D0448 | mefloquine

Molecular Formula C17H16F6N2O
Molecular Weight 378.31
State solid
Clearance * 30 mL/min
Volume of distribution * 20 L/kg [healthy adults]
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.
Protein binding 0.98
Half life 2 to 4 weeks
Absorption Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
Trade names Lariam, Mephaquin, Mefliam
Description phospholipid-interacting antimalarial drug (antimalarials)


P01BF02 Artesunate and mefloquine

[P01BF] Artemisinin and derivatives, combinations



[P] Antiparasitic products, insecticides and repellents

P01BC02 Mefloquine

[P01BC] Methanolquinolines



[P] Antiparasitic products, insecticides and repellents

Toxicity Dose Time Species Model Method Action Positive criterion Reference
GLUCOSE GALACTOSE IC50 RATIO 2.9 ± 1.1, 2.3 ± 1.0, 1.4 ,3.4 ± 1.3, 3.6 ± 2.2, 1.2 4hr H9c2 cells high-glucose–galactose cell viability assay with JC-1 mitochondrial membrane potential and ATP-depletion assays (CellTiter-Glo reagent ). glucose/galactose IC50 ratio (JC-1 IC50 in glucose, JC-1 IC50 in galactose, JC-1 glu/gla, ATP IC50 in glucose, ATP IC50 in galactose, ATP glu/gla ) 50

Target Dose Time Species Model Method Action Positive criterion Reference
ATP synthase inhibitor 35

Pictogram Signal Statements Precautionary Statement Codes

H302: Harmful if swallowed [Warning Acute toxicity, oral]

P264, P270, P301+P312, P330, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

  • (+)-(11S,2'R)-erythro-Mefloquine (+)-erythro-4-Quinolinemethanol, .alpha.-2-piperidinyl-2,8-bis(trifluoromethyl)- (-)-(11S,2'R)-erythro-Mefloquine
    (-)-Mefloquine (DL-erythro-alpha-2-Piperidyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol (S)-(2,8-bis(trifluoromethyl)quinolin-4-yl)((R)-piperidin-2-yl)methanol
    (S)-[2,8-bis(trifluoromethyl)-4-quinolinyl]-[(2R)-2-piperidinyl]methanol;hydrochloride (S)-[2,8-bis(trifluoromethyl)-4-quinolyl]-[(2R)-2-piperidyl]methanol (S)-[2,8-bis(trifluoromethyl)-4-quinolyl]-[(2R)-2-piperidyl]methanol;hydrochloride
    (S)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2R)-piperidin-2-yl]methanol;hydrochloride (S)-[2,8-bis(trifluoromethyl)quinolin-4-yl][(2R)-piperidin-2-yl]methanol (S,R)-MEFLOQUINE
    4-Quinolinemethanol, .alpha.-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, (.alpha.S)- 4-Quinolinemethanol, alpha-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, (alphaS)-; 4-Quinolinemethanol, alpha-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, (alphaS)-rel-
    4-Quinolinemethanol, alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-, (R*,S*)-(+-)- 51742-86-0 51742-87-1
    53230-10-7 BDBM50151865 BDBM79170
    BIDD:GT0596 BIDD:PXR0166 BRD-K40645748-003-08-5
    C07633 CHEBI:63687 CHEMBL172
    D04895 DTXSID4037168 HSDB 6853
    LS-142023 LS-187797 MLS001332559
    MMV000014 MMV000016 Mefloquin
    Mefloquina Mefloquina [INN-Spanish] Mefloquine (USAN/INN)
    Mefloquine [USAN:INN:BAN] Mefloquinum Mefloquinum [INN-Latin]
    Mephloquine NCGC00161831-01 NCGC00161831-02
    NCGC00161831-03 Q27084116 RO 13-7224
    RO 13-7225 RTI1188-1-1 RTI1189-1-1
    Racemic mefloquine Ro 21-5998 Ro 215998
    Ro-21-5998-001 SCHEMBL21780 SMR000875233
    UNII-TML814419R component XEEQGYMUWCZPDN-DOMZBBRYSA-N WR 142,490 WR 142490
    WR-142,490 WR-177,602 ZINC897085
    [(11S,2'R)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol cid_65329 mefloquine

    DrugBank Name mefloquine
    DrugBank DB00358
    CAS Number 147368-41-0, 51742-86-0, 51742-87-1, 51773-92-3, 53230-10-7
    PubChem Compound 40692
    KEGG Compound ID C07633
    KEGG Drug D04895
    ChEBI 63609
    PharmGKB PA450348