Sleep Flashcards
(191 cards)
1
Q
How do sedatives work? (four items)
A
Calms anxiety, decreases excitement and activity, does not produce drowsiness, and does not impair performance
2
Q
Do anxiolytics cause sleepiness or sedation
A
NO, anxiolytics are antianxiety medications that do not produce sleep or sedation. Not all anxiolytics are sedatives
3
Q
What do hypnotics do? (three things)
A
sleep-inducing, implies restful and refreshing sleep, NOT HYPNOTIZED
4
Q
What are narcotics? (two points)
A
Sleep producing, opioids or illegal drugs
5
Q
What structures does the reticular formation extend through? (3)
A
through the central core of the medulla oblongata, pons and midbrain
6
Q
What is the reticular formation composed of (2)
A
white matter and loosely clustered neurons
7
Q
What does the reticular formation do?
A
contains dopamine, adrenergic, serotonergic, and cholinergic neurons and regulates sleep-wake transitions and synchronization of EEG
8
Q
What are the 3 stages of sleep?
A
Wakefulness, NREM, REM
9
Q
How many stages are there in NREM and what are they?
A
4 stages
Stage 1= dozing
Stage 2= unequivocal sleep
Stage 3= voltage increase, frequency decrease
stage 4= delta waves
10
Q
What stage does REM look similar to on an EE? (1, 2, 3, 4, or awake)?
A
similar to awake on the EEG
11
Q
What are four factors that regulate sleep?
A
age, sleep history, drug ingestion, and circadian rhythms
12
Q
What is chronopharmacology?
A
the circadian clock picture essentially
13
Q
Which neurotransmitters regulate sleep? (8)
A
epinephrine, norepinephrine, dopamine, serotonin, histamine, acetylcholine, adenosine, GABA
14
Q
What neurotransmitter is the main target for sleep medications?
A
GABA
15
Q
Neuromodulators of sleep (5)
A
Growth Hormone, prolactin, cortisol, melatonin, endogenous peptides
16
Q
four components of GABA neurotransmission
A
GABAa receptors, GABAb receptors, GABA transporters (GAT-1), GABA transaminase (GABA-T)
17
Q
How many subunits are there on GABAa receptor
A
5 subunits
18
Q
What kind of ion channel is GABAa receptor
A
Chloride ion channel
19
Q
What are the orthosteric sites on GABAa receptor (2)
A
a1 and B2
20
Q
What are the allosteric sites on GABAa receptor (2) and what three things target them?
A
benzodiazepines, ethanol, glucocorticoid target a1 and gamma2
21
Q
What drug targets the channel pore of GABAa receptor
A
picrotoxin
22
Q
Mechanism of action Benzodiazepines
A
facilitate the action of GABA by increasing the frequency of the channel opening. a1-5
23
Q
what is the name of the drug class that are non-benzodiazepines that act at the BZD receptor
A
z-hypnotics
24
Q
what 3 drugs are part of z-hypnotics
A
zolpidem, zaleplon, eszopiclone
25
What specific receptors do non benzodiazepines work on?
BZ1 receptors of a1 on GABAa receptors
26
What drug is a BZD antagonist used for overdose treatment
flumazenil
27
what is an inverse BZD agonist
B carbolines
28
How do barbiturates work
increase the duration of GABAa receptor channel opening and have direct effects on GABAa AT HIGH DOSES
29
1 position alkylation of BZDS produces
active metabolites like oxazepam
30
annealing the 1-2 bond of BZDs with triazole or imidazole ring yields ____ affinity and ____ half-life
high, decreased
31
the half life of diazepam is ___ (long or short)
long
32
What gets removed from diazepam and at what position to make oxazepam, and active metabolite?
dealkylated at 1 position
33
What is desmethyldiazepam
the intermediate between diazepam and oxazepam
34
Which BZDS have slow elimination and active metabolites? (6)
Chlordiazepoxide, Diazepam, Flurazepam, Clorazepate, Quazepam, Prazepam
35
Which two drugs are anticonvulsants and sedatives?
Diazepam and Clonazepam
36
True or False: Prazepam is commonly used in the US
FALSE, currently unavailable in US
37
Which was the first BZD?
Chlordiazepoxide, Diazepam, Flurazepam, Clorazepate, Quazepam, Prazepam
38
Which BZDS have intermediate elimination rates? (5)
Alprazolam, Lorazepam, Clonazepam, Oxazepam, and Temazepam
39
Which two BZDs are rapidly eliminated
Midazolam (VERSED) and Triazolam
40
What kind of sleeplessness is best for BZDs that have slow elimination and formation of active metabolites?
patients who wake up in the middle of the night
41
BZDs that are rapidly eliminated cause rapid tolerance (T/F)
True
42
Intermediate to rapidly eliminated BZDs should be used in 2 populations
elderly, patients with hepatic problems
43
What does taking BZDs with food do
delays absorption
44
Increase lipid solubility will increase speed of delivery to _____
the brain
45
True/False: BZDs are not a concern during pregnancy and breastfeeding
false, cross placental barrier and are detected in breast milk
46
Which are more dangerous at high doses, barbiturates or BZDs?
