Alfentanil-induced miosis clearance as a liver CYP3A4 and 3A5 activity measure in healthy volunteers: Improvement of experimental conditions

Journal of Clinical Pharmacology

Volumn 45, Issue 12, 2005, Pages 1434-1441

  Baririan, Narine ^a   Horsmans, Yves ^a   Desager, Jean Pierre ^a   Verbeeck, Roger ^b   Vanbinst, Roger ^a   Wallemacq, Pierre ^a   Van Obbergh, Luc ^b  

^a CLINIQUES UNIVERSITAIRES SAINT LUC   (Belgium)

^b UNIVERSITÉ CATHOLIQUE DE LOUVAIN   (Belgium)

Author keywords

Alfentanil; CYP3A4; Miosis; Pharmacokinetics

Indexed keywords

ALFENTANIL; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; FENTANYL;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; ENZYME ACTIVITY; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; LIGHT INTENSITY; MALE; MIOSIS; NORMAL HUMAN; PHARMACOKINETICS; PUPILLOMETER; TANDEM MASS SPECTROMETRY; VALIDATION PROCESS;

ADULT; ALFENTANIL; ANALGESICS, OPIOID; CYTOCHROME P-450 ENZYME SYSTEM; FEMALE; HUMANS; MALE; METABOLIC CLEARANCE RATE; MIOSIS;

EID: 27844601564     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270005282629     Document Type: Article

References (30)

1. Walsky RL, Obach RS. Validated assays for human cytochrome P450 activities. Drug Metab Dispos. 2004;32:647-660.
2. Donato MT, Castell JV. Strategies and molecular probes to investigate the role of cytochrome P450 in drug metabolism: focus on in vitro studies. Clin Pharmacokinet. 2003;42:153-178.
3. Gibbs MA, Hosea NA. Factors affecting the clinical development of cytochrome p450 3A substrates. Clin Pharmacokinet. 2003;42:969-984.
4. Brockmoller J, Roots I. Assessment of liver metabolic function: clinical implications. Clin Pharmacokinet. 1994;27:216-248.
5. Watkins PB. Noninvasive tests of CYP3A enzymes. Pharmacogenetics. 1994;4:171-184.
6. Kivisto KT, Kroemer HK. Use of probe drugs as predictors of drug metabolism in humans. J Clin Pharmacol. 1997;37:40S-48S.
7. Streetman DS, Bertino JS Jr, Nafziger AN. Phenotyping of drug-metabolizing enzymes in adults: a review of in-vivo cytochrome P450 phenotyping probes. Pharmacogenetics. 2000;10:187-216.
8. Krecic-Shepard ME, Barnas CR, Slimko J, Gorski JC, Wainer IW, Schwartz JB. In vivo comparison of putative probes of CYP3A4/5 activity: erythromycin, dextromethorphan, and verapamil. Clin Pharmacol Ther. 1999;66:40-50.
9. Fleming CM, Branch RA, Wilkinson GR, Guengerich FP. Human liver microsomal N-hydroxylation of dapsone by cytochrome P-4503A4. Mol Pharmacol. 1992;41:975-980.
10. Wang JS, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT. Involvement of CYP1A2 and CYP3A4 in lidocaine N-deethylation and 3-hydroxylation in humans. Drug Metab Dispos. 2000;28:959-965.
11. Kinirons MT, O'Shea D, Downing TE, et al. Absence of correlations among three putative in vivo probes of human cytochrome P4503A activity in young healthy men. Clin Pharmacol Ther. 1993;54:621-629.
12. Kinirons MT, O'Shea D, Kim RB, et al. Failure of erythromycin breath test to correlate with midazolam clearance as a probe of cytochrome P4503A. Clin Pharmacol Ther. 1999;66:224-231.
13. Krivoruk Y, Kinirons MT, Wood AJ, Wood M. Metabolism of cytochrome P4503A substrates in vivo administered by the same route: lack of correlation between alfentanil clearance and erythromycin breath test. Clin Pharmacol Ther. 1994;56:608-614.
14. Kharasch ED, Russell M, Mautz D, et al. The role of cytochrome P450 3A4 in alfentanil clearance: implications for interindividual variability in disposition and perioperative drug interactions. Anesthesiology. 1997;87:36-50.
15. Labroo RB, Thummel KE, Kunze KL, Podoll T, Trager WF, Kharasch ED. Catalytic role of cytochrome P4503A4 in multiple pathways of alfentanil metabolism. Drug Metab Dispos. 1995;23:490-496.
16. Klees TM, Sheffels P, Thummel KE, Kharasch ED. Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5. Anesthesiology. 2005;102:550-556.
17. Klees TM, Sheffels P, Dale O, Kharasch ED. Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Drug Metab Dispos. 2005;33:303-311.
18. Lin JH, Chiba M, Baillie TA. Is the role of the small intestine in first-pass metabolism overemphasized? Pharmacol Rev. 1999;51:135-158.
19. Chauvin M, Bonnet F, Montembault C, Levron JC, Viars P. The influence of hepatic plasma flow on alfentanil plasma concentration plateaus achieved with an infusion model in humans: measurement of alfentanil hepatic extraction coefficient. Anesth Analg. 1986;65:999-1003.
20. Kharasch ED, Russell M, Garton K, Lentz G, Bowdle TA, Cox K. Assessment of cytochrome P450 3A4 activity during the menstrual cycle using alfentanil as a noninvasive probe. Anesthesiology. 1997;87:26-35.
21. Miller CD, Asbury AJ, Brown JH. Pupillary effects of alfentanil and morphine. Br J Anaesth. 1990;65:415-417.
22. Pickworth WB, Welch P, Henningfield JE, Cone EJ. Opiate-induced pupillary effects in humans. Methods Find Exp Clin Pharmacol. 1989;11:759-763.
23. Phimmasone S, Kharasch ED. A pilot evaluation of alfentanil-induced miosis as a noninvasive probe for hepatic cytochrome P450 3A4 (CYP3A4) activity in humans. Clin Pharmacol Ther. 2001;70:505-517.
24. Kharasch ED, Walker A, Hoffer C, Sheffels P. Intravenous and oral alfentanil as in vivo probes for hepatic and first-pass cytochrome P450 3A activity: noninvasive assessment by use of pupillary miosis. Clin Pharmacol Ther. 2004;76:452-466.
25. Kharasch ED, Hoffer C, Walker A, Sheffels P. Disposition and miotic effects of oral alfentanil: a potential noninvasive probe for first-pass cytochrome P4503A activity. Clin Pharmacol Ther. 2003;73:199-208.
26. Mautz DS, Labroo R, Kharasch ED. Determination of alfentanil and noralfentanil in human plasma by gas chromatography-mass spectrometry. J Chromatogr B Biomed Appl. 1994;658:149-153.
27. Gabrielsson J, Weiner D. Pharmacokinetic and Pharmacodynamic Data Analysis: Concepts and Applications. 3rd ed. Stockholm, Sweden: Kristianstads Boktryckeri AB and Swedish Pharmaceutical Press; 2005.
28. Bower S, Hull CJ. Comparative pharmacokinetics of fentanyl and alfentanil. Br J Anaesth. 1982;54:871-877.
29. Kharasch ED, Thummel KE. Human alfentanil metabolism by cytochrome P450 3A3/4. An explanation for the interindividual variability in alfentanil clearance? Anesth Analg. 1993;76:1033-1039.
30. Piafsky KM. Disease-induced changes in the plasma binding of basic drugs. Clin Pharmacokinet. 1980;5:246-262.