Geneva cocktail for cytochrome P450 and P-glycoprotein activity assessment using dried blood spots

Clinical Pharmacology and Therapeutics

Volumn 96, Issue 3, 2014, Pages 349-359

  Bosilkovska, M ^a   Samer, C F ^a,b   Deglon J ^c   Rebsamen, M ^a   Staub, C ^c   Dayer, P ^a,b   Walder, B ^a   Desmeules, J A ^a,b   Daali, Y ^a,b  

^a GENEVA UNIVERSITY HOSPITALS   (Switzerland)

^b Swiss Centre for Applied Human Toxicology   (Switzerland)

^c UNIVERSITY CENTER OF LEGAL MEDICINE   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

AMFEBUTAMONE; CYTOCHROME P450; DEXTROMETHORPHAN; FEXOFENADINE; FLURBIPROFEN; FLUVOXAMINE; MIDAZOLAM; MULTIDRUG RESISTANCE PROTEIN; OMEPRAZOLE; QUINIDINE; RIFAMPICIN; VORICONAZOLE;

AREA UNDER THE CURVE; ARTICLE; CAPILLARY BLOOD; CLINICAL RESEARCH; DRIED BLOOD SPOT TESTING; LIQUID CHROMATOGRAPHY; LOW DRUG DOSE; PHENOTYPE; PRIORITY JOURNAL; SAMPLING; SINGLE NUCLEOTIDE POLYMORPHISM; TANDEM MASS SPECTROMETRY;

ADMINISTRATION, ORAL; ADULT; BUPROPION; CAFFEINE; CAPSULES; CARBONATED BEVERAGES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CHROMATOGRAPHY, REVERSE-PHASE; COFFEE; CYTOCHROME P-450 ENZYME SYSTEM; DEXTROMETHORPHAN; DRIED BLOOD SPOT TESTING; ENZYME INHIBITORS; FEASIBILITY STUDIES; FLURBIPROFEN; HUMANS; ISOENZYMES; MALE; MIDAZOLAM; OMEPRAZOLE; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS; PHENOTYPE; PILOT PROJECTS; PREDICTIVE VALUE OF TESTS; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; SUBSTRATE SPECIFICITY; TANDEM MASS SPECTROMETRY; TERFENADINE; YOUNG ADULT;

EID: 84907874975     PISSN: 00099236     EISSN: 15326535     Source Type: Journal    
DOI: 10.1038/clpt.2014.83     Document Type: Article

References (49)

1. Konig, J., Muller, F. & Fromm, M.F. Transporters and drug-drug interactions: Important determinants of drug disposition and effects. Pharmacol Rev. 65, 944-966 (2013).
2. Chainuvati, S. et al. Combined phenotypic assessment of cytochrome p450 1A2, 2C9, 2C19, 2D6, and 3A, N-Acetyltransferase-2, and xanthine oxidase activities with the 'Cooperstown 5'1 cocktail. Clin. Pharmacol. Ther. 74, 437-447 (2003).
3. Ryu, J.Y. et al. Development of the 'Inje cocktail for high-Throughput evaluation of five human cytochrome P450 isoforms in vivo. Clin. Pharmacol. Ther. 82, 531-540 (2007).
4. Turpault, S. et al. Pharmacokinetic assessment of a five-probe cocktail for CYPs 1A2, 2C9, 2C19, 2D6 and 3A. Br. J. Clin. Pharmacol. 68, 928-935 (2009).
5. Christensen, M. et al. The Karolinska cocktail for phenotyping of five human cytochrome P450 enzymes. Clin. Pharmacol. Ther. 73, 517-528 (2003).
6. Zgheib, N.K., Frye, R.F., Tracy, T.S., Romkes, M. & Branch, R.A. Validation of incorporating flurbiprofen into the Pittsburgh cocktail. Clin. Pharmacol. Ther. 80, 257-263 (2006).
7. Dumond, J.B. et al. A phenotype-genotype approach to predicting CYP450 and P-glycoprotein drug interactions with the mixed inhibitor/inducer tipranavir/ritonavir. Clin. Pharmacol. Ther. 87, 735-742 (2010).
8. Pedersen, R.S., Damkier, P., Christensen, M.M. & Brosen, K. A cytochrome P450 phenotyping cocktail causing unexpected adverse reactions in female volunteers. Eur. J. Clin. Pharmacol. 69, 1997-1999 (2013).
9. Deglon, J., Lauer, E., Thomas, A., Mangin, P. & Staub, C. Use of the dried blood spot sampling process coupled with fast gas chromatography and negativeion chemical ionization tandem mass spectrometry: Application to fluoxetine, norfluoxetine, reboxetine, and paroxetine analysis. Anal. Bioanal. Chem. 396, 2523-2532 (2010).
10. Patel, P. et al. Dried blood spots and sparse sampling: A practical approach to estimating pharmacokinetic parameters of caffeine in preterm infants. Br. J. Clin. Pharmacol. 75, 805-813 (2013).
11. van der Elst, K.C. et al. Dried blood spot analysis suitable for therapeutic drug monitoring of voriconazole, fluconazole, and posaconazole. Antimicrob. Agents Chemother. 57, 4999-5004 (2013).
12. Daali, Y. et al. Oral flurbiprofen metabolic ratio assessment using a single-point dried blood spot. Clin. Pharmacol. Ther. 91, 489-496 (2012).
13. de Boer, T. et al. Application of dried blood spot sampling combined with LC-MS/MS for genotyping and phenotyping of CYP450 enzymes in healthy volunteers. Biomed. Chromatogr. 25, 1112-1123 (2011).
14. Ullmann, A.J. Review of the safety, tolerability, and drug interactions of the new antifungal agents caspofungin and voriconazole. Curr. Med. Res. Opin. 19, 263-271 (2003).
15. Bosilkovska, M. et al. Simultaneous LC-MS/MS quantification of P-glycoprotein and cytochrome P450 probe substrates and their metabolites in DBS and plasma. Bioanalysis 6, 151-164 (2014).
16. Fuhr, U., Jetter, A. & Kirchheiner, J. Appropriate phenotyping procedures for drug metabolizing enzymes and transporters in humans and their simultaneous use in the 'cocktail approach. Clin. Pharmacol. Ther. 81, 270-283 (2007).
17. Emmons, G. & Rowland, M. Pharmacokinetic considerations as to when to use dried blood spot sampling. Bioanalysis 2, 1791-1796 (2010).
18. Culm-Merdek, K.E., von Moltke, L.L., Harmatz, J.S. & Greenblatt, D.J. Fluvoxamine impairs single-dose caffeine clearance without altering caffeine pharmacodynamics. Br. J. Clin. Pharmacol. 60, 486-493 (2005).
19. Jeppesen, U., Gram, L.F., Vistisen, K., Loft, S., Poulsen, H.E. & Brøsen, K. Dosedependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine. Eur. J. Clin. Pharmacol. 51, 73-78 (1996).
20. Kanebratt, K.P. et al. Cytochrome P450 induction by rifampicin in healthy subjects: Determination using the Karolinska cocktail and the endogenous CYP3A4 marker 4beta-hydroxycholesterol. Clin. Pharmacol. Ther. 84, 589-594 (2008).
21. Backman, J.T., Granfors, M.T. & Neuvonen, P.J. Rifampicin is only a weak inducer of CYP1A2-mediated presystemic and systemic metabolism: Studies with tizanidine and caffeine. Eur. J. Clin. Pharmacol. 62, 451-461 (2006).
22. Mo, S.L., Liu, Y.H., Duan, W., Wei, M.Q., Kanwar, J.R. & Zhou, S.F. Substrate specificity, regulation, and polymorphism of human cytochrome P450 2B6. Curr. Drug Metab. 10, 730-753 (2009).
23. Loboz, K.K. et al. Cytochrome P450 2B6 activity as measured by bupropion hydroxylation: Effect of induction by rifampin and ethnicity. Clin. Pharmacol. Ther. 80, 75-84 (2006).
24. Palovaara, S., Pelkonen, O., Uusitalo, J., Lundgren, S. & Laine, K. Inhibition of cytochrome P450 2B6 activity by hormone replacement therapy and oral contraceptive as measured by bupropion hydroxylation. Clin. Pharmacol. Ther. 74, 326-333 (2003).
