Detection of tolcapone in the cerebrospinal fluid of parkinsonian subjects

Naunyn Schmiedebergs Arch Pharmacol. 1999 Dec;360(6):719-20. doi: 10.1007/s002109900168.

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.

Publication types

  • Clinical Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Aged
  • Aged, 80 and over
  • Antiparkinson Agents / administration & dosage
  • Antiparkinson Agents / adverse effects
  • Antiparkinson Agents / cerebrospinal fluid*
  • Benzophenones / administration & dosage
  • Benzophenones / adverse effects
  • Benzophenones / cerebrospinal fluid*
  • Blood-Brain Barrier
  • Catechol O-Methyltransferase / cerebrospinal fluid
  • Catechol O-Methyltransferase Inhibitors
  • Chromatography, High Pressure Liquid
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / cerebrospinal fluid*
  • Female
  • Humans
  • Male
  • Middle Aged
  • Nitrophenols
  • Parkinson Disease / cerebrospinal fluid*
  • Parkinson Disease / drug therapy*
  • Tolcapone

Substances

  • Antiparkinson Agents
  • Benzophenones
  • Catechol O-Methyltransferase Inhibitors
  • Enzyme Inhibitors
  • Nitrophenols
  • Tolcapone
  • Catechol O-Methyltransferase