Adult: As initial treatment in severe cases: 2.4 mg/kg via IM inj or slow IV bolus over 1-2 minutes; repeat dose after 12 and 24 hours, then once daily thereafter. Transfer the patient to an appropriate full course oral regimen after at least 24 hours of parenteral therapy and once oral medication is tolerated. Dosage recommendations may vary between countries. Refer to local treatment guidelines. Child: Same as adult dose.
Oral Uncomplicated falciparum malaria
Adult: In combination with other antimalarial agents (mefloquine, amodiaquine, or sulfadoxine-pyrimethamine): 200 mg once daily for 3 days. Dosage or treatment recommendations may vary between countries. Refer to local treatment guidelines.
Reconstitution
Reconstitute the vial with the appropriate diluent or solvent provided. Refer to detailed product guidelines for specific instructions on reconstitution.
Special Precautions
Patient with cardiac or gastrointestinal disease. Not indicated to treat hypnozoite liver stage forms of Plasmodium. Renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. anaphylaxis, urticaria, rash, pruritus), post-treatment delayed haemolysis or haemolytic anaemia, reversible reticulocytopenia. Blood and lymphatic system disorders: Anaemia. Cardiac disorders: Bradycardia. Gastrointestinal disorders: Diarrhoea, vomiting, abdominal pain, dysgeusia. General disorders and administration site conditions: Pyrexia. Hepatobiliary disorders: Jaundice. Investigations: Increased ALT and AST. Nervous system disorders: Dizziness, headache. Renal and urinary disorders: Haemoglobinuria, acute renal failure. Respiratory, thoracic and mediastinal disorders: Rhinitis, cough. Vascular disorders: Hypotension, phlebitis.
Monitoring Parameters
Monitor Hb, reticulocyte count, haptoglobin, LDH, and total bilirubin once weekly for up to 4 weeks after initiation of treatment. Assess for signs or symptoms of hypersensitivity.
Drug Interactions
Strong UGT inhibitors (e.g. axitinib, imatinib, diclofenac, vandetanib) may increase the plasma concentration of dihydroartemisinin (DHA), the active metabolite of artesunate. Nevirapine, ritonavir, or strong UGT inducers (e.g. carbamazepine, phenytoin, rifampicin) may decrease the plasma concentration of DHA, resulting in reduced or loss of efficacy.
Action
Description: Mechanism of Action: Artesunate is a semisynthetic artemisinin derivative and a prodrug that is metabolised to the active metabolite, DHA. Both artesunate and DHA contain an endoperoxide bridge that is activated by haeme iron ring binding, leading to oxidative stress, protein and nucleic acid synthesis inhibition, ultrastructural changes and reduced parasite growth and survival. They are active against the blood-stage asexual parasites and gametocytes of Plasmodium species, including chloroquine-resistant strains but inactive against the hypnozoite liver stage forms of Plasmodium vivax and Plasmodium ovale. Pharmacokinetics: Absorption: Time to peak plasma concentration: <1 hour (artesunate); within 15 minutes (DHA). Distribution: Enters breast milk (DHA). Volume of distribution: 68.5 L (artesunate); 59.7 L (DHA). Plasma protein-binding: Approx 93%. Metabolism: Rapidly hydrolysed by blood esterases into DHA, which undergoes glucuronidation. Excretion: Via urine. Elimination half-life: 0.3 hours (artesunate); 1.3 hours (DHA).
Chemical Structure
Artesunate Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6917864, Artesunic acid. https://pubchem.ncbi.nlm.nih.gov/compound/Artesunic-acid. Accessed Nov. 23, 2022.
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