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阿齐沙坦:新型血管紧张素受体阻滞剂。

Azilsartan: Novel Angiotensin Receptor Blocker.

作者信息

Dargad Ramesh R, Parekh Jai D, Dargad Rohit R, Kukrety Shweta

机构信息

Consulting Physician and Cardiologist, Lilavati, Seven Hills and L.H. Hiranandani Hospital.

Medical Graduate, B.J. Medical College, Pune, Maharashtra.

出版信息

J Assoc Physicians India. 2016 Mar;64(3):96-98.

PMID:27731574
Abstract

OBJECTIVE

To describe the efficacy and safety profile of the new angiotensin receptor blocker (ARB), "Azilsartan Medoxomil", reviewing data available from both clinical and pre-clinical studies.

MATERIAL

We completed a review of the English literature from PubMed using the keywords- azilsartan medoxomil, angiotensin receptor blockers (ARB), angiotensin converting enzyme inhibitors (ACEi) and hypertension.

DATA EVALUATION

Many clinical trials have been conducted comparing the efficacy of azilsartan with other ARB's and also with the ACEi ramipril. The trials have shown azilsartan to be more effective in reducing the mean 24-hour systolic blood pressure compared to its counterparts.

CONCLUSIONS

Azilsartan is a recently approved ARB and appears to be more efficacious in reducing blood pressure (BP) than the other ARBs with a similar safety and tolerability profile. Azilsartan's very high affinity to and slow dissociation from the angiotensin 1 receptor (AT1R) along with its inverse agonistic properties make it a very good candidate for clinical effects beyond simple BP control, potentially counteracting cardiac hypertrophy, cardiac fibrosis and insulin resistance, together with improved reno-protection and atherosclerotic plaque stabilization.

摘要

目的

通过回顾临床和临床前研究的现有数据,描述新型血管紧张素受体阻滞剂(ARB)“阿齐沙坦美洛昔酯”的疗效和安全性。

材料

我们使用关键词“阿齐沙坦美洛昔酯”、“血管紧张素受体阻滞剂(ARB)”、“血管紧张素转换酶抑制剂(ACEi)”和“高血压”,完成了对来自PubMed的英文文献的综述。

数据评估

已经进行了许多临床试验,比较阿齐沙坦与其他ARB以及与ACEi雷米普利的疗效。试验表明,与同类药物相比,阿齐沙坦在降低24小时平均收缩压方面更有效。

结论

阿齐沙坦是最近获批的一种ARB,在降低血压(BP)方面似乎比其他具有相似安全性和耐受性的ARB更有效。阿齐沙坦对血管紧张素1受体(AT1R)具有非常高的亲和力且与之解离缓慢,同时具有反向激动特性,这使其成为除简单控制血压之外还具有临床效果的非常好的候选药物,可能抵消心脏肥大、心脏纤维化和胰岛素抵抗,同时改善肾脏保护作用和稳定动脉粥样硬化斑块。

相似文献

1
Azilsartan: Novel Angiotensin Receptor Blocker.阿齐沙坦:新型血管紧张素受体阻滞剂。
J Assoc Physicians India. 2016 Mar;64(3):96-98.
2
Azilsartan medoxomil: a new angiotensin II receptor antagonist for treatment of hypertension.奥美沙坦酯:一种用于治疗高血压的新型血管紧张素 II 受体拮抗剂。
Ann Pharmacother. 2011 Dec;45(12):1506-15. doi: 10.1345/aph.1Q468. Epub 2011 Nov 24.
3
Azilsartan medoxomil for the treatment of hypertension.阿齐沙坦酯用于治疗高血压。
Drugs Today (Barc). 2011 Sep;47(9):647-51. doi: 10.1358/dot.2011.47.9.1688573.
4
Azilsartan medoxomil/chlorthalidone: a new fixed-dose combination antihypertensive.奥美沙坦酯/氢氯噻嗪:一种新型的固定剂量复方降压药。
Ann Pharmacother. 2013 May;47(5):694-703. doi: 10.1345/aph.1R618. Epub 2013 Apr 12.
5
Critical evaluation of the efficacy and tolerability of azilsartan.阿齐沙坦疗效与耐受性的批判性评估。
Vasc Health Risk Manag. 2012;8:299-305. doi: 10.2147/VHRM.S22589. Epub 2012 May 14.
6
The renin-angiotensin receptor blocker azilsartan medoxomil compared with the angiotensin-converting enzyme inhibitor ramipril in clinical trials versus routine practice: insights from the prospective EARLY registry.在临床试验与常规实践中比较肾素-血管紧张素受体阻滞剂阿齐沙坦美洛昔酯与血管紧张素转换酶抑制剂雷米普利:来自前瞻性EARLY注册研究的见解
Trials. 2015 Dec 19;16:581. doi: 10.1186/s13063-015-1100-8.
7
Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood pressure in patients with stages 1 and 2 hypertension.在 1 期和 2 期高血压患者中,血管紧张素受体阻断剂阿齐沙坦酯与奥美沙坦和缬沙坦对动态血压和诊室血压的影响。
Hypertension. 2011 Mar;57(3):413-20. doi: 10.1161/HYPERTENSIONAHA.110.163402. Epub 2011 Jan 31.
8
Azilsartan medoxomil in the treatment of hypertension: the definitive angiotensin receptor blocker?奥美沙坦酯治疗高血压:最终的血管紧张素受体阻滞剂?
Expert Opin Pharmacother. 2013 Nov;14(16):2249-61. doi: 10.1517/14656566.2013.834887. Epub 2013 Sep 26.
9
Antihypertensive efficacy of hydrochlorothiazide vs chlorthalidone combined with azilsartan medoxomil.氢氯噻嗪与氯噻酮联合奥美沙坦酯的降压疗效。
Am J Med. 2012 Dec;125(12):1229.e1-1229.e10. doi: 10.1016/j.amjmed.2012.05.023. Epub 2012 Aug 30.
10
Azilsartan Medoxomil, an Angiotensin II Receptor Antagonist for the Treatment of Hypertension.阿齐沙坦美洛昔酯,一种用于治疗高血压的血管紧张素II受体拮抗剂。
Basic Clin Pharmacol Toxicol. 2017 Oct;121(4):225-233. doi: 10.1111/bcpt.12800. Epub 2017 Jun 19.

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