25. European Medicines Agency. Guideline on the Investigation of Drug Interactions. (2012).
26. Liu, P., Foster, G., LaBadie, R.R., Gutierrez, M.J. & Sharma, A. Pharmacokinetic interaction between voriconazole and efavirenz at steady state in healthy male subjects. J. Clin. Pharmacol. 48, 73-84 (2008).
27. Zgheib, N.K., Frye, R.F., Tracy, T.S., Romkes, M. & Branch, R.A. Evaluation of flurbiprofen urinary ratios as in vivo indices for CYP2C9 activity. Br. J. Clin. Pharmacol. 63, 477-487 (2007).
28. Inui, N. et al. Chronological effects of rifampicin discontinuation on cytochrome P450 activity in healthy Japanese volunteers, using the cocktail method. Clin. Pharmacol. Ther. 94, 702-708 (2013).
29. Niioka, T., Uno, T., Sugimoto, K., Sugawara, K., Hayakari, M. & Tateishi, T. Estimation of CYP2C19 activity by the omeprazole hydroxylation index at a single point in time after intravenous and oral administration. Eur. J. Clin. Pharmacol. 63, 1031-1038 (2007).
30. Frank, D., Jaehde, U. & Fuhr, U. Evaluation of probe drugs and pharmacokinetic metrics for CYP2D6 phenotyping. Eur. J. Clin. Pharmacol. 63, 321-333 (2007).
31. Borges, S., Li, L., Hamman, M.A., Jones, D.R., Hall, S.D. & Gorski, J.C. Dextromethorphan to dextrorphan urinary metabolic ratio does not reflect dextromethorphan oral clearance. Drug Metab. Dispos. 33, 1052-1055 (2005).
32. Tamminga, W.J. et al. An optimized methodology for combined phenotyping and genotyping on CYP2D6 and CYP2C19. Eur. J. Clin. Pharmacol. 57, 143-146 (2001).
33. Chaobal, H.N. & Kharasch, E.D. Single-point sampling for assessment of constitutive, induced, and inhibited cytochrome P450 3A activity with alfentanil or midazolam. Clin. Pharmacol. Ther. 78, 529-539 (2005).
34. Eap, C.B. et al. Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity. Eur. J. Clin. Pharmacol. 60, 237-246 (2004).
35. Saari, T.I., Laine, K., Leino, K., Valtonen, M., Neuvonen, P.J. & Olkkola, K.T. Effect of voriconazole on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Clin. Pharmacol. Ther. 79, 362-370 (2006).
36. Backman, J.T., Kivistö, K.T., Olkkola, K.T. & Neuvonen, P.J. The area under the plasma concentration-Time curve for oral midazolam is 400-fold larger during treatment with itraconazole than with rifampicin. Eur. J. Clin. Pharmacol. 54, 53-58 (1998).
37. Hamman, M.A., Bruce, M.A., Haehner-Daniels, B.D. & Hall, S.D. The effect of rifampin administration on the disposition of fexofenadine. Clin. Pharmacol. Ther. 69, 114-121 (2001).
38. US Food and Drug Administration. Drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations. (2012).
39. Kirchheiner, J. et al. Bupropion and 4-OH-bupropion pharmacokinetics in relation to genetic polymorphisms in CYP2B6. Pharmacogenetics 13, 619-626 (2003).
40. Lasker, J.M., Wester, M.R., Aramsombatdee, E. & Raucy, J.L. Characterization of CYP2C19 and CYP2C9 from human liver: Respective roles in microsomal tolbutamide, S-mephenytoin, and omeprazole hydroxylations. Arch. Biochem. Biophys. 353, 16-28 (1998).
41. Streetman, D.S., Bertino, J.S. Jr & Nafziger, A.N. Phenotyping of drugmetabolizing enzymes in adults: A review of in-vivo cytochrome P450 phenotyping probes. Pharmacogenetics 10, 187-216 (2000).
42. Bosilkovska, M., Clément, M., Dayer, P., Desmeules, J. & Daali, Y. Incorporation of flurbiprofen in a 4-drug cytochrome P450 phenotyping cocktail. Basic Clin. Pharmacol. Toxicol. (2014); e-pub ahead of print 27 Mar 2014.
43. Croft, M., Keely, B., Morris, I., Tann, L. & Lappin, G. Predicting drug candidate victims of drug-drug interactions, using microdosing. Clin Pharmacokinet. (2012).
44. Takahata, T., Yasui-Furukori, N., Yoshiya, G., Uno, T., Sugawara, K. & Tateishi, T. Fexofenadine does not affect omeprazole pharmacokinetics: Both are putative P-glycoprotein substrates. Basic Clin. Pharmacol. Toxicol. 94, 252-256 (2004).
45. Jefferson, J.W., Pradko, J.F. & Muir, K.T. Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations. Clin. Ther. 27, 1685-1695 (2005).
46. Kotlyar, M. et al. Inhibition of CYP2D6 activity by bupropion. J. Clin. Psychopharmacol. 25, 226-229 (2005).
47. Reese, M.J., Wurm, R.M., Muir, K.T., Generaux, G.T., St John-Williams, L. & McConn, D.J. An in vitro mechanistic study to elucidate the desipramine/ bupropion clinical drug-drug interaction. Drug Metab. Dispos. 36, 1198-1201 (2008).
48. Hesse, L.M., Greenblatt, D.J., von Moltke, L.L. & Court, M.H. Ritonavir has minimal impact on the pharmacokinetic disposition of a single dose of bupropion administered to human volunteers. J. Clin. Pharmacol. 46, 567-576 (2006).
49. Rebsamen, M.C. et al. The AmpliChip CYP450 test: Cytochrome P450 2D6 genotype assessment and phenotype prediction. Pharmacogenomics J. 9, 34-41 (2009).