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Artemisinin, also called qinghaosu, antimalarial drug derived from the sweet wormwood plant, Artemisia annua. Artemisinin is a sesquiterpene lactone and is distilled from the dried leaves or flower clusters of A. annua.

Artemisinin may be administered orally, intramuscularly, or as a suppository. The drug reaches peak plasma levels within hours after administration and acts rapidly, significantly reducing malaria parasite burden in the first few days of treatment. Artesunate is unique among the artemisinin-derived agents because it can be administered intravenously, enabling the drug to take immediate effect.

Antimalarial

Artemisinin is effective against all the malaria-causing protozoal organisms in the genus Plasmodium. The drug is particularly useful in the treatment of infections involving chloroquine-resistant parasites and infections involving multidrug-resistant P. falciparum, which is the deadliest of the malaria protozoans. Artemisinin targets Plasmodium organisms in the schizont stage of development.

Stacking

Because artemisinin and its derivatives have a short duration of action and target malaria parasites in a specific stage of their life cycle, there is a high rate of disease relapse associated with the drugs when they are used alone in single-agent therapy. As a result, they are usually used in combination with other, longer-acting antimalarial drugs.

Examples of first-line artemisinin-based stack therapies used in the treatment of malaria include artesunate-mefloquine, artemether-lumefantrine, and artesunate-amodiaquine. Although these stack therapies also have proved valuable in preventing the emergence of artemisinin-resistant parasites, the persistent use of single-agent artemisinin therapy in some parts of the world has led to the development of resistant parasites and to high rates of treatment failure in these areas.

Side Effects

Artemisinin appears to have few side effects in humans. However, animal studies have shown that high doses can elicit symptoms of neurotoxicity, including respiratory depression and unsteady gait. These symptoms are associated with degeneration of the brainstem, though it remains unclear whether similar neurodegenerative effects occur at high doses in humans.