Effect of zolpidem on human cytochrome P450 activity, and on transport mediated by P-glycoprotein

Biopharmaceutics and Drug Disposition

Volumn 23, Issue 9, 2002, Pages 361-367

  von Moltke, Lisa L ^a,b   Weemhoff, James L ^a   Perloff, Michael D ^a   Hesse, Leah M ^a   Harmatz, Jerold S ^a   Roth Schechter, Barbara F ^c   Greenblatt, David J ^a,b  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b TUFTS MEDICAL CENTER   (United States)

^c Boston Res and Science Consulting   (United States)

Author keywords

Cytochromes P450; Drug interactions; P glycoprotein; Rhodamine 123; Zolpidem

Indexed keywords

ANALGESIC AGENT; ANTIDEPRESSANT AGENT; ANTINEOPLASTIC AGENT; ANTIRETROVIRUS AGENT; CARRIER PROTEIN; CYTOCHROME P450; GLYCOPROTEIN P; KETOCONAZOLE; OPIATE; RHODAMINE 123; RITONAVIR; TRIAZOLAM; VERAPAMIL; ZOLPIDEM;

ARTICLE; CELL CULTURE; CELL LINE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFECT; DRUG METABOLISM; DRUG TRANSPORT; ENZYME ACTIVITY; HUMAN; HUMAN CELL; INTESTINE CELL; LIVER MICROSOME;

BIOLOGICAL TRANSPORT, ACTIVE; CELLS, CULTURED; CYTOCHROME P-450 ENZYME SYSTEM; HUMANS; ISOENZYMES; MICROSOMES, LIVER; P-GLYCOPROTEIN; PYRIDINES; RHODAMINE 123;

EID: 0036903751     PISSN: 01422782     EISSN: None     Source Type: Journal    
DOI: 10.1002/bdd.329     Document Type: Article

References (58)

