Ketoconazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Ketoconazole interacts with 14-¥á demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the inhibition of endogenous respiration, interaction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone.
Pharmacology
Ketoconazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.
Ketoconazole¿¡ ´ëÇÑ Toxicity Á¤º¸ Hepatotoxicity, LD50=86 mg/kg (orally in rat)
Drug Interactions
Ketoconazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alfentanil The imidazole increases the effect and toxicity of alfentanilAlprazolam The imidazole increases the effect of the benzodiazepineAmitriptyline The imidazole increases the effect and toxicity of the tricyclicAnisindione The imidazole increases the effect of the anticoagulantAripiprazole The imidazole increases the effect of aripiprazoleBosentan The imidazole increases the effect and toxicity of bosentanBudesonide The imidazole increases levels/effect of budesonideCarbamazepine The imidazole increases the effect of carbamazepineChlordiazepoxide The imidazole increases the effect of the benzodiazepineCilostazol The imidazole increases the effect of cilostazolCinacalcet The imidazole increases the effect and toxicity of cinacalcetClonazepam The imidazole increases the effect of the benzodiazepineClorazepate The imidazole increases the effect of the benzodiazepineCyclosporine The imidazole increases the effect of immunosuppressantDiazepam The imidazole increases the effect of the benzodiazepineDicumarol The imidazole increases the effect of the anticoagulantAcenocoumarol The imidazole increases the effect of the anticoagulantWarfarin The imidazole increases the effect of the anticoagulantEplerenone The imidazole increases the effect and toxicity of eplerenoneEstazolam The imidazole increases the effect of the benzodiazepineEverolimus The imidazole increases everolimus levels/toxicityFentanyl The imidazole increases levels/toxicity of fentanylFlurazepam The imidazole increases the effect of the benzodiazepineHalazepam The imidazole increases the effect of the benzodiazepineHaloperidol The imidazole increases the effect and toxicity of haloperidolImatinib The imidazole increases the levels of imatinibImipramine The imidazole increases the effect and toxicity of the tricyclicMethylprednisolone The imidazole increases the effect and toxicity of the corticosteroidMidazolam The imidazole increases the effect of the benzodiazepineNortriptyline The imidazole increases the effect and toxicity of the tricyclicPrednisolone The imidazole increases the effect and toxicity of the corticosteroidPrednisone The imidazole increases the effect and toxicity of the corticosteroidQuazepam The imidazole increases the effect of the benzodiazepineQuinidine The imidazole increases the effect and toxicity of quinidineQuinidine barbiturate The imidazole increases the effect and toxicity of quinidineRamelteon The imidazole increases the levels/toxicity of ramelteonRitonavir The imidazole increases the effect and toxicity of ritonavirSaquinavir The imidazole increases the effect and toxicity of saquinavirSildenafil The imidazole increases the effect and toxicity of sildenafilSirolimus The imidazole increases the effect and toxicity of sirolimusTacrolimus The imidazole increases the effect of immunosuppressantTadalafil The imidazole increases tadalafil levelsTolterodine The imidazole increases the effect and toxicity of tolterodineTriazolam The imidazole increases the effect of the benzodiazepineValdecoxib The imidazole increases the effect and toxicity of valdecoxibVardenafil The imidazole increases the effect and toxicity of vardenafilVinblastine The imidazole increases the effect and toxicity of vinblastineVincristine The imidazole increases the effect and toxicity of the antineoplasicZiprasidone Ketoconazole increases the effect and toxicity of ziprasidoneTolbutamide Ketoconazole increases the effect and toxicity of tolbutamideSibutramine Ketoconazole increases the levels and toxicity of sibutramineRosiglitazone Ketoconazole increases the effect of rosiglitazoneQuetiapine Ketoconazole increases the effect/toxicity of quetiapinePioglitazone Ketoconazole increases the effect of pioglitazoneGalantamine Ketoconazole increases the effect and toxicity of galantamineIndinavir Ketoconazole increases the effect of indinavirIrinotecan Ketoconazole increases the effect and toxicity of irinotecanTrazodone This strong CYP3A4 inhibitor increases the effect and toxicity of trazodoneSunitinib Possible increase in sunitinib levelsSucralfate Sucralfate decreases the absorption of the imidazoleSolifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismAlfuzosin The antifungal increases the effect of alfuzosinAlmotriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanAprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitantCiclesonide Increased effects/toxicity of ciclesonideDarifenacin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolismDocetaxel The agent increases the serum levels and toxicity of docetaxelDofetilide This strong CYP3A4 inhibitor increases the effect and toxicity of dofetilideEletriptan This potent CYP3A4 inhibitor increases the effect and toxicity of the triptanErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibGefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinibIsoniazid Isoniazid decreases the effect of ketoconazoleNevirapine Nevirapine decreases the effect of ketoconazoleRifampin Rifampin dereases the effect of the imidazoleRanolazine Increased levels of ranolazine - risk of toxicityTerfenadine Increased risk of cardiotoxicity and arrhythmiasPimozide Increased risk of cardiotoxicity and arrhythmiasCisapride Increased risk of cardiotoxicity and arrhythmiasAstemizole Increased risk of cardiotoxicity and arrhythmiasAtorvastatin Increased risk of myopathy/rhabdomyolysisCerivastatin Increased risk of myopathy/rhabdomyolysisLovastatin Increased risk of myopathy/rhabdomyolysisSimvastatin Increased risk of myopathy/rhabdomyolysisAluminium The antacid decreases the effect of the imidazoleBismuth The antacid decreases the effect of the imidazoleMagnesium The antacid decreases the effect of the imidazoleMagnesium oxide The antacid decreases the effect of the imidazoleCalcium The antacid decreases the effect of the imidazoleBuspirone The macrolide increases the effect and toxicity of buspironeCimetidine The anti-H2 decreases the absorption of the imidazoleFamotidine The anti-H2 decreases the absorption of the imidazoleNizatidine The anti-H2 decreases the absorption of the imidazoleRanitidine The anti-H2 decreases the absorption of the imidazoleDihydroergotamine Possible ergotism and sever ischemia with this combinationErgotamine Possible ergotism and sever ischemia with this combinationEsomeprazole The proton pump inhibitor decreases the absorption of imidazoleLansoprazole The proton pump inhibitor decreases the absorption of imidazoleOmeprazole The proton pump inhibitor decreases the absorption of imidazolePantoprazole The proton pump inhibitor decreases the absorption of imidazoleRabeprazole The proton pump inhibitor decreases the absorption of imidazoleEthinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptiveMestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Ketoconazole¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.Take with food.
Ketoconazole¿¡ ´ëÇÑ Description Á¤º¸ Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. [PubChem]