Artesunate is a potent, water-soluble, semi-synthetic derivative of artemisinin, a sesquiterpene lactone endoperoxide extracted from the plant Artemisia annua. It is a first-line antimalarial agent for the treatment of severe and complicated Plasmodium falciparum malaria, as per WHO and National Center for Vector Borne Diseases Control (NCVBDC), India guidelines. It acts rapidly to reduce parasite biomass and is the drug of choice for initial parenteral therapy in severe malaria, often followed by a full course of an appropriate oral ACT (Artemisinin-based Combination Therapy).
Adult: Severe Malaria (IV/IM): 2.4 mg/kg body weight at 0, 12, and 24 hours, then once daily until oral therapy can be started (usually for a minimum of 3 doses). Uncomplicated Malaria (Oral ACT): As part of a fixed-dose combination. Common Indian ACT is Artesunate (100mg) + Sulfadoxine (500mg) + Pyrimethamine (25mg) as a single daily dose for 3 days. The 60mg strength is often used for pediatric dosing or in specific combinations.
Note: IV Injection: Reconstitute powder with 1 mL of 5% Sodium Bicarbonate solution provided. Shake gently for 2-3 minutes until clear. Then dilute to 5 mL with 5% Dextrose or Normal Saline. Administer by slow IV bolus over 3-5 minutes. IM Injection: Reconstitute as above and administer deep intramuscularly into the anterior thigh. Oral: Should be taken with food to enhance absorption and reduce GI upset. Always complete the full 3-day course of ACT.
Artesunate's antimalarial activity is attributed to its endoperoxide bridge. Inside the infected erythrocyte, the iron-rich environment (heme from hemoglobin digestion) catalyzes the cleavage of this endoperoxide bridge. This reaction generates highly reactive carbon-centered free radicals and reactive oxygen species (ROS). These reactive intermediates alkylate and oxidize vital parasite proteins (including PfATP6, a sarcoplasmic-endoplasmic reticulum calcium ATPase or SERCA), damage parasite membranes, and cause widespread macromolecular damage, leading to rapid parasite death.
Pregnancy: First Trimester: Contraindicated unless in life-threatening severe malaria where benefits outweigh risks. Second & Third Trimester: Recommended treatment for severe and uncomplicated falciparum malaria. Considered safe and effective.
Driving: Dizziness may occur; patients should be cautioned about driving or operating machinery if they experience such effects.
| Strong CYP2A6 Inducers (e.g., Rifampicin) | May increase metabolism of DHA, potentially reducing its plasma concentration and efficacy. | Moderate |
| Antiretroviral Protease Inhibitors (e.g., Lopinavir/Ritonavir) | May increase artesunate/DHA levels; clinical significance unknown. | Moderate |
| Other QT-prolonging drugs (e.g., Antiarrhythmics, Fluoroquinolones) | Theoretical additive risk of QTc prolongation. | Mild |
| Chloroquine | Antagonistic interaction reported in vitro; not recommended for combination. | Major |
Same composition (Artesunate (60mg)), different brands: