Artemether
1.White Crystal or crystalline powder. 2.Smell-less bitterness. 3.an antimalarial agent used to treat acute uncomplicated mal
1.White Crystal or crystalline powder. 2.Smell-less bitterness.3.an antimalarial agent used to treat acute uncomplicated malaria
4.usually administered in combination with lumefantrine for improved efficacy
| Indication | Artemether and lumefantrine combination therapy is indicated for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum, including malaria acquired in chloroquine-resistant areas. May also be used to treat uncomplicated malaria when the Plasmodium species has not been identified. Indicated for use in adults and children greater than 5 kg. |
| Pharmacodynamics | In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites. |
| Mechanism of action | Involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. |
| Absorption | Food increases absorption. |
| Volume of distribution | Not Available |
| Protein binding | Artemether, 95.4%; Dihydroartemisinin, 47-76% |
| Metabolism | Rapidly metablized to its active metabolite, dihydroartemisinin. |
| Route of elimination | Not Available |
| Half life | Artemether, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr |
| Clearance | Not Available |
| Toxicity | Common side effects of combination artemether/lumefantrine therapy in adults include headache, anorexia, dizziness, and asthenia. Common side effects in children include pyrexia, cough, vomiting, anorexia, and headache. Possible serious adverse effects include QT prolongation, bullous eruption, urticaria, splenomegaly (9%), hepatomegaly (adults, 9%; children, 6%), hypersensitivty reaction, and angioedema. |
| Affected organisms | Plasmodium |
Artemether
