title: Influence of ABCB1 genetic polymorphisms on the pharmacokinetics of risperidone in healthy subjects with CYP2D6*10/*10.
abstract: OBJECTIVE
  The objective of this study was to investigate the combined influence of genetic polymorphisms in ABCB1 and CYP2D6 genes on risperidone pharmacokinetics.
  
  
  METHODS
  Seventy-two healthy Korean volunteers receiving a single oral dose of 2 mg risperidone were included in this study.
  
  
  RESULTS
  Significant differences were observed between the ABCB1 3435C>T genotypes for the pharmacokinetic parameters (peak serum concentration) of risperidone and the active moiety (risperidone and its main metabolite, 9-hydroxyrisperidone). There were no significant differences in the area under the serum concentration-time curves of risperidone and the active moiety among the ABCB1 2677G>T/A and 3435C>T genotypes. However, the peak serum concentration and area under the serum concentration-time curves were significantly different among the ABCB1 3435C>T genotypes in CYP2D6*10/*10.
  
  
  CONCLUSIONS
  These findings indicate that polymorphisms of ABCB1 3435C>T in individuals with CYP2D6*10/*10, which has low metabolic activity, could play an important role in the potential adverse effects or toxicity of risperidone.
authors: College of Pharmacy and Institute of Bioequivalence and Bridging Study, Chonnam National University, Gwangju, Korea.
authors: Hee-Doo
authors: HD
authors: Yoo
authors: Sang-No
authors: SN
authors: Lee
authors: Hyun-Ah
authors: HA
authors: Kang
authors: Hea-Young
authors: HY
authors: Cho
authors: Il-Kwon
authors: IK
authors: Lee
authors: Yong-Bok
authors: YB
authors: Lee
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics* / Q000378:metabolism; D014150:Antipsychotic Agents / Q000097:blood / Q000493:pharmacokinetics; D018592:Cross-Over Studies; D019389:Cytochrome P-450 CYP2D6 / Q000235:genetics* / Q000378:metabolism; D005838:Genotype; D006801:Humans; D007555:Isoxazoles / Q000097:blood; D008297:Male; D000068882:Paliperidone Palmitate; D011110:Polymorphism, Genetic; D011743:Pyrimidines / Q000097:blood; D012189:Retrospective Studies; D018967:Risperidone / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D014150:Antipsychotic Agents; D007555:Isoxazoles; D011743:Pyrimidines; D019389:Cytochrome P-450 CYP2D6; D018967:Risperidone; D000068882:Paliperidone Palmitate