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Pharmacology III > Sleep > Flashcards

Sleep Flashcards

1
Q

What is a disorder characterized by complaints of difficulty falling asleep, difficulty staying asleep or experiencing non-restorative sleep?

A

Insomnia

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2
Q

What is non-REM sleep?

A

Quiet sleep

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3
Q

What is REM sleep?

A

Hyperactive brain in paralyzed body

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4
Q

What are the stages of non-REM “Quiet Sleep”?

A

Stage 1- light sleep
Stage 2 “true sleep”
Stage 3- deep sleep
Stage 4- Very deep sleep

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5
Q

What are the stages of REM “hyperactive brain in paralyed”?

A

Stage 5; dreams

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6
Q

How does sleep change for teenagers?

A

Known for daytime drowsiness

Most teenagers need an hour more sleep than children; however most get an hour LESS

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7
Q

How does sleep change for adults?

A

Between 20-30 years, amount of deep sleep drops and nighttime awakeness doubles
By age 40, later stages of sleep begin to diminish

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8
Q

How does sleep change for the elderly?

A

Deep sleep accounts for ~5% of sleep

Falling asleep takes longer

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9
Q

What is acute insomnia?

A
  • Several days up to 4 weeks

- Results from acute stress of changes in the environment

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10
Q

What are common precipitating conditions for acute insomnia?

A

Unfamiliar / uncomfortable sleep environment
Medical Illness
Shift work
Jet lag
Caffeine, EtOH, nicotine, or ADR’s
Life stressors (moving, divorce, marriage, bereavement, holidays ect.)

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11
Q

What is chronic insomnia?

A
  • Greater than 4 weeks duration (physical/emotional illness, RLS, sleep apnea)
  • Maybe be caused by medications, EtOH, or illicit drugs
  • Substance abuse-10%
  • Conditioned anxiety
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12
Q

What are the risk factors for insomnia?

A
  • Women, elderly, stressful lives
  • Lower socioeconomic or educational background
  • Separated, widowed, unemployed
  • Previous episodes of insomnia
  • Psychiatric/ mental conditions
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13
Q

Who is the largest group of the growing community with sleep disorders?

A

College students

Sunday=insomnia night; Wednesday- most efficient day of the week for sleeping

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14
Q

What is the diagnosis for primary sleep disorders based on?

A

–> 2 of the following for at least 1 month
Difficulty initiating sleep
Difficulty maintaining sleep
Poor sleep efficiency
Sleep disturbances on > 3 nights/week
Significant impairment in social, occupational, or other areas of functioning
–Social History-EtOH, caffeine, illicit drugs, marital status, living arrangement
–Review of Systems- Weight gain, angina, wheezing, nocturia, dyspnea, leg cramps
–Polysomnography- Used to assess and record variables that characterize sleep and aid in diagnosis of sleep disorders
Only if other sleep disorders are suspected
–Pharmacologically induced insomnia

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15
Q

What is insomnia that occurs following the discontinuation of sedative substances?

A

Rebound insomnia

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16
Q

What drugs are offenders of rebound insomnia?

A

Insomnia can be a symptom of withdrawal when “rebounding” from effects of sedative
EtOH, antihistamines, BZD’s, older hypnotics (chloral hydrate)
Antidepressants
TCA’s, MAOI’s, SSRI’s
Abused substances
Opiates, Marijuana, Cocaine

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17
Q

What are the screening questions for insomnia?

A 
REST
Restorative sleep?
Excessive daytime sleepiness, tiredness or fatigue 
Snoring nightly?
Total sleep time?
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18
Q

What is the treatment goal of insomnia?

A

Normalize sleep patterns as quickly as possible.

Fast onset of sleep, decrease night-time awakenings, improve day-time quality of life.

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19
Q

What are the non-pharmacologic treatment options?

A
  • Cognitive therapy: Stimulus control, sleep hygiene, sleep restriction, CBT
  • Behavioral or supportive therapy- relaxation techniques
  • Sleep diary
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20
Q

What is sleep hygiene treatment?

