Aliskiren: clinical experience and future perspectives of renin inhibition.
BACKGROUND
Aliskiren, the first renin inhibitor with sufficient bioavailability for oral use, is now available to clinicians treating hypertension.


OBJECTIVE
The novel mechanism by which aliskiren works was used to provide understanding of its therapeutic and adverse effects.


METHODS
After reviewing physiology and preclinical studies, human studies of aliskiren in hypertension were reviewed. Effects of aliskiren on serum levels and enzymatic activity of renin were explored.


CONCLUSIONS
Aliskiren has antihypertensive efficacy similar to existing medications such as thiazide diuretics, angiotensin-converting enzyme inhibitors and angiotensin receptor blockers, and can be used in drug combinations. Preclinical studies indicate possible cardioprotective and renoprotective effects, similar to other inhibitors of the renin-angiotensin cascade, but future studies are needed in humans.
Sureshkumar
Kalathil K
KK
Allegheny General Hospital, Division of Nephrology and Hypertension, 320 East North Avenue, Pittsburgh, PA 15212, USA. ksureshk@wpahs.org
Vasudevan
Sapna
S
Marcus
Richard J
RJ
Hussain
Sabiha M
SM
McGill
Rita L
RL
D000284:Administration, Oral; D000577:Amides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D004353:Drug Evaluation, Preclinical; D004359:Drug Therapy, Combination; D005650:Fumarates / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D016032:Randomized Controlled Trials as Topic; D012083:Renin / Q000378:metabolism; D000092502:Renin Inhibitors
D000577:Amides; D000959:Antihypertensive Agents; D005650:Fumarates; D012083:Renin; D000092502:Renin Inhibitors; C446481:aliskiren