Exercise tolerance in angina is improved by mivazerol—An alpha2-adrenoceptor agonist
- 15 Downloads
In a double-blind, placebo-controlled, randomized trial of treadmill exercise tolerance in six patients with chronic stable angina, intravenous mivazerol 1 µg, 2 µg, and 3 µg/kg increased in 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 µg, 1200 µg, and 1600 µg 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 alpha2-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.
Key Wordsmivazerol alpha2 adrenoceptor angina exercise tolerance
Unable to display preview. Download preview PDF.
- 2.Kharkevitch T, Guyaux M, Gobert J, Wulfert E. Mivazerol. A new α2-receptor agonist reduces ischaemia produced by coronary occlusion in rats and dogs.Cardiovasc Drugs Ther 1991;5:S407.Google Scholar
- 3.Kharkevitch T, Noyer M, Guyaux M, Riemersma RA, Gobert JK, Wulfert E. Mivazerol, a new α2-adrenergic agonist with anti-ischaemic effects in animal models of myocardial ischaemia. In:Proc Eur Assoc Cardiothorac Anaesthesiologists, 1992.Google Scholar
- 4.Du XJ, Hoet B, Kharkevitch T, Riemersma RA. Mivazerol inhibits neuronal norepinephrine release during myocardial ischaemia.J Mol Cell Cardiol 1992;24:S21.Google Scholar
- 6.Prichard BNC, Aelling WH, Richardson GA. The action of intravenous oxprenolol, practolol, propranolol and sotalol on acute exercise tolerance in angina pectoris: The effect on heart rate and the electrocardiogram.Postgrad Med J 1970;43(Nov suppl):77–83.Google Scholar
- 10.Thomas MG, Quiroz AC, Rice JC, Sander GE, Giles TD. Anti-anginal effects of clonidine.J Cardiovasc Pharmacol 1986;8(Suppl 3):S69-S75.Google Scholar
- 16.Seitelberger R, Guth BD, Heusch G, Lee JD, Katayama K, Ross J Jr. Intracoronary α2-adrenergic receptor blockade attenuates ischaemia in conscious dogs during exercise.Circ Res 1988;62:536–542.Google Scholar