A 
Avoid exercise to close to bed
Sleep in a comfortable environment
Avoid alcohol and stimulants
Avoid caffeine and nicotine for at least 6 hours prior to bedtime
Avoid going to bed excessively hungry
Spend time prior to bedtime relaxing
Establish a regular sleep schedule
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21
Q

What is stimulus control treatment?

A

Go to bed only if you feel sleepy
Avoid activities in your bedroom that keep you awake, other than sex
Sleep only in your bedroom
Leave the bedroom when awake, return only when sleepy
Arise at the same time each morning regardless of amount of sleep obtained
Avoid daytime napping

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22
Q

What are the pharmacologic treatment options for insomnia?

A

Antihistamines- (First go to because they are available OTC advertising help with sleep)
Sedative hypnotics
Antidepressants- TCA’s, Trazadone, Mirtazapine
Herbal products

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23
Q

What are the antihistamines used to treat insomnia?

A
  • Diphenhydramine [Benadryl]
  • Hydroxyzine [Atarax]
  • Doxylamine [Unisom]
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24
Q

Antihistamines (Diphenhydramine, hydroxyzine, doxylamine)- Indications

A

Insomnia, Anxiety, allergy

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25
Q

Antihistamines (Diphenhydramine, hydroxyzine, doxylamine)- MOA

A

Suppress REM sleep, may produce rebound upon withdrawl

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26
Q

Antihistamines (Diphenhydramine, hydroxyzine, doxylamine)- ADRs

A 
Anticholinergic effects (problamatic esp. in elderly)
Dizziness, confusion, next day sedation
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27
Q

What are the z-hypnotics?

A

Zolpidem (Ambien, Ambien CR)
Zaleplon (Sonata)
Eszopiclone

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28
Q

Z-hypnotics (Zolpidem, Zaleplon, Eszopiclone)- MOA

A

Newer therapies for insomnia

Selective for BZ-1 receptor of GABAa receptor (receptors important for depression throughout the brain)

29
Q

Zolpidem (Ambien and ambien CR)- Indications

A

Z-hypnotics
Used only as a hypnotic (only indication for this)
Should only be used short-term 7-10 days

30
Q

Zolpidem (Ambien and ambien CR)- Advantages

A

No withdrawal
Minimal rebound insomnia
Little or no tolerance
Immediate-release and extended release formulas

31
Q

Zolpidem (Ambien and ambien CR)- ADRs

A

GI upset- biggest ones

Agitation, HA, nightmares, dizziness, daytime drowsiness (biggest ones)

32
Q

Zolpidem (Ambien and ambien CR)- Drug interactions

A

P450 metabolism

Rifampin shortens t1/2

33
Q

Zaleplon (Sonata®)- indications

A

Z-hypnotics
Similar to Ambien in hypnotic actions
Ideal agent for sleep latency

34
Q

Zaleplon (Sonata®)- pharmacokinetics

A

Fewer residual effects on psychomotor and cognitive functions rapidly eliminated with t1/2 <1hr
CYP3A4 metabolism

35
Q

Zaleplon (Sonata®)- ADRs

A

ADR: HA, nausea, dyspepsia

36
Q

Eszopiclone (Lunesta®)- indications

A

Z-hypnotics

Proven to fall asleep quickly, maintain sleep through the night

37
Q

Eszopiclone (Lunesta®)- ADRs

A

Side effects include anxiety, dry mouth, chest pain, HA, migraine, peripheral edema, somnolence, unpleasant taste

38
Q

Eszopiclone (Lunesta®)- Advantages

A

Low abuse potential
No tolerance for up to 12 months
No withdrawal
Rarely associated with behavior changes ie., agitation, confusion, depression, suicidal thoughts, memory loss

39
Q

Ramelteon (Rozerem)- MOA

A

Z-hypnotics
Melatonin receptor agonist
More potent at MT1 and MT2 than MT3
No appreciable activity at GABA receptor

40
Q

Ramelteon (Rozerem)- indications

A

Indicated for use in treatment of insomnia characterized by difficulty with sleep onset
Approved for chronic use
Not a controlled substance

41
Q

Ramelteon (Rozerem)- Precautions and Warnings

A

Precautions
Do not give in conjunction with or shortly after high fat meals
Warnings
Use with caution in patients with moderate hepatic impairment
Do not use with severe hepatic impariment

42
Q

Ramelteon (Rozerem)- ADRs

A

Somnolence, FATIGUE, DIZZINESS nausea, myalgia

43
Q

Benzodiazepines- Indications

A

Not all good hypnotics
Balance sedative effect at bedtime with residual sedation on awakening
Flurazepam- not FDA approved for this indication
Reduces sleep-induction and number of awakenings
Increases duration of sleep

44
Q

Benzodiazepines- MOA

A

Effective up to 4 weeks

T1/2 85hr…daytime sedation and accumulation of drug

45
Q

What are the benzodiazepines?

