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Detomidine

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Detomidine
Clinical data
ATCvet code
Pharmacokinetic data
Elimination half-life30mins
Identifiers
  • 4-[(2,3-dimethylphenyl)methyl]-3H-imidazole
CAS Number
PubChem CID
ChemSpider
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC12H14N2
Molar mass186.253 g/mol g·mol−1
3D model (JSmol)
  • n1cc(nc1)Cc2c(c(ccc2)C)C
  • InChI=1S/C12H14N2/c1-9-4-3-5-11(10(9)2)6-12-7-13-8-14-12/h3-5,7-8H,6H2,1-2H3,(H,13,14) checkY
  • Key:RHDJRPPFURBGLQ-UHFFFAOYSA-N checkY
  (verify)

Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses. Usually available as detomidine hydrochloride. This is a prescription medication available to veterinarians sold under the trade name Dormosedan.

Properties

Detomidine is a sedative with analgesic properties[1]. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters. Due to inhibition of the sympathetic nervous system, detomidine also has cardiac and respiratory effects and an antidiuretic action[2].

Effects

A profound lethargy and characteristic lowering of the head with reduced sensitivity to environmental stimuli (sounds, etc.) are seen with detomidine. A short period of in-coordination is characteristically followed by immobility and a firm stance with front legs spread. Following administration there is an initial increase in blood pressure, followed by bradycardia and second degree atrioventricular block (this is not pathologic in horses). The horse commonly sweats to excess, especially on the flanks and neck. Other side effects reported include pilo erection (hair standing erect), ataxia, salivation, slight muscle tremors, and (rarely) penile prolapse.

Uses

Sedation and anaesthetic premedication in horses and other large animals, commonly combined with butorphanol for increased analgesia and depth of sedation. In conjunction with ketamine it may also be used for intravenous anaesthesia of short duration. Detomidine is only licenced for use in horses at the present time. The drug is normally administered by the intravenous route, and is fastest and most efficient when given intravenously (usually 2–5 minutes to take effect, although this is highly dependent upon the individual and the environment; some horses are highly resistant to sedation!). However, in recalcitrant animals, detomidine may be administered by the intramuscular or sublingual routes. The dose range advised by the manufacturers is 20-40 mcg/kg intravenous for moderate sedation. This dose may need to be higher if given intramuscular.

Cautions

As detomidine is an arrhythmogenic agent, extreme care should be exercised in horses with cardiac disease, and in the concurrent administration of other arrhythmogenics. The concurrent use of potentiated sulfonamide antibiotics is considered particularly dangerous.

Detomidine is a poor premedication when using Ketamine as an anesthetic in horses.

Anesthetic recoveries in horses that have received Ketamine following a Detomidine premedication are often violent with the horse having multiple failures to stand resulting in trauma to itself. Xylazine is a superior premedication with Ketamine resulting in safer recoveries.

References

  1. ^ England GC, Clake KW. α2 adrenoceptor in the horse: a review. Br Vet J. 1996 Nov;152(6):641-57.
  2. ^ Fornai F, Blandizzi C, del Tacca M. Pharmacol Res. 1990 Sep-Oct;22(5):541-54.