Cerebral uptake of mefloquine enantiomers with and without the P-gp inhibitor elacridar (GF1210918) in mice

British Journal of Pharmacology

Volumn 141, Issue 7, 2004, Pages 1214-1222

  De Lagerie, Sylvie Barraud ^a,b   Comets, Emmanuelle ^c   Gautrand, Céline ^a,b   Fernandez, Christine ^a   Auchere, Daniel ^a   Singlas, Eric ^b   Mentre, France ^c   Gimenez, François ^a,b  

^a UNIVERSITÉ PARIS SACLAY   (France)

^b HÔPITAL NECKER ENFANTS MALADES   (France)

^c BICHAT HOSPITAL   (France)

Author keywords

Blood brain barrier; Brain uptake; Efflux protein; Elacridar; Enantiomer; Mefloquine; P glycoprotein; Pharmacokinetics; Stereoselectivity

Indexed keywords

ELACRIDAR; MEFLOQUINE; PROTEIN INHIBITOR;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BRAIN FUNCTION; CONTROLLED STUDY; DEATH; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG EXCRETION; DRUG UPTAKE; ENANTIOMER; FEMALE; INJECTION SITE; LIQUID CHROMATOGRAPHY; MOUSE; NONHUMAN; PRIORITY JOURNAL; STEREOCHEMISTRY; TIME;

ACRIDINES; ANIMALS; AREA UNDER CURVE; BLOOD-BRAIN BARRIER; BRAIN; FEMALE; INJECTIONS, INTRAPERITONEAL; MEFLOQUINE; METABOLIC CLEARANCE RATE; MICE; P-GLYCOPROTEIN; STEREOISOMERISM; TETRAHYDROISOQUINOLINES; TIME FACTORS;

EID: 2342638285     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705721     Document Type: Article

References (39)

