The effects of the human MDR1 genotype on the expression of duodenal P-glycoprotein and disposition of the probe drug talinolol

Clinical Pharmacology and Therapeutics

Volumn 72, Issue 5, 2002, Pages 572-583

  Siegmund, Werner ^a   Ludwig, Karen ^a   Giessmann, Thomas ^a   Dazert, Peter ^a   Schroeder, Eike ^a   Sperker, Bernhard ^a   Warzok, Rolf ^a   Kroemer, Heyo K ^a   Cascorbi, Ingolf ^a  

^a UNIVERSITY OF GREIFSWALD   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; MESSENGER RNA; TALINOLOL;

ADULT; AMINO ACID SUBSTITUTION; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG SCREENING; DUODENUM; EXON; FEMALE; GENE; GENE FREQUENCY; GENE MUTATION; GENE PROBE; GENETIC VARIABILITY; GENOTYPE; HETEROZYGOTE; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; KRUSKAL WALLIS TEST; MALE; MULTIDRUG RESISTANCE GENE 1; NORMAL HUMAN; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; RANK SUM TEST; SINGLE NUCLEOTIDE POLYMORPHISM;

ADULT; AREA UNDER CURVE; DUODENUM; FEMALE; GENES, MDR; GENOTYPE; HUMANS; MALE; P-GLYCOPROTEIN; POLYMORPHISM, GENETIC; PROPANOLAMINES; RNA, MESSENGER;

EID: 0036881077     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1067/mcp.2002.127739     Document Type: Article

References (38)

