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Epilepsy > Part 2 > Flashcards

Part 2 Flashcards

1
Q

Pregabalin (PGB)

-Lyrica

A

C-5 controlled substance
-Available as capsule and soln

Used for:

  • adjunct therapy for adult patients with partial onset seizures
  • Neuropathic pain

-Structurally related to GABA, but DO NOT bind to GABA or benzodiazepine receptors

MOA:

    - Binds to alpha-2 delta subunit of voltage-dependent Ca2+ channels within the CNS and INHIBITS excitatory neurotransmitter release including:
                 - Glutamate
                 - NE
                 - Seratonin
                 - Dopamine
                 - Substance P
                 - Calcitonin gene related peptide

**100% RENALLY excreted

  • *CrCl < 60 ml/min
    - decrease the dose or extend the dosing interval (similar to gabapentin)

**Pregnancy C

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2
Q

Pregabalin (PGB)
-Lyrica

Side effects, monitor, DDIs

A

Side effects:
-Sedation
-Dizziness
-Edema
-Weight GAIN
-(Rarely) myopathy and rhabdomyolosis)
(dry mouth, blurred vision, difficulty concentrating)

Monitor:

        - Scr
        - Edema
        - Weight GAIN

DDIs:

    - Minimal
    - OK to use with oral contraceptives 
    - Caution with "glitazones" due to risk of additive edema (caution in CHF)
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3
Q

Pregabalin (PGB)
-Lyrica

Patient education

A
  • Drowsiness/dizziness

- If blurred vision, excessive swelling or muscle aches occur, contact MD

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4
Q

Topiramate

-Topamax

A

Used for:

  • Partial seizures
  • Primary generalized tonic-clonic seizures (as adjunct)
  • Lennox Gastuat (as adjunct)
  • Conversion to primary therapy from older drugs
  • Migraine prophylaxis

MOA:

        - Blocks Na+ channels that enhances GABA
        - Glutamate blocker
        - Weak carbonic anhydrase inhibitor
  • *70% is RENALLY eliminated
  • *CrCl < 70 ml/min
    - Decrease the dose by 50%
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5
Q

Topiramate products

A

Topiramate

     - Topamax
     - Topamax sprinkle 
     - Topiragen

Topiramate ER

     - Qudexy XR
     - Trokendi XR

**Available as capsules, ER capsules, tablets

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6
Q

Topiramate
-Topamax

Contraindications, side effects, monitor, drug interactions

A

Contraindications:

       - Trokendi XR 
               - Recent alcohol use (within 6 hours prior to and 6 hours after dose)
               - Metabolic acidosis + taking metformin

Side effects:

          - CNS/cognitive (i.e hyper-ammonia)
          - Anorexia (weight LOSS)
          - Parasthesia 

    -Less common:
          -Nephrolithiasis (kidney stones) 
          -Angle closure glaucoma (myopia, non-anion gap acidosis, oligohydrosis (reduced perspiration/hyperthermia, hyperammonia (both alone and in combination with VALPROIC ACID)

Monitor:

         - Scr
         - Serum bicarb

DDIs

        - Reduced efficacy of estrogenic oral contraceptives 
        - Increased risk of nephrolithiasis with:
                  - ketogenic diet
                  - acetazolamide
                  - zonisamide
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7
Q

Topiramate
-Topamax

Patient education

A
  • Drowsiness
  • Numbness/tingling
  • Keep adequate fluid intake to AVOID kidney stones
  • If forgetfulness, blurred vision, eye pain occurs, consult MD
  • Decreased efficacy of birth control, especially with doses >200 mg daily; use back up
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8
Q

Lamotrigine

-Lamictal

A

Broad spectrum (similar to Valproic acid)

Used for:

  • Partial seizures
  • Primary and secondary generalized tonic-clonic seizures
  • Lennox Gastaut
  • Bipolar

MOA:

     - Blocks Na+ channels
     - Inhibits glutamate release
  • *NOT a CYP450 substrate
  • *Hepatic UGT metabolism
    - When added to a UGT enzyme INDUCER (CBZ, PHT, PB, PRIM, Rifampin, lopinavir/ritonavir, estrogen-OCs):
    - t1/2 is REDUCED from 25 to 14 hours
          - When added to a UGT INHIBITOR (VPA)
              - t1/2 is INCREASED to 60 hours

