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ACE-Inhibitors in Hypertension: A Historical Perspective and Current Insights

  • Antihypertensive Agents: Mechanisms of Drug Action (M Ernst, Section Editor)
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Abstract

Purpose of Review

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.

Recent Findings

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.

Summary

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.

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Authors and Affiliations

  1. Department of Pharmacotherapy & Outcomes Science, Virginia Commonwealth University School of Pharmacy, 410 N. 12th St., Smith Building, 6th floor, Room 660, Richmond, VA, USA

    Stacey Cutrell, Ibrahim S. Alhomoud, Azita H. Talasaz, Benjamin Van Tassell & Dave L. Dixon

  2. Department of Pharmacy Practice, College of Pharmacy, Qassim University, Buraydah, Saudi Arabia

    Ibrahim S. Alhomoud

  3. Division of Cardiology, Virginia Commonwealth University, Richmond, VA, USA

    Anurag Mehta

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Correspondence to Dave L. Dixon.

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Conflict of Interest

Anarug Menta—Research Grant from VCU Health Pauley Heart Center. Benjamin VanTassell—Novo Nordisk Research Grant, Novartis Research Grant, Kiniksa Pharmaceuticals Consulting Fees, and Implicit Bioscience Consulting Fees. Dave Dixon—Boehringer Ingelheim Research Grant. Stacey Cutrell, Ibrahim S. Alhomoud, and Azita Talasaz declare that they have no conflict of interest.

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Cutrell, S., Alhomoud, I.S., Mehta, A. et al. ACE-Inhibitors in Hypertension: A Historical Perspective and Current Insights. Curr Hypertens Rep 25, 243–250 (2023). https://doi.org/10.1007/s11906-023-01248-2

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