Single-dose pharmacokinetics of methylphenidate in CYP2D6 extensive and poor metabolizers.
Six adults phenotyped as either extensive (N = 4) or poor (N = 2) metabolizers for cytochrome P450 (CYP) 2D6 were given a 10-mg oral dose of methylphenidate (MPH) on two separate occasions with and without quinidine, a potent CYP2D6 inhibitor. Quinidine had no significant effect on the pharmacokinetics of either MPH or ritalinic acid, its major metabolite, in either group of CYP2D6 metabolizers. These data suggest a lack of involvement of CYP2D6 in the metabolism of MPH. Drugs that are inhibitors of CYP2D6 when taken concurrently with MPH should not affect its plasma concentration.
DeVane
C L
CL
Department of Psychiatry and Behavioral Sciences, Medical University of South Carolina, Charleston 29425, USA. devanel@musc.edu
Markowitz
J S
JS
Carson
S W
SW
Boulton
D W
DW
Gill
H S
HS
Nahas
Z
Z
Risch
S C
SC
D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D000697:Central Nervous System Stimulants / Q000493:pharmacokinetics*; D002853:Chromatography, Liquid; D019389:Cytochrome P-450 CYP2D6 / Q000235:genetics / Q000378:metabolism*; D065690:Cytochrome P-450 CYP2D6 Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D008774:Methylphenidate / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics*; D008875:Middle Aged; D010641:Phenotype; D011110:Polymorphism, Genetic; D011802:Quinidine / Q000037:antagonists & inhibitors
D000697:Central Nervous System Stimulants; D065690:Cytochrome P-450 CYP2D6 Inhibitors; D004791:Enzyme Inhibitors; D008774:Methylphenidate; D019389:Cytochrome P-450 CYP2D6; C009189:ritalinic acid; D011802:Quinidine