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Pharmacological particulars
Pharmacotherapeutic group: α2-receptor antagonist (Antidote)
ATCvet code: QV03AB90
Pharmacodynamic properties
Atipamezole is a potent and selective α2-receptor blocking agent (α2-antagonist), which promotes the release of the neurotransmitter noradrenaline in the central as well as in the peripheral nervous systems. This leads to activation of the central nervous system due to sympathetic activation. Other pharmacodynamic effects such as impact on the cardiovascular system, are mild, although a transient decrease in blood pressure may occur within the first 10 minutes following administration of atipamezole hydrochloride. As an α2-antagonist, atipamezole is capable of eliminating (or inhibiting) the effects of the α2-receptor agonist, medetomidine or dexmedetomidine. Thus atipamezole reverses the sedative effects of (dex)medetomidine hydrochloride in cats and dogs to normal and may lead to a transient increase in heart rate.
Pharmacokinetic properties
Atipamezole hydrochloride is rapidly absorbed after intramuscular injection. The maximal concentration in the central nervous system is reached in 10-15 minutes. Volume of distribution (Vd) is about 1-2.5 l/kg. The half-life (t1/2) of atipamezole hydrochloride is reported to be approximately 1 hour. Atipamezole hydrochloride is rapidly and completely metabolised. The metabolites are mainly excreted in urine with a small amount excreted in faeces.