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伊曲康唑——侵袭性曲霉病治疗的前景

Itraconazole--perspectives for the management of invasive aspergillosis.

作者信息

Groll A H

机构信息

Infectious Disease Research Program, Center for Bone Marrow Transplantation, Division of Pediatric Hematology/Oncology, Department of Pediatrics, Wilhelms University Medical Center, Muenster, Germany.

出版信息

Mycoses. 2002;45 Suppl 3:48-55. doi: 10.1111/j.1439-0507.2002.tb04770.x.

DOI:10.1111/j.1439-0507.2002.tb04770.x
PMID:12690972
Abstract

Itraconazole has become an important option in the management of invasive aspergillosis. The compound has potent and broad spectrum antifungal activity in vitro against Aspergillus spp. with a species- and strain dependent fungicidal mode of action. In vivo, the antifungal efficacy of itraconazole has been demonstrated in several non-immunocompromised and immunocompromised animal models of disseminated and invasive pulmonary aspergillosis. Itraconazole is available in oral and intravenous formulations, displays non-linear plasma pharmacokinetics, and is usually well tolerated. Non-comparative clinical data of itraconazole for therapy of suspected or proven invasive aspergillosis suggest response rates similar to those of conventional amphotericin B; however, the experience with itraconazole for induction therapy of invasive aspergillosis is limited, particularly in profoundly neutropenic patients. Itraconazole has an important role for consolidation and maintenance therapy of patients with invasive aspergillosis, and novel combination therapies involving itraconazole are currently under intensive preclinical investigation as to their usefulness for primary therapy.

摘要

伊曲康唑已成为治疗侵袭性曲霉病的重要选择。该化合物在体外对曲霉属具有强大且广谱的抗真菌活性,其杀菌作用方式因菌种和菌株而异。在体内,伊曲康唑的抗真菌疗效已在多种非免疫受损和免疫受损的播散性及侵袭性肺曲霉病动物模型中得到证实。伊曲康唑有口服和静脉制剂,呈现非线性血浆药代动力学,且通常耐受性良好。伊曲康唑用于治疗疑似或确诊的侵袭性曲霉病的非对照临床数据表明,其有效率与传统两性霉素B相似;然而,伊曲康唑用于侵袭性曲霉病诱导治疗的经验有限,尤其是在严重中性粒细胞减少的患者中。伊曲康唑在侵袭性曲霉病患者的巩固和维持治疗中具有重要作用,目前关于伊曲康唑用于初始治疗的有效性,涉及伊曲康唑的新型联合疗法正在进行深入的临床前研究。

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