Sedatives/Hypnotics Flashcards
1
Q
Excessive worry, restlessness, irritability, or tension. Persists for at least 6 months
A
Anxiety
2
Q
3 core symptoms of anxiety
A
restlessness, irritability, tension
3
Q
_____ is a typical/normal reaction to stress
A
anxiety
4
Q
sleep disorders occur in ___% of the population
A
33%
5
Q
why are sleep disorders difficult to treat with medications
A
they are cause by multiple factors
psych conditions, parasomnias, dysomnias, limb movement disorders, alcohol, drugs, sleep apnea, illness
6
Q
what is a major contributor to sleep disorders
A
psychiatric conditions
7
Q
sleep/awake stages
A
awake, stage 1, 2, 3, 4, REM
8
Q
awake EEG: ______ frequency, ______ amplitude
A
HIGH frequency, LOW amplitude
9
Q
Stage 1 EEG: ______ frequency, ______ amplitude
A
ALPHA frequency, LOW amplitude
10
Q
Stage 2 EEG: ______ frequency, ______ amplitude
A
LOWER frequency, HIGHER amplitude
11
Q
stage 3+4 EEG: ______ frequency, ______ amplitude
A
VERY LOW frequency, HIGH amplitude
12
Q
which stage of sleep is “relaxed awake”
A
stage 1
13
Q
which stage of sleep is “non-REM sleep”
A
Stage 2
14
Q
which stages of sleep are “slow wave sleep”
A
stages 3+4
15
Q
REM sleep is very similar to ______, but ______
A
awake, dreaming
16
Q
cycle through sleep phases every _____
A
90 mins
17
Q
the greatest proportion of REM sleep occurs right before _____
A
birth
18
Q
quality of sleep _____ with age
A
diminishes
19
Q
rank sleep stages: high to low frequency
A
REM, stage 1, stage 2, stage 3,4
20
Q
rank sleep stages from High to low amplitude
A
stages 3/4, stage 2, stage 1, REM
21
Q
REM stands for
A
rapid eye movement
22
Q
when does first episode of REM sleep occur
A
~1 hour of sleep onset
23
Q
which stage of sleep is sensitive to sedative, hypnotics
A
REM
24
Q
which stage of sleep is associated with dreaming
A
REM
25
what stage of sleep has a rapid/immediate onset in narcolepsy
REM
26
REM sleep has an immediate onset in _______
narcolepsy
27
what is associated with reduced REM sleep, prolonged deep sleep, and a REM rebound
alcohol
28
effect of alcohol on sleep
more time in deep sleep, doesn't enter REM until right before waking up (REM rebound)
29
what is a REM rebound and when causes it to occur
when a person doesn't enter REM sleep until right before they wake up, can be caused by alcohol
30
what condition is associated with frequent REM
narcolepsy
31
effect of narcolepsy on sleep
frequent REM (Even during day), not a lot of deep sleep
32
what condition is associated with a lot more awake time
insomnia
33
drugs that produce partial or total loss of sensation, sometimes with complete loss of consciousness
anesthetics
34
anesthetics produce partial or total loss of _____, sometimes with loss of ______
sensation; consciousness
35
3 major indications for sedative hypnotics
anxiety disorders, sleep disorders, anesthesia
36
sedative refers to ______ properties of drugs
anxiolytic (anti-anxiety)
37
hypnotic refers to _______ or _________ properties of drugs
sleep-inducing or anesthetic properties
38
what is a Soporific
hypnotic
39
synonym for a hypnotic
soporific
40
do benzodiazepines or barbiturates have a STEEPER therapeutic-toxic dose-response relationship
barbiturates (not as safe)
41
4 GABAa receptor drug classes
alcohol, barbiturates, benzodiazepines, non-BZD Z-drugs
42
8 domains affected by sedative hypnotics
cognition, judgement, self control, coordination, awareness, memory, consciousness, respiration
43
tolerance develops to a drugs ______
EFFECTS
44
abrupt imbalance of glutamatergic and GABAergic activity
kindling
45
barbiturate and BZD withdrawal can be _____
fatal
46
The GABAa receptor is a
heteromeric glycoprotein
47
GABA interacts at 2 sites between the ___ and ___ subunits and triggers _______ channel opening and ________ of the membrane
alpha and beta subunits; chloride channel opening; hyperpolerazation
48
BZD, barbiturates, ethanol bind at specific sites between the ____ and _____ subunits
alpha and gamma
49
binding of sedative-hypnotics to the GABA receptor ______ the action of GABA, thus they are referred to as
increases; positive allosteric modulators
50
a positive allosteric modulator is functionally like an
indirect agonist
51
barbiturates increase the ______ of Cl- channel opening
duration
52
benzodiazepines increase the ______ of Cl- channel opening
frequency
53
ethanol increases the ______ and ______ of Cl- channel opening, as well as increasing the number of channel _____
frequency and duration, number of channel bursts
54
what class increase the DURATION of Cl- channel opening
barbiturates
55
what class increases the DURATION of Cl- channel opening
Benzodiazepines
56
which class increases BOTH (frequency and duration) of Cl- channel and increase the number of channel bursts
alcohol
57
ethanol and IV anesthetics are selective for GABAa receptors with what 2 subunits
beta 2 and beta 3
58
what anti-convulsant inhibits GABA metabolism
Vigabatrin
59
