AntiEpileptic Drugs- Pharm Flashcards

1
Q

Neurotransmitter’s that cause excitation

A

glutamate, aspartate

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2
Q

Neurotransmitter’s that cause inhibition

A

GABA

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3
Q

Block voltage-gated Na+ channels MOA

A

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

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4
Q

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

A

“open state” and “fast-inactivated state”

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5
Q

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

A

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

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6
Q

Name of drug that enhances slow inactivation of Na channels

A

Lacosamide

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7
Q

Name of drugs that inhibits post-synaptic AMPA receptor

A

Topiramate & Perampanel

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8
Q

What ions come through either the AMPA receptor/NMDA receptor

A

Na+ and Ca+2

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9
Q

Name of drug that inhibits NMDA receptor

A

Felbamate

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10
Q

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

A

glutamate

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11
Q

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

A

T-type Ca2+ channels

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12
Q

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

A

Ethosuximide and Zonisamide

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13
Q

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

A

Levetiracetam and Brivaracetam

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14
Q

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

A

Gabapentin and Pregabalin

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15
Q

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

A

Ezogabine

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16
Q

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

A

Tiagabine

17
Q

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

A

Valproic acid and Vigabatrin

18
Q

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

A

Valproic acid

19
Q

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

A

Valproic acid, Gabapentin, Pregabalin

20
Q

How do post-synaptic GABAergic receptors work

A

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

21
Q

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

A

Barbiturates, Benzodiazapines, Topiramate

22
Q

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

A

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

23
Q

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

A

Barbiturates (PB) (phenobarbital, primidone)

24
Q

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

A

Barbiturates

25
Q

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

A

Topiramate

26
Q

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

A

Hepatocellular injury

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

27
Q

General Warnings of AEDs

A

Stopping drug leads to increased epilespsy

Suicidal behaviors and ideations

28
Q

General facts about Phenytoin

A

Zero order
Inducer of CYP-450
Toxicity causes Gingival hyperplasia

29
Q

General facts about Carbamazepine

A

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

30
Q

General facts about Phenobarbital

A

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

31
Q

General facts about Vigabatrin

A

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

32
Q

Drugs that induce CYP-450

A

Carbamazepine
Phenytoin
Phenobarbital

33
Q

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

A

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

34
Q

Which AEDs block UGT, preventing metabolism of other drugs

A

Valproic acid & Lamotrigine

35
Q

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

A

Phenytoin, Carbamazepine & Phenobarbital

36
Q

Newer AEDs are cleared by?

A

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

37
Q

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

A

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