Plasma and cerebrospinal fluid concentrations of paracetamol after a single intravenous dose of propacetamol

Since the antipyretic and probably the analgesic effects of paracetamol are, at least in part, centrally mediated, its plasma and cerebrospinal fluid (CSF) concentrations were measured in 43 patients with nerve‐root compression pain. Each subject was given a short i.v. infusion of 2 g propacetamol, a prodrug which is hydrolysed to paracetamol within 7 min. Single blood and CSF samples were drawn concomitantly in each patient at intervals between 20 min and 12 h. Maximum CSF drug concentrations were observed at the 4th hour, subsequent concentrations exceeding those in plasma. The elimination half‐life of paracetamol calculated from pooled data was shorter in plasma (2.4 h) than in CSF (3.2 h). The time‐course of paracetamol in CSF may parallel that of analgesic effect.