Sedative Hypnotics Flashcards Preview

Block 6 > Sedative Hypnotics > Flashcards

Flashcards in Sedative Hypnotics Deck (68):
1

progression of sedative hypnotics

anxiolysis
sedation
hypnosis
anesthesia
death

2

use of barbiturates

induce anesthesia
rarely used

3

use of benzodiazepines

anxiety
insomnia
epilepsy

4

use of non-benzodiazepines (z drugs)

insomnia
safest for use

5

GABA receptor for sedative/hypnotic

alpha1

6

GABA receptor for anxiolytic and muscle relaxant

alpha2

7

GABA receptor for anticonvulsant

alpha3

8

GABA receptor for amnesia

alpha5

9

barbiturate action at GABA receptor

increase duration of opening
increases efficacy of GABA

10

benzodiazepine action at GABA receptor

increase frequency of opening
increases potency of GABA

11

barbiturates to recognize

thiopental
pentobarbital
amobarbital
phenobarbital

12

thopental

short acting barbiturate
used for amnesia prior to surgery

13

phenobarbital

long acting barbiturate
used for seizures

14

side effects of barbiturates

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

15

benzodiazepine side effects/toxicity

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

16

advantages of benzo use for insomnia over barbiturates

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

17

therapeutic use of bentos #1

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

18

flurazepam half life

40-100 (longest)

19

flurazepam use

short term mild/moderate insomina

20

flurazepam activity

prodrug
peak metabolite plasma concentration 1-3h

21

flurazepam delivery/absorption

good absorption orally

22

lorazepam half life

10-20hours

23

lorazepam use

short term mild/moderate insomnia with anxiety

24

lorazepam activity

slow
no active metabolites

25

lorazepam delivery/absorption

oral- slow
IM- good

26

temazepam half life

10-40h

27

temazepam use

short term severe insomina

28

temazepam delivery/absorption

slow and erratic oral absorption

29

temazepam warnings

distorts normal sleep pattern
do not use during pregnancy

30

triazolam half life

short term acute insomnia (jet lag)
**doesn't work for frequent awakenings

31

triazolam activity

fast acting- peak plasma levels 1h

32

triazolam delivery/absorption

good oral

33

triazolam warnings

higher abuse potential (fast acting)
more severe withdrawal with chronic use

34

use #2 of benzos

amnesia during anesthesia for procedures

35

midazolam

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

36

benzo overdose treatment

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

37

naloxone

drug for narcotic overdose

38

flumazenil

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

39

do not give flumazenil to

seizure history
barbiturate or TCA overdose
careful with ethanol intoxication

40

z drugs

benzodiazepine receptor agonsits

41

insomnia drugs with highest margin of safety

z drugs

42

MOA of z drugs

interacts with alpha1 receptors

43

z drug that is non selective

eszopiclone

44

effects of z drugs

hypnosis with little muscle relaxant or anticonvulsant effects

45

use of z drugs

decrease latency without affecting sleep cycles

46

why are z drugs better than benzos

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

47

z drug metabolism

liver
change dose for elderly and liver disease

48

3 z drugs

zolpidem
zaleplon
eszopiclone

49

zolpidem half life

2-2.5h
medium duration

50

zolpidem form

tablet
controlled release tablet
sublingual, lingual

51

zolpidem metabolism

CYP 3A4

52

zolpidem ADR

dizziness
diarrhea
GI irritation

53

zolpidem residual sleepiness

confusion and falls in elderly
memory impairment at high doses

54

zaleplon half life

1h
shorts duration
approved for use during night

55

zaleplon metabolism

aldehyde oxidase- works in patients with liver dysfunction

56

zaleplon ADR

impaired fertility
color disturbances

57

zaleplon tolerancee

rebound insomnia at high doses

58

eszopiclone half life

6h
longest duration

59

eszopiclone metabolism

CYP 3A4

60

eszopiclone ADR

taste disturbance
xerostomia

61

eszopiclone residual sleepiness

next day memory impairment
psychomotor impairment
rebound insomnia

62

z drugs causing rebound insomina

zaleplon
eszopiclone

63

longest duration z drug

eszopiclone

64

shortest duration z drug

zaleplon

65

CYP 3A4 metabolized z drugs

zolpidem
eszopiclone

66

suvorexant

orexin receptor antagonist used for insomina

67

ramelteon

synthetic melatonin- against at SCM MT1 and MT2 receptors

68

do not give sedative-hypnotics to

obstructive sleep apnea