Department of Pharmacotherapy & Outcomes Science, Virginia Commonwealth University School of Pharmacy, 410 N. 12th St., Smith Building, 6th floor, Room 660, Richmond, VA, USA.
Department of Pharmacy Practice, College of Pharmacy, Qassim University, Buraydah, Saudi Arabia.
Curr Hypertens Rep. 2023 Sep;25(9):243-250. doi: 10.1007/s11906-023-01248-2. Epub 2023 Jun 7.
This review describes the discovery and development of ACE inhibitors as antihypertensive agents, compares their efficacy, tolerability, and safety to ARBs, and highlights the contemporary issues surrounding ACE inhibitor use for HTN.
Angiotensin-converting enzyme (ACE) inhibitors are commonly prescribed medications for the management of hypertension (HTN) and other chronic conditions including heart failure and chronic kidney disease. These agents inhibit ACE, the enzyme that is responsible for converting angiotensin (AT) I to AT II. Inhibiting the synthesis of AT II causes arterial and venous vasodilation, natriuresis, and a decrease in sympathetic activity, resulting in the reduction of blood pressure. ACE inhibitors are first-line therapy in HTN management along with thiazide diuretics, calcium channel blockers, and angiotensin receptor blockers (ARB). Along with inhibiting AT II synthesis, inhibition of ACE causes accumulation of bradykinin, increasing the risk of bradykinin-mediated side effects like angioedema and cough. Since ARBs do not work on ACE in the renin-angiotensin system, the risk of angioedema and cough are lower with ARBs. Recent evidence has also suggested ARBs may have neuroprotective effects compared to other antihypertensives, including ACE inhibitors; however, this warrants further study. Currently, ACE inhibitors and ARBs have an equal class of recommendation for first-line treatment for the management of HTN. Recent evidence has shown ARBs to be just as effective as ACE inhibitors for HTN but with improved tolerability.
本篇综述描述了血管紧张素转换酶（ACE）抑制剂作为抗高血压药物的发现和发展，比较了它们与血管紧张素受体阻滞剂（ARB）的疗效、耐受性和安全性，并强调了 ACE 抑制剂在高血压治疗中当前面临的问题。
血管紧张素转换酶（ACE）抑制剂是常用于治疗高血压（HTN）和心力衰竭、慢性肾脏病等其他慢性疾病的处方药物。这些药物可抑制 ACE，该酶可将血管紧张素（AT）I 转化为 AT II。抑制 AT II 的合成可导致动脉和静脉扩张、利钠和交感神经活性降低，从而降低血压。ACE 抑制剂是高血压管理的一线治疗药物，与噻嗪类利尿剂、钙通道阻滞剂和 ARB 联合使用。除了抑制 AT II 的合成外，ACE 抑制剂还会导致缓激肽的蓄积，增加缓激肽介导的副作用（如血管性水肿和咳嗽）的风险。由于 ARB 不会在肾素-血管紧张素系统中作用于 ACE，因此 ARB 引起血管性水肿和咳嗽的风险较低。最近的证据还表明，与其他降压药（包括 ACE 抑制剂）相比，ARB 可能具有神经保护作用；但这需要进一步研究。目前，ACE 抑制剂和 ARB 具有同等的一线推荐类别，用于治疗高血压。最近的证据表明，ARB 与 ACE 抑制剂一样有效治疗高血压，但耐受性更好。
