The ideal pharmacokinetic properties of an antiepileptic drug: How close does levetiracetam come?

Emilio Perucca, Svein I. Johannessen

Research output: Contribution to journalArticlepeer-review


The pharmacokinetic properties of a drug are the primary determinant of the extent and duration of drug action, and influence susceptibility to clinically important drug interactions. Most of the older-generation antiepileptic drugs (AEDs) are far from ideal in terms of pharmacokinetics and interaction potential. For example, phenytoin, carbamazepine, and valproic acid exhibit non-linear kinetics; carbamazepine and valproic acid have relatively short half-lives; and most of these drugs cause either enzyme induction (phenytoin, phenobarbital, primidone, carbamazepine) or enzyme inhibition (valproic acid). Compared with older agents, certain new-generation AEDs offer a number of pharmacokinetic advantages, particularly in terms of reduced interpatient variability in drug clearance and a lower interaction potential. One of the most recently developed of these drugs, levetiracetam, comes especially close to fulfilling the desirable pharmacokinetic characteristics for an AED: (1) it has a high oral bioavailability, which is unaffected by food; (2) it is not significantly bound to plasma proteins; (3) it is eliminated partly in unchanged form by the kidneys and partly by hydrolysis to an inactive metabolite, without involvement of oxidative and conjugative enzymes; (4) it has linear kinetics; and (5) it is not vulnerable to important drug interactions, nor does it cause clinically significant alterations in the kinetics of concomitantly administered drugs. Although its half-life is relatively short (6 to 8 hours), its duration of action is longer than anticipated from its pharmacokinetics in plasma, and a twice-daily dosing regimen is adequate to produce the desired response.

Original languageEnglish
JournalEpileptic Disorders
Issue numberSUPPL. 1
Publication statusPublished - May 2003


  • Antiepileptic drugs
  • Drug interactions
  • Levetiracetam
  • Pharmacokinetics
  • Review

ASJC Scopus subject areas

  • Clinical Neurology


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