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The clinical pharmacokinetics of the new antiepileptic drugs.
Epilepsia. 1999; 40 Suppl 9:S7-13.E

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 oxcarbazepine may also reduce the efficacy of the contraceptive pill by stimulating its metabolism.

Authors+Show Affiliations

Department of Internal Medicine and Therapeutics, University of Pavia, Italy.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

10612356

Citation

Perucca, E. "The Clinical Pharmacokinetics of the New Antiepileptic Drugs." Epilepsia, vol. 40 Suppl 9, 1999, pp. S7-13.
Perucca E. The clinical pharmacokinetics of the new antiepileptic drugs. Epilepsia. 1999;40 Suppl 9:S7-13.
Perucca, E. (1999). The clinical pharmacokinetics of the new antiepileptic drugs. Epilepsia, 40 Suppl 9, S7-13.
Perucca E. The Clinical Pharmacokinetics of the New Antiepileptic Drugs. Epilepsia. 1999;40 Suppl 9:S7-13. PubMed PMID: 10612356.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The clinical pharmacokinetics of the new antiepileptic drugs. A1 - Perucca,E, PY - 1999/12/28/pubmed PY - 1999/12/28/medline PY - 1999/12/28/entrez SP - S7 EP - 13 JF - Epilepsia JO - Epilepsia VL - 40 Suppl 9 N2 - 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 oxcarbazepine may also reduce the efficacy of the contraceptive pill by stimulating its metabolism. SN - 0013-9580 UR - https://www.unboundmedicine.com/medline/citation/10612356/The_clinical_pharmacokinetics_of_the_new_antiepileptic_drugs_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0013-9580&date=1999&volume=40&issue=&spage=S7 DB - PRIME DP - Unbound Medicine ER -