Pharmacokinetic-pharmacodynamic modelling of fluvoxamine 5-HT transporter occupancy in rat frontal cortex

British Journal of Pharmacology

Volumn 154, Issue 6, 2008, Pages 1369-1378

  Geldof, M ^a,c   Freijer, J I ^b,d   Van Beijsterveldt, L ^c   Langlois, X ^c   Danhof, M ^a,b  

^a LEIDEN UNIVERSITY   (Netherlands)

^b LAP and P Consultants BV   (Netherlands)

^c JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^d Astellas Pharma Global Development   (Netherlands)

Author keywords

Blood brain barrier; Intracerebral microdialysis; Nonlinear mixed effects modeling; Pharmacokinetics; Selective serotonin reuptake inhibitor; SSRI

Indexed keywords

FLUVOXAMINE; SEROTONIN TRANSPORTER;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN TISSUE; CONTROLLED STUDY; DRUG BLOOD LEVEL; EX VIVO STUDY; EXTRACELLULAR FLUID; FRONTAL CORTEX; MALE; NONHUMAN; PHARMACODYNAMICS; PLASMA; PRIORITY JOURNAL; RAT;

ALGORITHMS; ANIMALS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DATA INTERPRETATION, STATISTICAL; FLUVOXAMINE; IMAGE PROCESSING, COMPUTER-ASSISTED; INFUSIONS, INTRAVENOUS; MALE; MICRODIALYSIS; MODELS, BIOLOGICAL; PREFRONTAL CORTEX; RATS; RATS, WISTAR; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; SEROTONIN UPTAKE INHIBITORS;

EID: 47249107302     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/bjp.2008.179     Document Type: Article

References (33)

