Pharmacology antiseizure chapter 24

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  • Phenytoin function Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Reduces low-threshold Ca2+ currents
  • Phenobarbital function Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate, Reduces low-threshold Ca2+ currents
  • Ethosuximide function Reduces low-threshold Ca2+ currents, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate
  • Primidone function Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Reduces low-threshold Ca2+ currents, Potentiates GABA(a) responses
  • Carbamazepine function Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Reduces low-threshold Ca2+ currents
  • Diazepam function Potentiates GABA(a) responses, Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Reduces low-threshold Ca2+ currents
  • Clonazepam function Potentiates GABA(a) responses, Reduces low-threshold Ca2+ currents, Enhances phasic GABA receptor responses and reduces excitatory synaptic responses, Block high-frequency firing of neurons through action on voltage gated Na+ channels and decrease synaptic release of glutamate
  • Gabapentin function Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Irreversibly inhibits GABA-transaminase, Blocks high firing of neurons and modifies amino acid metabolism, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Action on synaptic protein Sv2A, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Pregabalin function Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Irreversibly inhibits GABA-transaminase, Blocks high firing of neurons and modifies amino acid metabolism, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Action on synaptic protein Sv2A, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Vigabatrin function Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Blocks high firing of neurons and modifies amino acid metabolism, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Action on synaptic protein Sv2A, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Valproate function Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Action on synaptic protein Sv2A, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Lamotrigine function Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Action on synaptic protein Sv2A, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Levetiracetam function Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Enhance K+ channels opening, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Retigabine function Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Prolongs inactivation of voltage gated Na+ channels, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Rufinamide function Prolongs inactivation of voltage gated Na+ channels, Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Blocks GABA re-uptake in forebrain, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Tiagabine function Blocks GABA re-uptake in forebrain, Prolongs inactivation of voltage gated Na+ channels, Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Topiramate function Multiple actions on synaptic function, Blocks GABA re-uptake in forebrain, Prolongs inactivation of voltage gated Na+ channels, Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Zonisamide function Blocks high-frequency firing via action on voltage-gated Na+ channels, Blocks GABA re-uptake in forebrain, Prolongs inactivation of voltage gated Na+ channels, Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically, Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins
  • Lacosamide function Enhances slow inactivation of of Na+ channels and blocks effect of neurotrophins, Blocks high-frequency firing via action on voltage-gated Na+ channels, Blocks GABA re-uptake in forebrain, Prolongs inactivation of voltage gated Na+ channels, Enhance K+ channels opening, Action on synaptic protein Sv2A, Prolongs inactivation of voltage gated Na+ channels and decrease presynaptic glutamate release, Blocks high firing of neurons and modifies amino acid metabolism, Irreversibly inhibits GABA-transaminase, Decreases excitatory transmission by acting on voltage-gated Ca2+ channels presynaptically

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