S57 - Sleep Wake Disorders Flashcards

(32 cards)

1
Q

Classification of sleep disorders.

A

Difficulty in falling and staying asleep.
Disturbance in quality of sleep.
Excessive daytime sleepiness.

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2
Q

Primary insomnia is the most common for of dysomnias

A

true

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3
Q

Parasomnias are night terrors, sleep walking

A

true

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4
Q

NREM has four stages – 1,2,3 and 4 (< 45 min falling asleep).

A

Stage 1 – transition to sleep (0.5 – 7 min), low voltage EEG.
Stage 2 – sleep spindles 10-16 Hz EEG (50%).
Stage 3 and 4 – high amplitude, slow waves (20%).

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5
Q

REM – low voltage, mixed frequency.

A

First cycle 5-7 min., cycle lengthens to total time of 70-120 min. with 4-6 cycles/night. Dreams occur in the last part.

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6
Q

70-120 is sleep cycle that consist of Non-REM and REM

A

true

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7
Q

Sleep neurotransmitters invloved include:

Norepinephrine (NE) – locus ceruleus (LC) maintains normal sleep pattern, inc. activity dec. REM sleep.

Serotonin (5-HT) – sleep regulation. Dec. or DR destruction reduces sleep.

Dopamine (DA) has a alerting effect. Inc. DA wakefulness; dec. causes sleepiness.

A

true

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8
Q
NREM – five brain regions: 
dorsal raphe (DR), 
hypothalamus, 
basal forebrain, 
thalamus, 
medulla.
A

true

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9
Q

REM – cholinergic cells in the mesencephalic, medullary, and pons regions

A

true

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10
Q

Diagnostic criteria (DSM-5) – difficulty in falling asleep, maintaining sleep or nonrestorative sleep for at least three (3) months and 3 nights /week. Causes significant distress or impairment in function.

A

true

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11
Q

OTC treatment for primary insomnias

A

Antihistamines (diphenhydramine FDA approved)
melatonin
L-tryptophan
Valarein

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12
Q

L-tryptophan – agent alone removed by the FDA; caused 27 deaths to eosinophilia-myalgia.

A

true

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13
Q

Chloral Hydrate – oldest agent metabolized to trichloroethanol with a half-life = 8 hrs. REM/NREM are not markedly altered.

A

true

“Mickey fin”

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14
Q

Low-dose doxepin 3-6 mg FDA approved for insomnia maintenance.

A

true

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15
Q

Zolpidem (Ambien®) – selectively binds to the BZ-1 receptor producing minimal anxiolytic effects and no muscle relaxant and antiepileptic effects.

A

true

Use to help people FALL ASLEEP

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16
Q

Zolpidem (Ambien®)

CYP3A4 activity lower in women but this is one of the few drugs shown to have a PK difference

A

true

use lower doses in women

17
Q

Nonbenzodiazepines GABAA Agonists.
Zaleplon (Sonata®)
No tolerance, rebound insomnia or next day psychomotor activities

A

true

Use to help people FALL ASLEEP

18
Q

Treatment of insomnia
Eszopiclone (Lunesta®) – 1 mg, 2 mg and 3 mg tablets.
Dose < 2 mg for elderly patients.
FDA approved for up to 6 months.

A

true

Used to help people FALL ASLEEP and ALSO STAY ASLEEP

19
Q

Nonbenzodiazepines. – Ramelteon (Rozerem®).

Melatonin receptor agonist (M1 and M2) with one active metabolite (MII – has 1/10 and 1/5 potency).

20
Q

Nonbenzodiazepines. – Ramelteon (Rozerem®).

Do not take with food - increase AUC 31% and increase Cmax 22% with a delay of Tmax by 45 minutes.

21
Q

Nonbenzodiazepines. – Ramelteon (Rozerem®).

Drug interactions – fluvoxamine (increase 190 fold AUC, increase 70 fold Cmax)

22
Q

Benzodiazepines (BZ)
Reduce number of awakenings.
Increase total sleep time.
Increase stage 2 sleep, decreases durations of stages 1, 3 and 4.

23
Q

Benzodiazepines (BZ).

Anterograde amnesia

24
Q

Suvorexant (Belsomra®) – orexin receptor antagonist that decreases hyperarousal and improves sleep (C-IV).

A

true

FDA approval August 2014

25
Lemobrant (Dayvigo®)- FDA approved Dec. 2019. | Orexin receptor antagonist (OX1R, OX2R) used for sleep onset and maintenance.
true
26
Lemobrant (Dayvigo®)- FDA approved Dec. 2019. Drug interactions: “strong” or moderate CYP3A4 inhibitors inducers – avoid. Max. 5 mg dose with weak CYP3A4 inhibitors. PD EtOH interactions;  AUC drugs CYP2B6 substrates.
true
27
What is the typical length of one sleep cycle?
70-120 minutes
28
Does the pharmacokinetic profile of zolpidem differ between males and females?
YES… females need lower doses.
29
What are the pharmacologic class of agents used for insomnia?
GABA-A agonists, BDZs, M1/M2, OX1R/OX2R
30
GABA-A agonists,
Zolpidem (Ambien®) | Zaleplon (Sonata®)
31
M1/M2
Ramelteon (Rozerem®).
32
OX1R/OX2R
Suvorexant (Belsomra®) | Lemobrant (Dayvigo®)-