Chemically, artemisinin is a sesquiterpene lactone containing an unusual peroxide bridge. This peroxide is believed to be responsible for the drug's mechanism of action. Few other natural compounds with such a peroxide bridge are known.
Artemisinin and its endoperoxide derivatives have been used for the treatment of P. falciparum related infections but low bioavailability, poor pharmacokinetic properties and high cost of the drugs are a major drawback of their use. Use of the drug by itself as a monotherapy is explicitly discouraged by the World Health Organization, as there have been signs that malarial parasites are developing resistance to the drug. Therapies that combine artemisinin or its derivatives with some other antimalarial drug are the preferred treatment for malaria and are both effective and well tolerated in patients.
The drug is also increasingly being used in Plasmodium vivax malaria.
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