Complex drug interactions of the HIV protease inhibitors 3: Effect of simultaneous or staggered dosing of digoxin and ritonavir, nelfinavir, rifampin, or bupropion

Drug Metabolism and Disposition

Volumn 40, Issue 3, 2012, Pages 610-616

  Kirby, Brian J ^a   Collier, Ann C ^a   Kharasch, Evan D ^b   Whittington, Dale ^a   Thummel, Kenneth E ^a   Unadkat, Jashvant D ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

^b WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMFEBUTAMONE; DIGOXIN; NELFINAVIR; RIFAMPICIN; RITONAVIR;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG HALF LIFE; DRUG POTENTIATION; FEMALE; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; KIDNEY CLEARANCE; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PRIORITY JOURNAL; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADULT; BUPROPION; DIGOXIN; DRUG ADMINISTRATION SCHEDULE; DRUG INTERACTIONS; FEMALE; HIV PROTEASE INHIBITORS; HUMANS; MALE; NELFINAVIR; P-GLYCOPROTEINS; RIFAMPIN; RITONAVIR;

EID: 84857384372     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.042705     Document Type: Article

References (27)

1. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, and Unadkat JD (2007) Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos 35:1853-1859. (Pubitemid 47481578)
2. Drescher S, Glaeser H, Mürdter T, Hitzl M, Eichelbaum M, and Fromm MF (2003) P-glycoprotein-mediated intestinal and biliary digoxin transport in humans. Clin Pharmacol Ther 73:223-231. (Pubitemid 36269673)
3. Dussault I, Lin M, Hollister K, Wang EH, Synold TW, and Forman BM (2001) Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J Biol Chem 276:33309-33312.
4. Endres CJ, Hsiao P, Chung FS, and Unadkat JD (2006) The role of transporters in drug interactions. Eur J Pharm Sci 27:501-517. (Pubitemid 43363341)
5. Evered DC (1972) The binding of digoxin by the serum proteins. Eur J Pharmacol 18:236-244.
6. Frötschl R, Chichmanov L, Kleeberg U, Hildebrandt AG, Roots I, and Brockmöller J (1998) Prediction of aryl hydrocarbon receptor-mediated enzyme induction of drugs and chemicals by mRNA quantification. Chem Res Toxicol 11:1447-1452.
7. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, and Kroemer HK (1999) The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest 104:147-153.
8. Gupta A, Mugundu GM, Desai PB, Thummel KE, and Unadkat JD (2008) Intestinal human colon adenocarcinoma cell line LS180 is an excellent model to study pregnane X receptor, but not constitutive androstane receptor, mediated CYP3A4 and multidrug resistance transporter 1 induction: studies with anti-human immunodeficiency virus protease inhibitors. Drug Metab Dispos 36:1172-1180. (Pubitemid 351717476)
9. Hsiao P, Bui T, Ho RJ, and Unadkat JD (2008) In vitro-to-in vivo prediction of P-glycoprotein-based drug interactions at the human and rodent blood-brain barrier. Drug Metab Dispos 36:481-484. (Pubitemid 351397990)
10. Josephson F (2010) Drug-drug interactions in the treatment of HIV infection: focus on pharmacokinetic enhancement through CYP3A inhibition. J Intern Med 268:530-539.
11. Kharasch ED, Bedynek PS, Walker A, Whittington D, and Hoffer C (2008) Mechanism of ritonavir changes in methadone pharmacokinetics and pharmacodynamics: II. Ritonavir effects on CYP3A and P-glycoprotein activities. Clin Pharmacol Ther 84:506-512.
