Pharmacokinetics, pharmacodynamics, and metabolism of acepromazine following intravenous, oral, and sublingual administration to exercised Thoroughbred horses.
Abstract: Acepromazine is a tranquilizer used commonly in equine medicine. This study describes serum and urine concentrations and the pharmacokinetics and pharmacodynamics of acepromazine following intravenous, oral, and sublingual (SL) administration. Fifteen exercised adult Thoroughbred horses received a single intravenous, oral, and SL dose of 0.09 mg/kg of acepromazine. Blood and urine samples were collected at time 0 and at various times for up to 72 hr and analyzed for acepromazine and its two major metabolites (2-(1-hydroxyethyl) promazine and 2-(1-hydroxyethyl) promazine sulfoxide) using liquid chromatography-tandem mass spectrometry. Acepromazine was also incubated in vitro with whole equine blood and serum concentrations of the parent drug and metabolites determined. Acepromazine was quantitated for 24 hr following intravenous administration and 72 hr following oral and SL administration. Results of in vitro incubations with whole blood suggest additional metabolism by RBCs. The mean ± SEM elimination half-life was 5.16 ± 0.450, 8.58 ± 2.23, and 6.70 ± 2.62 hr following intravenous, oral, and SL administration, respectively. No adverse effects were noted and horses appeared sedate as noted by a decrease in chin-to-ground distance within 5 (i.v.) or 15 (p.o. and SL) minutes postadministration. The duration of sedation lasted 2 hr. Changes in heart rate were minimal.
© 2018 John Wiley & Sons Ltd.
Publication Date: 2018-02-18 PubMed ID: 29457257DOI: 10.1111/jvp.12494Google Scholar: Lookup
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- Journal Article
Summary
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The research paper is a scientific examination of how acepromazine, a commonly used horse tranquilizer, is absorbed, metabolized, and excreted in the body of Thoroughbred horses when administered intravenously, orally, and sublingually.
Methodology
- The study was conducted on fifteen adult Thoroughbred horses, all of which had engaged in physical exercise leading up to the research process.
- Each of these horses was administered a single dose of 0.09 mg/kg of acepromazine via intravenous, oral, and sublingual methods.
- Blood and urine samples were then collected from these horses at the commencement of the experiment and repeatedly over the course of 72 hours.
- These samples were analyzed using a technique known as liquid chromatography-tandem mass spectrometry to ascertain concentrations of the parent drug and its two primary metabolites in the bloodstream and urine.
- In-vitro testing was also conducted where acepromazine was combined with whole equine blood to see how it might additionally be metabolized by red-blood cells.
Results
- From the analysis of the blood and urine samples, it was discovered that acepromazine could be detected for about 24 hours after intravenous administration, and 72 hours after both oral and sublingual administration.
- The half-life of the drug, that is, the time taken for the concentration of the drug in the body to reduce to half its initial levels, was found to be around 5.16 hours, 8.58 hours, and 6.70 hours following intravenous, oral, and sublingual administration respectively.
- The study further revealed that the effects of the tranquilizer were visible within 5 minutes after intravenous administration, and within 15 minutes after both oral and sublingual administration, with the sedation lasting for a period of two hours.
- Notably, there were no observable adverse effects from the administration of the drug, with only minimal changes in the horses’ heart rates.
Conclusions
- The outcomes of this study provide valuable insight into how acepromazine works within the bodies of Thoroughbred horses following different modes of administration.
- These results could be instrumental in making sound veterinary decisions on the choice of administration and dosage of acepromazine as a tranquilizer for horses
Cite This Article
APA
Knych HK, Seminoff K, McKemie DS, Kass PH.
(2018).
Pharmacokinetics, pharmacodynamics, and metabolism of acepromazine following intravenous, oral, and sublingual administration to exercised Thoroughbred horses.
J Vet Pharmacol Ther, 41(4), 522-535.
https://doi.org/10.1111/jvp.12494 Publication
Researcher Affiliations
- K.L. Maddy Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, Davis, CA, USA.
- Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, Davis, CA, USA.
- K.L. Maddy Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, Davis, CA, USA.
- K.L. Maddy Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, Davis, CA, USA.
- Department of Population Health and Reproduction, School of Veterinary Medicine, University of California, Davis, Davis, CA, USA.
MeSH Terms
- Acepromazine / administration & dosage
- Acepromazine / blood
- Acepromazine / pharmacokinetics
- Acepromazine / pharmacology
- Administration, Oral
- Administration, Sublingual
- Animals
- Chromatography, Liquid / veterinary
- Female
- Horses / blood
- Horses / metabolism
- Hypnotics and Sedatives / administration & dosage
- Hypnotics and Sedatives / blood
- Hypnotics and Sedatives / pharmacokinetics
- Hypnotics and Sedatives / pharmacology
- Infusions, Intravenous / veterinary
- Male
- Physical Conditioning, Animal
- Tandem Mass Spectrometry / veterinary
Citations
This article has been cited 3 times.- Emanuel D, Kästner SBR, Delarocque J, Grob AJ, Bienert-Zeit A. Influence of Butorphanol, Buprenorphine and Levomethadone on Sedation Quality and Postoperative Analgesia in Horses Undergoing Cheek Tooth Extraction.. Vet Sci 2022 Apr 6;9(4).
- Kandeel M, Almubarak AI, Hussen J, El-Deeb W, Venugopala KN. Pharmacokinetic, Clinical, and Myeloid Marker Responses to Acepromazine Sedation in Arabian Camels.. Front Vet Sci 2021;8:725841.
- de Oliveira AR, Gozalo-Marcilla M, Ringer SK, Schauvliege S, Fonseca MW, Trindade PHE, Puoli Filho JNP, Luna SPL. Development, Validation, and Reliability of a Sedation Scale in Horses (EquiSed).. Front Vet Sci 2021;8:611729.
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