Dipyridamole enhances digoxin bioavailability via P-glycoprotein inhibition

Clinical Pharmacology and Therapeutics

Volumn 73, Issue 1, 2003, Pages 51-60

  Verstuyft, Céline ^a,b   Strabach, Soraya ^a,b   El Morabet, Hakima ^a,b   Kerb, Reinhold ^a,b   Brinkmann, Ulrich ^a,b   Dubert, Liliane ^a,b   Jaillon, Patrice ^a,b   Funck Brentano, Christian ^a,b   Trugnan, Germain ^a,b   Becquemont, Laurent ^a,b,c  

^a HÔPITAL SAINT ANTOINE   (France)

^b Epidauros Biotechnologie AG   (Germany)

^c SORBONNE UNIVERSITÉ   (France)

Author keywords

[No Author keywords available]

Indexed keywords

DIGOXIN; DIGOXINE NATIVELLE; DIPYRIDAMOLE; GLYCOPROTEIN P; PLACEBO;

ADULT; ANIMAL CELL; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN CACO 2; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG POTENTIATION; DRUG TRANSPORT; EXON; FEMALE; GENETIC POLYMORPHISM; GENOTYPE; HUMAN; HUMAN EXPERIMENT; KIDNEY CLEARANCE; MALE; NONHUMAN; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADULT; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CARDIOTONIC AGENTS; CROSS-OVER STUDIES; CYSTEINE; DIGOXIN; DIPYRIDAMOLE; ENZYME INHIBITORS; FEMALE; GENES, MDR; GENOTYPE; HUMANS; MALE; P-GLYCOPROTEIN; PHOSPHODIESTERASE INHIBITORS; PLATELET AGGREGATION INHIBITORS; POLYMORPHISM, GENETIC; REFERENCE VALUES; THREONINE;

EID: 0037261395     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1067/mcp.2003.8     Document Type: Article

References (30)

1. HGNC gene family nomenclature: human ABC-transporter genes, Available at http://www.gene.ucl.ac.uk/nomenclature/genefamily/abc.html. Accessed November 26, 2002.
2. Fromm MF, Eichelbaum M. The pharmacogenomics of human P-glycoprotein. In: Licinio J, Wong M-L, editors. Pharmacogenomics: the search for individualized therapies. Weinheim (Germany): Wiley-VCH; 2002. p. 159-78.
3. Fromm MF. P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs. Int J Clin Pharmacol Ther 2000;38:69-74.
4. 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.
5. 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.
6. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest 1999;104:147-53.
7. 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.
8. Yu DK. The contribution of P-glycoprotein to pharmacokinetic drug-drug interactions. J Clin Pharmacol 1999;39:1203-11.
9. Abernethy DR, Flockhart DA. Molecular basis of cardiovascular drug metabolism: implications for predicting clinically important drug interactions. Circulation 2000;101:1749-53.
10. 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.
11. 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.
12. Damle BD, Sridhar R, Desai PB. Dipyridamole modulates multidrug resistance and intracellular as well as nuclear levels of doxorubicin in B16 melanoma cells. Int J Cancer 1994;56:113-8.
13. Krishan A, Sridhar KS, Mou C, Stein WD, Lyubimov E, Hu YP, et al. Synergistic effect of prochlorperazine and dipyridamole on the cellular retention and cytotoxicity of doxorubicin. Clin Cancer Res 2000;6:1508-17.
14. Hoffmeyer S, Burk O, von Richter O, Arnold HP, Brockmoller J, Johne A, et al. Functional polymorphisms 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.
15. Artursson P, Palm K, Luthman K. Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv Drug Deliv Rev 2001;46:27-43.
16. Essodaigui M, Broxterman HJ, Garnier-Suillerot A. Kinetic analysis of calcein and calcein-acetoxymethylester efflux mediated by the multidrug resistance protein and P-glycoprotein. Biochemistry 1998;37:2243-50.
17. Livak KJ. Allelic discrimination using fluorogenic probes and the 5′ nuclease assay. Genet Anal 1999;14:143-9.
18. Radembino N, Poirier JM, Ragueneau I, Jaillon P. Improved sensitivity of digoxin assay by modification of the EMIT 2000 method. Ther Drug Monit 1999;21:256-8.
19. 3H]verapamil radioligand-binding assay. J Pharmacol Exp Ther 1999;288:348-57.
20. Lan LB, Ayesh S, Lyubimov E, Pashinsky I, Stein WD. Kinetic parameters for reversal of the multidrug pump as measured for drug accumulation and cell killing. Cancer Chemother Pharmacol 1996;38:181-90.
21. Bigger JT Jr, Leahey EB Jr. Quinidine and digoxin. An important interaction. Drugs 1982;24:229-39.
22. Latham TB, Prato FS, Wisenberg G, Reese L. Effects of dipyridamole infusion on human renal function observed using technetium-99m-DTPA. J Nucl Med 1992;33:355-8.
23. Sansoe G, Ferrari A, D'Alimonte P, Trenti T, Zoboli P, Romagnoli R, et al. Beneficial hemodynamic effects of dipyridamole on portal circulation in cirrhosis. Am J Gastroenterol 1998;93:429-33.
24. Chiou WL, Chung SM, Wu TC, Ma C. A comprehensive account on the role of efflux transporters in the gastrointestinal absorption of 13 commonly used substrate drugs in humans. Int J Clin Pharmacol Ther 2001;39:93-101.
25. Kohne CH, Hiddemann W, Schuller J, Weiss J, Lohrmann HP, Schmitz-Hubner U, et al. Failure of orally administered dipyridamole to enhance the antineoplastic activity of fluorouracil in combination with leucovorin in patients with advanced colorectal cancer: a prospective randomized trial. J Clin Oncol 1995;13:1201-8.
26. Leveque D, Jehl F. P-glycoprotein and pharmacokinetics. Anticancer Res 1995;15:331-6.
27. Leahey EB Jr, Bigger JT Jr, Butler VP Jr, Reiffel JA, O'Connell GC, Scaffidi LE, et al. Quinidine-digoxin interaction: time course and pharmacokinetics. Am J Cardiol 1981;48:1141-6.
28. 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.
29. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, et al. Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology 2001;120:525-33.
30. Dresser G, Bailey D, Leake B, Schwarz U, Dawson P, Freeman D, et al. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 2002;71:11-20.