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Spring 2024 Therapeutics 3 > Exam 4 Sleep > Flashcards

Exam 4 Sleep Flashcards

1
Q

What is a sedative?

A

-Calms anxiety
Decreases excitement and activity
-Does not cause drowsiness or impair performance

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2
Q

What is an anxiolytic?

A

Anti-anxiety
-Relieves anxiety without sedation

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3
Q

What is a hypnotic?

A

*Induces sleep

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4
Q

What is a narcotic?

A

“Sleep-inducing”

-now refers to opioids or illegal drugs

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5
Q

What brain region is involved in sleeping?

A

Reticular Formation

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6
Q

What are the 3 stages of sleep?

A

Wakefulness
Non-rapid eye movement (NREM)
Rapid eye movement (REM)

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7
Q

Waking up in the middle of which sleep stage makes you feel bad?

A

REM

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8
Q

What is REM sleep?

A

Similar to awake in EEG

*not sure why we have this or what benefit is

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9
Q

Which sleep stage is associated with dreaming?

A

REM

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10
Q

At what time does melatonin secretion stop?

A

7:30am

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11
Q

What time does high alertness begin?

A

10:00am

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12
Q

What are the biological regulators of sleep?

A

Neurotransmitters (GABA)

Neuromodulators

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13
Q

*What is the main target for current sleep medications?

A

GABA

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14
Q

Why do we target GABA for sleep?

A

Want to quiet down neurotransmitter activity

-GABA is inhibitory so we want to increase its effect

-GABA acts as a Cl channel, want to induce a Cl influx to hyperpolarize the cell membrane

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15
Q

What is the function of benzodiazepines?

A

Bind GABA receptors, make them function better

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16
Q

What type of ion channel is GABA?

A

Chloride

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17
Q

*What site on GABA do benzodiazepines target?

A

Benzodiazepine site (BZD): Allosteric a1 and y2

(allosteric means they do not bind at the active site)

*work at all a1-5

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18
Q

What affect do benzodiazepines have on GABA?

A

Facilitate GABA action

Increase frequency of channel opening*

*Work at a1-5 so they have many effects

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19
Q

What are the non-benzodiazepines that work at the benzodiazepine receptor?

A

Z-Hypnotics

-zolpidem
-zaleplon
-eszopiclone

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20
Q

*Where do the Z-hypnotics work on GABA?

A

BZ1 (benzodiazepine) receptors of a1

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21
Q

What is the benzodiazepine antagonist (used for overdose treatment)?

A

Flumazenil

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22
Q

*What affect do barbiturates have on the GABA channel and how does this compare to benzodiazepines?

A

Barbiturates: Increase duration of channel opening, have direct effects on GABA A

BZDs: Increase frequency of channel opening, have indirect effects on GABA

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23
Q

Which are more dangerous: benzodiazepines or barbiturates?

A

Barbiturates

-have a direct effect on GABA

**Benzodiazepines have a ceiling effect with how much they are able to increase the frequency of GABA channel opening

*Barbiturates do not show a ceiling effect with duration of channel opening and could theoretically keep the channels open forever
*If barbiturate dose gets too high patients can have seizures or go into a coma and die

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24
Q

*Positive alkylation of the benzodiazepine structure acts as what?

A

Source of active metabolites

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25
Q

*Annealating the 1-2 bond in the benzodiazepine structure with an “electron rich” ring causes what?

A

-High affinity
-Decreased half-life

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26
Q

*Does Diazepam have a short or long half-life?

A

LONG

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27
Q

Which benzodiazepine does not get metabolized into an active metabolite?

A

Lorazepam

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28
Q

Which benzodiazepines has a slow elimination rate (has an active metabolite)?

A

Diazepam

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29
Q

What are the active metabolites of diazepam?

A

-> Desmethyldiazepam -> Oxazepam

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30
Q

What two other indications is diazepam used for?

A

-Convulsive disorders (seizures)

-Accumulation of metabolites

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31
Q

Which benzodiazepine has an intermediate elimination rate?

A

Clonazepam

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32
Q

What other indication does clonazepam have?

A

Anticonvulsant

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33
Q

Which benzodiazepine has a rapid elimination rate?

A

Midazolam

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34
Q

Why do some benzodiazepines have slow elimination?

A

They have active metabolites that cause it

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35
Q

*What affect do benzodiazepines have on the sleep cycle?

A

Decrease REM

Decrease stage 3 and 4
-BAD, makes you not feel rested or recharged
***NOT AS COMMONLY USED AS A SLEEPING AID BECAUSE OF THIS

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36
Q

Besides sleep, what are benzodiazepines used for?

