单词 | ketoconazole |
释义 | ketoconazoleenUKke·to·co·na·zoleK0043450 (kē′tō-kə-nā′zōl′)ketoconazoleenUKketoconazole[ke″to-kon´ah-zōl]ketoconazolePharmacologic 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. ActionAlters fungal cell membranes, resulting in increased permeability, growth inhibition, and ultimately, cell death AvailabilityCream: 2% 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) Contraindications• Hypersensitivity to drug or its components • Concurrent oral astemizole, cisapride, triazolam, or terfenadine therapy PrecautionsUse cautiously in: • renal or hepatic disease, achlorhydria • pregnant or breastfeeding patients • children younger than age 2. Administration• 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. See Don't give concurrently with cisapride, available in U.S. for compassionate use only. (Astemizole and terfenadine are not available in U.S.) Adverse reactionsCNS: headache, nervousness, dizziness, drowsiness, severe depression, suicidal ideation EENT: photophobia GI: nausea, vomiting, diarrhea, abdominal pain, anorexia GU: erectile dysfunction, gynecomastia Hematologic: purpura, hemolytic anemia, thrombocytopenia, leukopenia Hepatic: hepatotoxicity Metabolic: hyperlipidemia 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 InteractionsDrug-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 Patient monitoringSee Assess for suicidal ideation and signs and symptoms of depression. See Monitor for evidence of hepatotoxicity, such as nausea, fatigue, jaundice, dark urine, and pale stools. • With long-term therapy, stay alert for adrenal crisis. Patient teachingSee Advise patient to watch for signs and symptoms of depression and to immediately report suicidal thoughts. See 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. ketoconazole(kē′tō-kə-nā′zōl′)ketoconazoleNizoral Infectious disease An oral imidazole that inhibits fungal cytochrome P450-dependent steroid synthesis, which is effective against candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycsis Adverse effects Liver problems, ↓ production of hormones–eg, testosteroneketoconazoleAn imidazole antifungal drug. Ketoconazole is absorbed into the blood from the intestine and can be used to treat internal (systemic) fungal infections as well as skin fungal infections. It can, however, damage the liver. Brand names are Daktarin Gold and Nizoral.antifungal agent |
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