Tissue distribution of clenbuterol in the horse.
Abstract: Plasma and tissue concentrations of clenbuterol (CLB) were determined following oral (p.o.) administration of 1.6 microg/kg twice daily (b.i.d.) for 2 weeks. Horses were administered the last dose on morning of day 15, killed at 0.25, 24, 48, and 72 h post-administration. At 0.25 h, the highest tissue concentrations of CLB were found in the liver (16.21 ng/g), lung (6.48 ng/g), left ventricle (4.99 ng/g), kidney (3.35 ng/g), bronchi (2.56 ng/g), right ventricle (2.08 ng/g), and eye fluids (1.09 ng/g) all of which were higher than that of plasma (1.10 ng/mL). The elimination half-lives (t(1/2k)) for CLB in tissues ranged from 21.2 to 56.3 h, the longest were in the eye fluids (56.9 h), spleen (21.2 h), cerebrum (27.1 h), cerebellum (21.5) and cecum (23.7 h). The t(1/2k) for plasma was 10.9 h. Tissue/plasma ratios of liver (14.7), lung (5.9), left ventricle (4.6), kidney (3.1), bronchi, (2.3) and right ventricle (1.9) were high at 0.25 h and remained elevated up to 72 h. Accumulation and sustained high concentration of CLB relative to plasma in these tissues contributed to the prolonged elimination and the ability to quantify CLB in plasma and urine for a prolonged period.
Publication Date: 2004-04-21 PubMed ID: 15096106DOI: 10.1111/j.1365-2885.2004.00558.xGoogle Scholar: Lookup
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- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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The research investigates the distribution and retention period of the drug clenbuterol (CLB) in different body tissues of a horse after oral administration. This study uncovered that the highest concentrations of CLB were found in certain tissues, contributing to the drug’s prolonged elimination and detectability.
Methodology
- The study was carried out on horses given an oral dose of clenbuterol (1.6 microg/kg) twice daily for two weeks.
- The horses were terminated at different time intervals (0.25, 24, 48, and 72 hours) after the last administered dose. This allowed the researchers to observe the concentration of the drug at different points in time.
Results
- The maximum clenbuterol concentration, within a quarter of an hour of the last dosage, was found in the liver (16.21 ng/g), followed by the lung, left ventricle, kidney, bronchi, right ventricle, and eye fluids. This concentration was notably higher than what was found in the plasma (1.10 ng/mL).
- The half-lives—that is, the time taken for the clenbuterol concentration to reduce by half—ranged from 21.2 to 56.3 hours in various tissues. The longest half-lives were observed in the eye fluids (56.9 hours), spleen, cerebrum, cerebellum, and cecum.
- The half-life for plasma, in contrast, was 10.9 hours.
Conclusion
- The research found that the tissue/plasma ratios of liver, lung, left ventricle, kidney, bronchi, and right ventricle remained high up to 72 hours post-administration.
- The elevated concentration of clenbuterol in these tissues, compared to plasma, contributed to the drug’s ability to remain in the system for a protracted period. Such a sustained level of concentration further allowed for the quantification of clenbuterol in plasma and urine over an extended duration.
Cite This Article
APA
Soma LR, Uboh CE, Guan F, Luo Y, Teleis D, Runbo L, Birks EK, Tsang DS, Habecker P.
(2004).
Tissue distribution of clenbuterol in the horse.
J Vet Pharmacol Ther, 27(2), 91-98.
https://doi.org/10.1111/j.1365-2885.2004.00558.x Publication
Researcher Affiliations
- School of Veterinary Medicine, University of Pennsylvania, New Bolton Center Campus, West Street Road, Kennett Square, PA 19348, USA. soma@mail.vet.upenn.edu
MeSH Terms
- Administration, Oral
- Animals
- Bronchodilator Agents / blood
- Bronchodilator Agents / pharmacokinetics
- Clenbuterol / blood
- Clenbuterol / pharmacokinetics
- Female
- Half-Life
- Horses
- Male
- Tissue Distribution
Citations
This article has been cited 2 times.- Burniston JG, Clark WA, Tan LB, Goldspink DF. Dose-dependent separation of the hypertrophic and myotoxic effects of the beta(2)-adrenergic receptor agonist clenbuterol in rat striated muscles. Muscle Nerve 2006 May;33(5):655-63.
- Burniston JG, Chester N, Clark WA, Tan LB, Goldspink DF. Dose-dependent apoptotic and necrotic myocyte death induced by the beta2-adrenergic receptor agonist, clenbuterol. Muscle Nerve 2005 Dec;32(6):767-74.
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