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外観
うすい黄色～くすんだ黄色～暗い緑色粉末～結晶
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効能
抗マラリア薬
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説明
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.
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化学的特性
Yellow Solid
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使用
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
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定義
ChEBI: Lumefantrine is an antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.
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抗菌性
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.
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獲得抵抗性
Treatment with artemether–lumefantrine can select for polymorphisms
in the P. falciparum pfmdr1 gene. Resistance has
been selected experimentally in murine malaria.
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一般的な説明
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.
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応用例（製薬）
A dichlorobenzylidene derivative given orally in combination
with artemether.
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薬物動態学
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.
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臨床応用
Treatment of P. falciparum infections (including mixed infections)
in a fixed-dose combination treatment with artemether.
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副作用
The most common adverse effects in combination with artemether
include headache, dizziness and gastrointestinal disturbances.
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代謝
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.
