MALAAT 20/120 TABLETS

Indications

• Uncomplicated Plasmodium falciparum malaria
• Treatment of malaria in combination with other antimalarial agents

Dosage

Children: Refer to BNF for Children for specific dosing recommendations.

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

Mechanism of action

Arthemeter exerts its antimalarial effects through the generation of free radicals when activated by iron in the parasite. These free radicals damage the parasite's cellular components, including proteins and lipids, leading to the death of the malaria organisms. The drug is particularly effective against the asexual forms of the Plasmodium species.

Pharmacodynamics

Arthemeter has a rapid onset of action, with its effects typically observed within a few hours of administration. The drug targets the intraerythrocytic stages of Plasmodium falciparum, disrupting the parasite's metabolism and growth. Its effectiveness is enhanced when used in combination with other antimalarial agents, reducing the likelihood of developing resistance and improving overall treatment outcomes.

Pharmacokinetics

Arthemeter is well absorbed after oral administration, with peak plasma concentrations occurring within 2 to 3 hours. It has a short half-life, necessitating multiple doses for sustained efficacy. The drug is extensively metabolized in the liver, primarily through oxidative pathways, with metabolites that also possess antimalarial activity. Excretion occurs mainly through the urine, with some elimination via feces.

Adverse effects

• Nausea
• Vomiting
• Headache
• Dizziness
• Fatigue
• Diarrhea
• Abdominal pain
• Anemia
• Hypersensitivity reactions

Interactions

• May interact with other antimalarial agents
• Potential interactions with drugs that affect liver enzymes

Precautions

• Use with caution in patients with liver impairment
• Monitor for signs of hypersensitivity
• Caution in patients with a history of seizures

Pregnancy

Amehtmer is classified as category C. The benefits may outweigh the risks in treating severe malaria.

Breast-feeding

It is not known whether artemether is excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablets
• Injectable formulations

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.