Artemether and Lumefantrine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Induces
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Riamet; Belgium: Riamet; Czech Republic: Riamet; France: Riamet; Germany: Riamet; Greece: Riamet; Netherlands: Riamet; Poland: Riamet; Portugal: Riamet; Sweden: Riamet; UK: Riamet.

North America

USA: Coartem.

Latin America

Brazil: Paluther (Artemether only).

Drug combinations


Artemether and Lumefantrine: C~46~H~58~Cl~3~NO~6~. Mw: 827.31482. 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl]ethanol – (4S,5R,8S,9R,10S,12R,13R)-10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[,13~.0~8,13~]hexadecane (1:1). CAS-71963-77-4 (Artemether). CAS-82186-77-4 (Lumefantrine).

Pharmacologic Category

Antiprotozoals; Antimalarials. (ATC-Code: P01BF01).

Mechanism of action

Artemether is rapidly metabolized into an active metabolite dihydroartemisinin. The anti-malarial activity of artemether and dihydroartemisinin has been attributed to endoperoxide moiety. The exact mechanism by which lumefantrine exerts its anti-malarial effect is not well defined. Available data suggest that lumefantrine inhibits the formation of b-hematin by forming a complex with hemin. Both artemether and lumefantrine were shown to inhibit nucleic acid and protein synthesis.

Therapeutic use

Treatment of acute, uncomplicated malaria infections due to Plasmodium falciparum in patients of ≥5 kg body weight. Effective in geographical regions where resistance to chloroquine has been reported. Should not be used to treat severe malaria or to prevent malaria.

Pregnancy and lactiation implications

May increase fetal loss in pregnancy. Should be used with caution in nursing women.

Unlabeled use


Hypersensitivity to artemether, lumefantrine, or any component of the formulation.

Warnings and precautions

Avoid use in patients with known QT-prolongation, those with hypokalemia or hypomagnesemia, and those taking other drugs that prolong the QT interval. Should not be administered with halofantrine within one month of each other due to potential additive effects on the QT interval. Antimalarials should not be given concomitantly, unless there is no other treatment option, due to limited safety data. QT prolonging drugs, including quinine and quinidine, should be used cautiously following artemether and lumefantrine combination. Substrates, inhibitors, or inducers of CYP3A4, including antiretroviral medications, should be used cautiously with this drug combination, due to a potential loss of efficacy of the concomitant drug or additive QT prolongation.



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