Atenolol, nadolol, and pindolol in angina pectoris on effort: effect of pharmacokinetics.
The duration of action of three beta blockers (atenolol in nine patients, nadolol in 18 patients, and pindolol in 11 patients) administered once a day was studied in three cohorts of patients with angina on effort. Compared with single-blind run-in placebo, all three beta blockers decreased angina frequency (p less than 0.01), exercise tolerance (p less than 0.01), heart rate recorded by ambulatory ECG, and submaximal heart rate when a treadmill exercise stress test was performed 3 hours after administration of the daily dose (p less than 0.0001). Twenty-four hours after the dose, the percentage of the maximal heart rate-attenuating effect was highest for nadolol (pharmacokinetic half-life, 15.5 hours), followed by atenolol and then by pindolol (half-life, 5.5 hours). A linear relationship between the logarithm of plasma concentration of beta blocker and the heart rate at submaximal exercise (r = 0.72 and p = 0.0001 for nadolol; r = 0.50 and p = 0.0001 for pindolol) was observed. The data suggest that in the treatment of angina on effort, beta blockers should be prescribed according to their pharmacokinetic properties to achieve adequate suppression of the heart rate during exercise.
D000319:Adrenergic beta-Antagonists / Q000097:blood / Q000627:therapeutic use*; D000787:Angina Pectoris / Q000188:drug therapy*; D001262:Atenolol / Q000097:blood / Q000627:therapeutic use*; D004562:Electrocardiography; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D009248:Nadolol; D005082:Physical Exertion; D010869:Pindolol / Q000097:blood / Q000627:therapeutic use*; D011412:Propanolamines / Q000097:blood / Q000627:therapeutic use*; D013997:Time Factors
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D009248:Nadolol; D001262:Atenolol; D010869:Pindolol