Mefloquine
- Atc Codes:P01BC02
- CAS Codes:53230-10-7#51773-92-3
- PHARMGKB ID:53230-10-7#51773-92-3
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Lariam; Belgium: Lariam; Cyprus: Eloquine, Lariam; Czech Republic: Lariam; Denmark: Lariam; Estonia: Lariam; Finland: Lariam; France: Lariam; Germany: Lariam; Greece: Lariam; Hungary: Lariam; Ireland: Lariam; Italy: Lariam; Latvia: Mephaquin; Lithuania: Mephaquin; Luxembourg: Lariam; Malta: Lariam, Mephaquin; Netherlands: Lariam; Portugal: Mephaquin; Romania: Eloquine; Slovakia: Lariam; Sweden: Lariam; UK: Lariam.
North America
Canada: Lariam, Mefloquine; USA: Mefloquine.
Latin America
Argentina: Tropicur; Brazil: Mephaquin.
Asia
Japan: Mephaquin.
Drug combinations
Mefloquine and Artesunate
Chemistry
Mefloquine: C~17~H~16~F~6~N~2~O. Mw: 378.31. (1) 4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-, (R*,S*)-(±)-; (2)(D,L-erythro-α-2-Piperidyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol. CAS-53230-10-7 (1975).
Mefloquine Hydrochloride: C~17~H~16~F~6~N~2~O HCl. Mw: 414.77. 4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-, monohydrochloride, (R*,S*) – (±)-. CAS-51773-92-3 (1984).
Pharmacologic Category
Antiprotozoals; Antimalarials. (ATC-Code: P01BC02).
Mechanism of action
Effectiveness of mefloquine in treatment and prophylaxis of malaria is due to destruction of asexual blood forms of malarial pathogens which affect humans, Plasmodium falciparum, P. vivax, P. malariae, P. ovale.
Therapeutic use
Treatment of acute malarial infections and prevention of malaria.
Pregnancy and lactiation implications
Mefloquine crosses placenta and is teratogenic in animals. Use with caution if traveling to endemic areas during pregnancy. Use not recommended while breast-feeding.
Unlabeled use
Contraindications
Hypersensitivity to mefloquine, related compounds (e.g. quinine and quinidine), or any component of the formulation. Prophylactic use in history of seizures or severe psychiatric disorder (including active or recent history of depression, generalized anxiety disorder, psychosis, or schizophrenia).
Warnings and precautions
CNS effects (dizziness, loss of balance, and other CNS disorders) reported. Possible psychiatric effects (anxiety, depression, hallucinations, paranoia and psychosis). Suicidal ideation and suicide reported rarely (no causal relationship established). Prophylactic use contraindicated in active or recent history of psychiatric disorders. Use with caution in significant cardiac disease (ECG changes). Use with caution in hepatic impairment (elimination might be prolonged). 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. Increased risk of seizures. Prophylactic use contraindicated in seizure disorder. Concurrent use with chloroquine may increase risk of seizures. Concurrent use with quinidine and quinine might increase risk of ECG abnormalities and seizures. Retinal abnormalities observed in rats (with long-term administration).