Artesunate

What it is and how it works

Artesunate is a water-soluble artemisinin derivative rapidly converted to dihydroartemisinin. Its endoperoxide bridge is activated by haem iron within the parasite, generating free radicals that damage parasite proteins and membranes, producing very rapid clearance of asexual blood-stage Plasmodium parasites.

Indications

Injection: first-line treatment of severe malaria in adults and children. Rectal: pre-referral treatment of suspected severe malaria in young children when injectable treatment is not available.

Dosage and administration (summary)

Injection: 2.4 mg/kg by intravenous (or intramuscular) injection at 0, 12 and 24 hours, then once daily until oral therapy can be tolerated, followed by a full course of an artemisinin-based combination therapy. Rectal: single dose of about 10 mg/kg before urgent referral, per WHO guidance.

Contraindications

Hypersensitivity to artesunate or other artemisinins.

Warnings and precautions

Post-artesunate delayed haemolysis may occur 1–3 weeks after treatment; monitor haemoglobin. Artesunate monotherapy must be followed by a complete course of combination therapy to prevent recrudescence and resistance. Rectal artesunate is a pre-referral measure only and does not replace definitive treatment.

Pregnancy

Recommended for severe malaria in all trimesters of pregnancy, as the benefit outweighs any risk.

Storage and supply

Store below 30 °C, protected from light; use the reconstituted solution within 1 hour.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.