CONAZ CONAZ KETOCONAZOLE TEZOLE TEZOLE MYCOLOCK KITCON MERIZON MERIZON KETOS KETOS KETOPIKE SPIKE SPIKE SPIKE SPIKE NIZORAL SCALP GEL NIZORAL NIZORAL KUTIC KETGAL KETO KENZOL KETONAZ KETOR KETOWIN KARE NIZODERM KETRY SOSTATIN SKINCARE KETOCON KETOCON KETOVAL KETOVAL KETACON KETACON KEMAQ MYCOBAN KONAZOLE KONAZOLE MYXOLE CREAM KANAGEN FUNGINIL TOCOZOLE DANFREE EXTINA KETOOZ KURIC MYXOLE LOTION MYXOLE LOTION ALFUNG KETAGEN KETAGEN KETOZOLE KETONE KETOREX

Dose: 200 to 400 mg
Single Dose: 300 (300)
Frequency: 24 hourly
Route: PO
Instructions:

Dose: 3 mg/kg
Single Dose: 3 (3)
Frequency: 24 hourly
Route: Oral
Instructions: -

. It is of Synthetic origin and belongs to Imidazole. It belongs to Antifungals pharmacological group.The Molecular Weight of Ketoconazole is 531.40. Its pKa is 6.5 , 2.94.

Ketoconazole is contraindicated in conditions like Hypersensitivity.

The severe or irreversible adverse effects of Ketoconazole, which give rise to further complications include Thrombocytopenia, Impotence, Papilloedema, Androgen suppression, Oligospermia, Gynecomastia.Ketoconazole produces potentially life-threatening effects which include Hepatitis, Anaphylaxis. which are responsible for the discontinuation of Ketoconazole therapy.The symptomatic adverse reactions produced by Ketoconazole are more or less tolerable and if they become severe, they can be treated symptomatically, these include Sleepiness, Dizziness, Headache, Nausea, Vomiting, Alopecia, Diarrhea, Abdominal pain, Urticaria, Pruritus, Irritation, Itching, Somnolence, Dermatitis, Photophobia, Paresthesias, Local burning sensation, Alopecia, dizziness.

Ketoconazole is primarily indicated in conditions like Candidal chronic paronychia, Chronic vaginal candidosis, Cutaneous candidiasis, Fungal prophylaxis, Histoplasmosis, Liver transplant, Pityriasis capitis, Pityriasis versicolor, Recalcitrant cutaneous dermatophyte infection, Renal transplant, Seborrheic dermatitis, Serious chronic resistant mucocutaneous candidiasis, Serious git mycoses, Severe chronic mucocutaneous candidiasis, Social anxiety disorder, Systemic mycoses, Ventricular arrhythmias; Paroxysmal supraventricular tachyarrhythmias, and can also be given in adjunctive therapy as an alternative drug of choice in Prophylaxis of organ rejection in kidney allograft recipients.

