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| AHFS/Drugs.com | International Drug Names |
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| Eliminationhalf-life | 30 min |
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| Formula | C12H14N2 |
| Molar mass | 186.258 g·mol−1 |
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Detomidine is animidazole derivative andα2-adrenergic receptoragonist,[1] used as a large animalsedative, primarily used inhorses. It is usually available as thesalt detomidinehydrochloride. It is aprescription medication available to veterinarians sold under various trade names.
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.[2][3] Detomidine's withholding period is 12–72 hours fordairy cattle and 2–3 days formeat cattle.[3]
Detomidine is a sedative withanalgesic properties.[4] α2-adrenergic receptor agonists produce dose-dependent sedative and analgesic effects, mediated by activation of α2catecholamine receptors, thus inducing anegative feedback response, reducing production of excitatory neurotransmitters. Due to inhibition of thesympathetic nervous system, detomidine also has cardiac and respiratory effects and anantidiuretic action.[5]
Detomidine is an α2-adrenergic receptor agonist that binds at a ratio of 260:1 withimidazoline receptor activity.[3]
Detomidine is administeredintramuscularly.Oral transmucosal has been investigated and is used in some countries although it has poor bioavailability of around 20–25%.[3]Intravaginal administration in the horse and alpaca has induced sedation.[3]
Detomidine administration in sheep activates pulmonary macrophages that damage theendothelium of capillaries andalveolar type I cells. This in turns causes alveolar haemorrhage and oedema causing hypoxaemia.[3][6][7]
