The absence of stereoselective P-glycoprotein-mediated transport of R/S-verapamil across the rat jejunum

Journal of Pharmacy and Pharmacology

Volumn 50, Issue 7, 1998, Pages 729-735

  Sandström, Rikard ^a   Karlsson, Anders ^b   Lennernäs, Hans ^a,c  

^a UPPSALA UNIVERSITY   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

^c UPPSALA UNIVERSITY   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORPROMAZINE; GLYCOPROTEIN P; NORVERAPAMIL; VERAPAMIL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG METABOLISM; DRUG TRANSPORT; ENANTIOMER; INTESTINE CELL; INTESTINE MUCOSA PERMEABILITY; INTESTINE SECRETION; INTRAVENOUS DRUG ADMINISTRATION; JEJUNUM; MALE; NONHUMAN; RAT; SMALL INTESTINE ABSORPTION; STEREOCHEMISTRY;

EID: 0031870979     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.1998.tb07133.x     Document Type: Article

References (31)

1. Borst, P., Schinkel, A. H., Smit, J. J., Wagenaar, E., Van, D. L., Smith, A. J., Eijdems, E. W., Baas, F., Zaman, G. J. (1993) Classical and novel forms of multidrug resistance and the physiological functions of P-glycoproteins in mammals. Pharmacol. Ther. 60: 289-299
2. Cashman, J. R., Yang, Z., Yang, L., Wrighton, S. A. (1993) Stereo- and regioselective N- and S-oxidation of tertiary amines and sulfides in the presence of adult human liver microsomes. Drug Metab. Dispos. 21: 492-501
3. De Waziers, I., Cugnenc, P. H., Yang, C. S., Leroux, J. P., Beaune, P. H. (1990) Cytochrome P 450 isoenzymes, epoxide hydrolase and glutathione transferase in rat and human hepatic and extrahepatic tissues. J. Pharmacol. Exp. Ther. 253: 387-394
4. Fagerholm, U., Johansson, M., Lennernäs, H. (1996) Comparison between permeability coefficients in rat and human jejunum. Pharm. Res. 13: 1336-1342
5. Fromm, M. F., Busse, D., Kroemer, H. K., Eichelbaum, M. (1996) Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin. Hepatology 24: 796-801
6. Gramatte, T., Oertel, R., Terhaag, B., Kirch, W. (1996) Direct demonstration of small intestinal secretion and site-dependent absorption of the beta-blocker talinolol in humans. Clin. Pharmacol. Ther. 59: 541-549
7. Higgins, C. F., Gottesman, M. M. (1992) Is the multidrug transporter a flippase? Trends Biochem. Sci. 17: 18-21
8. Karlsson, J., Kuo, S. M., Ziemniak, J., Artursson, P. (1993) Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br. J. Pharmacol. 110: 1009-1016
9. Kroemer, H. K., Echizen, H., Heidemann, H., Eichelbaum, M. (1992) Predictability of the in vivo metabolism of verapamil from in vitro data: contribution of individual metabolic pathways and stereoselective aspects. J. Pharmacol. Exp. Ther. 260: 1052-1077
10. Lennernäs, H., Regardh, C. G. (1993a) Dose-dependent intestinal absorption and significant intestinal excretion (exsorption) of the beta-blocker pafenolol in the rat. Pharm. Res. 10: 727-731
11. Lennernäs, H., Regardh, C. G. (1993b) Evidence for an interaction between the beta-blocker pafenolol and bile salts in the intestinal lumen of the rat leading to dose-dependent oral absorption and double peaks in the plasma concentration-time profile. Pharm. Res. 10: 879-883
12. Lennernäs, H., Ahrenstedt, O., Hallgren, R., Knutson, L., Ryde, M., Paalzow, L. K. (1992) Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man. Pharm. Res. 9: 1243-1251
13. Levitt, M. D., Kneip, J. M., Levitt, D. G. (1988) Use of laminar flow and unstirred layer models to predict intestinal absorption in the rat. J. Clin. Invest. 81: 1365-1369
