Purpose: Although lamotrigine (LTG) has been used for years as an antiepile
pic drug (AED), there are no data on penetration into the brain with the ex
ception of a single case report. It was our aim to determine the LTG conten
t in the brain and the tumor tissue and to bring the same into relation to
the serum concentration and protein binding in neurosurgically operated pat
ients.
Methods: Neurosurgical intervention was performed on 11 patients with brain
turners. 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 mu g/ml (range 1.1-9.8); in the brain, an
average of 6.8 mu g/g (range, 1.0-14.9); and in the tumor, an average of 4
.4 mu g/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 pe
netrates brain tissue well and can be proven even in the tumor tissue.