Detomidine
Chemical compound
From Wikipedia, the free encyclopedia
Detomidine is an imidazole derivative and α2-adrenergic receptor agonist,[1] 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.
- Veterinary use only
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| Elimination half-life | 30 min |
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| Formula | C12H14N2 |
| Molar mass | 186.258 g·mol−1 |
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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.[2][3] Detomidine's withholding period is 12–72 hours for dairy cattle and 2–3 days for meat cattle.[3]
Properties
Detomidine is a sedative with analgesic properties.[4] 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.[5]
Pharmacology
Detomidine is an α2-adrenergic receptor agonist that binds at a ratio of 260:1 with imidazoline receptor activity.[3]
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%.[3] Intravaginal administration in the horse and alpaca has induced sedation.[3]
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.[3][6][7]