Dr. Segars - Pharmacology of Seizures and Epilepsy Flashcards

1
Q

Transient alteration of behavior due to disordered, synchronous and rhythmic firing of populations of brain neurons is known as ________ .

A

Seizure

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2
Q

Acquired or inherited malfunction of neuronal ion channels or neurotransmitter systems disrupting normal electrical activity in the brain is known as _________ .

A

Epilepsy

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3
Q

Differentiate between simple and complex partial types of seizures.

A

Partial = Beginning focally in a cortical site

Simple Partial - Preservation of consciousness

Complex Partial - Impairment of consciousness

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4
Q

Absence, myoclonic and tonic-clonic seizures are all examples of _________ .

A

Generalized Seizures

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5
Q

Explain how Anti-Epileptic Drugs work.

A

They are going to enter the inside of the pore and bind to the “inactivation gate”, keeping the Voltage-Gated Na+ channels closed and preventing action potentials from occurring!

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6
Q

Pharmacological activity of AEDs is said to be _________ - dependent because you have to have the “pore” of the channel open in order for them to access the “inactivation gates”.

A

“State”

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7
Q

The probability of a Voltage-Gated Na+ Channel blockade is proportional to the __________ of Na channels opening and closing.

This is known as the “_____“-dependent side of the AEDs.

A

Frequency

Use

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8
Q

Carbamazepine, Oxcarbazepine, Eslicarbazepine, Lamotrigine, Phenytoin, Topiramate, Valporic Acid, Zonisamide and Lacosamide are all examples of __________ .

A

AEDs that will bind to the FAST inactivation state of Voltage-Gated Na+ Channels

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9
Q

What is special about Lacosamide?

A

It is not necessary for the “pore” to be open in order for Lacosamide to block the channel!

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10
Q

Topiramate and Perampanel are going to antagonize which receptor?

A

AMPA-receptors (Glutamate)

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11
Q

Fosphenytoin is the _______ form of the drug while phenytoin is the ________ .

A

IV

Water-soluble Pro-Drug

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12
Q

Which receptor does felbamate antagonize?

A

NMDA-Receptor (Glycine)

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13
Q

In Pre-Synaptic GABA-ergic Transmission, _____________ is going to inhibit the uptake of GABA by blocking ________ .

A

Tiagabine

GAT-1 (GABA Transporter)

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14
Q

In Pre-Synaptic GABA-ergic Transmission, _________ is going to inhibit the metabolism of GABA by inhibiting _______, ________ and ______.

A

Valproic Acid

  1. Glutamic acid decarboxylase
  2. GABA Transaminase (GABA-T)
  3. Succinic Semialdehyde Decarboxylase (SSD)
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15
Q

In Pre-Synaptic GABA-ergic Transmission, ________ is going to inhibit the metabolism of GABA by inhibiting _________ .

A

Vigabatrin

GABA transaminase (GABA-T)

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16
Q

Barbiturates (Phenobarbital/Primidone), Benzodiazapines and Topiramate are all going to act to ___________ Post-Synpatic GABA-ergic Neuronal Transmission.

A

Enhance

17
Q

Which drug is more lethal, Barbiturates or Benzodiazepines? And why?

A

Barbiturates!

They are able to bind to the GABA receptor in the absence of GABA (GABA-Independent)

18
Q

True or False. Benzodiazapines are GABA-Dependent when it comes to binding to the receptor.

A

True

19
Q

Barbituates are going to increase the ________ that the GABA receptor is open.

A

Duration

20
Q

Benzodiazapines are going to increase the _________ that the GABA receptor is open.

A

Frequency

21
Q

Which drug has the following three actions:

  1. GABA-A agonist (increase the frequency of GABA-A activation)
  2. Binds to Fast Inactivation gates in Voltage-Gated Na+ Channels
  3. AMPA-Receptor Antagonist
A

Topiramate

22
Q

T-Type Ca2+ channels that mediate 3-Hz spike and wave activity in the thalamus is a hallmark of ________ .

A

Absence (Petit mal) seizures

23
Q

Ethosuximide, Valporic Acid and Zonisamide are all antagonists of _______ .

A

T-Type Ca2+ channels

24
Q

What do you have to be careful when using Zonisamide in the treatment of Absence Seizures?

A

It is a sulfonamide and you need to double check to make sure the patient does not have any sulfur allergies!!!

25
Q

Levetiracetam and Brivaracetam are going to inhibit ________ .

A

Synaptic Vesicle Protein-2A

26
Q

Gabapentin and Pregabalin are going to inhibit _________ .

A

alpha 2 delta Ca2+ Channels

27
Q

Chronic administration of carbamazepine, phenytoin, phenobarbital and valproic acid can induce CYP450-dependent ___________.

A

Vitamin D catabolism

28
Q

Which drug participates in auto-induction (self-metabolism)?

A

Carbamazepine

29
Q

Which drug requires monitoring via a visual assessment?

A

Vigabatrin

30
Q

Which four drugs can induce Hepatic CYP 450?

A
  1. Carbamazepine
  2. Phenytoin
  3. Phenobarbital
  4. Valproate
31
Q

You can have an ___________ of oral contraceptives if you are taking AEDs simultaneously.

What might this set you up for?

A

Increased Clearance

Unplanned Pregnancy

32
Q

AED inducers can increase the clearance of warfarin (anticoagulants). In this scenario, you will have elevated risk for ___________ .

A

Arterial/Venous Thrombosis

33
Q

AED inducers can increase clearance of HIV medications. In this scenario, you will have elevated risk for _______ .

A

HIV replication

34
Q

Valporic acid and lamotrigene are going to _______ glucuronosyltransferases (UGT) and ________ the conversion of drug to inactive drug-conjugate.

A

Inhibit

Decrease

35
Q

Carbamazepine, Phenytoin and Phenobarbital are going to _______ glucuronosyltransferases (UGT) and ________ the conversion of drug to inactive drug-conjugate.

A

Induce

Increase

*** You may have to increase the dose of medication when taking it in conjunction with UGT inducers!

36
Q

Differentiate between Carbamazepine and Oxcarbazepine.

A

Oxcarbazepine is less toxic!

The cross-sensitivity is ~30%

37
Q

Describe the procedure for treating Status Epilepticus in adult pts.

A

0-5 mins: Stabilize Pt and attempt IV access

5-20 mins: Administer a Benzodiazapine

20-40 mins: Administer Phenytoin

40-60 mins: Repeat Second-Line Treatment

38
Q

What are some of the broad warnings for AEDs?

A
  1. Abrupt withdraw may elicit Status Epilepticus

2. Suicidal Behavior and Ideation