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50 Cards in this Set

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Whats the goal of anti-epileptic drugs?
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
What are themolecular targets of GLUTAMATE?
AMPA, NMDA, Voltage gated Na channel, Ca2+ channel, and K+ channel
What are the molecular targets of GABA?
GABA Transaminase

GABA A and B Receptors (A is primary target)
T/F: Most anti-epileptic drugs are orally effective
TRUE (80-100% into circulation)

Most do not highly bind plasma protein

predominantly distributed into total body water

Plasma clearance slow
T/F: The entire class of anti-epileptics is black boxed
TRUE
How are most Anti-epileptics cleared?
Hepatically
What drugs work for Partial seizures and general tonic-clonic seizures?
"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
What drug to do always choose for a seizure in which pt just stares ahead for a little bit where eyes may roll up?
This is an absence seizure = use Ethosuximide
Alternate drugs for seizures?
"Lora Clobbered (x3) Vagus Double Aces" = Lorezepam, Clonazepam, Clorasepate, Clobazam, Vagus n. Stim, Diazepam, Acetazolamide
MOA Phenytoin?
Alters Na+ = inactive state of Na+ channel - inhibits generation of repetitive APs (=dec. glutamate, inc., GABA)
Whats the more soluble form of Phenytoin given orally to be absorbed in GI tract?
Fosphenytoin
What metabolizes Phenytoin?
CYP2C9/2C19

And phenytoin induces 2C9/3A4
What are the three drugs that do zero order kinetics
Phenytoin, Aspirin, Alcohol
Pt presents with Hirsutism, Diplopia and Ataxia, Nyustagmus (and loss of smooth m. eye movement) and Gingival hyperplasia. What drug were they on?
Phentytoin

(Pneumonic for SE's = DANG = Diplopia (double vision), Ataxia, Nystagmus (eye movement), Gingival hyperplasia)
If infused too fast, what does phenytoin cause?
Hypotension and cardiac arrhythmias
All of the drugs for Seizures inhibit the Na receptor except which ones?
Inhibits GABA-T (GABA Aminotransferase) - Vigabatrin (vision loss)

Inhibit Ca2+ receptor = Bagapenrin, Pregabalin, Ethosuximide

Binds synaptic vessicle protein SV2A = Levetiracetam

Opens K+ Channel = Ezogabine
What is the ONLY way Carbamazepine can be given?
Orally
Carbamazepine toxicity?
Diplopia, ataxia, CNS depression, Blood Dyscrasias (leukopenia), Asians more likely to get Steven's Johnson
What are the Drugs that can cause Steven's Johnson?
Carbamazepine, Lamotrine, Tiagabine
Phenobarbital MOA?
Enhancement of inhibitory neurotransmission (binds GABA prolonging opening of Cl- channel)
MOA of Vigabatrin?
Irreversible inhibitor of GABA aminotransferase (GABA-T)
PT has vision loss, anemia, somnolence, and suicidal ideation. what drug are they on?
Vigabatrin
T/F: Via the SHARE program, only specific physicans and pharmacists can prescribe and distribute certain meds
TRUE
Lamotrigine - Adjunctive or Monotherapy?
Either...mostly Adjuctive
SE's Lamotrigine?
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)
MOA of Gabapentin and Pregabalin (and Ethosuximide)?
Block voltage-gated Ca2+ channels = modify release of GABA
Whats the MOA of Lacosamide?
Enhanced slow inactivation of Na+ Channel --> blocks actions of neurotropic factors of axonal and dendritic growth
Whats the BEST Use for Lacosamide?
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
MOA levetiracetam?
Binds to synaptic SV2A = may modify release of glutamate and GABA
SEs of Tigabine?
Steven's Johnson (=Carbamazepine, Lamotrine, Tiagabine) or toxic epidermal necrolysis

CNS depression, suicidal ideation
What are some things we can use Topiramate for other than seizures?
Lennox-Gustaut syndrome, West's syndrome, Absence seizures, migraine H
SE's Topiramate?
Urolithiasis = ONLY ONE that causes kidney stones

myopia, glaucoma, metabolic acidosis
What are the drugs that can cause Metabolic acidosis?
Zonisamide, Topiramate
MOA Felbamate?
Use-dependant block of NMDA receptors
SE's Felbamate?
Aplastic Anemia, Severe Hepatitis
SE's Rufinamide?
Short QT, V, Somnolence
MOA Ezogabine?
Opens K+ Channel (NOTE - ONLY ONE THAT DOES THIS!!!)

= suppressing epileptic activity
MOA Ethosuzimide, used for Absence Seizures?
Inhibits Ca2+ channels (others that do this too are Bagapenrin and Pregabalin)
What type of Seizure can Valproic Acid and Sodium Valproate treat?
Every
SE's for valproic acid and sodium valproate?
Hepatotoxicity, Pancreatitis, Inc. risk Spina Bifida in offspring of preggos taking it
What are the Benzodiazepines we talked about?
Diazepam and Lorazepam, Clonazepam, Clorazepate, and Clobazam
MOA of Acetazolamide?
Inhibits Carbonic Anhydraseq
What does Vagus nerve stimualation work best for?
Pts with refractory partial seizures

or when seizure meds are poorly tolerated
Define Vagus nerve stimulation
Wire into chest, wrapped around vagus n., regularly sends electrical pulses to vagus to try and prevent seizures.
Define Status Epilepticus
recurrent episodes of tonic-clonic seizures = remain unconscious without normal muscle movements between episodes

= requires IMMEDIATE CV, respiratory and metabolic management
Pt is seizing on floor of Wal-Mart - they're unconscious, don;t have movement between seizures. Tx?
1st = IV Diazepam or Lorazepam
2nd = IV Phenytoin, BUT More likely we'll use Fosphenytoin
3rd - IF no response to Fosphenytoin (phenytoin) try Phenobarbital
Women on what seizure meds need to use a non-hormonal BC?
Phenytoin, Phenobarbital, Carbamazepine, Topiramate, Oxcarbazepine, Felbamate
What Seizure meds are teratogenic?
Phenytoin, Valproate and Topiramate = don't use in preggos
A pt with epilepsy hasn't had a seizure for 3 years and wants to go off drugs. What do you tell them?
OK - Withdrawal can cause inc. frequency and severity of seizures

Benzodiazepines and Barbiturates are difficult to doscontinue - may take weeks to months
T/F: Generic anti-epileptic drugs are not as good as brand drugs
TRUE