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Pharmacological particulars
Pharmacotherapeutic group: Anesthetics, other general anaesthetics.
ATCvet code: QN01AX10.
Pharmacodynamic properties
Propofol is a short-acting, intravenous general anaesthetic, characterised by rapid onset, a short duration of anaesthesia and by rapid recovery. Propofol produces unconsciousness by depressing the central nervous system.
The depressant effects of propofol are primarily mediated through potentiation of postsynaptic GABAA receptors in the central nervous system. However, the glutaminergic and noradrenergic neurotransmitter systems are also thought to have a role in mediating the effects of propofol.
Pharmacokinetic particulars
Blood concentrations of propofol exhibit a tri-exponential decline in both dogs and cats. This is likely to reflect rapid distribution of propofol from the blood and brain to less well vascularised tissues, rapid metabolic clearance and slower redistribution from poorly vascularised tissues to blood. It is the first phase (t½, alpha approximately 10 min) that is clinically relevant, since animals awaken subsequent to the initial redistribution of propofol from the brain. The clearance of the drug is high in dogs but lower in cats, possibly due to inter-species differences in metabolism. In dogs, clearance is higher than hepatic blood flow, suggesting the presence of metabolic sites in addition to the liver. The volume of distribution is high in both dogs and cats. Propofol is highly bound to plasma protein (96-98%).
Clearance of the drug occurs through hepatic metabolism followed by renal elimination of the conjugated metabolites. A small amount is excreted in the faeces.