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Journal of veterinary pharmacology and therapeutics1989; 12(1); 65-72; doi: 10.1111/j.1365-2885.1989.tb00643.x

Single-dose pharmacokinetics of detomidine in the horse and cow.

Abstract: The pharmacokinetics of detomidine, a novel analgesic sedative, was studied in the major target species after high (80 micrograms/kg) i.v. and i.m. doses. In addition, drug residues in some organs were determined. Concentrations were measured using a sensitive, detomidine-specific radio-immunoassay method. Rapid absorption following i.m. dosing occurred. Absorption half-lives were 0.15 h (horse) and 0.08 h (cattle). The mean peak concentration in the horse (51.3 ng/ml) was achieved in 0.5 h and in the cow (65.8 ng/ml) in 0.26 h. The areas under the concentration curve after i.m. dosing were 66% (horse) and 85% (cow) of the corresponding i.v. values. Distribution was rapid with half-lives of 0.15 h (horse, i.v.) and 0.24 h (cow, i.v.). The apparent volume of distribution was higher after the i.m. dosing (horse 1.56 l/kg, cow 1.89 l/kg) than after i.v. dosing (horse 0.74 l/kg, cow 0.73 l/kg). Elimination half-lives were 1.19 h (horse) and 1.32 h (cow) for the i.v. dose and 1.78 h (horse) and 2.56 h (cow) for the i.m. dose. Total clearances ranged from 6.7 (horse, i.v.) to 12.3 (cow, i.m.) ml/min/kg. Renal clearances were less than 1% of the total clearances showing negligible excretion of the drug in urine and suggesting elimination by metabolism. A cross-reacting metabolite in urine corresponded to less than 1.5% of the detomidine dose's immunoreactivity. High-dose detomidine increased urine flow significantly. Excretion of detomidine in milk in cattle was extremely low. No detectable amounts were present 23 h after dosing.(ABSTRACT TRUNCATED AT 250 WORDS)
Publication Date: 1989-03-01 PubMed ID: 2704064DOI: 10.1111/j.1365-2885.1989.tb00643.xGoogle Scholar: Lookup
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  • Journal Article

Summary

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This research article presents an investigation into how the drug detomidine, a sedative used in veterinary treatment, is absorbed, distributed, and eliminated in horses and cows. It reveals direct links between how the drug is administered (intramuscularly or intravenously), and how this impacts the drug’s efficiency and effect on the animal’s body.

Overview of Research

  • The article’s main focus is evaluating how detomidine, an analgesic sedative used in animal medicine, affects horses and cows. It looks at how quickly this drug absorbs in the animal’s body, how it disperses and finally, how it’s eliminated.
  • This study used both intravenous (i.v.) and intramuscular (i.m.) methods of administering the drug, enabling it to compare the effects of the two approaches on detomidine’s performance.

Administration and Absorption

  • The research found that the drug is rapidly absorbed following intramuscular injection, with an absorption half-life of 0.15 hours in horses and 0.08 hours in cows.
  • Detomidine reached its mean peak concentration within 0.5 hours for the horse and slightly quicker, at 0.26 hours, for the cow.
  • The study identified that after intramuscular dosing, the areas under the concentration curve (representing the total exposure to the drug) were 66% for the horse and 85% for the cow compared to the corresponding intravenous values.

Distribution and Elimination

  • Distribution after administration was rapid, with the drug’s half-life indicated at 0.15 hours for the i.v. method in horses and 0.24 hours for i.v. in cows.
  • The volume of distribution, a term used to describe the extent of a drug’s penetration into the body, was found to be higher through intramuscular administration rather than intravenous.
  • The elimination half-life figures indicated that the drug persisted slightly longer in the body when administered via the intramuscular route as compared to the intravenous method.
  • The low percentages of renal clearances suggest that the drug was largely eliminated through metabolism rather than excretion in urine.
  • The authors also discovered that high doses of detomidine resulted in increased urine flow, despite relatively low levels of the drug appearing in urine output.

Residue in other biological substances

  • Lastly, the researchers observed that the residue of detomidine in cow’s milk was extremely low, with no detectable amounts found 23 hours after dosing.

Cite This Article

APA
Salonen JS, Vähä-Vahe T, Vainio O, Vakkuri O. (1989). Single-dose pharmacokinetics of detomidine in the horse and cow. J Vet Pharmacol Ther, 12(1), 65-72. https://doi.org/10.1111/j.1365-2885.1989.tb00643.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 12
Issue: 1
Pages: 65-72

Researcher Affiliations

Salonen, J S
  • Farmos Group Ltd., Research Center, Turku, Finland.
Vähä-Vahe, T
    Vainio, O
      Vakkuri, O

        MeSH Terms

        • Absorption
        • Analgesics / administration & dosage
        • Analgesics / pharmacokinetics
        • Analgesics / urine
        • Animals
        • Cattle / metabolism
        • Drug Residues / analysis
        • Female
        • Half-Life
        • Horses / metabolism
        • Hypnotics and Sedatives / administration & dosage
        • Hypnotics and Sedatives / pharmacokinetics
        • Hypnotics and Sedatives / urine
        • Imidazoles / administration & dosage
        • Imidazoles / pharmacokinetics
        • Imidazoles / urine
        • Injections, Intramuscular / veterinary
        • Injections, Intravenous / veterinary
        • Male
        • Milk / metabolism
        • Tissue Distribution

        Citations

        This article has been cited 5 times.
        1. Jarosinski SK, Simon BT, Hatfield R, Matthews NS, Arnold CE. The effects of xylazine or detomidine when used as a pre-anesthetic sedative on recovery quality and duration in horses undergoing elective equine castration. Can Vet J 2021 Sep;62(9):982-986.
          pubmed: 34475584
        2. 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
        3. Jones DL. Clinical effects of detomidine with or without atropine used for arthrocentesis in horses. Can Vet J 1993 May;34(5):296-300.
          pubmed: 17424223
        4. Lin HC, Branson KR, Thurmon JC, Benson GJ, Tranquilli WJ, Olson WA, Vähä-Vahe AT. Ketamine, Telazol, xylazine and detomidine. A comparative anesthetic drug combinations study in ponies. Acta Vet Scand 1992;33(2):109-15.
          doi: 10.1186/BF03547317pubmed: 1502994google scholar: lookup
        5. Salonen JS, Vuorilehto L, Gilbert M, Maylin GA. Identification of detomidine carboxylic acid as the major urinary metabolite of detomidine in the horse. Eur J Drug Metab Pharmacokinet 1992 Jan-Mar;17(1):13-20.
          doi: 10.1007/BF03189982pubmed: 1499593google scholar: lookup