Lumefantrine

CAS No:
82186-77-4 Category:
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Product Details:

  • CAS No: 82186-77-4
  • AHFC code: 08:30.1
  • Synonyms: Benflumetol
  • ATC Code: P01BF01
  • Chemical Formula: C18H22O4
  • Molecular Weight: 528.94
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB06708
  • SMILES: CCCCN(CCCC)CC(O)C1=C2C(=CC(Cl)=C1)C(=C/C1=CC=C(Cl)C=C1)C1=C2C=CC(Cl)=C1
  • InChl: DYLGFOYVTXJFJP-MYYYXRDXSA-N
  • PubChem: 5311253
  • IUPAC: 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-[(4-chlorophenyl)methylidene]-9H-fluoren-4-yl]ethan-1-ol

Additional Details

Indication:
Lumefantrine and artemether combination therapy is indicated for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum, including malaria acquired in chloroquine-resistant areas. May also be used to treat uncomplicated malaria when the Plasmodium species has not been identified. Indicated for use in adults and children greater than 5 kg.
Pharmacodynamics:
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 relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.
Mode of Action:
The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of _-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Metabolism:
Extensively metabolized in the liver primarily by cytochrome P450 3A4. The major metabolite found in plasma is desbutyl-lumefantrine.
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.
General Reference:
Artemether and Lumefantrine (2010). AHFS Drug Information [Electronic versionb]. Retrieved October 24, 2010. Artemether/Lumefantrine (2010). DrugPoints System [Electronic version]. Retrieved October 24, 2010. Novartis. Coartem (artemether/lumefantrine) tablets prescribing information. East Hanover, NJ; 2010 Feb.
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