Population pharmacokinetic analysis of risperidone and 9-hydroxyrisperidone with genetic polymorphisms of CYP2D6 and ABCB1

Journal of Pharmacokinetics and Pharmacodynamics

Volumn 39, Issue 4, 2012, Pages 329-341

  Yoo, Hee Doo ^a   Cho, Hea Young ^b   Lee, Sang No ^a   Yoon, Hwa ^a   Lee, Yong Bok ^a  

^a Chonnam National University   (South Korea)

^b CHA University   (South Korea)

Author keywords

9 hydroxyrisoeridone; ABCB1; CYP2D6; Pharmacogenetics; Pharmacokinetics; Population model; Risperidone

Indexed keywords

CYTOCHROME P450 2D6; GENOMIC DNA; MULTIDRUG RESISTANCE PROTEIN 1; PALIPERIDONE; RISPERIDONE;

ABCB1 GENE; ADULT; ARTICLE; BIOEQUIVALENCE; COMPARTMENT MODEL; CONTROLLED STUDY; CYP2D6 GENE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG ELIMINATION; GENE; GENETIC POLYMORPHISM; GENETIC VARIABILITY; GENOTYPE; HUMAN; HUMAN EXPERIMENT; MALE; NONLINEAR SYSTEM; NORMAL HUMAN; PHARMACOGENETICS; PLASMA CONCENTRATION-TIME CURVE; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; RETROSPECTIVE STUDY; SINGLE DRUG DOSE;

ADULT; ALLELES; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP2D6; GENOTYPE; HUMANS; ISOXAZOLES; MALE; MODELS, BIOLOGICAL; P-GLYCOPROTEIN; POLYMORPHISM, SINGLE NUCLEOTIDE; PYRIMIDINES; RISPERIDONE; YOUNG ADULT;

EID: 84865520087     PISSN: 1567567X     EISSN: 15738744     Source Type: Journal    
DOI: 10.1007/s10928-012-9253-5     Document Type: Article

References (45)

