Rifampin's acute inhibitory and chronic inductive drug interactions: Experimental and model-based approaches to drug-drug interaction trial design

Clinical Pharmacology and Therapeutics

Volumn 89, Issue 2, 2011, Pages 234-242

  Reitman, M L ^a   Chu, X ^a   Cai, X ^a   Yabut, J ^a   Venkatasubramanian, R ^a   Zajic, S ^a   Stone, J A ^a   Ding, Y ^a   Witter, R ^a   Gibson, C ^a   Roupe, K ^b   Evers, R ^a   Wagner, J A ^a   Stoch, A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b MDS Inc   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 3A4; DIGOXIN; MIDAZOLAM; RIFAMPICIN;

ADULT; AREA UNDER THE CURVE; ARTICLE; CELL ISOLATION; DRUG CONCENTRATION; DRUG EFFECT; DRUG HALF LIFE; DRUG INHIBITION; DRUG METABOLISM; DRUG TRANSPORT; DRUG WITHDRAWAL; GENETIC TRANSFECTION; HUMAN; HUMAN EXPERIMENT; IC 50; LIVER CELL; MALE; NORMAL HUMAN; PRIORITY JOURNAL;

ADULT; AREA UNDER CURVE; BIOLOGICAL TRANSPORT; DIGOXIN; DRUG INTERACTIONS; HUMANS; MALE; MIDAZOLAM; MIDDLE AGED; MODELS, BIOLOGICAL; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; P-GLYCOPROTEIN; RESEARCH DESIGN; RIFAMPIN;

EID: 78951479924     PISSN: 00099236     EISSN: 15326535     Source Type: Journal    
DOI: 10.1038/clpt.2010.271     Document Type: Article

References (47)

