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伊达比星:一种蒽环类抗肿瘤药物。

Idarubicin: an anthracycline antineoplastic agent.

作者信息

Cersosimo R J

机构信息

College of Pharmacy and Allied Health Professions, Northeastern University, Boston, MA 02115.

出版信息

Clin Pharm. 1992 Feb;11(2):152-67.

PMID:1551297
Abstract

The mechanism of action, pharmacokinetics, activity, adverse effects, and administration of idarubicin are reviewed. Idarubicin is currently approved for use with other agents in the management of acute nonlymphocytic leukemia in adults. This drug is a structural analogue of daunorubicin and has the same mechanism of action as daunorubicin and doxorubicin. Unlike the other currently available anthracyclines, idarubicin has significant oral bioavailability (average 28%), and an oral dosage form is currently under investigation. Idarubicin is at least as effective as daunorubicin for acute nonlymphocytic leukemia, and two studies indicate greater activity and longer survival with an idarubicin-cytarabine regimen than with a daunorubicin-cytarabine regimen. Additional data indicate activity in acute lymphocytic leukemia, lymphomas, and breast cancer. Adverse effects are similar to those seen with other anthracyclines, although idarubicin may be associated with less cardiotoxicity than doxorubicin or daunorubicin. A maximum cumulative dose to prevent chronic cardiomyopathy has not yet been defined. Idarubicin is an effective agent for the management of acute nonlymphocytic leukemia and is reportedly more potent and less cardiotoxic than daunorubicin or doxorubicin.

摘要

本文综述了伊达比星的作用机制、药代动力学、活性、不良反应及给药方式。伊达比星目前已获批与其他药物联合用于治疗成人急性非淋巴细胞白血病。该药是柔红霉素的结构类似物,作用机制与柔红霉素及阿霉素相同。与目前其他蒽环类药物不同,伊达比星具有显著的口服生物利用度(平均为28%),目前正在研究其口服剂型。伊达比星治疗急性非淋巴细胞白血病的疗效至少与柔红霉素相当,两项研究表明,与柔红霉素-阿糖胞苷方案相比,伊达比星-阿糖胞苷方案具有更强的活性和更长的生存期。其他数据表明,伊达比星对急性淋巴细胞白血病、淋巴瘤和乳腺癌也有活性。其不良反应与其他蒽环类药物相似,不过伊达比星的心脏毒性可能比阿霉素或柔红霉素小。目前尚未确定预防慢性心肌病的最大累积剂量。伊达比星是治疗急性非淋巴细胞白血病的有效药物,据报道,它比柔红霉素或阿霉素更有效,心脏毒性更小。

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