**Pregnancy C

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9
Q

Lamotrigine Products

A

Available as tablet, chewable, ODT

  • Lamotrigine
  • Lamictal
  • Lamictal starter**
    - Provide the recommended dose/titration schedule for the first 5 weeks; titration schedule is based on concomitant medications
  • Lamictal ODT**
    - Provide the recommended dose/titration schedule for the first 5 weeks; titration schedule is based on concomitant medications
  • Lamictal XR
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10
Q

Lamotrigine
-Lamictal

Dosing

A

Starting dose:
-50 - 250 mg BID

Week 1 and 2:
-25 mg daily

Week 3 and 4:
-50 mg daily

Week 5 and on:
-Can increase by 50 mg daily every 1-2 weeks

Maintainence dose:
-300 - 400 mg daily (split BID)

For patients on VPA: (cut dose in half)
-Week 1 and 2: 25 mg QOD

For patients on hepatic inducers (or smokers, you double the dose)
-Week 1 and 2: 50 mg daily

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11
Q

Lamotrigine
-Lamictal

Black box warning, tolerability/side effects, monitoring

A

Black box warning:

      - Serious rash
      - SJS/TEN
               - Risk factors:
                     1) young age (< 16 years) 
                     2) co-medication with VPA
                     3) Rapid titration
                     4) High starting dose

Tolerability/side effects:

         - Well tolerated
         - Low sedation and cognitive side effects
         - NO weight GAIN 
         - No osteopenia
         - Low teratogenicity (Pregnancy C)

Monitoring:

          - LFTs 
          - Signs/symptoms of rash
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12
Q

Lamotrigine
-Lamictal

Patient education

A
  • Drowsiness
  • Dizziness
  • Doses will be increased gradually; make take several weeks to reach maintenance dose
  • Comes in child-resistant packaging
  • Starter-kit packaging:
    - Orange: for those NOT taking interacting medications
          - Blue: for those taking VPA
      - Green: for those taking an INDUCER
  • *If rash occurs, contact MD immediately
  • *Folic acid

-Importance of compliance

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13
Q

Levetiracetam

  • Keppra
  • Keppra XR
  • Spritam
A

Used for:

  • Partial seizures
  • Secondary general tonic-clonic seizures

MOA:

     - Exact MOA is unknown 
     - May inhibit voltage-gated N-type Ca2+ channels and facilitate GABA-ergic inhibitory transmission through its displacement of negative modulators
  • *IV and oral
  • *100% oral bioavailability
  • *70% RENALLY excreted
  • *CrCl (less than or equal to) < 80 ml/min
    - Requires dose REDUCTION
  • WARNING
    - behavioral abnormalities and psychotic symptoms
    - SJS/TEN

Notable side effects:

     - Sedation
     - Dizziness
     - Weakness
     - Coordination difficulties
     - Dose related behavior changes

NO significant DDIs:

     - No effect on other AED levels
     - No effect on oral contraceptives
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14
Q

Levetiracetam

  • Keppra
  • Keppra XR
  • Spritam

Patient education

A
  • Drowsiness
  • Inform MD of any change in behavior or mood

-Spritam uses ZipDose technology with 3D printing to produce a porous tablet formulation that rapidly dissolves with a sip of liquid

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15
Q

Felbamate
-Felbatol

**tablet, suspension

A

Broad spectrum (similar to valproic acid and lamotrigine)

Used for:

  • Partial seizures
  • Primary and secondary generalized tonic-clonic seizures
  • Reserved for REFRACTORY cases*

MOA:

     - NMDA blocker
     - GABA enhancer

Black box warning:

      - Aplastic anemia 
              - Risk factors:
                      1) Hx of AED allergy or toxicity 
                      2) Immune disorder
                      3) Previous cytopenia 
                      4) Caucasian
                      5) Female
                       6) Adult 
        - Hepatotoxicity that can be FATAL

Side effects:

      - Insomnia
      - Anorexia (weight loss -- similar to Topiramate) 
      - Headache
      - N/V
      - Gingival hypertrophy (similar to phenytoin)

