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Pharmacology > Sedatives/Hypnotics > Flashcards

Sedatives/Hypnotics Flashcards

1
Q

Excessive worry, restlessness, irritability, or tension. Persists for at least 6 months

A

Anxiety

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2
Q

3 core symptoms of anxiety

A

restlessness, irritability, tension

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3
Q

_____ is a typical/normal reaction to stress

A

anxiety

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4
Q

sleep disorders occur in ___% of the population

A

33%

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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

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6
Q

what is a major contributor to sleep disorders

A

psychiatric conditions

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7
Q

sleep/awake stages

A

awake, stage 1, 2, 3, 4, REM

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8
Q

awake EEG: ______ frequency, ______ amplitude

A

HIGH frequency, LOW amplitude

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9
Q

Stage 1 EEG: ______ frequency, ______ amplitude

A

ALPHA frequency, LOW amplitude

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10
Q

Stage 2 EEG: ______ frequency, ______ amplitude

A

LOWER frequency, HIGHER amplitude

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11
Q

stage 3+4 EEG: ______ frequency, ______ amplitude

A

VERY LOW frequency, HIGH amplitude

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12
Q

which stage of sleep is “relaxed awake”

A

stage 1

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13
Q

which stage of sleep is “non-REM sleep”

A

Stage 2

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14
Q

which stages of sleep are “slow wave sleep”

A

stages 3+4

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15
Q

REM sleep is very similar to ______, but ______

A

awake, dreaming

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16
Q

cycle through sleep phases every _____

A

90 mins

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17
Q

the greatest proportion of REM sleep occurs right before _____

A

birth

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18
Q

quality of sleep _____ with age

A

diminishes

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19
Q

rank sleep stages: high to low frequency

A

REM, stage 1, stage 2, stage 3,4

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20
Q

rank sleep stages from High to low amplitude

A

stages 3/4, stage 2, stage 1, REM

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21
Q

REM stands for

A

rapid eye movement

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22
Q

when does first episode of REM sleep occur

A

~1 hour of sleep onset

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23
Q

which stage of sleep is sensitive to sedative, hypnotics

A

REM

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24
Q

which stage of sleep is associated with dreaming

A

REM

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25
Q

what stage of sleep has a rapid/immediate onset in narcolepsy

A

REM

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26
Q

REM sleep has an immediate onset in _______

A

narcolepsy

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27
Q

what is associated with reduced REM sleep, prolonged deep sleep, and a REM rebound

A

alcohol

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28
Q

effect of alcohol on sleep

A

more time in deep sleep, doesn’t enter REM until right before waking up (REM rebound)

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29
Q

what is a REM rebound and when causes it to occur

A

when a person doesn’t enter REM sleep until right before they wake up, can be caused by alcohol

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30
Q

what condition is associated with frequent REM

A

narcolepsy

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31
Q

effect of narcolepsy on sleep

A

frequent REM (Even during day), not a lot of deep sleep

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32
Q

what condition is associated with a lot more awake time

A

insomnia

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33
Q

drugs that produce partial or total loss of sensation, sometimes with complete loss of consciousness

A

anesthetics

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34
Q

anesthetics produce partial or total loss of _____, sometimes with loss of ______

A

sensation; consciousness

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35
Q

3 major indications for sedative hypnotics

A

anxiety disorders, sleep disorders, anesthesia

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36
Q

sedative refers to ______ properties of drugs

A

anxiolytic (anti-anxiety)

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37
Q

hypnotic refers to _______ or _________ properties of drugs

A

sleep-inducing or anesthetic properties

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38
Q

what is a Soporific

A

hypnotic

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39
Q

synonym for a hypnotic

A

soporific

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40
Q

do benzodiazepines or barbiturates have a STEEPER therapeutic-toxic dose-response relationship

A

barbiturates (not as safe)

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41
Q

4 GABAa receptor drug classes

A

alcohol, barbiturates, benzodiazepines, non-BZD Z-drugs

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42
Q

8 domains affected by sedative hypnotics

A

cognition, judgement, self control, coordination, awareness, memory, consciousness, respiration

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43
Q

tolerance develops to a drugs ______

A

EFFECTS

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44
Q

abrupt imbalance of glutamatergic and GABAergic activity

A

kindling

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45
Q

barbiturate and BZD withdrawal can be _____

A

fatal

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46
Q

The GABAa receptor is a

A

heteromeric glycoprotein

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47
Q

GABA interacts at 2 sites between the ___ and ___ subunits and triggers _______ channel opening and ________ of the membrane

A

alpha and beta subunits; chloride channel opening; hyperpolerazation

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48
Q

BZD, barbiturates, ethanol bind at specific sites between the ____ and _____ subunits

A

alpha and gamma

49
Q

binding of sedative-hypnotics to the GABA receptor ______ the action of GABA, thus they are referred to as

A

increases; positive allosteric modulators

50
Q

a positive allosteric modulator is functionally like an

A

indirect agonist

51
Q

barbiturates increase the ______ of Cl- channel opening

52
Q

benzodiazepines increase the ______ of Cl- channel opening

53
Q

ethanol increases the ______ and ______ of Cl- channel opening, as well as increasing the number of channel _____

A

frequency and duration, number of channel bursts

54
Q

what class increase the DURATION of Cl- channel opening

A

barbiturates

55
Q

what class increases the DURATION of Cl- channel opening

A

Benzodiazepines

56
Q

which class increases BOTH (frequency and duration) of Cl- channel and increase the number of channel bursts

57
Q

ethanol and IV anesthetics are selective for GABAa receptors with what 2 subunits

