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aNeuro exam 4: Lindsey's > Anxiolytic Agents > Flashcards

Anxiolytic Agents Flashcards

1
Q

What are the most commonly used txs for anxiety disorders?

A

SSRIs

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2
Q

What do you prescribe benzos for?

A

acute and situational anxiety

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3
Q

Why are barbs seldom used?

A

low safety margin, drug interactions, and abuse potential

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4
Q

Why is Buspirone used over benzos, even though it’s weaker?

A

fewer SEs

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5
Q

How do sedative/hypnotic drugs work, as a class?

A

they augment GABA neuronal inhibition and/or inhibit glutamate neuronal excitation

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6
Q

_______ drugs are described as decreasing activity, moderating excitement, and calming the recipient.

A

Sedative

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7
Q

______ drugs produce drowsiness and facilitate the onset and maintenance of sleep that resembles natural sleep and from which the recipient can be easily aroused.

A

Hypnotic

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8
Q

What does it mean that sedatives/hypnotics have a graded response? How do they act in the therapeutic range?

A

the CNS effects are dose-dependent; they produce antianxiety, anticonvulsant, muscle relaxant, sedative,
and hypnotic effects

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9
Q

Which drug class can be use for general anesthesia?

A

barbs

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10
Q

What is the major limiting SE of barbs?

A

respiratory and vasomotor depression –> coma/death

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11
Q

The great majority of sedative-hypnotic drugs act to facilitate the action of _______ at the GABAa receptor-chloride channel complex.

A

GABA (γ-aminobutyric acid)

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12
Q

The great majority of sedative-hypnotic drugs act to facilitate the action of GABA (γ-aminobutyric acid) at the _______.

A

GABAa receptor-chloride channel complex

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13
Q

GABA binding to its receptor ______.

A

opens an ion channel to increase Cl- conductance

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14
Q

Membrane hyperpolarization via GABA receptor binding causes?

A

decreased neuronal excitability and neurotransmission

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15
Q

Both benzodiazepines and barbiturates (each at a separate binding site) indirectly _______ to diminish neuronal excitability further.

A

increase the GABAergic effect

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16
Q

_______ intensify the effect of GABA, while _____ prolong the effect of GABA.

A 
Benzos = intensify
barbs = prolong
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17
Q

Benzodiazepines ______ the effect of GABA, while barbiturates ______ the effect of GABA.

A 
Benzos = intensify
barbs = prolong
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18
Q

At high concentrations, barbiturates interact directly with the ______ (presence of GABA is not required for effect).

A

GABA receptor

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19
Q

At _______, barbiturates interact directly with the GABA receptor (presence of GABA is not required for effect).

A

high concentrations

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20
Q

_____ action is less selective and also depresses excitatory neurotransmitters (glutamate).

A

Barbiturate

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21
Q

Barbiturate action is less selective and also depresses ______.

A

excitatory neurotransmitters (glutamate)

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22
Q

_____, _____, and _____ are non-benzodiazepines that interact with the benzodiazepine binding site as agonists and are commonly referred to as “Z”-drugs.

A

Zolpidem, eszopiclone, and zaleplon

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23
Q

Zolpidem, eszopiclone, and zaleplon are non-benzodiazepines that interact with ______ as agonists and are commonly referred to as “Z”-drugs.

A

the benzodiazepine binding site

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24
Q

Zolpidem, eszopiclone, and zaleplon are non-benzodiazepines that interact with the benzodiazepine
binding site as agonists and are commonly referred to as ______.

A

“Z”-drugs

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25
Q

______, an antagonist at the benzodiazepine binding site, reverses the CNS effects of benzodiazepines.

A

Flumazenil

26
Q

Name an antagonist at the benzodiazepine binding site.

A

Flumazenil

27
Q

Flumazenil reverses the CNS effects of ______.

A

benzodiazepines

28
Q

What is Flumazenil?

A

an antagonist at the benzodiazepine binding site

reverses the CNS effects of benzodiazepines

29
Q

GABA receptors with _____ subunits are highly expressed in the cortex and these receptors appear to mediate sedative (sleep), amnestic, and anticonvulsant actions of benzodiazepines.

A

α1

30
Q

GABA receptors with α1 subunits are highly expressed in the ______, and these receptors appear to mediate sedative (sleep), amnestic, and anticonvulsant actions of benzodiazepines.

A

cortex

31
Q

GABA receptors with α1 subunits are highly expressed in the cortex and these receptors appear to mediate _______ of benzodiazepines.

A

sedative (sleep), amnestic, and anticonvulsant actions

32
Q

GABA receptors with α1 subunits are highly expressed in the cortex and these receptors appear to mediate sedative (sleep), amnestic, and anticonvulsant actions of _________.

