Pharmacokinetics and safety of lamotrigine (Lamictal) in patients with epilepsy

Epilepsy Res. Nov-Dec 1991;10(2-3):191-200. doi: 10.1016/0920-1211(91)90012-5.

Abstract

In a double-blind parallel study, patients with epilepsy on stable regimen of antiepileptic drugs (AEDs) were given lamotrigine (8 pts) or placebo (3 pts). Patients were sequentially dosed with 100, 200 and 300 mg/day given as a b.i.d. regimen. After steady state was achieved, timed plasma lamotrigine levels were obtained post dose. No medical, psychogenic, neurologic, or hematologic changes were observed and no subjective effects were detected as a result of treatment with lamotrigine. No changes in heart rhythm or blood pressure were observed related to lamotrigine. Pharmacokinetic parameters were calculated using 1-compartment and non-compartment models. The results were similar using both models. Area under the plasma concentration vs. time curves increased linearly with dose. Mean half life (13.5 h), volume of distribution (1.36 l/kg) and clearance (1.27 ml/min/kg) were similar to previously reported results and did not change with increasing dose. These findings indicate that lamotrigine pharmacokinetics can be described by the 1-compartment model, has linear kinetics, and does not induce its own metabolism in patients on concomitant AEDs.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Anticonvulsants / adverse effects
  • Anticonvulsants / pharmacokinetics*
  • Double-Blind Method
  • Epilepsy / metabolism*
  • Female
  • Humans
  • Lamotrigine
  • Male
  • Middle Aged
  • Triazines / adverse effects
  • Triazines / pharmacokinetics*

Substances

  • Anticonvulsants
  • Triazines
  • Lamotrigine