THE EXCRETION OF PETHIDINE AND ITS DERIVATIVES

Abstract

The excretion of pethidine and its metabolite norpethidine is increased in acid urine and decreased in alkaline urine. Excretion of these two bases is the main route of removal of pethidine from the body if the urine is highly acid. If the urine is alkaline, excretion of the hydrolysis products meperidinic and normeperidinic acids, both as free acids and as conjugates, is the more important means of elimination of the drug. Acidification of the urine with ammonium chloride is indicated in the therapy of cases of pethidine poisoning in patients with reduced metabolic breakdown of the drug by the microsomal enzyme systems within liver cells. Reversed-phase chromatography of the dinitrophenyl derivative of norpethidine may prove to be of forensic importance in the diagnosis of pethidine poisoning or of pethidine addiction. Norpethidine can be detected in the urine by this method for at least 3 days after the last dose of pethidine. Analytical sensitivity is increased by acidification of the urine which produces a temporary rise of the excretion rate.