Лумефантрин
- английское имяLumefantrine
- CAS №82186-77-4
- CBNumberCB7854882
- ФормулаC30H32Cl3NO
- мольный вес528.94
- EINECS617-303-4
- номер MDLMFCD05662268
- файл Mol82186-77-4.mol
химическое свойство
| Температура плавления | 129-131°C |
| Температура кипения | 642.5±55.0 °C(Predicted) |
| плотность | 1.252 |
| температура хранения | 15-25°C |
| растворимость | DMSO: ≥20mg/mL |
| пка | 13.44±0.20(Predicted) |
| форма | powder |
| цвет | yellow |
| Мерк | 14,5597 |
| Справочник по базе данных CAS | 82186-77-4(CAS DataBase Reference) |
| FDA UNII | F38R0JR742 |
| WGK Германия | 3 |
| кода HS | 29221950 |
| Банк данных об опасных веществах | 82186-77-4(Hazardous Substances Data) |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
предупреждение
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вредная бумага
H315：При попадании на кожу вызывает раздражение.
H319：При попадании в глаза вызывает выраженное раздражение.
H335：Может вызывать раздражение верхних дыхательных путей.
H302：Вредно при проглатывании.
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оператор предупредительных мер
P261：Избегать вдыхания пыли/ дыма/ газа/ тумана/ паров/ аэрозолей.
P305+P351+P338：ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой в течение нескольких минут. Снять контактные линзы, если Вы ими пользуетесь и если это легко сделать. Продолжить промывание глаз.
Лумефантрин химические свойства, назначение, производство
Описание
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.Химические свойства
Yellow SolidИспользование
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
Определение
ChEBI: Lumefantrine is an antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.Антимикробная активность
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.Приобретенная устойчивость
Treatment with artemether–lumefantrine can select for polymorphisms in the P. falciparum pfmdr1 gene. Resistance has been selected experimentally in murine malaria.Общее описание
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.Фармацевтические приложения
A dichlorobenzylidene derivative given orally in combination with artemether.Фармакокине?тика
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.Клиническое использование
Treatment of P. falciparum infections (including mixed infections) in a fixed-dose combination treatment with artemether.Побочные эффекты
The most common adverse effects in combination with artemether include headache, dizziness and gastrointestinal disturbances.Метаболизм
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.Лумефантрин поставщик
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