Oxprenolol: clinical pharmacology, pharmacokinetics, and pharmacodynamics

Oxprenolol is clinically a well-established beta blocker that shares with other members of this group the ability to control a variety of disorders, in particular, hypertension and angina. Pharmacologically it is a nonselective beta blocker that possesses partial agonist activity (intrinsic sympathomimetic activity). Pharmacokinetically, oxprenolol behaves as a moderately lipophilic agent. This means that it is well absorbed, but then undergoes considerable first-pass loss. It penetrates well into most tissues, including the central nervous system. About 80% of oxprenolol is bound to protein in the blood, and when acute-phase proteins increase, as, for example, in patients with inflammatory disease, total plasma concentrations of oxprenolol also increase. Apart from this, the plasma concentration:time profile produced after the oral administration of oxprenolol is remarkably consistent and reproducible. Intrasubject and intersubject variability is small, and the administration of the drug after food or with many other drugs has very little effect. The beta-blocking effects of oxprenolol correlate well with the plasma concentrations, but as with other beta blockers, it has not been possible to correlate plasma concentrations directly with its therapeutic actions such as lowering blood pressure or controlling arrhythmias.