Susceptible systemic fungal infections (blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis) in those who have failed or are intolerant to other therapies.
Antifungals / Topical Antifungals & Antiparasites
Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability due to reduced amounts of ergosterol present in the fungal cell membrane. This metabolic inhibition also results in accumulation of 14α-methyl-3,6-diol, a toxic metabolite. The increase in membrane fluidity is also thought to produce impairment of membrane-bound enzyme systems as components become less closely packed.
Adult : PO Fungal infections 200 mg once daily, up to 400 mg once daily if needed. Topical/Cutaneous Seborrhoeic dermatitis As 2% foam: Apply bid for 4 wk. As 1 or 2% shampoo: Apply twice wkly for 2-4 wk. Prophylaxis: As 2% shampoo is used once every 1-2 wk. Pityriasis versicolor; Skin fungal infections As 2% cream: Apply 1-2 times/day. As 2% shampoo: Apply once daily for up to 5 days. Prophylaxis: As 2% shampoo: Use once daily for up to 3 days before exposure to sunshine. Should be taken with food.
No drug interaction in case of Shampoo and Cream. Drugs that reduce gastric acidity (eg.; acid neutralizing medicines such as aluminium hydroxide, suppressors such as H2 receptor antagonist and proton pump inhibitors) impair the absorption of Tablets.
Hypersensitivity; preexisting liver disease. Concurrent use w/ CYP3A4 substrates e.g. HMG-CoA reductase inhibitors (e.g. lovastatin, simvastatin), midazolam, triazolam, cisapride, dofetilide, eplerenone, nisoldipine, pimozide, quinidine, terfenadine, astemizole, ergot alkaloids (e.g. ergotamine, dihydroergotamine). Predisposition to adrenocortical insufficiency. Admin w/ acidic drink in patients w/ achlorhydria. Pregnancy and lactation.
Adrenal insufficiency; GI disturbances (e.g. abdominal pain, nausea, vomiting); rash, irritation, dermatitis, burning sensation, pruritus, urticaria, angioedema, anaphylaxis; alopecia, headache, dizziness, somnolence, fever and chills; thrombocytopenia, paraesthesia; menstrual irregularities, oligospermia, adrenal cortex suppression, gynaecomastia, impotence; raised intracranial pressure; photophobia, photosensitivity; asymptomatic, transient elevations in LFTs. Potentially Fatal: Hepatotoxicity.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Shampoo: Not expected as ketoconazole shampoo 2% is intended for external use only. In the event of accidental ingestion, only supportive measures should be carried out. To avoid aspiration, emesis or gastric lavage should not be performed.
Cream: Exaggerated topical application may lead to erythema, oedema and a burning sensation, which will disappear upon discontinuation of the treatment. If accidental ingestion of Ketoconazole 2% w/w cream occurs, no special measures have to be taken.
Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.
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