Adult: Initial treatment in severe cases: 2.4 mg/kg via slow IV bolus over 1-2 minutes or deep IM inj. Repeat after 12 hours and 24 hours then once daily thereafter. Transfer patient to an appropriate full course oral regimen after at least 24 hours of parenteral therapy and once oral medications are tolerated. Concomitant therapy with another antimalarial agent active against Plasmodium liver hypnozoites may be necessary for severe cases due to P. vivax or P. ovale. Consider local guidelines for the appropriate treatment regimen. Child: ≥20 kg: Same as adult dose.
Reconstitution
Reconstitute vial labelled as 60 mg of artesunate with the supplied diluent. IV: Add 5 mL of 5% glucose or 0.9% NaCl inj to reconstituted solution to obtain 6 mL of artesunate solution with a concentration of 10 mg/mL. IM: Add 2 mL of 5% glucose or 0.9% NaCl inj to reconstituted solution to obtain 3 mL of artesunate solution with a concentration of 20 mg/mL. Administer within 1.5 hours after reconstitution.
Contraindications
Hypersensitivity to artesunate.
Special Precautions
Patient with cardiac and gastrointestinal disease. Hepatic and renal impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Haemolysis, severe haemolytic anaemia, hypersensitivity (including anaphylaxis). Ear and labyrinth disorders: Tinnitus. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, taste alteration (metallic/bitter taste). General disorders and administration site conditions: Asthenia, pancreatitis, fever, fatigue, malaise, inj site pain. Hepatobiliary disorders: Jaundice. Musculoskeletal and connective tissue disorders: Muscle pain, arthralgia. Nervous system disorders: Ataxia, balance impairment, restlessness, tremor, dizziness, headache, paresis. Psychiatric disorders: Confusion. Renal and urinary disorders: Haemoglobinuria, acute renal failure. Respiratory, thoracic and mediastinal disorders: Cough, nasal symptoms. Skin and subcutaneous tissue disorders: Pruritus, rash.
Monitoring Parameters
Monitor for signs and symptoms of hypersensitivity and cardiotoxicity (high doses); Hb, reticulocyte count, haptoglobin, lactate dehydrogenase and total bilirubin once weekly for up to 4 weeks after treatment initiation. Monitor for evidence of haemolytic anaemia for 4 weeks after therapy. Consider performing direct antiglobulin test to determine if therapy for immune-mediated haemolysis is needed.
Drug Interactions
May decrease dihydroartemisinin (DHA) plasma concentration thus reduce efficacy of artesunate with ritonavir, nevirapine or UDP-glucuronosyltransferase (UGT) inducers (e.g. rifampicin, carbamazepine, phenytoin). May increase DHA plasma concentration thereby increase the risk of side effects with UGT inhibitors (e.g. axitinib, vandetanib, imatinib, diclofenac).
Action
Description: Artesunate is a semisynthetic artemisinin derivative and a prodrug that is metabolised to the active metabolite dihydroartemisinin (DHA). Artesunate and DHA contain endoperoxide bridge that is activated by a heme iron ring binding leading to oxidative stress, protein and nucleic acid synthesis inhibition, ultrastructural changes and decrease in 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 P. vivax and P. ovale. Pharmacokinetics: Absorption: Rapidly absorbed (IM). Time to peak plasma concentration: Within 15 minutes (DHA). Distribution: Enters the breast milk (DHA). Volume of distribution: 68.5 L (artesunate); 59.7 L (DHA). Plasma protein binding: Approx 93%. Metabolism: Rapidly hydrolysed by plasma esterases to DHA (active metabolite) which undergoes glucuronidation to form α-DHA-β-glucuronide metabolite. 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, Artesunate. https://pubchem.ncbi.nlm.nih.gov/compound/Artesunic-acid. Accessed Aug. 24, 2020.
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