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
Q

highly protein bound but have very few drug interactions

A

benzodiazepines

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26
Q

BZ-1 agonists [2]

A

zolpidem
zaleplon

(non-benzodiazepine BZ agonists)

27
Q

non-selective BZ agonist [1]

A

eszopiclone

(non-benzodiazepines BZ agonists)

28
Q

side effects include abnormal thinking/behavior such as hallucinations, sleepwalking, and amnesia

A

non-benzodiazepines BZ agonist

(Z-…)

FA: anxiety, headaches, confusion

29
Q

what contributes to the duration of long acting anxiolytics, like diazepam?

A

metabolites have anxiolytic activity

30
Q

very long acting anxiolytic that does not tend to produce dry mouth or tachycardia

A

diazepam

31
Q

what effects do barbituates have at sub-anesthetic doses?

A

no medullary depression

(no effect on resp/CV function)

32
Q

orexin antagonist used as a hypnotic

A

suvorexant

33
Q

used as prophylactic treatment in panic disorder

A

SSRIs

(due to increased synaptic availability of serotonin)

34
Q

used to treat acute panic attacks

A

benzodiapezines

alprazolam specifically

35
Q

benzodiazepine antagonist

A

flumazenil

36
Q

flumazenil can be used in overdose of

A

benzodiazepines

37
Q

non-benzodiazepine BZ1 agonist used as a hypnotic

A

zolpidem

zaleplon, esZopiclone as well

38
Q

H1 antagonist that is a common OTC sedative

A

diphenhydramine

39
Q

sedative that acts orexin antagonist

A

suvorexant

40
Q

sedative that acts as an agonist at the MT1 and MT2 melatonin receptors

A

ramelteon

41
Q

melatonin agonists

A

ramelteon

42
Q

orally available benzo that is sufficiently fast acting to be used in treating panic attacks when they occur

A

alprazolam

43
Q

non-depressant anxiolytic that is a partial agonist of 5-HT1A receptors

A

buspirone

44
Q

onset of buspirone typically takes how long?

A

1-2 weeks of treatment

45
Q

duration of action of lorazepam

A

intermediate

46
Q

duration of action of diazepam

A

very long acting

(half life 43 hours)

47
Q

rapidly and short acting benzo with profound amnestic effects
no clinical uses

A

flunitrazepam

(date rape drug)

48
Q

short acting benzo administered IV as a preanesthetic and anesthetic agent

A

midalozam (versed)

49
Q

partial agonist at 5-HT1A
slow onset of action 1-2 weeks
dysphoric at high doses

A

buspirone

50
Q

used for generalized anxiety and as prophylaxis for panic disorder

A

SSRIs

51
Q

H1 blocker
antipruritic, antiemetic
used pre and post operatively

A

hydroxyzine

52
Q

melatonin receptor agonist indicated for insomnia with prolonged sleep onset

A

ramelteon

53
Q

-rexants

A

orexin antagonists

54
Q

block actions of orexins
indicated for difficulties with sleep onset and/or sleep maintenance

A

-rexants

55
Q

H1 blocker
common OTC sedative

A

diphenhydramine

56
Q

blocks 5-HT reuptake, H1, and a1 receptors

classified as antidepressant, but so sedating it’s used as a hypnotic

A

trazodone

57
Q

benzo available in nasal spray for frequent seizure activity

A

midazolam

58
Q

benzo that can cause rebound anxiety

A

alprazolam

59
Q

[…] acting benzos are more likely to cause withdrawal symptoms

A

short

60
Q

which benzo is used for it’s particularly amnestic side effects?

A

midazolam

61
Q

increase the affinity of GABA receptors for GABA, increasing the likelihood of channel opening

A

benzo

62
Q

which barbiturate is the most lipophilic, and therefore has the fastest CNS penetration and accumulates in adipose tissue?

A

thiopental

(phenobarbital is the least)

63
Q

which barbiturate is the longest acting?

A

phenobarbital

64
Q

which barbiturate is ultra short acting and available in IV formulation?

A

thiopental

(faster CNS penetration, most accumulation in adipose)