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Lumefantrine

Antimalarial drug Physical and Chemical Properties Pharmacokinetics Dosage Adverse reactions Precautions
Lumefantrine
Lumefantrine structure
CAS No.
82186-77-4
Chemical Name:
Lumefantrine
Synonyms
CPG-56695;Benwuchun;benflumetol;Benflumelol;Lumefantrine;Benflumentol;LuMefentrine;Lumefruntrine;LuMenfantrine;BENFLUMETOLUM
CBNumber:
CB7854882
Molecular Formula:
C30H32Cl3NO
Formula Weight:
528.94018
MOL File:
82186-77-4.mol

Lumefantrine Properties

Melting point:
129-131°C
Boiling point:
642.5±55.0 °C(Predicted)
Density 
1.252
storage temp. 
Refrigerator
solubility 
DMSO: ≥20mg/mL
pka
13.44±0.20(Predicted)
form 
powder
color 
yellow
Merck 
14,5597
CAS DataBase Reference
82186-77-4(CAS DataBase Reference)
FDA UNII
F38R0JR742
SAFETY
  • Risk and Safety Statements
WGK Germany  3
HS Code  29221950

Lumefantrine price More Price(10)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich L5420 Lumefantrine 82186-77-4 5mg $91.6 2019-12-02 Buy
Sigma-Aldrich 1370746 Lumefantrine United States Pharmacopeia (USP) Reference Standard 82186-77-4 100mg $352.8 2019-12-02 Buy
TCI Chemical L0256 Lumefantrine >98.0%(HPLC)(T) 82186-77-4 5g $81 2020-06-24 Buy
TCI Chemical L0256 Lumefantrine >98.0%(HPLC)(T) 82186-77-4 25g $271 2020-06-24 Buy
Cayman Chemical 20678 Lumefantrine ≥98% 82186-77-4 1g $25 2020-06-24 Buy

Lumefantrine Chemical Properties,Uses,Production

Antimalarial drug

Benflumetol 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 Properties

Yellow 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.

Dosage

4d 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 Properties

Yellow Solid

Uses

Inhibits hemozoin formation. Antimalarial

Uses

A 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.

Definition

ChEBI: Lumefantrine is an antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.

Antimicrobial activity

Lumefantrine 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 resistance

Treatment with artemether–lumefantrine can select for polymorphisms in the P. falciparum pfmdr1 gene. Resistance has been selected experimentally in murine malaria.

General Description

Lumefantrine 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 Applications

A dichlorobenzylidene derivative given orally in combination with artemether.

Pharmacokinetics

Bioavailability 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 Use

Treatment of P. falciparum infections (including mixed infections) in a fixed-dose combination treatment with artemether.

Side effects

The most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.

Lumefantrine Preparation Products And Raw materials

Raw materials

Preparation Products


Lumefantrine Suppliers

Global( 226)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
zhangjiagang vinsce bio-pharm. limited.
86-512-58389969
sales1@swellxin.com CHINA 71 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile
+86-571-56059825 fandachem@gmail.com CHINA 3246 55
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 2399 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23977 58
Haihang Industry Co.,Ltd
86-531-88032799
+86 531 8582 1093 export@haihangchem.com CHINA 10173 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114
sales@amoychem.com CHINA 6371 58
HubeiwidelychemicaltechnologyCo.,Ltd
18627774460
faith@widelychemical.com CHINA 743 58

View Lastest Price from Lumefantrine manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2020-04-27 Lumefantrine
82186-77-4
US $0.00-0.00 / 公斤 1公斤 99.0% 500 tons Shaanxi Dideu Medichem Co. Ltd
2020-04-27 Lumefantrine
82186-77-4
US $0.00-0.00 / 公斤 1公斤 99.0% 500 tons Shaanxi Dideu Medichem Co. Ltd
2019-07-09 Lumefantrine
82186-77-4
US $7.00 / KG 1KG 99% 100KG career henan chemical co

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