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Detomidine

Chemical compound


Chemical compound

FieldValue
Verifiedfieldschanged
verifiedrevid477385293
IUPAC_name4-[(2,3-dimethylphenyl)methyl]-3H-imidazole
imageDetomidine.png
Drugs.com
pregnancy_AU
pregnancy_US
legal_AU
legal_CA
legal_UK
legal_US
legal_statusVeterinary use only
elimination_half-life30 min
CAS_number_Ref
CAS_number76631-46-4
ATCvetyes
ATC_prefixN05
ATC_suffixCM90
PubChem56032
DrugBank_Ref
ChEMBL_Ref
ChEMBL2110829
ChemSpiderID_Ref
ChemSpiderID50586
UNII_Ref
UNII7N8K34P2XH
KEGG_Ref
KEGGD07795
C12H=14N=2
smilesCc2cccc(Cc1cnc[nH]1)c2C
StdInChI_Ref
StdInChI1S/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)
StdInChIKey_Ref
StdInChIKeyRHDJRPPFURBGLQ-UHFFFAOYSA-N

| Drugs.com =

| elimination_half-life = 30 min

Detomidine is an imidazole derivative and α2-adrenergic receptor agonist, used as a large animal sedative, primarily used in horses. It is usually available as the salt detomidine hydrochloride. It is a prescription medication available to veterinarians sold under various trade names.

Use

Currently, detomidine is licensed for use only in non-meat horses in the United States, but it is also licensed for use in cattle in Europe and Australia. Detomidine's withholding period is 12–72 hours for dairy cattle and 2–3 days for meat cattle.

Properties

Detomidine is a sedative with analgesic properties. α2-adrenergic receptor agonists produce dose-dependent sedative and analgesic effects, mediated 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.

Pharmacology

Detomidine is an α2-adrenergic receptor agonist that binds at a ratio of 260:1 with imidazoline receptor activity.

Veterinary use

Detomidine is administered intramuscularly. Oral transmucosal has been investigated and is used in some countries although it has poor bioavailability of around 20–25%. Intravaginal administration in the horse and alpaca has induced sedation.

Detomidine administration in sheep activates pulmonary macrophages that damage the endothelium of capillaries and alveolar type I cells. This in turns causes alveolar haemorrhage and oedema causing hypoxaemia.

  • Medetomidine
  • Dexmedetomidine

References

References

  1. "Detomidine {{!}} α2-adrenergic Agonist {{!}} MedChemExpress".
  2. (2014). "Veterinary Anaesthesia".
  3. (November 1996). "Alpha 2 adrenoceptor agonists in the horse--a review". The British Veterinary Journal.
  4. (1990). "Central alpha-2 adrenoceptors regulate central and peripheral functions". Pharmacological Research.
  5. "Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones". Wiley Blackwell.
  6. (Feb 1999). "Histopathologic alterations induced in the lungs of sheep by use of alpha2-adrenergic receptor agonists". Am J Vet Res.
  7. (1997). "The comparative hypoxaemic effect of four α 2 adrenoceptor agonists (xylazine, romifidine, detomidine and medetomidine) in sheep". Journal of Veterinary Pharmacology and Therapeutics.
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