ARTIBASE FORTE TABLETS (Each tablet contains Arthemeter 80mg/ Lumefantrine 480mg

Indications

• Uncomplicated Plasmodium falciparum malaria
• Combination therapy for malaria

Dosage

Children: Refer to the BNF for Children for appropriate dosing information based on the child's weight and age.

Adults: Refer to the BNF for specific dosing information based on the severity of the infection and patient factors.

Mechanism of action

Artemether acts by producing free radicals through the cleavage of the endoperoxide bridge in the artemisinin structure. These free radicals damage the parasite's cellular components, leading to its death. The exact molecular pathways are not completely understood, but it is thought to interfere with the parasite's protein synthesis and disrupt its metabolism.

Pharmacodynamics

Artemether exhibits a rapid onset of action against the malaria parasites. It targets the asexual forms of Plasmodium species, particularly Plasmodium falciparum. The drug is known for its fast-acting properties, often leading to a reduction in fever and improvement in symptoms within hours of administration.

Pharmacokinetics

Artemether is well absorbed after oral administration, with peak plasma concentrations occurring approximately 2 hours after dosing. It undergoes extensive metabolism in the liver, primarily via cytochrome P450 enzymes. The half-life of artemether is about 2-3 hours, while its active metabolite, dihydroartemisinin, has a half-life of about 1-3 hours. It is excreted mainly in feces, with minimal renal excretion.

Contra-indications

• Hypersensitivity to artemether or any of its components
• Severe hepatic impairment

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Anorexia
• Dizziness
• Headache
• Fatigue
• Palpitations
• Hypersensitivity reactions

Interactions

• Caution is advised when co-administering with drugs that prolong the QT interval
• May enhance the effects of anticoagulants

Precautions

• Use with caution in patients with a history of epilepsy or other seizure disorders
• Monitor liver function in patients with pre-existing liver conditions

Pregnancy

Artemether should only be used in pregnancy if the benefits outweigh the risks. It is generally not recommended during the first trimester.

Breast-feeding

Artemether is excreted in breast milk. Use with caution and consider alternative treatments if necessary.

Storage

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

Formulations

• Oral tablets
• 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.