A

beta 2 and beta 3

58
Q

what anti-convulsant inhibits GABA metabolism

A

Vigabatrin

59
Q

which anti-convulsant inhibits reuptake of GABA

60
Q

which CNS excitatory agent directly blocks the Cl- channel

A

Picrotoxin

61
Q

which CNS excitatory agent interferes with GABA binding

A

Bicuculline

62
Q

alpha 1 subunit effects/adverse effects

A

Sedation ONLY; has amnesia and abuse potential

63
Q

alpha 2 subunit effect/adverse effects

A

anxiolytic, muscle relaxation, anticonvulsant (NO sedation)

NO amnesia or abuse potential

64
Q

alpha 3 subunit effects/adverse effects

A

muscle relaxation ONLY, NO amensia/abuse

65
Q

alpha 5 subunit effect/adverse effects

A

muscle relaxation ONLY, amnesia potential (no abuse)

66
Q

which subunit is ONLY for sedation

67
Q

which 2 subunits are ONLY for muscle relaxation

A

alpha 3 and 5

68
Q

which class of drugs is selective for alpha 1

69
Q

which subunits do BZD bind to

A

alpha 1, 2, 3, 5

70
Q

receptors with alpha 4 or 6 subunits have HIGH affinity for what

A

partial inverse agonists (Ro 15-4513)

71
Q

receptors with alpha 4 or 6 subunits have SOME affinity for what

A

BZD receptor antagonist (Flumazenil)

72
Q

what was Ro 15-4513 pursued for

A

possible antidote to ethanol

73
Q

which is safer: benzodiazepines or barbiturates

A

benzodiazepines

74
Q

what should NOT be treated with benzodiazepines

A

PTSD (could worsen)

75
Q

what should not be used to treat PTSD

A

benzodiazepines

76
Q

benzodiazepines are a contributor to what in the elderly population

A

falls and injuries

77
Q

benzodiazepines are _________ with alcohol and barbiturates

A

synergistic

78
Q

effect of benzodiazepines on sleep

A

decrease time spent in stage 1, 3, 4, REM
increase time spent in stage 2
increase number of sleep cycles

79
Q

anticonvulsant effects of benzodiazepines are at what subunit

A

alpha 2 ONLY

80
Q

benzodiazepines inhibit neural signaling by _________ the hyper polarizing effects of GABA

A

increasing

81
Q

which 2 BZD are approved for LONG TERM treatment of seizures

A

clonazepam, clorazepate

82
Q

which 2 BZD have well defined roles in managing status epilepticus

A

diazepam, lorazepam

83
Q

abuse and dependence of BZD is more likely with _____ acting and ______ potency drugs

A

faster acting, higher potency

84
Q

many BZD have ________ metabolites with _____ half lives

A

psychoactive metabolites, with long half lives

85
Q

Z drugs bind only to what subunit

86
Q

3 Z-Drugs

A

zolpidem, zaleplon, eszopiclone

87
Q

Z-drugs are approved for use up to _____ days

88
Q

which Z-drug is most associated with parasomnias (sleep walking/talking)

89
Q

dose of Z-drugs should be reduced in who

90
Q

dose of Z-drugs should be ______ in females

91
Q

which Z drug is approved for LONG TERM treatment of insomnia

A

eszopiclone

92
Q

what is an adverse effect of eszopiclone

A

bitter taste

93
Q

what drug is used to rescue someone from a BZD overdose

A

Flumazenil

94
Q

Flumazenil is a

A

benzodiazepine receptor antagonist

95
Q

unique binding size of Flumazenil produces ______ with ____ binding site and ______ binding site

A

steric hindrance, BZD and Z-drug binding sites

96
Q

how are barbiturates classified

A

by duration of action

97
Q

ultra short acting barbiturates are given by

A

IV injection

98
Q

ultra short acting barbiturates are rapidly distributed to the _____ and cause ________ in 30-45 seconds

A

brain, unconsciousness

99
Q

peak concentration of ultra short acting barbiturates occurs at

100
Q

4 indications of barbiturates

A

seizures, anxiety, insomnia, anesthesia

101
Q

will Flumazenil treat a barbiturate overdose

102
Q

2 treatments for barbiturate overdose

A

activated charcoal, urinary alkalinization

103
Q

Ramlteon is a _________ receptor agonist. it is indicated for insomnia characterized by ____________

A

MELATONIN receptor agonist. insomnia characterized by difficulty with SLEEP ONSET

104
Q

Tasimelteon is a _______ receptor agonist. it is indicated for

A

MELATONIN receptor agonist. indicated for non-24 hour sleep wake disorder

105
Q

what drug is indicated for non-24 hour sleep wake disorder

A

Tasimelteon

106
Q

Buspirone is a full agonist at _______ ____ receptors and a partial agonist at _______ ____ receptors.

A

full agonist at PREsynaptic 5HT1a receptors

partial agonist at POSTsynaptic 5HT1a receptors

107
Q

Suvorexant is a _______ receptor antagonist.

A

OREXIN receptor antagonist

108
Q

the effects of _______ make take 1 week of treatment

109
Q

which non-GABA receptor drug does NOT potentiate effects of alcohol, does NOT show abuse potential

110
Q

which non-GABA drug has a risk for abuse, may potentiate effects of alcohol, and increases parasomnias

A

Suvorexant

111
Q

which drug is an orexin receptor antagonist

A

Suvorexant

112
Q

which drug is a 5HT1a receptor agonist

113
Q

non medical use of sedative hypnotics

A

drug facilitated sexual assult

114
Q

1 drug used for sexual assault

115
Q

what drug is also known as “roofies”

A

Flunitrazepam

116
Q

___mg of Flunitrazepam can impair a victim for 8-12 hours

117
Q

what drug is odorless, colorless, and tasteless that is used for sexual assaults

A

Flunitrazepam

118
Q

effects of Flunitrazepam are ______ by concurrent alcohol use

Pharmacology (5 decks)

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