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血管加压素及血管加压素受体拮抗剂在心力衰竭中的应用

Vasopressin and vasopressin receptor antagonists in heart failure.

作者信息

Oghlakian Gerard, Klapholz Marc

机构信息

Division of Cardiovascular Diseases, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, 185 South Orange Avenue, Newark, NJ 07103, USA.

出版信息

Cardiol Rev. 2009 Jan-Feb;17(1):10-5. doi: 10.1097/CRD.0b013e318190e72c.

DOI:10.1097/CRD.0b013e318190e72c
PMID:19092365
Abstract

Antidiuretic hormone, also known as arginine vasopressin, is a hormone with a multitude of physiologic activities including the control of urinary free water excretion. Antidiuretic hormone also plays a role in vasoconstriction and has 3 receptors that have been identified. Vasopressin analogs and antagonists have been extensively studied in animal models as well as in humans. Because heart failure is associated with a state of water retention, several vasopressin antagonists have been evaluated for their potential aquaretic effect. Diuretics remain the mainstay of treatment in acute and chronic volume overload but are not shown to improve survival. In fact, they are associated with numerous side effects including hypotension, electrolyte abnormalities, worsening renal function, and activation of renin-angiotensin-aldosternone system. Tolvaptan, conivaptan, and lixivaptan are some of the vasopressin antagonists that have been studied in heart failure. The results were initially encouraging with alleviation of symptoms and effective aquaresis without worsening of hyponatremia or renal function, but yet failed to show any effect on mortality in heart failure. With an increasing number of more selective orally active vasopressin antagonists, further studies are underway to establish the role of "Vaptans" in the treatment of heart failure and other disease states with volume overload and hyponatremia.

摘要

抗利尿激素,也称为精氨酸加压素,是一种具有多种生理活性的激素,包括控制尿游离水排泄。抗利尿激素在血管收缩中也起作用,并且已鉴定出3种受体。加压素类似物和拮抗剂已在动物模型以及人类中进行了广泛研究。由于心力衰竭与水潴留状态相关,因此已对几种加压素拮抗剂的潜在利水作用进行了评估。利尿剂仍然是急性和慢性容量超负荷治疗的主要手段,但未显示能改善生存率。事实上,它们与许多副作用相关,包括低血压、电解质异常、肾功能恶化以及肾素-血管紧张素-醛固酮系统激活。托伐普坦、考尼伐坦和利昔伐坦是一些已在心力衰竭中进行研究的加压素拮抗剂。最初的结果令人鼓舞,症状得到缓解且有效利水,而低钠血症或肾功能未恶化,但仍未显示对心力衰竭死亡率有任何影响。随着越来越多更具选择性的口服活性加压素拮抗剂出现,正在进行进一步研究以确定“托伐普坦类药物”在治疗心力衰竭及其他伴有容量超负荷和低钠血症的疾病状态中的作用。

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