Sporanox [Rx Classification Antifungal

Action/Kinetics: Believed to inhibit cytochrome P-450-dependent synthesis of ergosterol, a necessary component of fungal cell membranes. Absorption appears to increase when taken with a cola beverage. Concentrates in fatty tissues, omentum, liver, kidney, and skin. t!/2, at steady-state: 64 hr. Extensively metabolized by the liver; the major metabolite is hydroxyitracona-zole, which also has antifungal activity. The drug and major metabolite are extensively bound (over 99%) to

■ plasma proteins. Metabolites are excreted in both the urine and feces. Uses: Treatment of blastomycosis (pulmonary and extrapulmonary) and histoplasmosis (including chronic cavitary pulmonary disease and disseminated, nonmeningeal histoplasmosis) in both immuno-compromised and nonimmunocom-promised clients. To treat aspergillus infections (pulmonary and extrapul-monary) in clients intolerant or refractory to amphotericin B. Onycho-mycosis due to tinea unguium of the toenail with or without fingernail involvement. The drug is effective against Blastomyces dermatitidis, Histoplasma capsulatum and H. du-boisii, Aspergillus flavus and A. fu-migatis, and Cryptococcus neoformans. Oropharyngeal and esopha-geal candidiasis. In vitro activity has also been found for a number of other organisms, including Sporo-thirx scheneckii, Trochophyton species, Candida albicans, and Candida species. Investigational: (1) Superficial mycoses including dermatophytoses (tinea capitis, tinea corporis, tinea cruris, tinea pedis, and tinea manu-um), pityriasis versicolor, candidiasis (vaginal, oral, chronic mucocutane-ous), and sebopsoriasis. (2) Systemic mycoses including dimorphic infections (paracoccidioidomycosis, coc-cidioidomycosis), cryptococcal infections (meningitis, disseminated), and candidiasis. (3) Miscellaneous mycoses including fungal keratitis, alternariosis, leishmaniasis (cutaneous), subcutaneous mycoses (chro-momycosis, sporotrichosis), and zygo-mycosis.

Contraindications: Concomitant use of astemizole, cisapride, triazolam, oral midazolam, or terfenadine. Hypersensitivity to the drug or its excipients. Lactation. Use for the treatment of onychomycosis in pregnant women or in women wishing to become pregnant.

Special Concerns: Safety and efficacy have not been determined in children although pediatric clients have been treated for systemic fungal infections.

Side Effects: GI: N&V, diarrhea, abdominal pain, anorexia, general GI disorders, flatulence, constipation, gastritis. CNS: Headache, dizziness, vertigo, insomnia, decreased libido, somnolence, depression. CV: Hypertension, orthostatic hypotension, vasculitis. Dermatologic: Rash (occurs more frequently in immuno-compromised clients also taking im-munosuppressant drugs), pruritus. Allergic: Rash, pruritus, urticaria, an-gioedema, and rarely, anaphylaxis and Stevens-Johnson syndrome. Miscellaneous: Edema, fatigue, fever, malaise, abnormal hepatic function, hypokalemia, albuminuria, tinnitus, impotence, adrenal insufficiency, gynecomastia, breast pain in males, menstrual disorder, hepatitis (rare), neuropathy (rare).

Drug Interactions Astemizole / T Astemizole levels ^ serious CV toxicity including ventricular tachycardia, torsades de pointes, and death Calcium blockers (especially amlodi-pine and nifedipine) / Development of edema

Cisapride / Cisapride levels serious CV toxicity including ventricular tachycardia, torsades de pointes, and death.

Cyclosporine and HMG-CoA reduc-tase inhibitors / Possible development of rhabdomyolysis. T Cyclo-sporine levels (dose of cyclosporine should be i by 50% if itraconazole

KETOCONAZOLE 273

doses are much greater than 100 mg/day)

Digoxin / T Digoxin levels

H2 Antagonists / i Plasma levels of itraconazole

Midazolam, oral / T Levels of oral midazolam ^ potentiation of sedative and hypnotic effects Isoniazid / i Plasma levels of itra-conazole

Phenytoin / i Plasma levels of itra-conazole; also, metabolism of phenytoin may be altered Rifampin / i Plasma levels of itra-conazole

Quinidine / Tinnitus and decreased hearing

Sulfonylureas / T Risk of hypogly-cemia

Tacrolimus / T Levels of tacrolimus Terfenadine / T Terfenadine levels ^ serious CV toxicity including ventricular tachycardia, torsades de pointes, and death Triazolam / Levels of triazolam po-tentiation of sedative and hypnotic effects

Warfarin / T Anticoagulant effect of warfarin

How Supplied: Capsule: 100 mg

Dosage----------------------------------------------------------------------------

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