Artesunate
Artemisinin derivatives are the potent and rapidly acting blood schizonticides. These are concentrated in parasitised erythrocytes. Artesunate acts rapidly, stopping parasite development and preventing subsequent cytoadherence and rosetting. Artesunate is well distributed and achieves high concentration in the intestines, liver and kidneys. Only a small amount of artesunate is excreted in the urine and in the stools.Severe malaria including cerebral malaria and as a second line treatment in chloroquine-resistant falciparum malaria.
Adults: Parenteral : 120mg on the first day followed by 60mg daily for the next four days. In severe cases : Extra dose of 60mg can be given on the first day itself 6 hours after the first dose. Oral: 100mg twice a day on the first day followed by 50mg twice daily for the next four days. children : 1.2mg/kg x 5 days (maximum 60mg)
Not known
Avoid in pregnant women, especially in the first trimester. Paediatrics: May be used if chloroquine resistant. Pregnancy: Contraindicated in 1st trimester. Lactation: Safety not established.
Transient and reversible reticulocytopenia, drug fever, drug rash, bradycardia, transient first degree heart block and transient & reversible elevation of serum transaminases.
Antimalarial action potentiated by oxidant drugs. Additive effect seen with chloroquine. Antagonistic effect seen with pyrimethamine and sulfonamides. Others: mefloquine, primaquine, tetracycline.
