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精氨酸加压素受体拮抗剂治疗低钠血症的研究进展
Development of arginine vasopressin receptor antagonists in the treatment of hyponatremia
【摘要】 精氨酸加压素(arginine vasopressin,AVP)能够调节机体体液与电解质平衡。AVP分泌紊乱能引起低钠血症。目前发现的AVP受体包括V1a、V1b,与V23种亚型。普坦类药物在结构上属于活性非肽类加压素受体拮抗剂,其中,V1a受体拮抗剂(relcovaptan)在治疗雷诺病与解痉方面有初步的效果,对V1b受体有选择性拮抗作用的SSR-149415对治疗精神疾病有一定疗效,V2受体拮抗剂(mozavaptan、lixivaptan、satavaptan与tolvaptan)与利尿剂作用原理不同,在不影响电解质排泄的前提下,通过诱导低渗性利尿,改善低钠血症,降低充血性心力衰竭引起的院内死亡率。V1a/V2非选择性AVP受体拮抗剂(conivaptan)作为美国食品药品监督管理局批准的静脉输液用于治疗低钠血症。本文通过探讨AVP受体拮抗剂治疗低钠血症的研究进展,希望为临床治疗提供一定的理论指导。
【Abstract】 Arginine vasopressin(AVP) regulates body fluid and electrolyte balance.AVP secretion disorder can cause hyponatremia.At present,the AVP receptor include V1a,V1b,and V2 subtypes.In terms of structure,vaptansin belongs to active non-peptide vasopressin receptor antagonists.Among them,the V1a receptor antagonist(relcovaptan) has a preliminary effect in the treatment of Raynaud’s disease and spasmolysis.SSR-149415 is a selective V1b receptor antagonist,showing beneficial effects in the treatment of psychiatric disorders.V2 receptor antagnosits,including mozavaptan,lixivaptan,satavaptan,and tolvaptan,unlike diuretic action principle,it can improve hyponatremia and reduce hospital mortality congestive heart failure without affecting electrolyte excretion.Conivaptan,a non-selective V1a/V2 AVP receptor antagonist,is an FDA-approved intravenous infusion for the treatment of hyponatremia.This paper aims to provide a theoretical guidance for clinical treatment of hyponatremia by discussing the research progress of AVP receptor antagonists.
【Key words】 arginine vasopressin; electrolyte excretion; hyponatremia; AVP receptor antagonist;
- 【文献出处】 临床药物治疗杂志 ,Clinical Medication Journal , 编辑部邮箱 ,2019年10期
- 【分类号】R591.1
- 【被引频次】6
- 【下载频次】213