INJ. RTITAS-100MG

Indications

• Uncomplicated Plasmodium falciparum malaria
• Malaria in cases of drug-resistant strains

Dosage

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

Adults: Refer to BNF for specific dosing recommendations.

Mechanism of action

Artemether exerts its antimalarial effects by generating reactive oxygen species and free radicals upon interaction with heme, a component of hemoglobin, in the malaria parasite. These reactive species damage the parasite's proteins and membranes, leading to cell death. The drug is particularly effective during the asexual blood stage of the parasite's lifecycle.

Pharmacodynamics

The pharmacodynamic profile of artemether indicates that it has a rapid onset of action, with significant reductions in parasitemia observed within hours of administration. Its effectiveness is enhanced when used in combination with other antimalarials, which can target different stages of the parasite's lifecycle. Resistance development has been less common with artemisinin derivatives compared to older antimalarial drugs.

Pharmacokinetics

Artemether is rapidly absorbed after oral administration and has a high bioavailability. It is extensively metabolized in the liver to dihydroartemisinin, which is the active metabolite that contributes to its therapeutic effects. The elimination half-life of artemether is relatively short, necessitating the use of combination therapies to prolong its antimalarial action. The drug is primarily excreted via the bile and urine.

Contra-indications

• Hypersensitivity to artemether or any of the excipients
• Severe hepatic impairment
• History of severe allergic reactions

Adverse effects

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

Interactions

• Co-administration with other antimalarial agents, particularly those that prolong the QT interval, may increase the risk of cardiac side effects
• Potential interaction with CYP450 enzyme inducers or inhibitors, which may alter drug metabolism

Precautions

• Monitor for signs of hypersensitivity reactions
• Use with caution in patients with a history of cardiovascular disease
• Assessment of liver function is recommended prior to use
• Caution in patients with malaria caused by Plasmodium falciparum as resistance may occur

Pregnancy

Artemether is classified as category C. It should be used during pregnancy only 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 at room temperature, away from moisture and direct sunlight. Keep out of reach of children.

Formulations

• Oral tablets
• Injectable solution