ルメファントリン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

ルメファントリン 価格

ルメファントリン 化学特性,用途語,生産方法

• 外観

  うすい黄色～くすんだ黄色～暗い緑色粉末～結晶

• 効能

  抗マラリア薬

• 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.

• 化学的特性

  Yellow Solid

• 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

• 定義

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

• 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.

• 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.

• 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.

• 応用例（製薬）

  A dichlorobenzylidene derivative given orally in combination with artemether.

• 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.

• 臨床応用

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

• 副作用

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

• 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.

ルメファントリン 生産企業

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