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Pharmakologie und klinische Bedeutung von Vasopressinantagonisten

Pharmacology and clinical relevance of vasopressin antagonists

  • Arzneimitteltherapie
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Zusammenfassung

Vasopressinrezeptoren sind in vielen verschiedenen Geweben lokalisiert. Theoretisch könnten daher Vasopressinantagonisten wertvolle Therapeutika in der Behandlung zahlreicher Erkrankungen sein. Über V1a- und V2-Rezeptor vermittelte Effekte des Vasopressin (antidiuretisches Hormon, ADH) spielen bei Krankheitsbildern wie Herzinsuffizienz, Hyponatriämie, Bluthochdruck, Nierenerkrankungen, Syndrom der inadäquaten ADH-Sekretion (Schwartz-Bartter-Syndrom), Leberzirrhose und Glaukom eine wesentliche Rolle. Der V1b-Rezeptorsubtyp ist auch im Zentralnervensystem lokalisiert. Selektive V1b-Antagonisten könnten daher bei emotionalen und psychiatrischen Erkrankungen wirksam sein. Die Vaptane sind nicht-peptidische Vasopressinantagonisten mit selektiver Wirkung auf V1a- (Relcovaptan) oder V2-Rezeptoren (Tolvaptan, Lixivaptan, Satavaptan) bzw. mit nicht-selektiver V1a/V2-Wirkung (Conivaptan). Conivaptan ist das erste Vaptan, das von der Food and Drug Administration (FDA) mit der Indikation euvolämische Hyponatriämie zugelassen wurde. Für weitere Indikationen wie die Therapie der Herzinsuffizienz laufen mehrere Studien.

Abstract

As vasopressin receptors 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 diseases and cardiovascular diseases, including heart failure, hyponatremia, hypertension, renal diseases, syndrome of inappropriate antidiuretic hormone secretion, cirrhosis, and ocular hypertension. Furthermore, V1a vasopressin antagonists might be useful in cerebral ischemia and stroke, Raynaud’s disease, dysmenorrhoea and tocolytic treatment. V1b selective vasopressin antagonists are discussed in terms of their usefulness in the treatment of emotional and psychiatric disorders. The vaptans are vasopressin receptor antagonists with V1a (relcovaptan) or V2 (tolvaptan, lixivaptan, satavaptan) selectivity or non-selective activity (conivaptan). Conivaptan is the first vaptan which has been approved by the FDA for the treatment of euvolemic hyponatremia. For further indications such as congenital heart failure, studies are going on.

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

    R. Lemmens-Gruber & M. Kamyar

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  1. R. Lemmens-Gruber
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Correspondence to R. Lemmens-Gruber.

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Lemmens-Gruber, R., Kamyar, M. Pharmakologie und klinische Bedeutung von Vasopressinantagonisten. Internist 49, 628–634 (2008). https://doi.org/10.1007/s00108-008-2017-z

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