Lumefantrine

• (RS ) -2 - ( Dibutylamino ) -1 - [( 9E) -2,7 - dichloro -9- [(4- chlorophenyl) - methylidene] - fluoren- 4-yl ] ethanol (IUPAC)
• (±) -2 - ( dibutylamino ) -1 - [( 9E) -2,7 - dichloro -9- [(4- chlorophenyl) - methylidene] - fluoren- 4-yl ] ethanol
• Rac -2-( Dibutylamino ) -1 - [( 9E) -2,7 - dichloro -9- [(4- chlorophenyl) - methylidene] - fluoren- 4-yl ] ethanol
• DL-2- ( dibutylamino ) -1 - [( 9E) -2,7 - dichloro -9- [(4- chlorophenyl) - methylidene] - fluoren- 4-yl ] ethanol

P01

Antiprotozoic

Hardly soluble in water, oil and most organic solvents, soluble in unsaturated fatty acids

Template: Infobox chemical / molecular formula search available

Lumefantrine (trade name: Riamet ®, manufactured by Novartis) is a drug for the treatment of falciparum malaria caused by Plasmodium.

Pharmacological properties

Lumefantrine probably interferes in the plasmodia with the removal of the toxic for the parasites to hemin Haemozin. The absorption of lipid-soluble substance is greatly facilitated by a high-fat meal as possible with oral administration. Lumefantrine has a half -life of four to six days. Lumefantrine is metabolized in the liver by the enzyme cytochrome P450 3A4.

Preparations and use

Lumefantrine is used exclusively as a combined preparation for the treatment of malaria with artemether. Mono-preparations of lumefantrine are not approved worldwide.

The focus for the use of artemether - lumefantrine combination products is the treatment of uncomplicated falciparum malaria, especially in plasmodia that are resistant to other drugs, such as chloroquine.

Stereoisomerism

The drug is used as a racemate ( 1:1 mixture of enantiomers ), although enantiomers typically have different pharmacological properties.