To assess the efficacy of oral betaxolol in the treatment of stable exertional angina pectoris and to determine the relationship between betaxolol doses/serum concentrations and clinical/hemodynamic responses the authors studied 24 patients prior to and following stepwise administration of 5, 10, 20, 40, and 80 mg doses. The major endpoint for the study was the achievement of clinical beta blockade (heart rate 50-60 beats/min and ≤ 20% rise in treadmill stage I heart rate). Betaxolol produced a decrease in mean angina pectoris frequency from 6.6 ± 1.9 episodes/week with placebo to 0.2 ± 0.5 episode/week during clinical beta blockade (p < 0.00005). Mean treadmill exercise time increased from 3.1 ± 1.7 min with placebo to 7.3 ± 2.3 min with doses sufficient to reduce angina pectoris frequency ≥ 75% (p < 0.00005) and to 8.0 ± 2.3 min during clinical beta blockade (p < 0.00005). The mean doses of betaxolol required to produce a ≥ 75% decrease in angina pectoris frequency and clinical beta blockade were 12 ± 5 mg (range 5-40 mg) and 28 ± 29 mg (range 5-80 mg) respectively. Mean serum concentrations associated with these clinical endpoints were 23.8 ± 9.7 ng/mL and 59.7 ± 54.0 ng/mL respectively. The results indicate that betaxolol, in widely ranging doses, is highly effective in reducing angina pectoris frequency and improving exercise capacity in patients with stable exertional angina pectoris.
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References
1.
Beresford R., Heel RC: Betaxolol: A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in hypertension. Drugs31:6-28, 1986.
2.
Ferrandes B., Durand A., Andre-Fraisse P., et al: Pharmacokinetics and metabolism of betaxolol in various animal Species and man. In: Betaxolol and Other Beta-1 Adrenergic Antagonists, ed. by Kilborn JR, Cavero I, Harrison DC, et al. New York: Raven Press, 1983, pp 51-61.
3.
Warrington S. , Turner P., Kilborn J., et al: Blood concentrations and pharmacodynamic effects of betaxolol (SL75212), a new beta adrenoreceptor antagonist, after oral and intravenous administration. Br J Clin Pharmacol10:449-452, 1980.
4.
Balnave K., Neill JD, Russell CJ, et al: Observations on the efficacy and pharmacokinetics of betaxolol (SL75212), a cardioselective beta-adrenergic blocking agent. Br J Clin Pharmacol11:171-190, 1981.
5.
Guidicelli JF, Richer C., Ganansia J., et al: Betaxolol: Beta adrenoreceptor blocking effects and pharmacokinetics in man. In: Betaxolol and Other Beta-1 Adrenoreceptor Antagonists , ed. by Morselli PL, Kilbom JR, Cavero I, et al. New York: Raven Press, 1983, pp 89-99.
6.
Bianchetti G. , Blatrix C., Gomeni R., et al: Pharmacokinetics of the new beta-adrenoreceptor blocking agent betaxolol (SL75212) in man after repeated oral administration. ArzremforshungDrug Res30:1912, 1980.
7.
Iskandrian AS , Nestico PF, Hakki AH, et al: Effects of beta-blockade on systolic and diastolic left ventricular function at rest and during exercise in patients with chronic stable angina pectoris. Am Heart J113:179-188, 1987.
8.
Stroobandt R. , Kesteloot H.: Dose related efficacy of betaxolol in combination with nitroglycerin in patients with angina pectoris: A double-blind cross-over study. Arch Int Pharmacodyn Ther267:299-309, 1984.
9.
de Backer G., Derese A.: Double-blind study of betaxolol in patients with stable angina pectoris. In: Betaxolol and Other Beta-1 Adrenoreceptor Antagonists, ed. by Morselli PL, Kilborn JR, Cavero I, et al. New York: Raven Press, 1983, pp 261-266.
10.
Brugmann U. , Blosini R.Comparison of the effect of a selective and a non-selective beta receptor blocker on the ischemic ST segment, lung function and stress induced decrease in blood glucose. Herz11:55-61, 1986.
11.
Biamino G.: Hemodynamics of betaxolol at rest and during exercise in patients with ischemic heart disease. In: Betaxolol and Other Beta-1 Adrenoreceptor Antagonists, ed. by Morselli PL, Kilborn JR, Cavero I, et al. New York: Raven Press, 1983, pp 251-255.
12.
McKee PA, Castelli WP, McNamara R.: The natural history of congestive heart failure: The Framingham study. N Engl J Med285:429-435, 1981.
13.
Cagueret H. , Bianchetti G.: Simple method for routine determination of betaxolol in blood and urine by automated high-performance liquid chromatography with fluorimetric detection. J Chromatography311:199-205, 1984.
14.
Henry WL, DeMaria A., Gramiak R., et al: Report of the American Society of Echocardiography Committee on Nomenclature and Standards in Two-Dimensional Imaging. Circulation62:212-217, 1980.
15.
Schiller NB , Acquatella H., Ports TA, et al: Left ventricular volume from paired biplane two-dimensional echocardiography. Circulation60:547-555, 1979.
16.
Parmley WW: Beta-blockers in cardiovascular disease. Cardiovasc Rev Rep2:655-667, 1981.
17.
Conolly ME, Kesting F., Dollery CT: The clinical pharmacology of beta-adrenergic blocking drugs. Prog Cardiovasc Dis19:203-234, 1976.
18.
Riddell IG, Shanks RG: Effects of betaxolol, propranolol and atenolol on isoproterenol-induced tachycardia . Clin Pharmacol Ther38:559, 1985.
19.
Alpert MA, Singh A., Holmes RA, et al: Effect of beta-blockade with betaxolol on left ventricular systolic function in patients with chronic stable angina pectoris and left ventricular dysfunction. Am J Cardiol57:721-724, 1986.
