It is a synthetic imidazole compound administered orally. It was the first oral Azole introduced into clinical use.
Indications
Blastomycosis,coccidioidomycosis,pseudallescheriasis,,ringworm, Tinea versicolor, chronic mucocutaneous Candidiasis, candida vulvovaginitis and oral and esophageal Candidiasis ,non meningeal ,localised histoplasmosis.
Contraindications
Adrenal and gonadal dysfunctions ,hepatic dysfunction ,hypertension.
Safety profile
It seems prudent to discontinue the drug before major surgical procedures and to avoid using high doses in patient with trauma, severe burns or other stressful conditions as it may precipitate addison’s disease type symptoms. In pregnancy use is not recommended due to teratogenic effect in animals.
Adverse effects
Nausea anorexia and vomiting, skin rashes and vocational elevation in aminotransferase levels leading to fatal hepatitis. It blocks the synthesis of adrenal steroids and testosterone and can cause gynecomastia and importance in men. Fertility and menstrual regulation can occur due to interference of biosynthesis of gonadal steroid hormones. Hypertension and fluid retention may occur.
Drug interactions
It inhibits mammalian cytochrome p450 can cause altered metabolism leading to enhance toxicity. Other Drugs like cyclosporine, midazolam ,warfarin, triazolam ,indinavir phenytoin and cisapride. Other Drugs accelerate metabolism of ketoconazole which include cimetidine, rifampicin, isoniazid, and rifabutin.
Dosage
Usual adult dose is 400m taken once daily and children are given 3.3- 6.6 MG per KG daily. Therapy is 5 days for candida vulvovaginitis, Two Weeks For candida oesophagitis and 6 to 12 months for Deep mycosis.