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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >A pharmacokinetic study of the combined administration of amiodarone and ximelagatran, an oral direct thrombin inhibitor.
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A pharmacokinetic study of the combined administration of amiodarone and ximelagatran, an oral direct thrombin inhibitor.

机译：胺碘酮和西美加群（口服直接凝血酶抑制剂）联合给药的药代动力学研究。

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The oral direct thrombin inhibitor ximelagatran is being developed for the prevention and treatment of thromboembolism. This single-blind, randomized, placebo-controlled, parallel-group study investigated the potential for the interaction of ximelagatran (36 mg every 12 hours for 8 days, measured as its active form melagatran in blood) and amiodarone (single 600-mg oral dose on day 4) in healthy male subjects (n = 26). For amiodarone + ximelagatran versus amiodarone + placebo, geometric mean ratios (90% confidence intervals for amiodarone AUC(0-120) and C(max) were 0.87 (0.69-1.08) and 0.86 (0.66-1.11), respectively. For desethylamiodarone, the principal metabolite of amiodarone, the corresponding ratios were 1.00 (0.89-1.12) for AUC(0-120) and 0.92 (0.77-1.09) for C(max).The geometric mean ratios (90% confidence intervals) for ximelagatran + amiodarone versus ximelagatran were 1.21 (1.17-1.25) for melagatran AUC(0-12) and 1.23 (1.18-1.28) for melagatran C(max). These confidence intervals were within or only slightly outside the interval, suggesting no interaction (0.8-1.25 for the effect of amiodarone on melagatran and 0.7-1.43 for the effect of melagatran on amiodarone or desethylamiodarone). Amiodarone did not affect the concentration-effect relationship of melagatran on activated partial thromboplastin time. Ximelagatran was well tolerated when coadministered with a single dose of amiodarone. Evaluation of the safety of the combination is needed to confirm that the relatively small pharmacokinetic changes in this study are of no clinical significance.
机译：口服直接凝血酶抑制剂西美加群正在开发中，用于预防和治疗血栓栓塞。这项单盲，随机，安慰剂对照，平行组研究调查了西美加仑（每12小时36毫克，共8天，以其在血液中的活性形式美加群测量）和胺碘酮（单剂600毫克，口服）的相互作用的潜力。在健康男性受试者中（n = 26）在第4天注射剂量。对于胺碘酮+西美加群与胺碘酮+安慰剂，几何平均比率（胺碘酮AUC（0-120）和C（max）的90％置信区间分别为0.87（0.69-1.08）和0.86（0.66-1.11）。胺碘酮的主要代谢物，AUC（0-120）的相应比率为1.00（0.89-1.12），C（max）的相应比率为0.92（0.77-1.09）。西美加仑+胺碘酮的几何平均比率（90％置信区间） melagatran AUC（0-12）与ximelagatran的相对值分别为1.21（1.17-1.25）和melagatran C（max）的1.23（1.18-1.28），这些置信区间在区间内或仅在区间外，表明没有相互作用（0.8-1.25）胺碘酮对美拉加群的影响为0.7-1.43（美洛群星对胺碘酮或去乙基胺碘酮的影响）（胺碘酮不影响美拉加群对活化的部分凝血活酶时间的浓度-效应关系。胺碘酮需要证实该组合的安全性，以确认该研究中相对较小的药代动力学变化没有临床意义。

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