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11 Cards in this Set
- Front
- Back
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Phenytoin
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MOA: inhibits voltage gated Na+ channels
pharmokinetics: metabolized by cytochrome p450 90% bound, mostly to albumin T1/2= 24 hours Unique properties: nonlinear elimination--> disproportionate rise with small increase loaded IV Toxicity: acute- cerebellar/ vestibular: nausea, vomit, vertigo, ataxia, nystagmus, gait drowsiness cardiac arrhythmias, hypotension chronic: gingival hyperplasia hirsutism peripheral neuropathy osteomalacia- weak bones |
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Carbamazepine
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MOA: inhibit voltage gated Na+ channels
Pharmokinetics: 70% protein bound P450 metabolized Side Effects: drowsiness, vertigo Diplopia aplastic anemia SIADH- hyponatremia Drug of choice for trigeminal neuralgia bipolar disease |
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Phenobarbital
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MOA: increases GABA-A receptor mediated currents by increasing duration of the response
Pharmokinetics: metabolized by P450 T1/2 = 96 hours less effective for partial onset seizures Toxicity: sedation/ slowed mentation children- paradoxical hyperactivity acute: ataxia/ nystagmus |
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Primidone
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metabolized to phenobarbitol and Phenylethylmalonamide
used for essential tremor |
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Valproic acid (Depakote)
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MOA: prolonged recovery of voltage gated Na Channels- partial onset seizures
reduces low threshold Ca current- general onset seizures increases GABA in brain by inhibiting its degradation properties: highly protein bound displaces phenytoin from albumin pharmokinetics 90% protein bound T1/2 - 15 hours uses: manic depressive migraines Side effects: GI- vomit, nausea, anorexia sedation tremor stimulation of appetite fatal fulminate hepatitis acute pancreatitis/ hyperammonemia |
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Benzodiazepines
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MOA: enhancement of GABA mediated synaptic inhibition
Pharmokinetics: max conc at 1-4 hours Side Effects: sedation death due to respiratory depression Uses: status epilepticus abrupt stoppage = withdrawal seizures due to short half life lorazepam, diazepam |
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Gabapentin
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MOA: promote non-vesicular release of GABA
Pharmokinetics: excreted unchanged Side effects: sedation dizziness fatigue other uses: pain and paresthsias from peripheral neuropathy |
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Lamotrgine (lamictal)
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MOA: inhibit voltage gated Na channels, inhibit glutamate release
Pharmokinetics: metabolized by glucuronidatoin, VPA increase conc. 4 weeks to therapeutic range Side effects: rash (rare) use: partial and generalized onset seizure, safer in pregnancy |
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Topiramate (Topamax)
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MOA: inhibits voltage gated Na channels, enhances postsynaptic GABA currents and limits glutamate receptor
side effects: numbness, tingling around mouth and hands/ feet due to carbonic anhydrase inhibitor effects Other: lowers estradiol- important for birth control |
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Levitiracetam (Keppra)
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MOA: inhibit burst firing and hypersynchronization of epileptiform activity without affecting normal neuronal excitablitiy
Pharmokinetics: not extensively metabolized uses: partial and generalized onset quick onset Side Effects: irritability, somnolence, dizziness, headache |
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Ethosuximide
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MOA: inhibits voltaged gated Ca channels
uses: absence seizures |
