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NMSP II Exam 1 > Antiepileptic Drugs (Segars) > Flashcards

Antiepileptic Drugs (Segars) Flashcards

1
Q

What is Status Epilepticus and what drugs are used in the First and Second IVs to help treat this condition (L/L)?

What are two other drugs that can be used alternatively in the 2nd IV if the first choice drug is NOT available (F/VA)?

A

SE: seizure persisting for sufficient length of time or is repeated frequently enough that recover between attacks does NOT occur

1st IV: LORAZEPAM (use other Diazepams as alt.)

2nd IV: LEVETIRACETAM (of Fosphenytoin or Valproic Acid)

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2
Q

What 2 states do Na Channel Blockers bind during?

A

Open State and Fast-Inactivated Gate (Activation Gate is NOT closed during either of these states)

drugs cannot bind to receptors if Activation Gate is closed

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3
Q

What is the probability of Na blockade proportional to and why is it important?

A
  • proportional to FREQUENCY of Na channel opening and dose
  • epileptic seizures involve neurons firing at higher frequency than normal –> drugs preferentially act on neurons involved in the disease
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4
Q

What are the 10 Na Channel Blockers we can use for epilepsy?

(C/O/E, L, P, T, VA, L/Z/R)

Which drug ALSO enhances SLOW inactivation of Na Channels?

A

Cabamazepine (Oxcarbazepine/Eslicarbazepine)

Lamotrigine

Phenytoin (Fosphenytoin - IV use)

Topiramate

Valproic Acid

Lacosamide (Zonisamide/Rufinamide)

Lacosamide enhances slow inactivation too

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5
Q

What two drugs (T/P) inhibit glutamate uptake at the AMPA receptors on the post-synaptic neuron?

A

Topiramate and perAMPAnel

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6
Q

What drug (F) inhibits glutamate uptake at the NMDA receptors on the post-synaptic neuron?

A

Felbamate

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7
Q

What seizure does Ethosuximide specifically treat and how?

What is a hallmark finding of this seizure type?

A
  • treats Absence (Petit Mal) seizure by blocking T-Type Ca channels

Hallmark: 3-Hz “spike and wave” activity in the thalamus

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8
Q

What is Zonisamide’s method of action?

A
  • blocks low-threshold Type-T Ca channels on pre-synaptic neurons
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9
Q

What two drugs (L/B) inhibit Synaptic Vesicle 2A (SV2A) proteins?

What is the common suffix of these drugs?

A

Levetiracetam and Brivaracetam

  • suffix: “-acetam”
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10
Q

What two drugs (G/P) block that alpha2delta subunit of T-Type Ca channels on the Presynaptic neuron?

What is similar between these two drugs?

A

Gabapentin and Pregabalin

  • both drugs have “GABA” in them
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11
Q

What drug (E) opens the KCNQ K channel on both the Presynaptic and Postsynaptic neurons?

A

Ezogabine

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12
Q

What do these drugs target in the Pre-Synaptic GABA neurons:

  1. Gabapentin and Pregabalin
  2. Tiagabine
  3. Vigabatrin
A
  1. inc. levels of Glutamic Acid Decarboxylase
  2. blocks GAT-1 = GABA Transporter 1 (blocks reuptake)
  3. blocks GABA-T (prevents GABA metabolism)
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13
Q

What three things does Valproic Acid target in the Pre-Synaptic GABA neurons?

A
  1. inc. Glutamic Acid Decarboxylase
  2. blocks GABA-T (prevents GABA metabolism)
  3. blocks SDD (prevents GABA metabolism)
    • Succinic Semialdehyde Dehydrogenase
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14
Q

Post-Synaptic GABA Neuronal Transmission

What is the MOA of Phenobarbitol and Primidone?

A

MOA: bind to BETA subunit of GABA receptors and increase DURATION of Cl channel opening
- GABA INdependent = INC. TOXICITY

Primidone is a PRODRUG of Phenobarbitol

  • both of these drugs are Barbiturates
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15
Q

Post-Synaptic GABA Neuronal Transmission

What is the MOA of Lorazepam, Diazepam, Clonazepam, and Clobazam?

A

MOA: bind to ALPHA subunit of GABA receptors and cause allosteric change that potentiates GABA binding = Cl channels open with greater frequency
- GABA DEpendent

  • all of these drugs are BENZODIAZEPINES
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16
Q

What are the 3 functions of Topiramate?

A
  1. inc. frequency of GABA receptor activation
  2. fast inactivation of Na channels
  3. AMPA receptor antagonist
17
Q

What effect do HIGH levels of Ezogabine have on GABA receptors?

A
  • inc. opening of GABA receptors

also used as K Channel opener on Pre- and Post-Synaptic Glutamate neurons

18
Q

What is the treatment for Dravet Syndrome and Lennox-Gastaut Syndrome?

A

Cannabidiol

19
Q

What are the two major risk factors of ALL Anti-Epileptic Drugs?

A
  1. Abrupt withdrawal can cause STATUS EPILEPTICUS

2. inc. suicidal behavior and ideations

20
Q

Phenytoin

What are is pharmacokinetics and what are two serious toxicities it can cause?

A

P: Zero-order = only so much can be metabolized meaning inc. dosage = TOXIC (serum lvls skyrocket)

T: Gingival Hyperplasia and Hypocalcemia

also well-known CYP450 enzymes

21
Q

What 4 drugs can cause Osteopenia/Osteoporosis via induction of CYP-450-dependent Vitamin D catabolism?

(C/P/P/VA)

A

Carbamazepine
Phenytoin
Phenobarbital
Valproic Acid

all dec. circulating Vitamin D lvls = PTH-mediated responses that demineralize bone

22
Q

Carbamazepine

What enzymes does it induce and what hematological issue can it cause?

A
  • CYP450 enzyme induce that can SELF-METABOLIZE

- can have bone marrow suppressant activity (leukopenia/neutropenia/thrombocytopenia) so make sure to GET BASELINE CBC

23
Q

Why are Oxcarbazepine and Eslicarbazepine safer options than Carbamazepine?

A
  • both are converted to S-licarbazine which is LESS toxic than the epoxide metabolic product that Carbamazepine produces
24
Q

What is a major toxicity of Vigabatrin use?

A
  • can cause permanent, progressive, bilateral, concentric VISION LOSS
    • D/C after max of 3 months if not reponse

prescribeable ONLY through REMS program

25
Q

What effect do Valproic Acid and Lamotrigine have on UGT?

A
  • both BLOCK UTG causing accumulation of parent drugs
26
Q

What effect do Phenytoin, Carbamazepine, and Phenobarbital have on UGT?

A
  • all 3 INDUCE UGT causing reduction or parent drugs
27
Q

CYP-450 Inducers

What are 3 drugs (C/P/P) can reduce levels of Oral Contraceptives, Warfarin, and Antivirals by inducing clearance via CYP-450?

A
  1. Carbamazepine
  2. Phenytoin
  3. Phenobarbitol

NMSP II Exam 1 (6 decks)

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