Medetomidine is a synthetic drug used as both a surgical anesthetic and analgesic. It is often used as the hydrochloridesalt, medetomidine hydrochloride, a crystalline white solid. It is an α2 adrenergic agonist[1] that can be administered as an intravenous drug solution with sterile water.
It was developed by Orion Pharma.[2] It is approved for dogs in the United States, and distributed in the United States by Pfizer Animal Health and by Novartis Animal Health in Canada under the product name Domitor. Other alpha-two agonists used in veterinary medicine include xylazine and detomidine, but their use is less common in small animal surgery. The marketed product is a racemic mixture of two stereoisomers; dexmedetomidine is the isomer with more useful effects, and is now marketed as Dexdomitor. The free base form of medetomidine is sold as Selektope for use as an antifouling substance in marine paints.[3]
In veterinary anesthesia, medetomidine is often used in combinations with opioids (butorphanol, buprenorphine etc.) as premedication (before a general anesthetic) in healthy cats and dogs. It can be given by intramuscular injection (IM), subcutaneous injection (SC) or intravenous injection (IV). When delivered intravenously, a significantly decreased dose is used. Some authors suggest a sublingual route is also effective. It is not recommended for diabetics, it is contraindicated in patients with cardiac disease. Due to its potent sedative effects it is commonly used in more aggressive animals, where a drug combination with a lesser effect (such as acepromazine plus an opioid, or an opioid plus a benzodiazepine) would not allow the administration of the inductive agent without risk to the veterinarian. As such the use of alpha-two agonists is only recommended in healthy animals.
Following administration, marked peripheral vasoconstriction and bradycardia are noted. Often the dosage of induction agents (e.g. propofol) may be drastically reduced, as may the volumes of anesthetic gases (i.e. halothane, isoflurane, sevoflurane) used to maintain general anesthesia.
It is sometimes used in combination with butorphanol and ketamine (given IM) to produce general anaesthesia for short periods in healthy but fractious felines that will not allow an intravenous induction agent to be given. It provides a good degree of muscle relaxation, an important factor in ketamine based anesthesia protocols.
Medetomidine has also been used in combination with morphine (or methadone), lidocaine and ketamine in constant rate infusion analgesia in canines. It is often used in so called microdoses for this analgesic effect.
It is thought that this family of drugs has a degree of analgesic action, though this is, in comparison to the sedative effect, minor.
Its effects can be reversed using atipamezole (distributed as Antisedan by Pfizer). IV use of atipamezole is not licensed, IM is the preferred route. Yohimbine may also be used in an emergency situation, but is not licensed.
Use in marine paintedit
Medetomidine can be used as an antifouling substance in marine paint. It is mainly effective against barnacles, but has also shown effect on other hard fouling like tube worms. When the barnacle cyprid larva encounters a surface containing medetomidine the molecule interacts with the octopamine receptor in the larva. This causes the settling larva to increase its kicking to more than 100 kicks per minute,[4] which makes becoming sessile nearly impossible. When the larva swims away from the surface, the effect disappears (reversible effect). The larva regains its pre-exposure function and can settle somewhere else.
^Sinclair MD (November 2003). "A review of the physiological effects of alpha2-agonists related to the clinical use of medetomidine in small animal practice". The Canadian Veterinary Journal. 44 (11): 885–97. PMC385445. PMID 14664351.
^. Orion Corporation. Archived from the original on March 15, 2013.
^Chaabane P. "The Selektope Story" (PDF). PCI Magazine. Retrieved 12 December 2018.
^Lind U, Alm Rosenblad M, Hasselberg Frank L, Falkbring S, Brive L, Laurila JM, et al. (August 2010). "Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine". Molecular Pharmacology. 78 (2): 237–48. doi:10.1124/mol.110.063594. PMID 20488921. S2CID 17792301.
Further readingedit
. Novartis Animal Health Canada. 2003. Archived from the original on 2007-09-24.
Lind U, Alm Rosenblad M, Hasselberg Frank L, Falkbring S, Brive L, Laurila JM, et al. (August 2010). "Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine". Molecular Pharmacology. 78 (2): 237–48. doi:10.1124/mol.110.063594. PMID 20488921. S2CID 17792301.
Dahlström M, Mårtensson LG, Jonsson PR, Arnebrant T, Elwing H (November 2000). "Surface active adrenoceptor compounds prevent the settlement of cyprid larvae of Balanus improvisus". Biofouling. 16 (2–4): 191–203. doi:10.1080/08927010009378444. S2CID 85603381.