1. Zhang, L., Reynolds, K.S., Zhao, P. & Huang, S.M. Drug interactions evaluation: an integrated part of risk assessment of therapeutics. Toxicol. Appl. Pharmacol. 243, 134-145 (2010).
2. Yuan, R., Flockhart, D.A. & Balian, J.D. Pharmacokinetic and pharmacodynamic consequences of metabolism-based drug interactions with alprazolam, Midazolam, And triazolam. J. Clin. Pharmacol. 39, 1109-1125 (1999).
3. Greiner, B.et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J. Clin. Invest. 104, 147-153 (1999).
4. Drescher, S., Glaeser, H., Mürdter, T., Hitzl, M., Eichelbaum, M. & fromm, M.F. P-glycoprotein-mediated intestinal and biliary digoxin transport in humans. Clin. Pharmacol. Ther. 73, 223-231 (2003).
5. Willson, T.M. & Kliewer, S.A. PXR, CaR and drug metabolism. Nat. Rev. Drug Discov. 1, 259-266 (2002).
6. Chu, V.et al. In vitro and in vivo induction of cytochrome p450: a survey of the current practices and recommendations: a Pharmaceutical Research and Manufacturers of america perspective. Drug Metab. Dispos. 37, 1339-1354 (2009).
7. Baciewicz, A.M., Chrisman, C.R., Finch, C.K. & Self, T.H. Update on rifampin and rifabutin drug interactions. Am. J. Med. Sci. 335, 126-136 (2008).
8. Prueksaritanont, T.et al. Simvastatin does not affect CyP3a activity, Quantified by the erythromycin breath test and oral midazolam pharmacokinetics, In healthy male subjects. J. Clin. Pharmacol. 40, 1274-1279 (2000).
9. Lam, J.L., Shugarts, S.B., Okochi, H. & Benet, L.Z. Elucidating the effect of finalday dosing of rifampin in induction studies on hepatic drug disposition and metabolism. J. Pharmacol. Exp. Ther. 319, 864-870 (2006).
10. Peloquin, C.A., Jaresko, G.S., Yong, C.L., Keung, A.C., Bulpitt, A.E. & Jelliffe, R.W. Population pharmacokinetic modeling of isoniazid, Rifampin, And pyrazinamide. Antimicrob. Agents Chemother. 41, 2670-2679 (1997).
11. Kullak-Ublick, G.A.et al. Organic anion-transporting polypeptide B (OaTP-B) and its functional comparison with three other OaTPs of human liver. Gastroenterology 120, 525-533 (2001).
12. Kirby, B., Kharasch, E.D., Thummel, K.T., Narang, V.S., Hoffer, C.J. & Unadkat, J.D. Simultaneous measurement of in vivo P-glycoprotein and cytochrome P450 3a activities. J. Clin. Pharmacol. 46, 1313-1319 (2006).
13. Larsen, U.L.et al. Human intestinal P-glycoprotein activity estimated by the model substrate digoxin. Scand. J. Clin. Lab. Invest. 67, 123-134 (2007).
14. Koup, J.R., Greenblatt, D.J., Jusko, W.J., Smith, T.W. & Koch-Weser, J. Pharmacokinetics of digoxin in normal subjects after intravenous bolus and infusion doses. J. Pharmacokinet. Biopharm. 3, 181-192 (1975).
15. Yang, J.et al. Cytochrome p450 turnover: regulation of synthesis and degradation, Methods for determining rates, And implications for the prediction of drug interactions. Curr. Drug Metab. 9, 384-394 (2008).
16. Bertalanffy, F.D. & Nagy, K.P. Mitotic activity and renewal rate of the epithelial cells of human duodenum. Acta Anat. (Basel). 45, 362-370 (1961).
17. Lipkin, M., Bell, B. & Sherlock, P. Cell Proliferation Kinetics in the Gastrointestinal Tract of Man. I. Cell Renewal in Colon and Rectum. J. Clin. Invest. 42, 767-776 (1963).
18. Branch, R.A. & Herman, R.J. Enzyme induction and beta-adrenergic receptor blocking drugs. Br. J. Clin. Pharmacol. 17 (suppl. 1), 77S-84S (1984).
19. Lee, K.H.et al. Time course of the changes in prednisolone pharmacokinetics after co-administration or discontinuation of rifampin. Eur. J. Clin. Pharmacol. 45, 287-289 (1993).
20. Imai, H.et al. The recovery time-course of CyP3a after induction by St John's wort administration. Br. J. Clin. Pharmacol. 65, 701-707 (2008).
21. Magnusson, M.O., Dahl, M.L., Cederberg, J., Karlsson, M.O. & Sandström, R. Pharmacodynamics of carbamazepine-mediated induction of CyP3a4, CyP1a2, And Pgp as assessed by probe substrates midazolam, Caffeine, And digoxin. Clin. Pharmacol. Ther. 84, 52-62 (2008).
22. Vavricka, S.R., Van Montfoort, J., Ha, H.R., Meier, P.J. & fattinger, K. Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 36, 164-172 (2002).
23. Tirona, R.G., Leake, B.F., Wolkoff, A.W. & Kim, R.B. Human organic anion transporting polypeptide-C (SLC21a6) is a major determinant of rifampinmediated pregnane X receptor activation. J. Pharmacol. Exp. Ther. 304, 223-228 (2003).
