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FDA definitions of inducers/inhibitors levels: Strong
- Inducer: 80+% decrease in AUC
- Inhibitor: 5+ fold increase in AUC
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FDA definitions of inducers/inhibitors levels: Moderate
- Inducer: 50-80% decrease in AUC
- Inhibitor: 2 - <5 fold increase in AUC
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FDA definitions of inducers/inhibitors levels: Weak
- Inducer: 20-50% decrease in AUC
- Inhibitor: 1.25 - <2 fold increase in AUC
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Inducers = PS PORCS
- Phenytoin
- Smoking
- Phenobarbital and primidone
- Oxcarbazepine
- Rifampin, rifabutin, rifapentine
- Carbamazepine
- St. John's wort
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Inhibitors = G ♡ PACMAN
- Grapefruit
- Protease inhibitors - ritonavir and others
- Azole antifungals - fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole, isavuconazonium
- Cyclospoine, cobicistat, cimetadine
- Macrolides - clarithromycin, erythromycin, NOT azithromycin
- Amiodarone and dronedarone
- NonDHP CCB - diltiazem, verapamil
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Substrates: 1A2
alosetron, aprepitant, clozapine, cyclobenzaprine, duloxetine, ethinyl estradiol, fluvoxamine, methadone, mirtazipine, olanzapine, ondansetron, pimozide, propranolol, rasagiline, ropinirole, theophylline, R-warfarin
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Substrates: 2C8
amiodarone, dasabuvir, pioglitazone, repaglinide, rosiglitazone
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Substrates: 2C9
alosetron, carvedilol, celecoxib, diazepam, diclofenac, fluvastatin, glyburide, glipizide, glimepiride, meloxicam, netaglinide, phenytoin, ramelteon, S-warfarin, tamoxifen, zolpidem
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Substrates: 2C19
clopidogrel, phenytoin, thioridazine, voriconazole
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Substrates: 2D6
Analgesics, antipsychotics/antidepressants
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Substrates: 3A4
Analgesics, anticoagulants, antidiabetic drugs, antiplatelets (not clopidogrel), cardiovascular drug (incdluing amiodarone), immunosuppressants, statins (atorv, lova, simva), key HIV (atazanavir, efavirenz, ritonavir, tipranavir), PDE-5 inhibitors, alfuzosin, aprepitant again, aripiprazole, benzos, buspirone, carbamazepine, citalopram, clarithromycin, colchicine, escitalopram, ethinyl estradiol, felbamate, haloperidol, ketoconazole, levonorgestrel, mirtazapine, ondansetron again, dutasteride, quetiapine, trazodone, venlafaxine, zolpidem
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Inducers: 3A4
carbamazepine, phenytoin, rifampin, smoking, St. Johns wort
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Inhibitors: 3A4
anti-infectives, CV, those key HIV, some more HIV, others (aprepitant, grapefruit juice, sertraline)
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PGP substrates
DOACs, CV (carvedilol, digoxin, ranolazine), immunosuppressants, HCV drugs, colchicine, posaconazole
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PGP inhibitors
anti-infectives, CV drugs, HIV drugs, HCV drugs, ticagrelor
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