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用于治疗高血压和心力衰竭的盐皮质激素受体拮抗剂

Mineralocorticoid Receptor Antagonists for Treatment of Hypertension and Heart Failure.

作者信息

Sica Domenic A

机构信息

Virginia Commonwealth University Health System, Richmond, Virginia.

出版信息

Methodist Debakey Cardiovasc J. 2015 Oct-Dec;11(4):235-9. doi: 10.14797/mdcj-11-4-235.

Abstract

Spironolactone and eplerenone are both mineralocorticoid-receptor antagonists. These compounds block both the epithelial and nonepithelial actions of aldosterone, with the latter assuming increasing clinical relevance. Spironolactone and eplerenone both affect reductions in blood pressure either as mono- or add-on therapy; moreover, they each afford survival benefits in diverse circumstances of heart failure and the probability of renal protection in proteinuric chronic kidney disease. However, as use of mineralocorticoid-blocking agents has expanded, the hazards inherent in taking such drugs have become more apparent. Whereas the endocrine side effects of spironolactone are in most cases little more than a cosmetic annoyance, the potassium-sparing effects of both spironolactone and eplerenone can prove disastrous, even fatal, if sufficient degrees of hyperkalemia emerge. For most patients, however, the risk of developing hyperkalemia in and of itself should not discourage the sensible clinician from bringing these compounds into play. Hyperkalemia should always be considered a possibility in patients receiving either of these medications; therefore, anticipatory steps should be taken to minimize the likelihood of its occurrence if long-term therapy of these agents is being considered.

摘要

螺内酯和依普利酮均为盐皮质激素受体拮抗剂。这些化合物可阻断醛固酮的上皮和非上皮作用,其中后者的临床相关性日益增加。螺内酯和依普利酮单药治疗或联合治疗均能降低血压;此外,它们在不同情况下的心力衰竭中均能带来生存获益,且在蛋白尿性慢性肾脏病中具有肾脏保护作用。然而,随着盐皮质激素阻断剂的使用范围扩大,服用此类药物所固有的风险变得更加明显。虽然螺内酯的内分泌副作用在大多数情况下只不过是令人烦恼的外观问题,但如果出现足够程度的高钾血症,螺内酯和依普利酮的保钾作用都可能是灾难性的,甚至是致命的。然而,对于大多数患者而言,发生高钾血症的风险本身不应阻碍明智的临床医生使用这些化合物。接受这两种药物治疗的患者始终应被视为有发生高钾血症的可能性;因此,如果考虑长期使用这些药物,应采取预防措施以尽量降低其发生的可能性。

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