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首页> 外文期刊>Drug Design, Development and Therapy >Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin
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Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin

机译：过氧化物酶体增殖物激活受体-γ激动剂洛贝格列酮对华法林的药代动力学和药效学缺乏影响

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Aims: Lobeglitazone has been developed for the treatment of type 2 diabetes mellitus. This study was conducted to evaluate potential drug–drug interactions between lobeglitazone and warfarin, an anticoagulant with a narrow therapeutic index.Methods: In this open-label, three-treatment, crossover study, 24 healthy male subjects were administered lobeglitazone (0.5?mg) for 1–12?days with warfarin (25?mg) on day 5 in one period. After a washout interval, subjects were administered warfarin (25?mg) alone in the other period. Pharmacokinetics of R- and S-warfarin and lobeglitazone, as well as pharmacodynamics of warfarin, as measured by international normalized ratio (INR) and factor VII activity, were assessed. Results: The geometric mean ratios (GMRs) and 90% confidence intervals (CIs) for area under the curve from time zero to the time of the last quantifiable concentration (AUClast) for warfarin + lobeglitazone: warfarin alone were 1.0076 (90% CI: 0.9771, 1.0391) for R-warfarin and 0.9880 (90% CI: 0.9537, 1.0235) for S-warfarin. The maximum observed plasma concentration (Cmax) values were 1.0167 (90% CI: 0.9507, 1.0872) for R-warfarin and 1.0028 (90% CI: 0.9518, 1.0992) for S-warfarin, both of which were contained in the interval 0.80–1.25. Lobeglitazone had no effect on the area under the effect–time curve from time 0 to 168?hours (AUEC) of INR and factor VII activity, as demonstrated by the GMRs of 1.0091 (90% CI: 0.9872, 1.0314) and 0.9355 (90% CI: 0.9028, 0.9695), respectively. In addition, the pharmacokinetics of lobeglitazone was also unaffected by warfarin.Conclusion: Concomitant administration of lobeglitazone and warfarin was well tolerated. Lobeglitazone had no meaningful effect on the pharmacokinetics or pharmacodynamics of warfarin. These findings indicate that lobeglitazone and warfarin can be coadministered without dosage adjustments for either drug.
机译：目的：洛贝格列酮已被开发用于治疗2型糖尿病。这项研究的目的是评估洛贝格列酮与华法林之间的潜在药物相互作用。华法林是一种治疗指标较窄的抗凝剂。方法：在这项开放标签，三项治疗的交叉研究中，对24名健康男性受试者进行了洛贝格列酮（0.5？mg ），在第1天的第5天服用华法林（25 mg）持续1-12天。冲洗时间间隔过后，在另一时期中，受试者仅服用华法林（25？mg）。评估了R-和S-华法林和洛贝格列酮的药代动力学，以及华法林的药效学（通过国际标准化比率（INR）和VII因子活性测得）。结果：华法林+来格列酮：零华法林的曲线平均面积（GMR）和曲线下面积的90％置信区间（CIs）从零时到最后可量化浓度（AUClast）时为1.0076（90％CI： R-华法令为0.9771，1.0391），而S-华法令为0.9880（90％CI：0.9537，1.0235）。 R-华法令的最大观测血浆浓度（Cmax）值为1.0167（90％CI：0.9507，1.0872），S-华法令的最大观测血浆浓度（Cmax）值为1.0028（90％CI：0.9518，1.0992），两者均在0.80– 1.25。洛贝格列酮对INR和VII因子活性从0到168？hours（AUEC）的作用时间曲线下的面积没有影响，GMR分别为1.0091（90％CI：0.9872，1.0314）和0.9355（90） ％CI：0.9028，0.9695）。此外，洛法格列酮的药代动力学也不受华法林的影响。结论：对雷贝格列酮和华法林的同时给药耐受性良好。洛贝格列酮对华法林的药代动力学或药效学没有有意义的影响。这些发现表明，可以将lobeglitazone和warfarin并用，而无需调整任何一种药物的剂量。

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