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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
Antihistamines (Diphenhydramine, hydroxyzine, doxylamine)- MOA
Suppress REM sleep, may produce rebound upon withdrawl
26
Antihistamines (Diphenhydramine, hydroxyzine, doxylamine)- ADRs
``` Anticholinergic effects (problamatic esp. in elderly) Dizziness, confusion, next day sedation ```
27
What are the z-hypnotics?
Zolpidem (Ambien, Ambien CR) Zaleplon (Sonata) Eszopiclone
28
Z-hypnotics (Zolpidem, Zaleplon, Eszopiclone)- MOA
Newer therapies for insomnia | Selective for BZ-1 receptor of GABAa receptor (receptors important for depression throughout the brain)
29
Zolpidem (Ambien and ambien CR)- Indications
Z-hypnotics Used only as a hypnotic (only indication for this) Should only be used short-term 7-10 days
30
Zolpidem (Ambien and ambien CR)- Advantages
No withdrawal Minimal rebound insomnia Little or no tolerance Immediate-release and extended release formulas
31
Zolpidem (Ambien and ambien CR)- ADRs
GI upset- biggest ones | Agitation, HA, nightmares, dizziness, daytime drowsiness (biggest ones)
32
Zolpidem (Ambien and ambien CR)- Drug interactions
P450 metabolism | Rifampin shortens t1/2
33
Zaleplon (Sonata®)- indications
Z-hypnotics Similar to Ambien in hypnotic actions Ideal agent for sleep latency
34
Zaleplon (Sonata®)- pharmacokinetics
Fewer residual effects on psychomotor and cognitive functions rapidly eliminated with t1/2 <1hr CYP3A4 metabolism
35
Zaleplon (Sonata®)- ADRs
ADR: HA, nausea, dyspepsia
36
Eszopiclone (Lunesta®)- indications
Z-hypnotics | Proven to fall asleep quickly, maintain sleep through the night
37
Eszopiclone (Lunesta®)- ADRs
Side effects include anxiety, dry mouth, chest pain, HA, migraine, peripheral edema, somnolence, unpleasant taste
38
Eszopiclone (Lunesta®)- Advantages
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
Ramelteon (Rozerem)- MOA
Z-hypnotics Melatonin receptor agonist More potent at MT1 and MT2 than MT3 No appreciable activity at GABA receptor
40
Ramelteon (Rozerem)- indications
Indicated for use in treatment of insomnia characterized by difficulty with sleep onset Approved for chronic use Not a controlled substance
41
Ramelteon (Rozerem)- Precautions and Warnings
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
Ramelteon (Rozerem)- ADRs
Somnolence, FATIGUE, DIZZINESS nausea, myalgia
43
Benzodiazepines- Indications
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
Benzodiazepines- MOA
Effective up to 4 weeks | T1/2 85hr…daytime sedation and accumulation of drug
45
What are the benzodiazepines?
Flurazepam Temazepam Triazolam
46
Temazepam
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
Triazolam
Induces sleep Tolerance develops with days Withdrawal of drug results in rebound insomnia
48
What are the antidepressants used for insomnia?
5HT2 blockers- Nefazodone, Mirtazapine, Trazodone | TCAs
49
5HT2 (Serotonin) blockers (Nefazodone, Mirtazapine, Trazodone)- Indications
Best documented if used for restoring sleep in SSRI- induced insomnia Increase sleep continuity and time
50
5HT2 (Serotonin) blockers (Nefazodone, Mirtazapine, Trazodone)- ADRs
Nausea, xerostomia, constipation, drowsiness, HA, rebound insomnia, priapism
51
What are the TCAs that are used as antidepressants?
Doxepin and Amtriptyline
52
TCAs (Doxepin and Amtriptyline)- Indication
Not FDA indicated for insomnia | Efficacy in insomnia has not been proven except for specific diagnoses: Anxiety and Depressive Disorders
53
TCAs (Doxepin and Amtriptyline)- ADRs
Increase with dosage; orthostatic hypotension, dizziness, sedation, xerostomia, blurred vision, constipation, urinary hesitancy
54
What are the natural products used for insomnia?
Melatonin | Valarian Root
55
Melatonin- Indications
Hormone released by pineal gland to regulate circadian rhythm Potential effectiveness: Jet lag, shift work, elderly
56
Melatonin- ADRs
Abdominal cramps (big one), HA, irritability
57
Valarian Root- Indications
``` Increases GABA (Depressive transmitter) in synaptic cleft Mild hypnotic, improves sleep latency and quality of sleep ```
58
Valarian root- ADRs
Severe HA
59
What is a condition during sleep in which respiration ceases for relatively brief periods of time?
Sleep Apnea
60
What is involved in sleep apnea to help the diagnosis?
``` > 2 or more of the following: Choking or gasping sleep Recurrent awakenings from sleep Non-restorative Sleep Daytime fatigue Impaired concentration ```
61
What is diagnostic of sleep apnea?
Overnight monitoring demonstrating > 5 obstructed breathing events / hour during sleep
62
What are the risk factors for sleep apnea?
Males, age (as you get older), obesity (central), craniofacial abnormalities
63
What is the non-pharmacologic treatment of sleep apnea?
Weight loss, positional change, continuous positive airway pressure (CPAP)
64
What is the pharmacologic treatment of sleep apnea?
Modafinil (C-IV) | Approved for treatment of residual daytime sleepiness despite traditional approaches (eg CPAP)
65
What is the standard of therapy for sleep apnea (first choice)?
CPAP
66
What is a creepy, crawly sensation in the legs at rest, relieved by movement that is worse in the evening and at night?
Restless leg syndrome
67
What is repetitive, rhythmic limb movement in series that lasts minutes, with movements occurring every 20-40seconds?
Periodic limb movement disorder
68
What is the pharmacologic treatment of restless leg syndrome and PLMD?
Ropinirole, Pramipexole | Off label therapy for these meds. These are dopamine drugs also used in parkinsons

Pharmacology III (19 decks)

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