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Updated: May 31, 2026

Improved Renal Denervation Mitigated Hypertension Induced by Angiotensin II Infusion
Published on: May 26, 2022
Aliskiren/amlodipine combination for the treatment of hypertension
Scott S Billecke1, P A Marcovitz
1William Beaumont Hospital, Ministrelli Women's Heart Center, Royal Oak, Michigan 48073, USA. Scott.Billecke@beaumont.edu
Insights
Managing hypertension often requires multiple drugs. The aliskiren/amlodipine pill offers a new approach by directly inhibiting renin, potentially improving blood pressure control and cardiovascular outcomes.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Hypertension management frequently necessitates combination therapy due to the limitations of monotherapy.
- Angiotensin-converting enzyme (ACE) inhibitors and calcium channel blockers (CCBs) combination therapy shows promise in controlling blood pressure and reducing cardiovascular events compared to ACE inhibitor/diuretic regimens.
- However, CCBs, ACE inhibitors, and angiotensin receptor blockers can activate the renin-angiotensin-aldosterone system (RAAS), leading to compensatory increases in plasma renin activity (PRA).
Purpose of the Study:
- To review the mechanisms of action, pharmacodynamics, and safety and efficacy of the aliskiren/amlodipine combination pill for hypertension management.
- To evaluate the impact of aliskiren/amlodipine on PRA and RAAS activation.
- To discuss the clinical implications of direct renin inhibition in antihypertensive combination therapy.
Main Methods:
- This monograph reviews existing preclinical and clinical data on aliskiren and amlodipine.
- Pharmacodynamic effects on PRA and blood pressure are analyzed.
- Safety and efficacy profiles are assessed based on published studies.
Main Results:
- Aliskiren directly inhibits renin, reducing PRA and subsequent angiotensin II production.
- The aliskiren/amlodipine combination demonstrates effective blood pressure reduction.
- Studies indicate a favorable safety profile for the combination therapy.
Conclusions:
- Aliskiren/amlodipine offers a novel approach to hypertension management by directly targeting renin.
- This combination may mitigate RAAS compensatory activation seen with other antihypertensive classes.
- The aliskiren/amlodipine pill presents a potentially valuable option for patients requiring combination therapy for blood pressure control.
Abstract:
The challenge of managing hypertension is exemplified by the limited success of monotherapy and necessity for multiple drug regimens targeting complimentary pathways. Recent evidence suggests that combination therapy including angiotensin-converting enzyme (ACE) inhibitors and calcium channel blockers (CCBs) provides blood pressure control while reducing cardiovascular mortality and morbidity over ACE inhibitor/diuretic therapy. However, CCBs, ACE inhibitors and angiotensin receptor blockers all increase plasma renin activity (PRA), promoting angiotensin I accumulation and angiotensin II production through alternative pathways. While the clinical ramifications of this and other compensatory pathways activating the renin-angiotensin-aldosterone system are unclear, the recently approved aliskiren/amlodipine antihypertensive combination pill has been shown to decrease PRA via aliskiren's direct inhibition of renin. The purpose of this monograph is to review the mechanisms of action, pharmacodynamics, and safety and efficacy profile of the aliskiren/amlodipine combination pill.
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