24. Letschert, K., Faulstich, H., Keller, D. & Keppler, D. Molecular characterization and inhibition of amanitin uptake into human hepatocytes. Toxicol. Sci. 91, 140-149 (2006).
25. Lau, Y.Y., Huang, Y., Frassetto, L. & Benet, L.Z. Effect of OaTP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clin. Pharmacol. Ther. 81, 194-204 (2007).
26. Seward, D.J., Koh, A.S., Boyer, J.L. & Ballatori, N. Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J. Biol. Chem. 278, 27473-27482 (2003).
27. Kodawara, T.et al. Organic anion transporter oatp2-mediated interaction between digoxin and amiodarone in the rat liver. Pharm. Res. 19, 738-743 (2002).
28. Mikkaichi, T.et al. Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc. Natl. Acad. Sci. USA 101, 3569-3574 (2004).
29. Furusawa, S., Nakano, S., Wu, J., Sasaki, K., Takayanagi, M. & Takayanagi, Y. Potentiation of pirarubicin activity in multidrug resistant cells by rifampicin. Biol. Pharm. Bull. 20, 1303-1306 (1997).
30. Fardel, O., Lecureur, V., Loyer, P. & Guillouzo, A. Rifampicin enhances anticancer drug accumulation and activity in multidrug-resistant cells. Biochem. Pharmacol. 49, 1255-1260 (1995).
31. Courtois, A., Payen, L., Vernhet, L., De Vries, E.G., Guillouzo, A. & fardel, O. Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells. Cancer Lett. 139, 97-104 (1999).
32. Zong, J. & Pollack, G.M. Modulation of P-glycoprotein transport activity in the mouse blood-brain barrier by rifampin. J. Pharmacol. Exp. Ther. 306, 556-562 (2003).
33. Yao, H.M. & Chiou, W.L. The complexity of intestinal absorption and exsorption of digoxin in rats. Int. J. Pharm. 322, 79-86 (2006).
34. Zhang, L., Zhang, Y.D., Strong, J.M., Reynolds, K.S. & Huang, S.M. A regulatory viewpoint on transporter-based drug interactions. Xenobiotica. 38, 709-724 (2008).
35. Stone, J.A.et al. Potential for interactions between caspofungin and nelfinavir or rifampin. Antimicrob. Agents Chemother. 48, 4306-4314 (2004).
36. Oswald, S.et al. Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, An inhibitor of multidrug transport proteins. Clin. Pharmacol. Ther. 80, 477-485 (2006).
37. Backman, J.T., Luurila, H., Neuvonen, M. & Neuvonen, P.J. Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites. Clin. Pharmacol. Ther. 78, 154-167 (2005).
38. He, Y.J.et al. Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin. Chim. Acta 405, 49-52 (2009).
39. Xiong, H.et al. Dual effects of rifampin on the pharmacokinetics of atrasentan. J. Clin. Pharmacol. 47, 423-429 (2007).
40. Van Giersbergen, P.L., Treiber, A., Schneiter, R., Dietrich, H. & Dingemanse, J. Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjects. Clin. Pharmacol. Ther. 81, 414-419 (2007).
41. Zheng, H.X., Huang, Y., Frassetto, L.A. & Benet, L.Z. Elucidating rifampin's inducing and inhibiting effects on glyburide pharmacokinetics and blood glucose in healthy volunteers: unmasking the differential effects of enzyme induction and transporter inhibition for a drug and its primary metabolite. Clin. Pharmacol. Ther. 85, 78-85 (2009).
42. Kyrklund, C., Backman, J.T., Neuvonen, M. & Neuvonen, P.J. Effect of rifampicin on pravastatin pharmacokinetics in healthy subjects. Br. J. Clin. Pharmacol. 57, 181-187 (2004).
43. Deng, S.et al. Effects of a concomitant single oral dose of rifampicin on the pharmacokinetics of pravastatin in a two-phase, Randomized, Single-blind, Placebo-controlled, Crossover study in healthy Chinese male subjects. Clin. Ther. 31, 1256-1263 (2009).
44. Bidstrup, T.B., Stilling, N., Damkier, P., Scharling, B., Thomsen, M.S. & Brøsen, K. Rifampicin seems to act as both an inducer and an inhibitor of the metabolism of repaglinide. Eur. J. Clin. Pharmacol. 60, 109-114 (2004).
45. Golstein, P.E., Boom, A., Van Geffel, J., Jacobs, P., Masereel, B. & Beauwens, R. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 437, 652-660 (1999).
46. Hochman, J.H.et al. Interactions of human P-glycoprotein with simvastatin, Simvastatin acid, And atorvastatin. Pharm. Res. 21, 1686-1691 (2004).
47. Kramer, W.G.et al. Pharmacokinetics of digoxin: comparison of a two- and a three-compartment model in man. J. Pharmacokinet. Biopharm. 2, 299-312 (1974).