Distribution and urinary excretion of the desethylmetabolites of chloroquine in the rat

Abstract

The tissue distribution of desethylchloroquine and bisdesethylchloroquine has been studied in rats after single intraperitoneal administration of the drugs at a dose of 10 mg kg-1. Concentrations of the chloroquine metabolites in the liver, heart, lungs, kidney and spleen were 34 to 250 times higher than their plasma concentrations 24 h after the drugs had been injected. Urinary excretion of the drugs was studied in rats after single intravenous administration of 2.5, 5 or 10 mg kg-1 doses. The total estimated urinary excretion of desethylchloroquine and bisdesethylchloroquine was 25 and 64% respectively of the administered dose, with the maximum urinary excretion occurring on the first day. The results show that the desethylmetabolites of chloroquine are concentrated in the tissues in the same manner as the parent compound.