December 14, 2023
medetomidine, this, article, needs, additional, citations, verification, please, help, improve, this, article, adding, citations, reliable, sources, unsourced, material, challenged, removed, find, sources, news, newspapers, books, scholar, jstor, january, 2016. This article needs additional citations for verification Please help improve this article by adding citations to reliable sources Unsourced material may be challenged and removed Find sources Medetomidine news newspapers books scholar JSTOR January 2016 Learn how and when to remove this template message Medetomidine is a synthetic drug used as both a surgical anesthetic and analgesic It is often used as the hydrochloride salt medetomidine hydrochloride a crystalline white solid It is an a2 adrenergic agonist 1 that can be administered as an intravenous drug solution with sterile water MedetomidineClinical dataAHFS Drugs comMonographATCvet codeQN05CM91 WHO Legal statusLegal statusVeterinary use onlyIdentifiersIUPAC name RS 4 1 2 3 Dimethylphenyl ethyl 3H imidazoleCAS Number86347 14 0 NPubChem CID68602DrugBankDB00633 YChemSpider61868 YUNIIMR15E85MQMKEGGD08165 YChEBICHEBI 48552 YChEMBLChEMBL77921 YCompTox Dashboard EPA DTXSID6048258ECHA InfoCard100 242 450Chemical and physical dataFormulaC 13H 16N 2Molar mass200 285 g mol 13D model JSmol Interactive imageChiralityRacemic mixtureSMILES n1cc nH c1 C c2c c ccc2 C C CInChI InChI 1S C13H16N2 c1 9 5 4 6 12 10 9 2 11 3 13 7 14 8 15 13 h4 8 11H 1 3H3 H 14 15 YKey CUHVIMMYOGQXCV UHFFFAOYSA N Y N Y what is this verify It was developed by Orion Pharma 2 It is approved for dogs in the United States and distributed in the United States by Pfizer Animal Health and by Novartis Animal Health in Canada under the product name Domitor Other alpha two agonists used in veterinary medicine include xylazine and detomidine but their use is less common in small animal surgery The marketed product is a racemic mixture of two stereoisomers dexmedetomidine is the isomer with more useful effects and is now marketed as Dexdomitor The free base form of medetomidine is sold as Selektope for use as an antifouling substance in marine paints 3 Contents 1 Veterinary use 2 Use in marine paint 3 References 4 Further readingVeterinary use editIn veterinary anesthesia medetomidine is often used in combinations with opioids butorphanol buprenorphine etc as premedication before a general anesthetic in healthy cats and dogs It can be given by intramuscular injection IM subcutaneous injection SC or intravenous injection IV When delivered intravenously a significantly decreased dose is used Some authors suggest a sublingual route is also effective It is not recommended for diabetics it is contraindicated in patients with cardiac disease Due to its potent sedative effects it is commonly used in more aggressive animals where a drug combination with a lesser effect such as acepromazine plus an opioid or an opioid plus a benzodiazepine would not allow the administration of the inductive agent without risk to the veterinarian As such the use of alpha two agonists is only recommended in healthy animals Following administration marked peripheral vasoconstriction and bradycardia are noted Often the dosage of induction agents e g propofol may be drastically reduced as may the volumes of anesthetic gases i e halothane isoflurane sevoflurane used to maintain general anesthesia It is sometimes used in combination with butorphanol and ketamine given IM to produce general anaesthesia for short periods in healthy but fractious felines that will not allow an intravenous induction agent to be given It provides a good degree of muscle relaxation an important factor in ketamine based anesthesia protocols Medetomidine has also been used in combination with morphine or methadone lidocaine and ketamine in constant rate infusion analgesia in canines It is often used in so called microdoses for this analgesic effect It is thought that this family of drugs has a degree of analgesic action though this is in comparison to the sedative effect minor Its effects can be reversed using atipamezole distributed as Antisedan by Pfizer IV use of atipamezole is not licensed IM is the preferred route Yohimbine may also be used in an emergency situation but is not licensed Use in marine paint editMedetomidine can be used as an antifouling substance in marine paint It is mainly effective against barnacles but has also shown effect on other hard fouling like tube worms When the barnacle cyprid larva encounters a surface containing medetomidine the molecule interacts with the octopamine receptor in the larva This causes the settling larva to increase its kicking to more than 100 kicks per minute 4 which makes becoming sessile nearly impossible When the larva swims away from the surface the effect disappears reversible effect The larva regains its pre exposure function and can settle somewhere else References editThis article includes a list of general references but it lacks sufficient corresponding inline citations Please help to improve this article by introducing more precise citations January 2016 Learn how and when to remove this template message Sinclair MD November 2003 A review of the physiological effects of alpha2 agonists related to the clinical use of medetomidine in small animal practice The Canadian Veterinary Journal 44 11 885 97 PMC 385445 PMID 14664351 Achievements Orion Corporation Archived from the original on March 15 2013 Chaabane P The Selektope Story PDF PCI Magazine Retrieved 12 December 2018 Lind U Alm Rosenblad M Hasselberg Frank L Falkbring S Brive L Laurila JM et al August 2010 Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2 adrenoceptor agonist medetomidine Molecular Pharmacology 78 2 237 48 doi 10 1124 mol 110 063594 PMID 20488921 S2CID 17792301 Further reading edit Domitor Novartis Animal Health Canada 2003 Archived from the original on 2007 09 24 Harari J 1996 Small Animal Surgery Williams and Wilkins ISBN 978 0 683 03910 8 Lind U Alm Rosenblad M Hasselberg Frank L Falkbring S Brive L Laurila JM et al August 2010 Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2 adrenoceptor agonist medetomidine Molecular Pharmacology 78 2 237 48 doi 10 1124 mol 110 063594 PMID 20488921 S2CID 17792301 Dahlstrom M Martensson LG Jonsson PR Arnebrant T Elwing H November 2000 Surface active adrenoceptor compounds prevent the settlement of cyprid larvae of Balanus improvisus Biofouling 16 2 4 191 203 doi 10 1080 08927010009378444 S2CID 85603381 Retrieved from https en wikipedia org w index php title Medetomidine amp oldid 1116655672, wikipedia, wiki, book, books, library,
