Massachusetts College of Pharmacy and Health Sciences and Harvard Vanguard Medical Associates, Boston, MA, USA.
Clin Ther. 2011 Nov;33(11):1577-89. doi: 10.1016/j.clinthera.2011.10.007. Epub 2011 Nov 8.
Azilsartan medoxomil is an angiotensin receptor blocker, approved on February 25, 2011 by the US Food and Drug Administration (FDA) for hypertension management.
The purpose of this study was to review the pharmacology, pharmacokinetics, efficacy, safety profile, and role of azilsartan for hypertension management.
Peer-reviewed clinical trials, review articles, and relevant treatment guidelines were identified from MEDLINE and Current Contents (both 1966 to August 31, 2011) using the search terms azilsartan, TAK-491, TAK-536, pharmacology, pharmacokinetics, pharmacodynamics, pharmacoeconomics, and cost-effectiveness. The FDA Web site and manufacturer prescribing information were also reviewed to identify other relevant information.
Compared with olmesartan 40 mg daily, azilsartan 80 mg reduced mean systolic blood pressure (SBP) by an additional 2.1 mm Hg (P = 0.038), whereas azilsartan 40 mg was noninferior to olmesartan 40 mg. Azilsartan 40 mg or 80 mg added to chlorthalidone 25 mg daily significantly reduced SBP to a greater extent than did chlorthalidone alone (P < 0.05), but there was no difference between azilsartan 40 mg and 80 mg (40 mg: -31.72 mm Hg; 80 mg: -31.3 mm Hg [P > 0.05]). When coadministered with amlodipine 5 mg daily, both azilsartan 40 mg and 80 mg + amlodipine decreased SBP significantly more than amlodipine alone (amlodipine: -13.6 mm Hg; with azilsartan 40 mg: -24.79 mm Hg; with azilsartan 80 mg: -24.51 mm Hg [P < 0.05]). Compared with ramipril 10 mg daily, both azilsartan 40 mg and 80 mg resulted in significantly (P < 0.001) greater reductions in mean SBP (-20.63 and -21.24 mm Hg, respectively; ramipril: -12.22 mm Hg). The most common adverse events reported were dizziness (4%), dyslipidemia (3.3%), and diarrhea (2%).
At the recommended dose of 80 mg once daily, azilsartan is reported to be an efficacious BP-lowering agent. With once-daily dosing and a favorable side-effect profile, azilsartan is an attractive option for the treatment of hypertension. There is a lack of data supporting the use of azilsartan for improvement in cardiovascular outcomes; therefore, azilsartan is not approved for indications other than the treatment of hypertension.
阿齐沙坦酯是一种血管紧张素受体阻断剂，于 2011 年 2 月 25 日获得美国食品和药物管理局（FDA）批准，用于高血压治疗。
本研究旨在综述阿齐沙坦酯的药理学、药代动力学、疗效、安全性概况及其在高血压治疗中的作用。
从 MEDLINE 和 Current Contents（均回溯至 1966 年 2 月至 2011 年 8 月 31 日）中检索到同行评议的临床试验、综述文章和相关治疗指南，检索词包括阿齐沙坦酯、TAK-491、TAK-536、药理学、药代动力学、药效学、药物经济学和成本效益。还查阅了 FDA 网站和制造商的处方信息，以确定其他相关信息。
与奥美沙坦酯 40 mg 每日相比，阿齐沙坦酯 80 mg 可使平均收缩压（SBP）进一步降低 2.1mmHg（P=0.038），而阿齐沙坦酯 40 mg 并不劣于奥美沙坦酯 40 mg。阿齐沙坦酯 40mg 或 80mg 联合氯噻酮 25mg 每日可显著降低 SBP（P<0.05），但阿齐沙坦酯 40mg 与 80mg 之间无差异（40mg：-31.72mmHg；80mg：-31.3mmHg[P>0.05]）。当与氨氯地平 5mg 每日联合使用时，阿齐沙坦酯 40mg 和 80mg 联合氨氯地平均可显著降低 SBP（氨氯地平：-13.6mmHg；阿齐沙坦酯 40mg：-24.79mmHg；阿齐沙坦酯 80mg：-24.51mmHg[P<0.05]）。与雷米普利 10mg 每日相比，阿齐沙坦酯 40mg 和 80mg 均可显著降低平均 SBP（P<0.001）（分别为-20.63 和-21.24mmHg；雷米普利：-12.22mmHg）。报告的最常见不良事件为头晕（4%）、血脂异常（3.3%）和腹泻（2%）。
推荐剂量为 80mg 每日一次时，阿齐沙坦酯是一种有效的降压药物。每日一次给药，且具有良好的不良反应谱，阿齐沙坦酯是治疗高血压的一个有吸引力的选择。目前缺乏支持阿齐沙坦酯改善心血管结局的数据，因此，阿齐沙坦酯除了用于高血压治疗外，其他适应证尚未获批。
