Oxprenolol
Oxprenolol, sold under the brand name Trasicor among others, is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure.
Medical uses
Oxprenolol is used in the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure.
It has been used to treat anxiety as well.
Contraindications
Oxprenolol is a potent beta blocker and should not be administered to asthmatics under any circumstances due to their low beta levels as a result of depletion due to other asthma medication, and because it can cause irreversible, often fatal, airway failure and inflammation.
Pharmacology
Pharmacodynamics
Oxprenolol is a beta blocker. In addition, it has been found to act as an antagonist of the serotonin 5-HT1A and 5-HT1B receptors with respective Ki values of 94.2 nM and 642 nM in rat brain tissue.
Pharmacokinetics
Oxprenolol is a lipophilic beta blocker which passes the blood–brain barrier more easily than hydrophilic beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than beta blockers with more hydrophilic molecules such as atenolol, sotalol, and nadolol. The brain-to-blood ratio of oxprenolol in humans has been found to be 50:1. For comparison, the brain-to-blood ratio of the highly lipophilic propranolol was 15:1 to 26:1 and of the hydrophilic atenolol was 0.2:1.
Chemistry
The experimental log P of oxprenolol is 2.10.
Stereochemistry
Oxprenolol is a chiral compound, the beta blocker is used as a racemate, e. g. a 1:1 mixture of --oxprenolol and --oxprenolol. Analytical methods for the separation and quantification of --oxprenolol and --oxprenolol in urine and in pharmaceutical formulations have been described in the literature.
Society and culture
Brand names of oxprenolol include Trasacor, Trasicor, Coretal, Laracor, Slow-Pren, Captol, Corbeton, Slow-Trasicor, Tevacor, Trasitensin, and Trasidex.