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