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Essentials of Diagnosis Characteristic pattern of inflammation on glabrous skin surfaces. The active border of infection is scaly, red, and slightly elevated. Wet mount preparation with potassium hydroxide (10-20%). Skin scraping of the active border shows branching, translucent, rod-shaped filaments (hyphae) in keratinized material under low-power microscopy (10-40×). Hyphae are uniformly wide and regularly septated. Wood’s light examination (UV light at 365 nm) shows blue-green fluorescence for Microsporum canis and Microsporum audouinii. Trichophyton schoenleinii is pale green, and tinea versicolor shows white-yellow fluorescence. Culture should be performed with hair, nail, and skin specimens from particularly inflammatory lesions, to make a definitive mycologic diagnosis. General Considerations Dermatophytes are molds that infect keratinized …

Itraconazole 100 mg Capsules (Sporanox)

Itraconazole is a synthetic dioxolane triazole compound. Itraconazole: Mechanism of action Like other azoles, it interferes with the cytochrome P-450-dependent enzyme, 14a-demethylase. This leads to 14-methylsterol accumulation and ergosterol depletion in fungal cells and this results in alterations in a number of membrane-associated cell functions. Itraconazole: Spectrum of action Itraconazole has a broad spectrum of action including Aspergillus species, Blastomyces dermatitidis, Candida species, Coccidioides immitis, Cryptococcus neoformans, Histoplasma capsulatum, Paracoccidioides brasiliensis, Scedosporium apiospermum and Sporothrix schenckii. It is active in dermatophytosis and pityriasis versicolor, but appears to be ineffective in mucormycosis. Itraconazole: Acquired resistance This is rare, but ketoconazole-resistant C. albicans strains from patients with chronic mucocutaneous candidosis have been cross-resistant …

Use and Administration of Itraconazole 100 mg (Sporanox)

Therapeutic use of Itraconazole 100 mg Capsules (Sporanox) Itraconazole can be used to treat various superficial fungal infections, including the dermatophytoses, pityriasis versicolor, and mucosal and cutaneous forms of candidosis. It is also effective in patients with subcutaneous infections, such as chromoblastomycosis, sporotrichosis and certain forms of phaeohyphomycosis. It has become the drug of choice for non-life-threatening forms of blastomycosis and histoplasmosis, and is a useful alternative to amphotericin B for invasive aspergillosis. Maintenance treatment with itraconazole has helped to prevent relapse in patients with AIDS with histoplasmosis or cryptococcosis, and prophylactic treatment with this drug has helped to prevent aspergillosis and candidosis in neutropenic patients. However, it has not been …

Pharmacokinetics of Itraconazole 100 mg Capsules (Sporanox)

Absorption of itraconazole from the gastrointestinal tract is incomplete (about 55%), but is improved if the drug is given with food. Oral administration of a single 100-mg capsule will produce peak serum concentrations of between 0.1 and 0.2mg/l about 2-4 h later. Higher concentrations are obtained after repeated dosing, but there is marked variation between individuals. As with ketoconazole, there is a disproportionate increase in blood levels with increasing dosage. Serum concentrations are markedly reduced when gastric acid production is impaired. Much higher blood concentrations (up to 1.0-1.5 mg/1) have been attained in patients with AIDS and neutropenic individuals following administration of a 5 mg/kg dose of the oral solution formulation …

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Itraconazole: Side Effects See also Antifungal azoles Itraconazole is a triazole antifungal drug. It is used orally to treat oropharyngeal and vulvovaginal candidiasis, pityriasis versicolor, dermatophytoses unresponsive to topical treatment, and systemic infections, including aspergillosis, blastomycosis, chromoblastomycosis, cocci-dioidomycosis, cryptococcosis, histoplasmosis, paracocci-dioidomycosis, and sporotrichosis. It is also used to prevent fungal infections in immunocompromised patients. Pharmacokinetics The systemic availability of itraconazole and the bioequi-valence of single 200 mg doses of itraconazole solution and two capsule formulations have been evaluated in a crossover study in 30 male volunteers. Itraconazole and hydroxyitraconazole were 30-37% more available from the solution and were greater than from either capsule formulation. However, the values of Cmax, fmax, and …