A

Flurazepam
Temazepam
Triazolam

46
Q

Temazepam

A

Doesn’t help fall asleep real fast unless you take it 2-3 hours before sleeping
Reduces number of awakenings
Peak sedative effect 2-3 hours after oral dose

47
Q

Triazolam

A

Induces sleep
Tolerance develops with days
Withdrawal of drug results in rebound insomnia

48
Q

What are the antidepressants used for insomnia?

A

5HT2 blockers- Nefazodone, Mirtazapine, Trazodone

TCAs

49
Q

5HT2 (Serotonin) blockers (Nefazodone, Mirtazapine, Trazodone)- Indications

A

Best documented if used for restoring sleep in SSRI- induced insomnia
Increase sleep continuity and time

50
Q

5HT2 (Serotonin) blockers (Nefazodone, Mirtazapine, Trazodone)- ADRs

A

Nausea, xerostomia, constipation, drowsiness, HA, rebound insomnia, priapism

51
Q

What are the TCAs that are used as antidepressants?

A

Doxepin and Amtriptyline

52
Q

TCAs (Doxepin and Amtriptyline)- Indication

A

Not FDA indicated for insomnia

Efficacy in insomnia has not been proven except for specific diagnoses: Anxiety and Depressive Disorders

53
Q

TCAs (Doxepin and Amtriptyline)- ADRs

A

Increase with dosage; orthostatic hypotension, dizziness, sedation, xerostomia, blurred vision, constipation, urinary hesitancy

54
Q

What are the natural products used for insomnia?

A

Melatonin

Valarian Root

55
Q

Melatonin- Indications

A

Hormone released by pineal gland to regulate circadian rhythm
Potential effectiveness: Jet lag, shift work, elderly

56
Q

Melatonin- ADRs

A

Abdominal cramps (big one), HA, irritability

57
Q

Valarian Root- Indications

A 
Increases GABA (Depressive transmitter) in synaptic cleft
Mild hypnotic, improves sleep latency and quality of sleep
58
Q

Valarian root- ADRs

A

Severe HA

59
Q

What is a condition during sleep in which respiration ceases for relatively brief periods of time?

A

Sleep Apnea

60
Q

What is involved in sleep apnea to help the diagnosis?

A 
> 2 or more of the following:
Choking or gasping sleep
Recurrent awakenings from sleep
Non-restorative Sleep
Daytime fatigue
Impaired concentration
61
Q

What is diagnostic of sleep apnea?

A

Overnight monitoring demonstrating > 5 obstructed breathing events / hour during sleep

62
Q

What are the risk factors for sleep apnea?

A

Males, age (as you get older), obesity (central), craniofacial abnormalities

63
Q

What is the non-pharmacologic treatment of sleep apnea?

A

Weight loss, positional change, continuous positive airway pressure (CPAP)

64
Q

What is the pharmacologic treatment of sleep apnea?

A

Modafinil (C-IV)

Approved for treatment of residual daytime sleepiness despite traditional approaches (eg CPAP)

65
Q

What is the standard of therapy for sleep apnea (first choice)?

A

CPAP

66
Q

What is a creepy, crawly sensation in the legs at rest, relieved by movement that is worse in the evening and at night?

A

Restless leg syndrome

67
Q

What is repetitive, rhythmic limb movement in series that lasts minutes, with movements occurring every 20-40seconds?

A

Periodic limb movement disorder

68
Q

What is the pharmacologic treatment of restless leg syndrome and PLMD?

A

Ropinirole, Pramipexole

Off label therapy for these meds. These are dopamine drugs also used in parkinsons

Pharmacology III (19 decks)

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