Lumefantrine [Benflumetol]

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Category:Active Pharmaceutical Ingredients

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Introduction

Catalog ID80018337

CAS NO.82186-77-4

Purity 98%

MDL NumberMFCD05662268

EINEColecular FormulaC30H32Cl3NO

Molecular Weight528.9402

Melting point: 125~133°C

Category Details
Chemical Properties Molecular formula: C30H32Cl3NO<br> Molecular weight: 528.9
Physical Properties Appearance: Yellow crystalline powder<br> Solubility: Freely soluble in N,N-dimethylformamide, chloroform, and ethyl acetate; soluble in dichloromethane; slightly soluble in ethanol and methanol; insoluble in water
Mechanism of Action Lumefantrine is an antimalarial agent. It is believed to inhibit the formation of β-hematin by forming a complex with hemin, thereby disrupting the parasite’s ability to detoxify heme. It also inhibits nucleic acid and protein synthesis in Plasmodium parasites.
Therapeutic Uses Used in combination with artemether (as Coartem Tablets) for the treatment of acute, uncomplicated malaria caused by Plasmodium falciparum.
Pharmacokinetics Absorption: Peak plasma concentrations of lumefantrine are reached about 6 to 8 hours after administration.<br> Food Effect: Absorption is significantly enhanced when taken with a high-fat meal.<br> Distribution: Highly bound to human serum proteins (99.7%).<br> Metabolism: Metabolized primarily in the liver.<br> Elimination: Half-life is approximately 101–119 hours.
Formulations Available in combination with artemether in fixed-dose tablets (Coartem Tablets) containing 20 mg artemether and 120 mg lumefantrine.
Safety and Precautions Pediatric Use: Safety and effectiveness established in pediatric patients weighing 5 kg or more.<br> Geriatric Use: Limited data in patients aged 65 years and over.<br> Hepatic and Renal Impairment: No dose adjustment needed for renal impairment; caution advised in severe hepatic impairment.<br> Drug Interactions: Use with caution in patients on antiretroviral drugs (e.g., lopinavir/ritonavir, efavirenz) as it may affect drug levels.<br> QT Prolongation: Increased lumefantrine concentrations may cause QT prolongation.
Storage Conditions Store at room temperature, protect from light and moisture.
Synonyms Benflumetol, Lumefantrine

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