Chemistry:Detomidine
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.
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]
References
- ↑ "Detomidine | α2-adrenergic Agonist | MedChemExpress". https://www.medchemexpress.com/detomidine.html?srsltid=AfmBOop2_l6_W7WPv9Ky9jWhDf64HSbIcSOZOCi8tA0mUmiLHrM2bPAB.
- ↑ Clarke, Kathy W.; Hall, Leslie W.; Trim, Cynthia M., eds (2014). "Principles of sedation, anticholinergic agents, and principles of premedication". Veterinary Anaesthesia. pp. 79–100. doi:10.1016/B978-0-7020-2793-2.00004-9. ISBN 978-0-7020-2793-2.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 "Sedatives and Tranquilizers". Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. Wiley Blackwell. pp. 338–344. ISBN 978-1-119-83027-6.
- ↑ "Alpha 2 adrenoceptor agonists in the horse--a review". The British Veterinary Journal 152 (6): 641–657. November 1996. doi:10.1016/S0007-1935(96)80118-7. PMID 8979422.
- ↑ "Central alpha-2 adrenoceptors regulate central and peripheral functions". Pharmacological Research 22 (5): 541–554. 1990. doi:10.1016/S1043-6618(05)80046-5. PMID 2177556.
- ↑ "Histopathologic alterations induced in the lungs of sheep by use of alpha2-adrenergic receptor agonists". American Journal of Veterinary Research (Am J Vet Res) 60 (2): 154–161. Feb 1999. ISSN 0002-9645. PMID 10048544.
- ↑ "The comparative hypoxaemic effect of four α 2 adrenoceptor agonists (xylazine, romifidine, detomidine and medetomidine) in sheep". Journal of Veterinary Pharmacology and Therapeutics 20 (6): 464–471. 1997. doi:10.1046/j.1365-2885.1997.00097.x. PMID 9430770.
External links
- "Medication Protocols for Horses". The Ontario Association of Equine Practitioners. 2005. http://www.oaep.on.ca/MedsSheets/MainPage.htm.
- Compendium of data sheets for animal medicines.. National Office of Animal Health. 2005. ISBN 978-0-9548037-0-4.
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