Description
Pharmacology
PROPERTIES:
LUMAPIL contains Artemether, a sesquiterpene lactone and the most active semi-synthetic derivative of the Artemisinines in a 1: 6 combination with Lumefantrine, a synthetic aryl-amino alcohol similar to Mefloquine and Halofantrine. This combination is a fixed-dose therapy that is effective and well-tolerated in malaria treatment and providing high cure rates even in areas of multi- drug resistance.
MODE OF ACTION:
Both components of LUMAPIL act as blood schizontocides and have their own site of action in the malarial parasite which is the food vacuole. They interfere with the conversion of haem, a toxic intermediate to haemozoin which is non-toxic.
Artemether interacts with haem, blocking its conversion to haemozoin while destroying existing haemozoin and releasing haem and a cluster of free radicals into the parasite.
Lumefantrine interferes with the haem polymerization process, a critical detoxifying pathway for the malaria parasite. Both components have a secondary action involving the inhibition of nucleic acid and protein synthesis within the malarial parasite.
LUMAPIL is active against the blood stages of P. vivax but not active against hypnozoites.
Therefore, an 8-amino¬quinoline derivative likes primaquine should be given sequentially after the combination in cases of mixed infections of P. falciparum and P. vivax to achieve hypnozoites eradication.
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