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Mefloquine: Uses, Dosage & Side Effects

Mefloquine is a medication used to prevent and treat malaria. It is especially recommended for travel to regions with chloroquine-resistant malaria parasites.

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Things worth knowing about "Mefloquine"

Mefloquine is a medication used to prevent and treat malaria. It is especially recommended for travel to regions with chloroquine-resistant malaria parasites.

What is Mefloquine?

Mefloquine is an antimalarial drug belonging to the quinoline derivative class. It is used for both prophylaxis (prevention) and treatment of malaria, particularly infections caused by Plasmodium falciparum, the parasite responsible for the most dangerous form of malaria. It is especially important for travelers visiting tropical regions where malaria parasites have developed resistance to other antimalarials such as chloroquine.

Mechanism of Action

Mefloquine acts against the blood-stage schizonts of the malaria parasite. It interferes with the parasite's digestive processes inside red blood cells by inhibiting the polymerization of haem, a toxic byproduct of the parasite's metabolism. This causes haem to accumulate within the parasite, ultimately leading to its death. However, the exact molecular mechanism has not yet been fully elucidated.

Indications

Malaria prophylaxis: Prevention of malaria in travelers to endemic regions, particularly in parts of Africa, Asia, and South America
Malaria treatment: Treatment of uncomplicated malaria caused by Plasmodium falciparum or Plasmodium vivax
Used in cases of chloroquine-resistant malaria strains

Dosage and Administration

Mefloquine is taken orally in tablet form. For prophylaxis, the standard adult dose is one tablet (250 mg) taken once weekly, starting one to three weeks before entering a malaria-risk area and continuing for four weeks after leaving. Dosing in children is based on body weight. The medication should always be taken with food and a full glass of water to improve gastrointestinal tolerability.

Side Effects

Mefloquine is known for its potential neuropsychiatric side effects, which can range from mild to severe and may affect a proportion of users:

Sleep disturbances, vivid dreams, nightmares
Dizziness, headache
Nausea, vomiting, diarrhea
Anxiety, depression, confusion
In rare cases: hallucinations, psychotic episodes, seizures

Because of these possible neuropsychiatric effects, it is recommended to start taking mefloquine well before departure so that any adverse reactions can be identified and managed in time.

Contraindications and Warnings

Mefloquine must not be used in individuals with:

Known hypersensitivity to mefloquine or related compounds (e.g., quinine)
A history of psychiatric disorders (e.g., depression, anxiety disorders, schizophrenia)
Seizure disorders (epilepsy)
Serious cardiac arrhythmias

During pregnancy, especially in the first trimester, mefloquine should only be used if clearly necessary and after consultation with a physician. Breastfeeding women are advised to discontinue breastfeeding during treatment.

Drug Interactions

Mefloquine may interact with several other medications. Special caution is advised when used simultaneously with:

Other antimalarials (e.g., quinine, chloroquine) – increased risk of cardiac arrhythmias
Antiepileptic drugs – possible reduction in efficacy
Beta-blockers and other cardioactive substances
Live oral typhoid vaccine – mefloquine may reduce the effectiveness of the vaccine

References

World Health Organization (WHO): International Travel and Health, Chapter on Malaria, WHO Press, Geneva, current edition.
Centers for Disease Control and Prevention (CDC): Malaria – Mefloquine (Lariam). Available at: www.cdc.gov/malaria (accessed 2023).
Schlagenhauf P et al.: Mefloquine tolerability during chemoprophylaxis. BMJ, 1996; 312: 1259–1263.

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