Ketoconazole is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAbiraterone acetateKetoconazole and other liver enzyme inhibitor (e.g clarithromycin, atazanavir, nefazodone, atazanavir, voriconazole) inhibits the metabolism of abiraterone acetate by inhibiting CYP3A4.combination should be avoided or used with caution.AdinazolamAfatinibketoconazole may increase the level of afatinibuse alternative or reduced doseAlcoholCoadministration results in disulfiram-like reactions(swaeting,nausea,flushing,headache)MinorWhile taking ketoconazole patient advised to minimize alcohol consumption.Alfentanil (HCl)Alfentanil (HCl)AliskirenAlprazolamAluminium Hydroxide and OxideAmphotericin BEffects of amphotericin B possibly antagonised by Ketoconazole.AprepitantIncrease the AUC and the mean terminal half-life of aprepitant. Concomitant administration of aprepitant capsules with strong CYP3A4 inhibitors should be approached cautiously.ArtesunateConcurrent use may increase artesunate serum concentrations. AstemizoleKetoconazole increases the plasma concentration of astemizole by inhbiting itsmetabolic clearence. Increased plasma level may lead to prolongation of QT interval on ECG, ventricular arrythmia, cardiac arrest and sudden death.MajorCoadministration is considered contraindicated. Loratadine, cetirizine or fexofenadine are considered safer alternatives.Beclomethasone (Dipropionate)ketoconazole and itraconazole increase serum-methylprednisolone concentration and enhance methyl prednisolones adrenal suppressive effectsBosentanPlasma concentration of Bosentan possibly increased byKetoconazole; avoid concomitant use.MajorCarbamazepineCo administration results in decreased plasma concentration of azole agent by accelerating azole clearance due to induction of enzymatic pathway by carbamazepine.ModerateMonitor cabamazepine toxicity and failure of ketoconazole treatment so dose adjustment is required. Less reactive like Terbinafine or fluconazole may be prescribed.CilostazoleCimetidine (HCl)Cimetidine decreases absorption and bioavailability of ketoconazole by increasing gastric pH thus decreases plasma ketoconazole concentration. ModerateThis combination should not be used.Fluconazole is a better replacement of ketoconazole.CisaprideKetoconazole increases the plasma concentration of cisapride by inhibiting its metabolic clearence resulting prolongation of QT interval, ventricular arrythmia, cardiac arrest and sudden death.MajorThis combination is considered contraindicated.Clidinium (Br)Clorazepate (K)conjugated Estrogens/Bazedoxifenemay increase the exposure of conjugated estrogensmonitor closelyCorticotropinCyclosporin ACyclosporin ADabigatranSystemic ketoconazole increased dabigatran AUC and Cmax values by 138% and 135%, respectively, after a single dose of 400 mg, and 153%, and 149%, respectively, after multiple daily doses of 400 mg.Dabigatran should be given at a dose of 75 mg twice daily.DabrafenibStrong CYP3A4 inhibitors may increase levels of dabrafenibConsider alternate therapyDapoxetine HCl increased the Cmax and AUCinf of dapoxetineconcomitant use of dapoxetine and potent CYP3A4 inhibitors is contraindicated DeflazacortDesonideDidanosineDocetaxelDonepezil (HCl)EfavirenzEletriptanEplerenoneConcomitant use with strong CYP3A4 Inhibitors (e.g. ketoconazole) may increase serum concentrations of Eplerenone.MajorConcomittant use is contraindicated.ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinibFamotidineAbsorption of Ketoconazole is reduced when administerd with famotidineFexofenadineKetoconazole increase plasma concentration of fexofenadineFlunisolideiloperidoneketoconazole can inhibit iloperidone elimination and cause increased blood levelsN/AIloperidone doses should be reduced by about one-half when administered with ketoconazole.IndacaterolStrong CYP3A4 inhibitors increase levels of indacaterolconsider alternate therapyIndinavir (Sulphate)ketoconazole enhances the mean area under the plasma concentration-time curve of indinavir by 68% by inhibiting CYP450 3A4 hepatic metabolism.ModerateReduce the dose in case of liver disease. Closely monitor the adverse and therapeutic effects of indinavir.Irinotecan (HCl Trihydrate)IsoniazidLoratadineKetoconazole inhibit the metabolism of Loratadine and increases the AUC upto 180% of loratadine and 56% for its metabolites due to inhibition of hepatic enzyme.MinorThis combination is considered safer to use.LovastatinLurasidoneketoconazole is a strong CYP3A4 inhibitor, increases Cmax and AUC of lurasidonecontraindicatedMacitentanketoconazole approximately double macitentan exposure.Avoid concomitant use of macitentan with strong CYP3A4 inhibitorsNevirapineNilotinibsystemic exposure to nilotinib was increased approximately 3-fold.patient should be closely monitored NizatidineNizatidine may interfere with the absorption of Ketoconazole.PaclitaxelPantoprazolePantoprazole may decrease the effectiveness of Ketoconazole.Phenytoin (Na)Phenytoin reduces the serum levels of ketoconazole upto 90% by enhancing first-pass and hepatic metabolism of ketoconazole.ModerateThis combination should be avoided.PomalidomidePomalidomide exposure is increased when co-administered