Verbalis J G
232 Building D, Division of Endocrinology and Metabolism, Georgetown University School of Medicine, 4000 Reservoir Road NW, Washington DC 20007, USA.
J Mol Endocrinol. 2002 Aug;29(1):1-9. doi: 10.1677/jme.0.0290001.
Hyponatremia, whether due to the syndrome of inappropriate antidiuretic hormone secretion (SIADH) or disorders of water retention such as congestive heart failure and cirrhosis, is a very common problem encountered in the care of medical patients. To date, available treatment modalities for disorders of excess arginine vasopressin (AVP) secretion or action have been limited and suboptimal. The recent discovery and development of nonpeptide AVP V(2) receptor antagonists represents a promising new treatment option to directly antagonize the effects of elevated plasma AVP concentrations at the level of the renal collecting ducts. By decreasing the water permeability of renal collecting tubules, excretion of retained water is promoted, thereby normalizing or improving hypo-osmolar hyponatremia. In this review, SIADH and other water retaining disorders are briefly discussed, after which the published preclinical and clinical studies of several nonpeptide AVP V(2) receptor antagonists are summarized. The likely therapeutic indications and potential complications of these compounds are also described.
低钠血症，无论是由于抗利尿激素分泌不当综合征（SIADH）还是诸如充血性心力衰竭和肝硬化等水潴留性疾病引起的，都是内科患者护理中非常常见的问题。迄今为止，针对精氨酸加压素（AVP）分泌或作用异常的现有治疗方法有限且效果欠佳。非肽类AVP V(2)受体拮抗剂的最新发现和研发代表了一种有前景的新治疗选择，可在肾集合管水平直接拮抗血浆AVP浓度升高的影响。通过降低肾集合小管的水通透性，促进潴留水的排泄，从而使低渗性低钠血症正常化或得到改善。在本综述中，简要讨论了SIADH和其他水潴留性疾病，之后总结了几种非肽类AVP V(2)受体拮抗剂已发表的临床前和临床研究。还描述了这些化合物可能的治疗适应证和潜在并发症。