Monitor:

       - CBC twice monthly
       - LFT weekly

DDIs:

       - P450 inducer and inhibitor 
              - decreases levels of oral contraceptives
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16
Q

Felbamate
-Felbatol

**tablet, suspension

Patient education

A
  • Insomnia
  • Loss of appetite
  • Weight LOSS
  • Sedation is less common

**Rarely may cause damage to the blood and liver

  • *Report to MD
    - Informed consent needs to be signed by the patient and prescriber PRIOR to dispensing
    - Symptoms of abnormal bleeding, suddent onset of infection or persistent abdominal pain
  • Importance of compliance/monitoring
  • Decreases levels of oral contraceptives; use back up
17
Q

Brivaracetam

-Briviact

A

Used for:
-Monotherapy or adjunct for partial onset seizures for adults > 16 years of age

-Available as injection, syrup, and film-coated tablets

MOA:
-Selective to synaptic protein vesicle 2A –> anti-seizure effect

**Major 2C19

Common side effects:

       - Drowsiness
       - Dizziness
       - Fatigue
       - N/V

Concerning side effects:

       - Suicide attempts
       - Agitation/aggression 
       - New or worsening depression 
       - Panic attacks
18
Q

Ethosuximide
-Zarontin

**Capsule and solution

A

Drug of choice for ABSENCE seizures

**May worsen generalized tonic-clonic seizures

MOA:

     - Succinimide
     - Inhibits Ca2+ currents that increase seizure threshold and suppresses paroxysmal spike-and-wave pattern in absence seizures

Therapeutic levels:
-40 - 100 mcg/mL

WARNING:

      - SJS/TEN
      - Blood dyscrasia

Side effects:

      - Nausea
      - Weight LOSS (similar to Topiramate and Felbamate) 
       - Hiccups
       - Rash
       - Hepatotoxicity

DDIs:
-VPA can INCREASE ethosuximide levels

19
Q

Tigabine

-Gabitril

A

Available as tablets

Used for:

  • Adjunct for partial seizures
  • OFF label for PTSD

MOA:
-Inhibits GABA reuptake into presynaptic nerve terminals

WARNING:

           - Worsening of seizures/new onset of seizures when used OFF label for other indications
           - SJS/TEN

Side effects:

           - Abnormal thinking
           - Dizziness
           - Drowsiness
           - Depression
           - Tremor
           - Asthenia

DDIs:

    - OK with oral contraceptives 
    - Caution with CNS depressants
20
Q

Zonisamide

-Zonegran

A

Broad spectrum efficacy
-available as a capsule

Used for:

  • Partial seizures
  • Primary and secondary generalized tonic-clonic seizures

MOA:

     - Multiple mechanisms
     - Weak carbonic anhydrase inhibitor

**Need to dose adjust for RENAL impairment

Notable side effects:

      * *Idiosyncratic rash, nephrolithiasis 
      - Weight LOSS
      - Sedation 
      - Dizziness 
      - Language difficulty
      - Depression
      - Psychosis

DDIs:

     - Minimal effect on other AED levels
     - Increased risk of nephrolithiasis with:
               - Ketogenic diet
               - Acetazolamide
               - Topiramate
      - No effect on oral contraceptives

Contraindications:
-Sulfa allergy

21
Q

Zonisamide

-Zonegran

A
  • Drowsiness
  • Dizziness
  • Unsteady gait upon initiation
  • Adequate fluid intake (to prevent nephrolithiasis)
22
Q

Lacosamide

-Vimpat

A

C-5 controlled substance

Available as tablet, PO liquid, injection, solution

Used for:
-Monotherapy or adjunct in partial-onset seizure for >17 year old

MOA:
-Enhancers of slow inactivation of Na+ channels

Side effects:

       - Dizziness
       - Headache
       - N/V
       - Double vision
       - Fatigue
       - Memory problems
       - Mood problems
       - ECG changes
  • *CrCl < 30 ml/min
    - 300 mg/daily max

