Lamotrigine concentrations in human serum, brain tissue, and tumor tissue

Epilepsia. 1999 Jan;40(1):68-73. doi: 10.1111/j.1528-1157.1999.tb01990.x.


Purpose: Although lamotrigine (LTG) has been used for years as an antiepilepic drug (AED), there are no data on penetration into the brain with the exception of a single case report. It was our aim to determine the LTG content in the brain and the tumor tissue and to bring the same into relation to the serum concentration and protein binding in neurosurgically operated patients.

Methods: Neurosurgical intervention was performed on 11 patients with brain tumors. Tumor tissue was removed, and LTG kinetics was carried out for 12 h. LTG was determined by means of (HPLC) and the protein binding by means of ultrafiltration.

Results: At the time of the section of the tumor, the LTG concentrations in the serum were an average of 3.7 microg/ml (range, 1.1-9.8); in the brain, an average of 6.8 microg/g (range, 1.0-14.9); and in the tumor, an average of 4.4 microg/g (range, 2.0-8.3). Brain/serum and tumor/serum ratios of 2.8 and 1.9, respectively, result from these data. The protein binding was on average 68% (range, 46-96).

Conclusions: LTG is a lipophile AED with a moderate protein binding that penetrates brain tissue well and can be proven even in the tumor tissue.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Animals
  • Anticonvulsants / analysis*
  • Anticonvulsants / blood
  • Anticonvulsants / pharmacokinetics
  • Blood-Brain Barrier
  • Brain / metabolism*
  • Brain Chemistry*
  • Brain Neoplasms / chemistry*
  • Brain Neoplasms / metabolism
  • Chromatography, High Pressure Liquid
  • Epilepsy / drug therapy
  • Epilepsy / metabolism
  • Female
  • Humans
  • Lamotrigine
  • Male
  • Middle Aged
  • Protein Binding
  • Tissue Distribution
  • Triazines / analysis*
  • Triazines / blood
  • Triazines / pharmacokinetics
  • Ultrafiltration


  • Anticonvulsants
  • Triazines
  • Lamotrigine