Olmesartan, an AT1-selective antihypertensive agent

被引:12
作者
Chilman-Blair, K [1 ]
Rabasseda, X [1 ]
机构
[1] Prous Sci, Dept Med Informat, Barcelona 08025, Spain
关键词
D O I
10.1358/dot.2003.39.10.799468
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Olmesartan is an angiotensin II receptor antagonist indicated for the treatment of essential hypertension. Angiotensin II is an important hormonal effector and end-product of the renin-angiotensin system. When it binds to its endogenous receptor sites, it causes widespread vasoconstriction and a subsequent increase in blood pressure. Olmesartan works by selectively binding to AT(1) receptors, thereby reducing the vasoconstrictive activity of angiotensin II through action at these sites. Olmesartan is the newest angiotensin II receptor antagonist to enter the market. It has attracted interest due to its superior efficacy compared to all other drug candidates in its class, combined with a tolerability profile comparable to that of placebo. The reduced incidence of adverse events following olmesartan administration has implications for both patient compliance rates and subsequent blood pressure control. The first-line treatment for hypertension is currently through angiotensin converting enzyme (ACE) inhibitors, which work by blocking a separate part of the same renin-angiotensin pathway. Angiotensin II receptor antagonists are, as a class, often utilized as an alternative to ACE inhibitors, although until now they have been less effective. Angiotensin II receptor antagonists have generally been prescribed when patients are not able to tolerate the side-effects associated with ACE inhibition (e.g., ACE inhibitors are renowned for causing an irritating cough). Opinion is changing, however, due to emerging evidence suggesting that olmesartan is at least as effective as its ACE predecessors and is associated with a much more favorable tolerability profile. The hypotensive efficacy of olmesartan has been reported in many clinical studies. A clear dose-dependent relationship is exhibited between olmesartan 10-80 mg/day and resultant decreases in both diastolic and systolic blood pressures. The efficacy of olmesartan has been observed to plateau between 20-40 mg/day; therefore, a once-daily 20 mg dose is currently recommended. Olmesartan has been proven to be as effective as other commonly administered antihypertensives, including atenolol, captopril and felodipine, and its efficacy profile is unrelated to patient age, sex or ethnicity. Olmesartan has also been associated with a number of cardioprotective and reno-protective effects. Animal studies have identified that olmesartan provides protection against the pathophysiologic events leading to diabetic nephropathy and cardiovascular morbidity/mortality. This end-organ protection is independent of olmesartan's blood pressure lowering properties and is therefore thought to be mediated by different mechanisms. In summary, olmesartan has an efficacy profile superior to other available anti hypertensive agents, with a tolerability profile comparable to that of placebo. In addition, the convenience of its once-daily dosing means that olmesartan should be considered not only as an alternative, but also as a first-line treatment for patients with mild to severe essential hypertension. Thus, olmesartan appears to be a very promising new therapy for the treatment of hypertension. (C) 2003 Prous Science. All rights reserved.
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页码:745 / 761
页数:17
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