Vasopressin antagonists

Vasopressin antagonists (group of vaptans ) are drugs that are approved for the treatment of heart failure , liver failure and the syndrome of inappropriate ADH secretion ( SIADH ). Vaptane are direct ADH antagonists that at vasopressin receptor subtypes V ₂ of the kidney , the effect of ADH ( vasopressin block). The installation of aquaporins in the walls of the collecting tube of the kidney is prevented and thus the excretion of electrolyte-free water is promoted.

Tolvaptan is the first and currently only oral selective V ₂ vasopressin receptor antagonist available in Europe . Other substances under development are lixivaptan , mozavaptan and satavaptan (V ₂ -selective), as well as relcovaptan (V _1A- selective).

Conivaptan is a US-approved "dual" vasopressin antagonist that inhibits the vasopression receptors V _1b and V ₂ .

Individual evidence

1. ↑ Schrier RW, Gross P, Gheorghiade M et al. Tolvaptan, a Selective Oral Vasopressin V2 Receptor Antagonist, for Hyponatremia. (SALT-1, SALT-2). NEJM. 2006; 355 (20): 2099-112
2. ↑ Udelson JE, Smith WB, Hendrix GH, et al .: Acute hemodynamic effects of conivaptan, a dual V (1A) and V (2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation 2001; 104: 2417-23. PMID 11705818

literature

• Decaux G, Soupart A, Vassart G: Non-peptide arginine-vasopressin antagonists: the vaptans. Lancet. 2008 May 10; 371 (9624): 1624-32. Review. PMID 18468546

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