Fluconazole Cyclosporine

Lopez-Gil JA. Fluconazole-cyclosporine interaction a dose-dependent effect Ann Pharmacother 1993 27(4) 427-30. 

Drugs that affect NSAIDs include the following Bisphosphonates, cholestyramine, cimetidine, colestipol, cyclosporine, diflunisal, DMSO, fluconazole, ketoconazole, phenobarbital, phenylbutazone, probenecid, rifampin, ritonavir, salicylates, sucralfate. 

Drugs that may affect fluconazole include cimetidine, hydrochlorothiazide, and rifampin. Drugs that may be affected by fluconazole include alfentanil, benzodiazepines, buspirone, carbamazepine, cisapride, oral contraceptives, corticosteroids, cyclosporine, haloperidol, HMG-CoA reductase inhibitors, losartan, nisoldipine, phenytoin, protease inhibitors, rifabutin, sirolimus, sulfonylureas, tacrolimus, theophylline, tolterodine, tricyclic antidepressants, vinca alkaloids, warfarin, zidovudine, and zolpidem. 

Drugs that may increase sirolimus blood concentrations include the following Nicardipine, verapamil, clotrimazole, fluconazole, itraconazole, clarithromycin, erythromycin, troleandomycin, cisapride, metoclopramide, bromocriptine, cimetidine, danazol, HIV-protease inhibitors, cyclosporine, diltiazem, azole antifungals. 

Drugs that may affect cyclosporine include allopurinol, amiodarone, androgens (eg, danazol, methyltestosterone), anticonvulsants (eg, carbamazepine, phenobarbital, phenytoin), azole antifungals (eg, fluconazole, ketoconazole), beta-blockers, bosentan, bromocriptine, calcium channel blockers, colchicine, oral contraceptives, corticosteroids, fluoroquinolones (eg, ciprofloxacin), foscarnet, HMG-CoA reductase inhibitors, imipenem-cilastatin, macrolide antibiotics, methotrexate, metoclopramide, nafcillin, nefazodone, orlistat, potassium-sparing diuretics, probucol, rifamycins (rifampin, rifabutin), serotonin reuptake inhibitors (SSRIs eg, fluoxetine, sertraline),... 

Drugs that may inhibit cytochrome P450 metabolism of other drugs include amiodarone, androgens, atazanavir, chloramphenicol, cimetidine, ciprofloxacin, clarithromycin, cyclosporine, delavirdine, diltiazem, diphenhydramine, disulfiram, enoxacin, erythromycin, fluconazole, fluoxetine, fluvoxamine, furanocoumarins (substances in grapefruit juice), indinavir, isoniazid, itraconazole, ketoconazole, metronidazole, mexile-tine, miconazole, nefazodone, omeprazole, paroxetine, propoxyphene, quinidine, ritonavir, sulfamethizole, verapamil, voriconazole, zafirlukast, and zileuton. 

Sirolimus is metabolized by CYP2A4 and is a substrate of the P-glycoprotein drug efflux pump drugs like voriconazole, itraconazole, fluconazole and erythromycin increase its blood concentration. Conversely, the inducers of CYP3A4 will decrease blood levels of sirolimus. Cyclosporine increases the bioavailability of sirolimus, possibly due to P-GP inhibition and competition for CYP3A4. The bioavailability is more than 30-40% when the two drugs are administered 4 h apart and is more than... 

Fluconazole Fluconazole may increase the plasma concentration of phenytoin, sulfonylurea (hypoglycemic), cyclosporin, zidovudine, cisapride, and terfenadine. Coadministration of fluconazole with rifampicin results in the reduced plasma concentration of fluconazole. Griseofulvin may reduce the plasma concentration of salicylates, coumarin, anticoagulants, and oral contraceptives. 

Osowski CL, Dix SP, Lin LS, Mullins RE, Geller RB, Wingard JR. Evaluation of the drug interaction between intravenous high-dose fluconazole and cyclosporine or... 

Sud K, Singh B, Krishna VS, Thennarasu K, Kohli HS, Jha V, Gupta KL, Sakhuja V. Unpredictable cyclosporin-fluconazole interaction in renal transplant recipients. Nephrol Dial Transplant 1999 14(7) 1698-703. 

