Artemether

Products

Artemether is commercially available as tablets and dispersible tablets as a fixed combination with lumefantrine (Riamet, some countries: Coartem). It has been approved in many countries since 1999.

Structure and properties

Artemether (C16H26O5, Mr = 298.4 g/mol) is a methyl ether dervate of the sesquiterpene artemisinin from the annual mugwort (, Qing Hao), a medicinal plant used in traditional Chinese medicine. Artemether exists as a white crystalline powder that is practically insoluble in water. It is a prodrug of the active metabolite dihydroartemisinin. Artemether belongs to the organic peroxides.

Effects

Artemether (ATC P01BE02) has antiparasitic properties against blood horizons. It acts at the level of the food vacuole of the pathogens, where toxic radicals are formed. This inhibits nucleic acid and protein synthesis. The relevant structural element is the endoperoxide. Artemether has a short half-life of about 2 hours.

Indications

For treatment of malaria caused by , including mixed infections.

Dosage

According to the SmPC. The tablets should be taken with food containing fat or with milk because this increases absorption and bioavailability. Adults require 24 tablets:

  • 4 tablets immediately after diagnosis or at the onset of symptoms.
  • After 8 hours, another 4 tablets
  • Then 4 tablets twice a day (morning and evening) for the following two days.

Children: see the professional information.

Contraindications

For complete precautions, see the drug label.

Interactions

Artemether is a substrate of CYP3A4 and corresponding drug interactions with CYP inhibitors and inducers are possible.

Adverse effects

The most common potential adverse effects include headache, poor appetite, dizziness, weakness, and muscle and joint pain.