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Antiepileptic Flashcards

1
Q

Carbamezepine (Tegretol)

- First Line for focal seizures

A
  • MOA: block Na channels, inactivate action potential
  • USE: generalized tonic clonic seizures/mixed seizures, pain control in trigeminal neuralgia
  • NOT for absence or myoclonic seizures
  • COMMON ADR: Neurocognitive (Drowsiness, diplopia, HA, ataxia, dizziness); Rash; GI (N/V/D/C, abd pain); Leukopenia; HypoNa
  • SERIOUS ADR: Aplastic anemia; Hepatitis; Pancreatitis; SJS/TEN
  • PREG CAT D (risk of spina bifida)
  • CONTRAINDICATIONS: bone marrow depression (risk of agranulocytosis, aplastic anemia)/ MAOi
  • P450 3A4 metabolized (Crazy strong!!!)
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2
Q

Oxcarbazepine (Trileptal)

- First Line for focal seizures

A
  • MOA: MHD metabolite inhibits Na channel
  • Cross reactivity w/ carbamazepine rash
  • COMMON ADR: sedation; dizziness; diplopia; HA; nausea (rash, liver, bone marrow issues less common than w/ carbamazepine)
  • SERIOUS ADR: SJS/TEN; HypoNa; angioedema; anaphylaxis
  • P450 3A4
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3
Q

Lamotrigine (Lamictal)

  • First Line for adjunctive therapy >2yrs: focal seizures/ primary generalized seizures (tonic-clonic/ absence)/ generalized seizures of Lennox-Gastaut syndrome
  • Second Line for monotherapy adults (>16yrs) for focal seizures
  • Second Line for Bipolar Disorder for adults
A
  • MOA: blocks voltage-dependent Na channels at high firing frequencies/ enhances H current/ modulates kainate receptors
  • WARNINGS: SJS; DRESS; Suicidal ideation; aseptic meningitis; interactions with OCPs, valproate
  • COMMON ADR: CNS (HA, insomnia, drowsiness, dizziness, diplopia, ataxis); Rash; Nausea
  • SERIOUS ADR: SJS/TEN; Risk- Peds/ taking with valproate/ Rapid titration or high starting dose
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4
Q 
Valproic Acid (Depakote, Depakene, Stavzor)
- First Line for focal/generalized tonic- clonic/ mixed/ absence
A
  • MOA: enhanced GABA transmission (more GABA– more STOP)/ Na channel inhibition/ modulation of T-type Ca channel
  • USE: migraine prophylaxis; Bipolar disorder
  • COMMON ADR: N/V; fatigue/dizziness/tremor/weight gain; depression (adults)/irritability (kids); Hyperammonemia (50%); irregular periods; bone loss
  • SERIOUS ADR: Hepatotoxicity (peds); pancreatitis; thrombocytopenia
  • BOX WARNING: hepatotoxicity; teratogenicity; pancreatitis
  • CONTRAINDICATIONS: liver dz (fatal liver toxicity)
  • PREG known fatal defects (neural tube, spina bifida)
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5
Q

Levetiracetam (Keppra)
- First Line adjunct treatment (focal seizures > 4yrs/ myoclonic seizures >12 yrs/ primary generalized tonic-clonic seizures >6yrs)

A
  • MOA: binding of reversible saturable specific binding site SV2a/ modulate kainate receptor activity/ reverse inhibition of GABA and glycine gated currents induced by negative allosteric modulators
  • COMMON ADR: dizziness, somnolence, asthenia, irritability
  • SERIOUS ADR: anxiety, agitation
  • WARNINGS: suicidal behavior/ideation
  • RENAL adjust
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6
Q

Topiramate (Topamax)

