Artesunate
A water-soluble artemisinin given IV or IM as first-line treatment for severe malaria, and by mouth in ACT combinations.
Drug card
- Class
- Artemisinin
- How it works
- Releasing free radicals when heme iron splits their peroxide bridge
- Used for
- Severe malaria, first-line (IV or IM)
- Uncomplicated falciparum malaria, with a partner drug
- Known for
- Delayed hemolytic anemia after treatment
- Its name
- arte- means an artemisinin antimalarial
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does artesunate work?
Artesunate is a water-soluble artemisinin that blood esterases convert within minutes to dihydroartemisinin (DHA). Heme iron activates the endoperoxide bridge of both, causing oxidative damage that kills blood-stage parasites, including chloroquine-resistant P. falciparum, and gametocytes. It does not reach the liver hypnozoites of P. vivax and P. ovale.
Like other artemisinins: Artemisinins carry an endoperoxide bridge. In infected red cells, heme iron splits this bridge, releasing free radicals and reactive oxygen species that damage parasite proteins and nucleic acids. They clear blood-stage parasites within 2 to 3 days, including chloroquine-resistant P. falciparum, and kill gametocytes, but miss the dormant liver forms. Artemether and artesunate both become dihydroartemisinin (DHA).
Uses
What is artesunate used for?
- Severe malaria, first-line (IV or IM)
- Uncomplicated falciparum malaria, with a partner drug
Side effects
Side effects of artesunate
- Delayed hemolytic anemia after treatmentKnown forSerious
- Acute kidney injury (in severe malaria)Serious
- Jaundice and raised liver enzymes
- Low white cell count
- Anaphylaxis and other allergic reactionsSerious
- Taste change
- Headache
- Dizziness
- Ringing in the ears (tinnitus)
- Vomiting and abdominal pain
- PancreatitisSerious
- Stevens-Johnson syndrome (rare)Serious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Check hemoglobin for 4 weeks after treatment: delayed hemolysis can be severe enough to need a transfusion.
- Once the patient can swallow, follow IV artesunate with a full course of an oral ACT.
- Pregnancy is no reason to delay it in severe malaria: WHO advises it in all trimesters.
- Strong UGT inducers (rifampicin, carbamazepine, phenytoin), ritonavir and nevirapine may weaken its effect.
Good to know: WHO's first choice for severe malaria in adults, children and pregnant women, preferred over quinine. Where full care is out of reach, one IM dose, or a rectal dose in young children, is given before referral.
Remember it
A way to remember it
Artemisinins carry a peroxide bomb that the parasite's heme sets off.
Heme iron inside the infected red cell splits the drug's endoperoxide bridge, releasing free radicals that damage the parasite.
Written for biofideX
Its name
arte- means artemisinin antimalarial
Artemether, artesunate and artemisinin itself share it. Artemether is given in a combination with lumefantrine.
- Every drug name stem
Its class
Artemisinins
Other artemisinins with a card:
Easily mixed up with 4-aminoquinolines and 8-aminoquinolines.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Antifungals and antiparasitics
Artesunate is one of 14 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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