Table 3.
Drugs for the treatment of animal trypanosomiasis.
Drug class | Drug | Molecular targets | Disease form | Drug form | Route of administration | Major limitations and side effects | References |
---|---|---|---|---|---|---|---|
Phenanthridine | Homidium, isometamidium | Inhibits topoisomerase-II during DNA biosynthesis | Prophylaxis and treatment of T. evansi, T. vivax, T. congolense, and T. vivax; widely used in the treatment of animal trypanosomiasis | Powder for reconstitution | IM route | Highly toxic, drug resistance, highly polar, and these drugs are available in powder form for parenteral use during treatment of the early stage of disease | (119–121) |
Aminoquinaldine | Quinapyramine | Trypanostatic, inhibits kinetoplastic DNA biosynthesis, loss of ribosomal function | Effective against T. congolense, T. vivax, T. brucei, and T. evansi | Powder for reconstitution | IM or IV route | Serious local reactions at site of injection, drug resistance | (122–124) |
Diamidine | Diminazene | Inhibition of the kinetoplasmatic DNA biosynthesis | Treatment of T. evansi; widely used to treat animal African trypanosomiasis; most used drug for early animal African trypanosomiasis (AAT) | Powder for reconstitution | IM or IV route | Highly polar, poor permeation, poor brain permeation due to its cationic polar nature, although it is well tolerated, it requires repeated administration, leading to poor patient compliance | (125–128) |
Melaminophenyl arsenical | Melarsomine | Inhibition of trypanothine reductase | T. evansi infection | Powder for reconstitution | Administered by IV or IM route | Rapidly metabolized in the plasma | (129–132) |