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Research in veterinary science2019; 128; 43-48; doi: 10.1016/j.rvsc.2019.10.022

Relaxing effects of clenbuterol, ritodrine, salbutamol and fenoterol on the contractions of horse isolated bronchi induced by different stimuli.

Abstract: β-adrenoceptor agonists are considered the most effective drugs to counteract bronchoconstriction in horses with asthma, but only clenbuterol is commonly employed in clinical practice. We evaluated the effects of different selective β agonists: clenbuterol, ritodrine, salbutamol, and fenoterol on the contractions of isolated bronchial muscle of horses induced by electrical field stimulation (EFS), carbachol, histamine, and KCl. All β agonists reduced the amplitude of contraction induced by the different stimuli but with variable efficacy and potency. Fenoterol and salbutamol were more effective than clenbuterol in relaxing the bronchial contractions induced by EFS and histamine, and were able to completely abolish carbachol-induced contractions, unlike clenbuterol and ritodrine. The respective potency values (pEC) of clenbuterol, ritodrine, salbutamol, and fenoterol were 7.74 ± 0.20, 7.77 ± 0.17, 7.30 ± 0.23, 8.01 ± 0.13, for EFS-induced contractions; 8.39 ± 0.26, 5.49 ± 0.28, 6.63 ± 0.14, 7.68 ± 0.11, for carbachol-induced contraction; 7.39 ± 0.27, 7.04 ± 0.28, 6.45 ± 0.34, 7.34 ± 0.22, for histamine-induced contraction; 7.15 ± 0.06, 6.07 ± 0.20, 6.48 ± 0.14, 6.70 ± 0.18, for KCl-induced contraction. Salbutamol and fenoterol showed a higher efficacy than clenbuterol in relaxing horse bronchial muscle pre-contracted by most stimuli. Clenbuterol displayed a good potency but a rather low efficacy, and this may be due to its partial agonist nature; ritodrine showed lower or not significantly different efficacy and potency compared to the other agonists. An evaluation of the clinical efficacy by fenoterol and salbutamol in horses with asthma could be of great interest to assess if they could represent more effective bronchodilators compared to clenbuterol.
Publication Date: 2019-10-31 PubMed ID: 31710963DOI: 10.1016/j.rvsc.2019.10.022Google Scholar: Lookup
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  • Journal Article

Summary

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This research investigates the comparative effects of β-adrenoceptor agonists, such as clenbuterol, ritodrine, salbutamol, and fenoterol, on bronchial contractions in horses. The study found that fenoterol and salbutamol were more effective than commonly-used clenbuterol in relaxing these contractions.

Study Design and Methods

  • The researchers examined four selective β agonists, known to counteract bronchoconstriction: clenbuterol, ritodrine, salbutamol, and fenoterol.
  • They studied the effects of these drugs on contractions of isolated bronchial muscle in horses using different stimuli, including electrical field stimulation (EFS), carbachol, histamine, and KCl.

Results and Findings

  • All the β agonists reduced the amplitude of contraction induced by the different stimulants, but the efficacy and potency varied.
  • Fenoterol and salbutamol were more effective than clenbuterol in countering bronchial contractions induced by EFS and histamine.
  • Fenoterol and salbutamol were also able to completely end contractions induced by carbachol, unlike clenbuterol and ritodrine.
  • Potency values (pEC) were measured for each agonist and stimulant, showing different levels of impact, with fenoterol and salbutamol generally showing higher pEC values, indicating higher efficacy.
  • Clenbuterol, despite its usual use in clinical practice, showed relatively low efficacy despite good potency. This may be due to being a partial agonist.
  • Ritodrine displayed lower or not significantly different efficacy and potency when compared to the other agonists.

Implications and Conclusions

  • The higher efficacy of salbutamol and fenoterol in relaxing horse bronchial muscle suggests they may be more effective bronchodilators than clenbuterol.
  • The researchers recommend further clinical evaluation of the efficacy of fenoterol and salbutamol in treating horses with asthma. They could potentially be more effective bronchodilators compared to clenbuterol.

Cite This Article

APA
Pozzoli C, Bertini S, Poli E, Placenza G, Menozzi A. (2019). Relaxing effects of clenbuterol, ritodrine, salbutamol and fenoterol on the contractions of horse isolated bronchi induced by different stimuli. Res Vet Sci, 128, 43-48. https://doi.org/10.1016/j.rvsc.2019.10.022

Publication

ISSN: 1532-2661
NlmUniqueID: 0401300
Country: England
Language: English
Volume: 128
Pages: 43-48
PII: S0034-5288(18)35409-2

Researcher Affiliations

Pozzoli, Cristina
  • Department of Medicine and Surgery, University of Parma, Via Volturno 39, 43125 Parma, Italy.
Bertini, Simone
  • Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy.
Poli, Enzo
  • Department of Medicine and Surgery, University of Parma, Via Volturno 39, 43125 Parma, Italy.
Placenza, Giuseppe
  • Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy.
Menozzi, Alessandro
  • Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy. Electronic address: alessandro.menozzi@unipr.it.

MeSH Terms

  • Adrenergic beta-2 Receptor Agonists / pharmacology
  • Albuterol / pharmacology
  • Animals
  • Bronchi / drug effects
  • Bronchi / physiology
  • Bronchodilator Agents / pharmacology
  • Clenbuterol / pharmacology
  • Fenoterol / pharmacology
  • Horses / physiology
  • Male
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / physiology
  • Ritodrine / pharmacology

Citations

This article has been cited 2 times.
  1. Secombe C, Adler A, Hosgood G, Raisis A, Mosing M. Can bronchoconstriction and bronchodilatation in horses be detected using electrical impedance tomography?. J Vet Intern Med 2021 Jul;35(4):2035-2044.
    doi: 10.1111/jvim.16152pubmed: 33977584google scholar: lookup
  2. Bolelli K, Ertan-Bolelli T, Unsalan O, Altunayar-Unsalan C. Fenoterol and dobutamine as SARS-CoV-2 main protease inhibitors: A virtual screening study. J Mol Struct 2021 Mar 15;1228:129449.