A

Anticonvulsants

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37
Q

What should benzodiazepines not be used with?

A

-Other sedatives

*Alcohol (also acts on GABA, could break ceiling effect and cause coma)

*Pregnancy and breastfeeding

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38
Q

What is Flumazenil used to treat?

A

Benzodiazepine overdose

Z-Hypnotic overdose

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39
Q

What drug do we use to treat a barbiturates overdose?

A

NONE
-cannot treat

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40
Q

*What Z-Hypnotics are used for SHORT-TERM treatment of insomnia? (7-10 days)

A

Zolpidem (Ambien)

Zaleplon (Sonata)

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41
Q

*What Z-Hypnotic is used for LONG-TERM treatment of insomnia?

A

Eszopiclone (Lunesta)

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42
Q

*What is a benefit of using Z-hypnotics over benzodiazepines?

A

Cause less negative effects on sleep patterns

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43
Q

*What are the side effects of Z-Hypnotics?

A

*PATIENTS MAY DO DAILY ACTIVITIES WHILE ASLEEP

-Sleep-driving, -cooking -eating, -sex

*WARN PATIENTS ABOUT THIS

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44
Q

True or False: Barbiturates are commonly used

A

False
-high abuse potential, less common now

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45
Q

What is the long-acting barbiturate?

A

Phenobarbital

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46
Q

What is the short to intermediate acting barbiturate?

A

Pentobarbital

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47
Q

Which barbiturate also acts as an anticonvulsant?

A

Phenobarbital

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48
Q

What side effect is the biggest concern with barbiturates?

A

Respiratory depression -> Death

(seizure, then coma, then death)

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49
Q

Top 3 most important facts about barbiturates:

A

-Bind to all GABA A “a1-5” receptors

-Increase duration of channel opening

-Direct effects on GABA

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50
Q

Top 2 most important facts about benzodiazepines:

A

-Bind all GABA A “a1-5” receptors

-Increase frequency of channel opening

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51
Q

Top 2 most important facts about Z-hypnotics:

A

-Bind GABA A “BZ1 receptors of a1”

-Increase frequency of channel opening

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52
Q

What is the difference between GABA A and GABA B?

A

GABA A= Cl ion channel

GABA B= GPCR

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53
Q

What type of receptor is the GABA B receptor?

A

Metabatropic (GPCR)

(initiates a number of metabolic steps to modulate cell activity)

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54
Q

What is the structure of the GABA B receptor?

A

Heterodimer

(made up of GABA B1 and GABA B2)

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55
Q

Which part of the GABA B Receptor heterodimer does GABA bind to?
(GABA B1 or GABA B2)

A

GABA B1

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56
Q

What is Xyrem?

A

-Sodium Oxybate, GHB*

-A strange drug that is not used often

-Sedative hypnotic

-Prescribers must be enrolled in a patient success program

*Huge abuse potential

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57
Q

What is Gamma-Hydroxybutyric Acid (GHB)?

A

-Sedative hypnotic

*High abuse potential

**Does not have an antagonist, cannot be reversed

58
Q

Why is abuse of Gamma-Hydroxybutyric Acid (GHB) a concern?

A

It has no antagonist

*Cannot be reversed

59
Q

When do melatonin levels peak?

A

The middle of the night

60
Q

What are the melatonin AGONISTS?

A

-Ramelteon

-Tasimelteon

61
Q

What is the nickname for Ramelteon and why is it called this?

A

“Master Clock”

-because it regulates circadian rhythms
(helps when melatonin is lost in aging and Alzheimer’s)

62
Q

What makes Ramelteon a good drug of choice?

A

No abuse, withdrawal, or dependency

63
Q

What disease state is Tasimelteon used to treat?

A

Non-24-hour sleep wake disorder

(in blind individuals)

64
Q

What type of product is Tasimelteon registered as?

A

Orphan product

*this is an FDA approval of a drug for a rare disease that very few people face

(in this case, Non-24-hour sleep wake disorder)

65
Q

What is orexin?

A

Neurotransmitter that works in the hypothalamus (sleep center) to promote wakefulness

*Want to reduce orexin to promote sleep

-Works on the reward pathway, some abuse potential

66
Q

What drug is an orexin receptor antagonist?

A

Suvorexant

67
Q

Where are receptors for Suvorexant located?

A

Hypothalamus

68
Q

What affect does Suvorexant have on the reward pathway of Orexin?

A

Reduces rewarding stimuli (DA release)

–done through receptors that modulate the mesolimbic projections between the VTA and the nucleus accumbens

69
Q

What was the label change made by the FDA for all sleep disorder drug products?

