Pharmacotherapeutic group:sedative and analgesic
ATCvet code: QN05CM90
Pharmacodynamic properties
The active ingredient of the product is 4-(2,3-dimethylbenzyl)-imidazole-hydrochloride (INN: Detomidine). Detomidine leads to sedation of the treated animals and relieves pain. Duration and intensity of the effects are dose related. Mode of action of Detomidine is a pronounced stimulation of alpha-2 adrenoceptors. Its analgesic effects are due to an inhibition of transmission of the pain impulse within the CNS.
Detomidine also reveals its effects on peripheral alpha-receptors, therefore increase in blood glucose levels and at higher dosages piloerection, sweating and diuresis may occur. Following an initial increase in mean blood pressure, it will return to normal or slightly below normal, and heart frequency will decrease. The ECG shows an enlarged PR-interval, and in the horse mild atrio-ventricular blocks may be seen. The above mentioned changes are transient. A respiratory response includes an initial decrease of respiration rate and is increasing to normal or slightly increased values within a few minutes.
Pharmacokinetic particulars
Detomidine is absorbed rapidly after intramuscular injection. Tmax is 15 - 30 min. Bioavailability after intramuscular administration is 66-85%. After rapid distribution of detomidine into the tissues, it is metabolised nearly completely mainly in the liver, t½ is 1 to 2 hours. Metabolites are mainly excreted via urine and faeces.