metadata toggle
Pharmacological particulars
Pharmacotherapeutic group: Other analgesics and antipyretics. ATCvet code: QN02BE01
Pharmacodynamic properties
Paracetamol or acetaminophen or N-acetyl-p-aminophenol is a paraminophenol derivative with analgesic and antipyretic properties.
Pharmacokinetic particulars
Absorption
Paracetamol is rapidly and almost completely absorbed after oral administration (bioavailability of about 90% after administration in the drinking water). Peak concentrations are reached in a little less than 2 hours after ingestion.
Metabolism
Paracetamol is mainly metabolised in the liver. The two major metabolic pathways are conjugation to glucuronate and conjugation to sulphate. The latter route is rapidly saturable at dosages higher than therapeutic doses. A minor pathway, catalysed by cytochrome P450 (CYP), leads to the formation of the intermediary reagent, N-acetyl-benzoquinoneimine which, under normal conditions of use, is rapidly detoxified by reduced glutathione and removed in urine after conjugation with cystein and mercapturic acid. On the contrary, after massive intoxication, the quantity of this toxic metabolite is increased.
Elimination
Paracetamol is mainly eliminated in the urine. In the pig, 63% of the ingested dose is eliminated by the kidneys in 24 hours mainly conjugated to glucuronate and suphate. Less than 5% is eliminated in unchanged form. The elimination half-life is approximately 5 hours.