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Current concepts: renin inhibition in the treatment of hypertension.
Curr Opin Pharmacol. 2008 Apr; 8(2):120-6.CO

Abstract

The development of aliskiren, the first orally effective renin inhibitor, utilized molecular modeling based upon X-ray crystallographic analysis of renin's active site to design a potent, low molecular weight renin inhibitor with improved bioavailability (approximately 2.6%). In patients with hypertension, dose-dependent BP reduction occurs with aliskiren 75-300 mg once daily; at these doses, the safety and tolerability profile is comparable to placebo. In direct comparison studies, BP reduction with aliskiren is equivalent to commonly used antihypertensive agents including diuretics, ACE inhibitors, and ARBs. Persistent BP reduction and prolonged suppression of plasma renin activity (PRA) is observed after aliskiren withdrawal. Aliskiren suppresses PRA when given either as monotherapy or in combination with other agents. When added to an ARB, aliskiren blocks compensatory RAS activation and produces significant additional BP reduction. In patients with diabetic nephropathy, addition of aliskiren to losartan, 100 mg resulted in a 20% greater reduction in proteinuria. Ongoing studies evaluating the long-term renal protective effects of aliskiren and its effects on ventricular remodeling are currently planned or underway.

Authors+Show Affiliations

Division of Cardiovascular Diseases, The Western Pennsylvania Hospital, 4800 Friendship Avenue, North Tower, Suite 3411, Pittsburgh, PA, USA. gradmanmd@aol.comNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

18308634

Citation

Gradman, Alan H., et al. "Current Concepts: Renin Inhibition in the Treatment of Hypertension." Current Opinion in Pharmacology, vol. 8, no. 2, 2008, pp. 120-6.
Gradman AH, Pinto R, Kad R. Current concepts: renin inhibition in the treatment of hypertension. Curr Opin Pharmacol. 2008;8(2):120-6.
Gradman, A. H., Pinto, R., & Kad, R. (2008). Current concepts: renin inhibition in the treatment of hypertension. Current Opinion in Pharmacology, 8(2), 120-6. https://doi.org/10.1016/j.coph.2008.01.003
Gradman AH, Pinto R, Kad R. Current Concepts: Renin Inhibition in the Treatment of Hypertension. Curr Opin Pharmacol. 2008;8(2):120-6. PubMed PMID: 18308634.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Current concepts: renin inhibition in the treatment of hypertension. AU - Gradman,Alan H, AU - Pinto,Rekha, AU - Kad,Rishi, Y1 - 2008/03/04/ PY - 2007/12/05/received PY - 2008/01/07/revised PY - 2008/01/07/accepted PY - 2008/3/1/pubmed PY - 2008/7/23/medline PY - 2008/3/1/entrez SP - 120 EP - 6 JF - Current opinion in pharmacology JO - Curr Opin Pharmacol VL - 8 IS - 2 N2 - The development of aliskiren, the first orally effective renin inhibitor, utilized molecular modeling based upon X-ray crystallographic analysis of renin's active site to design a potent, low molecular weight renin inhibitor with improved bioavailability (approximately 2.6%). In patients with hypertension, dose-dependent BP reduction occurs with aliskiren 75-300 mg once daily; at these doses, the safety and tolerability profile is comparable to placebo. In direct comparison studies, BP reduction with aliskiren is equivalent to commonly used antihypertensive agents including diuretics, ACE inhibitors, and ARBs. Persistent BP reduction and prolonged suppression of plasma renin activity (PRA) is observed after aliskiren withdrawal. Aliskiren suppresses PRA when given either as monotherapy or in combination with other agents. When added to an ARB, aliskiren blocks compensatory RAS activation and produces significant additional BP reduction. In patients with diabetic nephropathy, addition of aliskiren to losartan, 100 mg resulted in a 20% greater reduction in proteinuria. Ongoing studies evaluating the long-term renal protective effects of aliskiren and its effects on ventricular remodeling are currently planned or underway. SN - 1471-4892 UR - https://www.unboundmedicine.com/medline/citation/18308634/Current_concepts:_renin_inhibition_in_the_treatment_of_hypertension_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1471-4892(08)00004-0 DB - PRIME DP - Unbound Medicine ER -