ARTEMETHER 80 MG & LUMEFANTRINE 480 MG
Artemether is a semi synthetic derivative of artemisinin. It is active against all of the erythrocytic stages of parasites, including transmissible gametocytes, resulting in a rapid clinical benefit and decreased transmission of malaria. The Endoperoxide Bridge in artesunate molecule appears to interact with heme in the parasite and inhibits protein synthesis of parasite which results in lysis of the parasite.
- Absorption: – Artemether is absorbed with peak plasma concentrations reached about 2 hours after dosing. Absorption of lumefantrine, a highly lipophilic compound, starts after a lag-time of up to 2 hours, with peak plasma concentrations about 6 to 8 hours after administration.
- Distribution: – Artemether and lumefantrine are both highly bound to human serum proteins in vitro (95.4% and 99.7%, respectively). Dihydroartemisinin is also bound to human serum proteins (47% to 76%).
- Protein Binding: – The protein binding to human plasma proteins is linear.
- Metabolism: – The metabolism of artemether was catalyzed predominantly by CYP3A4/5. Dihydroartemisinin (DHA) is an active metabolite of artemether. The metabolism of artemether was also catalyzed to a lesser extent by CYP2B6, CYP2C9 and CYP2C19.In human liver microsomes and in recombinant CYP450 enzymes, lumefantrine was metabolized mainly by CYP3A4 to desbutyl-lumefantrine. The systemic exposure to the metabolite desbutyl-lumefantrine was less than 1% of the exposure to the parent compound.
- Elimination: – Artemether and DHA are cleared from plasma with an elimination half-life of about 2 hours. Lumefantrine is eliminated more slowly, with an elimination half-life of 3-6 days.
- It is indicated in treatment of uncomplicated falciparum malaria that is resistant to other antimalarials.