title: [The influence of clomipramine on CYP2D6 activity].
abstract: OBJECTIVE
  Genetically determined activity ofCYP2D6 may be modified by some drugs through inhibition processes. Inhibition properties of TCA's were confirmed mainly in in vitro studies. The aim of the study was to assess the influence of clomipramine on CYP2D6 activity in vivo.
  
  
  METHODS
  11 patients diagnosed with depression according to ICD-10 and DSM-IV (major depression) criteria were included in the study. In all the cases clomipramine therapy was indicated. CYP2D6 activity was assessed by the phenotyping method. All patients were treated simultaneously. Each of the patients ingested one tablet containing 100 mg of sparteine sulfate. Urine excreted during the following 6 h was collected. Based on sparteine metabolic ratio (MR) the phenotype status was estimated twice: after the wash-out period, before clomipramine treatment, sparteine metabolic ratio (MRI), and after 2-weeks of clomipramine treatment (MR2).
  
  
  RESULTS
  During clomipramine treatment MR2 values were statistically significantly higher than MRI. In 3 patients (27.3%) treated with clomipramine the changes of phenotype status were observed.
  
  
  CONCLUSIONS
  Clomipramine is a CYP2D6 inhibitor and may change the CYP2D6 phenotype status (EM into PM).
authors.affiliation: Katedra i Klinika Psychiatrii AM we Wrocławiu.
authors.forename: Monika
authors.initials: M
authors.lastname: Szewczuk-Bogusławska
authors.forename: Andrzej
authors.initials: A
authors.lastname: Kiejna
authors.forename: Magdalena
authors.initials: M
authors.lastname: Grzesiak
authors.forename: Jan Aleksander
authors.initials: JA
authors.lastname: Beszłej
authors.forename: Iwona
authors.initials: I
authors.lastname: Chlebowska
authors.forename: Krystyna
authors.initials: K
authors.lastname: Orzechowska-Juzwenko
authors.forename: Piotr
authors.initials: P
authors.lastname: Milejski
mesh_terms: D000328:Adult; D000368:Aged; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology* / Q000627:therapeutic use; D002997:Clomipramine / Q000494:pharmacology* / Q000627:therapeutic use; D019389:Cytochrome P-450 CYP2D6 / Q000187:drug effects* / Q000378:metabolism; D003863:Depression / Q000188:drug therapy* / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged
chemical_list: D000929:Antidepressive Agents, Tricyclic; D019389:Cytochrome P-450 CYP2D6; D002997:Clomipramine