B7-074 Anxiolytic and Sedative/Hypnotic Drugs Flashcards

1
Q

bind to specific binding site on GABA-a receptor [2]

A

barbiturates
benzodiazepines (BZ)

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2
Q

facilitate GABA by increase Cl- opening time

A

barbiturates

barbiDURATes increase DURATion

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3
Q

barbiturates effects on CNS

A

complete CNS depression

can be exacerbated by alcohol use

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4
Q

barbiturates effects on cardiopulmonary system

A

medullary depression

(causes decreased respiration and blood pressure at anesthetic doses)

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5
Q

barbiturates effects on liver

A

P450s inducer

(decreases plasma levels of other drugs)

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6
Q

-tal

belong to what class of drugs?

A

barbiturates

phenobarbital, pentobarbital

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7
Q

barbituates she said to know [3]

A

phenobarbital (least lipophilic)
pentobarbital
thiopental (most lipophilic)

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8
Q

acute adverse effects of barbiturates

A

overdose
additive effects with other depressants

extreme medullary depression, no reversal agent

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9
Q

chronic effects of barbiturates [3]

A

tolerance
addiction
withdrawal

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10
Q

withdrawal from […] can cause seizures, hyperthermia, and cardiovascular collapse

A

barbiturates

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11
Q

metabolized in the liver via CYP450

A

barbiturates

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12
Q

increase likelihood of Cl- channel opening

A

benzodiazepines

FREZOdiazepines increase FREquency

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13
Q

act at a smaller subset of GABA receptors than barbiturates

A

benzodiazepines

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14
Q

CNS effects of benzodiazepines [5]

A

incomplete depressants
decreased anxiety
skeletal muscle relaxant
anticonvulsant
hypnotic

additive effect with barbiturates, alcohol

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15
Q

side effects benzodiazepines

A

sedation
amnesia
withdrawal

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16
Q

acute overdose of benzodiazepines can be treated with

A

flumazenil (antagonist)

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17
Q

-lam
-pam

what class are these?

A

benzodiazepines

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18
Q

short acting benzodiazepines [2]

A

midazolam (versed)
remimazolam

(2-4 hrs)

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19
Q

moderative acting benzodiazepines [3]

A

alprazolam
chlordiazepoxide
lorazepam

(10-14 hrs)

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20
Q

benzodiazepine often used for ACUTE panic attacks due to oral formulation

but can cause rebound anxiety

A

alprazolam

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21
Q

long acting benzodiazepines [1]

A

clonazepam (24 hrs)

(anti-convulsant)

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22
Q

very long acting benzodiazepines [1]

A

diazepam

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23
Q

benzodiazepine antagonist

A

flumazenil

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24
Q

fast acting benzodiazepine
date rape drug

A

flunitrazepam

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25
highly protein bound but have very few drug interactions
benzodiazepines
26
BZ-1 agonists [2]
zolpidem zaleplon (non-benzodiazepine BZ agonists)
27
non-selective BZ agonist [1]
eszopiclone (non-benzodiazepines BZ agonists)
28
side effects include abnormal thinking/behavior such as hallucinations, sleepwalking, and amnesia
non-benzodiazepines BZ agonist (Z-...) | FA: anxiety, headaches, confusion
29
what contributes to the duration of long acting anxiolytics, like diazepam?
metabolites have anxiolytic activity
30
very long acting anxiolytic that does not tend to produce dry mouth or tachycardia
diazepam
31
what effects do barbituates have at sub-anesthetic doses?
no medullary depression (no effect on resp/CV function)
32
orexin antagonist used as a hypnotic
suvorexant
33
used as prophylactic treatment in panic disorder
SSRIs (due to increased synaptic availability of serotonin)
34
used to treat acute panic attacks
benzodiapezines | alprazolam specifically
35
benzodiazepine antagonist
flumazenil
36
flumazenil can be used in overdose of
benzodiazepines
37
non-benzodiazepine BZ1 agonist used as a hypnotic
zolpidem | zaleplon, esZopiclone as well
38
H1 antagonist that is a common OTC sedative
diphenhydramine
39
sedative that acts orexin antagonist
suvorexant
40
sedative that acts as an agonist at the MT1 and MT2 melatonin receptors
ramelteon
41
melatonin agonists
ramelteon
42
orally available benzo that is sufficiently fast acting to be used in treating panic attacks when they occur
alprazolam
43
non-depressant anxiolytic that is a partial agonist of 5-HT1A receptors
buspirone
44
onset of buspirone typically takes how long?
1-2 weeks of treatment
45
duration of action of lorazepam
intermediate
46
duration of action of diazepam
very long acting (half life 43 hours)
47
rapidly and short acting benzo with profound amnestic effects no clinical uses
flunitrazepam (date rape drug)
48
short acting benzo administered IV as a preanesthetic and anesthetic agent
midalozam (versed)
49
partial agonist at 5-HT1A slow onset of action 1-2 weeks dysphoric at high doses
buspirone
50
used for generalized anxiety and as prophylaxis for panic disorder
SSRIs
51
H1 blocker antipruritic, antiemetic used pre and post operatively
hydroxyzine
52
melatonin receptor agonist indicated for insomnia with prolonged sleep onset
ramelteon
53
-rexants
orexin antagonists
54
block actions of orexins indicated for difficulties with sleep onset and/or sleep maintenance
-rexants
55
H1 blocker common OTC sedative
diphenhydramine
56
blocks 5-HT reuptake, H1, and a1 receptors classified as antidepressant, but so sedating it's used as a hypnotic
trazodone
57
benzo available in nasal spray for frequent seizure activity
midazolam
58
benzo that can cause rebound anxiety
alprazolam
59
[...] acting benzos are more likely to cause withdrawal symptoms
short
60
which benzo is used for it's particularly amnestic side effects?
midazolam
61
increase the affinity of GABA receptors for GABA, increasing the likelihood of channel opening
benzo
62
which barbiturate is the most lipophilic, and therefore has the fastest CNS penetration and accumulates in adipose tissue?
thiopental (phenobarbital is the least)
63
which barbiturate is the longest acting?
phenobarbital
64
which barbiturate is ultra short acting and available in IV formulation?
thiopental (faster CNS penetration, most accumulation in adipose)