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Block 6 > Sedative Hypnotics > Flashcards

Sedative Hypnotics Flashcards

1
Q

progression of sedative hypnotics

A 
anxiolysis
sedation
hypnosis
anesthesia
death
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2
Q

use of barbiturates

A

induce anesthesia

rarely used

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3
Q

use of benzodiazepines

A

anxiety
insomnia
epilepsy

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4
Q

use of non-benzodiazepines (z drugs)

A

insomnia

safest for use

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5
Q

GABA receptor for sedative/hypnotic

A

alpha1

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6
Q

GABA receptor for anxiolytic and muscle relaxant

A

alpha2

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7
Q

GABA receptor for anticonvulsant

A

alpha3

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8
Q

GABA receptor for amnesia

A

alpha5

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9
Q

barbiturate action at GABA receptor

A

increase duration of opening

increases efficacy of GABA

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10
Q

benzodiazepine action at GABA receptor

A

increase frequency of opening

increases potency of GABA

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11
Q

barbiturates to recognize

A

thiopental
pentobarbital
amobarbital
phenobarbital

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12
Q

thopental

A

short acting barbiturate

used for amnesia prior to surgery

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13
Q

phenobarbital

A

long acting barbiturate

used for seizures

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14
Q

side effects of barbiturates

A

dose dependent respiratory depression
induction of liver enzymes
low margin of safety
increases porphyrin production- do not use with porphyria

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15
Q

benzodiazepine side effects/toxicity

A

tolerance to sedation and euphoria
cross tolerance with other CNS depressants
physical dependence- withdrawal symptoms

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16
Q

advantages of benzo use for insomnia over barbiturates

A

higher margin of safety than barbiturates- plateaus before bad effects
no cyp induction
milder withdrawal

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17
Q

therapeutic use of bentos #1

A 
insomnia- reduces time to sleep and increases total sleep time
moderate REM decrease
increase stage 2
decrease stage 4
REM rebound when ended
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18
Q

flurazepam half life

A

40-100 (longest)

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19
Q

flurazepam use

A

short term mild/moderate insomina

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20
Q

flurazepam activity

A

prodrug

peak metabolite plasma concentration 1-3h

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21
Q

flurazepam delivery/absorption

A

good absorption orally

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22
Q

lorazepam half life

A

10-20hours

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23
Q

lorazepam use

A

short term mild/moderate insomnia with anxiety

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24
Q

lorazepam activity

A

slow

no active metabolites

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25
Q

lorazepam delivery/absorption

A

oral- slow

IM- good

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26
Q

temazepam half life

A

10-40h

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27
Q

temazepam use

A

short term severe insomina

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28
Q

temazepam delivery/absorption

A

slow and erratic oral absorption

29
Q

temazepam warnings

A

distorts normal sleep pattern

do not use during pregnancy

30
Q

triazolam half life

A

short term acute insomnia (jet lag)

**doesn’t work for frequent awakenings

31
Q

triazolam activity

A

fast acting- peak plasma levels 1h

32
Q

triazolam delivery/absorption

A

good oral

33
Q

triazolam warnings

A

higher abuse potential (fast acting)

more severe withdrawal with chronic use

34
Q

use #2 of benzos

A

amnesia during anesthesia for procedures

35
Q

midazolam

A

benzo for amnesia
short term use
half life 2-6h

36
Q

benzo overdose treatment

A 
maintain respiration
rule out narcotics by giving naloxone
gastric lavage
hemodialysis
flumazenil
37
Q

naloxone

A

drug for narcotic overdose

38
Q

flumazenil

A

benzo antagonist that reverses respiratory depression
very short acting- requires close monitoring
causes withdrawal symptoms

39
Q

do not give flumazenil to

A

seizure history
barbiturate or TCA overdose
careful with ethanol intoxication

40
Q

z drugs

A

benzodiazepine receptor agonsits

41
Q

insomnia drugs with highest margin of safety

A

z drugs

42
Q

MOA of z drugs

A

interacts with alpha1 receptors

43
Q

z drug that is non selective

A

eszopiclone

44
Q

effects of z drugs

A

hypnosis with little muscle relaxant or anticonvulsant effects

45
Q

use of z drugs

A

decrease latency without affecting sleep cycles

46
Q

why are z drugs better than benzos

A

less: anti anxiety, anticonvulsant, muscle relaxant, impact on REM sleep

47
Q

z drug metabolism

A

liver

change dose for elderly and liver disease

48
Q

3 z drugs

A

zolpidem
zaleplon
eszopiclone

49
Q

zolpidem half life

A

2-2.5h

medium duration

50
Q

zolpidem form

A

tablet
controlled release tablet
sublingual, lingual

51
Q

zolpidem metabolism

A

CYP 3A4

52
Q

zolpidem ADR

A

dizziness
diarrhea
GI irritation

53
Q

zolpidem residual sleepiness

A

confusion and falls in elderly

memory impairment at high doses

54
Q

zaleplon half life

A

1h
shorts duration
approved for use during night

55
Q

zaleplon metabolism

A

aldehyde oxidase- works in patients with liver dysfunction

56
Q

zaleplon ADR

A

impaired fertility

color disturbances

57
Q

zaleplon tolerancee

A

rebound insomnia at high doses

58
Q

eszopiclone half life

A

6h

longest duration

59
Q

eszopiclone metabolism

A

CYP 3A4

60
Q

eszopiclone ADR

A

taste disturbance

xerostomia

61
Q

eszopiclone residual sleepiness

A

next day memory impairment
psychomotor impairment
rebound insomnia

62
Q

z drugs causing rebound insomina

A

zaleplon

eszopiclone

63
Q

longest duration z drug

A

eszopiclone

64
Q

shortest duration z drug

A

zaleplon

65
Q

CYP 3A4 metabolized z drugs

A

zolpidem

eszopiclone

66
Q

suvorexant

A

orexin receptor antagonist used for insomina

67
Q

ramelteon

A

synthetic melatonin- against at SCM MT1 and MT2 receptors

68
Q

do not give sedative-hypnotics to

A

obstructive sleep apnea

Block 6 (24 decks)

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