A

benzodiazepines

33
Q

GABA receptors with _____ subunits are highly expressed in the limbic system and brain stem and these receptors appear to mediate myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating effects of benzodiazepines.

A

α2/α5

34
Q

GABA receptors with α2/α5 subunits are highly expressed in the _______, and these receptors appear to mediate myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating effects of benzodiazepines.

A

limbic system and brain stem

35
Q

GABA receptors with α2/α5 subunits are highly expressed in the limbic system / and brain stem and these receptors appear to mediate _______ effects of benzodiazepines.

A

myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating

36
Q

GABA receptors with α2/α5 subunits are highly expressed in the limbic system / and brain stem and these receptors appear to mediate myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating effects of _______.

A

benzodiazepines

37
Q

_________ bind only to GABA-chloride channels with α1 subunits resulting in sleep without anxiolysis (reduced potential for dependence).

A

“Z-drugs” (zolpidem, zaleplon, eszopiclone)

38
Q

“Z-drugs” (zolpidem, zaleplon, eszopiclone) are not benzodiazepines structurally and bind to GABA-chloride channels with _____ subunits resulting in sleep without anxiolysis (reduced potential for dependence).

A

α1

39
Q

“Z-drugs” (zolpidem, zaleplon, eszopiclone) are not benzodiazepines structurally and bind only to GABA-chloride channels with α1 subunits resulting in ______.

A

sleep without anxiolysis (reduced potential for dependence)

40
Q

Higher doses of most barbiturates and some benzodiazepines inhibit formation and spread of ______ in _____.

A

seizure activity in cortical neurons

41
Q

What is the drug of choice for status epilepticus?

A

Diazepam

42
Q

How do benzos/barbs cause muscle relaxation?

A

inhibit spinal cord polysynaptic reflexes may aid in muscle spasms (at high doses with CNS SEs)

43
Q

Short-acting _______ (thiopental) are used to induce-maintain surgical anesthesia.

A

barbiturates

44
Q

Short-acting barbiturates (_______) are used to induce-maintain surgical anesthesia.

A

thiopental

45
Q

Name 3 benzos that have good oral absorption.

A

Diazepam, alprazolam, and triazolam

46
Q

What benzo is good for IM administration?

A

Lorazepam

47
Q

Many phase I metabolites of benzodiazepines are active with half-lives longer than the parent compounds. What is the significance of this fact?

A

Accumulation of these metabolites can occur when multiple doses are given, resulting in unwanted CNS effects such as daytime sedation, esp. in elderly pts

48
Q

Accumulation of these metabolites can occur when multiple doses are given, resulting in unwanted CNS effects such as daytime sedation, esp. in elderly pts.

A

phase I metabolites of benzodiazepines

49
Q

What benzos are safe to give your elderly and hepatic dysfunction pts and why?

A

Lorazepam and oxazepam are metabolized directly to the inactive glucuronides (NO P450 step) and as a result have shorter half-lives and fewer problems with cumulative and residual effects.

50
Q

Lorazepam and oxazepam are metabolized directly to the inactive glucuronides (NO P450 step) and as a result have shorter half-lives and fewer problems with cumulative and residual effects. What is the significance of this fact?

A

safe to give these drugs to elderly and hepatic dysfunction pts

51
Q

_______ are classic inducers of CYP450 enzymes and represent a major source of clinically significant drug interactions.

A

Barbiturates

52
Q

Barbiturates are classic inducers of _______ enzymes and represent a major source of clinically significant drug interactions.

A

CYP450

53
Q

Benzos can have an additive effect when given with what?

A

other agents that cause CNS depression (alcohol,

opioid analgesics, antipsychotic agents, anticonvulsants, antihistamines, TCADs)

54
Q

Benzos can cause anterograde amnesia. How? Why is this significant?

A

because they enhance GABA-ergic neuronal function

good: procedural amnesia
bad: roofies/date rape

55
Q

Why do benzos carry a black box warning?

A

strange sleep-related behavior and severe allergic reactions

56
Q

Benzos are contraindicated in which patients?

A

those with breathing problems, chronic pulmonary disease, and symptomatic sleep apnea

57
Q

Benzos can be used to treat which psych disorders?

A

acute: general anxiety
panic disorder
social anxiety

58
Q

What is Buspirone?

A

a 5HT1A partial agonist located presynaptically on nerve terminals used as an anxiolytic

59
Q

This is a 5HT1A partial agonist located presynaptically on nerve terminals used as an anxiolytic.

A

Buspirone

60
Q

What are the SEs of Buspirone?

A

dizziness, nausea, headache

61
Q

How must Buspirone be taken?

A

on a routine schedule for at least 2 weeks but 4-6 weeks for maximal efficacy

aNeuro exam 4: Lindsey's (37 decks)

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