Term
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Definition
Generalized tonic clonic seizures |
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Term
Phenobarbital-- mechanisms of action |
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Definition
1. **binds to GABA (A) receptors and prolongs amount of time chloride can flow into neuron (hyperpolarization)
2. decrease release of excitatory NT (glutamate)
3. decrease calcium channel activity |
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Term
Phenobarbital--kinetics issues |
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Definition
Best documented liver enxymes inducer; leads to drug-drug interactions
Causes decreased levels of other drugs that are metabolized by the liver enzymes |
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Term
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Definition
Metabolized into phenobarbital and PEMA (both act as anti-convulsants) |
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Term
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Definition
1. ** decrease sodium permability across neuron membrane |
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Term
Phenytoin- side effects at therapeutic doses |
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Definition
gingival hyperplasia
hypertrichosis
thickened facial features
folate deficiency
peripheral neuropathy |
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Term
Phenytoin- dose-dependent SE |
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Definition
20 mg/L--> nystagmus
30mg/L--> nystagmus, ataxia
40mg/L--> ataxia, lethargy and decreased cognitive function |
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Term
Phenytoin-- kinetics issues |
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Definition
exhibits MM (linear) kinetics--> small dose can result in large increase in plasma levels
IV incompatabilities. |
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Term
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Definition
GTCS
partial epilepsy
trigeminal neuralgia
bipolar disease |
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Term
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Definition
Enhances voltage gated sodium channel inactiavtion (increased recovery time after AP) |
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Term
Carbamazepine-- kinetics issues |
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Definition
autoinduction--> starts enhancing its own metabolism in the liver; takes 3-4 weeks to stabalize.
Levels should be monitored for the first ~28 days, followed by a dose adjustment
10, 11 epoxide metabolite (active and can be increased by valproate) |
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Term
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Definition
Keto-analog of CBZ
Less side effects but less potent
Approved for monotherapy for newly diagnosed patients and refractory partial epilepsy |
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Term
Carbamazepine-- adverse effects |
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Definition
GI
vision effects (diplopia)
hematologic effects (leukopenia--> usually transient; drug should be stopped is under 2500.)
thrombocytopenia
rash |
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Term
Valproate (Divalproex)-- MOA |
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Definition
1.Inhibits GABA metabolism (GABA transaminase and sicinic semialdehyde DH)
2.prevents GABA reuptake
3.stimulates GABA synthetic enzymes (from glutamate)
4. enhances sodium channel inactiavation (prolonged recorvery after AP)
5. Some effect on T-type calcium channels |
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Term
Valproate (Divalproex)-- uses |
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Definition
Most major seizure types (including absence) |
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Term
Valproate-- adverse effects |
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Definition
GI--common
alopecia (usually temp)
weight gain
hepatotoxicity (particularly of concern in patient under 2 yo on multi drugs)
metabolic effects
thrombocytopenia (increased ammonia, glucose, urea) |
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Term
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Definition
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Term
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Definition
Blocks T-type calcium channels in thalamic neurons |
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Term
Benzodiazapines-- individual agents and indications |
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Definition
Diazepam (status and alcohol withdrawal)
Lorazepam (status and alcohol withdrawal)
Clonazepam (akinetic seizures, myoclonic seizures, lennox-gastaut) |
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Term
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Definition
Binds GABA receptors and increases frequency of chloride channel openings |
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Term
Benzodiazapines-- adverse effects |
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Definition
abuse potential
tolerance (longterm use)
relatively safe unless combined with ethanol |
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Term
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Definition
adjunct for complex partial
Lennox-Gastaut (MR and mutliple seizure types) |
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Term
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Definition
antagonist of NMDA receptor (glutamate receptor) |
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Term
Falbamate-- adverse effects |
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Definition
**aplastic enemia and deadly hepatotoxicity
Rarely used; never first-line |
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Term
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Definition
complex partial seizures
monotherapy for refractory partial seizures |
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Term
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Definition
inhibits sustained repetitive sodium channel firing |
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Term
Lamotrigine-- adverse effects |
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Definition
rashes (Steven-Johnson), N and V, dizziness, diplopia, ataxia |
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Term
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Definition
adjunct in complex partial |
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Term
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Definition
binds to alpha2delta subunit of calcium channels and decreases calcium influx (decreases release of several NT)
inhibits Na currents
stimulates GABA release
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Term
Gabapentin-- adverse effects |
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Definition
it is eliminated by kidneys and water soluble, so not many drug interactions
reduced absorption with antacids |
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Term
