Pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures.
OBJECTIVE
The pharmacokinetics of gabapentin in paediatric patients with uncontrolled seizures was studied.


METHODS
Thirteen paediatric patients (mean age: 9.4 years) with uncontrolled partial seizures were included. Patients received gabapentin orally until doses were individualized to 9.6-39.8 mg/kg/day. Blood samples were obtained just prior to the dose and over 8 h after gabapentin was administered in the fasting state. The plasma concentration of gabapentin was measured by a high-performance liquid chromatography assay. Pharmacokinetic parameters for gabapentin were determined by non-compartment methods using multivariate regression analysis.


RESULTS
Data from nine patients were suitable for pharmacokinetic analysis. The C(max) from 0.9 to 5.8 microg/mL (mean: 2.6 +/- 1.7 microg/mL) and T(max) from 0.5 to 2.0 h (mean: 1.6 +/- 1.0 h). The apparent clearance (Cl/F) ranged from 0.12 to 1.12 L/h/kg (mean: 0.50 +/- 0.29 L/h/kg), and the elimination half-life from 3.2 to 12.2 h (mean: 5.5 +/- 0.8 h). Five patients experienced moderate (n = 4) to severe (n = 1) aggressive behaviour and another gained weight on gabapentin.


CONCLUSIONS
Our data suggests that gabapentin pharmacokinetics can vary substantially among paediatric patients. Gabapentin was well tolerated in patients with uncontrolled partial seizures up to 6 months of therapy.
Tallian
K B
KB
Children's Hospital, San Diego, CA, USA.
Nahata
M C
MC
Lo
W
W
Tsao
C-Y
CY
D000293:Adolescent; D000588:Amines / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000927:Anticonvulsants / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D002648:Child; D002675:Child, Preschool; D003509:Cyclohexanecarboxylic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D020937:Epilepsy, Partial, Sensory / Q000188:drug therapy*; D005260:Female; D000077206:Gabapentin; D006801:Humans; D008297:Male; D015999:Multivariate Analysis; D013997:Time Factors; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use
D000588:Amines; D000927:Anticonvulsants; D003509:Cyclohexanecarboxylic Acids; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin