TY - JOUR
T1 - Oral Direct Renin Inhibition
T2 - Premise, Promise, and Potential Limitations of a New Antihypertensive Drug
AU - Shafiq, Moiz M.
AU - Menon, Dileep V.
AU - Victor, Ronald G.
N1 - Funding Information:
Funded by the National Institutes of Health training grant in cardiovascular disease, T32-HL07360-29 (Dr Shafiq), American Society of Hypertension Fellowship grant (Dr Menon), and National Institutes of Health RO-1 HL044010 and the Donald W. Reynolds Foundation (Dr Victor). Dr Victor is on the Scientific Advisory Board of Novartis and CVRx, and is the recipient of research grants from Pfizer and Aetna Foundation.
PY - 2008/4
Y1 - 2008/4
N2 - The first oral direct renin inhibitor, aliskiren, recently received approval for the treatment of hypertension. This article addresses the premise, promise, and potential limitations of this new class of renin-angiotensin system inhibitor. Although aliskiren adds to a list of more than 100 drugs approved for the treatment of hypertension, its introduction into clinical medicine is of particular interest because of the novel mechanism of action: inhibition of renin's catalytic activity, the most proximal and rate-limiting step in renin-angiotensin system activation. By producing more complete renin-angiotensin system inhibition than with existing agents, direct renin inhibitors may afford greater protection from hypertensive complications. Other potential advantages include additional blood pressure reduction when used in combination therapy, a placebo-like side-effect profile, avid renal concentration, and long duration of action. Potential limitations include modest levels of blood pressure reduction that are equivalent to but not greater than angiotensin receptor blockers, reduced gastrointestinal absorption with a high-fat meal, and large reactive increases in renin secretion-the functional importance of which is under intense investigation. The results of outcomes trials are eagerly awaited.
AB - The first oral direct renin inhibitor, aliskiren, recently received approval for the treatment of hypertension. This article addresses the premise, promise, and potential limitations of this new class of renin-angiotensin system inhibitor. Although aliskiren adds to a list of more than 100 drugs approved for the treatment of hypertension, its introduction into clinical medicine is of particular interest because of the novel mechanism of action: inhibition of renin's catalytic activity, the most proximal and rate-limiting step in renin-angiotensin system activation. By producing more complete renin-angiotensin system inhibition than with existing agents, direct renin inhibitors may afford greater protection from hypertensive complications. Other potential advantages include additional blood pressure reduction when used in combination therapy, a placebo-like side-effect profile, avid renal concentration, and long duration of action. Potential limitations include modest levels of blood pressure reduction that are equivalent to but not greater than angiotensin receptor blockers, reduced gastrointestinal absorption with a high-fat meal, and large reactive increases in renin secretion-the functional importance of which is under intense investigation. The results of outcomes trials are eagerly awaited.
KW - Aliskiren
KW - Angiotensin
KW - Hypertension
KW - Renin
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U2 - 10.1016/j.amjmed.2007.11.016
DO - 10.1016/j.amjmed.2007.11.016
M3 - Review article
C2 - 18374681
AN - SCOPUS:41149143631
VL - 121
SP - 265
EP - 271
JO - American Journal of Medicine
JF - American Journal of Medicine
SN - 0002-9343
IS - 4
ER -