Abstract
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.
MeSH terms
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Adolescent
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Adult
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Area Under Curve
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Central Nervous System Stimulants / pharmacokinetics*
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Chromatography, Liquid
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Cytochrome P-450 CYP2D6 / genetics
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Cytochrome P-450 CYP2D6 / metabolism*
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Cytochrome P-450 CYP2D6 Inhibitors
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Enzyme Inhibitors / pharmacology
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Female
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Half-Life
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Humans
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Male
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Mass Spectrometry
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Methylphenidate / analogs & derivatives
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Methylphenidate / blood
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Methylphenidate / pharmacokinetics*
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Middle Aged
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Phenotype
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Polymorphism, Genetic
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Quinidine / antagonists & inhibitors
Substances
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Central Nervous System Stimulants
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Cytochrome P-450 CYP2D6 Inhibitors
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Enzyme Inhibitors
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Methylphenidate
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Cytochrome P-450 CYP2D6
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ritalinic acid
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Quinidine