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50 Cards in this Set
- Front
- Back
Whats the goal of anti-epileptic drugs?
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Suppress formation or spread of abnormal electrical discharges in brain
=inhibit Na or Ca influx responsible for neuronal depol Inc. inhibitory neurotransmission by GABA (=opne Cl- channels) Inhibit excitatory glutamate neurotransmision |
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What are themolecular targets of GLUTAMATE?
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AMPA, NMDA, Voltage gated Na channel, Ca2+ channel, and K+ channel
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What are the molecular targets of GABA?
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GABA Transaminase
GABA A and B Receptors (A is primary target) |
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T/F: Most anti-epileptic drugs are orally effective
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TRUE (80-100% into circulation)
Most do not highly bind plasma protein predominantly distributed into total body water Plasma clearance slow |
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T/F: The entire class of anti-epileptics is black boxed
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TRUE
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How are most Anti-epileptics cleared?
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Hepatically
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What drugs work for Partial seizures and general tonic-clonic seizures?
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"Find Cars Priced Very Low" = Pehnytoin, Carbamasepine, Primadone, Vigabatrin, Lamotrigine
"Find GABA Pre La Leve" = Phenobarbitol, Gabapentrin, Pregabalin, Lacosamide, Levetiracetam "Zoni Failed To Rufi Ezu Tia" = Zonisamide, Felbamate, Topiramate, Rufinamide, Ezogabine, Tiagabine |
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What drug to do always choose for a seizure in which pt just stares ahead for a little bit where eyes may roll up?
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This is an absence seizure = use Ethosuximide
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Alternate drugs for seizures?
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"Lora Clobbered (x3) Vagus Double Aces" = Lorezepam, Clonazepam, Clorasepate, Clobazam, Vagus n. Stim, Diazepam, Acetazolamide
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MOA Phenytoin?
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Alters Na+ = inactive state of Na+ channel - inhibits generation of repetitive APs (=dec. glutamate, inc., GABA)
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Whats the more soluble form of Phenytoin given orally to be absorbed in GI tract?
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Fosphenytoin
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What metabolizes Phenytoin?
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CYP2C9/2C19
And phenytoin induces 2C9/3A4 |
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What are the three drugs that do zero order kinetics
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Phenytoin, Aspirin, Alcohol
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Pt presents with Hirsutism, Diplopia and Ataxia, Nyustagmus (and loss of smooth m. eye movement) and Gingival hyperplasia. What drug were they on?
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Phentytoin
(Pneumonic for SE's = DANG = Diplopia (double vision), Ataxia, Nystagmus (eye movement), Gingival hyperplasia) |
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If infused too fast, what does phenytoin cause?
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Hypotension and cardiac arrhythmias
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All of the drugs for Seizures inhibit the Na receptor except which ones?
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Inhibits GABA-T (GABA Aminotransferase) - Vigabatrin (vision loss)
Inhibit Ca2+ receptor = Bagapenrin, Pregabalin, Ethosuximide Binds synaptic vessicle protein SV2A = Levetiracetam Opens K+ Channel = Ezogabine |
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What is the ONLY way Carbamazepine can be given?
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Orally
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Carbamazepine toxicity?
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Diplopia, ataxia, CNS depression, Blood Dyscrasias (leukopenia), Asians more likely to get Steven's Johnson
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What are the Drugs that can cause Steven's Johnson?
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Carbamazepine, Lamotrine, Tiagabine
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Phenobarbital MOA?
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Enhancement of inhibitory neurotransmission (binds GABA prolonging opening of Cl- channel)
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MOA of Vigabatrin?
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Irreversible inhibitor of GABA aminotransferase (GABA-T)
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PT has vision loss, anemia, somnolence, and suicidal ideation. what drug are they on?
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Vigabatrin
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T/F: Via the SHARE program, only specific physicans and pharmacists can prescribe and distribute certain meds
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TRUE
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Lamotrigine - Adjunctive or Monotherapy?
