A Possible Mechanism of Prolonged Antimalarial Activity
Summary
An enzyme system in the supernatant fraction of rabbit liver homogenate for the metabolism of chloroquine is described. Various compounds, including SKF 525-A (β-diethylaminoethyl diphenylpropylacetate·HCI) and a number of antimalarial drugs, constitute effective inhibitors in vitro to the metabolic transformation of chloroquine.
Plasma levels of chloroquine can also be prolonged in experimental animals with some of these compounds. The most effective drugs tested include amodiaquin, pamaquine, hydroxychloroquine and primaquine.
Author Notes
Present address: Laboratory of Biochemical Pharmacology, Joseph E. Seagram & Sons, Inc., Cranbury, New Jersey.