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Pharmacokinetics of carbetocin, a long-acting oxytocin analogue, following intravenous administration in horses.
Abstract: Current therapy protocols to treat persistent post mating endometritis and retained fetal membranes in mares typically include the administration of ecbolic drugs. Evaluation of the pharmacokinetics and tolerability of carbetocin, a long-acting oxytocin analogue, after i.v. administration is required. Objective: To determine the pharmacokinetic parameters (principally half-life) of carbetocin in horses. Methods: Five mature mares and one gelding received 0.175 mg carbetocin i.v. All animals were monitored periodically throughout the study for elevation in rectal temperature, heart rate, respiratory rate and signs of pain or discomfort. Plasma samples were collected for determination of carbetocin concentrations by radioimmunoassay. Results: Administration of carbetocin was well tolerated by all horses and its half-life was 17.2 min. Conclusions: The half-life of carbetocin is greater than that previously reported for oxytocin (6.8 min). Conclusions: Carbetocin is an attractive alternative to oxytocin therapy in broodmare management.
Publication Date: 2009-01-24 PubMed ID: 19165935DOI: 10.2746/042516408x334343Google Scholar: Lookup The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
Summary
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This research investigates the pharmacokinetics of carbetocin, a long-acting oxytocin analog, in horses following intravenous administration, and suggests it as a potential therapeutic alternative for treatment of post mating endometritis and retained fetal membranes in mares.
Objectives and Methodology
- The main goal of the study was to figure out the pharmacokinetic parameters, specifically the half-life of carbetocin, in horses.
- The experiment involved five mature mares and one gelding. Each animal was administered with 0.175 mg of carbetocin intravenously.
- Throughout the study, the animals were closely monitored, taking into account changes in their rectal temperature, heart rate, respiratory rate, and behavioral signs of discomfort or pain.
- Blood samples were collected from each horse in order to determine the concentration of carbetocin in their plasma, for which a radioimmunoassay analysis was used.
Findings
- The study found that the administered carbetocin was well tolerated by all horses, indicating that it did not seem to cause any adverse effects.
- The identified half-life of carbetocin in horses was 17.2 minutes.
Conclusions
- The concluded half-life of carbetocin was greater than the previously reported half-life for oxytocin, which is 6.8 minutes. A longer half-life means that carbetocin stays in the body longer than oxytocin, which could potentially make it more effective for treating medical conditions in horses.
- Due to its longer half-life, and well-tolerated nature, carbetocin may be an attractive alternative to oxytocin therapy in mares. Even though it is a synthetic analogue of oxytocin, it appears to be safer and more potent for broodmare therapies.
Cite This Article
APA
Schramme AR, Pinto CR, Davis J, Whisnant CS, Whitacre MD.
(2009).
Pharmacokinetics of carbetocin, a long-acting oxytocin analogue, following intravenous administration in horses.
Equine Vet J, 40(7), 658-661.
https://doi.org/10.2746/042516408x334343 Publication
Researcher Affiliations
- North Carolina State University, College of Veterinary Medicine, Department of Population Health and Pathobiology, 4700 Hillsborough Street, Raleigh, North Carolina 27606, USA.
MeSH Terms
- Animals
- Area Under Curve
- Female
- Half-Life
- Heart Rate / drug effects
- Horse Diseases / blood
- Horse Diseases / drug therapy
- Horses / blood
- Injections, Intravenous / veterinary
- Oxytocin / adverse effects
- Oxytocin / analogs & derivatives
- Oxytocin / pharmacokinetics
- Oxytocin / therapeutic use
- Pain / chemically induced
- Pain / epidemiology
- Pain / veterinary
- Radioimmunoassay / veterinary
- Respiration / drug effects
Citations
This article has been cited 9 times.- Tyrnenopoulou P, Fthenakis GC. Clinical Aspects of Bacterial Distribution and Antibiotic Resistance in the Reproductive System of Equids. Antibiotics (Basel) 2023 Mar 28;12(4).
- Xu Z, Zou Y, Gao X, Niu MM, Li J, Xue L, Jiang S. Dual-targeting cyclic peptides of receptor-binding domain (RBD) and main protease (Mpro) as potential drug leads for the treatment of SARS-CoV-2 infection. Front Pharmacol 2022;13:1041331.
- Canisso IF, Segabinazzi LGTM, Fedorka CE. Persistent Breeding-Induced Endometritis in Mares - a Multifaceted Challenge: From Clinical Aspects to Immunopathogenesis and Pathobiology. Int J Mol Sci 2020 Feb 20;21(4).
- Lawson EA, Olszewski PK, Weller A, Blevins JE. The role of oxytocin in regulation of appetitive behaviour, body weight and glucose homeostasis. J Neuroendocrinol 2020 Apr;32(4):e12805.
- Mull RW, Harrington A, Sanchez LA, Tal-Gan Y. Cyclic Peptides that Govern Signal Transduction Pathways: From Prokaryotes to Multi-Cellular Organisms. Curr Top Med Chem 2018;18(7):625-644.
- Cherepanov SM, Akther S, Nishimura T, Shabalova AA, Mizuno A, Ichinose W, Shuto S, Yamamoto Y, Yokoyama S, Higashida H. Effects of Three Lipidated Oxytocin Analogs on Behavioral Deficits in CD38 Knockout Mice. Brain Sci 2017 Oct 16;7(10).
- Mizuno A, Cherepanov SM, Kikuchi Y, Fakhrul AA, Akther S, Deguchi K, Yoshihara T, Ishihara K, Shuto S, Higashida H. Lipo-oxytocin-1, a Novel Oxytocin Analog Conjugated with Two Palmitoyl Groups, Has Long-Lasting Effects on Anxiety-Related Behavior and Social Avoidance in CD157 Knockout Mice. Brain Sci 2015 Jan 20;5(1):3-13.
- Zagrodnik E, Szczuko M, Kordek A, Surówka A, Szydłowska I, Rzewuska B, Steblovnik L, Ziętek M. Adverse Effects of Oxytocin Are More Prevalent than Those Associated with Carbetocin Administration During Cesarean Section. J Clin Med 2025 Oct 13;14(20).
- Nuti F, Larregola M, Staśkiewicz A, Retzl B, Tomašević N, Macchia L, Street ME, Jewgiński M, Lequin O, Latajka R, Rovero P, Gruber CW, Chorev M, Papini AM. Design, synthesis, conformational analysis, and biological activity of Cα(1)-to-Cα(6) 1,4- and 4,1-disubstituted 1H-[1,2,3]triazol-1-yl-bridged oxytocin analogues. J Enzyme Inhib Med Chem 2023 Dec;38(1):2254019.
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