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23 Cards in this Set
- Front
- Back
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Probe(s) for CYP1A2
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Caffeine
Induced by smoking, charbroiled foods |
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Probe(s) for CYP2C9
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(S) warfarin
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Probe(s) for CYP2C19
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Omeprazole
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Probe(s) for CYP2D6
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Debrisoquine
Dextromethorphan Inhibitor: quinidine Codeine and Sparteine also metabolized by CYP2D6 |
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Probe(s) for CYP2E1
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Chloroxazone
St. John's Wart and Rifampin are inducers |
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Probe(s) for CYP3A4
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Erythromycin
Midazolam Phenytoin and refampin are inducers |
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Drug X is metabolized from an inactive prodrug to the active X form by an enzyme. How will the D-R curve of Drug X shift if an inducer of the enzyme is given?
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Left
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Drug X is metabolized from an inactive prodrug to the active X form by an enzyme. How will the D-R curve of Drug X shift if an inhibitor of the enzyme is given?
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Right
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Drug X is an active parent compound that is metabolized to inactive metabolites by an enzyme. How will the D-R curve of Drug X shift if an inducer of the enzyme is given?
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Right
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Drug X is an active parent compound that is metabolized to inactive metabolites by an enzyme. How will the D-R curve of Drug X shift if an inhibitor of the enzyme is given?
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Left
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Ethanol, acetaminophen, and chlorzoxazone are substrates for which CYP isozyme?
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CYPE2A
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What changes take place in the elderly relative to creatinine?
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decreased creatinine clearance
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What areas of the body metabolize orally administered drugs vs. IV administered drugs?
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Oral - liver/small intestine
IV - liver only |
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Chronic alcohol and tobacco use have what effect on CYP450?
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Induction of CYP2E1
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What CYP450 metabolizes APAP to toxic intermediate?
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CYP2E1
Induced by alcohol |
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Characteristics of isozyme CYP1A2
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Metabolizes about 3% of drugs, including caffeine, R-warfarin.
Activity can be induced by smoking, chronic alcohol use, charbroiled foods, rifampin. Activity can be inhibited by omeprazole, fluvoxamine |
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Characteristics of isozyme CYP2C9
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Metabolizes NSAIDS, S-warfarin, phenytoin, tolbutamide.
Induced by rifampin, carbazepine, ethanol. Inhibited by Amiodarone, fluvastatin, fluconazole. Altered genes: decreased activity in 1-3% whites and 2% blacks |
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Characteristics of isozyme CYP2C19
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Metabolizes benzodiazepines, tricyclic antidepressants, omeprazole, citalopram.
Induced by rifampin. Inhibited by fluvoxamine, fluoxetine, and ticlopidine. Altered genes: decreased or lack of activity in 2-5% whites, 15-20% asians |
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Characteristics of isozyme CYP2D6
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2-6% of total liver CYP450
Metabolizes almost 25% of drugs NO INDUCERS Inhibited by quinidine and fluoxetine Genetic modifications: decreased in 5-10% whites, 1-3% chinese/black |
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Characteristics of isozyme CYP2E1
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Metabolizes ~1% of drugs
Activates and inactivates toxins Metabolizes mainly small organic molecules (e.g. ethanol, carbon tetrachloride) Numerous inducers/inhibitors. Inhibitors block formation of toxic intermediates, i.e. APAP |
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Characteristics of isozyme CYP3A4
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Major form in liver and intestines
Metabolizes ~50% of drugs Most first-pass metabolism Responsible for most drug interactions Induced by glucocorticoids, rifampin, carbamazepine, phenobarbitol, phenytoin Inhibited by macrolide antibiotics, azole antifungals, grapefruit juice |
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What are major CYP3A4 substrates?
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Amiodarone
Amlodipine/felodipine (CCB) Amprenavir/fosamprenavir Aprepitant Aripiprazole Atazanavir Benzphetamine Bisoprolol Bortezomib Bosentan Bromocriptine Budesonide Buprenorphine Buspirone Busulfan Carbamazepine Chloroquine Chlorpheniramine Cilostazole Citalopram/Escitalopram Clarithromycin Cocaine Colchicine Conivaptan Cyclophosphamide (activated) Cyclosporine Dantrolene Dapsone Delavirdine (NNRTI) Diltiazem (CCB) Disopyramide Doxetaxel Dexepin Doxycycline Doxorubicin Efavirenz (NNRTI) Eltriptan Enalapril Eplerenone Ergot derivatives Erythromycin Estrogens (contraceptives) Ethosuximide Etoposide Exemestane Felbamate Fentanyl Flutamide Fluticasone Gefitinib Haloperidol Ifosfamide Imatinib Indinavir (PI) Irinotecan Isosorbide derivatives Isradipine (CCB) Itraconazole Ketamine Ketoconazole Lansoprazole Lidocaine Losartan Mefloqine Methadone Miconazole Miglustat Mirtazapine Modafinil Montelukast Moricizine Nateglinide (DM) Nefazodone Nelfinavir (PI) Nevirapine (NNRTI) Nicardipine (CCB) Nifedipine (CCB) Nimodipine (CCB) Nisoldipiine (CCB) Odansetron Paclitaxel Pergolide Pimozide Primaquine (antiprotazoal) Quetiapine Quinidine Rabeprazole (PPI - with 2C19, which metabolizes all others) Ranolazine Repaglinide Rifabutin Ritonavir (PI) Salmeterol Saquinavir (PI) Sildenafil/Vardenafil (Levitra/Viagra) Sirolimus Sunitinib Tacrolimus Tamoxifen Tamsulosin Telithromycin Tetracycline Theophylline Tiagabine (anticonvulsant) Ticlopidine (platelet inhibitor) Trazodone Trimethoprim Trimipramine (TCA) Troleandomycin Venlafaxine Verapamil (CCB) Vinblastine/vincristine Vinorelbine Zolpidem Zonisamide Zopiclone Statins *except* pravastatin All benzos *except* lorazepam, lormetzepam, oxazepam, metaclazepam, nitrazepam, pinazepam, and temazepam. |
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What are common CYP450 3A4 inhibitors?
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Amiodarone
Clarithromycin Cyclosporine Danazol Delavirdine Diltiazem Erythromycin Fluoxetine Fluvoxamine Grapefruit juice Indinavir Itravonazole Ketovonazole Miconazole Nefazodone Nelfinavir Nicardipine Nifedipine Pimozide Propoxyphene Quinidine Ritonavir Saquinavir Sildenafil Tacrolimus Tamoxifen Testosterone Troleandomycin Verapamil Zafirlukast |
