Document Detail


Direct renin inhibitors as antihypertensive agents.
MedLine Citation:
PMID:  20479579     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Zafar H Israili; Manuel Velasco; Valmore Bermúdez
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  American journal of therapeutics     Volume:  17     ISSN:  1536-3686     ISO Abbreviation:  Am J Ther     Publication Date:    2010 May-Jun
Date Detail:
Created Date:  2010-05-18     Completed Date:  2010-08-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9441347     Medline TA:  Am J Ther     Country:  United States    
Other Details:
Languages:  eng     Pagination:  237-54     Citation Subset:  IM    
Affiliation:
Emory University School of Medicine, Department of Medicine, Atlanta, GA 30303, USA. zisrail@emory.edu
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MeSH Terms
Descriptor/Qualifier:
Amides / 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:
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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