ARTENAM 100MG/MLINJECTION

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