| Direct renin inhibitors as antihypertensive agents. | |
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MedLine Citation:
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PMID: 20479579 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Hypertension, a serious disease affecting almost a billion people (25% of adults) worldwide, is a major modifiable risk factor for cardiovascular (CV) and renal disease. Despite numerous advances in the pharmacologic treatment of high blood pressure (BP) and availability of several antihypertensive drugs to treat hypertension, a significant proportion of treated hypertensive patients still have uncontrolled high BP, and thus, face serious morbidity and mortality. Furthermore, it is not sufficient to aim for optimum BP control, but to treat all CV risk factors, protect end-organ damage, prevent progression of disease, and prevent long-range adverse effects of the drugs. Therefore, new therapeutic modalities have to be developed to achieve the above objectives. Some years ago, investigators identified renin inhibition as the preferred pharmacologic approach to blockade of the renin-angiotensin system. Renin is a monospecific enzyme that catalyzes the rate-limiting step in the synthesis of angiotensin II. Amplified enzymatic activity and additional physiologic effects occur when renin and prorenin bind to the (pro)renin receptor. Until very recently, development of clinically effective renin inhibitors remained elusive but molecular modeling was used to develop aliskiren and other renin inhibitors that produce sustained suppression of plasma renin activity after oral administration with a dose-dependent BP. Additional studies will ultimately determine the place of renin inhibition in the treatment of hypertension and related CV disorders. |
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Authors:
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Zafar H Israili; Manuel Velasco; Valmore Bermúdez |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: American journal of therapeutics Volume: 17 ISSN: 1536-3686 ISO Abbreviation: Am J Ther Publication Date: 2010 May-Jun |
Date Detail:
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Created Date: 2010-05-18 Completed Date: 2010-08-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9441347 Medline TA: Am J Ther Country: United States |
Other Details:
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Languages: eng Pagination: 237-54 Citation Subset: IM |
Affiliation:
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Emory University School of Medicine, Department of Medicine, Atlanta, GA 30303, USA. zisrail@emory.edu |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amides
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adverse effects,
pharmacology,
therapeutic use Animals Antihypertensive Agents / adverse effects, pharmacology*, therapeutic use Blood Pressure / drug effects Cardiovascular Diseases / etiology, prevention & control Drug Design Fumarates / adverse effects, pharmacology, therapeutic use Humans Hypertension / complications, drug therapy*, physiopathology Models, Molecular Renin / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/Amides; 0/Antihypertensive Agents; 0/Fumarates; 0/aliskiren; EC 3.4.23.15/Renin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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