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Vasopressinantagonisten

Neue Therapeutika zur Behandlung von Hyponatriämie und chronischer Herzinsuffizienz

Vasopressin antagonists

New drugs for the therapy of hyponatraemia and congestive heart failure

  • Klinische Pharmakologie
  • Published:
Der Kardiologe Aims and scope

Zusammenfassung

Vasopressinrezeptoren des Subtyps V1a, V1b und V2 sind in vielen verschiedenen Geweben lokalisiert, und sie haben neben ihrer physiologischen Bedeutung auch eine pathophysiologische Rolle z. B. bei Hyponatriämie, Herzinsuffizienz, Schwartz-Bartter-Syndrom, Aszites, Glaukom und psychischen Erkrankungen. Jedoch sind Vasopressinantagonisten mit Peptidstruktur nicht oral applizierbar und nur schwach wirksam. Deshalb war das Ziel, nichtpeptidische Vasopressinantagonisten (Vaptane) zu entwickeln. Aus der Reihe der Vaptane ist Conivaptan bis jetzt der einzige Vertreter, der von der FDA zur Behandlung lebensbedrohlicher euvolämischer und hypervolämischer Hyponatriämie bei hospitalisierten Patienten zugelassen wurde. Zur Therapie der Herzinsuffizienz ist Conivaptan noch nicht zugelassen, aber Studien zeigen eine gute Wirksamkeit. Langzeiteffekte und Nutzen der Vaptane müssen aber erst evaluiert werden. Aufgrund der Datenlage aus in vitro, präklinischen und klinischen Studien sind außer Hyponatriämie und chronischer Herzinsuffizienz zukünftig noch weitere Anwendungsgebiete für Vasopressinantagonisten zu erwarten.

Abstract

As vasopressin receptors (V1a, V1b, V2) are found in many different tissues, vasopressin antagonists may benefit the treatment of numerous disorders. Effects of vasopressin via V1a and V2 receptors are closely implicated in a variety of water-retaining and cardiovascular diseases, including heart failure, hyponatraemia, renal diseases, syndrome of inappropriate antidiuretic hormone secretion, cirrhosis and ocular hypertension. From the series of non-peptide vasopressin receptor antagonists (vaptans), conivaptan is the only compound, which has been approved by the FDA for the treatment of euvolaemic and hypervolaemic hyponatraemia so far. For further indications such as congenital heart failure, ongoing studies are promising. Based on data from in vitro studies as well as preclinical and clinical trials also other indications for vasopressin receptor antagonists besides hyponatraemia and heart failure are to be expected.

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  1. Department für Pharmakologie und Toxikologie, Universität Wien, Althanstraße 14, 1090, Wien, Österreich

    R. Lemmens-Gruber

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Correspondence to R. Lemmens-Gruber.

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Lemmens-Gruber, R. Vasopressinantagonisten. Kardiologe 3, 160–163 (2009). https://doi.org/10.1007/s12181-009-0170-9

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  • DOI: https://doi.org/10.1007/s12181-009-0170-9

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