Nifedipine Itraconazole

Tailor SA, Gupta AK, Walker SE, et al. Peripheral edema due to nifedipine itraconazole interaction a case report. Arch Dermatol 1996 132 350. 

Nifedipine was one of the first CYP3A4 substrates to be identified (167,168) and has been the subject of a large number of drug-drug interaction studies both in vitro and in vivo. Pharmacokinetic studies with nifedipine clearly identify inhibitors, such as itraconazole (169) and grapefruit juice (170), and inducers, such as the barbiturates (171) and rifampin (172). 

Abacavir Adinazolam 5-Aminosalicylic acid Atorvastatin Avitriptan Bromazepam Bumetanide Celecoxib CGP 43371 Clodronate Cyclosporin Danazol Didanosine Erythromycin Fexofenadine Furosemide Ganciclovir Halofantrine Inidnavir Itraconazole Levofloxacin Methotrexate Nifedipine Pravastatin Rifabutin Stavudine Tacrine... 

Clinically important, potentially hazardous interactions with amlodipine, anisindione, anticoagulants, aprepitant, atorvastatin, barbiturates, benzodiazepines, butabarbital, carbamazepine, chlordiazepoxide, clarithromycin, clonazepam, dorazepate, corticosteroids, cyclosporine, dexamethasone, diazepam, dicumarol, erythromycin, ethotoin, felodipine, flurazepam, fluvastatin, fosphenytoin, isradipine, itraconazole, ketoconazole, lorazepam, lovastatin, mephenytoin, mephobarbital, midazolam, nicardipine, nifedipine, nimodipine, nisoldipine, oxazepam, pentobarbital, phenobarbital, pimozide, pravastatin, primidone, quazepam, rifampin, secobarbital, simvastatin, St John s wort, temazepam, warfarin... 

Clinically important, potentially hazardous interactions with abacavir, atorvastatin, bepridil, bupropion, carbamazepine, clarithromycin, cyclosporine, dexamethasone, digoxin, felodipine, fluticasone propionate, fosamprenavir, itraconazole, ketoconazole, lovastatin, methadone, midazolam, nicardipine, nifedipine, phenobarbital, phenytoin, rifabutin, simvastatin, sirolimus, St John s wort, systemic lidocaine, tacrolimus, tenofovir, trazodone, vinblastine, vincristine, voriconazole, warfarin, zidovudine... 

Clinically important, potentially hazardous interactions with itraconazole, nifedipine, sirolimus... 

Clinically important, potentially hazardous interactions with amiodarone, amprenavir, anisindione, antacids, anticoagulants, aprepitant, atazanavir, atovaquone, beclomethasone, buprenorphine, corticosteroids, cortisone, cyclosporine, cyproterone, dabigatran, dapsone, darunavir, delavirdine, dexamethasone, dicumarol, digoxin, eszopiclone, flunisolide, fosamprenavir, gadoxetate, gestrinone, halothane, imatinib, isoniazid, itraconazole, ketoconazole, lapatinib, lorcainide, methylprednisolone, midazolam, nelfinavir, nifedipine, oral contraceptives, phenylbutazone, prednisone, protease inhibitors, pyrazinamide, ramelteon, ritonavir, saquinavir, solifenacin, sunitinib, tacrolimus, telithromycin, temsirolimus, tipranavir, tolvaptan, trabectedin, triamcinolone, triazolam, voriconazole, warfarin, zaleplon... 

Surface energies of a sample of drugs are as follows (81) ibuprofen, 52 dyne/cm naproxen, 42 dyne/cm nifedipine, 38 dyne/cm hydrocortisone acetate 37 dyne/cm and itraconazole 36 dyne/cm (82). 

CYP3A4 Alfentanil Alprazolam Astern izole Carbamazepine Cisapride Cyclosporine Diltiazem Erythromycin Felodipine Fluconazole Itraconazole Ketoconazole Lidocaine Lova statin Midazolam Nifedipine Quinidine Simvastatin Tacrolimus Terfenadine Verapamil... 

A4 28 34 clarithromycin, codeine, diazepam, erythromycin, indinavir, midazolam, nifedipine, quinidine, terfenadine, verapamil ketoconazole, itraconazole... 

Itraconazole can markedly raise the serum levels of felodipine, which Increases Its adverse effects, In particular ankle and leg oedema. A few case reports suggest that isradipine and nifedipine can interact similarly with itraconazole, and that fluconazole can also interact with nifedipine. Ketoconazole can markedly raise the plasma levels of lercanidipine and nisoldipine. Caution is warranted with all calcium-channel blockers when azole antifungals, particularly itraconazole and ketoconazole, are used. 

The interaction between felodipine and itraconazole would appear to be established and elinieally important. It also seems that isradipine, lercanidipine, nifedipine and nisoldipine ean interaet similarly with fluconazole, itraconazole or ketoconazole and, because they are metabolised by CYP3A4, it is likely that other calcium-channel blockers will behave in the same way. If itraconazole, ketoconazole, or fluconazole is given to a patient on established treatment with any calcium-channel blocker be alert for the need to lower the dosage of the calcium-channel blocker. However, some manufaeturers (e.g. felodipine, lercanidipine ) actually contraindicate concurrent use of itraconazole or ketoconazole, and others (e.g. nisoldipine ) additionally contraindicate fluconazole. In the US the guidance differs slightly and only caution is considered necessary with felodipine. The manufacturers of nimodipine predict that fluconazole, itraconazole and ketoconazole will substantially raise nimodipine levels. They say that concurrent use should be avoided, but, if this is not possible then the patient s blood pressure should be carefully monitored."... 

Fig. 5.1 MBP classification system (MCS). Circle stands for Easy drug and triangle stemds for Mfficult drug. DIP dipyridamole, DNZ danazol, FFB fenofibrate, GRI grisoeMvin, IDM indomethacin, 177 itraconazole, AIPX naproxen, AW nifedipine, Al/Lnilvadipine, ATP nitrendipine, PHE phenytoin, PMZ pimozide, PTX paclitaxel, KTZ ketoconazole. A-L, Roche in-house drugs. MBP preparation condition polymer HPMCAS pH 2 drug/polymer ratio = 3/7...

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