Serum concentration and effects of a single dose of enalapril maleate in patients with essential hypertension.
The antihypertensive effect of a non-sulfhydryl, long acting ACE (angiotensin converting enzyme) inhibitor, MK-421, was evaluated by administering a single dose of 10 mg to 13 patients with mild to moderate essential hypertension. The pharmacokinetic profile of MK-421 and its potent active metabolite, MK-422, was also assessed, together with the effect on the various components of the renin-angiotensin system. A single dose of MK-421 produced a significant fall in MBP from 2 to 24 hours post-drug. As could be expected, plasma ACE activity was suppressed up to 24 hours after MK-421. The half-life of MK-422, Cmax and [AUC]24(0) of MK-421 and MK-422 were measured. No significant change in plasma bradykinin or urinary excretion rate of kallikrein was observed, whereas a slight increase was observed in the urinary excretion rate of kinins after MK-421 in 8 patients. Significant correlations were observed between pretreatment PRA levels and the maximum fall in MBP.
Shionoiri
H
H
Gotoh
E
E
Miyazaki
N
N
Yasuda
G
G
Takagi
N
N
Uneda
S
S
Kaneko
Y
Y
D000328:Adult; D000368:Aged; D001794:Blood Pressure; D001920:Bradykinin / Q000097:blood; D004151:Dipeptides / Q000008:administration & dosage* / Q000097:blood; D004656:Enalapril; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D007700:Kinetics; D007705:Kinins / Q000652:urine; D008297:Male; D008875:Middle Aged; D012084:Renin-Angiotensin System
D004151:Dipeptides; D007705:Kinins; D004656:Enalapril; D001920:Bradykinin