which anti-convulsant inhibits reuptake of GABA
Tiagabine
60
which CNS excitatory agent directly blocks the Cl- channel
Picrotoxin
61
which CNS excitatory agent interferes with GABA binding
Bicuculline
62
alpha 1 subunit effects/adverse effects
Sedation ONLY; has amnesia and abuse potential
63
alpha 2 subunit effect/adverse effects
anxiolytic, muscle relaxation, anticonvulsant (NO sedation)
| NO amnesia or abuse potential
64
alpha 3 subunit effects/adverse effects
muscle relaxation ONLY, NO amensia/abuse
65
alpha 5 subunit effect/adverse effects
muscle relaxation ONLY, amnesia potential (no abuse)
66
which subunit is ONLY for sedation
alpha 1
67
which 2 subunits are ONLY for muscle relaxation
alpha 3 and 5
68
which class of drugs is selective for alpha 1
Z-drugs
69
which subunits do BZD bind to
alpha 1, 2, 3, 5
70
receptors with alpha 4 or 6 subunits have HIGH affinity for what
partial inverse agonists (Ro 15-4513)
71
receptors with alpha 4 or 6 subunits have SOME affinity for what
BZD receptor antagonist (Flumazenil)
72
what was Ro 15-4513 pursued for
possible antidote to ethanol
73
which is safer: benzodiazepines or barbiturates
benzodiazepines
74
what should NOT be treated with benzodiazepines
PTSD (could worsen)
75
what should not be used to treat PTSD
benzodiazepines
76
benzodiazepines are a contributor to what in the elderly population
falls and injuries
77
benzodiazepines are _________ with alcohol and barbiturates
synergistic
78
effect of benzodiazepines on sleep
decrease time spent in stage 1, 3, 4, REM
increase time spent in stage 2
increase number of sleep cycles
79
anticonvulsant effects of benzodiazepines are at what subunit
alpha 2 ONLY
80
benzodiazepines inhibit neural signaling by _________ the hyper polarizing effects of GABA
increasing
81
which 2 BZD are approved for LONG TERM treatment of seizures
clonazepam, clorazepate
82
which 2 BZD have well defined roles in managing status epilepticus
diazepam, lorazepam
83
abuse and dependence of BZD is more likely with _____ acting and ______ potency drugs
faster acting, higher potency
84
many BZD have ________ metabolites with _____ half lives
psychoactive metabolites, with long half lives
85
Z drugs bind only to what subunit
alpha 1
86
3 Z-Drugs
zolpidem, zaleplon, eszopiclone
87
Z-drugs are approved for use up to _____ days
7-10 days
88
which Z-drug is most associated with parasomnias (sleep walking/talking)
Zolpidem
89
dose of Z-drugs should be reduced in who
females
90
dose of Z-drugs should be ______ in females
reduced
91
which Z drug is approved for LONG TERM treatment of insomnia
eszopiclone
92
what is an adverse effect of eszopiclone
bitter taste
93
what drug is used to rescue someone from a BZD overdose
Flumazenil
94
Flumazenil is a
benzodiazepine receptor antagonist
95
unique binding size of Flumazenil produces ______ with ____ binding site and ______ binding site
steric hindrance, BZD and Z-drug binding sites
96
how are barbiturates classified
by duration of action
97
ultra short acting barbiturates are given by
IV injection
98
ultra short acting barbiturates are rapidly distributed to the _____ and cause ________ in 30-45 seconds
brain, unconsciousness
99
peak concentration of ultra short acting barbiturates occurs at
1 minute
100
4 indications of barbiturates
seizures, anxiety, insomnia, anesthesia
101
will Flumazenil treat a barbiturate overdose
no
102
2 treatments for barbiturate overdose
activated charcoal, urinary alkalinization
103
Ramlteon is a _________ receptor agonist. it is indicated for insomnia characterized by ____________
MELATONIN receptor agonist. insomnia characterized by difficulty with SLEEP ONSET
104
Tasimelteon is a _______ receptor agonist. it is indicated for
MELATONIN receptor agonist. indicated for non-24 hour sleep wake disorder
105
what drug is indicated for non-24 hour sleep wake disorder
Tasimelteon
106
Buspirone is a full agonist at _______ ____ receptors and a partial agonist at _______ ____ receptors.
full agonist at PREsynaptic 5HT1a receptors
| partial agonist at POSTsynaptic 5HT1a receptors
107
Suvorexant is a _______ receptor antagonist.
OREXIN receptor antagonist
108
the effects of _______ make take 1 week of treatment
Buspirone
109
which non-GABA receptor drug does NOT potentiate effects of alcohol, does NOT show abuse potential
Busprione
110
which non-GABA drug has a risk for abuse, may potentiate effects of alcohol, and increases parasomnias
Suvorexant
111
which drug is an orexin receptor antagonist
Suvorexant
112
which drug is a 5HT1a receptor agonist
Buspirone
113
non medical use of sedative hypnotics
drug facilitated sexual assult
114
#1 drug used for sexual assault
alcohol
115
what drug is also known as "roofies"
Flunitrazepam
116
___mg of Flunitrazepam can impair a victim for 8-12 hours
1mg
117
what drug is odorless, colorless, and tasteless that is used for sexual assaults
Flunitrazepam
118
effects of Flunitrazepam are ______ by concurrent alcohol use
increased
