Итраконазол

Описание

Itraconazole is an orally-active triazole antifungal indicated for use in the treatment of dermal, vaginal and systemic mycoses. In immunocompromised and AIDS patients, itraconazole has been shown to significantly reduce the incidence of relapses of cryptococcal meningitis.

Химические свойства

Off-White Crystalline Solid

Использование

Itraconazole is a triazole antifungal agent. It is used to inhibit cytochrome P-450-dependent enzymes and ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis, and aspergillosis. It?s different formulations are used to study Candida strains in murine invasive infections. It has been used to study proliferative changes of the forestomach mucosa in alloxan-induced diabetic rats..

Показания

Itraconazole (Sporanox) is effective in the treatment of histoplasmosis, blastomycosis, candidiasis, and dermatophyte infection. Its efficacy in the treatment of tinea capitis in children is equal to griseofulvin, and it is usually better tolerated (21). It is metabolized by the cytochrome P-450 system and may increase the levels ofwarfarin, cyclosporine, and digoxin among others. Its use is contraindicated with certain medications.
Itraconazole (Sporanox) is a triazole antifungal that is related to the imidazole ketoconazole. Similar to ketoconazole, it interferes with ergosterol synthesis and cell membrane integrity. It is clinically active against dimorphic fungi, yeast, dermatophytes, Blastomycetes, histoplasmosis, sporotrichosis, and Aspergillus. Itraconazole is a potent inhibitor of the cytochrome P450 3A enzyme system, which may elevate blood levels of other drugs metabolized by this system if taken concomitantly. Itraconazole levels may decrease in patients who are concurrently taking rifampin, phenobarbital, or phenytoin. Cyclosporine, felodipine, digoxin, warfarin, and oral hypoglycemic levels may increase when given in conjunction with itraconazole. Itraconazole, like ketoconazole, is contraindicated in patients taking cisapride. Itraconazole may induce torsades de pointes, ventricular arrhythmias, and congestive heart failure.

Антимикробная активность

The spectrum includes dermatophytes, dimorphic fungi (Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Paracocc. brasiliensis, Penicillium marneffei and Spor. schenckii), molds (including Aspergillus spp.), dematiaceous fungi and yeasts (Candida spp. and Cryptococcus spp.).

Приобретенная устойчивость

This is uncommon, but fluconazole-resistant C. albicans and C. glabrata are often cross-resistant to itraconazole. There are reports of itraconazole-resistant strains of A. fumigatus.

Общее описание

Itraconazole is an antifungal drug prescribed for oral or intravenous treatment of fungal infections. The drug is sold under trade names such as Sporanoxor Onmel^?. This Certified Spiking Solution^? is suitable as starting material for calibrators, controls, or linearity standards for clinical and diagnostic testing or therapeutic drug monitoring of itraconazole in patient blood, serum, or plasma samples by LC-MS/MS or HPLC.

Фармацевтические приложения

A synthetic dioxolane triazole available for oral or parenteral administration.

Клиническое использование

Aspergillosis
Systemic mycoses with dimorphic fungi (blastomycosis, coccidioidomycosis, histoplasmosis, paracoccidioidomycosis, penicilliosis) Subcutaneous mycoses (chromoblastomycosis, sporotrichosis)
Mucosal and cutaneous candidosis.
Dermatophytosis
Phaeohyphomycosis
Pityriasis versicolor

Побочные эффекты

Unwanted effects are more common with oral solution than with capsules, and are more severe. They include nausea, abdominal discomfort, dyspepsia, diarrhea, headache, pruritus and skin rash. Rare side effects include Stevens–Johnson syndrome, transient abnormalities of liver enzymes, reversible idiosyncratic hepatitis and hypokalemia.
Intravenous itraconazole has been associated with congestive heart failure. Neither intravenous nor oral itraconazole should be used to treat infections in patients with evidence of ventricular dysfunction unless the expected benefit clearly exceeds the risk. Patients with risk factors for congestive heart failure should be treated with caution and their condition monitored.