Sleep Wake 2

Question 1

What are the 3 “newer hypnotics?”

Answer 1

• Zolpidem
• Zaleplon
• Eszopiclone

Question 2

Do benzodiazepines or “newer hypnotics” bind more selectively?

Answer 2

Newer hypnotics

Question 3

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

Answer 3

Flumazenil

Question 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?

Answer 4

Thiopental

Question 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)

Answer 5

Barbiturates (tal)

Question 6

3 uses for Barbiturates

Answer 6

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

Question 7

Which drug?

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

Answer 7

Toxicities of Barbiturates

Question 8

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

Answer 8

• Barbiturates (coma)
• Benzodiazepines (anesthesia)

Question 9

______ & _____ induce liver enzymes causing drug interactions.

Answer 9

• Barbiturates
• Carbamates

Question 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

Answer 10

• porphyria
• Chloral hydrate

Question 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

Answer 11

Antihistamines

• anticholinergic

Question 12

Antihistamines

• Diphenhydramine & doxylamine are more sedating than ______.

Answer 12

pyrilamine

Question 13

Which drug?

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

Answer 13

Antidepressants

• amitriptyline
• doxepin
• nortriptyline

Question 14

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

Answer 14

Doxepin

(antidepressant)

Question 15

What are the 2 sedating antidepressants?

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

Answer 15

• Mirtazapine
• Trazodone

Question 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

Answer 16

Trazodone

Question 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)

Answer 17

Trazodone

Question 18

Which antidepressant turns off wake signaling orexin (hypocretin)?

Answer 18

Suvorexant

Question 19

What is the primary role of Orexin?

Answer 19

control of sleep and arousal

Question 20

Instead of inducing sleepiness, Suvorexant does what?

Answer 20

Turns off wake signaling

Question 21

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

Answer 21

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

Question 22

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

Answer 22

Remelteon (a melatonin receptor agonist)

Question 23

Ramelteon is a melatonin receptor agonist

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

Answer 23

• active metabolite
• HA, dizziness, somnolence

Question 24

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

Answer 24

• sleep onset difficulties
• COPD & sleep apnea

Question 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 \_\_\_\_\_.

Answer 25

**Valerian** * GABA

Question 26

Pts complain bc this drug smells like old gym socks

Answer 26

Valerian (herbal sleep remedy)

Question 27

What 4 characteristic sxs differentiate narcolepsy from other sleep disorders? ## Footnote **(Narcolepsy tetrad)**

Answer 27

* Excessive daytime sleepiness * Cataplexy * Hallucinations * Sleep paralysis

Question 28

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

Answer 28

**Excessive Daytime Sleepiness** | (Part of Narcolepsy Tetrad)

Question 29

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

Answer 29

**Cataplexy** * Seconds to several minutes

Question 30

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

Answer 30

**Hallucinations** | (1 of 4 characteristics of Narcolepsy)

Question 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

Answer 31

Sleep paralysis

Question 32

Narcolepsy is dysfunction of _____ system

Answer 32

hypocretin / orexin neurotransmitter system

Question 33

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

Answer 33

Are not

Question 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

Answer 34

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

Question 35

3 tx for EDS (Excessive Daytime Sleepiness) "MAM"

Answer 35

* Modafinil * Armodafinil * Methylphenidate

Question 36

Tx for Cataplexy?

Answer 36

**Tricyclic antidepressants** (TCA) SNRI, SSRI, MAOI

Question 37

Tx for EDS, Cataplexy, Hallucinations

Answer 37

Sodium oxybate

Question 38

What is the standard of tx for EDS? Which other drug is FDA approved?

Answer 38

* Modafinil * Armodafinil

Question 39

4 SE of Modafinil

Answer 39

* HA * nausea * Nervousness * Insomnia

Question 40

**Which 2 drugs?** * Fast onset of effect * One has more risk of abuse/tolerance * SE: insomnia, HTN, palpitations, irritability

Answer 40

**Amphetamines & Methylphenidate** (Amphetamines have more risk of abuse/tolerance)

Question 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 *

Answer 41

Cataplexy

Question 42

What is the drug tx for Hypersomnolence and Cataplexy?

Answer 42

**Selegiline** (REM suppression & increase in REM latency)

Question 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

Answer 44

Sodium oxybate

Question 45

**5 SE of Sodium oxybate** (used to tx EDS, sleep paralysis, cataplexy, hypnagogic hallucinations)

Answer 45

* Dizziness * Incontinence * Confusion * Somnolence * Nausea ## Footnote **(DICS Now)**