Document Detail

New approaches to blockade of the renin-angiotensin-aldosterone system: characteristics and usefulness of the direct renin inhibitor aliskiren.
MedLine Citation:
PMID:  20675959     Owner:  NLM     Status:  MEDLINE    
Since renin inhibition interferes with the first and rate-limiting steps in the renin-angiotensin system, the renin step is a very attractive target for lowering blood pressure and minimizing target-organ damage. The newly developed direct renin inhibitor aliskiren has several attractive characteristics: it definitively reduces plasma renin activity among inhibitors of the renin-angiotensin system, is remarkably specific for human renin, exhibits a long half-life in plasma comparable to that of amlodipine, and has a high affinity for renal glomeruli and vasculature. Although these characteristics suggest the clinical usefulness and safety of aliskiren, several problems remain unsolved. Why does aliskiren have beneficial effects on the heart and kidneys of patients treated with angiotensin-converting enzyme (ACE) inhibitors and/or angiotensin II type 1-receptor blockers (ARBs)? Is the blood-pressure-lowering effect of aliskiren dependent on the plasma renin activity? Does aliskiren exert a possible adverse effect via (pro)renin receptor-dependent intracellular signals? Here, we review the characteristics and usefulness of aliskiren and discuss the current issues associated with this direct renin inhibitor.
Atsuhiro Ichihara; Mariyo Sakoda; Asako Kurauchi-Mito; Tatsuya Narita; Kenichiro Kinouchi; Kanako Bokuda; Hiroshi Itoh
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Publication Detail:
Type:  Journal Article; Review     Date:  2010-07-27
Journal Detail:
Title:  Journal of pharmacological sciences     Volume:  113     ISSN:  1347-8648     ISO Abbreviation:  J. Pharmacol. Sci.     Publication Date:  2010  
Date Detail:
Created Date:  2010-08-20     Completed Date:  2010-12-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101167001     Medline TA:  J Pharmacol Sci     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  296-300     Citation Subset:  IM    
Department of Anti-Aging Medicine, Keio University School of Medicine, Tokyo, Japan.
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MeSH Terms
Amides / pharmacokinetics,  pharmacology*
Antihypertensive Agents / pharmacokinetics,  pharmacology*
Fumarates / pharmacokinetics,  pharmacology*
Renin / antagonists & inhibitors*
Renin-Angiotensin System / drug effects*
Reg. No./Substance:
0/Amides; 0/Antihypertensive Agents; 0/Fumarates; 0/aliskiren; EC

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