The mechanisms of action of commonly used antiepileptic drugs

Pharmacology and Therapeutics

Volumn 90, Issue 1, 2001, Pages 21-34

  Kwan, Patrick ^a   Sills, Graeme J ^a   Brodie, Martin J ^a  

^a WESTERN INFIRMARY   (United Kingdom)

Author keywords

Antiepileptic drugs; Epilepsy; Mechanisms of action

Indexed keywords

4 AMINOBUTYRIC ACID; ANTICONVULSIVE AGENT; BENZODIAZEPINE DERIVATIVE; CALCIUM CHANNEL; CARBAMAZEPINE; CLOBAZAM; CLONAZEPAM; DIAZEPAM; ETHOSUXIMIDE; ETIRACETAM; FELBAMATE; GABAPENTIN; GLUTAMIC ACID; LAMOTRIGINE; LORAZEPAM; OXCARBAZEPINE; PHENOBARBITAL; PHENYTOIN; POTASSIUM CHANNEL; SODIUM CHANNEL; TIAGABINE; TOPIRAMATE; VALPROIC ACID; VIGABATRIN; ZONISAMIDE;

CHANNEL GATING; CHEMICAL STRUCTURE; DRUG CLASSIFICATION; DRUG MECHANISM; DRUG POTENTIATION; DRUG STRUCTURE; DRUG TARGETING; HUMAN; NEUROMODULATION; NEUROTRANSMISSION; NONHUMAN; PRIORITY JOURNAL; REVIEW;

ANIMALS; ANTICONVULSANTS; EPILEPSY; GAMMA-AMINOBUTYRIC ACID; GLUTAMIC ACID; HUMANS; ION CHANNELS; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP; SYNAPTIC TRANSMISSION;

EID: 0034935392     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(01)00122-X     Document Type: Review

References (174)