1. Leysen JE, Gommeren W, Eens A, de Chaffoy de Courcelles D, Stoof JC, Janssen PA (1988) Biochemical profile of risperidone, a new antipsychotic. J Pharmacol Exp Ther 247(2):661-670
2. Janssen PA, Niemegeers CJ, Awouters F, Schellekens KH, Megens AA, Meert TF (1988) Pharmacology of risperidone (R 64 766), a new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties. J Pharmacol Exp Ther 244(2):685-693 (Pubitemid 18076615)
3. Frazier JA, Meyer MC, Biederman J, Wozniak J, Wilens TE, Spencer TJ, Kim GS, Shapiro S (1999) Risperidone treatment for juvenile bipolar disorder: a retrospective chart review. J Am Acad Child Adolesc Psychiatry 38(8):960-965 (Pubitemid 29353030)
4. McDougle CJ, Holmes JP, Carlson DC, Pelton GH, Cohen DJ, Price LH (1998) A double-blind, placebo-controlled study of risperidone in adults with autistic disorder and other pervasive developmental disorders. Arch Gen Psychiatry 55(7):633-641 (Pubitemid 28340352)
5. Fang J, Bourin M, Baker GB (1999) Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn Schmiedebergs Arch Pharmacol 359(2):147-151 (Pubitemid 29142884)
6. Yasui-Furukori N, Hidestrand M, Spina E, Facciola G, Scordo MG, Tybring G (2001) Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos 29(10):1263-1268 (Pubitemid 32896574)
7. Wang JS, Ruan Y, Taylor RM, Donovan JL, Markowitz JS, DeVane CL (2004) The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein. Int J Neuropsychopharmacol 7(4):415-419 (Pubitemid 39648071)
8. de Leon J, Wynn G, Sandson NB (2010) The pharmacokinetics of paliperidone versus risperidone. Psychosomatics 51(1):80-88
9. Kang RH, Jung SM, Kim KA, Lee DK, Cho HK, Jung BJ, Kim YK, Kim SH, Han C, Lee MS, Park JY (2009) Effects of CYP2D6 and CYP3A5 genotypes on the plasma concentrations of risperidone and 9-hydroxyrisperidone in Korean schizophrenic patients. J Clin Psychopharmacol 29(3):272-277
10. Bertilsson L, Dahl ML, Dalen P, Al-Shurbaji A (2002) Molecular genetics of CYP2D6: clinical relevance with focus on psychotropic drugs. Br J Clin Pharmacol 53(2):111-122 (Pubitemid 34264265)
11. Gan SH, Ismail R, Wan Adnan WA, Wan Z (2002) Correlation of tramadol pharmacokinetics and CYP2D6*10 genotype in Malaysian subjects. J Pharm Biomed Anal 30(2):189-195 (Pubitemid 35013483)
12. Chowbay B, Cumaraswamy S, Cheung YB, Zhou Q, Lee EJ (2003) Genetic polymorphisms in MDR1 and CYP3A4 genes in Asians and the influence of MDR1 haplotypes on cyclosporin disposition in heart transplant recipients. Pharmacogenetics 13(2):89-95 (Pubitemid 36259588)
13. Boulton DW, DeVane CL, Liston HL, Markowitz JS (2002) In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci 71(2):163-169 (Pubitemid 34595435)
14. Yasui-Furukori N, Mihara K, Takahata T, Suzuki A, Nakagami T, De Vries R, Tateishi T, Kondo T, Kaneko S (2004) Effects of various factors on steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone: lack of impact of MDR-1 genotypes. Br J Clin Pharmacol 57(5):569-575 (Pubitemid 38582176)
15. Nakagami T, Yasui-Furukori N, Saito M, Tateishi T, Kaneo S (2005) Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition. Clin Pharmacol Ther 78(1):43-51 (Pubitemid 40956930)
16. Gunes A, Spina E, Dahl ML, Scordo MG (2008) ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. Ther Drug Monit 30(5): 628-633
17. Kimchi-Sarfaty C, Oh JM, Kim IW, Sauna ZE, Calcagno AM, Ambudkar SV, Gottesman MM (2007) A "silent" polymorphism in the MDR1 gene changes substrate specificity. Science 315(5811): 525-528 (Pubitemid 46175758)
18. Nakamura T, Sakaeda T, Horinouchi M, Tamura T, Aoyama N, Shirakawa T, Matsuo M, Kasuga M, Okumura K (2002) Effect of the mutation (C3435T) at exon 26 of the MDR1 gene on expression level of MDR1 messenger ribonucleic acid in duodenal enterocytes of healthy Japanese subjects. Clin Pharmacol Ther 71(4):297-303 (Pubitemid 34311459)
19. Rodrigues AC, Rebecchi IM, Bertolami MC, Faludi AA, Hirata MH, Hirata RD (2005) High baseline serum total and LDL cholesterol levels are associated with MDR1 haplotypes in Brazilian hypercholesterolemic individuals of European descent. Braz J Med Biol Res 38(9):1389-1397 (Pubitemid 41288425)
20. Hoffmeyer S, Burk O, von Richter O, Arnold HP, Brockmoller J, Johne A, Cascorbi I, Gerloff T, Roots I, Eichelbaum M, Brinkmann U (2000) Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo. Proc Natl Acad Sci USA 97(7):3473-3478 (Pubitemid 30183327)
21. Yoo HD, Lee SN, Kang HA, Cho HY, Lee IK, Lee YB (2011) Influence of ABCB1 genetic polymorphisms on the pharmacokinetics of risperidone in healthy subjects with CYP2D6*10/*10. Br J Pharmacol 164(2b):433-443
