Artesunate is used primarily as treatment for malaria; it has also been shown to be >90% efficacious at reducing egg production in Schistosoma haematobium infection According to WHO intravenous AS is the drug of choice for severe malaria both in children and adults where there is low transmission.In regions where transmission is high, randomized trials among Asian adults and African children strongly advocates the use of artesunate over quinine as the treatment of choice for falciparum malaria. Artesunate is prepared from dihydroartemisinin (DHA) by reacting it with succinic acid anhydride in basic medium. Pyridine as base/solvent, sodium bicarbonate in chloroform and catalyst DMAP (N,N-dimethylaminopyridine) and triethylamine in 1,2-dichloroethane have been used, with yields of up to 100%. A large scale process involves treatment of DHA in dichloromethane with a mixture of pyridine, a catalytic amount of DMAP and succinic anhydride. The dichloromethane mixture is stirred for 6–9 h to get artesunate in quantitative yield. The product is further re-crystallized from dichloromethane. alpha-Artesunate is exclusively formed (m.p 135–137C).
1.Artemisinin 99% has effect on antibacterial, artemisinin has anti-influenza virus effect.
2.Artemisinin 99% is used for anti-parasite, artemisinin play the role of anti-schistosomiasis and leptospirosis.
3.Artemisinin 99% can be used for antimalarial, artemisinin has killing effect on the parasite within red blood cells, it can inhibit the parasite's maturity quickly.
Application
1.Artesunate is an antimalarial agent. It is a water-soluble hemisuccinate derivative of dihydroartemisinin.
2.Artemisinin is a sesquiterpene lactone isolated from Artemisia annua, a herb that has traditionally been used in China for the treatment of malaria.
3.Artesunate and its active metabolite dihydroartemisinin are potent blood schizonticides, active against the ring stage of the parasite.
4.Artesunate is ideal for the treatment of severe malaria, including cerebral malaria. It is also active against chloroquine and mefloquine resistant strains of P. falciparum.
5.Artesunate is unstable in neutral solution and is therefore only available for injections as artesunic acid.