- First Line focal/ generalized tonic-clonic/ Lennox-Gastaut syndroe

A
  • MOA: blocks Na channel/ increase GABA frequency (Cl channel)/ antagonize glutamate action at AMPA & kainate receptor/ inhibition of carbonic anhydrase
  • USE: Migraine prophylaxis/ Wt loss
  • OFF LABEL USE: Neuropathic pain, bipolar disorder
  • COMMON ADR: Somnolence; ataxia; speech problems/psychomotor slowing; vision change; memory/concentration problems; paresthesia; wt loss
  • SERIOUS ADR: bullous skin rx; hepatic problems (failure, hepatitis); eye problems (maculopathy, glaucoma); pancreatitis; nephrolithiasis; metabolic acidosis; neuropsych
  • WARNING: NEPHROLITHIASIS; acute myopia and secondary angle closure glaucoma; metabolic acidosis; suicidal ideation
  • DRUG INTERACTION: P450!/ poss decrease in OCP efficacy/ CNS depressants (additive)
  • PREG: cleft palate risk
  • RENAL adjust
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7
Q

Ethosuximide (Zarontin)

- First Line Absence seizures

A
  • MOA: blocks low threshold, “transient” (T-type) calcium channels in thalamic neurons
  • COMMON ADR: GI (N/V/D, abd problems); CNS (drowsiness, dizziness, HA, agitation); Pink-brown urine
  • SERIOUS ADR: blood dyscrasias; liver; kidney effects; SLE; rash; SJS; neuropsych
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8
Q

Phenytoin (Dilantin)

  • First Line generalized tonic-clonic/ focal
  • Not liked to be used anymore due to lots of drug interaction
A
  • MOA: slows recovery of Na channels
  • Nonlinear t1/2
  • DRUG INTERACTION (LOTS– lower levels of meds): AED; digoxin; OCP; warfarin
  • COMMON ADR: Sedation; impaired cognition; slurred speech; nystagmus; decreased coordination; confusion; dizziness; HA
  • SERIOUS ADR: Osteomalacia; lymphadenopathy; dermatitis (SJS/TEN/lupus)
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9
Q

Fosphenytoin (Cerebyx)

  • Short term use if phenytoin unavailable
  • For status epilepticus
A
  • Phenytoin prodrug

- IV only

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10
Q

Zonisamide (Zonegran)

  • 2nd line adjunct treatment of focal in ADULTS
  • NOT for monotherapy
A
  • MOA: blocks Na & Ca channels/ Mild carbonic anhydrase inhibitor
  • COMMON ADR: Somnolence; fatigue; anorexia; wt loss; dizziness; Neuro effects (confusion; abnormal thinking; ataxia; difficult memory and concentration)
  • SERIOUS ADR: nephrolithiasis; leukopenia; oligohidrosis; rash; depression; metabolic acidosis
  • CONTRAINDICATIONS: Sulfonamide allergy
  • WARNINGS: SJS; blood dyscrasias; oligohidrosis/hyperthermia in meds; metabolic acidosis; teratogenicity; kidney stones
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11
Q

Lacosamide (Vimpat)

  • 2nd line Adjunct treatment for adults with focal
  • limited efficacy for neuropathy, fibromyalgia
A
  • MOA: Enhances slow inactivation of Na channels
  • ADR: Diplopia; HA; dizziness; nausea
  • WARNINGS: dizziness/ataxia; Prolonged PR interval; afib/aflutter; syncope; DRESS
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12
Q

Perampanel (Fycompa)

- 2nd line focal in pts >12yrs/ generalized tonic-clonic

A
  • MOA: noncompetitive glutamate receptor antagonist
  • COMMON ADRs: anxiety/confusion/imbalance/diplopia/nausea/ wt gain; aggressive behavior/ paranonoia
  • P450 3A4 substrate
  • CIII
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13
Q

Barbiturates

- GABA drug

A 
Phenobarbital
Primidone (mysoline)
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14
Q

Phenobarbital

  • First Line alternative for status epilepticus
  • Strong anticonvulsant power
  • MANY ADRs
A
  • MOA: prolong GABA mediated Cl openings/ block kainate receptors
  • USE: short term SEDATIVE; generalized and focal seizures; Lennox-Gastaut syndrome
  • COMMON ADRs: CNS depressant (decreased cognition, somnolence, fatigue); depression/dizziness; decreased libido/ED; N/folate dificiency; Anemia; rash/fever; bone loss/hypocalcemia
  • Very potent anticonvulsant
  • Sedative-hypnotic
  • Broad spectrum of action
  • WARNINGS: addictive (CIV); hyperalgesia; pregnancy; peds; EtOH; respiratory depression
  • DRUG INTERACTIONS: Anticoagulants ; Corticosteroids; Griseogulvin; Doxycycline; other seizure meds; CNS DEPRESSANTS; MAOIs; hormones
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15
Q

