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Pharmacological particulars
Pharmacotherapeutic group: Hypnotics and sedatives.
ATCvet code: QN05CM90
Pharmacodynamic properties
Detomidine is an α2-adrenoceptor agonist. Detomidine is a sedative with analgesic properties (α2-adrenoceptor agonist). Detomidine causes sedation in animals and relieves pain. Duration and intensity of the effect is dependent from dose. The mode of action of detomidine is based on specific stimulation of central α2-adrenoceptors. The analgesic effect is based on inhibition of transfer of pain impulses in the CNS.
Because detomidine also acts on peripheral α-receptors, increase of blood glucose, and at higher doses pilo-erection, sweating and diuresis can occur. Following an initial decrease in blood pressure, it will return to normal or slightly below normal, and heart frequency will decrease. The ECG will show an enlarged PR interval and in horses a mild atrioventricular-block. These effects are transient. In most animals respiratory frequency decreases. Hyperventilation is rarely observed.
Pharmacokinetic properties
Detomidine is absorbed rapidly after intramuscular injection. Tmax is 15-30 minutes. Bioavailability after intramuscular administration is 66-85%. After rapid distribution of detomidine into the tissues, it is metabolised nearly completely mainly in the liver, t ½ is 1-2 hours. Metabolites are mainly excreted via urine and faeces.