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Pharmacology 200 > 2- drugs for seizures > Flashcards

2- drugs for seizures Flashcards

1
Q

what happens in the brain/neurons during a seizure

A

high frequency dischange of a group of neurons

starts in one area, then spreads

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2
Q

what determines the symptoms of seizures

A

the site of primary discharge and the extent of the spread

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3
Q

what happens with high frequency discharge (Seizure) in the motor cortex

A

convulsions

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4
Q

what happens with high frequency discharge (Seizure) in the brain stem

A

loss of consciousness

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5
Q

what is epilepsy

A

a disorder characterized by seizures

many different types with different origins, symptoms and causes

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6
Q

what are tonic/clonic seizures

  • how long do they last
  • how affect consciousness
  • main features
A

obvious physical effects via muscle contraction followed by relaxation
severe
loss of consciousness
can last minutes

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7
Q

what are general absence seizures

  • how long do they last
  • how affect consciousness
A

affect consciousness, can be short (seconds)

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8
Q

what are partial seizures

  • how long do they last
  • how affect consciousness
  • main features
A

confined to specific regions with minimal spread, consciousness retained (may be altered), can last minutes

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9
Q

what does tonic mean

A

loss of consciousness and muscle rigidity

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10
Q

what does clonic mean

A

muscles rapidly relax and contract

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11
Q

is glutamate excitatory or inhbitory to AMPA receptors

A

excitatory

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12
Q

is glutamate excitatory or inhbitory to NMDA receptors

A

excitatory

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13
Q

is GABA excitatory or inhbitory to GABA-A receptors

A

inhibitory

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14
Q

which ion flows through when GABA binds to GABA-A

what does this cause

A

Cl

hyperpolarization

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15
Q

which ions flow through when GLU binds to NDMA or AMPA

what does this cause

A

Na+, Ca++, K+

depolarization

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16
Q

what are the 4 targets for pharmacological intervention in seizures

A
  1. increase inhibitory influences (increase effects of GABA
  2. inhibit AP (voltage-gated Na influx)
  3. decrease spread of neuronal discharge (block low-voltage activated Ca channels)
  4. decrease excitatory influences (decrease glu LGIC receptor activity)
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17
Q

what are the common side effects of anti seixure drugs

A

sedation

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18
Q

what does GABA-T (GABA-transaminase) do

A

metabolizes free GABA in the nerve endings and astrocytes

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19
Q

what happens when you inhibit GABA-T

A

there will be more presynaptic GABA so that more can be released in depolarization events

20
Q

what is Vigabatrin

what kind of seizures is it good for

A

partial seizures

21
Q

how does Vigabatrin work

A

irreversible inhibitor of GABA-T

it may also inhibit GABA transporter

22
Q

how does Tiagabine work

A

inhibits GAT

allows more GABA to accumulate in synapse

23
Q

what does GAT do

A

transporter that removes GABA from the synaptic cleft

24
Q

which drug helps with fibromyalgia and anxiety

A

tiagabine

25
Q

what is use dependent block

A

when drugs preferentially bind to channels that have been open
more firing, more block produced

26
Q

why does use-dependent block work best at high rates

A

there isnt enough time between firing events for the drug to leave the channel

27
Q

why is use dependent block okay for normal function

A

because at normal firing rates, the drug leaves the site before the next potential is initiated

28
Q

what kind of drug is carbamazepine

A

use dependent voltage-gated-sodium-channel blocker

29
Q

side effects of carbamazepine

A

severe motor/mental disturbances, hyponatremia (dilution of Na in blood)
bone marrow depletion for Asians
speeds up its own metabolism

30
Q

which drug is great for partial seizures

A

vigabtrin

also tiagabine and carbamazepine

31
Q

which drug is good for most forms of epilepsy but not absence serizures

A

carbamazepine

32
Q

which drug is “add-on” therapy for partial seizures

A

tiagabine

33
Q

what do T-type low voltage activated calcium channels do in the brain

A

play a central role in depolarizing neurons and creating AP in the brain`

34
Q

what does ethosuximide do

A

blocks T-type calcium channels and prevents abnormal pattern of firing

35
Q

what kind of seizures is treatable with ethosuximide

A

absense serizures

36
Q

what makes absence seizures so different

A

there is a specific pattern of abnormal thalamocortical discharge (3Hz)
this normally happens in non-REM sleep, but it happens in absence seizures

37
Q

what is common about AMPA and NMDA receptors

A

they are both excited by glutamate

38
Q

what is the role of AMPA and NMDA in seizures

A

they play a central role in foci of seizures and spreading excitation to surrounding neurons

39
Q

what is peramphanel

A

allosteric AMPA receptor inhibitor

40
Q

how selective is peramphanel towards AMPA

A

very

41
Q

how selective is peramphanel towards NMDA

A

none

42
Q

what types of seizures is perampanel good for

A

many types except for absense

43
Q

half life of perampanel

A

long, like 110hours

44
Q

side effects of perampanel

A

aggression, hostility and violence

45
Q

what aggrevates perampanel side effects

A

more in adolescents and alcoholics, also dose-dependent

Pharmacology 200 (29 decks)

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