Clinically important, potentially hazardous interactions with amiodarone, anabolic steroids, antithyroid agents, barbiturates, bivalirudin, cimetidine, clofibrate, clopidogrel, cyclosporine, delavirdine, dextrothyroxine, disulfiram, fluconazole, glutethimide, imatinib, itraconazole, ketoconazole, metronidazole, miconazole, penicillins, phenylbutazones, piperacillin, quinidine, quinine, rifabutin, rifampin, rifapentine, rofecoxib, salicylates, sulfinpyrazone, sulfonamides, testosterone, thyroid, zileuton... 

Clinically important, potentially hazardous interactions with alfentanil, aminophylline, amisulpride, amoxicillin, ampicillin, anticonvulsants, astemizole, atorvastatin, benzodiazepines, bromocriptine, buprenorphine, bupropion, carbamazepine, cilostazol, ciprofloxacin, cisapride, clindamycin, colchicine, cyclosporine, dasatinib, digoxin, dihydroergotamine, diltiazem, disopyramide, enoxacin, eplerenone, ergotamine, eszopiclone, everolimus, fluconazole, fluoxetine, fluvastatin, gatifloxacin, HMG-CoA reductase inhibitors, imatinib, itraconazole, ketoconazole, lomefloxacin, lorazepam, lovastatin, methadone, methylprednisolone, methysergide, midazolam, mizolastine, moxifloxacin, nitrazepam, norfloxacin, ofloxacin, paroxetine, pimozide, pravastatin, quinolones, ranolazine, repaglinide, rupatadine, sertraline, sildenafil, simvastatin, sparfloxacin, sulpiride, tacrolimus, terfenadine, triazolam, troleandomycin, vardenafil, verapamil, vinblastine, warfarin, zaleplon, zolpidem, zuclopenthixol... 

Clinically important, potentially hazardous interactions with amprenavir, aprepitant, bedomethasone, buprenorphine, calcium, chloramphenicol, cimetidine, dobazam, clorazepate, cyclosporine, cyproterone, darunavir, dasatinib, delavirdine, dexamethasone, diazoxide, disulfiram, dopamine, fesoterodine, fluconazole, flunisolide, fluoxetine, fosamprenavir, ginkgo biloba, hydrocortisone, imatinib, indinavir, influenza vaccines, isoniazid, isradipine, itraconazole, lacosamide, lapatinib, lopinavir, meperidine, methylprednisolone, midazolam, mivacurium, nelfinavir, nilotinib, nilutamide, phenylbutazone, piracetam, posaconazole, prednisolone, prednisone, primrose, ritonavir, rivaroxaban, sage, saquinavir, solifenacin, St John s wort, sucralfate, telithromycin, temsirolimus, teniposide, ticlopidine, tizanidine, tolvaptan, triamcinolone, uracil/tegafur, vigabatrin... 

Clinically important, potentially hazardous interactions with alcohol, aprepitant, clarithromycin, cyclosporine, fluconazole, ketoconazole, phenobarbital, rifampin, ritonavir, St John s wort, verapamil... 

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

The interaction between ketoconazole and cyclosporine has been exploited in order to reduce drug costs associated with administration of cyclosporine following organ transplantation. Relative to ketoconazole and itraconazole, fluconazole appears to be intermediate in its ability to inhibit human cytochromes P450. The magnitude of fluconazole-induced inhibition of cyclosporine metabolism appears, however, to depend on the dosage of fluconazole. 

Noninterfering acetaminophen, N-acetylprocainamide, amikacin, amitriptyline, amlodi-pine, carbamazepine, cefotaxime, ceftazidime, chloramphenicol, ciprofloxacin, cisapride, clindamycin, clonidine, codeine, cyclosporine, digoxin, diphenhydramine, disopyramide, ethosuximide, fluconazole, gentamicin, gentamicin, heparin, labetalol, levothyroxine, li-docaine, lithium, methotrexate, metronidazole, minoxidil, nafcillin, nifedipine, phenobar-bital, phenobarbital, phenytoin, phenytoin, primidone, procainamide, propranolol, quini-dine, ranitidine, salicylic acid, theophylline, tobramycin, tobramycin, valproic acid, warfarin... 

Fluconazole inhibits CYP3A4 and CYP2C9 and thus significantly increases plasma concentrations of amprenavir, cisapride, cyclosporine, phenytoin, sulfonylureas, tacrolimus, theophylline, telithromycin, and warfarin. Patients receiving >400 mg daily or azotemic patients may experience additional drug interactions. Rifampin decreases the fluconazole AUC by -25%. 

---