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Itraconazole: Statins Itraconazole increases the risk of skeletal muscle toxicity of some statins by increasing their serum concentrations, but not all statins are equally affected. Concomitant use of atorvastatin, lovastatin, and simvastatin with itraconazole should be avoided or the doses should be reduced; fluvastatin and pravastatin have much less potential than other statins for clinically significant interactions with itraconazole and other CYP3A4 inhibitors; the effects of cerivastatin are intermediate. In a randomized, open, three-way, crossover study, 18 healthy subjects took single doses of cerivastatin 0.8 mg, atorvastatin 20 mg, or pravastatin 40 mg without or with itraconazole 200 mg. Concomitant cerivastatin + itraconazole and pravastatin + itraconazole produced small increases in …

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Itraconazole: Glucocorticoids Itraconazole can inhibit the metabolic clearance of glucocorticoids by interfering with CYP3A4 and can directly inhibit steroidogenesis, thereby causing serious adverse effects. The effects on different glucocorticoids differ. Budesonide Two patients with cystic fibrosis developed profound adrenal failure and impairment of inhaled steroid clearance, resulting in paradoxical Cushing’s syndrome, after long-term treatment with itraconazole and inhaled budenoside. Pituitary-adrenal axis and gonadal function was then assessed in 37 patients treated with itraconazole with or without budesonide. An adrenocorticotropic hormone (ACTH) test (tetracosactide 250 micrograms) was performed in 25 patients with cystic fibrosis taking itraconazole and budesonide and in 12 patients taking itraconazole alone (6 with cystic fibrosis and 6 with …

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Itraconazole: Drug-Drug Interactions Amphotericin The in vitro effects of the combination of amphotericin with itraconazole was tested using six strains of A. fumi-gatus, and an antagonistic effect was found after pretreat-ment for all strains in vitro and for one strain in a mouse model of aspergillosis. The effect of the combination of itraconazole with amphotericin on liver enzyme activities has been studied retrospectively in 20 patients with hematological malignancies or chronic lung disease complicated by fungal infection or colonization. They took itraconazole 200-600 mg/day for a median of 143 (range 44 days. Nine had no abnormal liver function tests, including periods of high concentrations of itraconazole (over 5000 µg/ml) and its …

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Itraconazole: Second-Generation Effects Teratogenicity Since embryotoxicity and teratogenicity have been found in rats, albeit after the administration of high doses, itraconazole should be avoided during pregnancy. Susceptibility Factors Age The safety, tolerability, and pharmacokinetics of itraconazole and its active metabolite hydroxyitraconazole after administration of itraconazole solution in hydroxy-propyl-P-cyclodextrin have been investigated in a multi-center study in 26 infants and children aged 6 months to 12 years with mucosal candidiasis or at risk of invasive fungal disease. There was a trend to lower minimum plasma concentrations in children aged 6 months to 2 years. The systemic absorption of the solubilizer hydro-xypropyl-P-cyclodextrin was less than 1%. Given at 5 mg/ kg/day, this formulation …

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Itraconazole: Organs and Systems Cardiovascular Ventricular fibrillation has been attributed to itracona-zole-induced hypokalemia. • Pleural and subsequent pericardial effusion developed in a woman treated with itraconazole 200 mg bd for a localized pulmonary infection with Aspergillus fumigatus. After more than 9 weeks of treatment she developed a pericardial effusion, which necessitated drainage. Itraconazole was withdrawn. Six weeks later, and 2 weeks after the resumption of itraconazole, she developed signs of pulmonary edema and cardiac enlargement. These signs disappeared rapidly on discontinuation of itraconazole. Studies in dogs and healthy human volunteers have suggested that itraconazole has a negative inotropic effect; the mechanism is unknown. A systematic analysis of data from the FDA’s …

Dosage forms of Itraconazole:
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Synonyms of Itraconazole:

ITC, ITCZ, ITR, Itraconazol [Spanish], Itraconazole, Itraconazolum [Latin], ITZ

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Therapeutic classes of Itraconazole:

Antifungal Agents, Antifungals, Antiprotozoal Agents, Antiprotozoals

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