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QuickView for Mefloquine (compound)


PubChem
Name: Mefloquine
PubChem Compound ID: 3000506
Description: A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
Molecular formula: C17H16F6N2O
Molecular weight: 378.312 g/mol
Synonyms:
RTI1172-1-1; (+/-)-threo-4-Quinolinemethanol, .alpha.-2-piperidinyl-2,8-bis(trifluoromethyl)-; AIDS055324; AIDS007692; (+)-threo-4-Quinolinemethanol, .alpha.-2-piperidinyl-2,8-bis(trifluoromethyl)-; RTI1173-1-1; AIDS-055324; (+)-Threo-Mefloquine; AIDS-007692
DrugBank
Identification
Name: Mefloquine
Name (isomeric): DB00358
Drug Type: small molecule
Description: A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
Synonyms:
Mefloquinone; Mefloquine HCL
Brand: Lariam
Category: Antimalarials
CAS number: 53230-10-7
Pharmacology
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>.
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...
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Mechanism of Action: Mefloquine has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
Absorption: Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
Protein binding: 98%
Biotransformation: Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities.
Route of elimination: There is evidence that mefloquine is excreted mainly in the bile and feces. Urinary excretion of unchanged mefloquine and its main metabolite under steady-state condition accounted for about 9% and 4% of the dose, respectively.
Half Life: 2 to 4 weeks
Clearance: 30 mL/min
Toxicity: Oral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.
Affected organisms: Plasmodium
Interactions
Food interaction:
Avoid alcohol.
Take with a full glass of water.
Take with food.
Drug interaction:
AnisindioneMefloquine may increase the anticoagulant effect of anisindione.
WarfarinMefloquine may increase the anticoagulant effect of warfarin.
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
HalofantrineIncreased risk of cardiac toxicity
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