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Journal of veterinary pharmacology and therapeutics2011; 34(1); 76-81; doi: 10.1111/j.1365-2885.2010.01193.x

Bioavailability of detomidine administered sublingually to horses as an oromucosal gel.

Abstract: The objective of the study was to determine the absorption, bioavailability and sedative effect of detomidine administered to horses as an oromucosal gel compared to intravenous and intramuscular administration of detomidine injectable solution. The study was open and randomized, with three sequences crossover design. Nine healthy horses were given 40 μg/kg detomidine intravenously, intramuscularly or administered under the tongue with a 7-day wash-out period between treatments. Blood samples were collected before and after drug administration for the measurement of detomidine concentrations in serum. The effects of the route of administration on heart rate and rhythm were evaluated and the depth of sedation assessed. Mean (±SD) bioavailability of detomidine was 22% (±5.3%) after sublingual administration and 38.2% (±7.9%) after intramuscular administration. The sedative effects correlated with detomidine concentrations regardless of the route of administration. We conclude that less detomidine is absorbed when given sublingually than when given intramuscularly, because part of it does not reach the circulation. Sublingual administration of detomidine oromucosal gel at 40 μg/kg produces safe sedation in horses. Slow absorption leads to fewer and less pronounced adverse effects than the more rapid absorption after intramuscular injection.
Publication Date: 2011-01-12 PubMed ID: 21219348DOI: 10.1111/j.1365-2885.2010.01193.xGoogle Scholar: Lookup
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  • Journal Article
  • Randomized Controlled Trial

Summary

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The research was conducted to understand the absorption, bioavailability, and effects of giving horses detomidine as an oromucosal gel under the tongue, comparing this with injecting the same substance through intravenous and intramuscular means. The study found that less detomidine is absorbed when administered under the tongue than when injected.

Study Design and Methodology

  • The experiment employed an open and randomized arrangement, utilizing a three sequences crossover design.
  • Nine healthy horses were involved in the experiment.
  • Each horse was administered a dose of 40 μg/kg detomidine. The administration was done either intravenously, intramuscularly, or under the tongue.
  • The researchers allowed for a 7-day ‘wash-out’ period between each method of drug administration. This prevented the build-up of the substance in the horses’ bodies that could affect the results.
  • Blood samples were taken before and after medication for detomidine concentration measures in the serum.

Assessment of Effects and Results

  • The impact of the different administration routes on heart rate and rhythm was evaluated.
  • The depth of sedation was assessed to determine the effectiveness of the medicine and how much was absorbed in each method.
  • The bioavailability of detomidine was found to be 22% (±5.3%) for sublingual administration and 38.2% (±7.9%) for intramuscular administration. This meant that detomidine absorption was lower when administered under the tongue than when injected into the muscle.

Findings and Conclusions

  • The study concluded that sublingually administered detomidine partially does not reach the circulation, leading to lower absorption.
  • Despite the lower absorption, sublingual administration of detomidine oromucosal gel at a dosage of 40 μg/kg was found to safely sedate horses.
  • The slower absorption rate resulting from the sublingual application led to fewer and less severe side effects than the intramuscular injection, which is characterized by quicker absorption.

Cite This Article

APA
Kaukinen H, Aspegrén J, Hyyppä S, Tamm L, Salonen JS. (2011). Bioavailability of detomidine administered sublingually to horses as an oromucosal gel. J Vet Pharmacol Ther, 34(1), 76-81. https://doi.org/10.1111/j.1365-2885.2010.01193.x

Publication

ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 34
Issue: 1
Pages: 76-81

Researcher Affiliations

Kaukinen, H
  • Orion Corporation, Orion Pharma, Turku, Finland Agrifood Research Finland, Ypäjä, Finland. helena.kaukinen@orionpharma.com
Aspegrén, J
    Hyyppä, S
      Tamm, L
        Salonen, J S

          MeSH Terms

          • Administration, Sublingual
          • Animals
          • Biological Availability
          • Cross-Over Studies
          • Drug Administration Routes
          • Female
          • Gels
          • Horses / blood
          • Hypnotics and Sedatives / blood
          • Hypnotics and Sedatives / pharmacokinetics
          • Imidazoles / blood
          • Imidazoles / pharmacokinetics
          • Male

          Citations

          This article has been cited 8 times.
          1. Dai F, Rausk J, Aspegren J, Huhtinen M, Cannas S, Minero M. Use of Detomidine Oromucosal Gel for Alleviation of Acute Anxiety and Fear in Horses: A Pilot Study. Front Vet Sci 2020;7:573309.
            doi: 10.3389/fvets.2020.573309pubmed: 33195566google scholar: lookup
          2. Davis JL, Schirmer J, Medlin E. Pharmacokinetics, pharmacodynamics and clinical use of trazodone and its active metabolite m-chlorophenylpiperazine in the horse. J Vet Pharmacol Ther 2018 Jun;41(3):393-401.
            doi: 10.1111/jvp.12477pubmed: 29333613google scholar: lookup
          3. Williams MD, Long CT, Durrant JR, McKeon GP, Shive HR, Griffith EH, Messenger KM, Fish RE. Oral Transmucosal Detomidine Gel in New Zealand White Rabbits (Oryctolagus cuniculus). J Am Assoc Lab Anim Sci 2017 Jul 1;56(4):436-442.
            pubmed: 28724493
          4. Cohen AE, Bennett SL. Oral transmucosal administration of dexmedetomidine for sedation in 4 dogs. Can Vet J 2015 Nov;56(11):1144-8.
            pubmed: 26538668
          5. Hokkanen AH, Raekallio MR, Salla K, Hänninen L, Viitasaari E, Norring M, Raussi S, Rinne VM, Scheinin M, Vainio OM. Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route. Vet Anaesth Analg 2014 Jul;41(4):372-7.
            doi: 10.1111/vaa.12150pubmed: 24628898google scholar: lookup
          6. Di Salvo A, Bazzano M, Rocca GD, Galarini R, Marchegiani A, Paoletti F, Giusepponi D, Mantovani M, Laus F. Pharmacokinetics of a single oral administration of two cannabidiol formulations in fed and fasted horses. Front Vet Sci 2025;12:1515833.
            doi: 10.3389/fvets.2025.1515833pubmed: 40046423google scholar: lookup
          7. Franzen V, Gruber NA, Klußmann S, Schoster A, May A. Effect of repetitive transcranial magnetic stimulation on trigeminal-mediated headshaking in 17 horses. J Vet Intern Med 2024 Sep-Oct;38(5):2758-2765.
            doi: 10.1111/jvim.17194pubmed: 39264234google scholar: lookup
          8. Smith P, Tolbert MK, Gould E, Taylor A, Knych H, Messenger K. Pharmacokinetics, sedation and hemodynamic changes following the administration of oral transmucosal detomidine gel in cats. J Feline Med Surg 2020 Dec;22(12):1184-1190.
            doi: 10.1177/1098612X20917305pubmed: 32643979google scholar: lookup