Overview
| Generic Names: | Mefloquine HCL; Mefloquine aziridine; Mefloquinone |
|---|---|
| Trade Names: | Lariam |
| PharmGKB Accession Id: | PA450348 |
Description
A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. PubChem (source: Drug Bank)
Indication
For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of <i>Plasmodium falciparum</i> (both chloroquine-susceptible and resistant strains) or by <i>Plasmodium vivax</i>. Also for the prophylaxis of <i>Plasmodium falciparum</i> and <i>Plasmodium vivax</i> malaria infections, including prophylaxis of chloroquine-resistant strains of <i>Plasmodium falciparum</i>. (source: Drug Bank)
ATC Therapeutic Category
- P01BC:Methanolquinolines
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Mefloquine has been found to produce swelling of the <i>Plasmodium falciparum</i> food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components. (source: Drug Bank)
Pharmacology
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. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take with a full glass of water.
Take with food.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against <i>Plasmodium falciparum</i>. The second metabolite, an alcohol, is present in minute quantities. (source: Drug Bank)
Protein Binding
98% (source: Drug Bank)
Absorption
Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption. (source: Drug Bank)
Toxicity
Oral, rat: LD<sub>50</sub> = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss. (source: Drug Bank)
Isomeric SMILES Code:
c1cc2c(cc(nc2c(c1)C(F)(F)F)C(F)(F)F)C(C3CCCCN3)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ABCB1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| HBA1 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
Mefloquine can increase the anticoagulant effect (source: Drug Bank) |
| dicumarol |
|
Mefloquine can increase the anticoagulant effect (source: Drug Bank) |
| halofantrine |
|
Increased risk of cardiac toxicity (source: Drug Bank) |
| rifampin |
|
Rifampin lowers mefloquine levels (source: Drug Bank) |
| ritonavir |
|
Mefloquine decreases the effect of ritonavir (source: Drug Bank) |
| warfarin |
|
Mefloquine can increase the anticoagulant effect (source: Drug Bank) |
| ziprasidone |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
Drug Toxicity |
|
Publications |
|
|
Induced psychotic disorder |
|
Publications |
|
|
Malaria |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.