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Therapeutics 3 - Spring 2018 > Exam 4 - Sedative/Hypnotics/Anxiety (Watts/Ott) > Flashcards

Exam 4 - Sedative/Hypnotics/Anxiety (Watts/Ott) Flashcards

1
Q

Definition of Sedative

A

calms anxiety
decreases excitement/activity
does NOT produce drowsiness or impair performance

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2
Q

Definition of Hypnotic

A

induces sleep!!

implies restful/refreshing sleep

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3
Q

Definition of Anxiolytic

A

Anti-anxiety
relieves anxiety w/out sleep or sedation
(*not all anxiolytics are sedatives….)

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4
Q

Definition of Narcotic

A

actually means “sleep producing”

noooow refers to opioids or illegal drugs

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5
Q

Reticular Formation:

regulates ________ and ___________

A

sleep-wake transitions
and
synchronization of EEG

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6
Q

Reticular Formation:

intricate system composed of __________ in what is otherwise _______

A

loosely clustered neurons

white matter

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7
Q

3 stages of Sleep

A

Wakefulness
Slow-wave sleep (NREM)
Paradoxic sleep (REM)

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8
Q

what are the stages of NREM Sleep

A

stage 1: dozing
stage 2: unequivocal sleeo
stage 3: voltage increase/frequency decrease
stage 4: delta waves

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9
Q

NREM Sleep Stages:

what is stage 1?

A

dozing

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10
Q

NREM Sleep Stages:

what is stage 2?

A

unequivocal sleep (asleep but easily awaken)

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11
Q

NREM Sleep Stages:

what is stage 3?

A

voltage increase/frequency decrease

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12
Q

NREM Sleep Stages:

what is stage 4?

A

delta waves

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13
Q

what are the GABA receptor subtypes

A

alpha 1
alpha 2
alpha 3
alpha 5

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14
Q

what GABA receptor subtype is most prevalent (~50%)

A

alpha 1

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15
Q

GABA alpha 1 receptors used to be known as _____ receptors

A

BZ1

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16
Q

GABA alpha 2, 3, 5 receptors used to be known as _____ receptors

A

BZ2

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17
Q

where are GABA alpha 1 receptors found

A

ubiquitous (anywhere in da brain)

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18
Q

where are GABA alpha 2 receptors found

A

cortex; limbic system; spinal cord

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19
Q

where are GABA alpha 3 receptors found

A

cortex; limbic system; spinal cord

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20
Q

where are GABA alpha 5 receptors found

A

Hippocampus

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21
Q

GABA alpha 1 receptor has roles in what?

A

sedation
anti-convulsion
amnesia
addiction

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22
Q

GABA alpha 2 receptor has roles in what?

A

anxiolytic

muscle relax

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23
Q

GABA alpha 3 receptor has roles in what?

A

muscle relaxation

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24
Q

GABA alpha 5 receptor has roles in what?

A

muscle relaxation

amnesia

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25
Q

T or F: GABA(A) receptor is pentameric

A

truuuue

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26
Q

GABA(A) receptor what are the subunits of it

A

2 alpha
2 beta
1 gamma
(5 total!!)

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27
Q

Does it bind on the orthosteric or allosteric site on GABA receptor?
GABA

A

orthosteric

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28
Q

Does it bind on the orthosteric or allosteric site on GABA receptor?
BZD

A

allosteric

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29
Q

Does it bind on the orthosteric or allosteric site on GABA receptor?
barbiturate

A

allosteric

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30
Q

Does it bind on the orthosteric or allosteric site on GABA receptor?
ethanol

A

allosteric

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31
Q

Does it bind on the orthosteric or allosteric site on GABA receptor?
glucocorticoid

A

allosteric

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32
Q

BZDs or Barbiturates have “internal safety system”

A

BZDs!! (why slightly safer than barbiturates)

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33
Q

what ligands act at the BZD receptor on GABA receptor…..

A

BZDs…
non-BZDs (zolpidem, zaleplon, eszopiclone)
BZD antagonist: flumazenil
BZD inverse agonist: B carboline

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34
Q

what drug is a GABA channel blocker

A

Picrotoxin

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35
Q

BZDs increase ______ of channel opening
vs
Barbiturates increase ______ of channel opening

A

BZD: frequency

Barbiturates: duration

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36
Q

how does alcohol work at the GABA receptor?

