Increased absorption of digoxin from the human jejunum due to inhibition of intestinal transporter-mediated efflux

Clinical Pharmacokinetics

Volumn 46, Issue 9, 2007, Pages 777-785

  Igel, Svitlana ^a   Drescher, Siegfried ^a,b   Mürdter, Thomas ^a   Hofmann, Ute ^a   Heinkele, Georg ^a   Tegude, Heike ^a   Glaeser, Hartmut ^a,b   Brenner, Stefanie S ^a   Somogyi, Andrew A ^c   Omari, Taher ^d   Schäfer, Christian ^e   Eichelbaum, Michel ^a   Fromm, Martin F ^a,b  

^a UNIVERSITY OF TÜBINGEN   (Germany)

^b UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^c UNIVERSITY OF ADELAIDE   (Australia)

^d WOMEN S AND CHILDREN S HOSPITAL   (Australia)

^e ROBERT BOSCH HOSPITAL   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLDIGOXIN; DIGOXIN; DRUG CARRIER; GLYCOPROTEIN P; PHENAZONE; QUINIDINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG MECHANISM; DRUG POTENTIATION; EFFUSION; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; INTESTINE ABSORPTION; JEJUNUM; MALE; NORMAL HUMAN; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; ADULT; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ANTIPYRINE; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT, ACTIVE; DIGOXIN; ENTEROCYTES; ENZYME INHIBITORS; EPITHELIAL CELLS; HUMANS; INTESTINAL ABSORPTION; JEJUNUM; MALE; P-GLYCOPROTEIN; PROTEIN TRANSPORT; QUINIDINE; XENOBIOTICS;

EID: 34548295855     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200746090-00005     Document Type: Article

References (26)

1. Dietrich CG, Geier A, Oude Elferink RP. ABC of oral bioavailability: transporters as gatekeepers in the gut. Gut 2003 Dec; 52 (12): 1788-95
2. Fromm MF. Importance of P-glycoprotein at blood-tissue barriers. Trends Pharmacol Sci 2004 Aug; 25 (8): 423-9
3. Kunta JR, Sinko PJ. Intestinal drug transporters: in vivo function and clinical importance. Curr Drug Metab 2004 Feb; 5 (1): 109-24
4. Watkins PB. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv Drug Deliv Rev 1997; 27 (2-3): 161-70
5. Drescher S, Schaeffeler E, Hitzl M, et al. MDR1 gene polymorphisms and disposition of the P-glycoprotein substrate fexofenadine. Br J Clin Pharmacol 2002 May; 53 (5): 526-34
6. Greiner B, Eichelbaum M, Fritz P, et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest 1999 Jul; 104 (2): 147-53
7. Westphal K, Weinbrenner A, Zschiesche M, 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 Oct; 68 (4): 345-55
8. Kim RB, Fromm MF, Wandel C, et al. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Invest 1998 101 (2): 289-94
9. Schinkel AH, Wagenaar E, van Deemter L, et al. Absence of the mdr1a P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest 1995 Oct; 96 (4): 1698-705
10. Drescher S, Glaeser H, Mürdter T, et al. P-glycoprotein-mediated intestinal and biliary digoxin transport in humans. Clin Pharmacol Ther 2003 Mar; 73 (3): 223-31
11. Tannergren C, Knutson T, Knutson L, et al. The effect of ketoconazole on the in vivo intestinal permeability of fexofenadine using a regional perfusion technique. Br J Clin Pharmacol 2003 Feb; 55 (2): 182-90
12. Glaeser H, Drescher S, Hofmann U, et al. Impact of concentration and rate of intraluminal drug delivery on absorption and gut wall metabolism of verapamil in humans. Clin Pharmacol Ther 2004 Sep; 76 (3): 230-8
13. von Richter O, Greiner B, Fromm MF, et al. Determination of in vivo absorption, metabolism, and transport of drugs by the human intestinal wall and liver with a novel perfusion technique. Clin Pharmacol Ther 2001 Sep; 70 (3): 217-27
14. Becquemont L, Glaeser H, Drescher S, et al. Effects of ursodeoxycholic acid on P-glycoprotein and cytochrome P450 3A4-dependent pharmacokinetics in humans. Clin Pharmacol Ther 2006 May; 79 (5): 449-60
15. Goromaru T, Noda A. The base-catalyzed deuteration of hydrogen in methyl group substituted at 3-position of pyrazolone ring. Chem Pharm Bull (Tokyo) 1978; 26: 2258-61
16. Wandel C, Kim RB, Kajiji S, et al. P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res 1999 Aug 15; 59 (16): 3944-8
17. Heck HA, Buttrill Jr SE, Flynn NW, et al. Bioavailability of imipramine tablets relative to a stable isotope-labeled internal standard: increasing the power of bioavailability tests. J Pharmacokinet Biopharm 1979 Jun; 7 (3): 233-48
18. Doering W. Quinidine-digoxin interaction: pharmacokinetics, underlying mechanism and clinical implications. N Engl J Med 1979 Aug 23; 301 (8): 400-4
19. de Lannoy IA, Silverman M. The MDR1 gene product, P-glycoprotein, mediates the transport of the cardiac glycoside, digoxin. Biochem Biophys Res Commun 1992 Nov 30; 189 (1): 551-7
20. Fromm MF, Kim RB, Stein CM, et al. Inhibition of P-glycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine. Circulation 1999; 99 (4): 552-7
21. Liu S, Tam D, Chen X, et al. P-glycoprotein and an unstirred water layer barring digoxin absorption in the vascularly perfused rat small intestine preparation: induction studies with pregnenolone-16alpha-carbonitrile. Drug Metab Dispos 2006 Sep; 34 (9): 1468-79
22. Kullak-Ublick GA, Ismair MG, Stieger B, et al. Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology 2001 Feb; 120 (2): 525-33
23. Mikkaichi T, Suzuki T, Onogawa T, et al. Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc Natl Acad Sci U S A 2004 Mar 9; 101 (10): 3569-74
24. Kobayashi D, Nozawa T, Imai K, et al. Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther 2003 Aug; 306 (2): 703-8
25. Glaeser H, Bailey DG, Dresser GK, et al. Intestinal drug transporter expression and the impact of grapefruit juice in humans. Clin Pharmacol Ther 2007 Mar; 81 (3): 362-70
26. Nilsson D, Fagerholm U, Lennernas H. The influence of net water absorption on the permeability of antipyrine and levodopa in the human jejunum. Pharm Res 1994 Nov; 11 (11): 1540-7