Pharmacokinetics and in vitro effects of tegaserod, a serotonin 5-hydroxytryptamine 4 (5-HT4) receptor agonist with prokinetic activity in horses.
Abstract: Tegaserod, a serotonin agonist, has been shown to have prokinetic effects in horses, but pharmacokinetic information is not currently available. The pharmacokinetics and in vitro effects of tegaserod were evaluated. Tegaserod increased the contractile activity of smooth muscle preparations of the equine pelvic flexure. Pertinent pharmacokinetic parameters for a single IV and oral dose were determined. Therapeutic plasma concentrations of tegaserod were achieved by a single oral dose at 0.27 mg/kg. These findings indicate that further clinical studies are warranted to investigate potential benefits in cases of functional gastrointestinal motility disorders in horses.
Publication Date: 2007-04-21 PubMed ID: 17447227
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- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.
The research paper explains that Tegaserod, a serotonin receptor stimulant, has demonstrated the ability to propel the digestive process (prokinetic effects) in horses. More comprehensive details about its physiological interactions (pharmacokinetics) and effects in a controlled environment (in vitro) were studied.
Overview and Purpose of the Research
- The purpose was to study the impact of Tegaserod on horses, focusing on its pharmacokinetics and effects in a controlled environment.
- The research was aimed at evaluating its prokinetic functions, how it accelerates the process of digestion in horses, and whether these effects could potentially treat functional gastrointestinal motility disorders in horses.
Investigative Process
- The impact of Tegaserod was specifically studied on the contractile activity of smooth muscle preparations of the equine pelvic flexure.
- The pharmacokinetic parameters of Tegaserod were assessed following a single Intravenous (IV) and oral administration of the drug.
Key Findings
- Tegaserod was found to increase the contractile activity of the equine pelvic flexure’s smooth muscles.
- A therapeutic dose, which would impact the physiology as intended, was achieved by administering a single oral dose of Tegaserod at 0.27 mg/kg. This implies that such a dose was sufficient to stimulate the intended prokinetic effects.
Conclusions and Implications
- The findings suggest that Tegaserod could potentially be used as a treatment for functional gastrointestinal motility disorders in horses, given its prokinetic effects.
- However, further clinical trials with a broader population of horses are needed to corroborate these initial findings and to investigate any potential adverse effects.
Cite This Article
APA
Delco ML, Nieto JE, Craigmill AL, Stanley SD, Snyder JR.
(2007).
Pharmacokinetics and in vitro effects of tegaserod, a serotonin 5-hydroxytryptamine 4 (5-HT4) receptor agonist with prokinetic activity in horses.
Vet Ther, 8(1), 77-87.
Publication
Researcher Affiliations
- Veterinary Medical Teaching Hospital, University of California, Davis, Davis, CA 95616, USA.
MeSH Terms
- Administration, Oral
- Administration, Rectal
- Animals
- Area Under Curve
- Colic / drug therapy
- Colic / veterinary
- Gastrointestinal Agents / administration & dosage
- Gastrointestinal Agents / blood
- Gastrointestinal Agents / pharmacokinetics
- Gastrointestinal Agents / pharmacology
- Gastrointestinal Motility / drug effects
- Horse Diseases / drug therapy
- Horses / metabolism
- Indoles / administration & dosage
- Indoles / blood
- Indoles / pharmacokinetics
- Indoles / pharmacology
- Injections, Intravenous / veterinary
- Muscle Contraction / drug effects
- Muscle, Smooth / drug effects
- Receptors, Serotonin, 5-HT4
- Serotonin Receptor Agonists / administration & dosage
- Serotonin Receptor Agonists / blood
- Serotonin Receptor Agonists / pharmacokinetics
- Serotonin Receptor Agonists / pharmacology
Citations
This article has been cited 2 times.- Beder NA, Mourad AA, Aly MA. Ultrasonographic evaluation of the effects of the administration of neostigmine and metoclopramide on duodenal, cecal, and colonic contractility in Arabian horses: A comparative study. Vet World 2020 Nov;13(11):2447-2451.
- Laus F, Fratini M, Paggi E, Faillace V, Spaterna A, Tesei B, Fettucciari K, Bassotti G. Effects of Single-Dose Prucalopride on Intestinal Hypomotility in Horses: Preliminary Observations. Sci Rep 2017 Jan 27;7:41526.
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