Detomidine
Chemical compound
title: "Detomidine" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["alpha2-adrenergic-agonists", "equine-medications", "imidazoles", "sedatives"] description: "Chemical compound" topic_path: "general/alpha2-adrenergic-agonists" source: "https://en.wikipedia.org/wiki/Detomidine" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0
::summary Chemical compound ::
::data[format=table title="Infobox drug"]
| Field | Value |
|---|---|
| Verifiedfields | changed |
| verifiedrevid | 477385293 |
| IUPAC_name | 4-[(2,3-dimethylphenyl)methyl]-3H-imidazole |
| image | Detomidine.png |
| Drugs.com | |
| pregnancy_AU | |
| pregnancy_US | |
| legal_AU | |
| legal_CA | |
| legal_UK | |
| legal_US | |
| legal_status | Veterinary use only |
| elimination_half-life | 30 min |
| CAS_number_Ref | |
| CAS_number | 76631-46-4 |
| ATCvet | yes |
| ATC_prefix | N05 |
| ATC_suffix | CM90 |
| PubChem | 56032 |
| DrugBank_Ref | |
| ChEMBL_Ref | |
| ChEMBL | 2110829 |
| ChemSpiderID_Ref | |
| ChemSpiderID | 50586 |
| UNII_Ref | |
| UNII | 7N8K34P2XH |
| KEGG_Ref | |
| KEGG | D07795 |
| C | 12 |
| smiles | Cc2cccc(Cc1cnc[nH]1)c2C |
| StdInChI_Ref | |
| StdInChI | 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) |
| StdInChIKey_Ref | |
| StdInChIKey | RHDJRPPFURBGLQ-UHFFFAOYSA-N |
| :: |
| Verifiedfields = changed | verifiedrevid = 477385293 | IUPAC_name = 4-[(2,3-dimethylphenyl)methyl]-3H-imidazole | image = Detomidine.png
| tradename = | Drugs.com = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Veterinary use only | routes_of_administration =
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = 30 min | excretion =
| CAS_number_Ref = | CAS_number = 76631-46-4 | ATCvet = yes | ATC_prefix = N05 | ATC_suffix = CM90 | PubChem = 56032 | DrugBank_Ref = | DrugBank = | ChEMBL_Ref = | ChEMBL = 2110829 | ChemSpiderID_Ref = | ChemSpiderID = 50586 | UNII_Ref = | UNII = 7N8K34P2XH | KEGG_Ref = | KEGG = D07795
| C=12 | H=14 | N=2 | smiles = Cc2cccc(Cc1cnc[nH]1)c2C | StdInChI_Ref = | StdInChI = 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) | StdInChIKey_Ref = | StdInChIKey = RHDJRPPFURBGLQ-UHFFFAOYSA-N
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.
References
References
- "Detomidine {{!}} α2-adrenergic Agonist {{!}} MedChemExpress".
- (2014). "Veterinary Anaesthesia".
- (November 1996). "Alpha 2 adrenoceptor agonists in the horse--a review". The British Veterinary Journal.
- (1990). "Central alpha-2 adrenoceptors regulate central and peripheral functions". Pharmacological Research.
- "Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones". Wiley Blackwell.
- (Feb 1999). "Histopathologic alterations induced in the lungs of sheep by use of alpha2-adrenergic receptor agonists". Am J Vet Res.
- (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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