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Flashcards in Sleep Wake 2 Deck (45):
1

What are the 3 "newer hypnotics?"

  • Zolpidem
  • Zaleplon
  • Eszopiclone

2

Do benzodiazepines or "newer hypnotics" bind more selectively?

Newer hypnotics

3

When taking "newer hypnotics," what drug can antagonize CNS depressant effects?

Flumazenil

4

What is a barbiturate that is not available in the US, is an adjunct to anesthesia (rapid / short acting) and is used as a truth serum?

Thiopental

5

Which drug?

  • Facilitates / prolongs inhibitory effects of GABA and glycine
  • Binds to receptor site different from benzodiazepines
  • Actions not antagonized by flumazenil
  • May also block excitatory transmitter glutamic acid & at high concentrations (sodium channels)

Barbiturates (tal)

6

3 uses for Barbiturates 

  • Anesthesia (thiopental)
  • Insomnia / Sedation (secobarbital)
  • Seizure disorders (phenobarbital)

7

Which drug?

  • Extension of CNS depressant actions
  • Tolerance
  • Dependence liability > benzodiazepine

Toxicities of Barbiturates

8

  • Which drug leads to coma/death?
  • Which drug leads to just medullary depression/anesthesia?

  • Barbiturates (coma)
  • Benzodiazepines (anesthesia)

9

______ & _____ induce liver enzymes causing drug interactions. 

  • Barbiturates
  • Carbamates

10

Barbiturates and carbamates induce liver enzymes causing drug interactions. 

  • Enzyme induction
  • Can precipitate acute intermittent _____ in susceptible patients
  • ___ ____ may displace coumarins from plasma protein binding sites and increase anticoagulant effects

  • porphyria
  • Chloral hydrate

11

Which drug?

  • exhibit sedating properties
  • effective in tx of mild insomnia & are generally safe
  • tolerance develops to sedative effects
  • increasing the dose will not produce linear increase in response
  • Disadvantage of ______ side effects
  • Histamine 1 receptor

Antihistamines

  • anticholinergic 

12

Antihistamines

  • Diphenhydramine & doxylamine are more sedating than ______. 

pyrilamine

13

Which drug?

  • Are effective for inducing "sleep continuity"
  • anticholinergic activity 
  • adrenergic blockade
  • cardiac conduction prolongation adverse effects

Antidepressants

  • amitriptyline
  • doxepin
  • nortriptyline

14

Low dose ____ has FDA approval for tx of sleep maintenance insomnia. 

Doxepin

(antidepressant)

15

What are the 2 sedating antidepressants?

  • ___ may promote sleep (cause daytime sedation/weight gain)
  • ____ at bedtime is sedating and can improve sleep continuity 

  • Mirtazapine
  • Trazodone

16

Which antidepressant should you prescribe for:

  • pts prone to substance abuse (dependence is NOT a problem)
  • pts w. selective serotonin reuptake inhibitor & buproprion-induced insomnia

Trazodone

17

Which drug's side effects?

  • Carryover sedation
  • alpha adrenergic blockage --> orthostasis can occur at any age, but is more dangerous in elderly
  • Priapism is a rare but serious side effect (prolonged erection)

Trazodone

18

Which antidepressant turns off wake signaling orexin (hypocretin)?

Suvorexant

19

What is the primary role of Orexin? 

control of sleep and arousal

20

Instead of inducing sleepiness, Suvorexant does what?

Turns off wake signaling

21

What are the 4 most commonly reported side effects of Suvorexant?

  • Somnolence (MC)
  • Sleep paralysis
  • Cataplexy
  • Narcolepsy-like sxs

22

  • What drug is approved for tx of sleep onset insomnia?
  • Selective MT1 & MT2 receptors
  • Regulates circadian rhythm & sleep onset

 

Remelteon (a melatonin receptor agonist)

23

Ramelteon is a melatonin receptor agonist 

  • forms _____ via CYP1A2
  • Generally well tolerated
  • What are the 3 MC adverse events?

