Table 1.
Overview of antileishmanial drugs systemically administered in treatment of visceral and/or cutaneous leishmaniasis (only includes information in human subjects, unless indicated otherwise)
| Antileishmanial drug | Formulations | Route of administration | Distribution | Metabolism | Excretion | |
|---|---|---|---|---|---|---|
| Highest accumulation | Skin | |||||
| Pentavalent antimonials | Sodium stibugluconate (SSG) Meglumine Antimoniate (MA) |
IM/IV | Liver, thyroid, heart | Confirmed | Intracellular reduction to SbIII | Renal clearance |
| Paromomycin | Paromomycin sulphate | IM | Not reported | Not reported | Not metabolized | Renal clearance |
| Pentamidine | Pentamidine dimesylate Pentamidine isethionate |
IM/IV | Kidney, liver, spleen, adrenal glands | Not reported | CYP1A1 (CYP2D6, CYP3A5 and CYP4A11) | Not excreted unchanged |
| Miltefosine | Miltefosine | Oral | Not reported (rats/mice: kidney, liver, spleen, intestines, adrenal) | Not reported (in rats: confirmed) | Intracellularly by phospholipase D | Not excreted unchanged (metabolised to endogenous compounds) |
| Amphotericin Ba | D-AMB L-AMB |
IV | Liver, spleen | Not reported (in rats: confirmed) | Metabolism not well-studied. Liposomes engulfed by RES | D-AMB: urinary excretion (21%); faecal excretion (43%) L-AMB: urinary excretion (5%); faecal excretion (4%) |
CYP cytochrome P450, D-AMB amphotericin B deoxylate, IM intramuscular, IV intravenous, L-AMB liposomal amphotericin B, RES Reticuloendothelial system
aMore lipid formulations exist of amphotericin B, but these are outside the scope of this review