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    Overview

    Artemether is an antimalarial agent used to treat acute uncomplicated malaria. Artemether is an artemisinin derivative, in which the lactone has been converted to the corresponding lactol methyl ether. Artemether is chemically described as (3R,5aS,6R,8aS,9R,10S,12R,12aR)-10-methoxy-3,6,9-trimethyldecahydro-3,12-epoxypyrano [4,3-j]-1,2-benzodioxepine. Its molecular formula is C16H26O5, which corresponds to a molecular weight of 298.37.

    Artemether appears as white crystals or a white, crystalline powder that is practically insoluble in Water, very soluble in Dichloromethane and Acetone, freely soluble in Ethyl acetate and dehydrated Ethanol. Its melting range is 86 to 90°C.

    Clinical Applications

    For uncomplicated malaria caused by P. falciparum (and chloroquine-resistant P. falciparum) or chloroquine-resistant P. vivax parasites.
    Artemether can also be used to treat severe malaria.
    For enhanced efficacy, it is given in combination with lumefantrine. This combination therapy exerts its effects against Plasmodium spp. erythrocytic stages.

    Mode of Administration

    Artemether is given by injection in a muscle. It is also available by mouth in combination with lumefantrine.

    Pharmacological Effects

    Artemether interacts with ferriprotoporphyrin IX (heme) or ferrous ions in the acidic parasite food vacuole and generates cytotoxic radical species. The accepted mode of action of the peroxide-containing drug involves its interaction with heme (byproduct of haemoglobin degradation), derived from proteolysis of haemoglobin. This interaction results in the formation of toxic oxygen and carbon-centred radicals.

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