1. Ochitill H, Dilley J, Kohlwes J. Psychotropic-drug prescribing for hospitalized-patients with acquired-immunodeficiency-syndrome. Am J Med 1991; 90: 601-605.
2. Rubinstein ML, Selwyn PA. High prevalence of insomnia in an outpatient population with HIV infection. J Acquired Immune Deficiency Syndromes 1998; 19: 260-265.
3. Ayuso JL. Use of psychotropic drugs in patients with HIV infection. Drugs 1994; 47: 599-610.
4. Clarke SE. In vitro assessment of human cytochrome P450. Xenobiotica 1998; 28: 1167-1202.
5. Smith G, Stubbins MJ, Harries LW, Wolf CR. Molecular genetics of the human cytochrome P450 monooxygenase superfamily. Xenobiotica 1998; 28: 1129-1165.
6. Smith DA, Abel SM, Hyland R, Jones BC. Human cytochrome P450s: selectivity and measurement in vivo. Xenobiotica 1998; 28: 1095-1128.
7. Wrighton SA, Stevens JC. The human hepatic cytochromes P450 involved in drug metabolism. Criti Rev Toxicol 1992; 22: 1-21.
8. Guengerich FP. Cytochrome P-450 3A4: regulation and role in drug metabolism. Annu Rev Pharmacol Toxicol 1999; 39: 1-7.
9. Ketter TA, Flockhart DA, Post RM, et al. The emerging role of cytochrome P450 3A in psychopharmacology. J Clin Psychopharmacol 1995; 15: 387-398.
10. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Human drug metabolism and the cytochromes P450: application and relevance of in vitro models. J Clin Pharmacol 2001; 41: 1149-1179.
11. Hunter J, Hirst BH. Intestinal secretion of drugs. The role of P-glycoprotein and related drug efflux systems in limiting oral drug absorption. Adv Drug Delivery Rev 1997; 25: 129-157.
12. Yu DK. The contribution of P-glycoprotein to pharmacokinetic drug-drug interactions. J Clin Pharmacol 1999; 39: 1203-1211.
13. Schuetz EG, Schinkel AH. Drug disposition as determined by the interplay between drug-transporting and drug-metabolizing systems. J Biochem Molecular Toxicol 1999; 13: 219-222.
14. Schinkel AH. P-glycoprotein, a gatekeeper in the blood-brain barrier. Adv Drug Delivery Rev 1999; 36: 179-194.
15. Fromm MF. P-glycoprotein: a defense mechanism limiting oral bioavaflabihty and CNS accumulation of drugs. Int J Clin Pharmacol Ther 2000; 38: 69-74.
16. Rodriguez I, Abernethy DR, Woosley RL. P-glycoprotein in clinical cardiology. Circulation 1999; 99: 472-474.
17. Lo A, Burckart GJ. P-glycoprotein and drug therapy in organ transplantation. J Clin Pharmacol 1999; 39: 995-1005.
18. Wacher VJ, Salphati L, Benet LZ. Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv Drug Delivery Rev 2001; 46: 89-102.
19. Kim RB. Transporters and drug disposition. Curr Opinion Drug Discovery Dev 2000; 3: 94-101.
20. Borst P, Evers R, Kool M, Wijnholds J. A family of drug transporters: the multidrug resistance-associated proteins. J Nat Cancer Inst 2000; 92: 1295-1302.
21. von Moltke LL, Greenblatt DJ, Granda BW, Duan SX, Grassi JM, Venkatakrishnan K, Harmatz JS, Shader RI. Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Br J Clin Pharmacol 1999; 48: 89-97.
22. Greenblatt DJ, von Moltke LL, Harmatz JS, Durol ALB, Daily JP, Graf JA, Mertzanis P, Hoffman JL, Shader RI. Differential impairment of triazolam and zolpidem clearance by ritonavir. J Acquired Immune Deficiency Syndromes 2000; 24: 129-136.
23. Greenblatt DJ, von Moltke LL, Harmatz JS, Mertzanis P, Graf JA, Durol ALB, Counihan M, Roth-Schechter B, Shader RI. Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole. Clin Pharmacol Ther 1998; 64: 661-671.
24. Greenblatt DJ, Wright CE, von Moltke LL, Harmatz JS, Ehrenberg BL, Harrel LM, Corbett K, Counihan M, Tobias S, Shader RI. Ketoconazole inhibition of triazolam and alprazolam clearance: differential kinetic and dynamic consequences. Clin Pharmacol Ther 1998; 64: 237-247.
25. von Moltke LL, Greenblatt DJ, Duan SX, Schmider J, Kudchadker L, Fogelman SM, Harmatz JS, Shader RI. Phenacetin O-deethylation by human liver microsomes in vitro: inhibition by chemical probes, SSRI antidepressants, nefazodone, and venlafaxine. Psychopharmacology 1996; 128: 398-407.
26. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Human cytochromes P450 mediating phenacetin O-deethylation in vitro: validation of the high affinity component as an index of CYP1A2 activity. J Pharm Sci 1998; 87: 1502-1507.
27. Hesse LM, Venkatakrishnan K, Court MH, von Moltke LL, Duan SX, Shader RI, Greenblatt DJ. CYP2B6 mediates the in vitro hydroxylation of bupropion: potential drug interactions with other antidepressants. Drug Metab Dispos 2000; 28: 1176-1183.
28. Hesse LM, von Moltke LL, Shader RI, Greenblatt DJ. Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. Drug Metab Dispos 2001; 29: 100-102.
29. Venkatakrishnan K, von Moltke LL, Court MH, Harmatz JS, Crespi CL, Greenblatt DJ. Comparison between cytochrome P450 (CYP) content and relative activity approaches to scaling from cDNA-expressed CYPs to human liver microsomes: ratios of accessory proteins as sources of discrepancies between the approaches. Drug Metab Dispos 2000; 28: 1493-1504.
30. Giancarlo GM, Venkatakrishnan K, Granda BW, von Moltke LL, Greenblatt DJ. Relative contributions of CYP2C9 and 2C19 to phenytoin 4-hydroxylation in vitro: inhibition by sulfaphenazole, omeprazole and ticlopidine. Eur J Clin Pharmacol 2001; 57: 31-36.
31. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Relative quantities of catalytically active CYP 2C9 and 2C19 in human liver microsomes: application of the relative activity factor approach. J Pharm Sci 1998; 87: 845-853.
