ABSORPTION AND EXCRETION OF RAPID AND SLOW RELEASE OXPRENOLOL AND THEIR EFFECTS ON HEART-RATE AND BLOOD-PRESSURE DURING EXERCISE

1. Plasma concentrations and heart rate and blood pressure effects of 160 mg oxprenolol as standard rapid release (RR) and slow release (SR) tablets were compared in healthy volunteers. Peak plasma concentrations were lower with SR tablets than with RR tablets and the peak was delayed. 2. Absorption of oxprenolol was described adequately by first order kinetics with both preparations. The apparent half‐life of absorption was 0.40 h with RR and 2.4 h for the SR formulation. The apparent elimination half‐life of oxprenolol was about 2 h. Relative bioavailabilities of the two formulations were similar. 3. The effectiveness of oxprenolol RR and SR were assessed by their effects on heart rate in severe exercise (EHR) and also by their effects on blood pressure at rest and during exercise. 4. Maximum reductions in these variables coincided with peak oxprenolol concentrations. The effects on EHR and blood pressure parameters had a distinct time course but there was no difference between the time course of inhibition of each variable for the two formulations over 24 h. 1979 The British Pharmacological Society