General Medicine Unit, Treviglio-Caravaggio Hospital, Medical Department, A.O. Treviglio, 24047 Treviglio (BG), Italy.
Expert Opin Pharmacother. 2011 Dec;12(17):2719-35. doi: 10.1517/14656566.2011.632367.
The modulation of the renin angiotensin aldosterone system (RAAS) is an important pathway in managing high blood pressure, and its overexpression plays a key role in target end-organ damage. Telmisartan is an angiotensin II receptor blocker (ARB) with unique pharmacologic properties, including the longest half-life among all ARBs; this leads to a significant and 24-h sustained reduction of blood pressure. Telmisartan has well-known antihypertensive properties, but there is also strong clinical evidence that it reduces left ventricular hypertrophy, arterial stiffness and the recurrence of atrial fibrillation, and confers renoprotection.
This paper reviews telmisartan's pharmacological properties in terms of efficacy for hypertension control and, importantly, focuses on its new therapeutic indications and their clinical implications.
ONTARGET (ongoing telmisartan alone and in combination with ramipril global endpoint trial) demonstrated, that telmisartan confers cardiovascular protective effects similar to those of ramipril, but with a better tolerability. Moreover, recent investigations focused on the capability of telmisartan to modulate the peroxisome proliferator-activated receptor-gamma (PPAR-γ), an established target in the treatment of insulin resistance, diabetes and metabolic syndrome, whose activation is also correlated to anti-inflammatory and, finally, anti-atherosclerotic properties. Telmisartan shows peculiar features that go beyond blood pressure control. It presents promising and unique protective properties against target end-organ damage, potentially able to open a scenario of new therapeutic approaches to cardiovascular disease.
肾素-血管紧张素-醛固酮系统（RAAS）的调节是治疗高血压的重要途径，其过度表达在靶器官损伤中起着关键作用。替米沙坦是一种血管紧张素 II 受体阻滞剂（ARB），具有独特的药理学特性，包括所有 ARB 中最长的半衰期；这导致血压显著且 24 小时持续降低。替米沙坦具有众所周知的降压特性，但也有强有力的临床证据表明它可减少左心室肥厚、动脉僵硬和心房颤动的复发，并具有肾脏保护作用。
本文回顾了替米沙坦在控制高血压方面的疗效的药理学特性，重要的是，还重点介绍了其新的治疗适应症及其临床意义。
ONTARGET（替米沙坦单独和与雷米普利联合的全球终点试验）表明，替米沙坦具有与雷米普利相似的心血管保护作用，但耐受性更好。此外，最近的研究集中在替米沙坦调节过氧化物酶体增殖物激活受体-γ（PPAR-γ）的能力上，PPAR-γ 是治疗胰岛素抵抗、糖尿病和代谢综合征的既定靶点，其激活也与抗炎和最终抗动脉粥样硬化特性相关。替米沙坦具有超越血压控制的独特特征。它具有针对靶器官损伤的有希望且独特的保护特性，可能为心血管疾病的新治疗方法开辟一个新的局面。
