Ruilope L
Hypertension Unit, Hospital 12 de Octubre, Madrid, Spain.
J Hypertens Suppl. 1997 Dec;15(7):S15-20.
Inhibition of the renin-angiotensin system has been the focus of considerable research as the enzymatic pathway resulting in the production of angiotensin II is implicated in the development of hypertension and cardiovascular disease.
Blocking the renin-angiotensin system with angiotensin converting enzyme (ACE) inhibitors is an effective blood pressure control measure, but is less than ideal due to incomplete blockade and the effects of concomitant blockade of kinase II.
Angiotensin II receptor antagonists block the renin-angiotensin system at the receptor level, and thus impede the system regardless of the pathway responsible for the formation of ACE. Irbesartan is a new, unique angiotensin II receptor antagonist with favorable pharmacokinetic/pharmacodynamic properties that are close to ideal for an antihypertensive agent. Irbesartan is a specific AT1 receptor antagonist with rapid oral bioavailability (peak plasma concentrations occurring at 1.5-2 h after administration) and a long half-life (11-15 h) that provides 24-h blood pressure control with a single daily dose. The maximal blood pressure fall occurs between 3 and 6 h after the dose. Unlike other angiotensin II receptor antagonists, irbesartan is relatively unaffected by food or drugs.
The pharmacokinetic/pharmacodynamic properties of irbesartan have been demonstrated to provide superior blood pressure control and tolerability in all classes of hypertension and patient populations.
肾素-血管紧张素系统的抑制一直是大量研究的焦点，因为导致血管紧张素II产生的酶促途径与高血压和心血管疾病的发展有关。
用血管紧张素转换酶（ACE）抑制剂阻断肾素-血管紧张素系统是一种有效的血压控制措施，但由于阻断不完全以及激酶II的伴随阻断作用，其效果并不理想。
血管紧张素II受体拮抗剂：血管紧张素II受体拮抗剂在受体水平阻断肾素-血管紧张素系统，因此无论负责ACE形成的途径如何，都能阻碍该系统。厄贝沙坦是一种新型独特的血管紧张素II受体拮抗剂，具有良好的药代动力学/药效学特性，接近理想的抗高血压药物。厄贝沙坦是一种特异性AT1受体拮抗剂，口服生物利用度高（给药后1.5 - 2小时达到血浆峰浓度），半衰期长（11 - 15小时），每日单剂量即可实现24小时血压控制。给药后3至6小时血压下降最大。与其他血管紧张素II受体拮抗剂不同，厄贝沙坦相对不受食物或药物影响。
已证明厄贝沙坦的药代动力学/药效学特性在所有类型的高血压和患者群体中均能提供更好的血压控制和耐受性。
