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A Modified Two Kidney One Clip Mouse Model of Renin Regulation in Renal Artery Stenosis
Published on: October 26, 2020
Direct renin inhibition: focus on aliskiren
1Baylor College of Medicine, Houston, TX 77030, USA. jpool@bcm.edu
Journal of Managed Care Pharmacy : JMCP
|November 22, 2007
Summary
Aliskiren, a direct renin inhibitor (DRI), effectively lowers blood pressure (BP) and blocks the renin-angiotensin aldosterone system (RAAS). It is a safe and well-tolerated option for hypertension management, used alone or with other drugs.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Hypertension remains a significant health concern, with many patients experiencing uncontrolled blood pressure despite treatment.
- The renin-angiotensin aldosterone system (RAAS) is a crucial target for managing blood pressure, cardiovascular health, and renal protection.
- Renin, the rate-limiting enzyme in the RAAS cascade, presents an optimal target for RAAS suppression.
Purpose of the Study:
- To provide a comprehensive overview of the direct renin inhibitor (DRI) aliskiren.
- To summarize its pharmacology, pharmacokinetics, and preclinical and clinical efficacy and safety data.
Main Methods:
- Review of preclinical studies and clinical trials (Phase II and III) evaluating aliskiren.
- Assessment of aliskiren's effects on blood pressure, plasma renin activity, and the RAAS.
- Evaluation of aliskiren as monotherapy and in combination with other antihypertensive agents.
Main Results:
- Aliskiren is a potent and specific renin inhibitor with favorable pharmacokinetics for once-daily dosing.
- It demonstrated dose-dependent blood pressure reduction, inhibition of plasma renin activity, and renal protection in animal models.
- Clinical trials showed significant blood pressure lowering with aliskiren monotherapy and enhanced efficacy when combined with other antihypertensives, with good tolerability.
Conclusions:
- Aliskiren offers more complete RAAS blockade compared to downstream inhibitors.
- As a direct renin inhibitor (DRI), aliskiren is a safe and effective antihypertensive agent.
- It provides valuable therapeutic options for improving blood pressure control, either as monotherapy or in combination regimens.
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