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Either...mostly Adjuctive
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SE's Lamotrigine?
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Skin rash, dizzy, H, Diplopia, N, somnolence
Life-threatening dermatitis in 1-2% of pediatric pts...ie Steven's Johnson or toxic epidermal necrosis (3 that cause Steven's Johnson = Carbamazepine, Lamotrine, Tiagabine) |
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MOA of Gabapentin and Pregabalin (and Ethosuximide)?
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Block voltage-gated Ca2+ channels = modify release of GABA
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Whats the MOA of Lacosamide?
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Enhanced slow inactivation of Na+ Channel --> blocks actions of neurotropic factors of axonal and dendritic growth
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Whats the BEST Use for Lacosamide?
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It doesn't have ANY effect on CYP450s and drug interactions are negligible so use in pts who are on a lot of other drugs
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MOA levetiracetam?
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Binds to synaptic SV2A = may modify release of glutamate and GABA
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SEs of Tigabine?
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Steven's Johnson (=Carbamazepine, Lamotrine, Tiagabine) or toxic epidermal necrolysis
CNS depression, suicidal ideation |
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What are some things we can use Topiramate for other than seizures?
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Lennox-Gustaut syndrome, West's syndrome, Absence seizures, migraine H
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SE's Topiramate?
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Urolithiasis = ONLY ONE that causes kidney stones
myopia, glaucoma, metabolic acidosis |
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What are the drugs that can cause Metabolic acidosis?
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Zonisamide, Topiramate
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MOA Felbamate?
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Use-dependant block of NMDA receptors
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SE's Felbamate?
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Aplastic Anemia, Severe Hepatitis
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SE's Rufinamide?
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Short QT, V, Somnolence
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MOA Ezogabine?
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Opens K+ Channel (NOTE - ONLY ONE THAT DOES THIS!!!)
= suppressing epileptic activity |
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MOA Ethosuzimide, used for Absence Seizures?
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Inhibits Ca2+ channels (others that do this too are Bagapenrin and Pregabalin)
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What type of Seizure can Valproic Acid and Sodium Valproate treat?
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Every
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SE's for valproic acid and sodium valproate?
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Hepatotoxicity, Pancreatitis, Inc. risk Spina Bifida in offspring of preggos taking it
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What are the Benzodiazepines we talked about?
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Diazepam and Lorazepam, Clonazepam, Clorazepate, and Clobazam
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MOA of Acetazolamide?
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Inhibits Carbonic Anhydraseq
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What does Vagus nerve stimualation work best for?
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Pts with refractory partial seizures
or when seizure meds are poorly tolerated |
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Define Vagus nerve stimulation
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Wire into chest, wrapped around vagus n., regularly sends electrical pulses to vagus to try and prevent seizures.
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Define Status Epilepticus
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recurrent episodes of tonic-clonic seizures = remain unconscious without normal muscle movements between episodes
= requires IMMEDIATE CV, respiratory and metabolic management |
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Pt is seizing on floor of Wal-Mart - they're unconscious, don;t have movement between seizures. Tx?
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1st = IV Diazepam or Lorazepam
2nd = IV Phenytoin, BUT More likely we'll use Fosphenytoin 3rd - IF no response to Fosphenytoin (phenytoin) try Phenobarbital |
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Women on what seizure meds need to use a non-hormonal BC?
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Phenytoin, Phenobarbital, Carbamazepine, Topiramate, Oxcarbazepine, Felbamate
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What Seizure meds are teratogenic?
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Phenytoin, Valproate and Topiramate = don't use in preggos
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A pt with epilepsy hasn't had a seizure for 3 years and wants to go off drugs. What do you tell them?
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OK - Withdrawal can cause inc. frequency and severity of seizures
Benzodiazepines and Barbiturates are difficult to doscontinue - may take weeks to months |
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T/F: Generic anti-epileptic drugs are not as good as brand drugs
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TRUE
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