14. Lown, K. S., Mayo, R. R., Leichtman, A. B., Hsiao, H. L., Turgeon, D. K., Schmiedlin, R. P., Brown, M. B., Guo, W., Rossi, S. J., Benet, L. Z., Watkins, P. B. (1997) Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin. Pharmacol. Ther. 62: 248-260
15. McGowan, F. X., Reiter, M. J., Pritchett, E. L., Shand, D. G. (1983) Verapamil plasma binding: relationship to alpha 1-acid glycoprotein and drug efficacy. Clin. Pharmacol. Ther. 33: 485-490
16. Mehvar, R., Reynolds, J. (1996) Reversal of stereoselectivity in the hepatic availability of verapamil in isolated perfused rat livers: role of protein binding. Drug Metab. Dispos. 24: 1088-1094
17. Plumb, J. A., Milroy, R., Kaye, S. B. (1990) The activity of verapamil as a resistance modifier in vitro in drug-resistant human tumour cell lines is not stereospecific. Biochem. Pharmacol. 39: 787-792
18. Robinson, M. A., Mehvar, R. (1996) Enantioselective distribution of verapamil and norverapamil into human and rat erythrocytes: the role of plasma protein binding. Biopharm. Drug Dispos. 17: 577-587
19. Saitoh, H., Aungst, B. J. (1995) Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Pharm. Res. 12: 1304-1310
20. Schinkel, A. H., Smit, J. J. M., Van, T. O., Beijnen, J. H., Wagenaar, E., Van, D. L., Mol, C. A. A. M., van der Valk, M. A., Robanus, M. E. C., Te, R. H. P. J., Berns, A. J. M., Borst, P. (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77: 491-502
21. Schinkel, A. H., Mayer, U., Wagenaar, E., Mol, C. A., Van, D. L., Smit, J. J., van der Valk, M., Voordouw, A. C., Spits, H., Van, T. O., Zijlmans, J. M., Fibbe, W. E., Borst, P. (1997) Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins. Proc. Natl Acad. Sci. USA 94: 4028-4033
22. Sparreboom, A., Van, A. J., Mayer, U., Schinkel, A. H., Smit, J. W., Meijer, D. K., Borst, P., Nooijen, W. J., Beijnen, J. H., Van, T. O. (1997) Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc. Natl Acad. Sci. USA 94: 2031-2035
23. Stein, W. D. (1997) Kinetics of the multidrug transporter (P-glycoprotein) and its reversal. Physiol. Rev. 77: 545-590
24. Terao, T., Hisanaga, E., Sai, Y., Tamai, I., Tsuji, A. (1996) Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J. Pharm. Pharmacol. 48: 1083-1089
25. Thummel, K. E., O'Shea, D., Paine, M. F., Shen, D. D., Kunze, K. L., Perkins, J. D., Wilkinson, G. R. (1996) Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin. Pharmacol. Ther. 59: 491-502
26. Turnheim, K., Lauterbach, F. (1977) Secretion of monoquaternary ammonium compounds by guinea-pig small intestine in vivo. Naunyn Schmiedebergs Arch. Pharmacol. 299: 201-205
27. Turnheim, K., Lauterbach, F. (1980) Interaction between intestinal absorption and secretion of monoquaternary ammonium compounds in guinea-pigs - a concept for the absorption kinetics of organic cations. J. Pharmacol. Exp. Ther. 212: 418-424
28. Verbeeck, R. K., Cardinal, J. A., Hill, A. G., Midha, K. K. (1983) Binding of phenothiazine neuroleptics to plasma proteins. Biochem. Pharmacol. 32: 2565-2570
29. Wacher, V. J., Wu, C. Y., Benet, L. Z. (1995) Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol. Carcinog. 13: 129-134
30. Wetterich, U., Spann, L. H., Mutschler, E., Terhaag, B., Rosch, W., Langguth, P. (1996) Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers: concentration- and dose-dependent absorption in vitro and in vivo. Pharm. Res. 13: 514-522
31. Winiwarter, S., Bonman, N., Hallberg, A., Lennernäs, H., Karlen, A. (1997) Correlation of drug permeability in humans (in vivo) with experimentally and theoretically derived parameters. Eur. J. Pharm. Sci. 5 (Suppl. 2): 50