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Pharmacologic class: Imidazole
Therapeutic class: Antifungal
Pregnancy risk category C
FDA Box Warning
• Oral form has been linked to hepatic toxicity, including some deaths. Inform patient of this risk, and monitor closely.
• Concurrent use of astemizole, cisapride, or terfenadine with ketoconazole tablets is contraindicated, because serious cardiovascular adverse events (including death, ventricular tachycardia, and torsades de pointes) have occurred.
Alters fungal cell membranes, resulting in increased permeability, growth inhibition, and ultimately, cell death
Shampoo: 1%, 2%
Tablets: 200 mg
Indications and dosages
➣ Blastomycosis; chronic mucocutaneous candidiasis; oral thrush; candiduria; coccidioidomycosis; histoplasmosis; chromomycosis; paracoccidioidomycosis; mucocutaneous or vaginal candidiasis
Adults: 200 to 400 mg P.O. daily
Children ages 2 and older: 3.3 to 6.6 mg/kg P.O. as a single daily dose. Duration depends on infection: for candidiasis, 1 to 2 weeks; other systemic mycoses, 6 months; recalcitrant dermatophyte infections involving glabrous skin, 4 weeks. Chronic mucocutaneous candidiasis requires maintenance therapy.
➣ Scaling caused by dandruff or seborrheic dermatitis
Adults: 2% shampoo applied topically twice weekly for 4 weeks, then as needed to control symptoms, with at least 3 days between applications; or 1% shampoo applied topically q 3 to 4 days for up to 8 weeks, then as needed to control dandruff
➣ Tinea corporis; tinea cruris; tinea versicolor; tinea pedis, cutaneous candidiasis
Adults: 2% cream applied topically to affected areas daily for 2 weeks (except for tinea pedis, which may require 6 weeks of therapy)
• Hypersensitivity to drug or its components
• Concurrent oral astemizole, cisapride, triazolam, or terfenadine therapy
Use cautiously in:
• renal or hepatic disease, achlorhydria
• pregnant or breastfeeding patients
• children younger than age 2.
• Apply cream to damp skin of affected area and wide surrounding area.
• To use shampoo, wet hair, then apply shampoo and massage into scalp for 1 minute. Leave on for 5 minutes before rinsing. Rinse and repeat, this time leaving shampoo on scalp for 3 minutes before rinsing.
• Don't apply shampoo to broken or inflamed skin.
• In achlorhydria, dissolve 200-mg tablet in 4 ml of 0.2N hydrochloric acid solution.
• Withhold antacids for at least 2 hours after giving oral ketoconazole.
☞ Don't give concurrently with cisapride, available in U.S. for compassionate use only. (Astemizole and terfenadine are not available in U.S.)
CNS: headache, nervousness, dizziness, drowsiness, severe depression, suicidal ideation
GI: nausea, vomiting, diarrhea, abdominal pain, anorexia
GU: erectile dysfunction, gynecomastia
Hematologic: purpura, hemolytic anemia, thrombocytopenia, leukopenia
Skin: pruritus, rash, dermatitis, urticaria, severe irritation, stinging, alopecia, abnormal hair texture, scalp pustules, oily skin, dry hair and scalp
Other: fever, chills, allergic reaction
Drug-drug. Antacids, anticholinergics, histamine2-receptor antagonists: decreased ketoconazole absorption
Cyclosporine: increased cyclosporine blood level
Isoniazid, rifampin: increased ketoconazole metabolism
Theophylline: decreased theophylline blood level
Topical corticosteroids: increased corticosteroid absorption
Triazolam (oral): increased triazolam effects
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase: increased levels
Hemoglobin, platelets, white blood cells: decreased levels
Drug-herbs. Yew: inhibited ketoconazole metabolism
☞ Assess for suicidal ideation and signs and symptoms of depression.
☞ Monitor for evidence of hepatotoxicity, such as nausea, fatigue, jaundice, dark urine, and pale stools.
• With long-term therapy, stay alert for adrenal crisis.
☞ Advise patient to watch for signs and symptoms of depression and to immediately report suicidal thoughts.
☞ Teach patient to recognize and immediately report signs and symptoms of hepatotoxicity, such as unusual tiredness or yellowing of skin or eyes.
• Advise patient not to take antacids for at least 2 hours after oral ketoconazole.
• Instruct patient to apply cream to damp skin of affected area and wide surrounding area.
• Tell patient to wet hair before applying shampoo and to massage into scalp for 1 minute; then leave on for 5 minutes before rinsing off. Tell him to shampoo again, leaving it on for 3 minutes this time before rinsing.
• Caution patient not to apply shampoo to broken or inflamed skin.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.