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Conivaptan

康伐普坦

Mechanism of action:

Conivaptan 是一種抗利尿激素受體拮抗劑（arginine vasopressin receptor antagonist）。Conivaptan 能同時阻斷 V₁A 與 V₂ 受體，V₁A 受體位於血管平滑肌，阻斷後可導致血管擴張，輕度降低血壓；V₂ 受體位於腎集尿管上皮細胞的基底外側膜，該受體遭到 conivaptan 阻斷後，cAMP 生成下降，水通道蛋白-2（aquaporin-2，AQP2）不被運輸至細胞膜，導致水分重新吸收減少，水排出增加，血鈉濃度上升。

​Reference(s):

1. Ali F et al. (2007). Conivaptan: a dual vasopressin receptor V1a/V2 antagonist. Cardiovasc Drug Rev. 


2. Mao ZL et al. (2009). Pharmacokinetics of conivaptan hydrochloride, a vasopressin V(1A)/V(2)-receptor antagonist, in patients with euvolemic or hypervolemic hyponatremia and with or without congestive heart failure from a prospective, 4-day open-label study. Clin Ther.

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