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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肾上腺素增强大鼠鞘内卡替洛尔和奥普萘洛尔造成的伤害性和运动性阻断

本研究考察了-受体阻滞剂和卡替洛尔/奥普那洛尔联合肾上腺素对脊髓伤害性阻滞和运动阻滞的影响，并与心得安进行了比较。方法观察大鼠鞘内注射卡替洛尔、奥普萘洛尔、美托洛尔、乙酰布洛尔和索他洛尔后的伤害性和运动阻滞。卡替洛尔和奥普那洛尔联合肾上腺素用于脊髓伤害性和运动性阻滞。心得安作为对照。结果在相同剂量0.6 μmol时，卡替洛尔和奥普那洛尔的效价高于心得安，且卡替洛尔和奥普那洛尔的作用时间长于心得安或与心得安相同。在ED50（50%有效剂量）下，药物的效价排名依次为卡替洛尔；心得平比;心得安(P >；0.01)。在ED25、ED50和ED75时，卡替洛尔诱导的完全恢复时间比奥普萘洛尔和心得安诱导的时间长。当在ED50时将1:40万肾上腺素加入β受体阻滞剂（卡替洛尔、奥普萘洛尔和心得安）时，与单独使用β受体阻滞剂相比，脊髓阻滞和作用时间增加(P >；0.05)。结论卡替洛尔和奥普萘洛尔治疗脊髓阻滞较心得安有效，其他受体阻滞剂疗效较差。与心得安相比，卡替洛尔和奥普萘洛尔的作用时间更长或相同。肾上腺素增强卡替洛尔、奥普萘洛尔和心得安的脊髓阻滞，提示α -肾上腺素能受体可能在增强β受体阻滞剂的抗伤害作用中起重要作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.