Efficacy of betaxolol in the treatment of stable exertional angina pectoris: a dose-ranging study.
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 less than or equal to 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 less than 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 greater than or equal to 75% (p less than 0.00005) and to 8.0 +/- 2.3 min during clinical beta blockade (p less than 0.00005). The mean doses of betaxolol required to produce a greater than or equal to 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.
Alpert
M A
MA
Department of Medicine, University of Missouri Health Sciences Center, Columbia.
Mukerji
V
V
Villarreal
D
D
Singh
A
A
Flaker
G C
GC
Sanfelippo
J F
JF
Beach
C L
CL
Morgan
R J
RJ
D000787:Angina Pectoris / Q000188:drug therapy* / Q000209:etiology; D015784:Betaxolol / Q000008:administration & dosage* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D005080:Exercise Test; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D005082:Physical Exertion; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D016037:Single-Blind Method
D011943:Receptors, Adrenergic, beta; D015784:Betaxolol