Mechanism of Action:
Artemether and Lumefantrine combination is a fixed dose artemisinin-based combination therapy (ACT) combining artemether, an artemisinin derivative and lumefantrine, a synthetic antimalarial drug.
Artemether is absorbed with peak plasma concentrations reached about 2 hours after dosing. Absorption of lumefantrine, a highly lipophilic compound, starts after a lag-time of up to 2 hours, with peak plasma concentrations about 6 to 8 hours after administration.
Artemether and lumefantrine are both highly bound to human serum proteins in vitro (95.4% and 99.7% respectively). Artemether are cleared from plasma with elimination half-life of about 2 hours. Lumefantrine is eliminated more slowly, with a terminal half-life of 3-6 days.
No specific pharmacokinetic studies have been performed in patients older than 65 years of age.
For the treatment of most forms and resistant types of malaria.
• Patients who are taking any drug which is metabolised by the cytochrome enzyme CYP2D6 (e.g. flecainide, metoprolol, imipramine, amitriptyline, clomipramine).
• Patients with disturbances of electrolyte balance e.g. hypokalemia.
• It must not be used in first Trimester of Pregnancy.
• It has not been evaluated for treatment of severe malaria
• For the treatment of most forms and resistant types of malaria.
It has the interactions with other antimalarials, CYP450 3M Inhibitors, Protease Inhibitor and anti-retroviral Drugs.
PREGNANCY AND LACTATION
There is insufficient data from the use of Arterhether and lumefantrine in pregnant women. Based on animal data, it is suspected to cause serious birth defects when administered during the first trimester of pregnancy.
During the second and third trimester, treatment should only be considered if the expected benefit to the mother outweighs the risk to the foetus.
Animal data suggest excretion into breast milk but no data are available in humans. Women taking the product should not breast-feed during their treatment.
Due to the long elimination half-life of lumefantrine (4 to 6 days), it is recommended that breastfeeding should not resume until at least one week after the last dose unless potential benefits to the mother and child outweigh-the risk of treatment.
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