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Artemether

Artemether

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PRODUCT NAME: Artemether
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

MP 86-88°C
storage temp.
Store at RT
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
Usage Derivative of Artemisinin (A777500). Antimalarial, used to treat strains of malaria which are multi-drug resistant. 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.

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