Section of Cardiology, AUSL 1 dell'Umbria, Perugia, Italy.
Expert Opin Drug Metab Toxicol. 2013 Mar;9(3):379-85. doi: 10.1517/17425255.2013.769521. Epub 2013 Feb 7.
Azilsartan medoxomil is a newly approved angiotensin-receptor blocker for the management of hypertension. It is a prodrug that is quickly hydrolyzed to the active moiety azilsartan, a potent and highly selective angiotensin-receptor blocker with estimated bioavailability of ∼ 60%. This new agent induces a potent and long-lasting antihypertensive effect. The effective therapeutic antihypertensive dosages of azilsartan medoxomil in humans vary from 40 to 80 mg/day.
The authors review the results of clinical trials published in journals indexed in Medline, Scopus and Google Scholar. Primarily the authors discuss articles that analyze the safety and efficacy of azilsartan in lowering blood pressure.
Clinical trials have demonstrated that azilsartan is superior to other angiotensin-receptor blockers in lowering blood pressure. However, the clinical blood pressure trials of azilsartan published to date have been mainly conducted in patients without serious comorbidities and it is not clear if azilsartan has advantages over other angiotensin-receptor blockers in the treatment of these types of hypertensive patients. In addition, it remains to be determined whether the specific pharmacologic and pharmacokinetic characteristics of azilsartan will have a clinically significant impact on long-term cardiovascular outcomes.
阿齐沙坦酯是一种新批准的血管紧张素受体阻滞剂，用于治疗高血压。它是一种前体药物，可迅速水解为活性成分阿齐沙坦，这是一种强效且高度选择性的血管紧张素受体阻滞剂，估计生物利用度约为 60%。这种新型药物可引起强效且持久的降压作用。阿齐沙坦酯在人体中的有效治疗性降压剂量为 40 至 80 毫克/天。
作者回顾了发表在 Medline、Scopus 和 Google Scholar 索引期刊上的临床试验结果。作者主要讨论了分析阿齐沙坦降低血压的安全性和疗效的文章。
临床试验表明，阿齐沙坦在降低血压方面优于其他血管紧张素受体阻滞剂。然而，迄今为止，已发表的关于阿齐沙坦的临床降压试验主要是在没有严重合并症的患者中进行的，目前尚不清楚阿齐沙坦在治疗这些类型的高血压患者方面是否优于其他血管紧张素受体阻滞剂。此外，阿齐沙坦的特定药理学和药代动力学特征是否会对长期心血管结局产生临床显著影响仍有待确定。
