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Mefloquine
- indication:For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of <i>Plasmodium falciparum</i> (both chloroquine-susceptible and resistant strains) or by <i>Plasmodium vivax</i>. Also for the prophylaxis of <i>Plasmodium falciparum</i> and <i>Plasmodium vivax</i> malaria infections, including prophylaxis of chloroquine-resistant strains of <i>Plasmodium falciparum</i>.
- pharmacologypharmacology:
- mechanism: Mefloquine has been found to produce swelling of the <i>Plasmodium falciparum</i> food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
- toxicity: Oral, rat: LD<sub>50</sub> = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.
- absorprion: Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
- halflife: 2 to 4 weeks
- roouteelimination: 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.
- volumedistribution: * 20 L/kg [healthy adults]
- clearance: * 30 mL/min