| Indication |
For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum. |
| Pharmacodynamics |
Mefloquine is an antimalarial agent which acts as a blood
schizonticide. Mefloquine is active against the erythrocytic stages of
Plasmodium species. However, the drug has no effect against the
exoerythrocytic (hepatic) stages of the parasite. Mefloquine is
effective against malaria parasites resistant to chloroquine. Mefloquine
is a chiral molecule. According to some research, the (+) enantiomer is
more effective in treating malaria, and the (-) enantiomer specifically
binds to adenosine receptors in the central nervous system, which may
explain some of its psychotropic effects. |
| Mechanism of action |
Mefloquine has been found to produce swelling of the Plasmodium falciparum
food vacuoles. It may act by forming toxic complexes with free heme
that damage membranes and interact with other plasmodial components. |
| Absorption |
Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption. |
| Volume of distribution |
|
| Protein binding |
98% |
| Metabolism |
Hepatic. Two metabolites have been identified in humans. The
main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is
inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities. |
| Route of elimination |
There is evidence that mefloquine is excreted mainly in the bile
and feces. Urinary excretion of unchanged mefloquine and its main
metabolite under steady-state condition accounted for about 9% and 4% of
the dose, respectively. |
| Half life |
2 to 4 weeks |
| Clearance |
|
| Toxicity |
Oral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss. |
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