Adrenaline enhances nociceptive and motor blockades by intrathecal carteolol and oxprenolol in rats

IF 2.1 4区医学 Q3 PHARMACOLOGY & PHARMACY

Fundamental & Clinical Pharmacology Pub Date : 2025-02-27 DOI:10.1111/fcp.70003

Chong-Chi Chiu, Kuo-Sheng Liu, Chieh-Yu Liu, Ching-Hsia Hung, Yu-Wen Chen, Jhi-Joung Wang

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Abstract

Background

This study examined the effects of beta-blockers and the combination of carteolol/oxprenolol with epinephrine on spinal nociceptive and motor blockades and compared them with propranolol.

Methods

Nociceptive and motor blockades were assessed in rats after intrathecal injection of carteolol, oxprenolol, metoprolol, acebutolol, and sotalol. Carteolol and oxprenolol were used in combination with epinephrine for spinal nociceptive and motor blockades. Propranolol was used as a control.

Results

At the same dose of 0.6 μmol, carteolol and oxprenolol are more potent than propranolol, and the duration of action of carteolol and oxprenolol is longer than or the same as that of propranolol. At ED₅₀ (50% effective dose), the potency rankings of drugs are carteolol > oxprenolol > propranolol (P > 0.01). At ED₂₅, ED₅₀, and ED₇₅, the time to full recovery induced by carteolol was longer than that induced by oxprenolol or propranolol. When 1:40,000 epinephrine was added to beta-blocker (carteolol, oxprenolol, and propranolol) at ED₅₀, spinal blockades and duration of action were increased compared to beta-blockers alone (P > 0.05).

Conclusion

Carteolol and oxprenolol are more effective than propranolol on spinal blockades, while other beta-blockers are relatively ineffective. Compared to propranolol, the duration of action of carteolol and oxprenolol is longer or the same. Epinephrine enhances spinal blockades of carteolol, oxprenolol, and propranolol, suggesting that alpha-adrenergic receptors may play an important role in enhancing the anti-nociceptive effects of beta-blockers.

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来源期刊

Fundamental & Clinical Pharmacology 医学-药学

CiteScore

5.30

自引率

6.90%

发文量

111

审稿时长

6-12 weeks

期刊介绍： Fundamental & Clinical Pharmacology publishes reports describing important and novel developments in fundamental as well as clinical research relevant to drug therapy. Original articles, short communications and reviews are published on all aspects of experimental and clinical pharmacology including: Antimicrobial, Antiviral Agents Autonomic Pharmacology Cardiovascular Pharmacology Cellular Pharmacology Clinical Trials Endocrinopharmacology Gene Therapy Inflammation, Immunopharmacology Lipids, Atherosclerosis Liver and G-I Tract Pharmacology Metabolism, Pharmacokinetics Neuropharmacology Neuropsychopharmacology Oncopharmacology Pediatric Pharmacology Development Pharmacoeconomics Pharmacoepidemiology Pharmacogenetics, Pharmacogenomics Pharmacovigilance Pulmonary Pharmacology Receptors, Signal Transduction Renal Pharmacology Thrombosis and Hemostasis Toxicopharmacology Clinical research, including clinical studies and clinical trials, may cover disciplines such as pharmacokinetics, pharmacodynamics, pharmacovigilance, pharmacoepidemiology, pharmacogenomics and pharmacoeconomics. Basic research articles from fields such as physiology and molecular biology which contribute to an understanding of drug therapy are also welcomed.