| Direct inhibition of renin as a cardiovascular pharmacotherapy: focus on aliskiren. | |
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MedLine Citation:
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PMID: 17700383 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The important role of renin-angiotensin-aldosterone system blockade in the treatment of systemic hypertension, heart failure, diabetic kidney disease, and atherogenesis has been clearly established. The theoretical therapeutic advantages for inhibiting the detrimental effects of the renin-angiotensin system at its most upstream point have served as the impetus for the development of renin inhibitors. The advent of aliskiren, the first in a novel class of orally active, nonpeptide, highly specific, human renin inhibitors, provides a new modality in the armamentarium of renin-angiotensin system antagonists. Studies in marmosets and rats demonstrated that aliskiren reduced blood pressure in a dose-dependent manner and is highly efficacious in blocking plasma renin activity with parallel reductions in the levels of the other downstream constituents of the renin-angiotensin system. Clinical trials in hypertensive patients have confirmed these benefits with aliskiren whose blood pressure-lowering efficacy is similar to or better than those of standard therapeutic doses of enalapril, losartan, irbesartan, and hydrochlorothiazide. Aliskiren is well tolerated, with few reported adverse effects even at the highest doses tested. Given the established beneficial effects of angiotensin-converting enzyme inhibitors and angiotensin receptor blockers in the treatment of cardiovascular and renovascular diseases, future studies may further elucidate a similar protective role for aliskiren both as a monotherapy and as part of a combination therapy. |
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Authors:
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Reza Sepehrdad; William H Frishman; Charles T Stier; Domenic A Sica |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Cardiology in review Volume: 15 ISSN: 1538-4683 ISO Abbreviation: Cardiol Rev Publication Date: 2007 Sep-Oct |
Date Detail:
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Created Date: 2007-08-16 Completed Date: 2007-09-06 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9304686 Medline TA: Cardiol Rev Country: United States |
Other Details:
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Languages: eng Pagination: 242-56 Citation Subset: IM |
Affiliation:
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Department of Internal Medicine, UC Davis Medical Center, Sacramento, California, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aldosterone
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blood Amides / adverse effects, chemistry, pharmacokinetics, pharmacology, therapeutic use* Angiotensin II / blood, physiology Angiotensin-Converting Enzyme Inhibitors / therapeutic use Animals Antihypertensive Agents / adverse effects, pharmacology*, therapeutic use Biphenyl Compounds / pharmacology, therapeutic use Blood Pressure / drug effects, physiology Fumarates / adverse effects, chemistry, pharmacokinetics, pharmacology, therapeutic use* Humans Kidney / blood supply Piperazines / pharmacology, therapeutic use Randomized Controlled Trials as Topic Receptors, Angiotensin / drug effects, physiology Regional Blood Flow Renin / antagonists & inhibitors*, physiology Renin-Angiotensin System / drug effects, physiology Structure-Activity Relationship Tetrazoles / pharmacology, therapeutic use Thiazoles / pharmacology, therapeutic use |
| Chemical | |
Reg. No./Substance:
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0/Amides; 0/Angiotensin-Converting Enzyme Inhibitors; 0/Antihypertensive Agents; 0/Biphenyl Compounds; 0/Fumarates; 0/Piperazines; 0/Receptors, Angiotensin; 0/Tetrazoles; 0/Thiazoles; 0/aliskiren; 11128-99-7/Angiotensin II; 138402-11-6/irbesartan; 138742-43-5/zankiren hydrochloride; 52-39-1/Aldosterone; EC 3.4.23.15/Renin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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