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Psych Exam 1 > Sedative-Hypnotics - Kinder > Flashcards

Sedative-Hypnotics - Kinder Flashcards

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
glucuronidation
phase 2
26
metabolism of lorazepam, oxazepam, tamazepam
conjugation good for hepatic impaired pt
27
metabolism of alphazolam and diazepam
oxiation
28
fast onset of action
diazepam and alprazolam
29
GABA-A receptor
two alpha 1, two beta 2, and one gamma 2 subunits activation - chloride ion to center cell - hyperpolarization
30
GABA binding receptor
two sites between alpha and beta subunits
31
binding of benzos and newer hypnotics on GABA
between alpha and gamma
32
flumazenil binding
between alpha and gamma subunits | -reverse hypnotic effect of zolpidem and benzos
33
MOA benzos
enhance effect of GABA allosterically | -increased frequency of channel opening
34
barbituate MOA
increased duration of GABA channel opening high concentration - directly activate receptor
35
eszopiclone, zaleplon, zolpidema
agonist at GABA-A receptor - only when alpha 1 subunit is included in receptor
36
flumazenil
block action of benzos, eszopiclone, zaleplon, and zolpidem
37
beta-carboline class
negative allosteric modulator of GABA receptor
38
dose dependent anterograde amnesia effect
benzos
39
increased total sleep time
eszopiclone
40
increased total sleep time
eszopiclone
41
stage 3 general anesthesia
high dose of barbs and older sedative-hypnotics
42
thiopental and methohexital
lipid soluble - to CNS rapidly - good for anesthesia
43
IV benzos
for anesthesia
44
postanesthetic resp depression
long use high dose benzos- long half life and active metabolites that are active
45
muscle relaxation
diazepam and meprobamate
46
cause of death with OD of sedative-hypnotics
resp depression
47
resp and cardiovasular depression of sedative-hypnotics
when given IV
48
tolerance
decreased responsive to drug after repeated exposure feature of sedative hypnotics
49
cross tolerance
tolerance to drugs in same structural or mechanistic class
50
benzo tolerance
down regulation of GABA-A receptors - hyperexcitability during withdrawal - sx of withdrawal
51
barbituates
stimulate production of hepatic CYPs - rapid removal and breakdown of barbituates
52
schedule III drug
meducal use allowed - limited potential for dependence
53
schedule IV drug
medical use accepted - limited dependence possible
54
physiologic dependence
altered physios tate requires drug admin anxiety, insomnia, CNS excitabilty
55
psychologic component of dependence
dependency of mind | -craving, irritable, insomnia, depression, anorexia
56
to avoid withdrawal symptoms
taper dose gradually over time
57
drugs with short half lives
sign of withdrawal between doses ex - triazolam - half life 4 hours - daytime anxiety - when used to treat sleep disorder
58
MOA flumazenil
competitive antagonist GABA-A receptor
59
flumazenil t-1/2
short - requires repeated admin of flumazenil to reverse CNS depression of benzos
60
adverse of flumazenil
agitation, confusion, dizzy, nausea can precipitate abstinence syndrome in those physiologically dependent
61
tx acute anxiety and long term GAD
benzos
62
tx panic disorders and agoraphobia
alprazolam more selective in these condictions
63
tx of GAD and phobias
SSRI and SNRI preferred
64
acute anxiety state
benzos
65
benzo pro and con of anxiety tx
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
tx sleep problem
zolpidem, zaleplon, eszopiclone - rapid onset of action, short t-1/2 (little hangover) zolpidem - biphasic - sustained over entire night
67
trouble falling asleep
zaleplon and zolpidem rapid t-1/2
68
awaken early and difficulty sleeping through night
eszopiclone - t-1/2 6 hours
69
failure to remit insomnia after 7-10 days
indicate primary psych or meical illness
70
muscle spasticity tx
diazepam
71
withdrawal of ethanol
use drug with longer t-1/2 | chlordiazepoxide, diazepam, phenobarb
72
drug interaction sedative-hypnotic
CNS depressant additive effect
73
induce P450
phenobarbital and meprobamate
74
ramelteon
for tx of insomnia due to difficulty with sleep onset
75
MOA ramelteon
agonist at MT1 and MT2 melatonin receptors suprachiasmatic nuclei
76
avoid with ramelteon
coadmin of fluvoxamine (SSRI) | -bc inhibitors of CYP 1A2
77
endocrine changes
with ramelteon decreased cortisol decreased testosterone increased PRL
78
buspirone
tx of GAD take 3-4 week before effective MOA - unknown
79
ADR buspirone
tachy, palps, nervous, GI distress, paresthesia, papillary constriction
80
flumazenil
blocks benzos and zolpidem, zaleplon, eszopiclone
81
MOA buspirone
unknown partial agonist at 5-HT receptor and affinity at D2 receptors
82
ramelteon
extensive first pass

Psych Exam 1 (16 decks)

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