Burnier M, Waeber B, Brunner H R
Division of Hypertension, CHUV, Lausanne, Switzerland.
J Hypertens Suppl. 1994 Jul;12(2):S7-15.
New approaches to renin-angiotensin blockade: The successful use of angiotensin converting enzyme (ACE) inhibitors in the treatment of hypertension and congestive heart failure has generated a great deal of research interest in developing new pharmacological approaches to block the renin-angiotensin system. In recent years, several new non-peptide angiotensin II antagonists have been synthesized and some of them are available for experimental and/or clinical investigations. Now that experience with the antagonist losartan is accumulating, it is important to compare the effects, the efficacy and the side effects of this agent with those of ACE inhibitors. Effects of losartan compared with ACE inhibitors: So far, ACE inhibitors and the angiotensin II antagonist losartan appear to have similar systemic and regional hemodynamic effects. The impact of ACE inhibition and angiotensin blockade on the various components of the renin-angiotensin system is also comparable except for a marked increase in plasma angiotensin II levels during angiotensin II blockade. This increase in circulating angiotensin II might theoretically lead to an excessive stimulation of the AT2 receptor subtype, but since the function of this receptor is not known it is impossible to evaluate the implications of this reactive rise. Renal effects of losartan: The renal effects of angiotensin II antagonists are also very similar to those of ACE inhibitors. However, a marked increase in uric acid excretion has been observed with the administration of losartan. This uricosuric effect of losartan might represent a clinical advantage unless a state of urinary supersaturation of undissociated uric acid is achieved.(ABSTRACT TRUNCATED AT 250 WORDS)
肾素 - 血管紧张素阻断的新方法：血管紧张素转换酶（ACE）抑制剂在治疗高血压和充血性心力衰竭方面的成功应用引发了大量关于开发阻断肾素 - 血管紧张素系统新药理学方法的研究兴趣。近年来，几种新型非肽类血管紧张素II拮抗剂已被合成，其中一些可用于实验和/或临床研究。鉴于氯沙坦拮抗剂的经验不断积累，将该药物与ACE抑制剂的效果、疗效及副作用进行比较很重要。氯沙坦与ACE抑制剂的效果比较：到目前为止，ACE抑制剂和血管紧张素II拮抗剂氯沙坦似乎具有相似的全身和局部血流动力学效应。除了在血管紧张素II阻断期间血浆血管紧张素II水平显著升高外，ACE抑制和血管紧张素阻断对肾素 - 血管紧张素系统各组分的影响也具有可比性。循环中血管紧张素II的这种升高理论上可能导致AT2受体亚型的过度刺激，但由于该受体的功能尚不清楚，因此无法评估这种反应性升高的影响。氯沙坦的肾脏效应：血管紧张素II拮抗剂的肾脏效应也与ACE抑制剂非常相似。然而，服用氯沙坦后观察到尿酸排泄显著增加。氯沙坦的这种促尿酸尿作用可能代表一种临床优势，除非达到未离解尿酸的尿过饱和状态。（摘要截选至250字）
