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QuickView for Artemether (compound)

Name: artemether
PubChem Compound ID: 10266705
Molecular formula: C16H26O5
Molecular weight: 298.375 g/mol
Name: artemether
Name (isomeric): DB06697
Drug Type: small molecule
Dihydroartemisinin methyl ether
Brand: Coartem
Brand name mixture: Coartem(artemether, lumefantrine), Riamet(artemether, lumefantrine)
Category: Antimalarials, Antiprotozoal Agents, Antimalarial Agents
CAS number: 71963-77-4
Indication: Artemether and lumefantrine combination therapy is indicated for the treatment of acute uncomplicated malaria caused by <i>Plasmodium falciparum</i>, including malaria acquired in chloroquine-resistant areas. May also be used to treat uncomplicated malaria when the <i>Plasmodium</i> species has not been identified. Indicated for use in adults and children greater than 5 kg.
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 rap...
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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, de...
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Absorption: Food increases absorption.
Protein binding: Artemether, 95.4%; Dihydroartemisinin, 47-76%
Biotransformation: Rapidly metablized to its active metabolite, dihydroartemisinin.
Half Life: Artemether, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr
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
Food interaction:
Take with food as food increases the absorption of artemether and lumefantrine.
Grapefruit juice may increase the toxicity of artemether and lumefantrine by inhibiting their metabolism.
Drug interaction:
PimozideAdditive QTc-prolongation may occur. Concomitant therapy is contraindicated.
ChlorpromazineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
MoxifloxacinAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
TrimipramineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
NorgestrelArtemether may decrease the effectiveness of norgestrel by increasing its metabolism via CYP3A4. Consider an alternate non-hormonal means of contraception during artemether therapy.
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