|AHFS/Drugs.com||International Drug Names|
|ATC code||P01BE02 (WHO)|
|Chemical and physical data|
|Molar mass||298.374 g/mol|
|3D model (Jmol)||Interactive image|
|(what is this?)|
It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system. It is available in combination with lumefantrine, known as artemether/lumefantrine, which is available as a generic medication.
Artemether is an antimalarial drug for uncomplicated malaria caused by P. falciparum (and chloroquine-resistant P. falciparum) or chloroquine-resistant P. vivax parasites. Artemether can also be used to treat severe malaria.
The World Health Organization recommends the treatment of uncomplicated P. falciparum with artemisinin-based combination therapy. Given in combination with lumefantrine, it may be followed by a 14 day regimen of primaquine to prevent relapse of P. vivax or P. ovale malarial parasites and provide a complete cure.
Artemether is rated category C by the FDA based on animal studies where artemisinin derivatives have shown an association with fetal loss and deformity. Some studies, however, do not show evidence of harm.
Possible side effects include cardiac effects such as bradycardia and QT interval prolongation. Also, possible central nervous system toxicity has been shown in animal studies.
Plasma artemether level was found to be lower when the combination product was used with lopinavir/ritonavir. There is also decreased drug exposure associated with concurrent use with efavirenz or nevirapine.
Artemether/lumefantrine should not be used with drugs that inhibit CYP3A4.
Mechanism of action
Artemether is an artemisinin derivative and the mechanism of action for artemisinins is unknown.
One of the proposed mechanisms is that through inhibiting anti-oxidant and metabolic enzymes, artemistinin derivatives inflict oxidative and metabolic stress on the cell. Some pathways affected may concern glutathione and glucose metabolism. As a consequence, lesions and reduced growth of the parasite may result.
Another possible mechanism of action suggests that arteristinin drugs exert their cidal action through inhibiting PfATP6. Since PfATP6 is an enzyme regulating cellular calcium concentration, its malfunctioning will lead to intracellular calcium accumulation, which in turns causes cell death.
Artemether is metabolized in the human body to the active metabolite, dihydroartemisinin, primarily by hepatic enzymes CYP3A4/5. Both the parent drug and active metabolite are eliminated with a half-life of about 2 hours.
Artemether is a methyl ether derivative of artemisinin, which is a peroxide-containing lactone isolated from the antimalarial plant Artemisia annua. It is also known as dihydroartemisinin methyl ether, but its correct chemical nomenclature is (+)-(3-alpha,5a-beta,6-beta,8a-beta, 9-alpha,12-beta,12aR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin. It is a relatively lipophilic and unstable drug, which acts by creating reactive free radicals in addition to affecting the membrane transport system of the plasmodium organism.
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