Barbiturates, may cause coma at doses that are too high whereas BZDs hit a plateau
47
Respiratory depression is a major concern for what drug class when combined with other agents?
BZDs
48
What is the result of BZDs on REM sleep? Which stages of sleep does it effect?
decreases REM sleep, decreases stages 3 and 4
49
Side effects of BZDs are ____ dependent
dose
50
What is Flumazenil used for
BZD antagonist for overdose
51
what is the max cumulative dose of Flumazenil for overdose?
3mg
52
What is the initial dose of Flumazenil for overdose
0.2mg IV over 30 seconds
53
What are some side effects of Flumazenil
induce convulsions, panic attacks, agitation, confusion, n/v, headache
54
is zolpidem short term or long term
short term
55
is zaleplon short term or long term
short term
56
is eszopiclone short term or long term
long term
57
how are z-hypnotics metabolized
cyp3a4
58
do z-hypnotics have less or more negative side effects on sleep patterns than BZDs
less!
59
FDA mandates that we must warn patients of what for z-hypnotics
weird behaviors during sleep, sleep cooking, sleep sex, sleep driving, sleep eating
60
Flunitrazepam is also called
roofies
61
Zolpidem can be used illicitly and is called
zombie pills or A-minus
62
is phenobarbital long acting or short acting
long acting
63
is pentobarbital long acting or short acting
short acting
64
What do Barbiturates do to REM sleep
decrease REM
65
Barbiturates may cause ____ and ____ depression
cardiovascular and respiratory
66
What part of the brain is GABAb receptor located in?
limbic system
67
what is the presynaptic ion for GABAb receptor? (increase or decrease)
Ca2+ decrease
68
What is the postsynaptic ion for GABAb receptor? (increase or decrease)
K+ increase
69
What are two drug agonists of GABAb receptors?
baclofen and GHB
70
Three antagonist drugs of GABAb receptor
phaclofen, saclofen, and 2-hydroxysaclofen
71
What are the two other names for GHB?
Xyrem and sodium oxybate
72
What should be given with GHB if it is chosen by a provider?
Give with concomitant stimulant use during the day to decrease excessive daytime sleepiness and decrease cataplexy (sudden loss of muscle tone during the day)
73
What is the target of GHB?
GABAa GABAb and GHB receptors
74
Liquid ecstasy, liquid x, juice, scoops are all street names for what drug
GHB, Sodium oxybate, Xyrem
75
Acute effects of GHB include 6 things
loss of reflexes/consciousness
amnesia
N/V
headache
seizures
death
76
How can you treat someone who has been spiked with GHB
THERE IS NO ANTAGONIST, supportive treatment only
77
Explain the levels of melatonin over the course of a day
melatonin begins being produced in the evening, peaks at night, and declines to low daytime amounts in the morning
78
what gland produces melatonin
pineal gland
79
What are the two melatonin agonists
Ramelteon and Tasimelteon
80
Ramelteon is metabolized by what cyp
CYP1A2
81
What kind of sleeplessness are melatonin agonists used for
insomnia characterized by difficulty with sleep onset
82
What is the benefit of melatonin agonists for patients?
No abuse, no withdrawal, no dependency, non-controlled substance
83
Receptor target of Ramelteon and Tasimelteon
high affinity for MT1 and MT2 melatonin receptors in the suprachiasmatic nucleus
84
which drug is an orphan product
tasimelteon
85
which drug can be used to treat non-24 hour sleep wake disorders in blind individuals?
tasimelteon
86
where are oxerin receptors in the brain
hypothalamus
87
what does oxerin do?
regulate wakefulness, arousal, and thermoregulation
88
what is the target of suvorexant
orexin receptor antagonist, OX1 and OX2 in hypothalamus
89
What are the indications of trazodone
antidepressant and hypnotic under investigation
90
What OTC drugs can be used as a hypnotic (3)
Antihistamines (diphenhydramine, doxylamine, pyrilamine)
91
What are the signs of sedative-hypnotic overdose?
