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Chemical Compound Review

Lariam     [2,8- bis(trifluoromethyl)quinolin- 4-yl]-(2...

Synonyms: Mefaquin, Mefloquin, Mefloquina, mefloquine, Mefloquinum, ...
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Disease relevance of mefloquine


Psychiatry related information on mefloquine


High impact information on mefloquine


Chemical compound and disease context of mefloquine


Biological context of mefloquine

  • The pfmdr1 gene has been associated with a drug-resistant phenotype in Plasmodium falciparum, and overexpression of pfmdr1 has been associated with mefloquine- and halofantrine-resistant parasites, but little is known about the functional role of pfmdr1 in this process [18].
  • The mefloquine-selected parasite lines also showed an inverse relationship between the level of chloroquine resistance and increased pfmdr1 gene copy number [19].
  • Macrorestriction maps of chromosome 5, where pfmdr1 is encoded, showed that this chromosome has increased in size in response to mefloquine selection, indicating the presence of a gene(s) in this area of the genome that confers a selective advantage in the presence of mefloquine [19].
  • 3D7 parasites were subsequently treated with experimentally derived IC50 concentrations of mefloquine, quinine and pyrimethamine. pfmdr1 transcript levels specifically increased 2.5-fold at 6 h in mefloquine-treated parasites and threefold in parasites treated with quinine for 30 min [20].
  • In the current issue of Molecular Microbiology, Sidhu and colleagues use powerful reverse genetics to demonstrate the importance of commonly occurring alleles of pfmdr1 in conferring resistance to the second-line drugs quinine and sensitivity to the new alternatives mefloquine and artemisinin [21].

Anatomical context of mefloquine

  • Mefloquine also blocked channels formed by the lens gap junction protein, Cx50 (IC(50) approximately 1.1 microM) [22].
  • Mefloquine, at 25 microM, blocked gap junctional coupling between interneurons in neocortical slices, with minimal nonspecific actions [22].
  • The more lipophilic quinolinemethanol drugs mefloquine and quinine do not appear to be concentrated so extensively in the food vacuole and may act on alternative targets in the parasite [23].
  • Equal numbers of parasitized erythrocytes were treated with various concentrations of pyrimethamine or mefloquine [24].
  • The strongest effect was observed with mefloquine, which abolished almost completely the neutrophil burst at concentrations of greater than 10 micrograms/ml whatever the stimulus used [25].