A

Label must include information about Sleep-Related behaviors

(sleep-driving, sleep-cooking/eating, sleep-phone calls)

70
Q

What are other drugs that have sedative properties?

A

Trazodone

Antihistamines (OTC):
-Diphenhydramine
-Doxylamine
-Pyrilamine

71
Q

What is the most commonly taken natural herbal/natural sedative?

A

Melatonin

72
Q

True or False: Melatonin is FDA approved for sleep

A

False

73
Q

Which herbal/natural sedative can cause hepatotoxicity?

A

Valerian

74
Q

What is a big problem with herbal/natural products?

A

Many products do not actually contain the product/amount that they are advertising

75
Q

What disease states are associated with insomnia?

A

Anxiety
Mood Disorders

76
Q

What substances are associated with insomnia?

A

Caffeine
Nicotine

77
Q

What drugs are associated with insomnia?

A

Modafinil
Amphetamines
Beta-agonists
Beta-blockers
Thyroid meds
Bupropion
Decongestants
Methylphenidate

78
Q

What defines an “insomnia disorder”?

A

Difficulties with sleep initiation (latency), sleep maintenance, and/or early-morning awakening

**Taking place at least 3 nights per week

**Lasting at least 3 months

79
Q

What is latency?

A

Sleep initiation

80
Q

What is first-line treatment for insomnia disorders?

A

NOT MEDICATIONS

-setting up a sleep schedule, sleep hygiene*, avoiding screen time, etc

81
Q

What are the most commonly used sleep medications?

A

Z-hypnotics

-Zolpidem
-Eszopiclone
-Zaleplon

82
Q

How is dosing of zolpidem adjusted?

A

Initial dose is lower in women and the elderly

(5mg)

83
Q

Which drug has metallic taste as a side effect?

A

Eszopiclone

84
Q

What are the side effects of Z-hypnotics?

A

-Somnolence
-Dizziness
-Ataxia
-Headaches

*Parasomnias (unusual actions while sleeping)

85
Q

What are Z-hypnotics a substrate of?

A

3A4

86
Q

What is a barrier to receiving Z-hypnotics?

A

They are controlled substances

87
Q

What is the preferred benzodiazepine for sleep?

A

Temazepam

88
Q

What are the side effects Temazepam?

A

-Drowsiness
-Dizziness
-Cognitive impairment
-Increased fall risk

89
Q

Which drug is contraindicated with Fluvoxamine?

A

Ramelteon

*concentration of this drug gets majorly increased by the other, cannot use together

90
Q

What are the side effects of Ramelteon?

A

-GI upset
-Next day somnolence
-Hyperprolactinemia
-Prolactinemia

91
Q

What is Ramelteon and Tasimelteon substrates of?

A

1A2

92
Q

True or False: Melatonin only helps with falling asleep, not staying asleep

A

True

93
Q

What are the orexin receptor antagonists?

A

Suvorexant

Lemborexant

Daridorexant

94
Q

What is required when taking orexin receptor antagonists that may limit their use?

A

Need at least 7 hours of sleep

95
Q

When are orexin receptor antagonists contraindicated?

A

With narcolepsy

96
Q

What side effects do orexin receptor antagonists cause?

A

Narcolepsy-like SE

97
Q

What are the orexin receptor antagonists substrates of?

A

3A4

98
Q

How does Doxepin work?

A

Tricyclic antidepressant (TCA)

-low doses exert effect through H1 receptor antagonism

99
Q

What are the side effects of Doxepin?

A

Anticholinergic

100
Q

True or False: Trazodone is not approved for insomnia

A

True

101
Q

What is a side effect of trazodone and why does it occur?

A

Daytime hangover

*because it has a long half-life

102
Q

When would we use Mirtazapine for sleep?

A

-Clinically used as a sleep agent, but especially in patients with depression who have difficulty sleeping

103
Q

When would we use Quetiapine for sleep?

A

Low doses are not recommended for insomnia use unless there is a co-morbid psychiatric disorder

104
Q

When should we consider melatonin use?

A

Jet lag

Patients with low melatonin levels

105
Q

What is melatonin a substrate of?

A

1A2

106
Q

What side effects can be caused by German chamomile?

A

Allergic reaction in patients with ragweed or daisy allergies

107
Q

In order to be diagnosed with obstructive sleep apnea, what must patients experience?

A

At least 5 obstructive apneas (with evidence) per hour of sleep confirmed by polysomnography

108
Q

What are the symptoms of obstructive sleep apnea?

A

Excessive daytime sleepiness
Snoring
Pauses in breathing during sleep
Headache
Irritability
Sore throat
Erectile dysfunction
Impaired memory
GERD
Mood disturbance

109
Q

If a patient has both insomnia and sleep apnea which is treated first?