12. Kharasch ED, Walker A, Whittington D, Hoffer C, and Bedynek PS (2009) Methadone metabolism and clearance are induced by nelfinavir despite inhibition of cytochrome P4503A (CYP3A) activity. Drug Alcohol Depend 101:158-168.
13. Kimoto E, Chupka J, Xiao Y, Bi YA, and Duignan DB (2011) Characterization of digoxin uptake in sandwich-cultured human hepatocytes. Drug Metab Dispos 39:47-53.
14. Kirby B, Kharasch ED, Thummel KT, Narang VS, Hoffer CJ, and Unadkat JD (2006) Simultaneous measurement of in vivo P-glycoprotein and cytochrome P450 3A activities. J Clin Pharmacol 46:1313-1319. (Pubitemid 44564360)
15. Kirby BJ, Collier AC, Kharasch ED, Dixit V, Desai P, Whittington D, Thummel KE, and Unadkat JD (2011a) Complex drug interactions of HIV protease inhibitors 2: in vivo induction and in vitro to in vivo correlation of induction of cytochrome P450 1A2, 2B6, and 2C9 by ritonavir or nelfinavir. Drug Metab Dispos 39:2329-2337.
16. Kirby BJ, Collier AC, Kharasch ED, Whittington D, Thummel KE, and Unadkat JD (2011b) Complex drug interactions of HIV protease inhibitors 1: inactivation, induction, and inhibition of cytochrome P450 3A by ritonavir or nelfinavir. Drug Metab Dispos 39:1070-1078.
17. Kirby BJ, Kalhorn T, Hebert M, Easterling T, and Unadkat JD (2008) Sensitive and specific LC-MS assay for quantification of digoxin in human plasma and urine. Biomed Chromatogr 22:712-718.
18. Lai AA and Schroeder DH (1983) Clinical pharmacokinetics of bupropion: a review. J Clin Psychiatry 44:82-84. (Pubitemid 13088842)
19. Laizure SC, DeVane CL, Stewart JT, Dommisse CS, and Lai AA (1985) Pharmacokinetics of bupropion and its major basic metabolites in normal subjects after a single dose. Clin Pharmacol Ther 38:586-589. (Pubitemid 16193901)
20. Lam JL, Shugarts SB, Okochi H, and Benet LZ (2006) Elucidating the effect of final-day dosing of rifampin in induction studies on hepatic drug disposition and metabolism. J Pharmacol Exp Ther 319:864-870.
21. Lau YY, Huang Y, Frassetto L, and Benet LZ (2007) effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clin Pharmacol Ther 81:194-204. (Pubitemid 46174816)
22. Penzak SR, Shen JM, Alfaro RM, Remaley AT, Natarajan V, and Falloon J (2004) Ritonavir decreases the nonrenal clearance of digoxin in healthy volunteers with known MDR1 genotypes. Ther Drug Monit 26:322-330. (Pubitemid 38703022)
23. Reitman ML, Chu X, Cai X, Yabut J, Venkatasubramanian R, Zajic S, Stone JA, Ding Y, Witter R, Gibson C, et al. (2011) Rifampin's acute inhibitory and chronic inductive drug interactions: experimental and model-based approaches to drug-drug interaction trial design. Clin Pharmacol Ther 89:234-242.
24. Soldner A, Christians U, Susanto M, Wacher VJ, Silverman JA, and Benet LZ (1999) Grapefruit juice activates P-glycoprotein-mediated drug transport. Pharm Res 16:478-485. (Pubitemid 29191290)
25. Taub ME, Mease K, Sane RS, Watson CA, Chen L, Ellens H, Hirakawa B, Reyner EL, Jani M, and Lee CA (2011) Digoxin is not a substrate for organic anion-transporting polypeptide transporters OATP1A2, OATP1B1, OATP1B3, and OATP2B1 but is a substrate for a sodium-dependent transporter expressed in HEK293 cells. Drug Metab Dispos 39:2093-2102.
26. Tirona RG, Leake BF, Wolkoff AW, and Kim RB (2003) Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. J Pharmacol Exp Ther 304:223-228. (Pubitemid 36008932)
27. Unadkat JD and Wang Y (2000) Protease inhibitors, in Metabolic Drug Interactions (Levy RH et al eds) pp 647-652, Lippincott Williams & Wilkins, Philadelphia.