Pharmacokinetics of intravenous and oral midazolam in plasma and saliva in humans: Usefulness of saliva as matrix for CYP3A phenotyping

British Journal of Clinical Pharmacology

Volumn 66, Issue 4, 2008, Pages 473-484

  Link, Bettina ^a   Haschke, Manuel ^a   Grignaschi, Nathalie ^a   Bodmer, Michael ^a   Aschmann, Yvonne Zysset ^a   Wenk, Markus ^a   Krähenbühl, Stephan ^a  

^a UNIVERSITY HOSPITAL BASEL   (Switzerland)

Author keywords

1 hydroxymidazolam; 4 hydroxymidazolam; CYP3A; LC MS MS; Midazolam; Phenotyping; Saliva

Indexed keywords

4 HYDROXYMIDAZOLAM; ALPHA HYDROXYMIDAZOLAM; CYTOCHROME P450 3A; DRUG METABOLITE; MIDAZOLAM; MIDAZOLAM MALEATE; RIFAMPICIN; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG MONITORING; DRUG SALIVA LEVEL; HUMAN; HUMAN EXPERIMENT; MALE; MORNING DOSAGE; NORMAL HUMAN; PATIENT COMPLIANCE; PHASE 2 CLINICAL TRIAL; PHENOTYPE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SEDATION; SIDE EFFECT;

AREA UNDER CURVE; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP3A; DRUG ADMINISTRATION ROUTES; HALF-LIFE; HUMANS; HYPNOTICS AND SEDATIVES; MALE; MIDAZOLAM; PHENOTYPE; SALIVA; SENSITIVITY AND SPECIFICITY;

EID: 51649119903     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2008.03201.x     Document Type: Article

References (34)

