Desipramine, substrate for CYP2D6 activity: Population pharmacokinetic model and design elements of drug-drug interaction trials

British Journal of Clinical Pharmacology

Volumn 70, Issue 4, 2010, Pages 523-536

  Gueorguieva, Ivelina ^a   Jackson, Kimberley ^a   Wrighton, Steven A ^b   Sinha, Vikram P ^b   Chien, Jenny Y ^b  

^a ELI LILLY AND COMPANY   (United States)

^b NONE

Author keywords

CYP2D6; desipramine; optimal sampling times; population pharmacokinetics; sample size

Indexed keywords

CYTOCHROME P450 2D6; DESIPRAMINE;

ADULT; AGED; ARTICLE; COMPARTMENT MODEL; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG INTERACTION; ENZYME ACTIVITY; ENZYME SUBSTRATE; FEMALE; GENOTYPE; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PHARMACOGENETICS; PHARMACOKINETICS; PRIORITY JOURNAL; SINGLE DRUG DOSE;

ADMINISTRATION, ORAL; ADULT; BAYES THEOREM; CYTOCHROME P-450 CYP2D6; DESIPRAMINE; ENZYME INHIBITORS; FEMALE; GENOTYPE; HUMANS; MALE; MIDDLE AGED; MODELS, BIOLOGICAL; PHENOTYPE;

EID: 77956590976     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2010.03731.x     Document Type: Article

References (35)

