LONART DISPERSIBLE TABLET

Indications

• Uncomplicated Plasmodium falciparum malaria
• Treatment of malaria in patients not requiring hospitalization

Dosage

Children: Refer to specific guidelines for dosing as per the BNF for Children.

Adults: Refer to specific guidelines for dosing as per the BNF.

Mechanism of action

Artemether works by producing free radicals when it interacts with the heme group released from hemoglobin during the digestion of red blood cells by malaria parasites. These free radicals damage the parasite's membranes and proteins, leading to cell death. Lumefantrine acts by inhibiting the β-haematin formation, which is crucial for the detoxification of heme within the parasite. The combination of these two mechanisms leads to a rapid reduction in parasitemia.

Pharmacodynamics

Artemether-lumefantrine exhibits synergistic antimalarial activity with a rapid onset of action due to artemether and sustained activity from lumefantrine. The combination has been shown to be effective against a range of malaria strains, including those resistant to other antimalarial drugs. The pharmacodynamic properties also indicate a strong correlation between drug concentration and therapeutic effect, with optimal dosing necessary to prevent recrudescence.

Pharmacokinetics

Artemether is rapidly absorbed, reaching peak plasma concentrations within 2 hours, while lumefantrine has a longer absorption phase with peak concentrations occurring around 6-8 hours post-administration. Both drugs are metabolized primarily in the liver, with lumefantrine having a longer elimination half-life compared to artemether. The combination results in a prolonged exposure of the malaria parasite to the active compounds, enhancing efficacy.

Contra-indications

• Hypersensitivity to artemether, lumefantrine, or any excipients
• Severe liver impairment
• Severe cardiac disorders, including arrhythmias

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Palpitations
• Headache
• Fatigue
• Dizziness
• Anemia
• Rash
• Elevated liver enzymes

Interactions

• Caution with drugs that prolong the QT interval
• Concomitant use with drugs that are potent CYP3A4 inducers or inhibitors may alter levels
• Antimalarials may interfere with the pharmacokinetics of other medications

Precautions

• Monitor for signs of hypersensitivity reactions
• Use with caution in patients with a history of arrhythmias
• Assess liver function prior to and during treatment
• Use in caution in patients with a history of seizures

Pregnancy

Artemether-lumefantrine is generally considered safe in pregnancy, particularly in the second and third trimesters, but should only be used if clearly needed.

Breast-feeding

Artemether-lumefantrine is excreted in breast milk; caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Tablets
• Oral suspension