Small molecule
PubChem CID 3878
Lamotrigine
Lamictal
- Mechanism of action
- Voltage-gated sodium channel blocker, anticonvulsant
- In plain language
- Blocks channels that overactive nerve cells use to fire rapid, repeated electrical signals, calming the brain activity that causes seizures; the same calming effect is thought to help even out mood swings in bipolar disorder, though exactly how isn't fully understood.
- How it works
- Lamotrigine (Lamictal) is an antiepileptic and mood-stabilizing agent whose precise mechanism of action is not fully established. Per the FDA label, in vitro pharmacological studies suggest lamotrigine inhibits voltage-sensitive sodium channels, stabilizing neuronal membranes and modulating presynaptic release of the excitatory neurotransmitters glutamate and aspartate. This sodium-channel effect is the proposed basis for its anticonvulsant activity, demonstrated across multiple animal seizure models, though the relevance of these models to human epilepsy and to its efficacy in bipolar disorder is not known.
- Therapeutic applications
- Lamotrigine is FDA-indicated as adjunctive therapy for partial-onset seizures, primary generalized tonic-clonic seizures, and the generalized seizures of Lennox-Gastaut syndrome in patients aged 2 years and older, and for conversion to monotherapy in adults with partial-onset seizures already being treated with a single other antiepileptic drug. It is also indicated for the maintenance treatment of bipolar I disorder, to delay the time to occurrence of mood episodes in patients already treated for an acute mood episode. It carries a boxed warning for serious, potentially life-threatening skin rashes, including Stevens-Johnson syndrome, with risk increased in pediatric patients and by coadministration with valproate or exceeding the recommended dose/escalation.
- Class
- Small molecule
- Therapeutic area
- CNS / Neurology
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