Associations of mefloquine with other chemical compounds


Gene context of mefloquine


Analytical, diagnostic and therapeutic context of mefloquine


  1. Effectiveness and tolerance of long-term malaria prophylaxis with mefloquine. Need for a better dosing regimen. Lobel, H.O., Bernard, K.W., Williams, S.L., Hightower, A.W., Patchen, L.C., Campbell, C.C. JAMA (1991) [Pubmed]
  2. Mefloquine-resistant falciparum malaria on the Thai-Burmese border. Nosten, F., ter Kuile, F., Chongsuphajaisiddhi, T., Luxemburger, C., Webster, H.K., Edstein, M., Phaipun, L., Thew, K.L., White, N.J. Lancet (1991) [Pubmed]
  3. Mefloquine-induced Stevens-Johnson syndrome. Van den Enden, E., Van Gompel, A., Colebunders, R., Van den Ende, J. Lancet (1991) [Pubmed]
  4. Fatal toxic epidermal necrolysis associated with mefloquine antimalarial prophylaxis. McBride, S.R., Lawrence, C.M., Pape, S.A., Reid, C.A. Lancet (1997) [Pubmed]
  5. Acute depressive symptoms after mefloquine treatment. Caillon, E., Schmitt, L., Moron, P. The American journal of psychiatry. (1992) [Pubmed]
  6. Mefloquine induces dose-related neurological effects in a rat model. Dow, G., Bauman, R., Caridha, D., Cabezas, M., Du, F., Gomez-Lobo, R., Park, M., Smith, K., Cannard, K. Antimicrob. Agents Chemother. (2006) [Pubmed]
  7. Case study: neuropsychiatric symptoms associated with the antimalarial agent mefloquine. Clattenburg, R.N., Donnelly, C.L. Journal of the American Academy of Child and Adolescent Psychiatry. (1997) [Pubmed]
  8. The risk of severe depression, psychosis or panic attacks with prophylactic antimalarials. Meier, C.R., Wilcock, K., Jick, S.S. Drug safety : an international journal of medical toxicology and drug experience. (2004) [Pubmed]
  9. Bipolar disorder after mefloquine treatment. Even, C., Friedman, S., Lanouar, K. Journal of psychiatry & neuroscience : JPN. (2001) [Pubmed]
  10. Pgh1 modulates sensitivity and resistance to multiple antimalarials in Plasmodium falciparum. Reed, M.B., Saliba, K.J., Caruana, S.R., Kirk, K., Cowman, A.F. Nature (2000) [Pubmed]
  11. Effects of artesunate-mefloquine combination on incidence of Plasmodium falciparum malaria and mefloquine resistance in western Thailand: a prospective study. Nosten, F., van Vugt, M., Price, R., Luxemburger, C., Thway, K.L., Brockman, A., McGready, R., ter Kuile, F., Looareesuwan, S., White, N.J. Lancet (2000) [Pubmed]
  12. Acute fatty liver after malaria prophylaxis with mefloquine. Grieco, A., Vecchio, F.M., Natale, L., Gasbarrini, G. Lancet (1999) [Pubmed]
  13. Long-term malaria prophylaxis with weekly mefloquine. Lobel, H.O., Miani, M., Eng, T., Bernard, K.W., Hightower, A.W., Campbell, C.C. Lancet (1993) [Pubmed]
  14. Halofantrine versus mefloquine in treatment of multidrug-resistant falciparum malaria. ter Kuile, F.O., Dolan, G., Nosten, F., Edstein, M.D., Luxemburger, C., Phaipun, L., Chongsuphajaisiddhi, T., Webster, H.K., White, N.J. Lancet (1993) [Pubmed]
  15. Trials of mefloquine in vivax and of mefloquine plus 'fansidar' in falciparum malaria. Harinasuta, T., Bunnag, D., Lasserre, R., Leimer, R., Vinijanont, S. Lancet (1985) [Pubmed]
  16. Qinghaosu, mefloquine, and pyrimethamine-sulfadoxine in falciparum malaria. Arnold, K. Lancet (1985) [Pubmed]
  17. Safety and immunogenicity of live oral cholera and typhoid vaccines administered alone or in combination with antimalarial drugs, oral polio vaccine, or yellow fever vaccine. Kollaritsch, H., Que, J.U., Kunz, C., Wiedermann, G., Herzog, C., Cryz, S.J. J. Infect. Dis. (1997) [Pubmed]
  18. Functional complementation of the ste6 gene of Saccharomyces cerevisiae with the pfmdr1 gene of Plasmodium falciparum. Volkman, S.K., Cowman, A.F., Wirth, D.F. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  19. Selection for mefloquine resistance in Plasmodium falciparum is linked to amplification of the pfmdr1 gene and cross-resistance to halofantrine and quinine. Cowman, A.F., Galatis, D., Thompson, J.K. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  20. Mapping of the Plasmodium falciparum multidrug resistance gene 5'-upstream region, and evidence of induction of transcript levels by antimalarial drugs in chloroquine sensitive parasites. Myrick, A., Munasinghe, A., Patankar, S., Wirth, D.F. Mol. Microbiol. (2003) [Pubmed]
  21. Multiple drug resistance genes in malaria -- from epistasis to epidemiology. Duraisingh, M.T., Refour, P. Mol. Microbiol. (2005) [Pubmed]
  22. Potent block of Cx36 and Cx50 gap junction channels by mefloquine. Cruikshank, S.J., Hopperstad, M., Younger, M., Connors, B.W., Spray, D.C., Srinivas, M. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  23. Quinoline antimalarials: mechanisms of action and resistance and prospects for new agents. Foley, M., Tilley, L. Pharmacol. Ther. (1998) [Pubmed]
  24. Malaria parasites giving rise to recrudescence in vitro. Nakazawa, S., Maoka, T., Uemura, H., Ito, Y., Kanbara, H. Antimicrob. Agents Chemother. (2002) [Pubmed]
  25. Effects of amodiaquine, chloroquine, and mefloquine on human polymorphonuclear neutrophil function in vitro. Labro, M.T., Babin-Chevaye, C. Antimicrob. Agents Chemother. (1988) [Pubmed]
  26. Combination of mefloquine with sulfadoxine-pyrimethamine compared with two sulfadoxine-pyrimethamine combinations in malaria chemoprophylaxis. Win, K., Thwe, Y., Lwin, T.T., Win, K. Lancet (1985) [Pubmed]
  27. Malaria among United States troops in Somalia. Wallace, M.R., Sharp, T.W., Smoak, B., Iriye, C., Rozmajzl, P., Thornton, S.A., Batchelor, R., Magill, A.J., Lobel, H.O., Longer, C.F., Burans, J.P. Am. J. Med. (1996) [Pubmed]
  28. In vitro interactions of artemisinin with atovaquone, quinine, and mefloquine against Plasmodium falciparum. Gupta, S., Thapar, M.M., Wernsdorfer, W.H., Björkman, A. Antimicrob. Agents Chemother. (2002) [Pubmed]
  29. Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG. Kang, J., Chen, X.L., Wang, L., Rampe, D. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  30. Decreased serum levels of TGF-beta in patients with acute Plasmodium falciparum malaria. Wenisch, C., Parschalk, B., Burgmann, H., Looareesuwan, S., Graninger, W. J. Clin. Immunol. (1995) [Pubmed]
  31. Failure of mefloquine chemoprophylaxis for malaria in Somalia. Magill, A.J., Smoak, B.L. N. Engl. J. Med. (1993) [Pubmed]
  32. Post-malaria neurological syndrome. Nguyen, T.H., Day, N.P., Ly, V.C., Waller, D., Nguyen, H.P., Bethell, D.B., Tran, T.H., White, N.J. Lancet (1996) [Pubmed]
  33. Effects of artemisinin derivatives on malaria transmissibility. Price, R.N., Nosten, F., Luxemburger, C., ter Kuile, F.O., Paiphun, L., Chongsuphajaisiddhi, T., White, N.J. Lancet (1996) [Pubmed]
  34. The present status of malaria chemotherapy: mefloquine, a novel antimalarial. Sweeney, T.R. Medicinal research reviews. (1981) [Pubmed]
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