Artemether
An artemisinin given with lumefantrine (artemether-lumefantrine) as tablets for uncomplicated falciparum malaria.
Drug card
- Class
- Artemisinin
- How it works
- Releasing free radicals when heme iron splits their peroxide bridge
- Used for
- Uncomplicated falciparum malaria (with lumefantrine)
- Severe malaria by IM injection when artesunate is lacking
- Known for
- Long QT interval
- 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 artemether work?
Artemether is converted, mainly by CYP3A4, to the active metabolite dihydroartemisinin, and its endoperoxide group damages the parasite. It is given as a fixed tablet with lumefantrine, which binds heme and stops it forming β-hematin. Artemether lasts only hours, while lumefantrine lingers (its half-life runs to days) and clears the parasites that remain.
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 artemether used for?
- Uncomplicated falciparum malaria (with lumefantrine)
- Severe malaria by IM injection when artesunate is lacking
Side effects
Side effects of artemether
- Long QT intervalKnown forSerious
- Headache
- Loss of appetite
- Dizziness
- Weakness and tiredness
- Joint pain
- Muscle pain
- Nausea, vomiting and abdominal pain
- Palpitations
- Sleep problems
- Delayed hemolytic anemiaSerious
- Allergic reactions, including anaphylaxisSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Avoid with a long QT interval, low potassium or magnesium, or other QT-prolonging drugs.
- Strong CYP3A4 inducers (St John's wort, rifampicin, carbamazepine, phenytoin) are contraindicated: treatment may fail.
- Food, fat above all, raises absorption several-fold; patients who cannot eat are at risk of the infection returning.
- May make hormonal contraceptives less effective, and it does not prevent vivax relapse.
Good to know: Always given with lumefantrine: artemether clears most parasites fast and slowly eliminated lumefantrine kills the rest. WHO recommends it for falciparum malaria in early pregnancy, including the first trimester.
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
Artemether 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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