Artemether

IUPAC: (3R, 5AS, 6R, 8aS, 9R, 10S, 12R, 12aR ) - decahydro -10 - methoxy-3 ,6,9 - trimethyl-3 ,12 -epoxy- 12H - pyrano [4,3- j] -1,2- benzodioxepin

P01BE02, P01BE52

Antiprotozoic

86-88 ° C

263 mg · kg -1 ( LD50, mouse, i.m. )

Template: Infobox chemical / molecular formula search available

Artemether is a derivative of artemisinin semisynthetic drug for the treatment of falciparum malaria caused by Plasmodium. The active ingredient Artemether has been included in the list of essential drugs of the World Health Organization of the World Health Organization (WHO ) in 1997. It is sold in Germany, Austria and Switzerland in combination with lumefantrine under the trade name Riamet ® and the world under the trade name Coartem ®.

Pharmacological properties

Artemether has a significantly improved bioavailability compared to artemisinin. Like all artemisinin derivatives act through an endogenous peroxide, which presumably releases toxic for the radicals in Plasmodium -infected erythrocytes. The absorption of lipid-soluble substance is facilitated by a high-fat meal as possible with oral administration. Another problem is the relatively short half-life of about two hours. Artemether is metabolized in the liver by the enzyme cytochrome P450 3A4.

Use

The focus for the application of artemether is the treatment of uncomplicated falciparum malaria, especially in plasmodia that are resistant to other drugs, such as chloroquine. The World Health Organization does not recommend the use as a single agent to reduce the risk of resistance to artemisinin derivatives.

Artemether is tentatively used in cancer therapy.

Production

Artemether is represented by reacting derived from Artemisia annua dihydroartemisinin with methanol in an acid medium. Artemether is water insoluble.