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Psych Exam 1 > Sedative-Hypnotics - Kinder > Flashcards

Sedative-Hypnotics - Kinder Flashcards

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1
Q

benzo antagonist

A

flumazenil

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2
Q

sedative

A

reduce anxiety

-calming effect

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3
Q

hypnotic

A

drowsiness - facilitate onset of sleep

more pronounced depression of CNS

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4
Q

older sedative-hypnotics

A

alcohol and barbituates

increased dose - more anesthesia and coma

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5
Q

newer sedative-hypnotics

A

benzos and other newer drugs

greater dose required for anesthesia and coma

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6
Q

MOA of benzodiazepends

A

promote GAVA binding - at GABA-A

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7
Q

increased frequency of GABA channel openings

A

benzos

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8
Q

increased duration of GABA channel opening

A

barbituate

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9
Q

MOA barbituate

A

bind GABA-A potentiate GABA Cl current

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10
Q

lower capacity for CNS depression fatality

A

benzos - have displaced barbituates

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11
Q

can activate GABA channels directly at high dose

A

barbituate

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12
Q

require presence of GABA

A

benzos

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13
Q

activation of melatonin receptors MT1 and MT2

A

ramelteon

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14
Q

all sedative-hypnotics

A

cross CNS, placental barrier, and breast milk

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15
Q

metabolism of benzos

A

hepatic
-phase 1 and 2

phase 1 metabolites - active

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16
Q

desmethyldiazepam

A

active metabolite of chlordiazepoxide, diazepam, and clorazepatate

with t-1/2 of 40 hours

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17
Q

triazolam

A

short elimination t-1/2

favors use as hypnotic rather than sedative

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18
Q

cummulative toxicity

A

benzos with long t-1/2 - additive toxicity with multi doses

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19
Q

benzos for pt with liver issues

A

triazolam
lorazepam
oxazepam

bc not extensive metabolism in liver

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20
Q

hepatic metabolism and unrine glucuronide conjugate excretion

A

barbituates - except phenobarbitol (20-30% excreted unchanged)

