The clinical pharmacokinetics of the new antiepileptic drugs

Research output: Contribution to journalArticle

Abstract

Because pharmacokinetics is a major determinant of the magnitude and duration of pharmacologic response, understanding the kinetic properties of the new antiepileptic drugs (AEDs) is essential for the correct use of these compounds in clinical practice. After oral administration, absorption is rapid and relatively efficient for the new AEDs, the most notable exception being gabapentin, whose bioavailability decreases with increasing dosage. None of the new AEDs is extensively bound to plasma proteins except for tiagabine, which is over 95% protein-bound. The route of elimination differs to an important extent from one compound to another, and elimination half- lives range from over 30 h for zonisamide to 5-7 h for gabapentin. For all drugs that are metabolized, half-life is shortened and clearance is increased when patients receive concomitant enzyme-inducing agents such as barbiturates, phenytoin, and carbamazepine. Lamotrigine metabolism is markedly inhibited by valproic acid, and felbamate may increase the serum levels of most other AEDs. Felbamate, topiramate, and oxcarhazepine may also reduce the efficacy of the contraceptive pill by stimulating its metabolism.

Original languageEnglish
JournalEpilepsia
Volume40
Issue numberSUPPL. 9
Publication statusPublished - 1999

Fingerprint

felbamate
Anticonvulsants
Pharmacokinetics
zonisamide
Barbiturates
Carbamazepine
Valproic Acid
Phenytoin
Contraceptive Agents
Biological Availability
Oral Administration
Half-Life
Blood Proteins
Enzymes
Serum
Pharmaceutical Preparations
Proteins
gabapentin

Keywords

  • Antiepileptics
  • Drug interactions
  • Pharmacokinetics

ASJC Scopus subject areas

  • Clinical Neurology
  • Neuroscience(all)

Cite this

The clinical pharmacokinetics of the new antiepileptic drugs. / Perucca, Emilio.

In: Epilepsia, Vol. 40, No. SUPPL. 9, 1999.

Research output: Contribution to journalArticle

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