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首页> 外文期刊>Pharmaceutical research >Divergent effects of raloxifene HCI on the pharmacokinetics and pharmacodynamics of warfarin.
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Divergent effects of raloxifene HCI on the pharmacokinetics and pharmacodynamics of warfarin.

机译：雷洛昔芬盐酸盐对华法林药代动力学和药效学的不同作用。

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PURPOSE: Evista (raloxifene HCl) is a nonsteroidal selective estrogen receptor modulator that displays estrogen agonist effects on bone and lipid metabolism but estrogen antagonist effects on the breast and endometrium. The potential for drug-drug interaction between raloxifene and warfarin was assessed in 15 healthy postmenopausal women. METHODS: Single doses of warfarin (20 mg) were administered prior to and during 2 weeks of dosing with raloxifene 120 mg/day. Each warfarin dose was followed by pharmacokinetic sampling and prothrombin time measurements. RESULTS: Raloxifene administration resulted in 7.1% and 14.1% decreases in the clearance (CLp/F) and 7.4% and 9.8% decreases in the volume of distribution (Vss/F) of R- and S-warfarin, respectively (all p < or = 0.05). In contrast to the slightly higher plasma concentrations of R- and S-warfarin, raloxifene reduced the maximum prothrombin time (PTmax) by 10% and the area under the PT versus time curve from 0-120 h (AUCPT) by 8% (p < 0.01). CONCLUSIONS: Raloxifene administration may result in a small increase in systemic warfarin exposure that is associated with a diminution, not augmentation, of the pharmacodynamic effect. Due to the small magnitude of this effect, concomitant administration of raloxifene and warfarin is not likely to result in clinically significant drug-drug interaction.
机译：用途：Evista（雷洛昔芬盐酸盐）是一种非甾体选择性雌激素受体调节剂，对骨骼和脂质代谢显示雌激素激动剂作用，但对乳房和子宫内膜有雌激素拮抗剂作用。在15名健康的绝经后妇女中评估了雷洛昔芬与华法林之间药物相互作用的潜力。方法：在服用雷洛昔芬120 mg /天的2周之前和给药期间，单剂华法林（20 mg）服用。每个华法林剂量后均进行药代动力学采样和凝血酶原时间测量。结果：施用雷洛昔芬导致R-和S-华法林的清除率（CLp / F）分别降低7.1％和14.1％，R-和S-华法林的分布量（Vss / F）分别降低7.4％和9.8％（所有p <或= 0.05）。与R-和S-warfarin的血浆浓度稍高相比，雷洛昔芬使最大凝血酶原时间（PTmax）降低了10％，PT与时间曲线下面积从0-120 h（AUCPT）降低了8％（p <0.01）。结论：雷洛昔芬的给药可能导致全身性华法林暴露量的少量增加，这与药效学作用减弱而不是增强有关。由于这种作用的程度很小，雷洛昔芬和华法林的并用不太可能导致临床上显着的药物相互作用。

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