Oxprenolol Hydrochloride: Pharmacology, Pharmacokinetics, Adverse Effects and Clinical Efficacy

Abstract

Oxprenolol is a nonselective beta‐adrenergic blocking agent that also possesses intrinsic sympathomimetic activity (ISA) and membrane stabilizing effects. Oxprenolol undergoes first pass metabolism with only 30% of an oral dose reaching the systemic circulation. The drug is approximately 80% protein bound and is eliminated primarily by glucuronidation in the liver. Less than 4% of oxprenolol is excreted unchanged in the urine. Oxprenolol may reduce the heart rate and prolong the effective and functional atrioventricular nodal refractory period. Oxprenolol has less negative inotropic and chronotropic effects than propranolol. Plasma renin activity is reduced; however, changes in plasma aldosterone level are not significant. Long term metabolic effects require further study. Oxprenolol appears to be comparable to other beta blockers in the treatment of hypertension and angina pectoris with no additional adverse reactions. If its partial agonist effect proves useful, it may have an advantage over other agents in treating patients with borderline cardiac reserve. Because of limited data, the use of oxprenolol for the treatment of arrhythmias, migraine, thyrotoxicosis, anxiety, and glaucoma cannot be recommended at this time.

Relationship between the rate of appearance of oxprenolol in the systemic circulation and the location of an oxprenolol Oros 16/260 drug delivery system within the gastrointestinal tract as determined by scintigraphy.

“…The drug osmotic principle and has been described in detail has a short elimination half-life of 1-2 h (Brunner (Theeuwes et al, 1985). et al, 1975;Mason & Winer, 1976;Russo & The performance of a novel controlled release Covinsky, 1983;John & Smith, 1985a). dosage form can be assessed by in vitro release Oxprenolol is well absorbed from the small and studies combined with a pharmacokinetic evalualarge intestines (Antonin et al, 1985; tion that involves collection and analysis of al., 1985;Langenbucher & Mysicka, 1985) and suitably timed blood samples followed by consequently therapeutic advantage can be gained mathematical deconvolution.…”