The purpose of this study was to investigate the efficacy, effective dose, administration frequency and antianginal effect of a new antianginal agent, nipradilol, in 12 patients with stable effort angina. A single blind design was employed; the test consisted of an observation period (1 week) and a treatment period (1-2 weeks). Twenty four hour Holter monitoring was performed on the penultimate day of each period. Nipradilol was administered twice a day at a daily dose of 3-12 mg (mean 7.9 +/- 3.3 mg). The mean frequency of ST-segment depression was 7.1 +/- 6.7 times per day at baseline and 3.1 +/- 2.7 after drug administration, showing a significant reduction (p less than 0.05). The suppression of ST-segment depression and decrease in heart rate due to this drug persisted for 12 hours following administration. The plasma drug concentration at a daily dose of 12 mg peaked at 9.5 +/- 2.4 ng/ml 1 hour after administration and the 12 hour value was 2.3 +/- 1.2 ng/ml. No side effects were observed. Therefore, it seems that, when administered twice a day (total daily dose 6 mg) this drug is effective in effort angina and that the antianginal effect is mainly attributable to beta-adrenoceptor blockade.