1. Juliano RL, Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 1976;455:152-62.
2. Schinkel A. The physiological function of drug-transporting P-glycoproteins. Semin Cancer Biol 1997;8:161-70.
3. Fromm M. P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs. Int J Clin Pharmacol Ther 2000;38:69-74.
4. Zhang Y, Benet LZ. The gut as a barrier to drug absorption. Combined role of cytochrome P4503A and P-glycoprotein. Clin Pharmacokinet 2001;40:159-68.
5. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, et al. The interaction of digoxin and rifampin: role of intestinal P-glycoprotein. J Clin Invest 1999;104:147-53.
6. Westphal K, Weinbrenner A, Zschiesche M, Franke G, Knoke M, Oertel R, et al. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Clin Pharmacol Ther 2000;68:345-55.
7. Lown KS, Mayo RR, Leichtman AB, Hsiao H, Turgeon K, Schmiedlin-Ren P, et al. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther 1997;62:248-60.
8. Geick A, Eichelbaum M, Burk O. Nuclear response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem 2001;276:14581-7.
9. Siegmund W, Altmannsberger S, Paneitz A, Hecker U, Zschiesche M, Franke G, et al. Effect of levothyroxine administration on intestinal P-glycoprotein expression: consequences for drug disposition. Clin Pharmacol Ther. In press 2002.
10. Johne A, Brockmöller J, Bauer S, Maurer A, Langheinrich M, Roots I. Pharmacokinetic interaction of digoxin with an herbal extract from St John's wort (Hypericum perforatum). Clin Pharmacol Ther 1999;66:338-45.
11. Dürr D, Stieger B, Kullak-Ublick GA, Rentsch KM, Steinert HC, Meier PJ, et al. St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin Pharmacol Ther 2000;68:598-604.
12. Fromm MF, Kim RB, Stein CM, Wilkinson GR, Roden DM. Inhibition of P-glycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine. Circulation 1999;99:552-7.
13. Kovarik JM, Rigaudy L, Guerret M, Gerbeau C, Rost KL. Longitudinal assessment of a P-glycoprotein-mediated drug interaction of valspodar on digoxin. Clin Pharmacol Ther 1999;66:391-400.
14. Gramatté T, Oertel R. Intestinal secretion of intravenous talinolol is inhibited by luminal R-verapamil. Clin Pharmacol Ther 1999;66:239-45.
15. Westphal K, Weinbrenner A, Giessmann T, Stuhr M, Franke G, Zschiesche M, et al. Oral bioavailability of digoxin is enhanced by talinolol: evidence for involvement of intestinal P-glycoprotein. Clin Pharmacol Ther 2000;68:6-12.
16. Kaplan B, Lown K, Craig R, Abecassis M, Kaufman D, Leventhal J, et al. Low bioavailability of cyclosporine microemulsion and tacrolimus in a small bowel transplant recipient. Transplantation 1999;67:333-8.
17. Farrell RJ, Murphy A, Long A, Donnelly S, Cherikuri A, O'Toole D, et al. High multidrug resistance (P-glycoprotein 170) expression in inflammatory bowel disease patients who fail medical therapy. Gastroenterology 2000;118:279-88.
18. Hoffmeyer S, Burk O, von Richter O, Arnold HP, Brockmöller J, Johne A, et al. Functional polymorphism of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo. Proc Natl Acad Sci U S A 2000;97:3473-8.
19. Cascorbi I, Gerloff T, Johne A, Meisel C, Hoffmeyer S, Schwab M, et al. Frequency of single nucleotide polymorphisms in the P-glycoprotein drug transporter MDR1 gene in white subjects. Clin Pharmacol Ther 2001;69:169-74.
20. Tanabe M, Ieiri I, Nagata N, Inoue K, Ito S, Kanamori Y, et al. Expression of P-glycoprotein in human placenta: Relation to genetic polymorphism of the multidrug resistance (MDR)-1 gene. J Pharmacol Exp Ther 2001;297:1137-43.
21. + natural killer cells. Pharmacogenetics 2001;11:293-8.
22. Ambudkar SV, Dey S, Hrycyna CA, Ramachandra M, Pastan I, Gottesman MM. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Ther 1999;39:361-98.
23. Kim RB, Leake BF, Choo EF, Dresser GK, Kubba SV, Schwarz UI, et al. Identification of functionally variant MDR1 alleles among European Americans and African Americans. Clin Pharmacol Ther 2001;70:189-99.
24. 1-adrenoceptor antagonist talinolol in man. Biopharm Drug Disp 1995;16:403-14.
25. Gramatté T, Oertel R, Terhaag B, Kirch W. Direct demonstration of small intestinal secretion and site-dependent absorption of the β-blocker talinolol in humans. Clin Pharmacol Ther 1996;59:541-9.
26. Siegmund W, Gielßmann T, Zschiesche M, Franke G, Sperker B, May K, et al. Carbamazepine induces intestinal P-glycoprotein and affects disposition of the probe drug talinolol (abstract). Pharmacol Toxicol 2001;89(Suppl 1):74.
27. Siegmund W, Giessmann T, Modess C, Zschiesche M, Engel G, Dazert P, et al. Disposition of repeated oral carvedilol after rifampicin: influence of CYP2D6 and intestinal P-glycoprotein (abstract). Naunyn Schmiedebergs Arch Pharmacol 2002;365(Suppl 1):R109.
28. Franke G, Westphal K, Weinbrenner A, Richter K, Schnabel F, Gramatté T, et al. Steady-state disposition of the bladder spamolytics propiverine is circadian time dependent in men (abstract). Eur J Clin Pharmacol 2000;56(Suppl):A26.
29. Giessmann T, Zschiesche M, Modess C, Tschuschke A, Hartmann V, Weitschies W, et al. Are there two absorption routes for talinolol? (abstract). Eur J Clin Pharmacol 2001;57:A20.
30. Haase K, Franke G, Zschiesche M, Kosowska-Stift, Hoffmann A, Terhaag B, et al. Single dose bioequivalence study to compare different talinolol formulations of Cordanum® (abstract). Eur J Clin Pharmacol 1998;54:A11.
31. Fellay J, Marzolini C, Meaden ER, Back DJ, Buclin T, Chave JP, et al. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet 2002;359:30-6.
32. Min DI, Ellingrod VL. C3435T mutation in exon 26 of the human MDR1 gene and cyclosporine pharmacokinetics in healthy subjects. Ther Drug Monit 2002;24:400-4.
33. von Ahsen N, Richter M, Grupp C, Ringe B, Oellerich M, Armstrong VW. No influence of the MDR1 C3435T polymorphism or a CYP3A4 promoter polymorphism (CYP3A4-V allele) on dose-adjusted cyclosporin A trough concentrations or rejection incidence in stable renal transplant recipients. Clin Chem 2001;47:1048-52.
34. Becquemont L, Verstuyft C, Kerb R, Brinkmann U, Lebot M, Jaillon P, et al. Effect of grapefruit juice on digoxin pharmacokinetics in humans. Clin Pharmacol Ther 2001;70:311-6.
35. Drescher S, Schaeffeler E, Hitzl M, Hofmann U, Schwab M, Brinkmann U, et al. MDR1 gene polymorphism and disposition of the P-glycoprotein substrate fexofenadine. Br J Clin Pharmacol 2002;53:526-34.
36. Sakaeda T, Nakamura T, Horinouchi M, Kakumoto M, Ohmoto N, Sakai T, et al. MDR1 genotype-related pharmacokinetics of digoxin after single oral administration in healthy Japanese subjects. Pharm Res 2001;18:1400-4.
37. Fairchild CR, Moscow JA, O'Brien EE, Cowan KH. Multidrug resistance in cells transfected with human genes encoding a variant P-glycoprotein and glutathione S-transferase-π. Mol Pharmacol 1990;37:801-9.
38. 1-blocker talinolol in humans. Clin Pharmacol Ther 1999;65:283-90.