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.
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)
Classification (with examples)
-
Barbiturates
- Enhance GABAergic activity at GABA-A receptors.
- Also inhibit voltage-gated calcium channels at higher concentrations.
- Examples:
- Phenobarbitone
- Metharbital
-
Hydantoins
- Block voltage-gated Na⁺ channels, stabilizing neuronal membranes.
- Examples:
- Phenytoin
- Mephenytoin
- Ethotoin
-
Oxazolidine Diones
- Suppress T-type Ca²⁺ currents in thalamic neurons.
- Primarily used in absence seizures.
- Examples:
- Trimethadione
- Paramethadione
-
Succinimides
- Selectively block T-type calcium channels in thalamic neurons.
- Effective for absence (petit mal) seizures.
- Examples:
- Phensuximide
- Methsuximide
- Ethosuximide
-
Ureas and Monoacylureas
- Block sodium channels, reduce repetitive neuronal firing.
- Examples:
- Phenacemide
- Carbamazepine
-
Benzodiazepines
- Potentiate the action of GABA at GABA-A receptors, increasing chloride influx and neuronal inhibition.
- Example:
- Clonazepam
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 |
Thank you for reading from Firsthope's notes, don't forget to check YouTube videos!