Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance

The serum concentration achieved and maintained following the administration of a fixed drug dosage is a direct consequence of the interactions of a wide variety of interrelated processes, including drug absorption, distribution, metabolism, and excretion, and the physiological status of the patient...

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Main Author: Svein I. Johannessen
Format: Article
Language:English
Published: Wiley 1990-01-01
Series:Behavioural Neurology
Online Access:http://dx.doi.org/10.3233/BEN-1990-31S102
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author Svein I. Johannessen
author_facet Svein I. Johannessen
author_sort Svein I. Johannessen
collection DOAJ
description The serum concentration achieved and maintained following the administration of a fixed drug dosage is a direct consequence of the interactions of a wide variety of interrelated processes, including drug absorption, distribution, metabolism, and excretion, and the physiological status of the patient. These interrelationships are reviewed with specific reference to the major anti-epileptic drugs, phenobarbitone, phenytoin, sodium valproate, and carbamazepine, as well as a new first-line antiepileptic, oxcarbazepine. Both older drugs, such as phenobarbitone and phenytoin, and newer drugs, such as carbamazepine (CBZ) and sodium valproate, have been studied extensively over the past years giving valuable information for drug treatment. An important feature of oxcarbazepine (OXC) , which was developed through minimal changes in the structure of CBZ in order to improve on the tolerability of CBZ without sacrificing efficacy, is that its metabolites do not include the 11-epoxide which has been implicated in the side-effects of CBZ. In man, OXC is metabolized to a monohydroxy derivative which has independent anti-epileptic properties. OXC seems to lack several disadavantageous pharmacokinetic properties common to other major anti-epileptic drugs. OXC does not influence its own metabolism after repeated administration, in contrast to the auto-induction displayed by CBZ. The metabolism of OXC is not influenced by anti-epileptic co-medication and does not influence the kinetics of other anti-epileptic drugs – or if it does, then to a lesser extent than CBZ.
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spelling doaj-art-d6450f8ea7bc47f1a192e2103631eb972025-02-03T05:44:17ZengWileyBehavioural Neurology0953-41801875-85841990-01-013111110.3233/BEN-1990-31S102Pharmacokinetics of Anti-Epileptic Drugs and their Clinical SignificanceSvein I. Johannessen0The National Centre for Epilepsy, NorwayThe serum concentration achieved and maintained following the administration of a fixed drug dosage is a direct consequence of the interactions of a wide variety of interrelated processes, including drug absorption, distribution, metabolism, and excretion, and the physiological status of the patient. These interrelationships are reviewed with specific reference to the major anti-epileptic drugs, phenobarbitone, phenytoin, sodium valproate, and carbamazepine, as well as a new first-line antiepileptic, oxcarbazepine. Both older drugs, such as phenobarbitone and phenytoin, and newer drugs, such as carbamazepine (CBZ) and sodium valproate, have been studied extensively over the past years giving valuable information for drug treatment. An important feature of oxcarbazepine (OXC) , which was developed through minimal changes in the structure of CBZ in order to improve on the tolerability of CBZ without sacrificing efficacy, is that its metabolites do not include the 11-epoxide which has been implicated in the side-effects of CBZ. In man, OXC is metabolized to a monohydroxy derivative which has independent anti-epileptic properties. OXC seems to lack several disadavantageous pharmacokinetic properties common to other major anti-epileptic drugs. OXC does not influence its own metabolism after repeated administration, in contrast to the auto-induction displayed by CBZ. The metabolism of OXC is not influenced by anti-epileptic co-medication and does not influence the kinetics of other anti-epileptic drugs – or if it does, then to a lesser extent than CBZ.http://dx.doi.org/10.3233/BEN-1990-31S102
spellingShingle Svein I. Johannessen
Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
Behavioural Neurology
title Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
title_full Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
title_fullStr Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
title_full_unstemmed Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
title_short Pharmacokinetics of Anti-Epileptic Drugs and their Clinical Significance
title_sort pharmacokinetics of anti epileptic drugs and their clinical significance
url http://dx.doi.org/10.3233/BEN-1990-31S102
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