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Antihypertensive Drugs: Direct Renin Inhibitors

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The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...

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Related Experiment Video

Updated: May 7, 2026

A Modified Two Kidney One Clip Mouse Model of Renin Regulation in Renal Artery Stenosis

A Modified Two Kidney One Clip Mouse Model of Renin Regulation in Renal Artery Stenosis

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Renin-angiotensin system blocking drugs.

Nicolás Roberto Robles¹, Isis Cerezo, Roman Hernandez-Gallego

¹1Cardiovascular Risk Chair, University of Salamanca School of Medicine, Salamanca, Spain.

Journal of Cardiovascular Pharmacology and Therapeutics

|September 17, 2013

Summary

This review covers drugs targeting the renin-angiotensin system (RAS), including angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers (ARBs). It discusses their efficacy in managing hypertension and cardiovascular events, and the role of direct renin inhibitors.

Keywords:

hypertension renin–angiotensin system

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Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

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Published on: June 7, 2016

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Last Updated: May 7, 2026

A Modified Two Kidney One Clip Mouse Model of Renin Regulation in Renal Artery Stenosis

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Published on: October 26, 2020

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

Area of Science:

Pharmacology
Cardiovascular Medicine
Nephrology

Background:

The renin-angiotensin system (RAS) plays a crucial role in regulating blood pressure and fluid balance.
Angiotensin-converting enzyme (ACE) inhibitors and selective AT1 receptor blockers (ARBs) are established drug classes targeting the RAS for hypertension management.
Direct renin inhibition offers a proximal blockade of the RAS, with aliskiren being a key example.

Purpose of the Study:

To provide an updated review of current knowledge on RAS-blocking drugs in clinical practice.
To explore the therapeutic implications of differing mechanisms of action among RAS-targeting drugs.
To summarize the efficacy and clinical outcomes associated with ACE inhibitors, ARBs, and direct renin inhibitors, including combination therapies.

Main Methods:

Literature review of clinical studies and therapeutic guidelines.
Analysis of drug mechanisms of action and their impact on related pathways.
Evaluation of clinical trial data on the efficacy and safety of RAS-blocking agents in hypertension, heart failure, and renal disease.

Main Results:

ACE inhibitors and ARBs are effective antihypertensive agents that reduce cardiovascular and renal event risks.
Direct renin inhibitors, like aliskiren, are efficacious for hypertension management.
Combined therapy with direct renin inhibitors and ACE inhibitors or ARBs has shown varied results in conditions like heart failure and proteinuria.

Conclusions:

RAS-blocking drugs, including ACE inhibitors, ARBs, and direct renin inhibitors, are vital in managing cardiovascular and renal diseases.
Understanding the distinct mechanisms of action is key to optimizing therapeutic strategies.
Further research is needed to fully elucidate the benefits and risks of combined RAS blockade therapies.