II. Indications
- Prophylaxis or Treatment of Malaria
- Preferred Malaria Prophylaxis agent in Chloroquine resistance areas (esp. longterm travel >6 months)
- Less commonly used for Malaria treatment
III. Contraindications
- Mefloquine resistant Malaria regions (some regions within southeast asia)
- History of Epilepsy (Seizure Disorder)
- History of major psychiatric disorder
- Cardiac conduction abnormalities (esp. QTc Prolongation)
- Concomitant Beta Blocker use
- First Trimester Pregnancy
- May be used in second or third trimester pregnancy
- Children under age 3 months
IV. Mechanism
- Structural analog of Quinine
V. Medications
- Mefloquine Tablets: 250 mg
- Take with food and full 8 oz glass of water
- Tablets may be crushed and mixed with a small amount of water, milk or other liquids
VI. Dosing: Malaria Prophylaxis
- Protocol
- Start dosing 1 week before exposure
- Complete dosing 4 weeks after exposure
- Adult
- Mefloquine 250 mg salt (228 mg base) orally once weekly
- Child
- Weight <9 kg
- Mefloquine 5 mg/kg salt (4.6 mg/kg base) orally once weekly
- Weight 9 to 19 kg
- Mefloquine 1/4 of adult tablet orally once per week
- Weight: 20 to 30 kg
- Mefloquine 1/2 of adult tablet orally once per week
- Weight: 31 to 45 kg
- Mefloquine 3/4 of adult tablet orally once per week
- Weight: >45 kg
- Mefloquine 1 adult tablet (250 mg) orally once per week
- Weight <9 kg
VII. Dosing: Malaria Treatment (CDC Guidelines)
- Adult
- Dose 1: Mefloquine 750 mg salt (684 mg base)
- Dose 2: Mefloquine 500 mg salt (456 mg base) in 8 to 12 hours after first dose
- Child
- Dose 1: Mefloquine 15 mg/kg salt (13.7 mg/kg base)
- Dose 2: Mefloquine 10 mg/kg salt (9.1 mg/kg base) in 8 to 12 hours after first dose
VIII. Pharmacokinetics
- Half-Life: 33 days
- Steady state reached
- Weekly dose: 7 weeks
- Loading dose: 4 days
IX. Adverse Effects
- Vestibular toxicity
- Arrhythmia in patients with cardiac conduction defect
- Neuropsychological effects (uncommon 1:200 to 1:500, but is a FDA black box warning)
- Insomnia
- Nightmares
- Anxiety
- Irritability
- Drowsiness
- Dizziness
- Tinnitus
- Major Depression
- Possible increased Suicidality
- Psychosis (paranoia, Hallucinations) or Seizures (rare)
X. Safety
- Considered safe in Lactation
- However, infant is not protected from Malaria by Breast Feeding (minimal medication in Breast Milk)
- Pregnancy Category B
- No significant adverse fetal affects in studies (any trimester)
XI. Drug Interactions
- Avoid Mefloquine for at least 12 hours after last dose of the following
- Agents to avoid overall with Mefloquine
- Agents that decrease Mefloquine levels
- Agents that are decreased by Mefloquine
XII. References
- (2013) Presc Lett 20(9)
- (2019) Drugs for Malaria Prophylaxis, Med Lett Drugs Ther, p. e104-5
- (2023) Presc Lett, Malaria Prophylaxis, Resource #350806
- Boudreau (1993) Trop Med Parasitol 44(3):257-65 [PubMed]
- Vanhauwere (1998) Am J Trop Med Hyg 58:17-21 [PubMed]
- Weimeke (1991) Am J Trop Med Hyg 45:86-9 [PubMed]
- Shahbodaghi (2022) Am Fam Physician 106(3): 270-8 [PubMed]
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Related Studies
mefloquine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
MEFLOQUINE HCL 250 MG TABLET | Generic | $3.99 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 |
Russian | MEFLOKHIN, МЕФЛОХИН |
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 |