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artesunate

P01BE03

Forms & Strengths

Powder for injection: 60 mg anhydrous artesunate with a separate ampoule of sodium bicarbonate 5% (reconstituted then diluted for IV or IM use)
Oral tablets: 50 mg

Adult Dosing

Severe malaria: 2.4 mg/kg IV or IM at 0, 12, and 24 hours, then once daily for a maximum of 7 days or until the patient can tolerate oral antimalarial therapy
Transition to a full course of oral combination therapy (ACT) once able to swallow, regardless of initial parasite burden

Pediatric Dosing

Severe malaria (weight < 20 kg): 3 mg/kg/dose IV or IM at 0, 12, and 24 hours, then once daily
Severe malaria (weight >= 20 kg): 2.4 mg/kg/dose IV or IM at 0, 12, and 24 hours, then once daily
Maximum duration: 7 days

Indications

Initial treatment of severe Plasmodium falciparum malaria
Preferred over quinine for severe malaria due to superior efficacy and rapid parasite clearance

Mechanism of Action

Water-soluble hemisuccinate derivative of dihydroartemisinin
Endoperoxide bridge interacts with intraparasitic heme/iron, generating reactive oxygen species and free radicals
Alkylation of parasite proteins and membranes leads to rapid death of asexual blood-stage malaria parasites

Contraindications

Known hypersensitivity to artesunate or other artemisinins
First trimester of pregnancy (preferred only if no other effective treatment is available)

Adverse Reactions

Post-artemisinin delayed hemolysis (can occur 1-3 weeks after treatment)
Transient reticulocytopenia and neutropenia
Elevated liver transaminases
Dizziness, headache, nausea, and vomiting
Hypersensitivity reactions including rash and anaphylaxis

Drug Interactions

Strong inducers or inhibitors of CYP2A6 and CYP2B6 may alter exposure to active metabolite dihydroartemisinin
Potential for additive QTc prolongation when co-administered with other QT-prolonging agents (though less than with quinidine/chloroquine)

Curated Content: Needs Vetting Before Put to Clinical Use