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48 Cards in this Set
- Front
- Back
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Phenytoin indications
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- generalized tonic-clonic
- focal seizures - post trauma/ neurosurgery prevention - 2nd line for status epilepticus |
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Phenytoin mechanism of action
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Blocks sodium channels- limits sustained firing
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Phenytoin PK
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- slow/variable absorption
- >90% protein bound - hepatic metabolism --> major substrate and inducer * non-linear PK: capacity limited, increase in dose doesn't always mean increase in conc. --> saturation effect |
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Phenytoin adverse effects
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- dizziness
- ataxia - dyskinesia - mood changes - Steven Johnson Syndrome - hyperglycemia - N/V - gum hyperplasia - SLE-like syndrome - folic acid depletion- monitor folate * facial coarsening * extravasation |
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Valproic acid indications
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- DOC for idiopathic generalized epilepsy
- absence - tonic-clonic - complex focal - juvenile myoclonic epilepsy - Lennox- Gaustaut |
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Valproic acid mechanism of action/ PK
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MOA: GABA potentiation, small effect on Na channels
PK: - 100% bioavailable - > 80% protein bound- dose dependent - hepatic metabolism |
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Valproic acid adverse effects
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- somnolence
- tremor - weight gain - N/V/D - pancreatitis - thrombocytopenia * liver failure - monitor LFTs |
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Phenobarbital indications
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Broad spectrum:
- generalized tonic-clonic - focal - 3rd line status epilepticus |
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Phenobarbital mechanism of action/ PK
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MOA: decreases excitation by increasing GABA
PK: - 95-100% bioavailable - 50% protein bound - hepatic metabolism |
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Phenobarbital adverse effects
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- bradycardia
- hypotension - somnolence - cognitive impairment - rash - apnea --> monitor hepatic and renal function, CBC, folate, mental status |
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Clonazepam indications
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- absence
- myoclonic - Lennox Gaustaut |
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Clonazepam MOA/PK
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MOA: increases GABA
PK: - 80-90% bioavailable - 80-90% protein bound - hepatic metabolism |
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Clonazepam adverse effects
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- hypotension
- drowsiness - memory impairment - ataxia - behavior changes - respiratory depression - dependence |
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Ethosuximide indications
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narrow spectrum:
- absence seizures |
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Ethosuximide MOA/PK
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MOA: thought to block calcium channels
PK: - 90-95% bioavailable - not protein bound - hepatic metabolism |
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Ethosuximide adverse effects
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- drowsiness
- ataxia - dizziness - Steven Johnson Syndrome - tongue swelling - N/V/D - gingivitis - blood dyscrasia |
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Carbamazepine indications
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Broad spectrum:
- generalized tonic-clonic - focal |
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Carbamezapine MOA/PK
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MOA: sodium channel blocker
PK: - erratic and slow absorption - 75-85% bioavailable - 75-90% protein bound - hepatic metabolism- CYP3A4 to active metabolite |
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Carbamezapine adverse effects
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- sedation
- dizziness - ataxia - Steven Johnson Syndrome - syndrome of inappropriate antidiuretic hormone - hyponatremia - nausea - blood dyscrasia - aplastic anemia - diplopia |
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Felbamate indications
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Not 1st line agent
- adjunctive and monotherapy for focal - adjunctive for Lennox Gaustaut |
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Felbamate MOA/PK
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MOA: unknown but though to be GABA potentiation
PK: - rapid/complete absorption - 25% protein bound - hepatic metabolism |
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Felbamate adverse effects
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- somnolence
- insomnia - gait abnormalities - anorexia - N/V - weight loss - Black box warning: aplastic anemia, liver failure --> last line |
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Gabapentin indications
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adjunctive treatment for complex focal
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Gabapentin MOA/PK
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MOA: unknown, thought to be related to calcium channel blockade
PK: - variable absorption - 30-60% bioavailable --> effected by food - not protein bound - no hepatic metabolism - excreted in urine/feces |
