摘要
目的 了解促胃肠动力药西沙必利与其他药物合用时的相互作用。方法 通过对近期文献的阅读、分析和归纳 ,加以综述。结果 西沙必利由细胞色素P 450 (CYP) 3A4代谢 ,有较强的首过效应 ,所以许多CYP3A4底物或 (和 )抑制剂都能抑制西沙必利的代谢 ,使其血药浓度升高 ,从而可能引起心脏QT间期延长、心律失常 ,甚至导致扭转型室速 (TdP)。药效学研究表明 ,西沙必利与可以引起QT间期延长的药物合用后 ,也可能增加心脏的毒性反应。结论 西沙必利应避免与CYP3A4抑制剂、CYP3A4底物及易引起QT间期延长的药物合用。如果必需合用 ,应密切观察合用后的情况 ,并进行心电监护或血药浓度的监测 。
OBJECTIVE To understand the interactions of cisapride, a prokinetic agent, with concomitant administered drugs. METHOD To summarize recent published literature on the pharmacokinetic and pharmacodynamic interactions of cisapride with other medicines. RESULTS Cisapride is extensively metabolized by cytochrome P 450 (CYP) 3A4 and has low bioavailability. Many CYP substrates or (and) inhibitors could inhibit the metabolism of cisapride, promote the blood concentration of the drug, thus prolong the QT interval and may also evoke torsade de pointes(Tdp). Pharmacodynamic studies show cisapride, used concomitantly with drugs that prolong the QT interval, could increase the toxicity of heart.CONCLUSION Cisapride is not recommended to be used concomitantly with CYP3A4 inhibitors or CYP3A4 substrates, and should be avoided with the drugs that have potential to prolong the QT interval. If necessary, ECG or blood concentration monitoring should accompany simultaneous use with cisapride.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2003年第2期116-119,共4页
Chinese Journal of Modern Applied Pharmacy
