Verbalis Joseph G
Department of Medicine, Georgetown University Medical Center, Washington, DC 20007, USA.
Cleve Clin J Med. 2006 Sep;73 Suppl 3:S24-33. doi: 10.3949/ccjm.73.suppl_3.s24.
The antidiuretic hormone arginine vasopressin (AVP) is primarily responsible for regulating osmotic and volume homeostasis of body fluids, largely through binding to vasopressin type 1A (V(1A)) and type 2 (V2) receptors. Increased AVP secretion leads to decreased free water excretion with resulting water retention, and can cause dilutional hyponatremia. A new class of medications known as AVP receptor antagonists induces free water diuresis without natriuresis or kaliuresis, an effect termed aquaresis. Numerous clinical trials show AVP antagonists to be effective at increasing free water excretion and serum sodium in patients with hyponatremia due to the syndrome of inappropriate antidiuretic hormone secretion or edema-forming states such as congestive heart failure and cirrhosis. This article reviews clinical trial data on the AVP antagonists in late development (lixivaptan, satavaptan, and tolvaptan) and recently approved for marketing (conivaptan).
抗利尿激素精氨酸加压素（AVP）主要负责调节体液的渗透压和容量平衡，主要是通过与1A型血管加压素（V(1A)）受体和2型（V2）受体结合来实现。AVP分泌增加会导致游离水排泄减少，进而引起水潴留，并可能导致稀释性低钠血症。一类名为AVP受体拮抗剂的新型药物可诱导游离水利尿，而不伴有利钠或利尿钾作用，这种效应被称为利水作用。大量临床试验表明，AVP拮抗剂对于因抗利尿激素分泌不当综合征或充血性心力衰竭、肝硬化等水肿形成状态导致低钠血症的患者，在增加游离水排泄和血清钠方面是有效的。本文回顾了处于后期研发阶段（利伐普坦、沙塔普坦和托伐普坦）且最近已获批上市（考尼伐坦）的AVP拮抗剂的临床试验数据。