**DO NOT use in severe hepatic impairment

**DO NOT stop abruptly – withdraw over 1 week

**CAUTION in patients with pre-existing heart disease, AV block

23
Q

Rufinamide

-Banzel

A

-Available as tablets and oral suspension

Used for:
-Adjunctive tx of seizures of Lennox Gastaut Syndrome

MOA:
-Enhancers of slow inactivation of Na+ channel

-Take with food

Side effects:

         - Somnolence
         - Vomiting
         * **Shortening of QT interval

Contraindications:
-Patients with familial short QT syndrome due to QT shortening (dose-related)

24
Q

Vigabatrin

-Sabril

A

Available as a tablet and packet for solution

Used for:
-Adjunct treatment of adults with REFRACTORY partial seizures, infantile spasms

MOA:
-Enhances GABA by irreversibly inhibiting GABA transaminase

Renal adjustments:

  • CrCl 50-80 ml/min = reduce the dose by 25%
  • CrCl 30-50 ml/min = reduce the dose by 50%
  • CrCl 140 ml/min = reduce the dose by 75%

Black box warning:

        - Permanent peripheral vision loss
                - Ideally, don't give to infants because of this

Side effects:

       - MRI abnormalities
       - Drowsiness
       - Fatigue
       - Headache
       - Dizziness

Monitor:
-Baseline eye exam every 3 months during therapy and 3-6 months after discontinuation

  • *SHARE program
    - Only physicians and pharmacies registered with the SHARE program can prescribe and dispense Vigabatrin
25
Q

Ezogabine

-Potiga

A

C-5 controlled medication

Used for:

  • Adjunct treatment of partial onset seizure in patients 18 years and older
  • REFRACTORY partial seizures

MOA:
-K+ channel opener

CrCl < 50 ml/min = initial 150 mg/daily, up to a max of 600mg/daily

Hepatic impairtment = dose adjust

Pregnancy C

26
Q

Ezogabine
-Potiga

Black box warning, side effects, DDIs

A

Black box warning:

       - Retinal abnormalities and potential visual loss
             - 33% of patients after 4 years of treatment

Side effects:
-Blue skin discoloration
-QT prolongation
**Orange/brown urine discoloration
(diplopia, urinary retention, dose-related psychosis and hallucinations within first 8 weeks of tx)

DDIs:
-May POTENTIATE Digoxin – monitor

27
Q

Perampanel

-Fycompa

A

C-3 controlled medication

Used for:
-Adjunct therapy for the tx of partial onset seizures with or without secondary generalized seizures in patients with epilepsy aged 12 years and older

MOA:
-Selective, non-competitive AMPA glutamate receptor antagonist

Max recommended dose: 12 mg daily QHS (bedtime)

Pregnancy C

28
Q

Perampanel
-Fycompa

Black box warning, DDIs, side effects,

A

Black box warning:
-Risk of serious psychiatric and behavioral reactions such as aggression, hostility, irritability, anger and homicidal ideation in the first 6 weeks

**NOT recommended in severe RENAL and HEPATIC impairment

DDIs:

    - Antagonized by CYP450 inducers
    - Antagonizes Midazolam 
    - Potentiated by Ketoconazole
    - Potentiates oxcarbazepine

    -Reduces the effectiveness of oral contraceptives, use back up 
Side effects:
           -Somnolence
           -Dizziness
           -Fatigue
           -Irritability
           -Weight GAIN 
(falls, nausea, vertigo, ataxia, gait disturbance, balance disorder)

**Ca2+ and Vitamin D supplement is recommended

29
Q

Eslicarbazepine

-Aptiom

A

Used for:

  • Adjunct therapy or monotherapy for partial onset seizures
  • REFRACTORY partial seizures

MOA:

     - Eslicarbazepine acetate is the active metabolite of oxcarbazepine which exerts the therapeutic effects 
     - Na+ channel blocker

CrCl < 50 ml/min = reduce initial titration and maintenance dose by 50%

  • *Same warnings and side effects as Oxcarbazepine
    - HYPO-natremia
    - HYPO-thyroid
    - SJS
    - Suicide attempts

**Moderate 3A4 and 2C19 inducer

Monitor:

     - CBC
     - Platelets
     - LFT
     - Sodium

Epilepsy (2 decks)

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