  • active metabolite
  • HA, dizziness, somnolence 

24

Ramelteon (melatonin receptor agonist) effectively treats ____ in patients w/ which 2 conditions?

  • sleep onset difficulties
  • COPD & sleep apnea

25

Which drug?

  • herbal sleep remedy
  • studied for its sedative-hypnotic properties in pts w/ insomnia
  • MOA not fully understood
  • May involve increasing concentrations of _____. 

Valerian

  • GABA

26

Pts complain bc this drug smells like old gym socks

Valerian (herbal sleep remedy)

27

What 4 characteristic sxs differentiate narcolepsy from other sleep disorders?

(Narcolepsy tetrad)

  • Excessive daytime sleepiness
  • Cataplexy
  • Hallucinations
  • Sleep paralysis 

28

  • Impairment of both onset and offset of REM/NREM sleep
  • Arousals & disturbed sleep during the night

Excessive Daytime Sleepiness

(Part of Narcolepsy Tetrad)

29

  • Sudden bilateral loss of muscle tone varying severity / duration w/o loss of consciousness 
  • Often precipitated by highly emotional situations
  • Brief, lasting ___ to ____

Cataplexy

  • Seconds to several minutes

30

  • Falling asleep (hypnagogic) & on awakening (hypnopompic)
  • Brief, dream-like experiences that intrude wakefulness
  • 70% of narcoleptics experience this

Hallucinations 

(1 of 4 characteristics of Narcolepsy)

31

  • Episodic loss of voluntary muscle tone that occurs when the individual is falling asleep or waking
  • Conscious but not able to move or speak

Sleep paralysis

32

Narcolepsy is dysfunction of _____ system 

hypocretin / orexin neurotransmitter system

33

Vaccines licensed in US w/o adjuvants are or are not associated w/ increased risk of narcolepsy?

Are not

34

Wake Disorder Tx options include 

  • encouragement of good sleep hygiene and __ or more daytime naps daily (as little as 15 mins)
  • Pharmacotherapy focuses on ____ and ____ sleep abnormalities

  • 2
  • EDS (Excessive Daytime Sleepiness) & REM sleep

35

3 tx for EDS (Excessive Daytime Sleepiness)

"MAM"

  • Modafinil
  • Armodafinil
  • Methylphenidate

36

Tx for Cataplexy?

Tricyclic antidepressants (TCA)

SNRI, SSRI, MAOI

37

Tx for EDS, Cataplexy, Hallucinations

Sodium oxybate

38

What is the standard of tx for EDS?

Which other drug is FDA approved?

  • Modafinil
  • Armodafinil

39

4 SE of Modafinil

  • HA
  • nausea
  • Nervousness
  • Insomnia

40

Which 2 drugs?

  • Fast onset of effect
  • One has more risk of abuse/tolerance
  • SE: insomnia, HTN, palpitations, irritability

Amphetamines & Methylphenidate

(Amphetamines have more risk of abuse/tolerance)

41

Drug tx for what condition?

  • MOA: blockade of serotonin & norepinephrine reuptake in locus coeruleus & raphe and subsequent suppression of REM sleep
  • Tricyclic antidepressants
  • SNRI
  • SSRI
  •  

Cataplexy

42

What is the drug tx for Hypersomnolence and Cataplexy?

Selegiline 

(REM suppression & increase in REM latency)

43

44

Which drug?

  • Tx for EDS, sleep paralysis, cataplexy, & hypnagogic hallucinations
  • Potent sedative (hypnotic)
  • Should NOT be used concomitantly w/ any other sedating medications
  • Changes "sleep architecture" to resemble normal sleep

Sodium oxybate

45

5 SE of Sodium oxybate

(used to tx EDS, sleep paralysis, cataplexy, hypnagogic hallucinations)

  • Dizziness
  • Incontinence
  • Confusion
  • Somnolence
  • Nausea

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