European Journal of Biomedical and Pharmaceutical Sciences

REVIEW ON ARAKODA (TAFENOQUINE) & ITS APPROACH AS AN ANTI-MALARIAL AGENT

*Mohsina Abid and Syeda Sana

ABSTRACT

Tafenoquine is an analogue of primaquine with an improved therapeutic and safety profile. It has a long half-life and activity against liver-stage malaria parasites, so may be useful for chemoprophylaxis. Antimalarial agents are drugs used for the treatment or prophylaxis of malaria. Malaria is caused by four species of Plasmodium, such as Plasmodium falciparum, P. malariae, P. ovale, and P. vivax. ARAKODA contains tafenoquine succinate, an antimalarial agent for oral administration. The molecular formula of tafenoquine succinate is C24H28F3N3O3∙C4H6O4 and its molecular weight is 581.6 as the succinate salt. It is given in prophylaxis of malaria patient aged 18 years older. Tafenoquine is active against pre-erythrocytic (liver) and erythrocytic (asexual) forms as well as gametocytes of Plasmodium species. G6PD test is performed before giving the drug. Analytical studies were on NMR,IR,MS,HPLC, Flourimetry analysis. In vitro studies have shown that tafenoquine presents an average 50% inhibitory concentration of 0.436 mcg against blood stages of seven strains of P. falciparum. The long‐acting 8‐aminoquinoline tafenoquine (TQ) coadministered with chloroquine (CQ) may radically cure Plasmodium vivax malaria. Coadministration therapy was evaluated for a pharmacokinetic interaction and for pharmacodynamic, safety and tolerability characteristics. Volume of distribution. The activation of tafenoquine needs the activity of CYP 2D6 liver microsomal enzyme. Routes of elimination is through feces.

Keywords: TQ,PQ, plasmodium vivax, p.falciparum, tafenoquine, G6PD, Arakoda, 5,6 ortho-qunine, CYP 2D6, Mefloquine.