Mefloquine

Indications
 Oral
Malaria
Adult: 20-25 mg/kg as a single dose or preferably in 2 or 3 divided doses at 6-8 hrs interval. Max dose 1.5 g.
Child: 20-25 mg/kg taken in 2 divided doses.
Oral
Prophylaxis of malaria
Adult: 250 mg once wkly taken 1-3 wk before exposure and continuing for 4 wk after leaving the malarious area.
Child: <45 kg: 250 mg once wkly; 30-45 kg: 187.5 mg once wkly; 20-30 kg: 125 mg once wkly; 10-20 kg: 62.5 mg once wkly; 5-10 kg: 31.25 mg once wkly. Start prophylaxis 1-3 wk before exposure and continue for 4 wk after leaving malarious area.
Contraindications
 Treatment with quinine during the preceding 12 hr. Prophylaxis in patients with history of psychiatric illness, seizure, hepatic disorder. Co-admin with halofantrine due to increased risk of cardiac arrhythmias.
Warnings / Precautions
 Epilepsy; delay admin until at least 12 hr 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.
Adverse Reactions
 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.
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.
See Below for More mefloquine Drug Interactions
Mechanism of Actions
 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 wk
Administration
 Should be taken with food. (Best taken w/ meals & a full glass of water.)
ATC Classification
 P01BC02 - mefloquine ; Belongs to the class of methanolquinoline antimalarials.
Available As
  • Mefloquine 250 mg

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