Transfer of pethidine to CSF following intravenous administration

To help delineate the contributions to analgesia evoked by central and spinal opiate receptors, pethidine was administered intravenously to dogs by bolus followed by infusion. Plasma and cerebrospinal fluid were sampled and assayed for pethidine. Cerebrospinal fluid concentrations followed a similar time course to plasma but with lower concentrations. The average cerebrospinal fluid:plasma ratio was 0.4 and resembled the fraction of unbound pethidine in plasma. It was concluded that cerebrospinal fluid concentrations after intravenous administration were so low that spinal action would be unlikely.