Anti-Epileptic Drugs - GABA Flashcards
The drugs that affect GABA want to do what to its concentration/actions?
Increase GABA concentration/actions!
What are 3 classes of drugs that block GABA re-uptake or metabolism?
- GAD stimulation
- GAT-1 inhibition
- GABA-T inhibition
What does GAD do?
Makes more GABA in the pre-synaptic vesicle
What are 3 drugs that stimulate GAD?
Valproic Acid
Gabapentin
Pregabalin
What are 3 drugs that stimulate GAD?
Valproic Acid
Gabapentin
Pregabalin
Which 2 drugs are both blockers of alpha-2-delta subunit of T-type Ca++ channels and also GAD stimulators?
Gabapentin
Pregabalin
What does GAT-1 do?
Re-uptakes GABA into the pre-synaptic neuron
What is 1 GAT-1 inhibitor?
Tiagabine
What is 1 GAT-1 inhibitor?
Tiagabine
What does GABA-T do?
Metabolizes GABA in the pre-synaptic neuron
What are 2 GABA-T inhibitors?
Vigabatrin
Valproic Acid
What are 2 GABA-T inhibitors?
Vigabatrin
Valproic Acid
What is the side effect of Vigabatrin?
Permanent and progressive concentric vision loss
What drug is a Na voltage gated channel blocker, a GAD stimulator and a GABA-T inhibitor?
Valproic Acid
When GABA binds to its receptor on the Cl- channel on the post-synaptic neuron, what does that do?
Allows Cl- into the cell and hyperpolarizes to stop the AP
What 2 classes of drugs + 1 other drug potentiate GABAa receptor Cl- currents on the post-synaptic neuron?
Barbituates
Benzodiazapines
Topiramate
Which drug class binds to the Cl- channel on the post-synaptic neuron INDEPENDENTLY of GABA? – opens Cl- channel even without GABA binding
Barbituates
What is the Barbituate drug and its prodrug form?
Phenobarbital
– prodrug = primidone
What is the Barbituate drug and its prodrug form?
Phenobarbital
– prodrug = primidone
Which drug class is GABA DEPENDENT and helps GABA open the Cl- channels on the post-synaptic neuron more?
Benzodiazapines
What are the 4 Benzodiazapines?
Lorazepam
Diazepam
Clonazepam
Clobazam
What are the 4 Benzodiazapines?
Lorazepam
Diazepam
Clonazepam
Clobazam
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?
Topiramate
Since Barbituates do not need GABA to bind and open the Cl- channels, they are more?
Toxic – potentially fatal
Which additional drug is used for specific syndromes and alongside other anti-epileptic drugs?
Cannabidiol
What is the possible side effect of Cannabidiol?
Hepatocellular injury especially if used with Valproic Acid
What lab tests should you get before and after starting a patient on Cannabidiol?
AST/ALT and Albumin levels
– may cause Hepatocellular injury especially if used with Valproic acid
What are 2 side effects of ALL anti-epileptic drugs?
- Abrupt withdrawal = status epilepticus risk
- Suicide ideation
What 4 drugs INDUCE CYP450 metabolism?
Carbamazepine
Phenytoin
Phenobarbital
Valproic ACid
What 4 drugs INDUCE CYP450 metabolism?
Carbamazepine
Phenytoin
Phenobarbital
Valproic Acid
List the 4 complications of the 4 inducers of CYP450 metabolism
- Osteoporosis
- Increases clearance of Warfarin –> clot
- Increases clearance of Oral Contraceptives –> pregnancy
- Increases clearance of HIV meds –> virus replicates
List the 4 complications of the 4 INDUCERS of CYP450 metabolism
- Osteoporosis
- Increases clearance of Warfarin –> clot
- Increases clearance of Oral Contraceptives –> pregnancy
- Increases clearance of HIV meds –> virus replicates
What 2 drugs (-) the conjugation of drugs by UGT?
Valproic Acid
Lamatrigine
What 2 drugs (-) the conjugation of drugs by UGT?
Valproic Acid
Lamotrigine
What is the result of Valproic Acid and Lamotrigine (-) the conjugation of other drugs by UGT?
INCREASES the parent drug concentration
What 3 drugs INDUCE the conjugation of other drugs by UGT?
Carbamazepine
Phenytoin
Phenobarbital
What 3 drugs INDUCE the conjugation of other drugs by UGT?
Carbamazepine
Phenytoin
Phenobarbital
What is the result of Carbamazepine, Phenytoin, and Phenobarbital inducing the conjugation of drugs by UGT?
DECREASES the parent drug concentration
What is Status Epilepticus?
Seizure that persists or occurs in frequencies where recovery between attacks does NOT occur
What is the 2 meds that should be given with Status Epilepticus?
- IV Lorazepam (or Diazepam)
2. Fosphenytoin (or Valproic acid or Levetiracetam)