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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

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
benzodiazepines addiction
GABA regulation of VTA DAergic neurons
26
benzodiazepines withdrawal
rebound insomnia (decrease dose slowly)
27
triazolam
slow-acting BZD (
28
temazepam, estazolam
intermediate-acting BZD (12-24hr) sleep maintenance insomnia conjugated w/glucuronide
29
flurazepam
long-acting BZD (>24hr) sleep onset and maintenance insomnia active metabolite
30
quazepam
long-acting BZD (>24hr) sleep maintenance insomnia
31
benzodiazepines absorption
lipophilic rapidly absorbed completely distributed
32
benzodiazepines metabolism
active metabolites: flurazepam inactive metabolites: triazolam conjugated: temazepam (safe for elderly, liver impaired)
33
benzodiazepines use
prolong stage 2 sleep suppress stage 3 and 4 sleep (SWS) suppress REM sleep, prolong REM latency
34
benzodiazepine other use
``` antiepileptic general anesthesia muscle relaxation anti-nausea, anti-vertigo alcohol withdrawal ```
35
benzodiazepine SE
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
benzodiazepine Rx interactions
potentiates opiates & sedatives
37
benzodiazepine OD
if given w/other CNS depressants Tx: flumazenil - rapid reversal of sedation, may cause SE in pts dependent on BZD
38
benzodiazepine contraindications
h/o alcoholism or drug abuse liver impairment elderly (lower dose)
39
selective BZD receptor agonists (Z drugs)
rapid onset, short duration less tolerance, dependence, abuse doesn't affect stage 4 sleep
40
Z drug MOA
selectively bind alpha1 subunits of GABA-A receptor (sedation, amnesia)
41
zolpidem
Z drug short-term insomnia (sleep onset) 30min onset 2.5hr duration inactive metabolites (CYP3A) SE: somnolence, amnesia
42
zaleplon
Z drug short-term insomnia (sleep onset and maintenance) 30min onset 1hr duration inactive metabolites (CYP3A) SE: drowsiness, Rx interactions
43
eszopiclone
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
barbiturates
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
melatonin receptor agonists
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
ramelteon
melatonin receptor agonist sleep onset insomnia first-pass metabolism CYP1A2 t1/2 = 1-3hr SE: somnolence, increase serum prolactin
47
tasimelteon
melatonin receptor agonist non 24-hr sleep disorder first-pass metabolism CYP1A2, CYP3A4 t1/2 = .5-3hrs Rx interactions: CYP1A2 (fluvoxamine), CYP3A4 (ketoconazole)
48
suvorexant
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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