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Ketoconazole

Systems	Systemic and Topical
Category	Antifungal (Imidazole)

Pharmacokinetics

Ketoconazole is water soluble and is well absorbed from the GIT ;low gastric pH enhances the absorption. It is highly protein bound in the plasma. It gets metabolised in the liver.Distributed widely in all tissues but CNS penetration is poor.Plasma half life is 8 hrs.

Indications

Ketaconazole is used to treat serious fungal infections that may occur in any part of the body.They act against dermatophytes, yeast and dimorphic fungi .Ketaconazole is preferred because of its lower toxicity in histoplasmosis, mucocutaneous candidiasis,paracoccidiodomycosis and chromoblastomycosis.

Routes of Administration and Dosage

200 to 400 mgs once daily,preferably after food .The duration of the therapy ranges between 1 to 4 weeks .Treatment is given for a minimum of 6 months in systemic mycosis.

Contra Indications

Ketoconazole is contraindicated in pregnancy, hepatic disease, and in lactation.

Precautions

Alcohol abuse may increase the chance of adverse effects caused by azole antifungals.

Interactions

Astemizole, Terfenadine. Methylphenidate, Nizatidine, Omeprazole, Orphenadrine, Oxybutynin, Procainamide, Promethazine, Quinidine, and Trimeprazine: may decrease the effects of Ketoconazole these drugs should be taken at least 2 hours after Ketaconazole therapy.Cisapride should not be taken with oral Ketaconazole, which may increase the chance of serious adverse effects of Cisapride. Use of Didanosine with ketaconazole may decrease the effects of both drugs. Ketaconazole should be taken at least 2 hours before or 2 hours after Didanosine is given.

Brand Names

Funazole(Khandelwal), Fungicide 200(Torrent), Kenazole(PCI), Ketovate(Bal Pharma), Ketozole(Rexcel), Nizral(Ethnor), Phytoral(Brown & Burk).