A

enhances actions of GABA at GABA(A) receptor

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37
Q

what are the 2 structure activity relationships we need to know for BZDs

A

1 Position alkylation leads to source of active metabolites
and
annealating the 1-2 bond with an electron rich ring yields high affinity and decrease half life

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38
Q

BZD and Structure activity

annealating the ___ bond with an electron rich ring yields ____ affinity and _____ half life

A

1-2 bond
HIGH affinity
DECREASE half life

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39
Q

BZDs with ______ elimination rates all have active metabolites

A

slow

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40
Q

what BZDs have slow elimination rates

A 
Chlordiazepoxide
Diazepam
Flurazepam
Clorazepate
Quazepam
Prazepam
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41
Q

what BZDs have intermediate elimination rates

A 
alprazolam
lorazepam
clonazepam
oxazepam
temazepam
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42
Q

what BZDs have rapid elimiation rates

A

Midazolam

Triazolam

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43
Q

BZDs that are slowly or intermed./rapidly eliminated are useful in pts who “wake up”

A

slowly

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44
Q

BZDs that are slowly or intermed./rapidly eliminated are preferable in elderly pts?

A

intermed/rapid

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45
Q

BZDs that are slowly or intermed./rapidly eliminated are preferable in pts with hepatic problems?

A

interm/rapid

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46
Q

BZDs that are slowly or intermed./rapidly eliminated are known to have rapid tolerance

A

intermed/rapid

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47
Q

BZDs that are slowly or intermed./rapidly eliminated are known to cause rebound insomnia

A

intermed/rapid

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48
Q

BZDs that are slowly or intermed./rapidly eliminated are known to have active metabolites

A

slow

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49
Q

BZDs that are slowly or intermed./rapidly eliminated are known to have accumulation

A

slow

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50
Q

General Considerations for BZDs:

Readily absorbed or delayed absorption?

A

readily absorbed!

thus can be delayed by food!!

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51
Q

General Considerations for BZDs:

Increased ______ solubility will increase speed of delivery to brain

A

lipid

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52
Q

General Considerations for BZDs:

redistribution to highly perfused tissue may _______ duration of action

A

decrease (more high perfusion = less at brain!!)

53
Q

General Considerations for BZDs:

T or F: cant cross placental barrier/is not detectable in breast milk

A

false!! it can cross placenta and get in breast milk

54
Q

General Considerations for BZDs:

has _______ binding — NOT clinically relevant though

A

extensive protein

55
Q 
BZDs: Pharmacological Properties:
For Sleep Physiology:
\_\_\_\_\_ sleep latency
\_\_\_\_\_\_ total sleep time
\_\_\_\_\_\_ stage 2
\_\_\_\_\_ REM
\_\_\_\_\_\_ stage 3 and 4

(increase or decrease in each blank?)

A

reduce latency

increase total time

increase stage 2

decrease REM

decrease stage 3 and 4

56
Q

BZDs: Pharmacological Properties:

does it increase or decrease stage 2

A

increase

57
Q

BZDs: Pharmacological Properties:

does it increase or decrease stages 3 and 4

A

decrease

58
Q

BZDs: Pharmacological Properties:

does it increase or decrease REM

A

decrease

59
Q

BZDs: Pharmacological Properties:

does it increase or decrease sleep latency

A

decrease

60
Q

BZDs: Pharmacological Properties:

does it increase or decrease total sleep time

A

increase

61
Q

what drug can be used for BZD overdose

A

Flumazenil

62
Q

2 big side effects with Flumazenil

A

Induce convulsions

Panic Attacks

63
Q

what drugs are “z-hypnotics”

A

zolpidem
Zaleplon
Eszopiclone

64
Q

Z-Hypnotics act a ______ binding site/_____ receptor

A

BZD;

BZ1

65
Q

what Z-hypnotic is approved for long term use

A

Eszopiclone

66
Q

what Z-hypnotics is approved for short term use

A

zolpidem

zaleplon

67
Q

how to treat overdose of Z-hypnotics

A

flumazenill! (same as BZD)

68
Q

BZD or Z-hypnotics

which one cases less negative effects on sleep patterns

A

Z-hypnotics…why used for sleep more

69
Q

ultra short acting, short/intermediate, or long acting barbiturates?
are used as anticonvulsants

A 
long acting 
(Phenobarbitol, mephobarital)
70
Q

ultra short acting, short/intermediate, or long acting barbiturates?
are used as sedative hypnotics?

