LUM-ARTEM 20/120MG TABLET

Indications

• Acute uncomplicated malaria caused by Plasmodium falciparum
• Severe malaria (as part of combination therapy)
• Prophylaxis against malaria in endemic areas

Dosage

Children: Refer to BNF for Children for appropriate dosing guidance in paediatric patients.

Adults: Refer to national guidelines or BNF for specific dosing recommendations for adults.

Mechanism of action

Artemether exerts its antimalarial effects by generating free radicals when it interacts with heme, a byproduct of hemoglobin breakdown in the malaria parasite. These free radicals cause damage to the parasite's cell membranes and proteins, leading to its death. The drug is particularly effective against the blood stages of malaria, disrupting the life cycle of Plasmodium species.

Pharmacodynamics

The pharmacodynamics of artemether involve its rapid onset of action, leading to a decrease in parasitemia within a short period. It is effective against both drug-sensitive and drug-resistant strains of Plasmodium falciparum. The combination with other antimalarials helps to ensure a more sustained therapeutic effect and further reduces the risk of resistance development.

Pharmacokinetics

Artemether is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 2 hours after oral administration. It undergoes extensive hepatic metabolism, primarily via cytochrome P450 enzymes, leading to the formation of active metabolites, including dihydroartemisinin. The elimination half-life of artemether is approximately 2 to 3 hours, while its active metabolite has a longer half-life, contributing to its prolonged antimalarial effect. The drug is excreted mainly in the urine as metabolites.

Contra-indications

• Hypersensitivity to artemether, lumefantrine, or any component of the formulation
• Severe malaria (cerebral malaria, severe anemia, or respiratory distress)

Adverse effects

• Nausea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Palpitations
• Anemia
• Transaminase elevation

Interactions

• Caution when used with other antimalarials, as additive effects may occur
• Potential interactions with drugs that affect liver enzymes (CYP450), which may alter plasma concentrations of bartemether

Precautions

• Monitor for signs of hypersensitivity reactions
• Use with caution in patients with a history of cardiac arrhythmias or pre-existing heart conditions
• Assess liver function prior to and during treatment

Pregnancy

Data on the use of bartemether in pregnancy is limited, thus it should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Limited data suggests that the use of bartemether is compatible with breastfeeding; however, it is recommended to monitor the infant for any adverse effects.

Storage

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

Formulations

• Oral tablets
• Combination with lumefantrine for enhanced efficacy against malaria

Indications

• Uncomplicated malaria due to Plasmodium falciparum
• Coartem (lumefantrine and artemether) for rapid malaria treatment

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, it is suggested that lumefantrine inhibits the formation of beta-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.

Pharmacodynamics

Lumefantrine is active against the erythrocytic stages of Plasmodium falciparum. When administered with artemether, it is believed to have cooperative antimalarial effects, with artemether providing rapid symptom relief and lumefantrine clearing residual parasites due to its longer half-life.

Pharmacokinetics

Lumefantrine has a long half-life, allowing for sustained effects after administration. It is absorbed from the gastrointestinal tract and is extensively metabolized in the liver. Its pharmacokinetic profile supports its use in combination therapy with rapidly acting agents like artemether.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Fatigue
• Dizziness
• Palpitations

Interactions

• Drug interactions with artemether; co-administration may enhance antimalarial effects
• Potential interactions with drugs that affect liver enzymes, which may alter lumefantrine metabolism

Precautions

• Use with caution in patients with a history of cardiac arrhythmias
• Monitor for signs of hepatotoxicity in patients with pre-existing liver disease
• Consider potential for drug interactions in patients receiving multiple medications

Pregnancy

Lumefantrine should only be used in pregnancy if clearly needed; consult guidelines for specific considerations.

Breast-feeding

Use with caution while breastfeeding; consult healthcare provider for recommendations.

Storage

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

Formulations

• Tablets
• Oral suspension

Mechanism of action

The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.

Pharmacodynamics

Lumefantrine is a blood schizonticide active against erythrocytic stages of <i>Plasmodium falciparum</i>. It is thought that administration of lumefantrine with artemether results in cooperate antimalarial clearing effects. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thus thought to provide rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.