Insomnia drugs [3] Flashcards

1
Q

Admin of which drug is most likely to produce memory disturbances such as anterograde amnesia?
(aka which one enhances GABA fxn?)

A

BDZ: Diazepam (anxiolytic)
Glutamate is active when forming memory
Enhancing GABA indirectly reduces Glu

(note: a1 enhance sleep, a2-5 lessens anxiety)

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2
Q

Phenelzine

A

MAOI

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3
Q

Monoaminergic cell groups activate cerebral cortex to facilitate PROCESSING of these thalamic inputs:

List the NT these red pathways secrete

  • Locus ceruleus
  • Raphe
  • Tuberomamillary
  • VTA
  • Basal forebrain
A
  • Locus ceruleus: NE
  • Raphe: 5HT
  • Tuberomamillary: His
  • VTA: DA
  • Basal forebrain: ACh
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4
Q

GABA is (select one) Off/ON when you are awake. _____ Enhances GABA and promote sleep.

A

OFF
BDZ
(GABA released from anterior hypothalamus

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5
Q

High ACh, 5HT, and GABA help you go towards (pick one) wakefulness/sleep

A

sleep

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6
Q

Z drugs are good at preserving which part of your sleep?

A

REM (20-25% of your sleep, stage of recall-able dreams)

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7
Q

Which stage of sleep predominates?

A
Stage 2 (50%)
- ligh sleep, EEG slower
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8
Q

BDZ for sleep

A

Triazolam
Temazepam
Flurazepam

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9
Q

Z drugs for sleep

A

zolpidem (closest to ideal)
zaleplon
eszopiclone

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10
Q

BDZ effects of stages of sleep

  • Sleep latency
  • Duration
  • 1
  • 2
  • 3
  • 4
  • REM
A
  • Sleep latency: ↓
  • Duration: ↑
  • 1: ↑
  • 2: ↑
  • 3: ↓
  • 4: ↓
  • REM: ↓

sleep faster + stay asleep
*note (latency, duration, 1 are like Z drugs)

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11
Q

Z drugs effects of stages of sleep

  • Sleep latency
  • Duration
  • 1
  • 2
  • 3
  • 4
  • REM
A
  • Sleep latency: ↓
  • Duration: ↑
  • 1: ↑
  • 2: ↑
  • 3: no effect
  • 4: no effect
  • REM: no effect

sleep faster + stay asleep

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12
Q

diff btwn a1 and a2-5 location effects

A

a1: cortex
- sleep
- anticonvulsant

a2-5: limbic system + brain stem

  • anxiolytic
  • myorelaxant
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13
Q

Diff btwn Z drugs and BDZ (triazolam)

for: hypnotic, anticonvulsant, myorelaxant
- quantal vs graded

A

Z drug:
quantal response: bam you asleep (immediate release)
upping the dose → see anticonvulsant and myorelaxant effects

BDZ:
Graded (gradual)
intially see anticonvulsant and myorelaxant → up the dose and get hypnotic effect
(feel relax b4 sleep unlike Z drug)

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14
Q

Why wont Tamazepam be impaired as you get older?

A

goes out phase II

metab not affected by age

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15
Q

Hangover effect is least likely seen in drugs with long or short half lives?

A

short

hangover effect is seen in drugs with long half lives

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16
Q

Which of the Z drugs:

  • have the longest half life?
  • reduces nocturnal awakenings?
  • best for middle of the night awakenings?
  • is best for sleep maintanence
A

Eszopiclone

Zolpidem

Zaleplon (short half life)

Eszopiclone (long half life)

17
Q

Do BDZ or Z drugs cause anterograde amnesia?

Which has high therapeutic index relative to barbs?

A

Both (a1)

Both

18
Q

Trazodone

  • MOA
  • ADRs
  • clinical use
A

Mixed Serotonin receptor antagonist and reuptake blocker

Oversedation, orthostasis (a1), Priapism

*an antidepressant

19
Q

Ramelteon

  • MOA
  • ADRs
  • clinical use
A

Melatonin receptor agonist

dizziness, somnolence, fatigue, nausea

*sedative

20
Q

Diphenhydramine (benadryl)

  • MOA
  • clinical use
A

H1 and muscarinic R antagonist

sedative, hypnotic, anxiolytic
have to get into the brain to cause sleepiness - 1st gen

21
Q

Quetiapine effects on sleep

A

(atypical antipsychotic agent)
D2 antagonist
- leave Extrapyramidal side effects alone better than typical
- improve DA release in mesocortical pathway- control negative symp

Can be used as an adjunctive (just like melatonin and diphenhydramine)

22
Q

which agents used in tx of insomnia are likely to cause anticholinergic side effects?

A

1st gen antihistamines
(block muscarinic receptors as well as H1)
- Diphenhydramine
- Doxylamine