A

short/intermediate

71
Q

ultra short acting, short/intermediate, or long acting barbiturates?
are used as IV anesthetics?

A

ultra short acting

thiopental, methohexital, thiamylal

72
Q

Barbiturates:

Has serious ADEs of ______ depression and ______ depression

A

cariodvascular; respiratory

73
Q

PK of Barbiturates:

duration of action is _______ proportional to lipid solubility

A

directly

74
Q

GABA(B) receptors:

is a G______ coupled receptor,

A

Gi/o

75
Q

GABA(B) receptors:

Heterodimer or homodimer

A

heterodimer (two related seven transmembrane domain receptor subunits)

76
Q 
GABA(B) receptors: 
act inhibitory by....
Presynaptic ---> \_\_\_\_\_\_ conductance
and
Postsynaptic ---> \_\_\_\_\_\_ conductance
A

pre: decrease Ca2+
post: increase K+

(aka overall makes cell more negative = inhibitory)

77
Q

what are some GABA(B) agonists

A

GHB

baclofen

78
Q

what are the GABA(B) antagonists

A

phaclofen, saclofen, 2-hydroxysaclofen

79
Q

what are the subtypes of GABA(B)

A

GABA(B)1
and
GABA(B)2
….

80
Q

what is the name of the Rx drug of GHB

A

Sodium Oxybate
or
Xyrem

81
Q

Concerns of using Xyrem/GHB

A

no antagonist available
use of other sedative-hypnotics
amnesia
date rape

82
Q

MOA of Ramelteon?

A

high affinity of MT1 and MT2 melatonin receptors

receptors are in SCN (superchiasmatic nucleus)

83
Q

what is known as the “master clock” of the body and is known to regulate circadian rhythms?

A

SCN (superchiasmatic nucleus)

84
Q

metabolism of ramelteon?

A

CYP1A2

85
Q

brand for ramelteon?

A

Rozerm

86
Q

what other drug is known as a melatonin agonist? (not ramelteon)

A

Tasimelteon (Hetiloz)

87
Q

why is ramelteon a good option

A

no abuse/withdrawal/dependency

negligible risk for hangover effect next day

88
Q

Orexin is known to cause wakefullness or sleepiness?

A

wakefullness

89
Q

what drug is an orexin receptor antagonist

A

Suvorexant (belsomra)

90
Q

what is brand for suvorexant

A

belsomra

91
Q

MOA for suorexant

A

antagonists for OX1 and OX2 orexin receptors

92
Q

what drugs can cause anxiety

A

cocaine
beta agonists
psychostimulants (caffeine)
corticosteroids

93
Q

what diseases can cause anxiety

A

CHF
COPD
diagnosis of terminal diseases

94
Q

how is NE related to anxiety

A

NE stimulates autonomic nervous system

NE is seen to be dysregulated in GAD and other types of anxiety

95
Q

how is serotonin related to anxiety?

A

involves amygdala(emotions) and NE

96
Q

4 main tx options of ranxiety

A

BZDs
Antidepressants
Buspirone
Beta blockers

97
Q

Buspirone is a partial agonist for _____ receptor s and has moderate affinity for _____ receptors`

A

5HT1A

D2

98
Q

Diagnostic criteria for insomnia disorder

A

present for at least 3 mos
takes place at least 3 nights per week
primary complaint of unsatisfying sleep quantity or quality
difficulties with sleep initiation (latency); sleep maintenance, and/or early morning awakening

99
Q

Duration of Insomnia Disorders:

Episodic: lasting _____?

A

1 month to less than 3 mos

100
Q

Duration of Insomnia Disorders:

Persistent: lasting ______?

A

greater than 3 months

101
Q

Duration of Insomnia Disorders:

Recurrent: experiencing?

A

2 or more episodes during 1 year

102
Q

Diagnostic criteria for insomnia disorder:
present for at least _____
takes place at least ______ per week

A

3 mos

3 nights

103
Q

1st line tx for insomnia?

