17.7 : 抗てんかん薬：SV2A タンパク質を介した神経伝達物質放出の調節剤

Antiepileptic drugs, like levetiracetam and brivaracetam, leverage the synaptic vesicle protein SV2A to mitigate seizures.

SV2A is a transmembrane glycoprotein primarily located in the brain and plays a key role in modulating neurotransmitter release.

These drugs exhibit a high affinity to the SV2A protein and inhibit neuronal voltage-gated sodium channels. Binding to SV2A modulates the release of neurotransmitters like glutamate and GABA, impacting neuronal excitability.

This control over neurotransmitter release reduces neuronal hyperexcitability and suppresses seizures.

Levetiracetam is approved for myoclonic, focal-onset, and generalized tonic-clonic seizures, while brivaracetam is indicated solely for focal-onset seizures.

These drugs exhibit good oral bioavailability and are not extensively metabolized. The half-life of these drugs is approximately 6-8 hours, indicating efficient pharmacokinetics.

These drugs are generally well tolerated but can cause side effects such as drowsiness, ataxia, dizziness, behavioral changes, and GI disturbances.