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neuro > sedatives hypnotics > Flashcards

sedatives hypnotics Flashcards

1
Q

sedative

A

reduce anxiety, produce calming effect w/o impairing mental function

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2
Q

sedative

A

reduce anxiety, produce calming effect w/o impairing mental function

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3
Q

hypnotic

A

produce state of drowsiness, facilitate onset/maintenance of sleep

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4
Q

sleep function

A

restoration/repair

optimize storage of memories

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5
Q

sleep stages (ultradian rhythm)

A

90min, 4-5/night

1 - transition
2 - longest
3 - sort deep delta wave sleep SWS
4 - long deep delta wave sleep SWS
5 - REM
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6
Q

sleep initiation

A

time to fall asleep (30min)

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7
Q

hypnotic

A

produce state of drowsiness, facilitate onset/maintenance of sleep

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8
Q

sleep function

A

restoration/repair

optimize storage of memories

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9
Q

sleep stages (ultradian rhythm)

A

90min, 4-5/night

1 - transition
2 - longest
3 - sort deep delta wave sleep SWS
4 - long deep delta wave sleep SWS
5 - REM
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10
Q

sleep initiation

A

time to fall asleep (30min)

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11
Q

sleep efficiency

A

time sleeping / time in bed (>85%)

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12
Q

arousal pathway

A

cholinergic, aminergic, orexin

tuberomammillary nucleus
locus coeruleus
dorsal raphe nucleus

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13
Q

sleep promoting pathway

A

GABA

VLPO

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14
Q

orexin

A

stabilized sleep/wake transition

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15
Q

GABA

A

inhibitory

sleep induction/maintenance
executive functions

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16
Q

melatonin

A

secreted from pineal gland in darkness

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17
Q

dyssomnias

A

disturbance in normal rhythm/pattern of sleep

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18
Q

parasomnias

A

sleep terrors, nightmares, sleep walking

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19
Q

insomnia S/S

A

delayed sleep onset
early morning wake-ups
unrefreshing sleep
trouble maintaining sleep

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20
Q

transient insomnia

A
21
Q

short-term insomnia

A

3days-3wks
personal stressor
Tx: intermittent hypnotics

22
Q

chronic insomnia

A

> 3wks
no identifiable stressor
Tx: complete medical evaluation

23
Q

ideal hypnotic

A

no active metabolites
rapid sleep induction
sleep maintenance
no adverse effects

24
Q

benzodiazepines MOA

A

bind allosteric site on GABA-A receptor complex, increase frequency of channel openings, increase affinity of GABA for receptor

25
Q

benzodiazepines addiction

A

GABA regulation of VTA DAergic neurons

26
Q

benzodiazepines withdrawal

A

rebound insomnia (decrease dose slowly)

27
Q

triazolam

A

slow-acting BZD (

28
Q

temazepam, estazolam

A

intermediate-acting BZD (12-24hr)

sleep maintenance insomnia

conjugated w/glucuronide

29
Q

flurazepam

A

long-acting BZD (>24hr)

sleep onset and maintenance insomnia

active metabolite

30
Q

quazepam

A

long-acting BZD (>24hr)

sleep maintenance insomnia

31
Q

benzodiazepines absorption

A

lipophilic
rapidly absorbed
completely distributed

32
Q

benzodiazepines metabolism

A

active metabolites: flurazepam
inactive metabolites: triazolam
conjugated: temazepam (safe for elderly, liver impaired)

33
Q

benzodiazepines use

A

prolong stage 2 sleep
suppress stage 3 and 4 sleep (SWS)
suppress REM sleep, prolong REM latency

34
Q

benzodiazepine other use

A 
antiepileptic
general anesthesia
muscle relaxation
anti-nausea, anti-vertigo
alcohol withdrawal
35
Q

benzodiazepine SE

A

CNS - somnolence, drowsiness, sedation
pregnancy - cross placental barrier, cleft palate (1st trimester), floppy infant syndrome (3rd trimester)
elderly - confusion, amnesia, falls, fractures
paradoxical psychological effects - excitement, anxiety, mild euphoria, hallucinations

36
Q

benzodiazepine Rx interactions

A

potentiates opiates & sedatives

37
Q

benzodiazepine OD

A

if given w/other CNS depressants

Tx: flumazenil - rapid reversal of sedation, may cause SE in pts dependent on BZD

38
Q

benzodiazepine contraindications

A

h/o alcoholism or drug abuse
liver impairment
elderly (lower dose)

39
Q

selective BZD receptor agonists (Z drugs)

A

rapid onset, short duration
less tolerance, dependence, abuse
doesn’t affect stage 4 sleep

40
Q

Z drug MOA

A

selectively bind alpha1 subunits of GABA-A receptor (sedation, amnesia)

41
Q

zolpidem

A

Z drug

short-term insomnia (sleep onset)
30min onset
2.5hr duration

inactive metabolites (CYP3A)

SE: somnolence, amnesia

42
Q

zaleplon

A

Z drug

short-term insomnia (sleep onset and maintenance)
30min onset
1hr duration

inactive metabolites (CYP3A)

SE: drowsiness, Rx interactions

43
Q

eszopiclone

A

Z drug

insomnia (sleep maintenance)
alpha1 and alpha 3 (on switch)
30min onset
6hr duration

metabolized by CYP3A4

SE: rebound insomnia, unpleasant taste, dry mouth, drowsiness, Rx interaction

44
Q

barbiturates

A

selectively bind GABA-A receptor at allosteric site, prolonging duration of Cl- channel opening

SE: P450 inducers, low therapeutic index, high potential for dependence/abuse

45
Q

melatonin receptor agonists

A

maintain circadian rhythms

selectively binds MT1 (sleepiness) and MT2 (phase-shifting) receptors in SCN

metabolized by CYP3A

less abuse, tolerance, dependence, doesn’t affect stage 4 sleep

46
Q

ramelteon

A

melatonin receptor agonist

sleep onset insomnia

first-pass metabolism CYP1A2

t1/2 = 1-3hr

SE: somnolence, increase serum prolactin

47
Q

tasimelteon

A

melatonin receptor agonist

non 24-hr sleep disorder

first-pass metabolism CYP1A2, CYP3A4

t1/2 = .5-3hrs

Rx interactions: CYP1A2 (fluvoxamine), CYP3A4 (ketoconazole)

48
Q

suvorexant

A

orexin receptor antagonist

selectively blocks binding of orexin to OX1 and OX2 receptors

improves sleep inset, reduces sleep maintenance

t1/2 = 12hr

SE: daytime sleepiness

neuro (12 decks)

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