Coartem® /Riamet®
Coartem®
Coartem® is a safe and effective combination therapy that provides an important addition to the armamentarium against malaria. To date, it is the only fixed-dose artemisinin-based combination therapy (ACT) combining artemether, an artemisinin derivative, and lumefantrine, a synthetic antimalarial drug. Artemisinin is a compound derived from the sweet wormwood plant and has been used for centuries in traditional Chinese medicine to treat fever.
Structures of lumefantrine and artemether
Coartem® - overview of product characteristics
Coartem® : is highly effective against acute, uncomplicated malaria caused by P. falciparum in areas of multi-drug resistance; eliminates parasites and symptoms significantly faster than most current antimalarials;1, 2 is rapidly gametocytocidal, helping to reduce transmission; achieves high cure rates; is well tolerated, particularly when compared to most established antimalarials;3 is an easy-to-use fixed-dose combination treatment: simplifies compliance - tested by GCP (Good Clinical Practice) standards.
Mode of action of Coartemether
Artemether and lumefantrine work at different points in the Plasmodium life cycle, making emergence of resistance unlikely. Parasites in the infected erythrocytes ingest and degrade haemoglobin and concentrate the iron in a food vacuole in the form of toxic haem A. Normally, the haem is then made harmless by conversion into haemozoin B.
Artemether is concentrated in the food vacuole. It then splits its endoperoxide bridge as it interacts with haem, blocking conversion to haemozoin, C destroying existing haemozoin and releasing haem D and a cluster of free radicals into the parasite E.
Lumefantrine F also targets haem, preventing its detoxification G. Toxic haem and free radicals are jointly responsible for the death of the parasite H.
Artemether provides rapid onset of action to kill the parasite; lumefantrine has a slower onset but long-acting activity preventing reappearance or recrudescence.
