JAHA:达格列净与布美他尼在正常人体内的相互作用!

2018-02-11 xing.T MedSci原创

由此可见,布美他尼和达格列净的首次治疗Na+排泄量并不增加,但每周给予一种利尿剂可增强初始Na+排泄量,从而证明存在相互适应的利钠协同作用。联合治疗逆转布美他尼诱导的高尿酸血症。

达格列净可抑制肾脏近端小管中的钠-葡萄糖-共同转运蛋白2,由此促进糖尿排泄以降低2型糖尿病患者的高血糖症。由于这些患者可能需要袢利尿剂,并且钠-葡萄糖共同转运蛋白2抑制可能会导致渗透性利尿。近日,心血管疾病领域权威杂志JAHA上发表了一篇研究文章,研究人员评估了达格列净和布美他尼之间的利尿相互作用。

健康受试者(n = 42)接受固定≈110mmol·d-1的Na+饮食,被随机分入布美他尼1mg·d-1、达格列净10 mg·d-1或两种药物治疗7天,第二阶段为布美他尼联合达格列净再治疗7天。没有明显的药代动力学相互作用。

研究人员发现第一阶段达格列净治疗Na+排泄中等(22±6 mmol·d−1; P<0.005),而第一阶段布美他尼治疗Na+排泄更多(74±7 mmol·d-1,P<0.005),两种利尿剂合用时差异并不显著(80±5 mmol·d-1; P<0.005)。然而,当达格列净治疗1周后加用布美他尼(64±6mmol·d-1)时,Na+排泄量增加了190%(P<0.005),而布美他尼治疗1周后加用达格列净(101±8 mmol·d-1)的Na +排泄量增加了36%(P<0.005)。布美他尼治疗使血清尿酸盐升高了4%,但达格列净治疗降低了40%,联合治疗降低了20%(P<0.05)。

由此可见,布美他尼和达格列净的首次治疗Na+排泄量并不增加,但每周给予一种利尿剂可增强初始Na+排泄量,从而证明存在相互适应的利钠协同作用。联合治疗逆转布美他尼诱导的高尿酸血症。

原始出处:

Christopher S. Wilcox,et al. Interaction Between the Sodium‐Glucose–Linked Transporter 2 Inhibitor Dapagliflozin and the Loop Diuretic Bumetanide in Normal Human Subjects.JAHA.2018. https://doi.org/10.1161/JAHA.117.007046

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    2018-02-13 zhaohui6731
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    2018-02-13 ylz8405
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