Robert J
Fondation Bergonié, Bordeaux, France.
Bull Cancer. 1988;75(2):167-74.
Several new anthracyclines have been recently made available for clinical use or for clinical trials. Each molecule is characterized by original metabolic and pharmacokinetic features, which can be compared to those of the reference anthracyclines, doxorubicin and daunorubicin. Idarubicin is transformed into idarubicinol to a high extent, similarly to the transformation of daunorubicin to daunorubicinol, whereas the 13-dihydroderivatives of esorubicin, epirubicin or pirarubicin are present in plasma at lower levels than the parent drugs. Epirubicin is the only anthracycline able to form glucuronides, and pirarubicin can be transformed into doxorubicin itself. The elimination half-life of epirubicin or esorubicin is similar to that of doxorubicin (30 h) and the elimination half-life of unchanged idarubicin or pirarubicin is shorter (15-20 h). The novel anthracyclines have generally a higher plasma clearance than doxorubicin or daunorubicin, and a higher volume of distribution. Less than 10% of the injected dose of any anthracycline is found in urines, the major elimination pathway being the bile. The knowledge of anthracycline pharmacokinetics may allow the prediction of their behavior when special administrations are used (continuous infusion, locoregional therapy...).
最近有几种新型蒽环类药物可供临床使用或用于临床试验。每种分子都具有独特的代谢和药代动力学特征，可与参考蒽环类药物多柔比星和柔红霉素的特征进行比较。伊达比星在很大程度上转化为伊达比星醇，类似于柔红霉素转化为柔红霉素醇，而表柔比星、表柔比星或吡柔比星的13-二氢衍生物在血浆中的水平低于母体药物。表柔比星是唯一能够形成葡萄糖醛酸苷的蒽环类药物，吡柔比星可自身转化为多柔比星。表柔比星或表柔比星的消除半衰期与多柔比星相似（30小时），未变化的伊达比星或吡柔比星的消除半衰期较短（15-20小时）。新型蒽环类药物的血浆清除率通常比多柔比星或柔红霉素高，分布容积也更大。任何蒽环类药物注射剂量中不到10%在尿液中发现，主要消除途径是胆汁。了解蒽环类药物的药代动力学可能有助于预测在使用特殊给药方式（持续输注、局部区域治疗等）时它们的行为。
