LUMITER DT 20/120MG TABLET

Indications

• Uncomplicated Plasmodium falciparum malaria
• Malaria prophylaxis in endemic areas

Dosage

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

Adults: Refer to clinical guidelines or the BNF for specific dosing information.

Mechanism of action

Artemether exerts its antimalarial effects through the generation of reactive oxygen species (ROS) and free radicals after the activation of its endoperoxide bridge by heme, which is released during the digestion of hemoglobin by the malaria parasite. This leads to damage to the parasite's cellular components, ultimately resulting in cell death.

Pharmacodynamics

Artemether is effective against asexual stages of malaria parasites, particularly Plasmodium falciparum. The drug acts rapidly, typically producing a quick reduction in parasitemia. Its action is enhanced when used in combination with other antimalarial agents, leading to improved treatment outcomes.

Pharmacokinetics

Artemether is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 2 to 3 hours. It has a high volume of distribution and is extensively distributed into tissues, including the liver and lungs. The drug undergoes hepatic metabolism, primarily via CYP3A4, to form its active metabolite, dihydroartemisinin. The elimination half-life of artemether is approximately 2 to 3 hours, and it is primarily excreted in the urine as metabolites.

Adverse effects

• Nausea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Hypotension
• Tachycardia
• Allergic reactions

Interactions

• CYP3A4 inhibitors may increase artemether levels
• CYP3A4 inducers may decrease artemether levels
• Concomitant use with other antimalarials should be approached with caution

Precautions

• Use with caution in patients with a history of hypersensitivity to artemisinins
• Monitor for signs of neurological toxicity in high doses
• Assess for potential drug interactions if the patient is on multiple medications

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 administering to nursing mothers.

Storage

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

Formulations

• Oral tablet
• Injectable solution

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.