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Drug | Target Receptor | Mechanism of Action |
Phenytoin | Inhibits Na+ channels | Modifies neuronal excitability; for Partial seizures Many drug and OC interactions, induces hepatic enzymes Adverse: gingival hyperplasia, hirsutism, interfere w/ thyroid tests |
Carbamazepine | Inhibits Na+ channels | Decreases synaptic transmission; Partial seizures Many drug and OC interactions, induces own hepatic enzymes Adverse: epoxide int., liver damage, leukopenia, LFTs required |
Oxcarbazepine | Inhibits Na+ & Ca++ channels Enhances K+ currents | Metabolite is active form Adverse: hyponatremia, less hepatic enzyme induction |
Phenobarbitol (barbiturate) | GABAa, inhibits Ca channels | Enhance inhibition, GABA binding, Partial and Tonic-clonic Adverse: accumulation, addiction, cross tolerance, induces CYP450, drug and OC interactions |
Primidone (barbiturate) | Inhibits Na+ channels | Metabolized to phenobarbitol and PEMA; Partial and Tonic-clonic Adverse: sedation/intoxication immediately after administration, induces CYP450, drug and OC interactions |
Gabapentin | Unknown | Amino acid analog of GABA; wide usage, no interactions Partial seizure adjunct therapy |
Tiagabine | GABA (GAT-1) uptake inhibitor | availability of GABA, inhibition Partial seizure adjunct therapy |
Zonisamide | Inhibits Na & Ca (T type) channels | Sulfonamide derivative, Partial seizure adjunct therapy Adverse: allergies, renal calculi, teratogen, few interactions |
Levetiracetam | Inhibits K+ rectifier channel, inhibits Ca (N type) channel | Inhibits negative modulation of GABAa by Zn++ and b-carboline, no interactions discovered yet, Partial seizure adjunct therapy |
Felbamate | Inhibits NMDA receptors | GABA transmission, glutamate excitation, Refractory cases Adverse: affects CYP450 to lesser degree, aplastic anemia, liver failure, LFTs required |
Vigabatrin | Inhibits GABA transaminase degradation enzyme | Not approved in US. GABA availability, Refractory cases Adverse: irreversible visual field deficits |
Ethosuximide | Inhibits Ca (T type) channels | Absense seizures, few interactions Adverse: skin reactions, blood dyscrasias |
Valproic acid/ Sodium Valproate | Inhibits Na & Ca (T type) channels & GABA-T | GABA synthesis, membrane hyperpolarization, Broad Spectrum Adverse: hepatotoxicity in children, pancreatitis, LFTs required, inhibits CYP450 |
Lamotrigine | Inhibits Na+ channels, inhibits glutamate release | For Lennox-Gastaut syndrome in children, Broad Spectrum Adverse: Stevens-Johnson syn, few drug and OC interactions |
Topiramate | Inhibits Na channels, AMPA/KA antagonist | GABA transmission, glutamate excitability, Broad Spectrum Adverse: myopia, oligohydrosis, metabolic acidosis, weight loss, affects CYP450 to lesser degree |
Category: Pharmacology Notes
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