Chemical formula: C₁₇H₁₆F₆N₂O Molecular mass: 378.312 g/mol PubChem compound: 4046
Mefloquine acts on and destroys the asexual intraerythocytic forms of the human malaria parasites: Plasmodium falciparum, P. vivax. P. malariae and P. ovale. It is effective in the treatment and prophylaxis of malaria.
Mefloquine is also effective against malarial parasites resistant to other antimalarials such as chloroquine and other 4-aminoquinoline derivatives, proguanil, pyrimethamine and pyrimethamine-sulphonamide combinations.
The maximum plasma concentration is reached within 6 to 24 hours after a single oral dose of mefloquine. The level in micrograms per litre is roughly equivalent to the dose in milligrams (for example approximately 1000 μg/l after a single dose of 1000 mg). The presence of food significantly enhances the rate and extent of absorption.
At a dose of 250 mg once weekly, maximum steady state plasma concentrations of 1000–2000 μg/l are reached after 7-10 weeks. The RBC concentration is almost twice as high as the plasma level. Plasma protein binding is about 98%. Clinical experience suggests a minimal suppressive plasma concentration of mefloquine in the order of 600 μg/l.
Mefloquine is extensively metabolised in the liver by the cytochrome P450 system. In vitro and in vivo studies strongly suggest that CYP3A4 is the major isoform involved.
The average half-life of mefloquine in Europeans is 21 days. There is evidence that mefloquine is excreted mainly in the bile and faeces. In volunteers, urinary excretion of unchanged mefloquine and its main metabolite accounted for about 9% and 4% of the dose, respectively.
The pharmacokinetics of mefloquine may be altered in acute malaria. Pharmacokinetic differences have been observed between various ethnic populations. In practice however, these are of minor importance compared with the host immune status and sensitivity of the parasite.
Mefloquine crosses the placenta. Excretion into breast milk appears to be minimal.
Mefloquine crosses the placenta and is teratogenic when administered to rats and mice in early gestation.
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