Artesunate/ Mefloquine

• Fixed-dose combinations vary by manufacturer. Common formulations include:
• Artesunate 100 mg + Mefloquine 220 mg
• Artesunate 200 mg + Mefloquine 440 mg
• Tablets should be taken according to body weight and local guidelines.

• Take with food to improve mefloquine absorption and reduce GI upset.
• Complete the full 3-day course, even if symptoms resolve early.
• If vomiting occurs within 1 hour of dose, repeat the dose.
• Do not use for prophylaxis due to artesunate’s short half-life.

Mechanism of Action:

• Artesunate: Rapidly acting artemisinin derivative that generates free radicals inside parasitized erythrocytes, killing the parasite.
• Mefloquine: Inhibits heme polymerization in the parasite’s food vacuole, causing toxic heme accumulation.

Pharmacokinetics:

• Artesunate: Short half-life (~1 hr), rapid onset.
• Mefloquine: Long half-life (~2–4 weeks), provides long-lasting protection after treatment.

Common:

• Dizziness
• Nausea, vomiting
• Insomnia
• Headache
• Anorexia
• Abdominal pain
• Serious (mainly due to Mefloquine):
• Neuropsychiatric effects: anxiety, depression, hallucinations, psychosis

Seizures (rare)

• QT prolongation (rare, mainly with high doses)

• History of seizures or major neuropsychiatric disorders (especially with mefloquine)
• Known hypersensitivity to either drug

• Other QT-prolonging drugs: Increased risk of arrhythmia.
• Antidepressants/antipsychotics: May enhance CNS side effects.
• Beta-blockers and calcium channel blockers: Monitor cardiac function if co-administered.
• Anticonvulsants: May interact with mefloquine metabolism.