A

Sleep apnea

-treating insomnia without having the patient on a sleeping mask could kill them

*recognized that these conditions often go together

110
Q

What is the diagnostic test for sleep apnea and when do we use it?

A

Polysomnography

Only if:
-Significant cardiorespiratory disease
-Potential respiratory muscle weakness due to neuro-muscular condition
-Chronic opioid medication
-History of stroke
-Sever insomnia

111
Q

What are the non-pharm treatments for sleep apnea?

A

-Weight loss (adjunct, not cure)
-Smoking cessation
-Avoid alcohol and CNS depressants
-Sleep on side, not back

112
Q

What is the pharm cure for sleep apnea?

A

CPAP machine

-continuous positive airway pressure

113
Q

How do we treat excessive daytime sleepiness (EDS)?

A

Modafinil

Armodafinil

**need to review CPAP adherence first and possibility of RLS or PLMS

114
Q

What symptoms are considered “The Narcolepsy Tetrad”?

A

-Excessive Daytime Sleepiness (EDS)
-Cataplexy
-Hallucinations
Sleep Paralysis

*patients may experience all or some of the symptoms

115
Q

What % of narcolepsy patients experience Excessive Daytime Drowsiness (EDS)?

A

100%

*generally more severe in Type 1 narcolepsy (with cataplexy or hypocretin deficiency syndrome)

116
Q

What is cataplexy?

A

Sudden loss of muscle tone triggered by emotion

117
Q

What percent of narcolepsy patients experience cataplexy?

A

75%

118
Q

What % of narcolepsy patients experience hallucinations?

A

30-60%

119
Q

What % of narcolepsy patients experience sleep paralysis?

A

25-50%

120
Q

What % of narcolepsy patients experience all 4 symptoms in the narcoleptic triad?

A

10-33%

121
Q

How do we treat cataplexy?

A

-Sodium oxybate

-Xywav

-Lumryz

122
Q

Which cataplexy med has lower sodium content?

A

Xywav

123
Q

Which cataplexy med is approved in children?

A

Xywav

*for adults + children 7 and older

124
Q

Which cataplexy med is also approved for Idiopathic Hypersomnia in adults?

A

Xywav

125
Q

Which cataplexy med is the original base med?

A

Sodium Oxybate (Xyrem)

126
Q

Which cataplexy med is an ER dosage form that only requires once nightly dosing?

A

Lumryz

127
Q

What is a side effect of Modafinil/Armodafinil?

A

Possible life-threatening rash

128
Q

Which medications were recently FDA approved for excessive daytime sleepiness?

A

Pitolisant

Solraimfetol

129
Q

What is the MOA of Pitolisant?

A

H3 receptor antagonist/inverse agonist

130
Q

When is Pitolisant contraindicated?

A

Severe hepatic impairment

131
Q

What are two negative affects that Pitolisant can have?

A

-Reduces effectiveness of contraception (3A4 inducer)

-Prolongs QT interval

132
Q

What is Pitolisant a substrate of?

A

2D6/3A4

133
Q

What drugs should we avoid using with Pitolisant?

A

Centrally-acting H1 receptor antagonists
(OTC antihistamine)

134
Q

What is the MOA of Solriamfetol?

A

Dopamine norepinephrine reuptake inhibitor (DNRI)

135
Q

What is Solriamfetol indicated for?

A

Improvement in wakefulness in adults with excessive daytime sleepiness due to narcolepsy or sleep apnea

136
Q

What is the renal impairment dosing for Solriamfetol?

A

Moderate: Start 37.5mg, may increase to 75mg after 7 days

Severe: 37.5mg is starting and max dose

137
Q

What are the warnings associated with Solriamfetol?

A

BP and HR increases

-Avoid in unstable CV disease and arrhythmias
-Caution in patients with history of psychosis or bipolar disorder
-Decrease or discontinue dose if psychiatric symptoms occur
-Caution with dopaminergic drugs

138
Q

What drugs are used to treat shift work sleep disorder?

A

Modafinil and Armodafinil

*take 1 hour before work period starts
*WE WANT WAKEFULLNESS

139
Q

What treatment do we use for Restless Legs Syndrome?

A

Gabapentin encarbile (preferred)

Dopamine agonists (IR pramipexole or IR ropinirole)

Iron supplementation is low iron is cause

140
Q

What is Gabapentin encarbil?

A

Prodrug of Gabapentin

*FDA approved for RLS

*First-line

Spring 2024 Therapeutics 3 (24 decks)

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