1. Electrophysiologic analysis of the actions of valproate on pyramidal neurons in the rat hippocampal slices
2. Randomised, placebo-controlled study of vigabatrin as first-line treatment of infantile spasms
3. Ion channel mutations affecting muscle and brain
4. Progress report on new antiepileptic drugs: A summary of the fourth Eilat conference
5. Levetiracetam (ucb L059) affects in vitro models of epilepsy in CA3 pyramidal neurons without altering normal synaptic transmission
6. Molecular heterogeneity of the γ-aminobutyric acid (GABA) transport system
7. Tiagabine, SKF 89976-A, CI-966, and NNC-711 are selective for cloned GABA transporter GAT-1
8. Primidone, phenobarbital and PEMA: I. Seizure protection, neurotoxicity and therapeutic index of individual compounds in mice
9. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain γ-aminobutyric acid uptake carrier
10. Tiagabine pharmacology in profile
11. Monostars: An aid to choosing an antiepileptic drug as monotherapy
12. Antiepileptic drugs
13. Established antiepileptic drugs
14. Management of epilepsy in adolescents and adults
15. The "star" systems: Overview and use in determining drug choice for patients with epilepsy
16. Lamotrigine substitution study - Evidence for synergism with sodium valproate?
17. Action of GP 47779, the active metabolite of oxcarbazepine, on the corticostriatal system I. Modulation of corticostriatal synaptic transmission
18. Cellular and molecular biology of voltage-gated sodium channels
19. Structure and function of voltage-gated ion channels
20. Acute anticonvulsant activity of structural analogues of valproic acid and changes in brain GABA and aspartate content
21. Anticonvulsant activity of intracerebroventricularly administered valproate and valproate analogues. A dose-dependent correlation with changes in brain aspartate and GABA levels in DBA/2 mice
22. An in vitro investigation of the action of lamotrigine on neuronal voltage-activated sodium channels
23. Selective antagonism of the anticonvulsant effects of felbamate by glycine
24. Antiepileptic drug cellular mechanisms of action: Where does lamotrigine fit in?
25. Calcium currents in rat thalamocortical relay neurones: Kinetic properties of the transient low-threshold current
26. Specific petit mal anticonvulsants reduce calcium currents in thalamic neurons
27. Characterization of ethosuximide reduction of low-threshold calcium currents in thalamic neurons
28. Modulated anticonvulsant block of sodium channels in nerve and muscle
29. Compartmentation of brain glutamate metabolism in neurons and glia
30. Anticonvulsant doses of carbamazepine increase hippocampal extracellular serotonin in genetically epilepsy-prone rats: Dose response relationships
31. 2+
32. Mechanisms of action of antiepileptic drugs
33. Effects of topiramate on sustained repetitive firing and spontaneous recurrent seizure discharges in cultured hippocampal neurons
34. New antiepileptic drugs
35. Voltage-dependent calcium channels and their modulation by neurotransmitters and G proteins
36. The effect of tiagabine HCl on extracellular GABA levels in the human hippocampus
37. Sodium valproate
38. Oxcarbazepine
39. The γ-aminobutyric acid (GABA) uptake inhibitor, tiagabine, increases extracellular brain levels of GABA in awake rats
40. + channel openers decrease seizures in genetically epileptic rats
41. The novel anticonvulsant drug, gabapentin (Neurontin), binds to the α2δ subunit of a calcium channel
42. Piracetam and levetiracetam: Close structural similarities but different pharmacological and clinical profiles
43. Cellular actions of topiramate: Blockade of kainate-evoked inward currents in cultured hippocampal neurons
44. Effects of the anticonvulsant drug gabapentin on enzymes in the metabolic pathways of glutamate and GABA
45. Interaction of felbamate and diazepam against maximal electroshock seizures and chemoconvulsants in mice
46. Effects of gabapentin on release of γ-aminobutyric acid from slices of rat neostriatum
47. Modulation of the γ-aminobutyric acid type A receptor by the antiepileptic drugs carbamazepine and phenytoin
48. Cloning and expression of a rat brain GABA transporter
49. 2+ channel diversity
50. Carbamazepine inhibition of N-methyl-D-aspartate-evoked calcium influx in rat cerebellar granule cells
51. A receptor pharmacology
52. γ-Vinyl GABA (4-amino-hex-5-enoic acid), a new irreversible inhibitor of GABA-T: Effects on brain GABA metabolism in mice
53. Vigabatrin, a gabaergic antiepileptic drug, causes concentric visual field defects
54. 2+ mobilization in rat hippocampus
55. Valproic acid selectively reduces the low-threshold (T) calcium current in rat nodose neurons
56. GABA uptake inhibitors: Relevance to antiepileptic drug research
57. + channels in rat hippocampal neurones
