Artesunate
Antimalarials
Antimalarials
Water-soluble artemisinin given IV or IM as first treatment for severe malaria of any species; it clears parasites faster and is safer than quinine.
Quick facts
- Group
- Antimalarials
- Target
- Parasite heme iron, which opens the endoperoxide bridge (activation), and many parasite proteins
- Used for
- Severe · Pre-referral treatment
- Key effects
- Nausea and other mild stomach upset · Dizziness
- Monitor
- Level of consciousness · Blood glucose
- ATC
- P01BE03
No doses: the clinician sets them by the current guideline.
Mechanism of action
A hemisuccinate derivative of dihydroartemisinin. Plasma esterases turn it within minutes into dihydroartemisinin, its active form. Inside the parasite, heme iron opens the endoperoxide bridge, producing reactive intermediates that alkylate and damage parasite proteins. It kills all red-cell stages, including young ring forms, which is why parasite counts fall faster than with quinine; it has no useful activity against liver stages.
- Esterases convert it to dihydroartemisinin
- Heme iron opens the endoperoxide bridge
- Free radicals alkylate parasite proteins
- Ring stages to schizonts die quickly
Indications
- Severe (complicated) malaria of any species in adults, children, pregnant women in any trimester and breastfeeding women Malaria →
- Pre-referral treatment: a single IM dose (or a rectal dose in young children) before transfer when full treatment is not possible Malaria →
- Oral artesunate is part of several artemisinin combinations (with amodiaquine, mefloquine, pyronaridine or sulfadoxine-pyrimethamine)
Adverse effects
Common
- Nausea and other mild stomach upset
- Dizziness
- Cough, rash and joint pain
- Falls in reticulocytes and neutrophils
Contraindications
- Known hypersensitivity to artesunate or other artemisinin derivatives
Key interactions
- Oral partner drug (ACT)
- Artesunate alone is never a full treatment: a complete oral ACT course must follow
- Rifampicin (during the follow-on artemether + lumefantrine course)
- Lowers artemether, dihydroartemisinin and lumefantrine exposure
What is monitored
- Level of consciousness, vital signs and urine output
- Blood glucose, frequently in unconscious patients
- Parasite count until it clears
- Haemoglobin in the weeks after treatment (delayed haemolysis), especially after hyperparasitaemia
Administration and safety
- Parenteral (IV or IM into the anterior thigh) at set times, until the patient can take oral medicine; then a full oral ACT course.
- The powder is first dissolved in the sodium bicarbonate supplied in the kit, then diluted with the supplied saline (more for IV, less for IM).
- Prepare a fresh solution for each dose; discard it if cloudy, if a precipitate forms or if it is not used within the first hour.
- IV injection is given slowly over a minute or two; children under a weight threshold receive a slightly higher dose per kilogram.
Pregnancy and breastfeeding
For severe malaria it is recommended in every trimester because it can save the mother's life; animal data showed early-pregnancy fetal toxicity, without evidence of teratogenicity in humans.
Nursing care
- Before: weight (dose is per kilogram), blood glucose, smear and baseline haemoglobin.
- During: neuro checks, vital signs, urine output and glucose; watch for convulsions and bleeding.
- Switch to oral treatment only when the patient can swallow and keep tablets down, and make sure the full oral course is given.
- After discharge: teach the patient to report pallor, tiredness, dark urine or yellow eyes in the following weeks (delayed haemolysis).
Pharmacokinetics
- Absorption
- Given IV or IM for severe malaria (peak within minutes); rectal form for pre-referral treatment of young children
- Distribution
- Dihydroartemisinin is mostly bound to plasma proteins
- Metabolism
- Rapid hydrolysis by plasma esterases to dihydroartemisinin, then glucuronidation
- Elimination
- Dihydroartemisinin glucuronides are excreted in urine
- Half-life
- Very short: artesunate and dihydroartemisinin are cleared rapidly
Test yourself
Think of the answer, then tap the question to see it.
Why is artesunate preferred over quinine for severe malaria?
In trials it lowered mortality compared with parenteral quinine; it clears parasites faster, including young ring forms, and is better tolerated.
What late complication is watched for after IV artesunate?
Delayed haemolysis starting about a week later, as red cells cleared of parasites in the spleen return with a shorter life span; haemoglobin is followed.
What must follow parenteral artesunate?
A complete oral course of an artemisinin-based combination (in Colombia artemether + lumefantrine) once the patient tolerates oral drugs.
Connections
← Back to the class: Antimalarials
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Adopción Parcial de Guía de Práctica Clínica Diagnóstico y tratamiento de la malaria, OMS 2022. Guía para Colombia, GPC #67-2022 (Ministerio de Salud y Protección Social (Colombia), 2022); Malaria in the United States: Treatment Tables (Centers for Disease Control and Prevention (CDC), 2026); Malaria (World Health Organization, 2025).
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Representative model, for educational purposes only.