1. BASCO, L.K., GILLOTIN, C., GIMENEZ, F., FARINOTTI, R. & LEBRAS, J. (1992). In vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline against Plasmodium falciparum. Br. J. Clin. Pharmacol., 33, 517-520.
2. BAUDRY, S., PHAM, Y.T., BAUNE, B., VIDREQUIN, S., CREVOISIER, C., GIMENEZ, F. & FARINOTTI, R. (1997). Stereoselective passage of mefloquine through the blood-brain barrier in the rat. J. Pharm. Pharmacol., 49, 1086-1090.
3. BOURAHLA, A., MARTIN, C., GIMENEZ, F., SINGHASIVANON, V., ATTANATH, P., SABCHEARON, A., CHONGSUPHAJAISIDDHI, T. & FARINOTTI, R. (1996). Stereoselective pharmacokinetics of mefloquine in young children. Eur. J. Clin. Pharmacol., 50, 241-244.
4. CHUNG, H., JIMMERSON, V.R., ROZMAN, R.S. & SANDERS, J.E. (1982). Disposition of the diastereoisomer of mefloquine in mice. Pharmacology, 24, 267-274.
5. COORAY, H.C., BLACKMORE, C.G., MASKELL, L. & BARRAND, M.A. (2002). Localisation of breast cancer resistance protein in microvessel endothelium of human brain. Neuroreport, 13, 2059-2063.
6. CUMMINS, C.L., JACOBSEN, W. & BENET, L.Z. (2002). Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J. Pharmacol. Exp. Ther., 300, 1036-1045.
7. DONLY, C., JEVNIKAR, J., MCLEAN, H. & CAVENEY, S. (2000). Substrate-stereoselectivity of a high-affinity glutamate transporter cloned from the CNS of the cockroach Diploptera punctata. Insect Biochem. Mol. Biol., 30, 369-376.
8. DUCHARME, J., FERNANDEZ, C., GIMENEZ, F. & FARINOTTI, R. (1996). Critical issues in chiral drug analysis in biological fluids by high-performance liquid chromatography. J. Chromatogr. B Biomed. Appl., 686, 65-75.
9. EVERS, R., KOOL, M., SMITH, A.J., VAN DEEMTER, L., DE HAAS, M. & BORST, P. (2000). Inhibitory effect of the reversal agents V-104, GF120918 and Pluronic L61 on MDR1 Pgp-, MRP1- and MRP2-mediated transport. Br. J. Cancer, 83, 366-374.
10. GIMENEZ, F., PENNIE, R.A., KOREN, G., CREVOISIER, C., WAINER, I.W. & FARINOTTI, R. (1994). Stereoselective pharmacokinetics of mefloquine in healthy Caucasians after multiple doses. J. Pharm. Sci., 83, 824-827.
11. HELLGREN, U., BERGGREN-PALME, I., BERGQVIST, Y. & JERLING, M. (1997). Enantioselective pharmacokinetics of mefloquine during long-term intake of the prophylactic dose. Br. J. Clin. Pharmacol., 44, 119-124.
12. HOOIVELD, G.J., HEEGSMA, J., VAN MONTFOORT, J.E., JANSEN, P.L., MEIJER, D.K. & MULLER, M. (2002). Stereoselective transport of hydrophilic quaternary drugs by human MDR1 and rat Mdrlb P-glycoproteins. Br. J. Pharmacol., 135, 1685-1694.
13. HUET, S., BOUVIER, A., GRUET, M. & JOLIVET, E. (1996). Statistical Tools for Nonlinear Regression. New York: Springer-Verlag.
14. IHAKA, R. & GENTLEMAN, R. (1996). A language for data analysis and graphics. J. Comput. Graph Stat., 5, 299-314.
15. IMBERT, F., JARDIN, M., FERNANDEZ, C., GANTIER, J.C., DROMER, F., BARON, G., MENTRE, F., VAN BEIJSTERVELDT, L., SINGLAS, E. & GIMENEZ, F. (2003). Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans. Drug Metab. Dispos., 31, 319-325.
16. JONKER, J.W., BUITELAAR, M., WAGENAAR, E., VAN DER VALK, M.A., SCHEFFER, G.L., SCHEPER, R.J., PLOSCH, T., KUIPERS, F., ELFERINK, R.P., ROSING, H., BEIJNEN, J.H. & SCHINKEL, A.H. (2002). The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria. Proc. Natl. Acad. Sci. U.S.A., 99, 15649-15654.
17. LAN, L.B., AYESH, S., LYUBIMOV, E., PASHINSKY, I. & STEIN, W.D. (1996). Kinetic parameters for reversal of the multidrug pump as measured for drug accumulation and cell killing. Cancer Chemother. Pharmacol., 38, 181-190.
18. LITMAN, T., DRULEY, T.E., STEIN, W.D. & BATES, S.E. (2001). From MDR to MXR: new understanding of multidrug resistance systems, their properties and clinical significance. Cell Mol. Life Sci., 58, 931-959.
19. LOETCHUTINAT, C., HEYWANG, C., PRIEBE, W. & GARNIER-SUILLEROT, A. (2001). The absence of stereoselective P-glycoprotein- and multidrug resistance-associated protein-mediated transport of daunorubicin. Biochem. Pharmacol., 62, 561-567.
