Anti-Epileptic Drugs - GABA

Question 1

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

Answer 1

Increase GABA concentration/actions!

Question 2

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

Answer 2

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

Question 3

What does GAD do?

Answer 3

Makes more GABA in the pre-synaptic vesicle

Question 4

What are 3 drugs that stimulate GAD?

Answer 4

Valproic Acid
Gabapentin
Pregabalin

Question 5

What are 3 drugs that stimulate GAD?

Answer 5

Valproic Acid
Gabapentin
Pregabalin

Question 6

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

Answer 6

Gabapentin

Pregabalin

Question 7

What does GAT-1 do?

Answer 7

Re-uptakes GABA into the pre-synaptic neuron

Question 8

What is 1 GAT-1 inhibitor?

Answer 8

Tiagabine

Question 9

What is 1 GAT-1 inhibitor?

Answer 9

Tiagabine

Question 10

What does GABA-T do?

Answer 10

Metabolizes GABA in the pre-synaptic neuron

Question 11

What are 2 GABA-T inhibitors?

Answer 11

Vigabatrin

Valproic Acid

Question 12

What are 2 GABA-T inhibitors?

Answer 12

Vigabatrin

Valproic Acid

Question 13

What is the side effect of Vigabatrin?

Answer 13

Permanent and progressive concentric vision loss

Question 14

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

Answer 14

Valproic Acid

Question 15

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

Answer 15

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

Question 16

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

Answer 16

Barbituates
Benzodiazapines
Topiramate

Question 17

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

Answer 17

Barbituates

Question 18

What is the Barbituate drug and its prodrug form?

Answer 18

Phenobarbital

– prodrug = primidone

Question 19

What is the Barbituate drug and its prodrug form?

Answer 19

Phenobarbital

– prodrug = primidone

Question 20

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

Answer 20

Benzodiazapines

Question 21

What are the 4 Benzodiazapines?

Answer 21

Lorazepam
Diazepam
Clonazepam
Clobazam

Question 22

What are the 4 Benzodiazapines?

Answer 22

Lorazepam
Diazepam
Clonazepam
Clobazam

Question 23

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?

Answer 23

Topiramate

Question 24

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

Answer 24

Toxic – potentially fatal

Question 25

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

Answer 25

Cannabidiol

Question 26

What is the possible side effect of Cannabidiol?

Answer 26

Hepatocellular injury especially if used with Valproic Acid

Question 27

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

Answer 27

AST/ALT and Albumin levels | -- may cause Hepatocellular injury especially if used with Valproic acid

Question 28

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

Answer 28

- Abrupt withdrawal = status epilepticus risk | - Suicide ideation

Question 29

What 4 drugs INDUCE CYP450 metabolism?

Answer 29

Carbamazepine Phenytoin Phenobarbital Valproic ACid

Question 30

What 4 drugs INDUCE CYP450 metabolism?

Answer 30

Carbamazepine Phenytoin Phenobarbital Valproic Acid

Question 31

List the 4 complications of the 4 inducers of CYP450 metabolism

Answer 31

1. Osteoporosis 2. Increases clearance of Warfarin --> clot 3. Increases clearance of Oral Contraceptives --> pregnancy 4. Increases clearance of HIV meds --> virus replicates

Question 32

List the 4 complications of the 4 INDUCERS of CYP450 metabolism

Answer 32

1. Osteoporosis 2. Increases clearance of Warfarin --> clot 3. Increases clearance of Oral Contraceptives --> pregnancy 4. Increases clearance of HIV meds --> virus replicates

Question 33

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

Answer 33

Valproic Acid | Lamatrigine

Question 34

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

Answer 34

Valproic Acid | Lamotrigine

Question 35

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

Answer 35

INCREASES the parent drug concentration

Question 36

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

Answer 36

Carbamazepine Phenytoin Phenobarbital

Question 37

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

Answer 37

Carbamazepine Phenytoin Phenobarbital

Question 38

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

Answer 38

DECREASES the parent drug concentration

Question 39

What is Status Epilepticus?

Answer 39

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

Question 40

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

Answer 40

1. IV Lorazepam (or Diazepam) | 2. Fosphenytoin (or Valproic acid or Levetiracetam)