with a strong CYP1A2 inhibitor (fluvoxamine) in the presence of a strong CYP3A4/5 and P-gp inhibitor (ketoconazole).Avoid co-administration, if medically necessary Pomalidomide dose should be reduced by 50%.Prednisolone and Prednisoneketoconazole impair metabolism and renal clearance of prednisolone and prednisoneQuetiapineQuinidineCo-administration increases the plasma concentration of quiniddine by inhibiting the hepatic enzyme responsible for metabolic clearance of quinidine.Quinidine also prolongate the QT interval thus potentiate the risk of ventricular arrhythmias as well as cardiac arrest.MajorCo-administration should be avoided.If co-administration is necessary pharmacological response and Quinidine plasma levels should be monitored more closely and adjust the dose.RanitidineRanitidine increases gastric pH and decrease the absorption of ketoconazole thus reduces its bioavailability upto 75% to 80% results decreased plasma level.ModerateCo-administration is not recommended.RanolazineKetoconazole (200 mg twice daily) increases average steady-state plasma concentrations of ranolazine 3.2-fold [seeDo not use (ranolazine) with strong CYP3A inhibitors, including ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir.RepaglinideKetoconazole may increase the levels/effects of repaglinide.RifampicinRifampicinRiociguatincrease the level or effects of riociguatclosely monitor/use alternativeRitonavirCo-admistration increases the plasma concentration of ketoconazzole by inhibiting ritonavir metabolism.ritonavir increases Cmax and AUC of ketoconazole upto 55%.ModerateTo avoid excessive plasma drug levels ketoconazole should not exceed to 200mg/day.co-administration increases risk of hepatotoxicity,impairment of testosterone and cortisol productionRivaroxabanstrong Inhibitor of CYP3A4, P-Glycoprotein ( Other e.g; include Itraconazole, posaconazole, voriconazole) may increase plasma concentration, lead to bleeding.Not indicatedSalmeterolCoadministration of salmeterol (50 mcg twice daily) and ketoconazole (400 mg once daily) for 7 days resulted in greater systemic exposure to salmeterol.SibutramineSildenafilClearance of Sildenafil is decreased due to inhibition of CYP450SimvastatinSolifenacin succinatesolifenacin succinate is a CYP3A4 substrate , while the ketoconazole is potent CYP3A4 inhibitor so ketoconazole may increase Cmax and AUC of solifenacin succinate by 1.5 and 2.7 foldit is recommended not to exceed a 5mg daily dose of solifenacin succinate when co administrered with ketonconazole or other potent CYP3A4 inhibitorsSucralfateSunitinibmay increases sunitinib concentrations.TacrolimusTadalafilKetoconazole (400 mg daily), a selective and potent inhibitor of CYP3A4, increased tadalafil 20 mg single-dose exposure (AUC) by 312% and Cmax by 22%, relative to the values for tadalafil 20 mg alone.Tamsulosin HydrochlorideTamsulosin is extensively metabolized, mainly by CYP3A4 and CYP2D6. Therefore should not be used in combination with strong inhibitors of CYP3A4 e.g Ketoconazole.Terfenadine Co-administration increases the plasma concentration, prolong QT interval, ventricular arrhythmia and cardiac arrest of terfenadine by inhibiting metabolic clearanceof terfenadine. MajorKetoconazole at multiple doses of 400mg or higher with Terfenadine is considered contraindicated.Loratidine,Cetrizine or fexofenadine are safer alternatives to use.TheophyllineCo-administration decreases serum theophylline concentration by decreased absorption.MinorDose adjustment is necessary. Altered efficacy of theophylline should be monitored.Ticagrelorketoconazole is a strong CYP3A4 inhibitor, increase Cmax of Ticagrelor, while the CMAX and AUC of Active metabolite reduced by 89% and 56%ContraindicatedTolbutamideTolterodine (Tartrate)TorasemideKetoconazole, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Ketoconazole is initiated, discontinued or dose changed.VemurafenibKetoconazole inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.Vilazodoneketonconazole a strong CYP3A4 inhibitor , it can increase vilazodone plasma concentration by 50%.vilazodone dose should be reduced to 20mg if coadministered with a strong inhibitor of CYP3A4VORICONAZOLEKetoconazole may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects Warfarin (Na)Ketoconazole may decrease the metabolism of Warfarin. ModerateConsider an alternative drug in order to avoid toxicity of Warfarin. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of Warfarin if Ketoconazole is initiated/dose increased, and decreased effects if Ketoconazole is discontinued/dose decreased. Zidovudine These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

False Positive Levels of Triglycerides

Drug should not be given to Pregnant Mothers, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Tab Store Below 40°C.

Ketoconazole should be used only if clearly needed during pregnancy. It should be used with caution in patients with any pre-existing illnesses or any allergy. Ketoconazole should be used with caution in the children under 2 years of age. It should also be used with caution in the patient with Azole hypersensitivity. Ketoconazole not be given to pateint with hepatotoxicity.