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Gabapentin adverse effects
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- somnolence
- ataxia - fatigue - behavior changes --> dose limiting - weight gain - nystagmus - diplopia ---> may exacerbate absence and myoclonic seizures |
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Lamotrigine indications
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Broad spectrum:
- focal - generalized - Lennox Gaustaut - absence |
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Lamotrigine MOA/PK
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MOA: sodium channel blocker
PK: - 98% bioavailable - >75% metabolized in liver via glucoronidation (phase 2)--> excreted as glucoronide conjugates in urine |
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Lamotrigine adverse effects
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- somnolence
- dizziness - ataxia * Steven Johnson Syndrome * toxic epidermal necrolysis - blurred vision - diplopia |
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Lamotrigine interactions
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- valproic acid: decreases clearance and half life of lamotrigine
- oral contraceptives: decrease concentration |
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Topiramate indications
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- focal
- generalized - adjunctive for Lennox Gaustaut |
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Topiramate MOA/PK
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MOA: unknown, thought to be GABA/Na/Ca blocker
PK: - rapid absorption - 15-41% protein bound - not extensive liver metabolism - 70% excreted unchanged in urine |
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Topiramate adverse effects
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- somnolence
- fatigue - dizziness - attention difficulties - aggression - weight loss * metabolic acidosis - anorexia - hyperthermia --> caution in pts. w/ existing behavior/learning issues |
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Tiagabine indications
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- focal
- generalized tonic-clonic --> best used as a second line adjunctive for refractory seizures |
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Tiagabine MOA/PK
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MOA: potentiates GABA
PK: - rapid and complete absorption - 89% bioavailable - 96% protein bound - extensive liver metabolism - phase 1&2 -- major substrate of CYP 3A4 - renal/fecal excretion |
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Tiagabine adverse effects
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- somnolence
- fatigue - asthenia - dizziness - nervousness - tremors |
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Levetriacetem (Keppra) indication
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- adjunctive for focal
- myoclonic - generalized |
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Levetriacetem MOA/PK
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MOA: unknown, may be GABA potentiation
PK: - 60% bioavailable - 40% protein bound - doesn't undergo extensive hepatic metabolism - renal excretion --> adjust dose in renal failure |
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Levetriacetem adverse effects
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- somnolence
- hostility - nervousness - asthenia - hyperactivity - aggression |
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Oxcarbazepine indication
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- focal
- generalized tonic-clonic - most common= adjunctive for focal |
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Oxcarbazepine MOA/PK
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MOA: unknown, may be Na/Ca/K channel blocker
PK: - >95% bioavailable - 67% protein bound - extensive metabolism in the liver - >95% excreted in urine |
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Oxcarbazepine adverse effects
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- headache
- ataxia - somnolence - dizziness - fatigue - hyponatremia - N/V - diplopia |
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Zonisamide indications
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broad spectrum:
- focal - generalized tonic-clonic - absence - myoclonic |
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Zonisamide MOA/PK
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MOA: unknown, may be sodium and calcium channel blocker
PK: - 85% bioavailable - 40% protein bound - metabolized and conjugated in the liver- major CYP3A4 substrate - 62% excreted in urine |
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Zonisamide adverse effects
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- somnolence
- fatigue - ataxia - decreased activity - dizziness - cognitive impairment - rash - anorexia - hyperthermia |
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Vigabatrin indications
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treatment of infantile spasms
- best for tx those assoc. w/ tuberous sclerosis |
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Vigabatrin MOA/PK
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MOA: inhibits GABA
PK: - complete absorption - induces CYP2C9 - renal elimination |
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Vigabatrin interactions
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- carbamezapine: increase effects
- phenytoin: decreases plasma levels |
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Vigabatrin adverse effects
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- MRI abnormalities
- somnolence - headaches - fatigue - dizziness - irritability - sedations - weight gain black box warning: irreversible peripheral visual field defects |