1. Nordt SP, Clark RF. Midazolam: a review of therapeutic uses and toxicity. J Emerg Med 1997 15: 357 65.
2. 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.
3. Bauer TM, Ritz R, Haberthur C, Ha HR, Hunkeler W, Sleight AJ, Scollo-Lavizzari G, Haefeli WE. Prolonged sedation due to accumulation of conjugated metabolites of midazolam. Lancet 1995 346: 145 7.
4. 14C- midazolam in humans following oral dosing. Arzneimittelforschung 1981 31: 2220 3.
5. Kronbach T, Mathys D, Umeno M, Gonzalez FJ, Meyer UA. Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. Mol Pharmacol 1989 36: 89 96.
6. Maurer HH. Advances in analytical toxicology: the current role of liquid chromatography-mass spectrometry in drug quantification in blood and oral fluid. Anal Bioanal Chem 2005 381: 110 8.
7. Aps JK, Martens LC. Review: the physiology of saliva and transfer of drugs into saliva. Forensic Sci Int 2005 150: 119 31.
8. Choo RE, Huestis MA. Oral fluid as a diagnostic tool. Clin Chem Lab Med 2004 42: 1273 87.
9. Kidwell DA, Holland JC, Athanaselis S. Testing for drugs of abuse in saliva and sweat. J Chromatogr B Biomed Sci Appl 1998 713: 111 35.
10. Kintz P, Samyn N. Use of alternative specimens: drugs of abuse in saliva and doping agents in hair. Ther Drug Monit 2002 24: 239 46.
11. Drummer OH. Review: pharmacokinetics of illicit drugs in oral fluid. Forensic Sci Int 2005 150: 133 42.
12. Link B, Haschke M, Wenk M, Krahenbuhl S. Determination of midazolam and its hydroxy metabolites in human plasma and oral fluid by liquid chromatography/electrospray ionization ion trap tandem mass spectrometry. Rapid Commun Mass Spectrom 2007 21: 1531 40.
13. Lee JI, Chaves-Gnecco D, Amico JA, Kroboth PD, Wilson JW, Frye RF. Application of semisimultaneous midazolam administration for hepatic and intestinal cytochrome P450 3A phenotyping. Clin Pharmacol Ther 2002 72: 718 28.
14. Lee LS, Bertino JS Jr., Nafziger AN. Limited sampling models for oral midazolam: midazolam plasma concentrations, not the ratio of 1-hydroxymidazolam to midazolam plasma concentrations, accurately predicts AUC as a biomarker of CYP3A activity. J Clin Pharmacol 2006 46: 229 34.
15. Li J, Karlsson MO, Brahmer J, Spitz A, Zhao M, Hidalgo M, Baker SD. CYP3A phenotyping approach to predict systemic exposure to EGFR tyrosine kinase inhibitors. J Natl Cancer Inst 2006 98: 1714 23.
16. Chaobal HN, Kharasch ED. Single-point sampling for assessment of constitutive, induced, and inhibited cytochrome P450 3A activity with alfentanil or midazolam. Clin Pharmacol Ther 2005 78: 529 39.
17. Lin YS, Lockwood GF, Graham MA, Brian WR, Loi CM, Dobrinska MR, Shen DD, Watkins PB, Wilkinson GR, Kharasch ED, Thummel KE. In vivo phenotyping for CYP3A by a single-point determination of midazolam plasma concentration. Pharmacogenetics 2001 11: 781 91.
18. Rogers JF, Nafziger AN, Kashuba AD, Streetman DS, Rocci ML Jr., Choo EF, Wilkinson GR, Bertino JS Jr. Single plasma concentrations of 1′-hydroxymidazolam or the ratio of 1′-hydroxymidazolam:midazolam do not predict midazolam clearance in healthy subjects. J Clin Pharmacol 2002 42: 1079 82.
19. Zhu B, Ou-Yang DS, Cheng ZN, Huang SL, Zhou HH. Single plasma sampling to predict oral clearance of CYP3A probe midazolam. Acta Pharmacol Sin 2001 22: 634 8.
20. Paine MF, Shen DD, Kunze KL, Perkins JD, Marsh CL, McVicar JP, Barr DM, Gillies BS, Thummel KE. First-pass metabolism of midazolam by the human intestine. Clin Pharmacol Ther 1996 60: 14 24.
21. Bodmer M, Link B, Grignaschi N, Kummer O, Ruegg S, Haschke M, Krähenbühl S. Pharmacokinetics of midazolam and metabolites in a patient with refractory status epilepticus treated with excessive doses of midazolam. Ther Drug Monit 2008 30: 120 4.
22. Loscher W, Frey HH. Kinetics of penetration of common antiepileptic drugs into cerebrospinal fluid. Epilepsia 1984 25: 346 52.
23. Friedrich G, Krieger A, Stritt W, Vach W. Pilot study of dose dependence in glucuronidation of morphine to morphine-3- and morphine-5-glucuronide. Beitr Gerichtl Med 1992 50: 215 20.
24. Backman JT, Olkkola KT, Neuvonen PJ. Rifampin drastically reduces plasma concentrations and effects of oral midazolam. Clin Pharmacol Ther 1996 59: 7 13.
25. Gorski JC, Vannaprasaht S, Hamman MA, Ambrosius WT, Bruce MA, Haehner-Daniels B, Hall SD. The effect of age, sex, and rifampin administration on intestinal and hepatic cytochrome P450 3A activity. Clin Pharmacol Ther 2003 74: 275 87.
26. Kupferschmidt HH, Ha HR, Ziegler WH, Meier PJ, Krahenbuhl S. Interaction between grapefruit juice and midazolam in humans. Clin Pharmacol Ther 1995 58: 20 8.
27. Ebert U, Thong NQ, Oertel R, Kirch W. Effects of rifampicin and cimetidine on pharmacokinetics and pharmacodynamics of lamotrigine in healthy subjects. Eur J Clin Pharmacol 2000 56: 299 304.
28. Soars MG, Petullo DM, Eckstein JA, Kasper SC, Wrighton SA. An assessment of udp-glucuronosyltransferase induction using primary human hepatocytes. Drug Metab Dispos 2004 32: 140 8.
29. Oesch F, Arand M, Benedetti MS, Castelli MG, Dostert P. Inducing properties of rifampicin and rifabutin for selected enzyme activities of the cytochrome P-450 and UDP-glucuronosyltransferase superfamilies in female rat liver. J Antimicrob Chemother 1996 37: 1111 9.
30. Reinach B, de Sousa G, Dostert P, Ings R, Gugenheim J, Rahmani R. Comparative effects of rifabutin and rifampicin on cytochromes P450 and UDP-glucuronosyl-transferases expression in fresh and cryopreserved human hepatocytes. Chem Biol Interact 1999 121: 37 48.
31. Zhu B, Bush D, Doss GA, Vincent SH, Franklin RB, Xu S. Characterization of 1′-hydroxymidazolam glucuronidation in human liver microsomes. Drug Metab Dispos 2008 36: 331 8.
32. Nakajima M, Suzuki T, Sasaki T, Yokoi T, Hosoyamada A, Yamamoto T, Kuroiwa Y. Effects of chronic administration of glucocorticoid on midazolam pharmacokinetics in humans. Ther Drug Monit 1999 21: 507 13.
33. Eap CB, Buclin T, Cucchia G, Zullino D, Hustert E, Bleiber G, Golay KP, Aubert AC, Baumann P, Telenti A, Kerb R. Oral administration of a low dose of midazolam (75 microg) as an in vivo probe for CYP3A activity. Eur J Clin Pharmacol 2004 60: 237 46.
34. Chainuvati S, Nafziger AN, Leeder JS, Gaedigk A, Kearns GL, Sellers E, Zhang Y, Kashuba AD, Rowland E, Bertino JS Jr. 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 2003 74: 437 47.