Lumefantrine

Bezeichnung:Lumefantrine

CAS-Nr82186-77-4

Englisch Name:Lumefantrine

CBNumberCB7854882

SummenformelC30H32Cl3NO

Molgewicht528.94

MOL-Datei82186-77-4.mol

Lumefantrine physikalisch-chemischer Eigenschaften

Schmelzpunkt	129-131°C
Siedepunkt	642.5±55.0 °C(Predicted)
Dichte	1.252
storage temp.	15-25°C
Löslichkeit	DMSO: ≥20mg/mL
pka	13.44±0.20(Predicted)
Aggregatzustand	powder
Farbe	yellow
Merck	14,5597
CAS Datenbank	82186-77-4(CAS DataBase Reference)

Sicherheit

WGK Germany	3
HS Code	29221950
Giftige Stoffe Daten	82186-77-4(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Lumefantrine Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Lumefantrine is a derivative of halofantrine that has been reported to exhibit antimalarial activity when combined with artemether in the treatment of multidrug-resistant Plasmodium falciparium . No evidence of cardiotoxicity has been reported with this combination, which may offer promise for successful treatment of resistant organisms.
Beschreibung
Lumefantrine is an antimalarial drug that is used in combination with artemether . The pairing of lumefantrine and artemether is a major form of oral artemisinin combination therapy used against uncomplicated P. falciparum malaria. Lumefantrine also blocks the rapidly activating delayed-rectifier potassium channel (I_Kr; IC₅₀ = 8.1 μM).
Chemische Eigenschaften
Yellow Solid
Verwenden
Lumefantrine has been used:
to study its effect on ex-vivo?Plasmodium falciparum?sensitivity using the tritiated hypoxanthine-based assay
as a standard in the quantification of combined tablet formulation using HPTLC
as a drug molecule in in vitro growth inhibition assay for in vitro B. caballi?growth inhibition studies
Verwenden
Inhibits hemozoin formation. Antimalarial.
Verwenden
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.
Allgemeine Beschreibung
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.
Pharmazeutische Anwendungen
A dichlorobenzylidene derivative given orally in combination with artemether.
Biochem/physiol Actions
Lumefantrine is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
Pharmakokinetik
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.
Nebenwirkungen
The most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.
Stoffwechsel
Primaquine is almost totally metabolized by CYP3A4 (99%), with the primary metabolite being carboxyprimaquine. Trace amounts of N-acetylprimaquine plus aromatic hydroxylation and conjugation metabolites also have been reported.

Lumefantrine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

82186-77-4, Lumefantrine Verwandte Suche:

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