Toxicology and pharmacokinetics of piperaquine in mice

Abstract

Pharmacokinetic and toxicological data for piperaquine (PQ) - a bisquinoline antimalarial drug - are limited, despite strong evidence of clinical efficacy. Our aim was to conduct a detailed toxicological investigation of PQ in Swiss mice. The study comprised three phases: (i) oral PQ phosphate (PQP) at doses ranging from 0 to 600 mg/(kg day) for 5 days. Pathology tests included haematological and biochemical indices, and histopathology of the liver, heart and kidneys. (ii) PQP doses of 0-300 mg/(kg day) for 12 days and pathology tests as described. (iii) Pharmacokinetic parameters determined from mice given 100 mg/(kg day) PQP for 5 days. Blood was harvested from mice over 56 days and plasma..