Mineralocorticoid receptor blocker eplerenone improves endothelial function and inhibits Rho-associated kinase activity in patients with hypertension.
Hypertension is associated with endothelial dysfunction and activated Rho-associated kinases (ROCKs). The purpose of this study was to evaluate the effects of the selective mineralocorticoid receptor blocker, eplerenone, on endothelial function and ROCK activity in patients with hypertension. The study was carried out over 48 weeks in 60 untreated patients with hypertension who were randomly assigned to eplerenone, nifedipine, and losartan groups. We evaluated the effects of each treatment on flow-mediated vasodilation (FMD) and ROCK activity in peripheral leukocytes. Eplerenone increased FMD and decreased leukocyte ROCK activity. Nifedipine decreased ROCK activity but did not alter FMD. Losartan increased FMD but did not alter ROCK activity. Hypotensive effects were similar in the three groups, as was nitroglycerin-induced vasodilation during the follow-up period. There were no significant differences between the groups with respect to other parameters. The study results show that eplerenone improves endothelial function and inhibits ROCK activity in patients with essential hypertension.
Analysis Center of Life Science, Hiroshima University, Hiroshima, Japan.
N
N
Fujimura
K
K
Noma
T
T
Hata
J
J
Soga
T
T
Hidaka
N
N
Idei
Y
Y
Fujii
S
S
Mikami
T
T
Maruhashi
Y
Y
Iwamoto
Y
Y
Kihara
K
K
Chayama
H
H
Kato
J K
JK
Liao
Y
Y
Higashi
D047228:Angiotensin II Type 1 Receptor Blockers / Q000494:pharmacology / Q000627:therapeutic use; D002121:Calcium Channel Blockers / Q000494:pharmacology / Q000627:therapeutic use; D002465:Cell Movement / Q000187:drug effects; D004730:Endothelium, Vascular / Q000187:drug effects* / Q000502:physiology; D000077545:Eplerenone; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000201:enzymology / Q000503:physiopathology; D007962:Leukocytes / Q000201:enzymology; D019808:Losartan / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D000451:Mineralocorticoid Receptor Antagonists / Q000494:pharmacology* / Q000627:therapeutic use*; D009543:Nifedipine / Q000494:pharmacology / Q000627:therapeutic use; D005996:Nitroglycerin / Q000494:pharmacology; D013148:Spironolactone / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D013234:Stem Cells / Q000187:drug effects; D042461:Vascular Endothelial Growth Factor A / Q000819:agonists; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
D047228:Angiotensin II Type 1 Receptor Blockers; D002121:Calcium Channel Blockers; D000451:Mineralocorticoid Receptor Antagonists; D042461:Vascular Endothelial Growth Factor A; D013148:Spironolactone; D000077545:Eplerenone; D054460:rho-Associated Kinases; D005996:Nitroglycerin; D009543:Nifedipine; D019808:Losartan