32. von Moltke LL, Greenblatt DJ, Grassi JM, Granda BW, Venkatakrishnan K, Schmider J, Harmatz JS, Shader RI. Multiple human cytochromes; contribute to biotransformation of dextromethorphan in vitro: role of CYP2C9, CYP2C19, CYP2D6, and CYP3A. J Pharm Pharmacol 1998; 50: 997-1004.
33. Schmider J, Greenblatt DJ, Fogelman SM, von Moltke LL, Shader RI. Metabolism of dextromethorphan in vitro: involvement of cytochromes P450 2D6, 3A3/4, with a possible role of 2E1. Biopharm Drug Dispos 1997; 18: 227-240.
34. von Moltke LL, Greenblatt DJ, Harmatz JS, Duan SX, Harrel LM, Cotreau-Bibbo MM, Pritchard GA, Wright CE, Shader RI. Triazolam biotransformation by human liver microsomes in vitro: effects of metabolic inhibitors, and clinical confirmation of a predicted interaction with ketoconazole. J Pharmacol Exp Ther 1996; 276: 370-379.
35. von Moltke LL, Greenblatt DJ, Duan SX, Harmatz JS, Shader RI. Inhibition of triazolam hydroxylation by ketoconazole, itraconazole, hydroxyitraconazole and fluconazole in vitro. Pharm Pharmacol Commun 1998; 4: 443-445.
36. Perloff MD, von Moltke LL, Court MH, Kotegawa T, Shader RI, Greenblatt DJ. Midazolam and triazolam biotransformation in mouse and human liver microsomes: relative contribution of CYP3A and CYP2C9 isoforms. J Pharmacol Exp Ther 2000; 292: 618-628.
37. von Moltke LL, Greenblatt DJ, Grassi JM, Granda BW, Duan SX, Fogelman SM, Daily JP, Harmatz JS, Shader RI. Protease inhibitors as inhibitors of human cytochromes P450: high risk associated with ritonavir. J Clin Pharmacol 1998; 38: 106-111.
38. Störmer E, von Moltke LL, Perloff MD, Greenblatt DJ. P-glycoprotein interactions of nefazodone and trazodone in cell culture. J Clin Pharmacol 2001; 41: 708-714.
39. Störmer E, Perloff MD, von Moltke LL, Greenblatt DJ. Methadone inhibits rhodamine123 transport in caco-2 cells. Drug Metab Dispos 2001; 29: 954-956.
40. Perloff MD, von Moltke LL, Marchand JE, Greenblatt DJ. Ritonavir induces P-glycoprotein expression, multidrug resistance-associated protein (MRP1) expression, and drug transporter-mediated activity in a human intestinal cell line. J Pharm Sci 2001; 90: 1829-1837.
41. Hochman JH, Chiba M, Nishime J, Yamazaki M, Lin JH. Influence of P-glycoprotein on the transport and metabolism of indinavir in Caco-2 cells expressing cytochrome P-450 3A4. J Pharmacol Exp Ther 2000; 292: 310-318.
42. Yumoto R, Murakami T, Nakamoto Y, Hasegawa R, Nagai J, Takano M. Transport of rhodamine 123, a P-glycoprotein substrate, across rat intestine and Caco-2 cell monolayers in the presence of cytochrome P-450 3A-related compounds. J Pharmacol Exp Ther 1999; 289: 149-155.
43. Profit L, Eagling VA, Back DJ. Modulation of P-glycoprotein function in human lymphocytes and Caco-2 cell monolayers by HIV-1 protease inhibitors. AIDS 1999; 13: 1623-1627.
44. Dresser GK, Spence JD, Bailey DG. Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition. Clin Pharmacokinet 2000; 38: 41-57.
45. Lin JH, Lu AY. Inhibition and induction of cytochrome P450 and the clinical implications. Clin Pharmacokinet 1998; 35: 361-390.
46. Thummel KE, Wilkinson GR. In vitro and in vivo drug interactions involving human CYP3A. Annu Rev Pharmacol Toxicol 1998; 38: 389-430.
47. Pelkonen O, Mäenpää J, Taavitsainen P, Rautio A, Raunio H. Inhibition and induction of human cytochrome P450 (CYP) enzymes. Xenobiotica 1998; 28: 1203-1253.
48. Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, Sugiyama Y. Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 1998; 50: 387-412.
49. Bertz RJ, Granneman GR. Use of in vitro and in vivo data to estimate the likelihood of metabolic pharmacokinetic interactions. Clin Pharmacokinet 1997; 32: 210-258.
50. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Effects of the antifungal agents on oxidative drug metabolism in humans: clinical relevance. Clin Pharmacokinet 2000; 38: 111-180.
51. von Moltke LL, Greenblatt DJ, Schmider J, Wright CE, Harmatz JS, Shader RI. In vitro approaches to predicting drug interactions in vivo. Biochem Pharmacol 1998; 55: 113-122.
52. Salvà P, Costa J. Clinical pharmacokinetics and pharmacodynamics of zolpidem: therapeutic implications. Clin Pharmacokinetics 1995; 29: 142-153.
53. Thénot JP, Hermann P, Durand A, et al. Pharmacokinetics and metabolism of zolpidem in various animal species and in humans. In Sauvanet JP, Langer SZ, Morselli PL. (eds), vol. 6. Imidazopyridines in Sleep Disorders: a Novel Experimental and Therapeutic Approach. Raven Press: New York, 1988; 139-153.
54. Sadeque AJ, Wandel C, He H, Shah S, Wood AJ. Increased drug delivery to the brain by P-glycoprotein inhibition. Clin Pharmacol Ther 2000; 68: 231-237.
55. 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: 552-557.
56. Boyd RA, Stern RH, Stewart BH, Wu X, Reyner EL, Zegarac EA, Randinitis EJ, Whitfield L. Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P-glycoprotein-mediated secretion. J Clin Pharmacol 2000; 40: 91-98.
57. Schwartz JB, Migliore PJ. Effect of nifedipine on serum digoxin concentration and renal digoxin clearance. Clin Pharmacol Ther 1984; 36: 19-24.
58. Merry C, Barry MG, Mulcahy F, Ryan M, Heavey J, Tjia JF, Gibbons SE, Breckenridge AM, Back DJ. Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients. AIDS 1997; 11: F29-F33.