Disposition of perphenazine is related to polymorphic debrisoquin hydroxylation in human beings.
The pharmacokinetics of a single oral dose of 6 mg perphenazine was studied in a group of six slow and six rapid hydroxylators of debrisoquin. Peak serum concentrations of perphenazine were significantly higher in slow hydroxylators than they were in rapid hydroxylators (2.4 +/- 0.6 versus 0.7 +/- 0.3 nmol/L, p less than 0.001). The AUC(0-12) was also higher in slow hydroxylators than it was in rapid hydroxylators (18.5 +/- 6.2 versus 4.5 +/- 2.5 nmol.L-1.hr, p less than 0.001). The data suggest that the disposition of the antipsychotic drug perphenazine covaries with polymorphic debrisoquin hydroxylation.
Dahl-Puustinen
M L
ML
Department of Clinical Pharmacology, Karolinska Institute, Huddinge Hospital, Sweden.
Lidén
A
A
Alm
C
C
Nordin
C
C
Bertilsson
L
L
D000284:Administration, Oral; D000328:Adult; D003647:Debrisoquin / Q000378:metabolism*; D005260:Female; D006801:Humans; D006900:Hydroxylation; D007546:Isoquinolines / Q000378:metabolism*; D008297:Male; D010546:Perphenazine / Q000493:pharmacokinetics*; D011110:Polymorphism, Genetic
D007546:Isoquinolines; D010546:Perphenazine; D003647:Debrisoquin