Basic information Antimalarial drug Physical and Chemical Properties Pharmacokinetics Dosage Adverse reactions Precautions Safety Related Supplier
Lumefantrine Chemical Properties
- Melting point:129-131°C
- Boiling point:642.5±55.0 °C(Predicted)
- Density 1.252
- storage temp. Refrigerator
- solubility DMSO: ≥20mg/mL
- form powder
- color yellow
- Merck 14,5597
- CAS DataBase Reference82186-77-4(CAS DataBase Reference)
- WGK Germany 3
- HS Code 29221950
- Hazardous Substances Data82186-77-4(Hazardous Substances Data)
Lumefantrine Usage And Synthesis
- Antimalarial drugBenflumetol and artemether are the widely used antimalarial drugs currently in clinical , they are the main ingredients of the well-known anti-malarial drugs called Compound artemether of Novartis ,which can kill plasmodia asexual, insecticidal rate is high, the cure rate is about 95%, but it is invalid in the pre-erythrocytic stage and gametophyte . Animal experiments suggest it is drug with micro toxicity,but the mutagenic and teratogenic tests are negative. It is mainly used for the treatment of falciparum malaria in clinical, especially for the chloroquine-resistant falciparum malaria treatment.
- Physical and Chemical PropertiesYellow crystalline powder, bitter almond smell, tasteless. Soluble in chloroform, slightly soluble in acetone, almost insoluble in alcohol, melting point of 125~131 ℃.
- Pharmacokinetics Oral absorption is slow, elimination is also slow,it can stay a long time in the body . Tmax after administration is 4~5h, t1/2 is 24~72h.
- Dosage4d therapy: Adults eat 800mg at draught on the first day ,on day 2, 3, 4, each 400mg at draught; children daily take 8mg/kg at draught, and continue for 4d, the first dose is doubled, but the first dose does not exceed the maximum dose of 0.6g.
The above information is edited by the chemicalbook of Tian Ye.
- Adverse reactions There are no significant adverse reactions, a small number of patients suffer with electrocardiographic Q~T interval transient mild extending.
- Precautions Patients with heart, kidney dysfunction,should use with caution. After symptoms are controlled in patients with malignant malaria and the parasite is killed in the pre-erythrocytic stage ,primaquine can be used to kill gametocytes. It is saved in the dark, sealed, cool and dry place.
- Chemical PropertiesYellow Solid
- UsesInhibits hemozoin formation. Antimalarial
- UsesA drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human.
- DefinitionChEBI: Lumefantrine is an antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.
- Antimicrobial activityLumefantrine has marked blood schizonticidal activity against a wide range of plasmodia, including chloroquineresistant P. falciparum. The 50% and 90% effective concentrations (EC50 and EC90) in vitro are similar: <10 and 40 nmol/L, respectively. The racemate and the two enantiomers exhibit similar activities. Blood schizonticidal activity of desbutylbenflumetol is four to five times greater than benflumetol in vitro.
- Acquired resistanceTreatment with artemether–lumefantrine can select for polymorphisms in the P. falciparum pfmdr1 gene. Resistance has been selected experimentally in murine malaria.
- General DescriptionLumefantrine was developed in China. Itsmechanism of action is poorly understood. There is some evidencethat it inhibits the formation of β-hematin by forming acomplex with hemin. Lumefantrine is very lipophilic and is marketed in combination with the lipophilic artemesininderivedartemether.
- Pharmaceutical ApplicationsA dichlorobenzylidene derivative given orally in combination with artemether.
- PharmacokineticsBioavailability after oral administration is variable; absorption is substantially increased by co-administration with food, particularly with a high fat content. Peak plasma concentrations occur after 6–8 h. The elimination half-life is 4–6 days. It is almost completely protein bound and metabolized mainly in the liver by CYP3A4.
- Clinical UseTreatment of P. falciparum infections (including mixed infections) in a fixed-dose combination treatment with artemether.
- Side effectsThe most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.
- 2,7-Dichlorofluorene Lumefantrine Methylene Blue Dichlorodiphenylsilane Acetonitrile 4,4'-Diphenylmethane diisocyanate Sulfamic acid Diethylene glycol dibenzoate Basic Violet 1 Polyol benzoate Dichloroethane EC 184.108.40.206 Methylene Chloride Methanol Methyl acrylate Methyl Methylparaben Dichloromethylphenylsilane
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