Selected CSF biochemistry and gabapentin concentrations in the CSF and plasma in patients with partial seizures after a single oral dose of gabapentin

Epilepsy Res. 1992 Mar;11(1):45-9. doi: 10.1016/0920-1211(92)90020-t.


Gabapentin (GBP) is a neutral amino acid and a GABA analog which in animal experimental models has shown a broad anticonvulsant spectrum. To evaluate the penetration of GBP into the CSF in humans as well as its possible effects on free and total GABA, homovanillic acid (HVA), and 5-hydroxyindoleacetic acid (5-HIAA), a special investigation was performed as part of a placebo controlled add-on study of GBP in partial epilepsy. At the end of the 3-month double-blind period, 5 patients on placebo were given a single oral dose of GBP. Four patients received 600 mg and 1 patient 1200 mg GBP. CSF was collected immediately before and at 6, 24 and 72 h after the single dose. 5 ml of plasma was collected at 1, 2, 3, 6, 12, 24, 48 and 72 h. Plasma concentrations and plasma elimination half-life (4-6 h) of GBP were in agreement with the results of previous studies. The CSF/plasma concentration ratio of GBP 6 h after drug was 0.1. After 24 h, GBP could only be recovered in the CSF of the patient given 1200 mg. The CSF/plasma ratio at that time was 0.3. Free and total GABA concentrations did not change, but CSF 5-HIAA and HVA increased at 24 and 72 h post dose. The CSF/plasma ratio of gabapentin is similar to that of other amino acids.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Acetates / blood
  • Acetates / cerebrospinal fluid
  • Acetates / pharmacokinetics*
  • Acetates / pharmacology
  • Administration, Oral
  • Adult
  • Amines*
  • Anticonvulsants / blood
  • Anticonvulsants / cerebrospinal fluid
  • Anticonvulsants / pharmacokinetics*
  • Anticonvulsants / pharmacology
  • Chromatography, High Pressure Liquid
  • Cyclohexanecarboxylic Acids*
  • Epilepsies, Partial / blood
  • Epilepsies, Partial / cerebrospinal fluid
  • Epilepsies, Partial / drug therapy*
  • Female
  • Gabapentin
  • Homovanillic Acid / cerebrospinal fluid
  • Humans
  • Hydroxyindoleacetic Acid / cerebrospinal fluid
  • Male
  • Serotonin / cerebrospinal fluid
  • gamma-Aminobutyric Acid / cerebrospinal fluid


  • Acetates
  • Amines
  • Anticonvulsants
  • Cyclohexanecarboxylic Acids
  • Serotonin
  • Hydroxyindoleacetic Acid
  • gamma-Aminobutyric Acid
  • Gabapentin
  • Homovanillic Acid