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21
Q

short t-1/2

A

eszopiclone, zolpidem, zaleplon

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22
Q

alkanized urine

A

can increase elimination of phenobarbitol

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23
Q

MOA eszopiclone, zaleplon, zolpidem

A

GABA-A receptor agonists

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24
Q

CYP3A4

A

phase 1

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25
Q

glucuronidation

A

phase 2

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26
Q

metabolism of lorazepam, oxazepam, tamazepam

A

conjugation

good for hepatic impaired pt

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27
Q

metabolism of alphazolam and diazepam

A

oxiation

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28
Q

fast onset of action

A

diazepam and alprazolam

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29
Q

GABA-A receptor

A

two alpha 1, two beta 2, and one gamma 2 subunits

activation - chloride ion to center cell - hyperpolarization

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30
Q

GABA binding receptor

A

two sites between alpha and beta subunits

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31
Q

binding of benzos and newer hypnotics on GABA

A

between alpha and gamma

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32
Q

flumazenil binding

A

between alpha and gamma subunits

-reverse hypnotic effect of zolpidem and benzos

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33
Q

MOA benzos

A

enhance effect of GABA allosterically

-increased frequency of channel opening

34
Q

barbituate MOA

A

increased duration of GABA channel opening

high concentration - directly activate receptor

35
Q

eszopiclone, zaleplon, zolpidema

A

agonist at GABA-A receptor - only when alpha 1 subunit is included in receptor

36
Q

flumazenil

A

block action of benzos, eszopiclone, zaleplon, and zolpidem

37
Q

beta-carboline class

A

negative allosteric modulator of GABA receptor

38
Q

dose dependent anterograde amnesia effect

A

benzos

39
Q

increased total sleep time

A

eszopiclone

40
Q

increased total sleep time

A

eszopiclone

41
Q

stage 3 general anesthesia

A

high dose of barbs and older sedative-hypnotics

42
Q

thiopental and methohexital

A

lipid soluble - to CNS rapidly - good for anesthesia

43
Q

IV benzos

A

for anesthesia

44
Q

postanesthetic resp depression

A

long use high dose benzos- long half life and active metabolites that are active

45
Q

muscle relaxation

A

diazepam and meprobamate

46
Q

cause of death with OD of sedative-hypnotics

A

resp depression

47
Q

resp and cardiovasular depression of sedative-hypnotics

A

when given IV

48
Q

tolerance

A

decreased responsive to drug after repeated exposure

feature of sedative hypnotics

49
Q

cross tolerance

A

tolerance to drugs in same structural or mechanistic class

50
Q

benzo tolerance

A

down regulation of GABA-A receptors

  • hyperexcitability during withdrawal
  • sx of withdrawal
51
Q

barbituates

A

stimulate production of hepatic CYPs - rapid removal and breakdown of barbituates

52
Q

schedule III drug

A

meducal use allowed - limited potential for dependence

53
Q

schedule IV drug

A

medical use accepted - limited dependence possible

54
Q

physiologic dependence

A

altered physios tate requires drug admin

anxiety, insomnia, CNS excitabilty

55
Q

psychologic component of dependence

A

dependency of mind

-craving, irritable, insomnia, depression, anorexia

56
Q

to avoid withdrawal symptoms

A

taper dose gradually over time

57
Q

drugs with short half lives

A

sign of withdrawal between doses

ex - triazolam - half life 4 hours - daytime anxiety - when used to treat sleep disorder

58
Q

MOA flumazenil

A

competitive antagonist GABA-A receptor

59
Q

flumazenil t-1/2

A

short - requires repeated admin of flumazenil

to reverse CNS depression of benzos

60
Q

adverse of flumazenil

A

agitation, confusion, dizzy, nausea

can precipitate abstinence syndrome in those physiologically dependent

61
Q

tx acute anxiety and long term GAD

A

benzos

62
Q

tx panic disorders and agoraphobia

A

alprazolam

more selective in these condictions

63
Q

tx of GAD and phobias

A

SSRI and SNRI preferred

64
Q

acute anxiety state

A

benzos

65
Q

benzo pro and con of anxiety tx

A

pro - high therapeutic index

  • have flumazenil fro OD
  • low risk DDI

con - risk dependence

  • depression CNS function
  • amnestic effect
  • with ethanol - additional CNS depression
66
Q

tx sleep problem

A

zolpidem, zaleplon, eszopiclone - rapid onset of action, short t-1/2 (little hangover)

zolpidem - biphasic - sustained over entire night

67
Q

trouble falling asleep

A

zaleplon and zolpidem rapid t-1/2

68
Q

awaken early and difficulty sleeping through night

A

eszopiclone - t-1/2 6 hours

69
Q

failure to remit insomnia after 7-10 days

A

indicate primary psych or meical illness

70
Q

muscle spasticity tx

A

diazepam

71
Q

withdrawal of ethanol

A

use drug with longer t-1/2

chlordiazepoxide, diazepam, phenobarb

72
Q

drug interaction sedative-hypnotic

A

CNS depressant additive effect

73
Q

induce P450

A

phenobarbital and meprobamate

74
Q

ramelteon

A

for tx of insomnia due to difficulty with sleep onset

75
Q

MOA ramelteon

A

agonist at MT1 and MT2 melatonin receptors

suprachiasmatic nuclei

76
Q

avoid with ramelteon

A

coadmin of fluvoxamine (SSRI)

-bc inhibitors of CYP 1A2

77
Q

endocrine changes

A

with ramelteon

decreased cortisol
decreased testosterone
increased PRL

78
Q

buspirone

A

tx of GAD

take 3-4 week before effective

MOA - unknown

79
Q

ADR buspirone

A

tachy, palps, nervous, GI distress, paresthesia, papillary constriction

80
Q

flumazenil

A

blocks benzos and zolpidem, zaleplon, eszopiclone

81
Q

MOA buspirone

A

unknown

partial agonist at 5-HT receptor and affinity at D2 receptors

82
Q

ramelteon

A

extensive first pass

Psych Exam 1 (16 decks)

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