A

non-pharm: behavioral therapies/sleep restriciton therapy/relaxation training
SLEEP HYGIENE!!!

104
Q

what are the main options for insomnia?

A

z-hypnotics (most popular)
BZDs
Melatonin Agonists
Doxepin

105
Q

BZDs and Insomnia:

longer acting agents can cause significant ______

A

daytime hangover

106
Q

BZDs and Insomnia:

T or F: Any BZD can be used for insomnia

A

Truueeee

107
Q

BZDs and Insomnia:
MUST consider tapering when discontinuing!!
to avoid ___________
tapering can take up to _______

A

avoid life threatening withdrawal/seizures

4 months

108
Q

Melatonin Agonists are good for sleep ______

A

latency/initiation

109
Q

per AASM Guidelines: (aka sleep medicine)

what drugs are used for sleep maintenance ONLY

A

suvorexant

doxepin

110
Q

per AASM Guidelines: (aka sleep medicine)

use for sleep onset ONLY

A

zaleplon
triazolam
ramelteon

111
Q

suvorexant is known to block the binding of wake promoting neuropeptides known as _______ and _____ which is thought to suppress the “______”

A

orexin a and orexin b

wake drive

112
Q

how do you dose suvorexant?

A

10 mg 30 mins before bed — need at least 7 hours left to sleep!!

may increase to 20 mg

113
Q

Big caution for suvorexant?

A

daytime somnolence risk
(10 mg: caution for impaired driving risk the next day
if 20mg: literally dont freakin drive)

114
Q

can nacrolepsy pts use suvorexant?

A

hell nah!

could cause paralysis/hypnogogic/hypnopompic hallucinations and cateplexy

115
Q

CYP interaction with suvorexant

A

3A4 substrate

116
Q

Diagnostic criteria for sleep apnea

A

pts must have evidence of least 5 obstructive apneas per hour of sleep (confirmed by polysomnography)
plus nocturnal breathing disturbances OR daytime sleepiness
OR
evidence of 15 or more obstructive apneas per hous of sleep regardless of other symptoms (confirmed by polysomnography)

117
Q

if apnea and insomnia - what do you treat first?

A

apnea; b/c they cant breathe,dawg

118
Q

Tx of sleep apnea

A

weight loss
CPAP
tx excessive daytime sleepiness with modafinil or armodafinil (also review CPAP adherence)
surgery is an option

119
Q

Diagnostic criteria for Narcolepsy

A

recurring episodes of irresistible need to sleep, fall asleep, or nap:
3 x per week over past 3 mos
AND at least one of the following:
- cataplexy episodes
- hypocretin deficiency
- REM sleep latency < 15 mins on night w/ polysomnography (and other things with lots a numbers that I dont want to learn yet :( )

120
Q

mild narcolepsy = ?

A

infrequency cataplexy attacks (<1 per week)

121
Q

moderate narcolepsy?

A

cataplexy attacks daily or every few days
and/or(?)
nocturnal sleep disturbances

122
Q

severe narcolepsy?

A

cataplexy seen as drug resistant w/ multiple attacks per day
almost constant sleepines…
and
nocturnal sleep disturbances

123
Q

what drug is used to treat cataplexy

A

Xyrem (sodium oxybate) GHB

124
Q

how is sodium oxybate taken

A

dosed twice per night

first dose right before bed; second dose is 3 - 4 hours later

125
Q

black box warning for sodium oxybate

A

respiratory depression and misuse risk

126
Q

what drugs can be used for the excessive daytime sleepiness

A

methylphenidates/amphetamine stuff
modfainil/armodafinil
sodium oxybate
selegiline (gets metabolized to amphetamine)

127
Q

how to pharmacologically treat shift sleep work disorder

A

take armodafinil/modafinil 1 hour before work period starts during “wake time”

128
Q

Drug therapy options for RLS (restless leg syndrome)

A 
dopamine agonists 1st line!! (pramipexole, ropinirole)
maybe LD/CD
horizant (gabapentin enacarbil)
NO opiods!!
iron supplement IF iron deficient
maybe clonazepam

Therapeutics 3 - Spring 2018 (20 decks)

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