20. LU, L., LEONESSA, F., BAYNHAM, M.T., CLARKE, R., GIMENEZ, F., PHAM, Y.T., ROUX, F. & WAINER, I.W. (2001). The enantioselective binding of mefloquine enantiomers to P-glycoprotein determined using an immobilized P-glycoprotein liquid chromatographic stationary phase. Pharm. Res., 18, 1327-1330.
21. MALIEPAARD, M., SCHEFFER, G.L., FANEYTE, I.F., VAN GASTELEN, M.A., PIJNENBORG, A.C., SCHINKEL, A.H., VAN DE VIJVER, M.J., SCHEPER, R.J. & SCHELLENS, J.H. (2001). Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues. Cancer Res., 61, 3458-3464.
22. MARTIN, C., GIMENEZ, F., BANGCHANG, K.N., KARBWANG, J., WAINER, I.W. & FARINOTTI, R. (1994). Whole blood concentrations of mefloquine enantiomers in healthy Thai volunteers. Eur. J. Clin. Pharmacol., 47, 85-87.
23. MU, J.Y., ISRAILI, Z.H. & DAYTON, P.G. (1975). Studies of the disposition and metabolism of mefloquine HC1 (WR 142,490), a quinolinemethanol antimalarial, in the rat. Limited studies with an analog, WR 30,090. Drug Metab. Dispos., 3, 198-210.
24. OZVEGY, C., LITMAN, T., SZAKACS, G., NAGY, Z., BATES, S., VARADI, A. & SARKADI, B. (2001). Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells. Biochem. Biophys. Res. Commun., 285, 111-117.
25. PHAM, Y.T., NOSTEN, F., FARINOTTI, R., WHITE, N.J. & GIMENEZ, F. (1999). Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria. Int. J. Clin. Pharmacol. Ther., 37, 58-61.
26. PHAM, Y.T., REGINA, A., FARINOTTI, R., COURAUD, P., WAINER, I.W., ROUX, F. & GIMENEZ, F. (2000). Interactions of racemic mefloquine and its enantiomers with P-glycoprotein in an immortalised rat brain capillary endothelial cell line, GPNT. Biochim. Biophys. Acta, 1524, 212-219.
27. PHILLIPS-HOWARD, P.A. & TER KUILE, F.O. (1995). CNS adverse events associated with antimalarial agents. Fact or fiction? Drug Saf., 12, 370-383.
28. RIFFKIN, C.D., CHUNG, R., WALL, D.M., ZALCBERG, J.R., COWMAN, A.F., FOLEY, M. & TILLEY, L. (1996). Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine. Biochem. Pharmacol., 52, 1545-1552.
29. ROCHAT, B., BAUMANN, P. & AUDUS, K.L. (1999). Transport mechanisms for the antidepressant citalopram in brain microvessel endothelium. Brain Res., 831, 229-236.
30. SANDSTROM, R., KARLSSON, A. & LENNERNAS, H. (1998). The absence of stereoselective P-glycoprotein-mediated transport of R/S-verapamil across the rat jejunum. J. Pharm. Pharmacol., 50, 729-735.
31. SCHINKEL, A.H., WAGENAAR, E., MOL, C.A. & VAN DEEMTER, L. (1996). P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J. Clin. Invest., 97, 2517-2524.
32. SHAO, Y.M., AYESH, S. & STEIN, W.D. (1997). Mutually co-operative interactions between modulators of P-glycoprotein. Biochim. Biophys. Acta, 1360, 30-38.
33. SICCARDI, D., KANDALAFT, L.E., GUMBLETON, M. & MCGUIGAN, C. (2003). Stereoselective and concentration-dependent polarized epithelial permeability of a series of phosphoramidate triester prodrugs of d4T: an in vitro study in Caco-2 and Madin-Darby canine kidney cell monolayers. J. Pharmacol. Exp. Ther., 307, 1112-1119.
34. SUN, H., DAI, H., SHAIK, N. & ELMQUIST, W.F. (2003). Drug efflux transporters in the CNS. Adv. Drug Deliv. Rev., 55, 83-105.
35. SVENSSON, U.S., ALIN, H., KARLSSON, M.O., BERGQVIST, Y. & ASHTON, M. (2002). Population pharmacokinetic and pharmacodynamic modelling of artemisinin and mefloquine enantiomers in patients with falciparum malaria. Eur. J. Clin. Pharmacol., 58, 339-351.
36. SZABO, D. & MOLNAR, J. (1998). The role of stereoselectivity of chemosensitizers in the reversal of multidrug resistance of mouse lymphoma cells. Anticancer Res., 18, 3039-3044.
37. TANG, C., ZHANG, K., LEPAGE, F., LEVY, R.H. & BAILLIE, T.A. (1994). Metabolic chiral in version of stiripentol in the rat. II. Influence of route of administration. Drug Metab. Dispos., 22, 554-560.
38. VIDREQUIN, S., GIMENEZ, F., BASCO, L.K., MARTIN, C., LEBRAS, J. & FARINOTTI, R. (1996). Uptake of mefloquine enantiomers into uninfected and malaria-infected erythrocytes. Drug Metab. Dispos., 24, 689-691.
39. WEINKE, T., TRAUTMANN, M., HELD, T., WEBER, G., EICHENLAUB, D., FLEISCHER, K., KERN, W. & POHLE, H.D. (1991). Neuropsychiatric side effects after the use of mefloquine. Am. J. Trop Med. Hyg., 45, 86-91.