Anticonvulsants

Definition of Anticonvulsants

  • Anticonvulsants (also called antiepileptic drugs or AEDs) are agents used to prevent or reduce the frequency and severity of seizures in epilepsy and other seizure disorders.
  • They work by modulating the activity of excitatory and inhibitory neurotransmitters or ion channels in the brain.

Anticonvulsants

Mechanism of Action of Anticonvulsants

  • Anticonvulsants work mainly by:
  • Modulating voltage-gated sodium channels (e.g., Phenytoin, Carbamazepine)
  • Enhancing GABAergic inhibition (e.g., Benzodiazepines, Barbiturates)
  • Inhibiting T-type calcium channels (e.g., Ethosuximide)
  • Inhibiting glutamate receptors or release (e.g., Felbamate)
  • Altering synaptic transmission via GABA or voltage-gated channels (e.g., Valproic acid)
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Classification (with examples)

Classification of Anticonvulsants

  1. Barbiturates

    • Enhance GABAergic activity at GABA-A receptors.
    • Also inhibit voltage-gated calcium channels at higher concentrations.
    • Examples:
      • Phenobarbitone
      • Metharbital
  2. Hydantoins

    • Block voltage-gated Na channels, stabilizing neuronal membranes.
    • Examples:
      • Phenytoin
      • Mephenytoin
      • Ethotoin
  3. Oxazolidine Diones

    • Suppress T-type Ca² currents in thalamic neurons.
    • Primarily used in absence seizures.
    • Examples:
      • Trimethadione
      • Paramethadione
  4. Succinimides

    • Selectively block T-type calcium channels in thalamic neurons.
    • Effective for absence (petit mal) seizures.
    • Examples:
      • Phensuximide
      • Methsuximide
      • Ethosuximide
  5. Ureas and Monoacylureas

    • Block sodium channels, reduce repetitive neuronal firing.
    • Examples:
      • Phenacemide
      • Carbamazepine
  6. Benzodiazepines

    • Potentiate the action of GABA at GABA-A receptors, increasing chloride influx and neuronal inhibition.
    • Example:
      • Clonazepam
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Classification of Anticonvulsants

Class Mechanism Examples Uses Common Side Effects
1. Barbiturates Enhance GABA-A activity; at high doses, inhibit Ca²⁺ channels Phenobarbitone, Metharbital Generalized tonic-clonic & partial seizures Sedation, respiratory depression, dependence
2. Hydantoins Block voltage-gated Na⁺ channels Phenytoin, Mephenytoin, Ethotoin Generalized tonic-clonic & partial seizures Gingival hyperplasia, ataxia, hirsutism
3. Oxazolidine Diones Suppress T-type Ca²⁺ currents in thalamus Trimethadione, Paramethadione Absence seizures Visual disturbances, sedation, teratogenicity
4. Succinimides Block T-type calcium channels in thalamic neurons Ethosuximide, Phensuximide, Methsuximide Absence seizures (petit mal) GI upset, lethargy, headache
5. Ureas & Monoacylureas Block Na⁺ channels; stabilize membranes Carbamazepine, Phenacemide Partial & generalized tonic-clonic seizures Dizziness, rash, hyponatremia, aplastic anemia
6. Benzodiazepines Potentiate GABA-A activity; increase Cl⁻ influx Clonazepam Absence, myoclonic seizures, status epilepticus Sedation, tolerance, withdrawal, dependence

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