depressed respiration, low blood pressure, no reflexes, hypothermia
92
Disease states, medications, substances associated with insomnia (12)
anxiety, caffeine, modafinil, amphetamines, beta-agonists, beta-blockers, nicotine, thyroid meds, mood disorders, bupropion, decongestants, methylphenidate
93
The DSM-5 renamed sleep disorder chapter to what
sleep/wake disorders to recognize its more than just not being able to sleep
94
two sleep related movement disorders
restless leg syndrome and periodic leg movements in sleep (PLMS)
95
two breathing related sleep disorders
obstructive sleep apnea and central sleep apnea
96
two types of circadian rhythm sleep-wake disorders
non-24-hr sleep-wake (blind) and shift work type
97
what is insomnia
difficulties with sleep initiation, sleep maintenance, and/or early morning waking
98
how often must insomnia take place and how long must it be present
3 times per week for at least 3 months
99
what kind of sleep disorder can be classified as transient (jet lag), short term (up to 4 weeks), and long term (more than 4 weeks)
insomnia
100
what five medications are used to help sleep onset only
zolpidem, eszopiclone, zaleplon, triazolam, ramelteon
101
what four medications are used for sleep maintance only
suvorexant, doxepin, eszopiclone, zolpidem
102
what three medications can be used for both sleep onset and sleep maintenance
zolpidem, eszopiclone, and temazepam
103
What is the first line therapy for sleep disorders
non-pharmacological and sleep hygiene
104
What class of medications (bonus if you can name them) are used most commonly for sleep disorders
z-hypnotics (zolpidem, eszopiclone, zaleplon)
105
what is intermezzo and what is it approved for
sublingual dosage form of zolpidem that is used if a patient wakes up in the middle of the night with at least 4 hours of sleep left
106
What is the initial dose of zolpidem in women and the elderly
5 mg, lower to reduce fall risk
107
what do some patients complain of when taking lunesta (eszopiclone)
metallic taste
108
z-hypnotics are metabolized by what enzyme
cyp3a4
109
four side effects of z hypnotics
somnolence, dizziness, ataxia, headaches
110
what are parasomnias and what drug class causes them
z hypnotics, unusual actions while a person is sleeping
111
T/F, Z-hypnotics are not controlled substances
false, high potential for misuse
112
what causes more daytime hangover, z-hypnotics or BZDs
Z-hypnotics
113
Which is the preferred BZD for sleep
temazepam
114
side effects of BZDs for insomnia
drowsiness, dizziness, cognitive impairment, increased fall risk
115
what are warning associated with doxepin for sleep
suicidality and sleep behaviors
116
all sleep medications have what warning
odd sleep behaviors (sleep sex)
117
Melatonin agonist have a greater affinity for melatonin receptors than melatonin, true or false
TRUE
118
Two contraindications of ramelteon
with fluvoxamine or angioedema with past used
119
how fast is sleep onset after taking ramelteon
30 minutes, see results after 3 weeks
120
side effects of ramelteon
GI upset, next day somnolence, hyperprolactinemia, prolactinoma
121
what is the dose of ramelteon
8mg 30 minutes before bedtime
122
what is the unique indications of tasimelteon
non-24 sleep wake disorder in adults (BLIND)
123
Addition side effects of tasimelteon
increased ALT, nightmares, unusual dreams
124
dose of tasimelteon
20mg before bedtime on empty stomach at the same time every night
125
melatonin agonists are substrates of which enzyme
1a2
126
suvorexant dose
10mg 30 minutes before bed, must have at least 7 hours to sleep
127
what is the warning associate with taking 20mg of suvorexant
warning against daytime driving
128
Contraindication of suvorexant, lemborexant, and daridorexant
CI in narcolepsy due do cause narcolepsy-like side effects
129
what enzyme metabolizes suvorexant, lemborexant, and daridorexant
3a4
130
dose of lemborexant
5mg at bedtime with at least 7 hours of sleep
131
dose of daridorexant
25mg at bedtime with at least 7 hours of sleep
132
At what doses of suvorexant, lemborexant, daridorexant respectively should the patient be advised to avoid daytime driving
20mg, 10mg, and 40mg
133
what happens to onset of effects of orexin receptor antagonists if the medication is taken with high-fat, high calorie meals, or food in general
the absorption is delayed and the effects are delayed
134
orexin receptor antagonists can worsen what
depression and suicidal ideation
135
doxepin receptor target
H1 receptor antagonism at low doses
136
what kind of side effects are common on doxepin
anticholinergic side effects (4 Can'ts. CAN'T-See – blurred vision; CAN'T-Pee – urinary retention; CAN'T-Spit – dry mouth; CAN'T-Shit – constipation)
137
True or false, trazodone is approved for insomnia
False
138
What property of trazodone causes daytime hangover
long-half life
139
how does the AASM feel about using trazodone for sleep
recommends against, though is clinically effective
140
Mirtazapine is best used for sleep if patients have what other condition
clinically effective if patient has depression and difficulty sleeping
141
what dose of mirtazapine is more effective (high or low)
low, 7mg is more sedating than 30mg
142
Quetiapine recommendation for insomnia
not recommended for insomnia unless patient has a comorbid psychiatric disorder
143
what kind of antipsychotic is quetiapine
atypical
144
what is the recommendation for diphenhydramine for insomnia by AASM
not recommended
145
side effects of diphenhydramine
anticholinergic and paradoxical hyperactivity, especially in children
146
What co-morbid conditions should diphenhydramine be avoided in (3)
narrow angle glaucoma, acute asthma, and BPH due to anticholinergic effects
147
what is melatonin metabolized by
1a2
148
what kind of sleep issue should melatonin be used for
jet lag
149
What should we warn patients about with german chamomile for sleep
allergic reactions in patients with daisy or ragweed allergies
150
what is a CI of Kava
hepatotoxicity
151
what is the FDA approved duration for sleep medication
short term use of 10 days...