58. + currents: Quantitative distinction from phenytoin and possible therapeutic implications
59. Early identification of refractory epilepsy
60. Zonisamide for progressive myoclonus epilepsy: Long-term observations in seven patients
61. + current
62. Lamotrigine, phenytoin and carbamazepine interactions on the sodium current present in N4TG1 mouse neuroblastoma cells
63. Lamotrigine: Clinical use
64. Tiagabine
65. Effects of tiagabine and vigabatrin on GABA uptake into rat cortical astrocytes in primary culture
66. Neurochemical actions of gabapentin in mouse brain
67. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action
68. Zonisamide
69. Efficacy and safety of zonisamide: Results of a multicenter study
70. 4-Amino-hex-5-eonic acid, a selective catalytic inhibitor of 4-aminobutyric-acid aminotransferase in mammalian brain
71. New visions in the pharmacology of anticonvulsion
72. Valproate: A reappraisal of its pharmacodynamic properties and mechanisms of action
73. Profile of ucb L059, a novel anticonvulsant drug, in models of partial and generalized epilepsy in mice and rats
74. The novel antiepileptic drug levetiracetam (ucb L059) induces alterations in GABA metabolism and turnover in discrete areas of rat brain and reduces neuronal activity in substantia nigra pars reticulata
75. Mechanisms of action of new antiepileptic drugs
76. Antiepileptic drug mechanisms of action
77. A receptor channel of mouse spinal neurones in culture
78. Specific and potent interactions of carbamazepine with brain adenosine receptors
79. ucb L059, a novel anticonvulsant, reduces bicuculline-induced hyperexcitability in rat hippocampal CA3 in vivo
80. A receptor-associated epileptiform effect of bicuculline in rat hippocampus
81. Comparison of carbamazepine, phenobarbital, phenytoin and primidone in partial and secondary generalised tonic-clonic seizures
82. Evidence of anticonvulsant and neuroprotective action of felbamate mediated by strychnine-insensitive glycine receptors
83. Multiple actions of phenytoin on mouse spinal cord neurons in cell culture
84. Sodium valproate, but not ethosuximide, produces use- and voltage-dependent limitation of high frequency repetitive firing of action potentials of mouse central neurons in cell culture
85. Oxcarbazepine: Mechanisms of action
86. Neurotransmission in epilepsy
87. Update on the mechanism of action of antiepileptic drugs
88. Glutamate as a neurotransmitter in the brain: Review of physiology and pathology
89. Basic mechanisms of Gabitril (tiagabine) and future potential developments
90. Glutamate receptors and transporters in genetic and acquired models of epilepsy
91. Sodium diphenyl hydantoinate in the treatment of convulsive disorders
92. er memoire: Proprietes antiepileptique
93. 3H]Zonisamide binding in rat brain
94. Ion channels in epilepsy
95. + channels by phenytoin in rat neuroblastoma cells
96. The novel antiepileptic drug levetiracetam (ucb L059) appears to act via a specific binding site in CNS membranes
97. Effects of zonisamide on dopaminergic system
98. GABA and epileptogenesis
99. 2+ channel defects in migraine, ataxia and epilepsy
100. Felbamate: An update
101. Measuring human brain GABA in vivo: Effects of GABA-transaminase inhibition with vigabatrin
102. The effect of gabapentin on brain γ-aminobutyric acid in patients with epilepsy
103. Human brain GABA levels rise after initiation of vigabatrin therapy but fail to rise further with increasing dose
104. Topiramate increases brain GABA, homocarnosine, and pyrrolidinone in patients with epilepsy
105. Electrophysiological actions of felbamate on rat striatal neurones
106. Voltage-gated potassium channels: From hyperexcitability to excitement
107. New antiepileptic drugs: From serendipity to rational discovery
108. Effects of the antiepileptic drug felbamate on long-term potentiation in the CA1 region of rat hippocampal slices
109. A receptor research
110. Sodium channels as molecular targets for antiepileptic drugs
111. + channels
112. Anticonvulsant therapy, megaloblastic haemopoiesis and folic acid metabolism
113. The pharmacologic basis of antiepileptic drug action
114. A receptors
115. A receptors by barbiturates in cultured rat hippocampal neurons
116. Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate
117. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912): A novel anticonvulsant
118. Comparison of the effect of GABA uptake blockers, tiagabine and nipecotic acid, on inhibitory synaptic efficacy in hippocampal CA1 neurones
119. + channels and the molecular pathogenesis of epilepsy: Implications for therapy
120. Antiepileptic drugs: Pharmacological mechanisms and clinical efficacy with consideration of promising developmental stage compounds
121. D-23129: A new anticonvulsant with a broad spectrum activity in animal models of epileptic seizures
