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{{Short description|Chemical compound}} |
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{{drugbox |
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{{Drugbox |
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| Verifiedfields = changed |
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| Verifiedfields = changed |
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| verifiedrevid = 477385293 |
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| Watchedfields = changed |
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| IUPAC_name = 4--3''H''-imidazole |
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| UNII_Ref = {{fdacite|changed|FDA}} |
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| UNII = 7N8K34P2XH |
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| image = Detomidine.png |
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| verifiedrevid = 412690003 |
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<!--Clinical data--> |
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| IUPAC_name = 4--3''H''-imidazole |
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| tradename = |
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| image = Detomidine.png |
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| Drugs.com = {{drugs.com|international|detomidine}} |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category = |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = Veterinary use only |
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| routes_of_administration = |
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<!--Pharmacokinetic data--> |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = 30 min |
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| excretion = |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|changed|??}} |
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| CAS_number = 76631-46-4 |
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| ATCvet = yes |
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| ATC_prefix = N05 |
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| ATC_suffix = CM90 |
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| PubChem = 56032 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = 2110829 |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 50586 |
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| ChemSpiderID = 50586 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| InChI = 1/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) |
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| UNII = 7N8K34P2XH |
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| smiles = n1cc(nc1)Cc2c(c(ccc2)C)C |
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| KEGG_Ref = {{keggcite|changed|kegg}} |
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| InChIKey = RHDJRPPFURBGLQ-UHFFFAOYAM |
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| KEGG = D07795 |
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<!--Chemical data--> |
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| C=12 | H=14 | N=2 |
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| smiles = Cc2cccc(Cc1cnc1)c2C |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| 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) |
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| 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) |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = RHDJRPPFURBGLQ-UHFFFAOYSA-N |
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| StdInChIKey = RHDJRPPFURBGLQ-UHFFFAOYSA-N |
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| CAS_number = 86347-15-1 |
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| ATCvet = yes |
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| ATC_prefix = N05 |
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| ATC_suffix = CM90 |
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| PubChem = 56032 |
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| DrugBank = |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG = D07795 |
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| C=12|H=14|N=2 |
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| molecular_weight = 186.253 g/mol |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = 30mins |
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| excretion = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category= |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = |
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| routes_of_administration = |
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}} |
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}} |
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'''Detomidine''' is an ] derivative and ] ], used as a large animal ], primarily used in ]. It is usually available as the ] detomidine ]. It is a ] available to veterinarians sold under the trade name Dormosedan. |
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'''Detomidine''' is an ] derivative and ] ],<ref>{{Cite web |title=Detomidine {{!}} α2-adrenergic Agonist {{!}} MedChemExpress |url=https://www.medchemexpress.com/detomidine.html?srsltid=AfmBOop2_l6_W7WPv9Ky9jWhDf64HSbIcSOZOCi8tA0mUmiLHrM2bPAB |access-date=2024-11-29 |website=MedchemExpress.com}}</ref> used as a large animal ], primarily used in ]s. It is usually available as the ] detomidine ]. It is a ] available to veterinarians sold under various trade names. |
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Currently, detomidine is licensed for use only in horses in the US but it is also licensed for use in cattle in Europe and Australasia.<ref>{{cite book |doi=10.1016/B978-0-7020-2793-2.00004-9 |chapter=Principles of sedation, anticholinergic agents, and principles of premedication |title=Veterinary Anaesthesia |year=2014 |pages=79–100 |isbn=978-0-7020-2793-2 |editor1-last=Clarke |editor1-first=Kathy W. |editor2-last=Hall |editor2-first=Leslie W. |editor3-last=Trim |editor3-first=Cynthia M. }}</ref> |
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==Properties== |
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==Properties== |
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Detomidine is a sedative with ] properties.<ref>{{cite journal | author = England GC, Clake KW. α2 adrenoceptor in the horse: a review. | journal = Br Vet J. | year = 1996 | volume = 152 | issue = 6 | pages = 641–657}}</ref> α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 ] receptors, thus inducing a ] response, reducing production of excitatory neurotransmitters. Due to inhibition of the ], detomidine also has cardiac and respiratory effects and an ] action.<ref>{{cite journal | author = Fornai F, Blandizzi C, del Tacca M. | journal = Pharmacol Res. | year = 1990 | volume = 22 | issue = 5 | pages = 541–54}}</ref> |
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Detomidine is a sedative with ] properties.<ref name="England 1996">{{cite journal | vauthors = England GC, Clarke KW | title = Alpha 2 adrenoceptor agonists in the horse--a review | journal = The British Veterinary Journal | volume = 152 | issue = 6 | pages = 641–57 | date = November 1996 | pmid = 8979422 | doi = 10.1016/S0007-1935(96)80118-7 }}</ref> α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediated by activation of α2 ] receptors, thus inducing a ] response, reducing production of excitatory neurotransmitters. Due to inhibition of the ], detomidine also has cardiac and respiratory effects and an ] action.<ref name="Fornai 1990">{{cite journal | vauthors = Fornai F, Blandizzi C, del Tacca M | title = Central alpha-2 adrenoceptors regulate central and peripheral functions | journal = Pharmacological Research | volume = 22 | issue = 5 | pages = 541–54 | date = 1990 | pmid = 2177556 | doi = 10.1016/S1043-6618(05)80046-5 }}</ref> |
