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Larimef

Mefloquine ·Healthcare Pharmaceuticals Ltd.·Tablet

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Administration

Adult:
  • 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.
In Children 6 Months and Older:
  • 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.
Geriatric Use: Experiences have not identified differences in responses between the elderly and younger patients.

Should be taken with food. Best taken with meals & a full glass of water.

Effects

Among subjects who received Mefloquine for prophylaxis of malaria, following side effects was observed:
  • The most frequently observed sied-effects were vomiting, dizziness, syncope, extrasystoles and other complaints affecting less than 1%. Among subjects who received Mefloquine for treatment, following side-effects was observed:
  • The most frequently observed side-effects included : dizziness, myalgia, nausea, fever, headache, vomiting, chills, diarrhoea, skin rash, abdominal pain fatigue, loss of appetite, and tinnitus

In cases of overdosage with Mefloquine, the symptoms may be more pronounced. The following procedure is recommended in case of overdosage:
  • Induce vomiting or perform gastric lavage, as appropriate.
  • Monitor cardiac function (if possible by ECG), neurologic and psychiatric status for at least 24 hours.
  • Provide Symptomatic and intensive supportive treatment as required, particularly of cardiovascular disturbance.
  • Treat vomiting or diarrhoea with standard fluid therapy.

Indications

Mefloquine is indicated in-
  • Acute Malaria Infections caused by Mefloquine-susceptible strains of Plasmodium falciparum (both chloroquine- susceptible and resistant strains) or by P. vivax
  • Prophylaxis of P. falciparum and P. vivax malaria infections

Pharmacology

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.

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.

Precautions

Warnings: Mefloquine may cause psychiatric symptoms in a number of patients, ranging from anxiety, paranoia, and depression to hallucinations and psychotic behavior. Rare cases of suicidal ideation and suicide have been reported though no relationship to drug administration has been confirmed. Mefloquine should be used with caution in patients with a previous history of depression. Concomitant administration of Mefloquine and quinine or quinidine may produce electrocardiographic abnormalities and may increase risk of convulsions.

Precautions: In patients with epilepsy, Mefloquine may increase the risk of convulsions. Caution should be exercised with regard to activities requiring alertness and fine motor coordination such as driving, piloting aircraft and operating machinery. Mefloquine should be used with caution in patients with psychiatric disturbances. In patients with impaired liver function the elimination of Mefloquine may be prolonged, leading to higher plasma levels.

Therapeutic

Anti-malarial drugs

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