Tchambaz Lydia, Schlatter Chantal, Jakob Max, Krähenbühl Anita, Wolf Peter, Krähenbühl Stephan
Division of Clinical Pharmacology & Toxicology, University Hopsital, Basel, Switzerland.
Drug Saf. 2006;29(6):509-22. doi: 10.2165/00002018-200629060-00004.
Dose adaptation for liver disease is important in patients treated with antineoplastic drugs because of the high prevalence of impaired liver function in this population and the dose-dependent, frequently serious adverse effects of these drugs. We classified the antineoplastic drugs marketed in Switzerland at the end of 2004 according to their bioavailability and/or hepatic extraction to predict their kinetic behaviour in patients with decreased liver function. This prediction was compared with kinetic studies carried out with these drugs in patients with liver disease. The studies were identified by a structured, computer-based literature search. Of the 69 drugs identified, 52 had a predominant extrarenal (in most cases hepatic) metabolism and/or excretion. For 49 drugs, hepatic extraction could be calculated and/or bioavailability data were available, allowing classification according to hepatic extraction. For 18 drugs, kinetic studies have been reported in patients with impaired liver function, with the findings generally resulting in quantitative recommendations for adaptation of the dosage. In particular, recommendations are precise for 16 drugs excreted by the bile (e.g. doxorubicin and derivatives and vinca alkaloids). Validation studies comparing such recommendations with kinetics and/or dynamics of antineoplastic drugs in patients with decreased liver function have not been published. We conclude that there are currently not enough data for safe use of cyctostatics in patients with liver disease. Pharmaceutical companies should be urged to provide kinetic data (especially hepatic extraction data) for the classification of such drugs and to conduct kinetic studies for drugs with primarily hepatic metabolism in patients with impaired liver function to allow quantitative advice to be given for dose adaptation.
由于该人群肝功能受损的发生率较高,且抗肿瘤药物具有剂量依赖性、常导致严重不良反应,因此对于接受抗肿瘤药物治疗的肝病患者,剂量调整非常重要。我们根据2004年底在瑞士上市的抗肿瘤药物的生物利用度和/或肝脏摄取率对其进行分类,以预测它们在肝功能下降患者中的动力学行为。将这一预测结果与这些药物在肝病患者中进行的动力学研究结果进行比较。这些研究通过基于计算机的结构化文献检索来确定。在识别出的69种药物中,52种主要通过肾外(大多数情况下是肝脏)代谢和/或排泄。对于49种药物,可以计算肝脏摄取率和/或获得生物利用度数据,从而根据肝脏摄取率进行分类。对于18种药物,已报道了其在肝功能受损患者中的动力学研究结果,这些结果通常会给出剂量调整的定量建议。特别是,对于16种经胆汁排泄的药物(如阿霉素及其衍生物和长春花生物碱),建议较为精确。尚未发表将这些建议与肝功能下降患者抗肿瘤药物的动力学和/或动态学进行比较的验证研究。我们得出结论,目前尚无足够数据支持在肝病患者中安全使用细胞抑制剂。应敦促制药公司提供此类药物分类所需的动力学数据(尤其是肝脏摄取率数据),并对主要经肝脏代谢的药物在肝功能受损患者中进行动力学研究,以便能给出剂量调整的定量建议。