Ketoconazole (Ketoconazole)
Overview of Ketoconazole
Ketoconazole is an imidazole antifungal agent. It was the first oral azole introduced into clinical use for the treatment of systemic mycoses. It has a broad spectrum of action. Ketoconazole is active against many Candida species, endemic mycoses and dermatophytes. It was approved by the FDA in 1981.Like other azole antifungals, it exerts its effect by altering the fungal cell membrane.it inhibits ergosterol synthesis by interacting with 14-� demethylase, a cytochrome P-450 enzyme that is necessary for the conversion of lanosterol to ergosterol, an essential component of the membrane.
Indication of Ketoconazole
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.
Contraindication of Ketoconazole
Ketoconazole is contraindicated in conditions like Hypersensitivity.
Side Effects of Ketoconazole
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.
Precautions of Ketoconazole
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.