Anti-Epileptic Drugs - GABA Flashcards

1
Q

The drugs that affect GABA want to do what to its concentration/actions?

A

Increase GABA concentration/actions!

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2
Q

What are 3 classes of drugs that block GABA re-uptake or metabolism?

A
  1. GAD stimulation
  2. GAT-1 inhibition
  3. GABA-T inhibition
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3
Q

What does GAD do?

A

Makes more GABA in the pre-synaptic vesicle

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4
Q

What are 3 drugs that stimulate GAD?

A

Valproic Acid
Gabapentin
Pregabalin

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5
Q

What are 3 drugs that stimulate GAD?

A

Valproic Acid
Gabapentin
Pregabalin

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6
Q

Which 2 drugs are both blockers of alpha-2-delta subunit of T-type Ca++ channels and also GAD stimulators?

A

Gabapentin

Pregabalin

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7
Q

What does GAT-1 do?

A

Re-uptakes GABA into the pre-synaptic neuron

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8
Q

What is 1 GAT-1 inhibitor?

A

Tiagabine

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9
Q

What is 1 GAT-1 inhibitor?

A

Tiagabine

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10
Q

What does GABA-T do?

A

Metabolizes GABA in the pre-synaptic neuron

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11
Q

What are 2 GABA-T inhibitors?

A

Vigabatrin

Valproic Acid

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12
Q

What are 2 GABA-T inhibitors?

A

Vigabatrin

Valproic Acid

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13
Q

What is the side effect of Vigabatrin?

A

Permanent and progressive concentric vision loss

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14
Q

What drug is a Na voltage gated channel blocker, a GAD stimulator and a GABA-T inhibitor?

A

Valproic Acid

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15
Q

When GABA binds to its receptor on the Cl- channel on the post-synaptic neuron, what does that do?

A

Allows Cl- into the cell and hyperpolarizes to stop the AP

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16
Q

What 2 classes of drugs + 1 other drug potentiate GABAa receptor Cl- currents on the post-synaptic neuron?

A

Barbituates
Benzodiazapines
Topiramate

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17
Q

Which drug class binds to the Cl- channel on the post-synaptic neuron INDEPENDENTLY of GABA? – opens Cl- channel even without GABA binding

A

Barbituates

18
Q

What is the Barbituate drug and its prodrug form?

A

Phenobarbital

– prodrug = primidone

19
Q

What is the Barbituate drug and its prodrug form?

A

Phenobarbital

– prodrug = primidone

20
Q

Which drug class is GABA DEPENDENT and helps GABA open the Cl- channels on the post-synaptic neuron more?

A

Benzodiazapines

21
Q

What are the 4 Benzodiazapines?

A

Lorazepam
Diazepam
Clonazepam
Clobazam

22
Q

What are the 4 Benzodiazapines?

A

Lorazepam
Diazepam
Clonazepam
Clobazam

23
Q

Which drug is a Na voltage gated channel blocker, AMPA receptor blocker and potentiates the GABA receptor Cl- channel current by binding the receptor with GABA?

A

Topiramate

24
Q

Since Barbituates do not need GABA to bind and open the Cl- channels, they are more?

A

Toxic – potentially fatal

25
Q

Which additional drug is used for specific syndromes and alongside other anti-epileptic drugs?

A

Cannabidiol

26
Q

What is the possible side effect of Cannabidiol?

A

Hepatocellular injury especially if used with Valproic Acid

27
Q

What lab tests should you get before and after starting a patient on Cannabidiol?

A

AST/ALT and Albumin levels

– may cause Hepatocellular injury especially if used with Valproic acid

28
Q

What are 2 side effects of ALL anti-epileptic drugs?

A
  • Abrupt withdrawal = status epilepticus risk

- Suicide ideation

29
Q

What 4 drugs INDUCE CYP450 metabolism?

A

Carbamazepine
Phenytoin
Phenobarbital
Valproic ACid

30
Q

What 4 drugs INDUCE CYP450 metabolism?

A

Carbamazepine
Phenytoin
Phenobarbital
Valproic Acid

31
Q

List the 4 complications of the 4 inducers of CYP450 metabolism

A
  1. Osteoporosis
  2. Increases clearance of Warfarin –> clot
  3. Increases clearance of Oral Contraceptives –> pregnancy
  4. Increases clearance of HIV meds –> virus replicates
32
Q

List the 4 complications of the 4 INDUCERS of CYP450 metabolism

A
  1. Osteoporosis
  2. Increases clearance of Warfarin –> clot
  3. Increases clearance of Oral Contraceptives –> pregnancy
  4. Increases clearance of HIV meds –> virus replicates
33
Q

What 2 drugs (-) the conjugation of drugs by UGT?

A

Valproic Acid

Lamatrigine

34
Q

What 2 drugs (-) the conjugation of drugs by UGT?

A

Valproic Acid

Lamotrigine

35
Q

What is the result of Valproic Acid and Lamotrigine (-) the conjugation of other drugs by UGT?

A

INCREASES the parent drug concentration

36
Q

What 3 drugs INDUCE the conjugation of other drugs by UGT?

A

Carbamazepine
Phenytoin
Phenobarbital

37
Q

What 3 drugs INDUCE the conjugation of other drugs by UGT?

A

Carbamazepine
Phenytoin
Phenobarbital

38
Q

What is the result of Carbamazepine, Phenytoin, and Phenobarbital inducing the conjugation of drugs by UGT?

A

DECREASES the parent drug concentration

39
Q

What is Status Epilepticus?

A

Seizure that persists or occurs in frequencies where recovery between attacks does NOT occur

40
Q

What is the 2 meds that should be given with Status Epilepticus?

A
  1. IV Lorazepam (or Diazepam)

2. Fosphenytoin (or Valproic acid or Levetiracetam)