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肾素抑制剂。

Renin inhibitors.

机构信息

Division of Endocrinology, Diabetes and Hypertension, Hypertension Services, Brigham and Women's Hospital, Boston, MA, USA.

出版信息

J Clin Hypertens (Greenwich). 2011 Sep;13(9):662-6. doi: 10.1111/j.1751-7176.2011.00514.x. Epub 2011 Jul 27.

Abstract

KEY POINTS AND PRACTICAL RECOMMENDATIONS

•  Aliskiren, the sole oral renin inhibitor approved by the US Food and Drug Administration, is indicated for the treatment of hypertension, either as monotherapy or in combination, with reductions in blood pressure similar to other agents. •  Early evidence suggests that aliskiren confers additional benefit in patients with diabetic nephropathy. Data are not yet available to determine whether protection will extend to cardiovascular disease. •  No initial dosage adjustment is required in elderly patients or for patients with mild to severe renal impairment; however, clinical experience is limited in patients with significant renal impairment, and with renal artery stenosis. •  It appears rational to combine aliskiren with agents that otherwise increase plasma renin activity, including thiazide diuretics, angiotensin-converting enzyme inhibitors, and angiotensin receptor blockers. •  While there is a reactive rise in renin in response to aliskiren, probably larger than that induced by angiotensin receptor blockers and angiotensin-converting enzyme inhibitors, there is no evidence that this rise is harmful. •  In placebo-controlled studies, the incidence of edema anywhere in the body was 0.4% with aliskiren compared with 0.5% with placebo. It is unknown whether angioedema rates are higher in blacks with aliskiren. •  Aliskiren is associated with a slight increase in cough, with rates of about one third to one half seen with angiotensin-converting enzyme inhibitors. •  Increases in serum potassium >5.5 meq/L were infrequent in patients with essential hypertension treated with aliskiren alone (0.9% compared with 0.6% with placebo).

摘要

要点和实用建议

  • 阿利吉仑是唯一经美国食品和药物管理局批准的口服肾素抑制剂,可用于治疗高血压,可单独使用或与其他药物联合使用,降压效果与其他药物相似。

  • 早期证据表明,阿利吉仑可使糖尿病肾病患者获益增加。目前尚无数据确定这种保护作用是否会扩展到心血管疾病。

  • 老年患者或轻至重度肾功能损害患者无需初始剂量调整;然而,在有严重肾功能损害和肾动脉狭窄的患者中,临床经验有限。

  • 将阿利吉仑与其他可增加血浆肾素活性的药物联合使用似乎是合理的,包括噻嗪类利尿剂、血管紧张素转换酶抑制剂和血管紧张素受体阻滞剂。

  • 虽然阿利吉仑会引起肾素反应性升高,可能比血管紧张素受体阻滞剂和血管紧张素转换酶抑制剂引起的升高更大,但没有证据表明这种升高是有害的。

  • 在安慰剂对照研究中,阿利吉仑组全身水肿的发生率为 0.4%,安慰剂组为 0.5%。目前尚不清楚阿利吉仑是否会使黑人患者的血管性水肿发生率更高。

  • 阿利吉仑与咳嗽略有增加相关,其发生率与血管紧张素转换酶抑制剂相当,约为三分之一至一半。

  • 在单独使用阿利吉仑治疗的原发性高血压患者中,血清钾升高>5.5 meq/L 的情况很少见(阿利吉仑组为 0.9%,安慰剂组为 0.6%)。

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