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==Effects== |
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==Effects== |
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{{Unreferenced section|date=December 2020}} |
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A profound lethargy and characteristic lowering of the head with reduced sensitivity to environmental stimuli (sounds, etc.) are seen with detomidine. A short period of in-coordination is characteristically followed by immobility and a firm stance with front legs spread. Following administration there is an initial increase in blood pressure, followed by ] and second degree ] (this is not ] in horses). The horse commonly ]s to excess, especially on the flanks and neck. Other side effects reported include pilo erection (hair standing erect), ], ], slight muscle tremors, and (rarely) penile prolapse. |
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A profound lethargy and characteristic lowering of the head with reduced sensitivity to environmental stimuli (sound, pain, etc.) are seen with detomidine. A short period of reduced coordination is characteristically followed by immobility and a firm stance with front legs spread. Following administration there is an initial increase in blood pressure, followed by ] and second degree ] (this is not ] in horses). The horse commonly ]s to excess, especially on the flanks and neck. Other side effects reported include pilo erection (hair standing erect), ], ], slight muscle tremors, and (rarely) penile prolapse. |
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==Uses== |
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==Uses== |
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{{Unreferenced section|date=December 2020}} |
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Sedation and anaesthetic ] in horses and other large animals, commonly combined with ] for increased analgesia and depth of sedation. In conjunction with ] it may also be used for intravenous ] of short duration. Detomidine is only licenced for use in horses at the present time. |
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Sedation and anaesthetic ] in horses and other large animals, commonly combined with ] for increased analgesia and depth of sedation. In conjunction with ] it may also be used for intravenous ] of short duration. |
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The drug is normally administered by the ] route, and is fastest and most efficient when given intravenously (usually 2–5 minutes to take effect, although this is highly dependent upon the individual and the environment; some horses are highly resistant to sedation!). However, in recalcitrant animals, detomidine may be administered by the ] or ] routes. The dose range advised by the manufacturers is 20-40 mcg/kg intravenous for moderate sedation. This dose may need to be higher if given intramuscular. |
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The drug is normally administered by the ] route, and is fastest and most efficient when given intravenously . However, in recalcitrant animals, detomidine may be administered by the ] or ] routes. The dose range advised by the manufacturers is 20–40 μg/kg intravenous for moderate sedation, but this dose may need to be higher if given intramuscularly. |
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When given intravenously, detomidine usually takes effect in 2–5 minutes, and recovery is full within 30–60 minutes. However, this is highly dependent upon the dosage, environment, and the individual animal; some horses are highly resistant to sedation. |
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==Cautions== |
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==Cautions== |
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{{Unreferenced section|date=December 2020}} |
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As detomidine is an ] agent, extreme care should be exercised in horses with cardiac disease, and in the concurrent administration of other arrhythmogenics. The concurrent use of potentiated ] ] is considered particularly dangerous. |
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As detomidine is an ] agent, extreme care should be exercised in horses with cardiac disease, and in the concurrent administration of other arrhythmogenics. The concurrent use of potentiated ] ] is considered particularly dangerous. |
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Anesthetic recoveries in horses that have received ketamine following a detomidine premedication are often violent with the horse having multiple failures to stand resulting in trauma to itself. ] is a superior premedication with ketamine resulting in safer recoveries. |
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Detomidine is a poor premedication when using Ketamine as an anesthetic in horses. |
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== See also == |
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Anesthetic recoveries in horses that have received Ketamine following a Detomidine premedication are often violent with the horse having multiple failures to stand resulting in trauma to itself. Xylazine is a superior premedication with Ketamine resulting in safer recoveries. |
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* ] |
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* ] |
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==References== |
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== References == |
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{{Reflist}} |
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{{Reflist}} |
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== External links == |
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* The Ontario Association of Equine Practitioners, ''Medication Protocols for Horses'' 2005 <http://www.oaep.on.ca/MedsSheets/MainPage.htm> |
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{{refbegin}} |
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* NOAH Compendium of Data Sheets for Animal Medicines 2005 |
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* {{cite web | work = The Ontario Association of Equine Practitioners | title = Medication Protocols for Horses | date = 2005 | url = http://www.oaep.on.ca/MedsSheets/MainPage.htm | archive-url = https://web.archive.org/web/20070417021529/http://www.oaep.on.ca/MedsSheets/MainPage.htm | url-status = dead | archive-date = 2007-04-17 }} |
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* {{cite book |title=Compendium of data sheets for animal medicines. | date = 2005 |publisher=National Office of Animal Health |isbn=978-0-9548037-0-4}} |
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{{refend}} |
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{{Hypnotics and sedatives}} |
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{{Adrenergic agonists}} |
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{{Adrenergic receptor modulators}} |
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