Determination of gabapentin-lactam in serum of patients under gabapentin therapy.
Gabapentin (1-(aminomethyl)cyclohexane acetic acid, CAS 601 42-96-3, GBP, Neurontin) and its derivative gabapentin-lactam (8-aza-spiro[5,4]decan-9-one, GBP-L) were determined by HPLC in the serum of patients with focal epilepsy treated with GBP. In patients in whom serum was acquired within 3 h after oral intake, GBP-L could be detected at concentrations up to 8.2 micromol/l. As GBP-L has been previously shown to exert neuroprotective effects in a similar concentration range, this finding suggests that clinically relevant effects of GBP-L may occur in patients treated with GBP. The possible neuroprotective efficacy of GBP-L should be the subject of further preclinical and clinical investigations.
Knörle
Rainer
R
Institut für biochemische Analysen und Methodenentwicklung GbR, Freiburg/Brsg., Germany.
Feuerstein
Thomas J
TJ
Schulze-Bonhage
Andreas
A
D000085:Acetates / Q000097:blood* / Q000627:therapeutic use; D000328:Adult; D000588:Amines; D000927:Anticonvulsants / Q000097:blood* / Q000627:therapeutic use; D001372:Aza Compounds / Q000097:blood* / Q000627:therapeutic use; D002852:Chromatography, Ion Exchange; D003509:Cyclohexanecarboxylic Acids; D004305:Dose-Response Relationship, Drug; D004827:Epilepsy / Q000188:drug therapy*; D005260:Female; D000077206:Gabapentin; D006801:Humans; D008297:Male; D008875:Middle Aged; D013141:Spiro Compounds / Q000097:blood* / Q000627:therapeutic use; D005680:gamma-Aminobutyric Acid
D000085:Acetates; D000588:Amines; D000927:Anticonvulsants; D001372:Aza Compounds; D003509:Cyclohexanecarboxylic Acids; D013141:Spiro Compounds; C404763:gabapentin-lactam; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin