Due to very limited treatment options for leishmaniasis patients, optimisation of current drug dosages and drug combinations is of utmost importance, for which this review provides a solid pharmacokinetic basis.

This review describes the absorption, distribution, metabolism and excretion, as well as the clinical pharmacokinetics and potential drug–drug interactions of the antileishmanial drugs pentavalent antimonials, paromomycin, pentamidine, miltefosine and amphotericin B in the context of leishmaniasis.

The pharmacokinetics of two out of five antileishmanial drugs have never been evaluated in leishmaniasis patients. Exposure–response studies and pharmacokinetic data in special patient populations such as HIV co-infected patients are lacking. More research in this area will improve clinical outcomes via informed dosing regimens and combinations of drugs.