Medetomidine

Structural formula
	( R ) -isomer (top) and ( S ) -isomer (bottom)
General
Non-proprietary name	Medetomidine
other names	( RS ) -4- [1- (2,3-Dimethylphenyl) ethyl] -1 H -imidazole
Molecular formula	C 13 H 16 N 2
External identifiers / databases
EC number	811-718-6
ECHA InfoCard	100.242.450
PubChem	68602
ChemSpider	61868
Wikidata	Q427179
Drug information
ATC code	Q N05CM91
Drug class	sedative
Mechanism of action	α 2 adrenoreceptor agonist
properties
Molar mass	200.28 g · mol -1
Physical state	firmly
Melting point	172–173 ° C (medetomidine hydrochloride)
solubility	little in water
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
H and P phrases	H: 300-330-336-370-372-410
	P: ?
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Medetomidine is a chemical compound from the imidazole group that is used in animal and human medicine as a sedative and pain reliever . The pharmacologically active enantiomer in the racemate [1: 1 mixture of the ( R ) form and the ( S ) form] is the ( R ) - (+) - form. The racemate is mainly used as a water-soluble, white, crystalline medetomidine hydrochloride.

effect

In addition to its sedative properties, medetomidine has a pain-relieving ( analgesic ), anxiolytic and muscle-relaxing effect . The active ingredient shows analgesic effects in 41–44% of patients and, when given together with another pain reliever, also reduces the necessary dose.

Medetomidine binds to α ₂ -adrenoceptors and thus reduces the release and turnover of norepinephrine . Compared to the related xylazine , the α2 specificity is about 10 times higher. The active isomer here is dexmedetomidine , while the mirror isomer levomedetomidine has no influence on the α ₂ -adrenoceptors. As a side effect, the active ingredient reduces the heart's capacity : bradycardia and, under certain circumstances, an irregular heartbeat occur . A antagonism with atipamezole possible. In very high (but not common in veterinary medicine) doses, medetomidine also acts on the α1-adrenoceptors , whereby the sedation is abolished.

application

Medetomidine can be used intravenously or intramuscularly in all small domestic and pet animals. It can also be used on reptiles and birds. Use on animals that provide food is not permitted. The half-life in the blood is about an hour. The breakdown takes place in the liver , the excretion via the kidneys .

Medetomidine is mainly used to calm down (sedation and analgesia) and to induce anesthesia . In combination with ketamine , propofol or midazolam and fentanyl , it can also be used to carry out smaller, not very painful operations. It can also be used for immobilization in zoo and wild animals.

In cardiac , sugar and kidney disease and pregnant animals should not be used medetomidine.

Medetomidine is being investigated for its usefulness as an active ingredient in underwater paints .

Trade names

Cepetor KH, Domitor, Dorbene, Dormilan, Medeson, Sedator, Sededorm, Sedin, Selektope

Web links

Entry on medetomidine at Vetpharm, accessed on November 21, 2011.

Individual evidence

↑ ^a ^b ^c F. v. Bruchhausen, S. Ebel, E. Hackenthal, U. Holzgrabe: Hagers Handbook of Pharmaceutical Practice: Volume 4: Substances AK. 5th edition, Springer 1999, ISBN 978-3-540-62644-2 , pp. 325-326.
↑ Entry on (RS) -4- [1- (2,3-Dimethylphenyl) ethyl] -1H-imidazole in the GESTIS substance database of the IFA , accessed on December 30, 2019(JavaScript required) .
↑ Entry on (RS) -4- [1- (2,3-dimethylphenyl) ethyl] -1H-imidazole in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on December 30, 2019. Manufacturers or distributors can use the expand harmonized classification and labeling .
↑ H. Buschmann, G. Bahrenberg, T. Christoph, E. Friderichs: Analgesics: from chemistry and pharmacology to clinical application. Wiley-VCH, Weinheim 2002, ISBN 978-3-527-30403-5 , p. 276.
↑ adrenoceptor and Other Pharmacoactive compounds as antifoulants Putative doi : 10.1007 / 3-540-30016-3_7 .

[hager-1] F. v. Bruchhausen, S. Ebel, E. Hackenthal, U. Holzgrabe: Hagers Handbook of Pharmaceutical Practice: Volume 4: Substances AK. 5th edition, Springer 1999, ISBN 978-3-540-62644-2 , pp. 325-326.

[GESTIS-2] Entry on (RS) -4- [1- (2,3-Dimethylphenyl) ethyl] -1H-imidazole in the GESTIS substance database of the IFA , accessed on December 30, 2019(JavaScript required) .

[CLP_100.242.450-3] Entry on (RS) -4- [1- (2,3-dimethylphenyl) ethyl] -1H-imidazole in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on December 30, 2019. Manufacturers or distributors can use the expand harmonized classification and labeling .

[4] H. Buschmann, G. Bahrenberg, T. Christoph, E. Friderichs: Analgesics: from chemistry and pharmacology to clinical application. Wiley-VCH, Weinheim 2002, ISBN 978-3-527-30403-5 , p. 276.

[5] renoceptor and Other Pharmacoactive compounds as antifoulants Putative doi : 10.1007 / 3-540-30016-3_7 .