1. Ables AZ, Baughman III OL (2003). Antidepressants: update on new agents and indications. Am Fam Physician 67: 547-554.
2. Alexander SP, Mathie A, Peters JA (2007). Guide to Receptors and Channels (GRAC), 2nd edition (2007 revision). Br J Pharmacol 150 (Suppl 1): S1-S168.
3. Auerbach SB, Hjorth S (1995). Effect of chronic administration of the selective serotonin (5-HT) uptake inhibitor citalopram on extracellular 5-HT and apparent autoreceptor sensitivity in rat forebrain in vivo. Naunyn Schmiedebergs Arch Pharmacol 352: 597-606.
4. Bel N, Artigas F (1992). Fluvoxamine preferentially increases extracellular 5-hydroxytryptamine in the raphe nuclei: an in vivo microdialysis study. Eur J Pharmacol 229: 101-103.
5. Benmansour S, Cecchi M, Morilak DA, Gerhardt GA, Javors MA, Gould GG et al. (1999). Effects of chronic antidepressant treatments on serotonin transporter function, density, and mRNA level. J Neurosci 19: 10494-10501.
6. Blier P, Bouchard C (1994). Modulation of 5-HT release in the guinea-pig brain following long-term administration of antidepressant drugs. Br J Pharmacol 113: 485-495.
7. Bosker FJ, Klompmakers AA, Westenberg HG (1995). Effects of single and repeated oral administration of fluvoxamine on extracellular serotonin in the median raphe nucleus and dorsal hippocampus of the rat. Neuropharmacology 34: 501-508.
8. Bouw MR, Hammarlund-Udenaes M (1998). Methodological aspects of the use of a calibrator in in vivo microdialysis - further development of the retrodialysis method. Pharm Res 15: 1673-1679.
9. Colburn WA, Lee JW (2003). Biomarkers, validation and pharmacokinetic-pharmacodynamic modelling. Clin Pharmacokinet 42: 997-1022.
10. Coppen A (1967). The biochemistry of affective disorders. Br J Psychiatry 113: 1237-1264.
11. Danhof M, Alvan G, Dahl SG, Kuhlmann J, Paintaud G (2005). Mechanism-based pharmacokinetic-pharmacodynamic modeling - a new classification of biomarkers. Pharm Res 22: 1432-1437.
12. De Lange EC, Danhof M, de Boer AG, Breimer DD (1997). Methodological considerations of intracerebral microdialysis in pharmacokinetic studies on drug transport across the blood-brain barrier. Brain Res Brain Res Rev 25: 27-49.
13. Fuller RW (1994). Uptake inhibitors increase extracellular serotonin concentration measured by brain microdialysis. Life Sci 55: 163-167.
14. Geldof M, Freijer J, Van Beijsterveldt L, Danhof M (2008). Pharmacokinetic modeling of non-linear brain distribution of fluvoxamine in the rat. Pharm Res 25: 792-804.
15. Geldof M, Freijer J, Van Beijsterveldt L, Timmerman P, Ahnaou A, Drinkenburg WH et al. (2007a). Population pharmacokinetic model of fluvoxamine in rats: utility for application in animal behavioral studies. Eur J Pharm Sci 30: 45-55.
16. 11C]-DASB, a tool for in vivo measurement of SSRI-induced occupancy of the serotonin transporter: PET characterization and evaluation in cats. Synapse 47: 123-133.
17. Hirano K, Kimura R, Sugimoto Y, Yamada J, Uchida S, Kato Y et al. (2005). Relationship between brain serotonin transporter binding, plasma concentration and behavioural effect of selective serotonin reuptake inhibitors. Br J Pharmacol 144: 695-702.
18. Horschitz S, Hummerich R, Schloss P (2001). Structure, function and regulation of the 5-hydroxytryptamine (serotonin) transporter. Biochem Soc Trans 29: 728-732.
19. Isaac M (1999). Where are we going with SSRIs? Eur Neuropsychopharmacol 9 (Suppl 3): S101-S106.
20. Jolling K, Ruixo JJ, Hemeryck A, Piotrovskij V, Greway T (2004). Population pharmacokinetic analysis of pegylated human erythropoietin in rats. J Pharm Sci 93: 3027-3038.
21. Kuipers JA, Boer F, de Roode A, Olofsen E, Bovill JG, Burm AG (2001). Modeling population pharmacokinetics of lidocaine: should cardiac output be included as a patient factor? Anesthesiology 94: 566-573.
22. Langlois X, te Riele P, Wintmolders C, Leysen JE, Jurzak M (2001). Use of the beta-imager for rapid ex vivo autoradiography exemplified with central nervous system penetrating neurokinin 3 antagonists. J Pharmacol Exp Ther 299: 712-717.
23. Lesch KP, Aulakh CS, Wolozin BL, Tolliver TJ, Hill JL, Murphy DL (1993). Regional brain expression of serotonin transporter mRNA and its regulation by reuptake inhibiting antidepressants. Brain Res Mol Brain Res 17: 31-35.
24. Meyer JH, Wilson AA, Ginovart N, Goulding V, Hussey D, Hood K et al. (2001). Occupancy of serotonin transporters by paroxetine and citalopram during treatment of depression: a [(11)C]DASB PET imaging study. Am J Psychiatry 158: 1843-1849.
25. 11C]DASB positron emission tomography study. Am J Psychiatry 161: 826-835.
26. Moghaddam B, Bunney BS (1989). Ionic composition of microdialysis perfusing solution alters the pharmacological responsiveness and basal outflow of striatal dopamine. J Neurochem 53: 652-654.
27. Owens MJ, Nemeroff CB (1994). Role of serotonin in the pathophysiology of depression: focus on the serotonin transporter. Clin Chem 40: 288-295.
28. Paxinos G, Watson C (1982). The Rat Brain in Stereotaxic Coordinates. Academic Press: New York, USA.
29. Pineyro G, Blier P, Dennis T, de Montigny C (1994). Desensitization of the neuronal 5-HT carrier following its long-term blockade. J Neurosci 14: 3036-3047.
30. Ramamoorthy S, Blakely RD (1999). Phosphorylation and sequestration of serotonin transporters differentially modulated by psychostimulants. Science 285: 763-766.
31. Rolan P (1997). The contribution of clinical pharmacology surrogates and models to drug development - a critical appraisal. Br J Clin Pharmacol 44: 219-225.
32. Suhara T, Takano A, Sudo Y, Ichimiya T, Inoue M, Yasuno F et al. (2003). High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Arch Gen Psychiatry 60: 386-391.
33. Takano A, Suhara T, Ichimiya T, Yasuno F, Suzuki K (2006). Time course of in vivo 5-HTT transporter occupancy by fluvoxamine. J Clin Psychopharmacol 26: 188-191.