Table 1.
AED | Dosage in human63 | Reported doses and mechanisms in vitro | Tested doses |
---|---|---|---|
Carbamazepine | 200–1200 mg/daya | Inhibits VGSCs with an IC50 of ~30μM23 | 1, 5, and 50 μM |
Phenytoin | 300–600 mg/dayb | Inhibits VGSCs with an IC50 of ~30 μM23 | 5 and 50 μM |
Valproate | 10–60 mg/kg/day | Inhibits Na+ conductance and changes other parameters of Na+ currents at a concentration of 1 mM24 | 1 mM |
Lamotrigine | 25–375 mg/kg/daya | Inhibits human VGSCs with an IC50 of 56 μM26 | 60 μM |
Zonisamide | 100–400 mg/dayb | Enhances steady-state fast inactivation of Na+ current with a dissociation constant of 12 μM and reduces T-type Ca2+ currents by 38% at 50 μM27,64 | 50 μM |
Felbamate | 1200–3600 mg/dayc | Inhibits neuronal firing in striatal neurons with an IC50 of 28 μM and reduces NMDA-mediated currents by 29% at 100 μM65 | 100 μM |
Gabapentin | 900–3600 mg/daya | Inhibits VGCC-mediated currents with an IC50 of 167 nM and a saturated dose of 25 μM in DRG neurons66 | 50 μM |
Levetiracetam | 1000–3000 mg/dayd | Inhibits VGCC-mediated currents with an IC50 of 14.7 μM in hippocampal neurons67 | 100 μM |
Ethosuximide | 20 mg/kg/daye | Inhibits T-type VGCC-mediated currents with an IC50 of 500 μM68 | 500 μM |
Tiagabine | 4–32 mg/daya | Prolongs the duration of IPSPs and inhibits epileptiform bursting at a concentration of 25 μM69 | 30 μM |
Vigabatrin | 0.5–3 g/dayb | Increased cellular GABA concentrations in slices and tonic GABA currents in cultured neurons at a concentration of 100 μM70,71 | 200 μM |
aDoses for adults and children over 12 years of age.
bDoses for adults.
cDoses for adults and children over 14 years of age.
dDoses for adults and children over 16 years of age.
eThe optical dose for pediatric patients.