122. Differential effects of phenytoin and sodium valproate on seizure-induced changes in γ-aminobutyric acid and glutamate release in vivo
123. The novel anticonvulsant retigabine activates M-currents in Chinese hamster ovary-cells transfected with human KCNQ2/3 subunits
124. Review of the mechanisms of action of antiepileptic drugs
125. Zonisamide enhances slow sodium inactivation in Myxicola
126. Audiogenic seizure protection by elevated brain GABA concentration in mice: Effects of γ-acetylenic GABA and γ-vinyl GABA, two irreversible GABA-T inhibitors
127. Effect of n-dipropylacetate on amino acid concentrations in mouse brain: Correlation with anticonvulsant activity
128. Effects of phenytoin, carbamazepine, and gabapentin on calcium channels in hippocampal granule cells from patients with temporal lobe epilepsy
129. + currents in mammalian myelinated nerve fibers
130. Topiramate: Preclinical evaluation of a structurally novel anticonvulsant
131. Antiepileptic drug action in primary cultures of rat cortical astrocytes
132. Neurochemical studies with the novel anticonvulsant levetiracetam in mouse brain
133. Vigabatrin and tiagabine are pharmacologically different drugs. A pre-clinical study
134. Concentration-effect studies with topiramate on selected enzymes and intermediates of the GABA shunt
135. Differential block of two types of sodium channels by anticonvulsants
136. Benzodiazepine receptors in rat brain
137. +-stimulated release of glutamate from mouse cortex
138. Action of GP 47779, the active metabolite of oxcarbazepine, on the corticostriatal system. II. Modulation of high-voltage-activated calcium currents
139. Felbamate inhibits dihydropyridine-sensitive calcium channels in central neurons
140. 2+ currents in cortical neurons: Functional implications
141. Voltage-activated calcium channels: Targets of antiepileptic drug therapy?
142. The functional states of the thalamus and the associated neuronal interplay
143. Diazepam and ( - )-pentobarbital: Fluctuation analysis reveals different mechanisms for potentiation of γ-aminobutyric acid responses in cultured central neurons
144. Transport of gabapentin, a γ-amino acid drug, by system l γ-amino acid transporters: A comparative study in astrocytes, synaptosomes, and CHO cells
145. Zonisamide blocks T-type calcium channels in cultured neurons of rat cerebral cortex
146. + channels from human and rat brain
147. In vitro and in vivo electrophysiology effects of the anticonvulsant gabapentin
148. 3-Alkyl GABA and 3-alkylglutamic acid analogues: Two new classes of anticonvulsant agents
149. A summary of mechanistic hypotheses of gabapentin pharmacology
150. 2+ concentration
151. Oxcarbazepine
152. Effect of lamotrigine on the electrically-evoked release of endogenous amino acids from slices of dorsal horn of the rat spinal cord
153. Effect of anticonvulsant felbamate on GABA receptor system
154. A comparison of four treatments for generalized convulsive status epilepticus
155. Excitatory amino acid agonists and antagonists: Pharmacology and therapeutic applications
156. Basis of the antiseizure action of phenytoin
157. Differential regulation of γ-aminobutyric acid receptor channels by diazepam and phenobarbital
158. Mechanisms of action of new antiepileptic drugs: Rational design and serendipitous findings
159. Valproate reduces excitability by blockage of sodium and potassium conductance
160. Similar potency of carbamazepine, oxcarbazepine, and lamotrigine in inhibiting the release of glutamate and other neurotransmitters
161. Limitation by gabapentin of high frequency action potential firing by mouse central neurons in culture
162. Lamotrigine effects on ion channels in cultured neuronal cells
163. Inhibition of N-type calcium currents by lamotrigine in rat amygdalar neurones
164. Comparative anticonvulsant and mechanistic profile of established and newer antiepileptic drugs
165. The anticonvulsant topiramate displays a unique ability to potentiate GABA-evoked chloride currents
166. Felbamate modulates the strychnine-insensitive glycine receptor
167. Topiramate enhances GABA-mediated chloride flux and GABA-evoked chloride currents in murine brain neurons and increases seizure threshold
168. New antiepileptic drugs
169. Effects of anticonvulsant drugs on 4-aminopyridine-induced seizures in mice
170. Modulation of high-voltage-activated calcium channels in dentate granule cells by topiramate
171. Effects induced by the antiepileptic drug valproic acid upon the ionic currents recorded in rat neocortical neurons in cell culture
172. Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture
173. Effects induced by the anticonvulsant drug topiramate on voltage-gated sodium currents generated by cerebellar granule cells in tissue culture
174. Topiramate attenuates voltage-gated sodium currents in rat cerebellar granule cells