ketoconazole

HOW SUPPLIED

Tablets: 200 mg

Oral suspension: 100 mg/5 ml
ACTION

Inhibits purine transport and DNA, RNA, and protein synthesis; increases cell-wall permeability, making the fungus more susceptible to osmotic pressure

INDICATIONS & DOSAGE

Systemic candidiasis, chronic mucocandidiasis, oral thrush, candiduria, coccidioidomycosis, blastomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis; severe cutaneous dermatophyte infections resistant to therapy with topical or oral griseqfulvin -

Adults and children over 40 kg (88Ib): initially, 200 mg P.O. daily in a single dose. Dose may be increased to 400 mg once daily in patients who don't respond.

Children ages 2 and older: 3.3 to 6.6 mg/kg P.O. daily as a single dose.
ADVERSE REACTIONS

CNS: headache, nervousness, dizziness, somnolence, photophobia, suicidal tendencies, severe depression.

GI: nausea, vomiting, abdominal pain, diarrhea.

GU: impotence, gynecomastia with tenderness.

Hematologic: thrombocytopenia, hemolytic anemia, leukopenia.

Hepatic: elevated liver enzymes, fatal hepatotoxicity.

Metabolic: hyperlipidemia.

Skin: pruritus.
Other: fever, chills.

INTERACTIONS

Drug-drug. Antacids, anticholinergics, H2O blockers: decreased absorption of ketoconazole. These drugs should not be administered until at least 2 hours after ketoconazole dose.

Anticoagulants: effects may be enhanced. INR, PT, and PTT must be monitored and the dose adjusted as needed.

Cisapride: may cause ventricular arrhythmias. Avoid concomitant use.

Cyclosporine: may increase cyclosporine plasma levels. Serum levels must be monitored.

Isoniazid, rifampin: increased ketoconazole metabolism. A decreased antifungal effect may occur.

Paclitaxel: metabolism inhibited. Use together cautiously.

Theophylline: may decrease theophylline plasma levels. Serum levels must be monitored.

Drug-herb. Yew: inhibits ketoconazole metabolism. Avoid concomitant use.
EFFECTS ON DIAGNOSTIC TESTS

None reported.
CONTRAINDICATIONS

Contraindicated in patients with hypersensitivity to drug.
SPECIAL CONSIDERATIONS

Use cautiously in patients with hepatic disease and in those who are taking other hepatotoxic drugs.

Because of the potential for serious hepatotoxicity, don't use ketoconazole for less serious conditions, such as fungus infections of the skin or nails.

Elevated liver enzymes and nausea that does not subside as well as unusual fatigue, jaundice, dark urine, or pale stool should be monitored; all are signs or symptoms of possible hepatotoxicity.

Note that much larger doses (up to 800 mg/day) can be used to treat fungal meningitis and intracerebral fungal lesions.

Patient teathing

If you have achlorhydria, dissolve each tablet in 4 ml aqueous solution of 0.2 N hydrochloric acid, sip mixture through a glass or plastic straw (to avoid contact with tecth), and finish by drinking a glass of water because ketoconazoJe requires gastric acidity for dissolution and absorption.

Treatment must continue until all tests indicate that acti ve fungal infection has subsided. If drug is discontinued too soon, infection will recur. Minimum treatment for candidiasis is 7 to 14 days; for other systemic fungal infections, 6 months; for resistant dermatophyte infections, at least 4 weeks.

Nausea, common early in therapy, will subside. To minimize, divide daily dose into two doses or take dose with meals

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