22. Ll A, Berecz R, Dorado P, de la Garza CS, Norberto MJ, Caceres M, Gutierrez JR (2003) Determination of risperidone and 9-hydroxyrisperidone in human plasma by liquid chromatography: application to the evaluation of CYP2D6 drug interactions. J Chromatogr B Analyt Technol Biomed Life Sci 783(1):213-219 (Pubitemid 35351648)
23. Lee SJ, Lee SS, Jung HJ, Kim HS, Park SJ, Yeo CW, Shin JG (2009) Discovery of novel functional variants and extensive evaluation of CYP2D6 genetic polymorphisms in Koreans. Drug Metab Dispos 37(7):1464-1470
24. Cascorbi I, Gerloff T, Johne A, Meisel C, Hoffmeyer S, Schwab M, Schaeffeler E, Eichelbaum M, Brinkmann U, Roots I (2001) Frequency of single nucleotide polymorphisms in the P-glycoprotein drug transporter MDR1 gene in white subjects. Clin Pharmacol Ther 69(3):169-174 (Pubitemid 32225417)
25. Beal S, Sheiner L (1992) NONMEM User's Guide, Part I. University of California at San Francisco, San Francisco
26. Vermeulen A, Piotrovsky V, Ludwig EA (2007) Population pharmacokinetics of risperidone and 9-hydroxyrisperidone in patients with acute episodes associated with bipolar I disorder. J Pharmacokinet Pharmacodyn 34(2):183-206 (Pubitemid 46536257)
27. Mandema JW, Verotta D, Sheiner LB (1992) Building population pharmacokinetic-pharmacodynamic models. I. Models for covariate effects. J Pharmacokinet Biopharm 20(5):511-528 (Pubitemid 23034413)
28. Jonsson EN, Karlsson MO (1999) Xpose-an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput Methods Programs Biomed 58(1): 51-64 (Pubitemid 29049052)
29. Jonsson EN, Karlsson MO (1998) Automated covariate model building within NONMEM. Pharm Res 15(9):1463-1468 (Pubitemid 28427937)
30. Hooker AC, Staatz CE, Karlsson MO (2007) Conditional weighted residuals (CWRES): a model diagnostic for the FOCE method. Pharm Res 24(12):2187-2197 (Pubitemid 350060706)
31. Parke J, Holford NH, Charles BG (1999) A procedure for generating bootstrap samples for the validation of nonlinear mixedeffects population models. Comput Methods Programs Biomed 59(1):19-29 (Pubitemid 29125558)
32. Lee SY, Sohn KM, Ryu JY, Yoon YR, Shin JG, Kim JW (2006) Sequence-based CYP2D6 genotyping in the Korean population. Ther Drug Monit 28(3):382-387 (Pubitemid 44314926)
33. Feng Y, Pollock BG, Coley K, Marder S, Miller D, Kirshner M, Aravagiri M, Schneider L, Bies RR (2008) Population pharmacokinetic analysis for risperidone using highly sparse sampling measurements from the CATIE study. Br J Clin Pharmacol 66(5):629-639
34. Locatelli I, Kastelic M, Koprivsek J, Kores-Plesnicar B, Mrhar A, Dolzan V, Grabnar I (2010) A population pharmacokinetic evaluation of the influence of CYP2D6 genotype on risperidone metabolism in patients with acute episode of schizophrenia. Eur J Pharm Sci 41(2):289-298
35. Hoy SM, Scott LJ, Keating GM (2010) Intramuscular paliperidone palmitate. CNS drugs 24(3):227-244
36. Si T, Shu L, Liu Y, Su YA, Guo C, Zhang H (2010) Single-dose pharmacokinetics of paliperidone extended-release tablets in healthy Chinese subjects. Hum Psychopharmacol 25(5):404-409
37. Huang ML, Van Peer A, Woestenborghs R, De Coster R, Heykants J, Jansen AA, Zylicz Z, Visscher HW, Jonkman JH (1993) Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Clin Pharmacol Ther 54(3):257-268 (Pubitemid 23294526)
38. Miksys SL, Cheung C, Gonzalez FJ, Tyndale RF (2005) Human CYP2D6 and mouse CYP2Ds: organ distribution in a humanized mouse model. Drug Metab Dispos 33(10):1495-1502 (Pubitemid 41323998)
39. Jovanovic N, Bozina N, Lovric M, Medved V, Jakovljevic M, Peles AM (2010) The role of CYP2D6 and ABCB1 pharmacogenetics in drug-naive patients with first-episode schizophrenia treated with risperidone. Eur J Clin Pharmacol 66(11): 1109-11017
40. Benet LZ, Cummins CL (2001) The drug efflux-metabolism alliance: biochemical aspects. Adv Drug Deliv Rev 50(Suppl 1): S3-11
41. Wu CY, Benet LZ (2005) Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 22(1):11-23 (Pubitemid 40558141)
42. Mannens G, Huang ML, Meuldermans W, Hendrickx J, Woestenborghs R, Heykants J (1993) Absorption, metabolism, and excretion of risperidone in humans. Drug Metab Dispos 21(6): 1134-1141 (Pubitemid 23348354)
43. Singh S, Muthu MS (2007) Preparation and characterization of nanoparticles containing an atypical antipsychotic agent. Nanomedicine (Lond) 2(2):233-240 (Pubitemid 46845769)
44. Mahatthanatrakul W, Sriwiriyajan S, Ridtitid W, Boonleang J, Wongnawa M, Rujimamahasan N, Pipatrattanaseree W (2012) Effect of cytochrome P450 3A4 inhibitor ketoconazole on risperidone pharmacokinetics in healthy volunteers. J Clin Pharm Ther 37(2):221-225
45. Kim KA, Park PW, Liu KH, Kim KB, Lee HJ, Shin JG, Park JY (2008) Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. J Clin Pharmacol 48(1):66-72