Primidone (Mysoline)

- 2nd line generalized tonic clonic (may work for refractory)/ psychomotor/ focal seizures

A
  • MOA: not known/ Metabolized to phenobarbital in the liver (Prodrug of phenobarbital)
  • ADR: ataxia, vertigo, N/V, diplopia
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16
Q

Benzodiazepines (BDZs)

- GABA drug (increase Cl channel openings)

A 
Clonazepam (Klonopin)
Diazepam (Valium)
Lorazepam IV (Ativan)
Midazolam IV (Versed)
Clobazam (Onfi)
17
Q

Clonazepam (Klonopin)

A
  • Lennox Gastaut syndrome as monotherapy/ adjunct

- 2nd line absence

18
Q

Diazepam (Valium)

A
  • First Line status epilepticus

- prolonged or severe recurrent seizures

19
Q

Lorazepam (Ativan)

A
  • First Line for status epilepticus
20
Q

Midazolam (Versed)

A
  • First Line for status epilepticus
21
Q

Clobazam (Onfi)

A
  • Adjunct treatment of Lennox Gastaunt syndrome
22
Q

Gabapentin (Neurontin)

  • Focal seizure (no for absence)
  • Post herpetic neuralgia
  • GABA drug
A
  • MOA: doesn’t do GABA things (blocks Ca channel/Enhances H current/ suppress presynaptic vesicle release/ suppress NMDA receptor)
  • USE: peripheral neuropathy; bipolar disorder
  • ADR: sedation; somnolence; dizziness; wt gain
  • WARNINGS: pancreatic cancer; DRESS; multiorgan hypersensitivity
  • PREVENTS: allodynia, hyperalgesia, peripheral pain responses, decrease pain- related response after inflammation
  • RENAL adjust
23
Q

Pregabalin (Lyrica)

  • Neuropathic pain!
  • Not really for seizures
  • GABA drug
A
  • Son of gabapentin
  • USE: diabetic peripheral neuropathy; postherpetic neuralgia; adjunctive therapy for adult with focal seizures; fibromyalgia; neuropathic pain from spinal cord injury
  • ADR: Angioedema; peripheral edema; wt gain; somnolence; dizziness
  • Better absorbed than gabapentin (greater potency for seizure/neuropathic pain)
  • RENAL adjust
  • CV (controlled substance)
  • Poss preg defect (preg cat C)
24
Q

Tiagabine (Gabitril)

  • adjunct therapy for focal in pt > 12 yrs
  • GABA drug
A
  • MOA: Interferes with GABA re-uptake by binding uptake carrier (more GABA available)
  • USE: anxiety; bruxism; migraine; neuropathic pain
  • COMMON ADR: Neuro effects (dizziness; asthenia; nervousness; tremor; difficulty concentrating)
  • WARNING: new onset seizure w/o prior h/o epilepsy
25
Q

Vigabatrin (Sabril)

  • Refractory focal in adults
  • Infantile spasms (west syndrome) up to age 2
  • GABA drug
A
  • MOA: GABA analog (irreversibly inhibits GABA transaminase)

- Associated with progressive, permanent vision loss— med restrict use

26
Q

Ezogabine (Potiga)

- 3rd line adjunct therapy for focal in adults

A
  • MOA: opens K channel
  • ADR: URINARY RETENSION; blue skin discoloration; retinal pigment changes; neuro stuff
  • DRUG INTERACTION: digoxin, EtOH
  • CV
27
Q

Felbamate (Felbatol)

  • REFRACTORY PARTIAL SEIZURES
  • Last Line due to risk of aplastic anemia
A
  • MOA: blocks Na channel; modulates NMDA receptor (block)/GABA receptors (enhanced)
  • USE: Lennox-Gastaut syndrome
  • ADR: ACUTE HEPATIC FAILURE
28
Q

