胺碘酮对安搏律定血药浓度的影响

Effect of amiodarone on the plasma concentration of aprindine

对6名健康志愿者进行口服安搏律定(AP)与胺碘酮(AM)的相互作用研究。单用AP40mg,bid共7d;合用AP40mg,bid及AM0.2,qd共7d,比较AP的血药浓度和药动学参数。结果:AP的谷浓度提高;t_(1/2)β延长;AUC_(0→12h)增加,CL减慢。而Tm、Vd两组差异无显著意义。说明AM能显著提高AP的血药浓度,改变AP的部分药动学参数,推测AM通过抑制AP的肝微粒体酶,而使AP的代谢减慢。建议在合并应用AP及AM两药时,应适当降低AP的剂量。

The interaction of aprindine-amiodarone was studied in6 healthy Chinese volunteers. They were treated withaprindine 40mg bid for 7 days. Two weeks later, they weregiven aprindine 40 mg bid and amiodarone 0. 2 g qd for an-other 7 days. The plasma concentrations and partial pharma-cokinetic parameters of aprindine were compared. The resultsindicate that by adding amiodarone, the plasma level ofaprindine was increased, t_(1/2)β prolonged, AUC_(0～12) increased,and CI decreased, while Tm, Vd showed no significantchanges. The possible mechanism is that amiodarone inhibitsthe metabolism enzymes of aprindine. It is suggested that ifamiodarone and aprindine are taken together, the dosage ofaprindine should be properly decreased.