152
Patient must have evidence of at least _ obstructive apneas per hour of sleep confirmed by polysomnography
5
153
what are the two obstructive apnea signs
daytime sleepiness, nocturnal breathing disturbances
154
What are the symptoms of obstructive sleep apnea
daytime sleepiness, snoring, pauses in breathing, headache, irritability, sore throat, erectile dysfunction, impaired memory, GERD, mood disturbances
155
How do you treat insomnia and sleep apnea
treat sleep apnea first. Many patients have both that will need to be treated.
156
When should a patient get polysomnography (6)
significant cardiorespiratory disease, potential muscle weakness due to neuro-muscular condition, sleep-related hypoventilation, chronic opioid medication use, hx of stroke, severe insomnia
157
non-pharm treatments of obstructive sleep apnea (4)
weight loss, smoking cessation, avoid alcohol and other CNS depressants, sleep on side instead of back
158
What is a cpap and what should it be used for
continuous positive airway pressure for sleep apnea
159
what two drugs can be used for excessive daytime sleepiness
modafinil and armodafinil
160
what should be reviewed first before initiating modafinil and armodafinil for daytime sleepiness
CPAP adherence and possibility of RLS or PLMS
161
What is narcolepsy
recurring episodes of irresistible need to sleep, fall asleep, or nap at least 3 times per week over the last 3 months
162
What is common for narcoleptics
sleep paralysis
163
What is the narcolepsy tetrad
EDS, cataplexy, hallucination, and sleep paralysis
164
three drugs used for cataplexy
sodium oxybate (xyrem/GHB)
Xywav
lumryz
165
what electrolyte is GHB high in
sodium (also called sodium oxybate)
166
what age is Xywav approved for
adults and children 7 or older
167
How is the sodium content of Xywav compared to GHB?
Xywav has lower sodium content
168
Lumryz is IR and can be used for children
False, Lumryz is ER and is for adults only
169
when should lumryz be taken
once at night
170
sodium content of lumryz
high
171
what is a black box warning for lumryz
respiratory depression and misuse
172
what is a life threatening risk of taking modenafil and armodafinil for EDS
life-threatening rash
173
in addition to cataplexy, GHB can be used for what tetrad of narcolepsy
EDS (excessive daytime sleepiness)
174
what two drugs were recently approved for EDS
pitolisant and solriamfetol
175
What is the receptor target of pitolisant
H3 receptor antagonist/inverse agonist
176
Pitolisant is contraindicated in patients who have ____
severe hepatic impairment and moderate/severe renal impairment
177
what enzyme does pitolisant induce or inhibit
3a4 inducer
178
what medication should we be worried about having reduced efficacy when taken with pitolisant
oral contraceptive due to inducing cyp3a4 metabolism
179
What OTC should pitolisant be avoided being used with
h1 receptor antagonists like OTC antihistamines
180
what is a side effect of pitolisant
QTc prolongation
181
What two neurotransmitters does solriamfetol prevent being uptaken
dopamine and norepinephrine
182
is solriamfetol an agonist or inhibitor
inhibitor, prevents uptake of neurotransmitters
183
what is the indication of solriamfetol
improve wakefulness in adults with EDS due to narcolepsy and OSA
184
What is the starting and max dose of solriamfetol for patients with moderate renal impairment
37.5mg starting, max 75mg after at least 7 days
185
what is the starting and max dose of solriamfetol for patients with severe renal impairment
37.5 is starting and max dose
186
What patients should not get solriamfetol
patients with unstable CVD and arrhythmias, caution in patients with history of psychosis or Bipolar disorder
187
what are the two drugs of choice for shift work sleep disorder
modafinil and armodafinil, taken 1 hour before the work period starts
188
what is restless leg syndrome
the urge to move the legs in response to an uncomfortable or unpleasant sensation that begins or worsens during periods of rest, is partially relieved by movement, or is worse in the evening or night
189
gabapentin enacarbil is a potential first line agent approved for what type of sleep/wake disorder
restless leg syndrome
190
what two dopamine agonists may be used for RLS
pramipexole or ropinirole
191
what supplement is recommended for restless leg syndrome
iron supplementation
