Larimef Tablet

Larimef Tablet 250 mg is an antimalarial drug used for the prevention and treatment of malaria caused by Plasmodium falciparum and Plasmodium vivax. It interferes with parasite survival within red blood cells, helping eliminate the infection. Larimef Tablet 250 mg is effective for both malaria prophylaxis and treatment but is associated with a risk of serious neuropsychiatric adverse effects, including anxiety, depression, hallucinations, and seizures in susceptible individuals, requiring careful patient selection and monitoring.

Larimef Tablet 250 mg is an antimalarial agent used in the prophylaxis and treatment of malaria caused by Plasmodium falciparum and Plasmodium vivax.

Larimef Tablet 250 mg is indicated for the treatment of mild to moderate cases of malaria caused by Plasmodium falciparum and Plasmodium vivax. It is effective against chloroquine-resistant forms of Plasmodium falciparum. Larimef Tablet 250 mg is also indicated for the prophylaxis of malaria caused by Plasmodium falciparum and Plasmodium vivax, including chloroquine-resistant forms of Plasmodium falciparum.

• Malaria caused by Plasmodium falciparum
• Malaria caused by plasmodium vivax

Sporozoites located in the salivary glands of mosquitoes infected with malaria parasites are introduced into the bloodstream of a human host during mosquito feeding. These sporozoites rapidly invade the liver, where they mature into liver-stage schizonts, rupturing and releasing 2,000 - 40,000 merozoites that invade red blood cells. Larimef Tablet 250 mg is an antimalarial drug acting as a blood schizonticide, preventing and treating malaria.

The mechanism of action of mefloquine is not completely understood. Some studies suggest that mefloquine specifically targets the 80S ribosome of the Plasmodium falciparum, inhibiting protein synthesis and causing subsequent schizonticidal effects. There are other studies in the literature with limited in vitro data on mefloquine's mechanism of action.

Larimef Tablet 250 mg is readily absorbed from the gastrointestinal tract; food significantly increases absorption and increases bioavailability by 40%. The bioavailability of tablets compared with the oral solution preparation of mefloquine is over 85%. Cmax is achieved in 6 to 24 hours in healthy volunteers after a single dose. Average blood concentrations range between 50 to 110 ng/ml/mg/kg. A weekly dose of 250 mg leads to steady-state plasma concentrations of 1000 to 2000 μg/L, after 7 to 10 weeks of administration.

The apparent volume of distribution is in healthy adults is about 20 L/kg with wide tissue distribution. Various estimates of the total apparent volume of distribution range from 13.3 to 40.9L/kg. Larimef Tablet 250 mg can accumulate in erythrocytes that have been infected with malaria parasites.

The binding of mefloquine to plasma proteins is over 98%.

Larimef Tablet 250 mg is believed to be excreted in the bile and feces. In healthy volunteers who have achieved steady-state concentrations of mefloquine, the unchanged drug was excreted at 9% of the ingested dose, and excretion of its carboxylic metabolite under was measured at 4% of the ingested dose. Concentrations of other metabolites could not be determined.

The terminal elimination half-life of mefloquine ranges from 0.9 - 13.8 days, according to one pharmacokinetic review. In various studies of healthy adults, the mean elimination half-life of mefloquine varied between 2 and 4 weeks, with a mean half-life of approximately 21 days.

The systemic clearance of mefloquine ranges from 0.022 to 0.073 L/h/kg, with an increased clearance during pregnancy. Prescribing information mentions a clearance rate of 30 mL/min.

The oral TDLO of mefloquine in humans is 11 mg/kg/2W (intermittent) and 880 mg/kg in the rat. Intraperitoneal LD50 in the rat is 130 mg/kg. Symptoms of an overdose with mefloquine may manifest as a worsening of adverse effects. In the case of an overdose, symptomatic and supportive care should be provided. There is no known antidote for an overdose with mefloquine. Monitor cardiac function by ECG, follow neuropsychiatric status for at least 24 hours, and provide treatment as required.

• Avoid alcohol.
• Take with a full glass of water.
• Take with food. The presence of food significantly enhances the rate and extent of absorption, leading to about a 40% increase in bioavailability.

• Malaria prevention: 1 tablet (250 mg) once per week starting 1-2 weeks before departure and continued for 4 weeks after leaving malarious area.
• Malaria treatment: 5 tablets (5X250 mg) in a single dose (up to max. 1.5 gm) or preferably in 2 divided doses 6 to 8 hours apart.

• Malaria prevention: Approximately 5 mg/kg body weight once per week (250 mg for children weighing over 45 kg, decreasing in proportion to body weight for children weighing 45 kg or less).
• Malaria treatment: 20 to 25 mg/kg body weight which may be split into two doses 6 to 8 hours apart to reduce the occurrence or severity of adverse reactions.