Pharmacokinetics of atenolol and its clinical consequences in patients with angina pectoris

Pharmacokinetics and clinical effects of daily oral doses of 100 mg and 200 mg atenolol, respectively, were studied in patients with angina pectoris by means of a double-blind cross-over randomized study. Half-lives and areas under the curve were of the same magnitude as described earlier for healthy volunteers and hypertensive patients. However, a steady state level was built up during 4-week medication of 100 mg or 200 mg atenolol daily. Intra-patient correlations of plasma levels and reductions in exercising heart rate were moderate (r = 0.56-0.85). Only plasma levels and exercising heart rates revealed significant differences after a 100 mg and 200 mg dose. These findings, together with the remaining clinical observations, demonstrated that a single daily dose of 100 mg atenolol is useful in patients with exercise-induced angina pectoris.