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The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come?
Epileptic Disord. 2003 May; 5 Suppl 1:S17-26.ED

Abstract

The pharmacokinetic properties of a drug are the primary deter-minant 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 num-ber of pharmacokinetic advantages, particularly in terms of reduced inter-patient 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.

Authors+Show Affiliations

Clinical Pharmacology Unit, University of Pavia, Pavia, Italy. perucca@unipv.itNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

12915337

Citation

Perucca, Emilio, and Svein I. Johannessen. "The Ideal Pharmacokinetic Properties of an Antiepileptic Drug: How Close Does Levetiracetam Come?" Epileptic Disorders : International Epilepsy Journal With Videotape, vol. 5 Suppl 1, 2003, pp. S17-26.
Perucca E, Johannessen SI. The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come? Epileptic Disord. 2003;5 Suppl 1:S17-26.
Perucca, E., & Johannessen, S. I. (2003). The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come? Epileptic Disorders : International Epilepsy Journal With Videotape, 5 Suppl 1, S17-26.
Perucca E, Johannessen SI. The Ideal Pharmacokinetic Properties of an Antiepileptic Drug: How Close Does Levetiracetam Come. Epileptic Disord. 2003;5 Suppl 1:S17-26. PubMed PMID: 12915337.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come? AU - Perucca,Emilio, AU - Johannessen,Svein I, PY - 2003/8/14/pubmed PY - 2003/10/24/medline PY - 2003/8/14/entrez SP - S17 EP - 26 JF - Epileptic disorders : international epilepsy journal with videotape JO - Epileptic Disord VL - 5 Suppl 1 N2 - The pharmacokinetic properties of a drug are the primary deter-minant 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 num-ber of pharmacokinetic advantages, particularly in terms of reduced inter-patient 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. SN - 1294-9361 UR - https://www.unboundmedicine.com/medline/citation/12915337/The_ideal_pharmacokinetic_properties_of_an_antiepileptic_drug:_how_close_does_levetiracetam_come L2 - https://medlineplus.gov/epilepsy.html DB - PRIME DP - Unbound Medicine ER -