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口服唑类药物作为全身性抗真菌治疗。

Oral azole drugs as systemic antifungal therapy.

作者信息

Como J A, Dismukes W E

机构信息

Department of Medicine, University of Alabama, Birmingham School of Medicine.

出版信息

N Engl J Med. 1994 Jan 27;330(4):263-72. doi: 10.1056/NEJM199401273300407.

Abstract

The oral azole drugs--ketoconazole, fluconazole, and itraconazole--represent a major advance in systemic antifungal therapy. Among the three, fluconazole has the most attractive pharmacologic profile, including the capacity to produce high concentrations of active drug in cerebrospinal fluid and urine. Ketoconazole, the first oral azole to be introduced, is less well tolerated than either fluconazole or itraconazole and is associated with more clinically important toxic effects, including hepatitis and inhibition of steroid hormone synthesis. However, ketoconazole is less expensive than fluconazole and itraconazole--an especially important consideration for patients receiving long-term therapy. All three drugs are effective alternatives to amphotericin B and flucytosine as therapy for selected systemic mycoses. Ketoconazole and itraconazole are effective in patients with the chronic, indolent forms of the endemic mycoses, including blastomycosis, coccidioidomycosis, and histoplasmosis; itraconazole is also effective in patients with sporotrichosis. Fluconazole is useful in the common forms of fungal meningitis--namely, coccidioidal and cryptococcal meningitis. In addition, fluconazole is effective for selected patients with serious candida syndromes such as candidemia, and itraconazole is the most effective of the azoles for the treatment of aspergillosis.

摘要

口服唑类药物——酮康唑、氟康唑和伊曲康唑——代表了全身抗真菌治疗的重大进展。在这三种药物中,氟康唑具有最具吸引力的药理学特性,包括能够在脑脊液和尿液中产生高浓度的活性药物。酮康唑是最早引入的口服唑类药物,其耐受性不如氟康唑或伊曲康唑,且伴有更多具有临床重要性的毒性作用,包括肝炎和类固醇激素合成抑制。然而,酮康唑比氟康唑和伊曲康唑便宜——这对于接受长期治疗的患者来说是一个特别重要的考虑因素。这三种药物都是两性霉素B和氟胞嘧啶治疗某些全身性真菌病的有效替代药物。酮康唑和伊曲康唑对患有慢性、惰性形式的地方性真菌病(包括芽生菌病、球孢子菌病和组织胞浆菌病)的患者有效;伊曲康唑对孢子丝菌病患者也有效。氟康唑对常见类型的真菌性脑膜炎——即球孢子菌性和隐球菌性脑膜炎——有用。此外,氟康唑对患有严重念珠菌综合征(如念珠菌血症)的特定患者有效,而伊曲康唑是治疗曲霉病最有效的唑类药物。

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