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Journal of veterinary pharmacology and therapeutics1987; 10(3); 218-226; doi: 10.1111/j.1365-2885.1987.tb00532.x

Pharmacokinetics of dantrolene sodium in horses.

Abstract: The pharmacokinetics of dantrolene sodium were investigated in horses following both intravenous (2 mg/kg) and intragastric (4 mg/kg) administration. Two ponies also received dantrolene sodium intravenously (2 mg/kg) in a pilot study to obtain preliminary kinetic data and to determine urinary and biliary excretion of the intact drug. Distribution and elimination of dantrolene was rapid, resulting in an elimination half-life of 129 +/- 8 (SEM) min and a whole body clearance of 4.16 +/- 0.52 ml/min/kg. Following intragastric administration, dantrolene rapidly acheived peak concentrations within 1.5 h, but was incompletely absorbed, with a bioavailability of 39 +/- 10%. Small amounts of intact drug were recovered in urine and bile. Based upon disposition kinetics of dantrolene in these studies, intravenous and intragastric dosage regimens were determined which would maintain blood dantrolene concentrations within the predicted clinically effective range.
Publication Date: 1987-09-01 PubMed ID: 3656508DOI: 10.1111/j.1365-2885.1987.tb00532.xGoogle Scholar: Lookup
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  • Comparative Study
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research article studies the pharmacokinetics of dantrolene sodium in horses, investigating its distribution and elimination after intravenous and intragastric administration.

Objective of the Research

  • This research aimed to understand the way horses absorb, distribute, metabolize, and excrete dantrolene sodium; a muscle relaxation drug commonly used in medicine. It involved both intravenous (IV) and intragastric (IG) administration of the drug, which helps in determining its effectiveness and dosage guidelines.

Study Design and Participants

  • The research involved administering the drug to horses, with both IV and IG routes being used. The dosage was 2 mg/kg for intravenous and 4 mg/kg for intragastric administrations.
  • Additionally, two ponies received an intravenous dose of the drug in a pilot study, providing preliminary kinetic data and helping in the assessment of urinary and biliary excretion of the medication.

Findings from the Research

  • The results showed that the distribution and elimination of dantrolene were rapid in horses, with an elimination half-life of approximately 129 minutes and a whole-body clearance rate of around 4.16 ml/min/kg.
  • After intragastric administration, the peak concentration of dantrolene was achieved rapidly, within 1.5 hours. However, absorption was incomplete, resulting in a bioavailability of around 39%.
  • Only small quantities of the intact drug were recovered in urine and bile, suggesting most of the medication was metabolized.

Implication of the Findings

  • The findings from this research are crucial as they help establish dosage guidelines for veterinary application of dantrolene sodium, aiming to maintain the blood concentration of the drug within the predicted clinically effective range.

Cite This Article

APA
Court MH, Engelking LR, Dodman NH, Anwer MS, Seeler DC, Clark M. (1987). Pharmacokinetics of dantrolene sodium in horses. J Vet Pharmacol Ther, 10(3), 218-226. https://doi.org/10.1111/j.1365-2885.1987.tb00532.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 10
Issue: 3
Pages: 218-226

Researcher Affiliations

Court, M H
  • Department of Surgery, Tufts University, School of Veterinary Medicine, North Grafton, Massachusetts 01536.
Engelking, L R
    Dodman, N H
      Anwer, M S
        Seeler, D C
          Clark, M

            MeSH Terms

            • Animals
            • Bile / metabolism
            • Dantrolene / administration & dosage
            • Dantrolene / blood
            • Dantrolene / pharmacokinetics
            • Dantrolene / urine
            • Female
            • Horses / metabolism
            • Injections, Intravenous
            • Intubation, Gastrointestinal

            Citations

            This article has been cited 1 times.
            1. Fernandez-Fuente M, Terracciano CM, Martin-Duque P, Brown SC, Vassaux G, Piercy RJ. Calcium homeostasis in myogenic differentiation factor 1 (MyoD)-transformed, virally-transduced, skin-derived equine myotubes. PLoS One 2014;9(8):e105971.
              doi: 10.1371/journal.pone.0105971pubmed: 25148524google scholar: lookup