AntiEpileptic Drugs- Pharm

Question 1

Neurotransmitter’s that cause excitation

Answer 1

glutamate, aspartate

Question 2

Neurotransmitter’s that cause inhibition

Answer 2

GABA

Question 3

Block voltage-gated Na+ channels MOA

Answer 3

the drug will only work when the activation gate of the Na channels are open

Question 4

What states are the voltage-gated Na+ channels’ activation gate open

Answer 4

“open state” and “fast-inactivated state”

Question 5

What are the names of the 6 drugs that are Voltage-gated Na+ channel blockers

Answer 5

Carbamazepine (Oxcarbazepine/Eslicarbazepine), Lamotrigine, Phenytoin (Fosphenytoin; IV form), Topiramate, Valproic acid/Divalproex (Valproate; IV form), Lacosamide (Zonisamide/Rufinamide)

Question 6

Name of drug that enhances slow inactivation of Na channels

Answer 6

Lacosamide

Question 7

Name of drugs that inhibits post-synaptic AMPA receptor

Answer 7

Topiramate & Perampanel

Question 8

What ions come through either the AMPA receptor/NMDA receptor

Answer 8

Na+ and Ca+2

Question 9

Name of drug that inhibits NMDA receptor

Answer 9

Felbamate

Question 10

What NT binds to the AMPA/NMDA receptor to open it

Answer 10

glutamate

Question 11

What type of channel is active and is the hallmark of petit-mal seizures

Answer 11

T-type Ca2+ channels

Question 12

Name of drugs that blocks T-type Ca2+ channels (pre-synaptic)

Answer 12

Ethosuximide and Zonisamide

Question 13

Name of Drugs that inhibit synaptic vesicle 2A (SV2A) protein

Answer 13

Levetiracetam and Brivaracetam

Question 14

Name of drugs that block the a2d subunit of T-type Ca2+ channels

Answer 14

Gabapentin and Pregabalin

Question 15

Name of drug that opens (stimulates) K+ channels (pre-/post-synaptic)

Answer 15

Ezogabine

Question 16

Name of drug that inhibits the reuptake of GABA by GAT-1

Answer 16

Tiagabine

Question 17

Name of drugs that inhibit the metabolization of GABA via GABA-T (GABA Transaminase)

Answer 17

Valproic acid and Vigabatrin

Question 18

Name of drug that inhibits the metabolization of GABA via SSD (Succinic Semialdehyde Dehydrogenase)

Answer 18

Valproic acid

Question 19

Drugs that stimulate the enzyme GAD (Glutamic acid decarboxylase) that converts glutamate to GABA

Answer 19

Valproic acid, Gabapentin, Pregabalin

Question 20

How do post-synaptic GABAergic receptors work

Answer 20

GABA binds to the GABA receptor, this causes the Cl- channels to open; Cl- rushes into post-synaptic cell

Question 21

List the names of the drugs that enhance post-synaptic GABA-ergic neuronal transmission

Answer 21

Barbiturates, Benzodiazapines, Topiramate

Question 22

Which drug binds to an allosteric site, this potentiates GABA binding, and then causes the Cl- channels open with greater frequency

Answer 22

Benzodiazepines (BZD) (Clonazepam, Clobazam, Lorazepam, Diazepam)

Question 23

Which drug binds to a distinct allosteric site and increases the duration of Cl- channel opening

Answer 23

Barbiturates (PB) (phenobarbital, primidone)

Question 24

Which drug is GABA INdependent and therefore is extremely lethal in high doses

Answer 24

Barbiturates

Question 25

Which drug has multiple MOAs? Look it up in the slides, slide 58

Answer 25

Topiramate

Question 26

What is the main side-effect of Cannabidiol (Epidiolex)

Answer 26

Hepatocellular injury | obtain AST/ALT & Albumin levels, ESPECIALLY if given with Valproic acid

Question 27

General Warnings of AEDs

Answer 27

Stopping drug leads to increased epilespsy | Suicidal behaviors and ideations

Question 28

General facts about Phenytoin

Answer 28

Zero order Inducer of CYP-450 Toxicity causes Gingival hyperplasia

Question 29

General facts about Carbamazepine

Answer 29

Inducer of CYP-450 and autoinduction (self-metabolism) Toxicities: Leukopenia/Neutropenia/Thrombocytopenia Baseline CBC (WBC) to compare Oxcarbazepine & S-Licarbazone is a less toxic analog Less hematological AE’s and less potent inducer of CYP

Question 30

General facts about Phenobarbital

Answer 30

Requires serum drug monitoring Risk of coma/resp. Depression & fatality Inducer of CYP Toxicities: CNS depressant and hypocalcemia/Vit D deficit/Osteoporosis

Question 31

General facts about Vigabatrin

Answer 31

Toxicities: Permanent, progressive, bilateral, concentric vision loss D/C after 3 months if no effective response REMS program req

Question 32

Drugs that induce CYP-450

Answer 32

Carbamazepine Phenytoin Phenobarbital

Question 33

AED's can cause Drug Rxns, what are they?

Answer 33

Increase oral contraceptive clearance → risk of pregnancy Increases clearance of anticoags (Warfarin) → arterial/venous thrombosis Increase clearance of HIV meds → HIV replication

Question 34

Which AEDs block UGT, preventing metabolism of other drugs

Answer 34

Valproic acid & Lamotrigine

Question 35

Which AEDs induce UGT, which helps with drug metabolism of other drugs

Answer 35

Phenytoin, Carbamazepine & Phenobarbital

Question 36

Newer AEDs are cleared by?

Answer 36

the kidneys, adjust medication dose if there is injury to the kidneys

Question 37

What is the treatment algorithm if an adult comes into the hospital with a seizure?

Answer 37

Convulsive Status Epilepticus in Adults - Tx Algorithim Initial therapy: Lorazepam IV Alt. Initial therapy: Diazepam If no IV access: Midazolam Second IV: Fosphenytoin or Valproic acid or Levetiracetam or Phenytoin