1. Detection of tolcapone in the cerebrospinal fluid of parkinsonian subjects.
- Author
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Russ H, Müller T, Woitalla D, Rahbar A, Hahn J, and Kuhn W
- Subjects
- Administration, Oral, Adult, Aged, Aged, 80 and over, Antiparkinson Agents administration & dosage, Antiparkinson Agents adverse effects, Benzophenones administration & dosage, Benzophenones adverse effects, Blood-Brain Barrier, Catechol O-Methyltransferase cerebrospinal fluid, Catechol O-Methyltransferase Inhibitors, Chromatography, High Pressure Liquid, Enzyme Inhibitors administration & dosage, Enzyme Inhibitors adverse effects, Female, Humans, Male, Middle Aged, Nitrophenols, Tolcapone, Antiparkinson Agents cerebrospinal fluid, Benzophenones cerebrospinal fluid, Enzyme Inhibitors cerebrospinal fluid, Parkinson Disease cerebrospinal fluid, Parkinson Disease drug therapy
- Abstract
The cerebral availability of the peripherally and centrally acting catechol-O-methyltransferase (COMT) inhibitor tolcapone is not known in humans. Therefore, we determined the concentration of tolcapone in cerebrospinal fluid (CSF) of 12 parkinsonian subjects 1-4 h after oral application of 200 mg of the drug. The mean concentration was 56.4+/-35.5 nmol/l (mean +/- SD). This concentration was calculated to cause 75.2+/-15% (mean +/- SD) inhibition of COMT in CSF. Thus, tolcapone efficiently inhibits COMT after crossing the blood-brain barrier in humans.
- Published
- 1999
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