No

Antimalarial Agent

Treatment of acute malarial infections and prevention of malaria

C

Hypersensitivity to any component

Caution is warranted with lactation; discontinue if unexplained neuropsychiatric disturbances occur, caution in epilepsy patients or in patients with significant cardiac disease. If mefloquine is to be used for a prolonged period, periodic evaluations including liver function tests and ophthalmic examinations should be performed. (Retinal abnormalities have not been observed with mefloquine in humans; however, it has with long-term administration to rats.) In cases of life-threatening, serious, or overwhelming malaria infections due to Plasmodium falciparum, patients should be treated with intravenous antimalarial drug. Mefloquine may be given orally to complete the course. Caution should be exercised with regard to driving, piloting airplanes, and operating machines since dizziness, disturbed sense of balance; neuropsychiatric reactions have been reported with mefloquine.

1% to 10%:

Central nervous system: Difficulty concentrating, headache, insomnia, lightheadedness, vertigo

Gastrointestinal: Vomiting (3%), diarrhea, stomach pain, nausea

Ocular: Visual disturbances

Otic: Tinnitus

<1%: Bradycardia, extrasystoles, syncope, anxiety, dizziness, confusion, seizures, hallucinations, mental depression, psychosis

Symptoms of overdose include vomiting, diarrhea; cardiotoxic

Following GI contamination supportive care only

Decreased effect of valproic acid

Increased toxicity of beta-blockers; chloroquine, quinine, and quinidine (hold treatment until at least 12 hours after these later drugs)

Mefloquine is a quinoline-methanol compound structurally similar to quinine; mefloquine's effectiveness in the treatment and prophylaxis of malaria is due to the destruction of the asexual blood forms of the malarial pathogens that affect humans, Plasmodium falciparum, P. vivax, P. malariae, P. ovale

Absorption: Oral: Well absorbed

Distribution: V_d: 19 L/kg; concentrates in erythrocytes; appears in breast milk; distributed to blood, urine, CSF, and tissues; concentrates in erythrocytes

Protein binding: 98%

Half-life: 21-22 days

Elimination: ~1.5% to 9% of dose excreted unchanged in urine

Oral:

15-19 kg: 1/4 tablet

20-30 kg: 1/2 tablet

31-45 kg: 3/4 tablet

>45 kg: 1 tablet

Administer weekly starting 1 week before travel, continuing weekly during travel and for 4 weeks after leaving endemic area

Adults:

Treatment of mild to moderate malaria infection: 5 tablets (1250 mg) as a single dose with at least 8 oz of water

Malaria prophylaxis: 1 tablet (250 mg) weekly starting 1 week before travel, continuing weekly during travel and for 4 weeks after leaving endemic area

LFTS; ocular examination

May cause dizziness, insomnia, or difficulty concentrating; may rarely cause anxiety, confusion, hallucination, or depression

Concurrent use with valproic acid may valproate blood levels; monitor levels

No information available to require special precautions

No effects or complications reported

Take on schedule as directed, with a full 8 oz glass of water. Ophthalmic exams will be necessary when used long-term. When taking for prophylaxis, begin 1 week before traveling to endemic areas, continue during travel period, and for 4 weeks following return. You may experience GI distress (frequent small meals may help). You may experience dizziness, changes in mentation, insomnia, headache, visual disturbances (use caution when driving or engaging in tasks that require alertness until response to drug is known). Pregnancy/breast-feeding precautions: Use reliable contraception during and for 2 months following treatment. Breast-feeding is not recommended.

Monitor LFTS; ocular examination

Tablet, as hydrochloride: 250 mg

Panisko DM and Keystone JS, "Treatment of Malaria - 1990," Drugs, 1990, 39(2):160-89.

White NJ, "The Treatment of Malaria," N Engl J Med, 1996, 335(11):800-6.

Wyler DJ, "Malaria Chemoprophylaxis for the Traveler," N Engl J Med, 1993, 329(1):31-7.