Mepacrine can be used as an anti-malarial drug, an antibiotic and as a treatment for some types of systemic lupus, as well as giardasis.

The exact anti parasitic mechanism of action is unknown, but mepacrine is thought to interfere with the outer membranes of Protozoa.

Research is currently being undergone to ascertain whether Mepacrine would be a suitable treatment for persons affected with Creutzfeldt Jakob Disease (mad cow disease).