康尼伐坦:双重抗利尿激素受体v1a/v2拮抗剂[更正]。

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Ali F, Raufi MA, Washington B, Ghali JK

康尼伐坦:双重抗利尿激素受体v1a/v2拮抗剂[更正]。

中华心血管病杂志;2007;25(3):261-79。

PubMed ID

17919259 (PubMed视图

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摘要

一些液体潴留状态，如心力衰竭、肝硬化和抗利尿激素分泌不当综合征，都与血浆精氨酸抗利尿素(AVP)水平的不适当升高有关。AVP是一种由下丘脑分泌的神经肽，在调节血清渗透压和循环稳态中起关键作用。AVP的作用由三种受体亚型V1a、V2和V1b介导。V1a受体调节血管舒张和细胞肥大，而V2受体调节游离水排泄。V1b受体调节促肾上腺皮质激素的释放。康尼伐坦是一种非肽双V1a/V2 AVP受体拮抗剂。它以高亲和力、竞争性和可逆性结合于V1a/V2受体亚型;其拮抗作用呈浓度依赖性。它抑制CYP3A4肝酶，并提高由该酶代谢的其他药物的血浆水平。它只被批准用于短期静脉注射。输注部位反应是停药最常见的原因。 In animals conivaptan increased urine volume and free water clearance. In heart failure models it improved hemodynamic parameters and free water excretion. Conivaptan has been shown to correct hyponatremia in euvolemic or hypervolemic patients. Its efficacy and safety for short-term use have led to the Food and Drug Administration (FDA) approval of its intravenous form for the correction of hyponatremia in euvolemic and hypervolemic states. Despite its ability to block the action of AVP on V1a receptors, no demonstrable benefit from this action was noted in patients with chronic compensated heart failure and it is not approved for this indication. Consideration should be given to further evaluation of its potential benefits in patients with acute decompensated heart failure.

引用本文的药物库数据

药物

Conivaptan

药物靶点

药物	目标	种类	生物	药理作用	行动
Conivaptan	抗利尿激素V1a受体	蛋白质	人类	是的	拮抗剂	细节
Conivaptan	抗利尿激素V2受体	蛋白质	人类	是的	拮抗剂	细节

药物酶

药物	酶	种类	生物	药理作用	行动
Conivaptan	细胞色素P450 3A4	蛋白质	人类	未知的	底物 抑制剂	细节