Update on the Mechanism of Action of Antiepileptic Drugs

Update on the Mechanism of Action of Antiepileptic Drugs Summary: Novel antiepileptic drugs (AEDs) are thought to act on voltage‐sensitive ion channels, on inhibitory neurotransmission or on excitatory neurotransmission. Two successful examples of rational AED design that po tentiate GABA‐mediated inhibition are vigabatrin (VGB) by irreversible inhibition of GABA‐transaminase, and ti‐agabine (TGB) by blocking GAB A uptake. Lamotrigine (LTG) prolongs inactivation of voltage‐dependent sodium channels. The anticonvulsant action of remacemide (RCM) is probably largely due to blockade of NMDA receptors and prolonged inactivation of sodium channels induced by its desglycinated metabolite. Felbamate (FBM) apparently blocks NMDA receptors, potentiates GABA‐mediated responses, blocks L‐type calcium channels, and possibly also prolongs sodium channel inactivation. Similarly, to piramate (TPM) has multiple probable sites of action, including sodium channels, GABA receptors, and glutamate (AMPA) receptors. Gabapentin (GBP) apparently has a completely novel type of action, probably involving potentiation of GABA‐mediated inhibition and possibly also inactivation of sodium channels. The therapeutic advantages of the novel AEDs are as yet only partially explained by our present understanding of their. Mechanisms of action. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Epilepsia Wiley

Update on the Mechanism of Action of Antiepileptic Drugs

Epilepsia, Volume 37 – Dec 1, 1996

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Publisher
Wiley
Copyright
Copyright © 1996 Wiley Subscription Services, Inc., A Wiley Company
ISSN
0013-9580
eISSN
1528-1167
D.O.I.
10.1111/j.1528-1157.1996.tb06038.x
Publisher site
See Article on Publisher Site

Abstract

Summary: Novel antiepileptic drugs (AEDs) are thought to act on voltage‐sensitive ion channels, on inhibitory neurotransmission or on excitatory neurotransmission. Two successful examples of rational AED design that po tentiate GABA‐mediated inhibition are vigabatrin (VGB) by irreversible inhibition of GABA‐transaminase, and ti‐agabine (TGB) by blocking GAB A uptake. Lamotrigine (LTG) prolongs inactivation of voltage‐dependent sodium channels. The anticonvulsant action of remacemide (RCM) is probably largely due to blockade of NMDA receptors and prolonged inactivation of sodium channels induced by its desglycinated metabolite. Felbamate (FBM) apparently blocks NMDA receptors, potentiates GABA‐mediated responses, blocks L‐type calcium channels, and possibly also prolongs sodium channel inactivation. Similarly, to piramate (TPM) has multiple probable sites of action, including sodium channels, GABA receptors, and glutamate (AMPA) receptors. Gabapentin (GBP) apparently has a completely novel type of action, probably involving potentiation of GABA‐mediated inhibition and possibly also inactivation of sodium channels. The therapeutic advantages of the novel AEDs are as yet only partially explained by our present understanding of their. Mechanisms of action.

Journal

EpilepsiaWiley

Published: Dec 1, 1996

References

  • Cellular and molecular biology of voltage‐gated sodium channels
    Catterall, Catterall
  • A review of the preclinical pharmacology of tiagabine: a potent and selective anticonvulsant GABA uptake inhibitor
    Suzdak, Suzdak; Jansen, Jansen
  • Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA
    Goldlust, Goldlust; Su, Su; Welty, Welty; Taylor, Taylor; Oxender, Oxender
  • The effect of gabapentin on brain GABA in patients with epilepsy
    Petroff, Petroff; Rothman, Rothman; Behar, Behar; Lamoureux, Lamoureux; Mattson, Mattson
  • Felbamate block of the N‐methyl‐D‐aspartate receptor
    Subramaniam, Subramaniam; Rho, Rho; Penix, Penix; Donevan, Donevan; Fielding, Fielding; Rogawski, Rogawski
  • Electrophysiological actions of felbamate on rat striatal neurones
    Pisani, Pisani; Stefani, Stefani; Siniscalchi, Siniscalchi; Mercuri, Mercuri; Bernardi, Bernardi; Calabresi, Calabresi

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