbamazepine Griseofulvin Rifampin Phenytoin
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What is pneumonic for remembering inhibitors?
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Ken's Car is Equally F(Ph)ast Ketocanazole Carbamazepine Ethambutol Phenytoin
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