Insomnia Flashcards

1
Q

what NT keep you alert

A

NE

Ach

dopamine

histamine

hypocretin/orexin

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2
Q

what NT make you sleepy

A

adenosine

GABA

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3
Q

what drugs make you sleepy

A

anticholinergic

antihistamines

benzos

suvorexant

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4
Q

what meds keep you awake

A

amphetamines

adenosine antagonists

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5
Q

order of tx for insomnia

A
  1. address underlying causes
  2. assess for stimulating drugs
  3. CBT
  4. drugs
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6
Q

underlying causes of insomnia

A

sleep apnea

pain

RLS

anxiety/dpn

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7
Q

stimulating meds that might cause insomnia

A

caffeine

decongestants

stimulants

SSRIs

diuretics

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8
Q

preferred tx for insomnia

A

CBT

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9
Q

first line pharm for insomnia

A

nonbenzos → zolpidem, rameleton

short acting benzos → tamezepam

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10
Q

ability of drug to rapidly induce sleep is influenced by

A

rate of absorption

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11
Q

ability to maintain sleep is influenced by

A

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12
Q

rebound insomnia is caused by __

and influenced by __

A

abrupt d/c

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13
Q

what drug is first line for insomnia

A

zolpidem - ambien → “z drug”

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14
Q

3 z drugs to know

A

zolpidem → ambien

eszopiclone → lunesta

zaleplon → sonata

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15
Q

4 other drug agents for insomnia besides z drugs

A

benzos

orexin antagonists

melatonin agonists

1st gen antihistamines

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16
Q

2 benzos used for insomnia

A

temazepam → restoril

triazolam → halcion

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17
Q

orexin antagonist to know

A

suvorexant → belsomra

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18
Q

melatonin agonist to know

A

ramelteon → rozerem

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19
Q

2 1st gen antihistamines to know

A

diphenhydramine

doxylamine → Nyquil

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20
Q

t/f: there is no receptor for benzos

A

T!

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21
Q

where do benzos bind

A

binding site on GABA chloride channel

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22
Q

which drugs bind to alpha 1 subunit

A

benzos

z drugs

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23
Q

alpha 1 is located in the __

and has __ therapeutic action (2)

A

cortex

sleep/anticonvulsant

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24
Q

negative effects associated w. alpha 1 activation (benzos and z drugs)

A

amnesia

additive CNS dpn

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25
Q

which drug binds to alpha2 and alpha5 subunits

A

benzos

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26
Q

alpha 2 and 5 subunits are located in the (2)

and have __ therapeutic actions (2)

A

limbic system/brain stem

anxiolytic myorelaxant

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27
Q

negative effects related to alpha 2 and 5 subunit activation (benzos)

A

motor incoordination

tolerance/dependence

addiction

decreased REM

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28
Q

which chloride subunit do both benzos AND z drugs bind to

A

alpha 1

29
Q

z drugs bind only to __ Cl subunit

benzos bind to __ subunits (3)

A

z drugs: alpha 1

benzos: alpha1, alpha2, alpha5

30
Q

tolerance to benzos occurs if used > __

A

1 week

31
Q

benzos, etoh, and barbs all negatively affect which stage of sleep

A

REM

32
Q

z drugs are rapidly absorbed and eliminated via __ meatbolism

A

hepatic

33
Q

which sleep drug has the longest t½

A

escopiclone → lunesta

34
Q

most widely prescribed agent for insomnia

A

zolpidem → ambien

35
Q

immediate release ambien is used to

A

reduce sleep latency

36
Q

sustained release ambien (CR) is used to

A

reduce nocturnal awakenings

37
Q

low dose sublingual ambien (intermezzo) is used for

A

middle of the night awakening

38
Q

which z drug is safe for long term use

and used for sleep maintenance

A

escopiclone → lunesta

39
Q

which z drug has minor role in insomnia, but is used to decrease time to sleep onset

A

zalepon → sonata

rapid oral onset

40
Q

common s.e of z drugs

A

drowsiness

amnesia

HA

GI

rarely bizarre behavioral disturbances

41
Q

what class are Z drugs

A

IV

42
Q

is dependence-withdrawal likely w. z drugs

A

yes, but unlikely

43
Q

fatal overdoses are rare w. z drugs and benzos, unless

A

taken in combo w. other CNS depressants

44
Q

what 2 benzos are used for insomnia

A

triazolam → halcion

temazepam → restoril

45
Q

t½ of:

triazolam:

temazepam:

A

trazolam: short
temazepam: intermediate

46
Q

which benzo used for insomnia can cause rebound insomnia

A

triazolam (halcion)

d.t rapid elimination

47
Q

which benzo has minimal effect on sleep latency

A

temazepam

dt longer t½

48
Q

triazolam has less __

but more __

A

daytime sedation

rebound insomnia

dt short t½

49
Q

benzos have declining use for insomnia due to

A

daytime sedation/performance impairment

rebound insomnia

anterograde amnesia

psychologic and physiologic dependence

50
Q

4 insomnia drugs w. non GABA benzo binding site mechanisms

A

suvorexant

ramelteon

antidepressants

antihistamines

51
Q

hypothalamic neuropeptides that innervate all arousal systems and fxn to maintain wakefulness

A

orexins

52
Q

what insomnia drug is an orexin antagonist

A

suvorexant

53
Q

ADR of suvorexant

A

dose related next-day somnolence

54
Q

what class is suvorexant

A

IV → abuse liability

55
Q

suvorexant is FDA approved for __

but is really only used when __

A

sleep-onset/maintenance

first line drugs have failed

56
Q

what insomnia drug is an agonist a melatonin receptors

A

ramelteon

57
Q

MT1 receptor fxn:

MT2 receptor fxn:

A

MT1: induces sleep

MT2: regulates circadian rhythms

58
Q

ADRs of ramelteon

A

dizziness

somnolence

fatigue

nausea

59
Q

ramelteon is used for:

but melatonin may be better for:

A

reducing sleep latency

jet lag

60
Q

what insomnia drug is a serotonin receptor antagonist and reuptake blocker

A

trazodone

61
Q

ADRs of trazodone

A

oversedation

orthostasis

priapism

62
Q

what class of drug is trazodone

A

antidepressant → SARI

63
Q

pro of trazodone

A

no concerns w. tolerance or dependence

64
Q

what insomnia drug is an antagonist at CNS histamine H-1 and muscarinic receptors

A

diphenhydramine - doxylamine

65
Q

diphenhydramine/doxylamine might not be best for elderly due to what ADR

A

antimuscarinic

66
Q

3 first line drugs for sleep onset

A

zeleplon → z drug

zolpidem → z drug

ramelton → melatonin receptor agonist

67
Q

1st line for sleep onset and maintenance

A

zolpidem CR (extended release) → z drug

eszopiclone → z drug

68
Q

2nd line for insomnia:

adjunctive for insomnia:

A

2nd line: trazodone → antidepressant

+/- temazepam

adjunctive: melatonin, diphenhydramine → antihistamine