Exercise tolerance in angina is improved by mivazerol--an alpha 2-adrenoceptor agonist.
In a double-blind, placebo-controlled, randomized trial of treadmill exercise tolerance in six patients with chronic stable angina, intravenous mivazerol 1 microgram, 2 micrograms, and 3 micrograms/kg increased the time to onset of angina by 39%, 48%, and 76%; the time to 1-mm ST depression by 36%, 76%, and 104%; and total exercise duration by 15%, 23%, and 30%, respectively. In a subsequent double-blind, placebo-controlled, randomized trial involving a further 12 patients, a single oral dose of mivazerol of 800 micrograms, 1200 micrograms, and 1600 micrograms increased the time to onset of angina by 4%, 11%, and 30%; the time to 1-mm ST depression by 33%, 43%, and 53%; and the total exercise duration by 10%, 18%, and 23%, respectively. Mivazerol is an imidazole derivative with agonist properties at the alpha 2-adrenoceptor and appears to be an effective antianginal. Mivazerol may improve exercise performance by attenuating the effects of exercise-induced sympathetic nervous system activity on the ischemic myocardium.
Wright
R A
RA
Cardiovascular Research Unit, University of Edinburgh, Scotland.
Decroly
P
P
Kharkevitch
T
T
Oliver
M F
MF
D000284:Administration, Oral; D000316:Adrenergic alpha-Agonists / Q000627:therapeutic use*; D000328:Adult; D000368:Aged; D000787:Angina Pectoris / Q000188:drug therapy* / Q000503:physiopathology; D004311:Double-Blind Method; D005080:Exercise Test; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000009:adverse effects / Q000627:therapeutic use*; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D017202:Myocardial Ischemia / Q000188:drug therapy / Q000209:etiology; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects* / Q000502:physiology
D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D018341:Receptors, Adrenergic, alpha-2; C087969:mivazerol