1. Gram LF, Christiansen J. First pass metabolism of imipramine in man. Clin Pharmacol Ther 1975 17:555 563.
2. Nagy A, Treiber L. Quantitative determination of imipramine and desipramine in human blood plasma by direct densitometry of thinlayer chromatograms. J Pharm Pharmacol 1973 25:599 603.
3. Zeidenberg P, Perel JM, Kanzler M, Warthon RN, Malitz S. Clinical and metabolic studies with imipramine in man. Am J Psychiatry 1971 127:1321 1326.
4. Christiansen J, Gram LF, Kofod B, Rafaelsen OJ. Imipramine metabolism in man. Psychopharmacologia 1967 11:255 264.
5. Alexanderson B. Pharmacokinetics of desmethylimipramine and nortriptyline in man after single and multiple oral doses. Eur J Clin Pharmacol 1972 5:1 5.
6. Devane CL, Savett M, Jusko WJ. Desipramine and 2-hydroxydesipramine pharmacokinetics in normal volunteers. Eur J Clin Pharmacol 1981 19:61 4.
7. Brosen K, Gram LF. First pass metabolism of imipramine and desipramine: impact of the sparteine oxidation phenotype. Clin Pharmacol Ther 1988 43:400 406.
8. Salee FR, Pollock BG. Clinical pharmacokinetics of imipramine and desipramine. Clin Pharmacokinet 1990 18:346 364.
9. Ciraulo DA, Barnhill JG, Jaffe JH. Clinical pharmacokinetics of imipramine and desipramine in alcoholics and normal volunteers. Clin Pharmacol Ther 1988 43:509 518.
10. Bertilsson L, Aberg-Wistedt A. The debrisoquine hydroxylation test predictes steady-state plasma levels of desipramine. Br J Clin Pharmacol 1983 15:388 390.
11. Dahl ML, Iselius L, Alm C, Svensson JO, Lee D, Johansson I, Ingleman-Sundberg M, Sjoqvist F. Polymorphic 2-hydroxylation of desipramine. A population and family study. Eur J Clin Pharmacol 1993 44:445 450.
12. Bronsen K, Hansen JG, Nielsen KK, Sindrup SH, Gram LF. Inhibition by paroxetine of desipramine metabolism in extensive but not in poor metabolisers of sparteine. Eur J Clin Pharmacol 1993 44:349 355.
13. Laine K, de Bruyn S, Bjorklund H, Rouru J, Hanninen J, Scheinin H, Anttila M. Effect of the novel anxiolytic drug deramciclane on cytochrome P450 2D6 activity as measured by desipramine pharmacokinetics. Eur J Clin Pharmacol 2004 59:893 898.
14. Spina E, Pollocino AM, Avenso A, Campo GM, Perucca E, Caputi AP. Effect of fluvoxamine on the pharmacokinteics of imipramine and desipramine in healthy subjects. Ther Drug Monit 1993 15:243 246.
15. Bergstrom RE, Peyton AL, Lemberger L. Quantification and mechanism of the fluoxetine and tricyclic antidepressant interaction. Clin Pharmacol Ther 1992 51:239 248.
16. Kurtz DL, Bergstrom RF, Goldberg MJ, Cerimele BJ. The effect of sertraline on the pharmacokinetics of desipramine and imipramine. Clin Pharmacol Ther 1997 62:145 156.
17. Swanson JR, Jones GR, Krasselt W, Denmark LN, Ratti F. Death of two subjects due to imipramine and desipramine metabolite accumulation during chronic therapy: a review of the literature and possible mechanisms. J Forensic Sci 1997 42:335 339.
18. Leucht S, Hackl HJ, Steimer W, Angerbach D, Zimmer R. Effect of adjunctive paroxetine on serum levels and side effects of tricyclic antidepressants in depressive inpatients. Psychopharmacology 2000 147:378 383.
19. Eichelbaum M, Spannbrucker N, Steincke B, Dengler HJ. Defective N-oxidation of sparteine in man: a new pharmacogenetic defect. Eur J Clin Pharmacol 1979 16:183 187.
20. Mahgoub A, Idle JR, Dring LG, Lancaster R, Smith RL. Polymorphic hydroxylation of debrisoquine in man. Lancet 1977 2:584 586.
21. Peart GF, Boutagy J, Shenfield GM. Debrisoquine oxidation in an Australian population. Br J Clin Pharmacol 1986 21:465 471.
22. Borges S, Desta Z, Li L, Skaar TC, Ward BA, Nguyen A, Jin Y, Storniolo AM, Nikoloff DM, Wu L, Hillman G, Hayes DF, Stearns V, Flockhart DA. Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: implication for optimization of breast cancer treatment. Clin Pharmacol Ther 2006 80:61 74.
23. Abernethy DR, Greenblatt DJ, Shader R. Imipramine and desipramine disposition in the elderly. J Pharmacol Exp Ther 1985 232:183 188.
24. Beal S, Sheiner LB. The NONMEM system. Am Stat 1980 34:118 119.
25. Beal S, Sheiner LB, eds. NONMEM Users Guides. NONMEM Project Group. San Francisco, CA:University of California, 1998.
26. Brown RP, Delp MD, Lindstedt SL, Rhomberg LR, Beliles RP. Physiological parameter values for physiologically based pharmacokinetic models. Toxicol Ind Health 1997 13:407 484.
27. Spiegelhalter D, Thomas A, Best N. WinBUGS Version 1.3 User Manual. Cambridge:Medical Research Council Biostatistics Unit, 2000.
28. Lunn DJ, Best N, Thomas A, Wakefield J, Spiegelhalter D. Bayesian analysis of population PK/PD models: general concepts and software. J Pharmacokinet Pharmacodyn 2002 29:271 307.
29. Best NG, Cowles MK, Vines SK. CODA: Convergence Diagnosis and Output Analysis Software for Gibbs Sampling Output, Version 0.4. Cambridge:MRC Biostatistics Unit, 1997. Available at http://www.mrc-bsu.cam.ac.uk/bugs/ classic/coda04/readme.shtml (last accessed 21 July 2010).
30. Gueorguieva I, Ogungbenro K, Graham G, Glatt S, Aarons L. A program for individual and population optimal design for univariate and multivariate response pharmacokinetic-pharmacodynamic models. Comput Methods Programs Biomed 2007 86:51 61.
31. Nix DE, Gallicano K. Design and data analysis of drug interaction studies. In:Infectious Disease: Drug Interactions in Infectious Diseases, 2nd edn, eds Piscitelli SC, Rodvold KA. Totowa, NJ:© Humana Press Inc., 2005 483 505.
32. Hauschke D, Kieser M, Diletti E, Burke M. Sample size determination for providing equvalence based on theratio of two means for normally distributed data. Stat Med 1999 18:93 105.
33. Karlsson MO, Sheiner LB. The importance of modelling inter-occasion variability in population pharmacokinetic analyses. J Pharmacokinet Biopharm 1993 21:735 750.
34. Lunn DJ, Aarons LJ. Markov chain monte carlo techniques for studying interoccasion and intersubject variability: application to pharmacokinetic data. Appl Stat 1997 46:73 91.
35. Rowland M, Tozer T. Clinical Pharmacokinetics: Concepts and Applications, 3rd revised edn. Baltimore, MD:Lippincott Williams and Wilkins, 1995, 20.