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Definition
adjunct for complex partial |
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Term
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Definition
binds alpha2delta subunit of calcium channel and decreases calcium influx (decreases release of several NT) |
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Term
Pregabalin-- adverse effects |
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Definition
eliminated by kidneys and water soluble, not many drug interactions
blurred vision, peripheral edema, dry mout, weight gain |
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Term
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Definition
complex partial, GTCS, Lennox-Gastaut |
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Term
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Definition
inhibits sodium channels
enhances GABA
attenuates kainate-induced seizures
AMPA antag? |
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Term
Topiramate-- adverse effects |
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Definition
kidney stones, ataxia, GI, tremors |
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Term
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Definition
adjunct for complex partial |
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Term
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Definition
inhibition of GABA reuptake |
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Term
Tiagabine-adverse effects |
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Definition
nervousness, tremor
spike-wave stupor--> do not use off-label |
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Term
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Definition
adjunct for complex partial |
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Term
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Definition
binds selectively to SV2A
(which may be modifying synaptic release of glutamate and GABA) |
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Term
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Definition
adjunct complex partial epilepsy |
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Term
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Definition
poorly understood; inhibits voltage gated sodium currents adn T-type calcium channels (in vitro)
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Term
Zonisamide-- adverse effects |
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Definition
kidney stones, rash, ataxia |
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Term
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Definition
infantile spasms
refractory epilepsy (last line) |
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Term
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Definition
GABA transaminase inhibitor
inhibition of GABA reuptake |
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Term
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Definition
blindness (30%)-- only used because one of few things that can treat infantile spasms |
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Term
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Definition
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Term
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Definition
enhances slow actiavtion of sodium channels
100% bioavailable |
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Term
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Definition
no significant drug interaction
PR-interval prolongation (caution when using with other drugs causing prolonged PR or people with cardiac disease) |
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Term
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Definition
adjunct for Lennox-Gastautover 4yo |
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Term
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Definition
prolonged inactiavtion of sodium channels |
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Term
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Definition
shortened QT interval, hypersensetivity (rash)
(caution when using other drugs that shorten QT interval like digoxin and lamotrigine)
EUPHORIA-- Schedule V controlled substnace |
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Term
teratogenic effects of anticonvulsants |
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Definition
fetal anticonvulsant syndrome
neural tube defects (cleft lip, cleft palte, spinal cord like myelomeningocele)
poor cognitive outcome (especially Valproate) |
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Term
common cause of cleft lip and cleft palate |
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Definition
phenytoin and phenobarbital |
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Term
common cause of spinal column defects |
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Definition
carbamazepine and valproate |
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Term
fetal anticonvlsant syndrome |
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Definition
thin upper lip
small, upturned nose
long, flat nasal bridge
mild to moderate MR
ptosis
occular hypertelorism
long philtrum
hypoplasia of distal phalanges
small nails
Might be caused by folate deficiency or interruption of hyaluronic acid metabolism |
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Term
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Definition
valproate, phenytoin and phenobarbital |
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Term
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Definition
-caused by various anticonvulsants like lamotrigine, carbemazepine, barbiruates, phenytoin, ethosuxamide
-severe febrile hypersensitivity reaction
-array of macules, papules, vesicles, and cytotoxicty
-remove causative agent and admin IV steroids and antibiotics |
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Term
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Definition
- SE of ethosuxamide, phenytoin and phenobarbital and other anticonvulsants
-under 20,000 platelets
-echymoses, petechial hemorrhages in skin and MM
-might be due to drug-induced folate deficiency |
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Term
major side effects of anticonvulsants |
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Definition
-teratogenic effects
-steven-johnson syndrome
-thrombocytopenia
-hepatic failure
-aplastic anemia and bone marrow suppression
-lupus-like sydrome |
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Term
less severe side effects of anti-convulsants |
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Definition
-rashes (urticaria, 'fixed drug eruption,' etc)
-gingival hyperplasia (phenytoin)
-angioedema
-cystic acne (phenytoin)
-hirsutism (phenytoin)
-thickened facial features (phenytoin)
-alopecia (valproate) |
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Term
Lennox-Gastaut treatments |
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Definition
rufinamide
topiramate
felbemate
clonazepam |
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