
Lumefantrine [Benflumetol]
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Category:Active Pharmaceutical Ingredients
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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