Detomidine

Detomidine
Clinical data
AHFS/Drugs.com	International Drug Names
ATCvet code	QN05CM90 (WHO) ;
Legal status
Legal status	Veterinary use only;
Pharmacokinetic data
Elimination half-life	30 min
Identifiers
	IUPAC name 4-[(2,3-dimethylphenyl)methyl]-3H-imidazole;
CAS Number	76631-46-4 ;
PubChem CID	56032;
ChemSpider	50586 ;
UNII	7N8K34P2XH;
KEGG	D07795 ;
ChEMBL	ChEMBL2110829 ;
CompTox Dashboard (EPA)	DTXSID00227457 ;
Chemical and physical data
Formula	C12H14N2
Molar mass	186.258 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc2cccc(Cc1cnc[nH]1)c2C;
	InChI 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) ; Key:RHDJRPPFURBGLQ-UHFFFAOYSA-N ;
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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". MedchemExpress.com. Retrieved 2024-11-29.
^ Clarke KW, Hall LW, Trim CM, 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.
^ ^a ^b ^c ^d ^e ^f Lamont LA, Creighton CM. "Sedatives and Tranquilizers". In Lamont L, Grimm K, Robertson S, Love L, Schroeder C (eds.). Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. Wiley Blackwell. pp. 338–344. ISBN 978-1-119-83027-6.
^ England GC, Clarke KW (November 1996). "Alpha 2 adrenoceptor agonists in the horse--a review". The British Veterinary Journal. 152 (6): 641–657. doi:10.1016/S0007-1935(96)80118-7. PMID 8979422.
^ Fornai F, Blandizzi C, del Tacca M (1990). "Central alpha-2 adrenoceptors regulate central and peripheral functions". Pharmacological Research. 22 (5): 541–554. doi:10.1016/S1043-6618(05)80046-5. PMID 2177556.
^ CS C, OS A, WN M, WD B (Feb 1999). "Histopathologic alterations induced in the lungs of sheep by use of alpha2-adrenergic receptor agonists". American Journal of Veterinary Research. 60 (2). Am J Vet Res: 154–161. ISSN 0002-9645. PMID 10048544.
^ Celly C, McDONELL W, Young S, Black W (1997). "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. doi:10.1046/j.1365-2885.1997.00097.x. PMID 9430770.

External links

"Medication Protocols for Horses". The Ontario Association of Equine Practitioners. 2005. Archived from the original on 2007-04-17.
Compendium of data sheets for animal medicines. National Office of Animal Health. 2005. ISBN 978-0-9548037-0-4.

[1] "Detomidine | α2-adrenergic Agonist | MedChemExpress". MedchemExpress.com. Retrieved 2024-11-29.

[2] Clarke KW, Hall LW, Trim CM, 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.

[lamont-3] ^ ^a ^b ^c ^d ^e ^f Lamont LA, Creighton CM. "Sedatives and Tranquilizers". In Lamont L, Grimm K, Robertson S, Love L, Schroeder C (eds.). Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. Wiley Blackwell. pp. 338–344. ISBN 978-1-119-83027-6.

[England_1996-4] England GC, Clarke KW (November 1996). "Alpha 2 adrenoceptor agonists in the horse--a review". The British Veterinary Journal. 152 (6): 641–657. doi:10.1016/S0007-1935(96)80118-7. PMID 8979422.

[Fornai_1990-5] Fornai F, Blandizzi C, del Tacca M (1990). "Central alpha-2 adrenoceptors regulate central and peripheral functions". Pharmacological Research. 22 (5): 541–554. doi:10.1016/S1043-6618(05)80046-5. PMID 2177556.

[6] CS C, OS A, WN M, WD B (Feb 1999). "Histopathologic alterations induced in the lungs of sheep by use of alpha2-adrenergic receptor agonists". American Journal of Veterinary Research. 60 (2). Am J Vet Res: 154–161. ISSN 0002-9645. PMID 10048544.

[7] Celly C, McDONELL W, Young S, Black W (1997). "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. doi:10.1046/j.1365-2885.1997.00097.x. PMID 9430770.

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