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Mefloquine information from DrugsUpdate  

See Available Brands of Mefloquine in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Mefloquine is an orally administered antimalarial drug used prophylactically against and as a treatment for malaria. It also goes by the trade name Lariam (manufactured by F. Hoffmann–La Roche) or Mefaquin and by the chemical name mefloquine hydrochloride (formulated with HCl). Mefloquine was developed in the 1970s at the Walter Reed Army Institute of Research in the U.S. as a synthetic analogue of quinine.

Pharmacodynamics

Pharmacokinetics

Mefloquine is a 4-methanolquinine antimalarial which acts as a blood schizontocide. It is active against most Plasmodium species and is used both as prophylaxis and treatment against malaria.

Absorption
Well absorbed from the GIT (oral).

Distribution
Widely distributed; small amount enters breast milk, crosses placenta. Protein-binding: 98%

Metabolism
Hepatic (small amounts).

Excretion
Urine (as unchanged drug and metabolites), faeces. Elimination half-life: 2-4 weeks.

Mefloquine Indications / Mefloquine Uses

Information Not Available

Mefloquine Adverse Reactions / Mefloquine Side Effects

Nausea, vomiting, abdominal pain, diarrhoea; dysphoria, dizziness; headache; sleep disorders; vertigo; neuropsychiatric reactions; bradycardia; visual/auditory disturbances; pruritus; sialorrhea, arthralgia and fatigue; syncope; extrasystole.

Potentially Fatal: Seizures, thrombocytopenia, leucopenia, AV block, encephalopathy.

Precautions

Information Not Available

Special Precautions

Epilepsy; delay admin until at least 12 hours after the last dose of quinine/quinine-related compounds (monitoring of cardiac and neurological functions is warranted). Avoid driving or operating machines during and up to 3 wk after mefloquine use. Pregnancy, lactation; cardiac conduction disturbances; children <3 mth or 5 kg.

Other Drug Interactions

Mefloquine may compromise adequate immunization by live typhoid vaccine. Increased risk of ventricular arrhythmias with amiodarone, atomoxetine, ivrabradine, moxifloxacin, pimozide. Increased risk of cardiac toxicity and/or convulsions when used with quinidine, quinine, chloroquine and hydroxychloroquine. May antagonise anticonvulsant effects of antiepileptics. Bradycardia may occur with digoxin, calcium channel blockers and β-blockers.

Potentially Fatal: Avoid concommitant use with halofantrine as potentially fatal cardiac arrythmias may occur.

Other Interactions

Information Not Available

Dosage

Oral
Malaria
Adult: 20-25 mg/kg as a single dose or preferably in 2 or 3 divided doses at 6-8 hours interval. Max dose 1.5 g.
Child: 20-25 mg/kg taken in 2 divided doses.

Oral
Prophylaxis of malaria
Adult: 250 mg once weekly taken 1-3 wk before exposure and continuing for 4 weeks after leaving the malarious area.
Child: <45 kg: 250 mg once weekly; 30-45 kg: 187.5 mg once weekly; 20-30 kg: 125 mg once wkly; 10-20 kg: 62.5 mg once weekly; 5-10 kg: 31.25 mg once weekly. Start prophylaxis 1-3 weeks before exposure and continue for 4 weeks after leaving malarious area.

Food(before/after)

Should be taken with food. (Best taken w/ meals & a full glass of water.)

List of Contraindications

Mefloquine and Pregnancy

Caution when used during pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Mefloquine and Lactation

Caution when used during lactation

Mefloquine and Children

Information Not Available

Mefloquine and Geriatic

Information Not Available

Mefloquine and Other Contraindications

Treatment with quinine during the preceding 12 hours. Prophylaxis in patients with history of psychiatric illness, seizure, hepatic disorder. Co-admin with halofantrine due to increased risk of cardiac arrhythmias.

Storage

Information Not Available

Lab interference

Information Not Available

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