Eslicarbazepine (Aptiom)

- Monotherapy/adjunct for partial onset seizures

A
  • MOA not clear
  • COMMON ADR: vertigo; vision changes; N/V; fatigue; dizziness; fatigue; HA; ataxia; balance disorder
  • SERIOUS ADR: SJS/TEN/DRESS; anaphylaxis; elevated LFTs; thyroid function
  • DRUG INTERACTION: 3A4 inducer/2C19 inhibitor– OCPs, warfarin, statins
  • Preg cat C
29
Q

Brivaracetam (Briviact)

- adjunct treatment for partial onset seizures >15 yrs

A
  • Oral/injectable

- ADR: somnolence/sedation; dizziness; fatigue; N/V

30
Q

Acute/ Dose related ADRs- Neurologic/psychiatric: most common

A
  • sedation, fatigue; unsteadiness, incoordination, dizziness
  • tremor (valproic acid)
  • paresthesia (topiramate, zonisamide)
  • diplopia, blurred vision, visual distortion (carbamazepine, lamotrigine)
  • mental/motor slowing or impairment (topiramate)
  • mood or behavioral changes (levetiracetam)
  • changes in libido or sexual function (carbamazepine, phenytoin, phenobarbital)
31
Q

Acute/Dose related ADR- GI

A
  • nausea
  • heartburn
  • wt gain/appetite changes (valproic acid, gabapentin, pregabalin, vigabatrin)
  • wt loss (topiramate, zonisamide, felbamate)
32
Q

Acute/Dose related ADR- lab changes

A
  • Hyponatremia (carbamazepine, oxcarbazepine)
  • Increases in ALT/AST
  • Leukopenia
  • Thrombocytopenia
33
Q

Acute/Dose related ADR- Skin related

A
  • rash, exfoliation
  • SJS (most common in Iamotrigine pt)
  • signs of SJS: hepatic damage, early sx (abd pain, V, jaundice), fever and mucus membrane involvement
34
Q

Acute/Dose related ADR- Hematologic damage

A
  • marrow aplasia, agranulocytosis
  • early sx: abnormal bleeding, acute onset of fever, sx of anemia
  • felbamate aplastic anemia
35
Q

Long term ADR- Endocrine/metabolic effects

A
  • osteomalacia, osteoporosis (Vit D deficiency): carbamazepine, barbiturates, phenytoin, oxcarbazepine, valproate
  • Teratogenesis (folate deficiency): barbiturates, phenytoin, carbamazepine, valproate (neural tube defects), topiramate (cleft lip/cleft palate)
  • altered connective tissue metabolism or growth (facial coarsening, hirsutism, gingival hyperplasia or contractures): phenytoin, phenobarbital
36
Q

Long term ADR- neurologic

A
  • neuropathy: phenytoin, carbamazepine

- cerebellar degeneration (phenytoin)

37
Q

Long term ADR- sexual dysfunction (polycystic overies)

A

phenytoin, carbamazepine, phenobarbital, primidone

38
Q

AED hypersensitivity syndrome

A
  • rash, systemic involvement
  • lack of epoxide hydrolase
  • cross reactivity: phenytoin, carbamazepine, phenobarbital, oxcarbazepine
  • relative cross reactivity: lamotrigine
39
Q

Status Epilepticus Algorithm (All with continuous EEG monitoring)

A

Step 1: Stabilize pt, time seizure from onset, monitor vitals, get lab work

Step 2: Benzodiazepine

  • IM midazolam vs IV lorazepam vs IV diazepam
  • if above not available: IV phenobarbital vs rectal diazepam vs intranasal midazolam

Step 3: 2nd line options (single dose)

  • IV fosphenytoin vs IV valproic acid vs IV levetiracetam
  • if above not available: IV phenobarbital

Step 4: repeat 2nd line OR anesthetic doses
- thiopental, midazolam, pentobarbital, propofol

Pharm (9 decks)

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