ARTEFAN 1X24 20/120MG TABLETS

Indications

• Uncomplicated Plasmodium falciparum malaria
• Malaria caused by other Plasmodium species in specific cases

Dosage

Children: Refer to BNF for Children for appropriate dosing guidelines in pediatric populations.

Adults: Refer to local guidelines or BNF for specific dosing recommendations, as dosages may vary based on the context of use and combination therapies.

Mechanism of action

Artemether exerts its antimalarial effects through the formation of reactive oxygen species when it interacts with heme released from the digestion of hemoglobin by the malaria parasite. This process leads to oxidative stress and damage to the parasite's membranes and proteins, ultimately causing parasite death. The drug is particularly effective against the asexual blood stages of the malaria parasite.

Pharmacodynamics

The pharmacodynamic profile of artemether includes rapid elimination of the malaria parasite from the bloodstream, resulting in a significant reduction in parasite burden and clinical symptoms. Artemether is often administered with a partner drug to enhance therapeutic efficacy and ensure complete eradication of the parasite.

Pharmacokinetics

Artemether is rapidly absorbed after oral administration, with peak plasma concentrations typically reached within 2 hours. It has a high volume of distribution and is extensively metabolized in the liver, primarily by cytochrome P450 enzymes. The elimination half-life of artemether is approximately 2 to 3 hours, and it is excreted mainly in the form of metabolites through urine and feces.

Contra-indications

• Hypersensitivity to artemether or any component of the formulation
• Severe hepatic impairment

Adverse effects

• Nausea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Anemia
• Rash
• Cough
• Palpitations
• Abdominal pain

Interactions

• Concomitant use with drugs that prolong the QT interval may increase the risk of arrhythmias
• Potential interactions with antiretroviral medications
• May affect the metabolism of other drugs metabolized by CYP450 enzymes

Precautions

• Use with caution in patients with a history of arrhythmias
• Monitor liver function in patients with existing liver disease
• Be cautious in patients with known allergies to other antimalarials
• Not recommended for use in patients with severe malaria

Pregnancy

Artemether is classified as category C. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Artemether is excreted in breast milk. Caution should be exercised when administered to breastfeeding women.

Storage

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

Formulations

• Oral tablets
• Intramuscular injection
• Suspension for oral administration

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.