Nav spike-suppressor blocker
Spike-suppressing voltage-gated sodium channel blocker
- Use-dependent block of the fast transient Na⁺ current: the faster the firing, the more block
- Suppresses seizure discharges and neuropathic pain signaling
- Spares normally firing neurons
- Dizziness, diplopia, ataxia (dose-related)
Drugs with this mechanism (21)
- Carbamazepine — Anticonvulsant/mood stabilizer and potent autoinducer; HLA-B*1502 rash risk.
- Carbamazepine-10,11-epoxide — Active epoxide metabolite of carbamazepine; cleared by epoxide hydrolase, which valproate inhibits.
- Carbamazepine ER capsules — Bead-filled extended-release carbamazepine capsule; can be opened and sprinkled.
- Carbamazepine ER (Equetro) — Carbamazepine ER capsule - the only carbamazepine approved for acute bipolar mania.
- Eslicarbazepine — Once-daily sodium-channel anticonvulsant related to oxcarbazepine.
- Lamotrigine XR — Extended-release lamotrigine for seizures; slow titration reduces serious-rash risk.
- Lamotrigine — Well-tolerated mood stabilizer for bipolar depression; slow titration for rash risk.
- Phenobarbital — Oldest barbiturate anticonvulsant; sedating, enzyme-inducing, largely historical.
- Phenytoin — Classic sodium-channel anticonvulsant with nonlinear kinetics and many interactions.
- Topiramate ER (sprinkle) — Sprinkle-capsule extended-release topiramate for epilepsy and migraine prevention.
- Rufinamide — Sodium-channel anticonvulsant for Lennox-Gastaut drop attacks; uniquely shortens QT.
- Safinamide — Reversible MAO-B inhibitor; levodopa adjunct for wearing-off; can worsen dyskinesia.
- Carbamazepine XR — Extended-release carbamazepine for seizures and trigeminal neuralgia; potent enzyme inducer.
- Topiramate — Weight-reducing anticonvulsant for seizures and migraine; cognitive slowing limits it.
- Topiramate ER — Extended-release topiramate for seizures; cognitive slowing, kidney stones and fetal oral clefts.
- Valproic acid — Broad-spectrum anticonvulsant and mood stabilizer; highly teratogenic and metabolically burdensome.
- Divalproex DR — Delayed-release broad-spectrum antiseizure drug and mood stabilizer; highly teratogenic.
- Divalproex ER — Extended-release broad-spectrum antiseizure drug and mood stabilizer; highly teratogenic.
- Valproate sodium IV — Intravenous valproate for seizures when oral therapy is unavailable; broad-spectrum but highly teratogenic.
- Divalproex sprinkle — Valproate sprinkle capsule for seizures; useful when intact tablets cannot be swallowed.
- Zonisamide — Broad anticonvulsant associated with weight loss.
Self-check
- How does firing frequency affect use-dependent sodium blockade?
Faster firing produces more block. - Which dose-related neurologic effects accompany spike-current blockade?
Dizziness, diplopia and ataxia.
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