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QuickView for Lumefantrine (compound)

Name: lumefantrine
PubChem Compound ID: 5311253
Molecular formula: C30H32Cl3NO
Molecular weight: 528.939 g/mol
Name: lumefantrine
Name (isomeric): DB06708
Drug Type: small molecule
Brand: Coartem
Brand name mixture: Coartem(Artemether and Lumefantrine)
Category: Antimalarials, Antimalarial Agents
CAS number: 82186-77-4
Indication: Lumefantrine and artemether combination therapy is indicated for the treatment of acute uncomplicated malaria caused by <i>Plasmodium falciparum</i>, including malaria acquired in chloroquine-resistant areas. May also be used to treat uncomplicated malaria when the <i>Plasmodium</i> species has not been identified. Indicated for use in adults and children greater than 5 kg.
Lumefantrine is a blood schizonticide active against erythrocytic stages of Plasmodium falciparum. It is thought that administration of lumefantrine with artemether results in cooperate antimalarial clearing effects. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thus thought to provide rapid symptomatic r...
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Mechanism of Action: The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Absorption: Food increases absorption.
Protein binding: 99.7% bound
Biotransformation: Extensively metabolized in the liver primarily by cytochrome P450 3A4. The major metabolite found in plasma is desbutyl-lumefantrine.
Half Life: ~ 4.5 days
Toxicity: Common side effects of combination artemether/lumefantrine therapy in adults include headache, anorexia, dizziness, and asthenia. Common side effects in children include pyrexia, cough, vomiting, anorexia, and headache. Possible serious adverse effects include QT prolongation, bullous eruption, urticaria, splenomegaly (9%), hepatomegaly (adults, 9%; children, 6%), hypersensitivty reaction, and angioedema.
Affected organisms: Plasmodium
Food interaction:
Take with food as food increases the absorption of lumefantrine and artemether.
Grapefruit juice may increase the toxicity of artemether and lumefantrine by inhibiting their metabolism.
Drug interaction:
PimozideAdditive QTc-prolongation may occur. Concomitant therapy is contraindicated.
TacrolimusAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
SotalolAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
ChlorpromazineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
TrimipramineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
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