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Compound

Oxprenolol

Also called Coretal, Trasicor, Osprenololo

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Part of the metabolic pathway of Oxprenolol. See the timeline on the metabolic highway.

Overview

Oxprenolol, sold under the brand name Trasicor among others, is a non-selective beta blocker with some intrinsic sympathomimetic activity. It was used for the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure.[1] WP

Uses, dosage and effects

Medical uses

Oxprenolol has been used in the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure. WP

It has been used to treat anxiety as well.[2][3] WP

Risks and side effects

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.[4] WP

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.[5] WP

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.[6][7] WP

Chemistry

Formula
C15H23NO3 PC
CAS number
6452-71-7 PC
Molar mass (g/mol)
265.35 PC
IUPAC name (computed by PubChem)
1-(propan-2-ylamino)-3-(2-prop-2-enoxyphenoxy)propan-2-ol PC
SMILES
CC(C)NCC(COC1=CC=CC=C1OCC=C)O PC
InChIKey
CEMAWMOMDPGJMB-UHFFFAOYSA-N PC
PubChem CID
4631

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

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Sources

  1. Other Oxprenolol
  2. Journal / agency Boyce TG, Ballone NT, Certa KM, Becker MA. The Use of β-Adrenergic Receptor Antagonists in Psychiatry: A Review. J Acad Consult Liaison Psychiatry. 2021. doi:10.1016/j.jaclp.2020.12.009 · PMID 34210401
  3. Journal / agency Archer C, Wiles N, Kessler D, Turner K, Caldwell DM. Beta-blockers for the treatment of anxiety disorders: A systematic review and meta-analysis. J Affect Disord. January 2025. doi:10.1016/j.jad.2024.09.068 · PMID 39271062
  4. Journal / agency Williams IP, Millard FJ. Severe asthma after inadvertent ingestion of oxprenolol. Thorax. February 1980. doi:10.1136/thx.35.2.160 · PMID 7376124 · PMC471246
  5. Journal / agency Langlois M, Brémont B, Rousselle D, Gaudy F. Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors. European Journal of Pharmacology. January 1993. doi:10.1016/0922-4106(93)90061-d · PMID 8093601
  6. Journal / agency McDevitt DG. Comparison of pharmacokinetic properties of beta-adrenoceptor blocking drugs. European Heart Journal. December 1987. doi:10.1093/eurheartj/8.suppl_M.9 · PMID 2897304
  7. Journal / agency Drayer DE. Lipophilicity, hydrophilicity, and the central nervous system side effects of beta blockers. Pharmacotherapy. 1987. doi:10.1002/j.1875-9114.1987.tb04029.x · PMID 2891122

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.