Tablet Presentation

1. Each uncoated tablets contains:
a) Artemether IP              40 mg
Lumefantrine IP             240 mg
b) Artemether IP              80 mg
Lumefantrine IP             480 mg

2.Each dispersible tablets contains:
a) Artemether IP              40 mg
Lumefantrine IP             240 mg
b) Artemether IP              80 mg
Lumefantrine IP             480 mg

The combination of artemether and lumefantrine have better efficacy. Both the drugs act in the erythrocytic stage of plasmodium falcipuram.

Indications

• As antimalarial
• In chloroquine resistance malaria

About composition

Artemether:

Artemether is the semi-synthetic derivative of artemisnin obtained from artemisia annua (herb) is antimalarial drug. It is active against plasmodium falcipuram. It is also used in the chloroquine resistance malaria

Lumefantrine:

Lumefantrine is the synthetic racemic fluorine derivative with schizontocidal activity

Mechanism of action

Artemether is metabolized into its active form i.e dihydroartemisinin which works by inhibiting the nucleic acid and protein synthesis in the erythrocytic stage of p. falcipuram
Lumefantrine forms the complex with hematin and inhibit nucleic acid and protein synthesis

Pharmacokinetics

Absorption - Absorption increases with food
Protein binding - Both the drugs are highly bound to serum proteins
Metabolism - Artemether is rapidly metabolized to its active form dihydroartemisinin
Lumefantrine is metabolized in the liver to desbutyl-lumefantrine

Side effects

• Headache
• Anorexia
• Vomiting
• Raised body temperature
• Dizziness
• Cough
• Asthenia (physical weakness)

Contraindications

• Contraindicated in torsades de pointes.
• Contraindicated in people with low potassium and magnesium level.

Pregnancy: This combination is safe to use during pregnancy

Drug interactions

• Rifampin
• Ketoconazole
• Levonorgestrel
• Halofantrine