Drug information of Ketoconazole


Ketoconazole

Drug group:

Ketoconazole is an antifungal medication Ketoconazole is not for use in treating fungal infections of the fingernails or toenails. This medicine is also not for use in treating prostate cancer or Cushing syndrome. This medicine should be used only when you cannot use other antifungal medications. Ketoconazole can cause serious harm to your liver that may result in liver transplant or cause death.

Mechanism of effect

Ketoconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. This results in an accumulation of methylated sterol precursors and a depletion of ergosterol within the cell membrane thus weakening the structure and function of the fungal cell membrane.

Pharmacodynamic

Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.

Pharmacokinetics

Absorption:Moderate In vitro, the plasma protein binding is about 99% mainly to the albumin fraction. Ketoconazole is widely distributed into tissues; however, only a negligible proportion reaches the cerebrospinal fluid. Metabolism:Hepatic Half life:2 hours Approximately 13% of the dose is excreted in the urine, of which 2 to 4% is unchanged drug. The major route of excretion is through the bile into the intestinal tract with about 57% being excreted in the feces.

Drug indications

fungal infections

Dosage

Usual Adult Dose for Blastomycosis Initial dose: 200 mg orally once a day If clinical responsiveness insufficient within expected time: Dose may be increased to 400 mg orally once a day. Duration of therapy: 6 months (usual duration for systemic infection) Usual Pediatric Dose for Blastomycosis 2 years or older: 3.3 to 6.6 mg/kg orally once a day Duration of therapy: 6 months (usual duration for systemic infection)

Interactions

Aluminium MGS , Aprepitant , Erlotinib , Everolimus , Oxybutynin , Ipratropium bromide , Irinotecan , Ifosfamide , Betamethasone , Bromocriptin , Budesonide , Bortezomib , Buspirone , Bosentan , Propafenone , Pantoprazole , Paclitaxel , pimecrolimus , Tadalafil , Tamsulosin , Trazodone , Tretinoin , Triamcinolone , Topotecan , Tinidazol , Daunorubicin , Dexamethasone , Docetaxel , Domperidone , Rabeprazole , Repaglinide , Zolpidem , Zonisamide , Sunitinib , Sodium bicarbonate , Sirolimus , Sildenafil , Cilostazol , Simvastatin , Cyclosporine , Fluticasone propinate , Flurazepam , Fingolimod , Galantamine , Lovastatin , Methylprednisolone , Nitrazepam , Nilotinib , Nimodipine , Hyoscine , Vardenafil , Venlafaxine , Carbamazepine , Alprazolam , Ergotamine-C , Pimozide , Cisapride , Midazolam , Quinidine , Colchicine , Clobazam , Disulfiram , Bisoprolol , escitalopram , eplerenone , fentanyl , Ranolazine , astemizole , Pioglitazone , Donepzil , Buprenorphine , Dabigatran , Oxycodone , propoxyphene , Axitinib , Almotriptan , ritonavir , saquinavir , nelfinavir , nevirapine , Ivabradine , Prednisolone , Mifepristone , Afatinib , vandetanib , Indinavir , Procainamide , Hyoscyamine , Mefloquine , Indapamide , echinacea , Anagrelide , brigatinib , Abiraterone , Budesonide , nasal Mometasone , Dutasteride , Dienogest , Bexarotene , Copanlisib , Tipranavir , Simeprevir , lumacaftor and Ivacaftor , Etravirine , Dabrafenib , Estropipate , Acalabrutinib , Cabazitaxel , Maraviroc , Halofantrine , Grepafloxacin , Darifenacin , Nicardipine , Nisoldipine , Terfenadine , Fesoterodine , Aluminium Mg , Alfuzosin , Ergoloid Mesylate , Erdafitinib , Pazopanib , Palbociclib , Ixazomib , Pimavanserin , Betrixaban , Desloratadine , Duvelisib , Flibanserin , Avanafil , Estazolam , Edoxaban , bazedoxifene/conjugated estrogens

Alerts

1-Ketoconazole Tablets should be used only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential risks. 2-Serious hepatotoxicity, including cases with a fatal outcome or requiring liver transplantation has occurred with the use of oral ketoconazole. 3-Coadministration of the following drugs with ketoconazole is contraindicated: dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, dronedarone, ranolazine. Ketoconazole can cause elevated plasma concentrations of these drugs and may prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias such as torsades de pointes 4-The use of Ketoconazole Tablets are contraindicated in patients with acute or chronic liver disease.

Points of recommendation

1- Patients should be instructed to report any signs and symptoms which may suggest liver dysfunction so that appropriate biochemical testing can be done. Such signs and symptoms may include unusual fatigue, anorexia, nausea and/or vomiting, abdominal pain, jaundice, dark urine or pale stools 2-Take with food. 3-Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.

Pregnancy level

C


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