A Possible Mechanism of Prolonged Antimalarial Activity

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  • U. S. Department of Health, Education, and Welfare, Public Health Service, National Institutes of Health, National Institute of Allergy and Infectious Diseases, Laboratory of Parasite Chemotherapy, Bethesda, Maryland


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.