II. Indications

  1. Prophylaxis or Treatment of Malaria
  2. Preferred prophylaxis agent in Chloroquine resistance areas
  3. Less commonly used for Malaria treatment

III. Contraindications

  1. History of Epilepsy (Seizure Disorder)
  2. History of psychiatric disorder
  3. Concomitant Beta Blocker use
  4. First Trimester Pregnancy
    1. May be used in second or third trimester pregnancy
  5. Children under age 3 months

IV. Pharmacokinetics

  1. Half-Life: 33 days
  2. Steady state reached
    1. Weekly dose: 7 weeks
    2. Loading dose: 4 days

V. Adverse Effects

  1. Vestibular toxicity
    1. Risk of longterm Vertigo and Tinnitus
  2. Arrhythmia in patients with cardiac conduction defect
    1. QT Prolongation
    2. Bradycardia
  3. Neuropsychological effects (uncommon 1:200 to 1:500, but is a FDA black box warning)
    1. Insomnia
    2. Nightmares
    3. Anxiety
    4. Irritability
    5. Major Depression
      1. Possible increased Suicidality
    6. Psychosis (paranoia, Hallucinations) or Seizures (rare)
      1. Prophylaxis Incidence: <1:10,000
      2. Treatment Incidence: 1:100 to 1:1500
  4. Pregnancy
    1. No significant adverse fetal affects in studies

VI. Directions

  1. Take with food and full glass of water

VII. Dosing: Malaria Prophylaxis

  1. Protocol
    1. Start dosing 1 week before exposure
    2. Complete dosing 4 weeks after exposure
  2. Adult
    1. Mefloquine 250 mg salt (228 mg base) orally once weekly
  3. Child
    1. Weight <9 kg
      1. Dose: 5 mg/kg salt (4.6 mg/kg base) orally once weekly
    2. Weight 9 to 19 kg
      1. Mefloquine 1/4 of adult tablet orally once per week
    3. Weight: 20 to 30 kg
      1. Mefloquine 1/2 of adult tablet orally once per week
    4. Weight: 31 to 45 kg
      1. Mefloquine 3/4 of adult tablet orally once per week
    5. Weight: >45 kg
      1. Mefloquine 1 adult tablet (250 mg) orally once per week

VIII. Dosing: Malaria Treatment

  1. Adult: 750 mg salt (684 mg base) for first dose, then second dose of 500 mg salt (456 mg base) in 6 to 12 hours
  2. Child: 15 mg/kg salt (13.7 mg/kg base) for first dose, then second dose of 10 mg/kg salt (9.1 mg/kg base) in 6 to 12 hours

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Related Studies

Cost: Medications

mefloquine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
MEFLOQUINE HCL 250 MG TABLET Generic $4.87 each

Ontology: Mefloquine (C0025153)

Definition (NCI) A quinolinemethanol derivative with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the exact mechanism remains to be elucidated, mefloquine, a weak base, preferentially accumulates in lysosomes and disrupts lysosomal function and integrity, thereby leading to host cell death. Similar to chloroquine, the chemosensitizing and radiosensitizing activities of this agent may be related to its inhibition of autophagocytosis, a cellular mechanism involving lysosomal degradation that minimizes the production of reactive oxygen species (ROS) related to tumor reoxygenation and tumor exposure to chemotherapeutic agents and radiation. Compared to chloroquine, mefloquine has better blood-brain-barrier (BBB) penetration.
Definition (MSH) A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015767
SnomedCT 387505001, 87567009
LNC LP21305-5, MTHU013611
English Mefloquine, Mephloquine, 4-Quinolinemethanol, alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-, (R*,S*)-(+-)-, mefloquine (medication), Mefloquine [Chemical/Ingredient], mephloquine, mefloquine, MEFLOQUINE, Mefloquine product, Mefloquine (product), Mefloquine (substance)
Swedish Meflokin
Czech meflochin
Finnish Meflokiini
Japanese メフロキン
Polish Meflochina
Spanish mefloquina (producto), mefloquina (sustancia), mefloquina, Mefloquina
French Méfloquine
German Mefloquin
Italian Meflochina
Portuguese Mefloquina

Ontology: Lariam (C0699989)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015767
English lariam, Lariam, Hoffmann La Roche Brand of Mefloquine Hydrochloride, Hoffmann-La Roche Brand of Mefloquine Hydrochloride, Roche Brand of Mefloquine Hydrochloride