Pharmacology - Anticonvulsants (Exam 2) Flashcards

1
Q

Brief, temporary disturbance in electrical activity of the brain; a single episode of jerky movements

A

Seizure (convulsion)

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2
Q

Recurring seizures; group of disorders characterized by abnormal electrical discharge from CNS neurons in the form of imbalance between excitatory and inhibitory impulses

A

Epilepsy

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3
Q

Excitatory receptors

A

NMDA
AMPA

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4
Q

Excitatory neurotransmitters

A

Glutamate
Aspartate

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5
Q

Inhibitory receptor

A

GABA-R

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6
Q

Inhibitory neurotransmitter

A

GABA

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7
Q

Benzodiazepines cause increased _______, leading to ______ __________ and ________

A

inhibition; CNS depression and sedation

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8
Q

If you have too much __________ signals or too little ________ signals, you can have __________

A

excitatory; inhibitory; epilepsy

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9
Q

Petit mal

A

Absence seizures

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10
Q

Seizures that cause you to lose focus, blink rapidly, or stare out into space for a few seconds

A

Absence seizures

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11
Q

Grand mal

A

Tonic-clonic seizures

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12
Q

Seizures that cause you to cry out, fall to the ground, or experience strong muscle jerking or contractions

A

Tonic-clonic seizures

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13
Q

What are the 2 generalized seizures?

A
  1. Absence seizures
  2. Tonic-clonic seizures
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14
Q

What are the 3 focal (partial) seizures?

A
  1. Simple
  2. Complex
  3. Secondary generalized
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15
Q

Seizures that affect a small part of the brain and can have minimal symptoms like a small twitch or strange taste in your mouth

A

Simple focal seizure

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16
Q

Seizures that involve multiple areas of the brain and cause confusion; disoriented or unable to respond for a few seconds to minutes

A

Complex focal seizure

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17
Q

Seizures that begin as focal seizure in one part of the brain and progress to a generalized seizure

A

Secondary generalized seizure

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18
Q

Seizures that are very prolonged and cause brain damage or death; EMS must be called

A

Status epilepticus

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19
Q

How do anti-seizure drugs work?

A

Reduce excitatory signals
Enhance inhibitory signals

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20
Q

How do you reduce excitatory signals?

A

Inhibit glutamate/aspartate release

Inhibit NMDA/AMPA signaling

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21
Q

How do you enhance inhibitory signals?

A

Block GABA reuptake

Enhance GABA-R signaling

22
Q

How to block action potential

A
  1. Enhance Cl- channels
  2. Block Na+ channel
  3. Enhance K+ channel
23
Q

What drug is a barbiturate? What is it used to treat?

A

Phenobarbital; treats seizures

24
Q

How does phenobarbital work?

A

Enhance binding of GABA

Increase the time that GABA-A activated Cl- channels are open

25
Q

What is an adverse effect of barbiturates?

A

Osteomalacia

26
Q

What drugs are hydantoins?

A

Phenytoin
Dilantin

27
Q

How do phenytoin, dilantin, and carbamazepine work?

A

Reversible binding to inactivated Na+ channels
Stabilize Na+ channels in inactivated state

28
Q

What factors can alter phenytoin protein binding? What do all of these factors cause?

A

Hypoalbuminemia
Renal disease
Presence of displacing drugs (ex: aspirin)

Causes increased unbound (“free”) drug

29
Q

What are the adverse effects of hydantoins?

A

Fetal hydantoin syndrome (cleft lip, cleft palate, congenital heart disease, neural tube defect)

Osteomalacia (interferes with Ca2+ absorption)

30
Q

Which drug causes gingival overgrowth?

A

Phenytoin

31
Q

What drug is the 1st choice for absence seizures?

A

Ethosuximide

32
Q

What is the mechanism for ethosuximide?

A

Reduce Ca2+ influx through T type Ca2+ channels

33
Q

What is the mechanism for valproic acid?

A

Binds to inactivated Na+ channels
Reduces Ca2+ influx through T type Ca2+ channels
Enhances GABA activity

34
Q

What can valproic acid cause?

A

Spina bifida and neural tube defects

35
Q

What are the 3 things GABA drugs do?

A
  1. Increase GABA-R activation
  2. Inhibit GABA transaminase
  3. Inhibit GABA transporter-1
36
Q

What drugs are benzodiazepines?

A

Diazepam
Midazolam

37
Q

What is the mechanism for diazepam and midazolam? What do they treat in emergencies?

A

Increase GABA-R activation

Treat status epilepticus

38
Q

What drug is a neurosteroid?

A

Ganaxolone

39
Q

What is the mechanism for ganaxolone?

A

Steroid binding site (allosteric site) on GABA-R

40
Q

What is the mechanism of vigabatrin?

A

Inhibits GABA transaminase

(vigabaTRin - TRansaminase)

41
Q

What is the mechanism for tiagabine?

A

Inhibits GABA transporter-1

(Tiagabine - Transporter)

42
Q

What is the mechanism for gabapentin?

A

Inhibits L-type Ca2+ channels

43
Q

What is the mechanism for lamotrigine?

A

Binds to inactivated Na+ channels

44
Q

What is the mechanism for levetiracetam?

A

Synaptic vesicle glycoprotein inhibition - modulates glutamate release

45
Q

Which drugs are the GABA acting drugs (gabanoids)?

A

Vigabatrine
Tigabine
Ganaxolone
Gabapentin

46
Q

What is the main aim for anti-epileptic drugs?

A

Control seizures with least # of drugs

47
Q

T/F you should never stop treatment with anti-epileptic drugs suddenly

A

True, stopping suddenly could cause status epilepticus

48
Q

What should you do if a patient has a seizure in your office?

A

Inject midazolam intra buccal, IV, IM

49
Q

Repeated or continuous seizures for > 5 minutes or no return to baseline

A

Status epilepticus (emergency!)

50
Q

Which drugs can treat status epilepticus?

A

Benzodiazepines:
Diazepam
Midazolam