Zalcitabine。
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Shelton MJ, O'Donnell AM, Morse GD
Zalcitabine。
中华药物学杂志1993 4月27日(4):480-9。
- PubMed ID
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8097417 (PubMed视图］
- 摘要
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目的:综述zalcitabine (2'3'-dideoxycytidine, ddC)的化学、细胞内代谢、药代动力学和临床试验。资料来源:英文文章及会议程序。所使用的索引术语为zalcitabine, 2'3'-二脱氧胞苷和ddC。研究选择:除了制造商的包装说明书外，还回顾了可用的I期和I/II期研究。数据提取:ddC的临床经验仅限于非对照研究和扩大准入计划。疗效仅通过艾滋病毒疾病的替代标记物进行评估:CD4+淋巴细胞计数和p24抗原测定。临床终点，如疾病进展和存活率，必须提供给食品和药物管理局(FDA)继续批准。数据综合:FDA已批准使用ddC联合齐多夫定(ZDV)治疗CD4+淋巴细胞计数<或= 300细胞/mm3且临床或免疫功能明显恶化的HIV感染患者。虽然ddC具有与其他核苷类似物相同的作用机制，但它在摩尔基础上更有效。该药物在胃pH值中是稳定的，具有良好的生物利用度(约70- 90%)，但从血浆中迅速清除(半衰期约1-3小时)。活性形式的ddC三磷酸在细胞内的浓度可能与血浆浓度有关，但可能比母体药物在血浆中的持续时间更长。 When used as primary therapy in patients with CD4+ < or = 300 cells/mm3, ddC/ZDV increased CD4+ lymphocyte counts and reduced plasma p24 antigen concentrations. In comparison to ZDV monotherapy data taken from other studies, ddC/ZDV appeared to demonstrate a more pronounced and sustained increase in CD4+ cell counts; however, this observation cannot be confirmed until the results of ZDV-controlled comparisons are available. Overall, 17-31 percent of the patients receiving the currently recommended initial dosage of ddC experience peripheral neuropathy. CONCLUSIONS: In combination with ZDV, ddC appears to augment the CD4+ cell response of ZDV monotherapy in the treatment of HIV infection for ZDV-naive patients, although controlled studies and rigorous statistical analyses are lacking at present. The efficacy of ddC/ZDV in patients who received prior treatment with ZDV monotherapy is unclear at the present.
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