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NBB 2 > Sedative Hypnotic Agents > Flashcards

Sedative Hypnotic Agents Flashcards

1
Q

Reduces anxiety and exerts a calming effect

A

Sedative (anxiolytics)

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2
Q

Promotes drowsiness and encourages the onset and maintenance of sleep

A

Hypnotic drug

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3
Q

Indicated for patients experiencing symptoms severe enough to produce functional disability

A

Anxiolytic medication

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4
Q

The most effective and commonly prescribed drugs for rapid relief of acute anxiety symptoms in GAD and panic disorder

A

Benzodiazepines (BZs)

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5
Q

A major determinant of the rate at which a given BZ enters the CNS

A

Lipophilicity

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6
Q

Cross the placental barrier and may contribute to depression of neonatal function

A

BZs

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7
Q

BZs for which the parent drug or its active metabolites have long t1/2’s are more likely to cause cumulative effects with

A

Multiple doses

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8
Q

The BZs bind to the molecular components of the

A

GABA-A receptor

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9
Q

Functions as a Cl- ion channel

A

GABA-A receptor

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10
Q

A heteropentameric glycoprotein assembled from 5 subunits

A

GABA-A receptor

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11
Q

All neuropharmacological agents are usually very

A

Lipophilic

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12
Q

Interacts at 2 sites between the alpha and beta subunits, triggering Cl- ion channel opening with resulting membrane hyperpolarization

A

GABA

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13
Q

The binding of BZs to GABA-A occurs at a single site between the

-BZ antagonists also target here

A

Alpha and gamma subunits

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14
Q

Potentiate the Cl- ion channel effects of GABA as well as GABAnergic inhibition at all levels of the neuraxis

A

BZs

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15
Q

Which BZ has the fastest time to peak blood level?

A

Midazolam

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16
Q

Have a fast time to peak blood level and a long half life

A

BZs

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17
Q

There is little justification for long-term therapy of

A

BZs

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18
Q

In the elderly, we want to decrease the dose of BZs by

A

1/2

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19
Q

Do not combine with any other anti-anxiety agents, antihistamines, anticholinergics, and ethanol

A

BZs

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20
Q

The BZ that acts the fastest but has the shortest half-life

-Labeled for sedation prior to medical or surgical procedures

A

Midazolam

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21
Q

Can cause significant dose-related anterograde amnesia and can significantly impair the ability to learn new information

A

BZs

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22
Q

Can present as lethargy or a sate of exhaustion. Or, alternatively, as gross symptoms of ethanol intoxication

A

BZ toxicity

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23
Q

Tolerance, psychological dependence, and physiologic dependence can result from

A

Prolonged BZ use

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24
Q

The drugs most frequently involved in deliberate overdoses

A

Sedative-hypnotics

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25
Q

Increase the frequency at which the Cl- channel opens

A

BZs

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26
Q

Are addictive, can cause depression of CNS functions, and cause amnesia effects

A

BZs

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27
Q

Synthetic BZ derivative that binds to the BZ site on the GABA-A receptor

A

Flumazenil (Romazicon)

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28
Q

Antagonizes the actions of the BZs and the newer hypnotics zolpidem, zaleplon, and eszopiclone, but NOT the barbiturates

A

Flumazenil (Romazicon)

29
Q

Approved for use in reversing the CNS depressant effects of BZ overdose and hastens recovery after BZ use in medical procedures

A

Flumazenil

30
Q

Newer-generation antidepressants for the chronic management of GAD include:

A

SSRIs and SNRIs

31
Q

A lack of dependency and a tolerable adverse effect profile make these drugs the preferred choice for long term treatment of GAD

A

SSRI’s and SNRI’s

32
Q

The anti-anxiety response of antidepressants requires

A

2-4 weeks or longer

33
Q

Has selective anxiolytics effects without causing marked sedative, hypnotic, or euphoric effects

A

Buspirone

34
Q

Thought to exert its anxiolytics effects by acting as a partial agonist at brain 5-HT1A receptors

A

Buspirone

35
Q

Also has affinity for brain dopamine D2 receptors

A

Buspirone

36
Q

It’s anxiolytics affect take 2 weeks or longer to become established, making the drug unsuitable for acute anxiety states

A

Buspirone

37
Q

Buspirone interacts with

A

Inducers and inhibitors of CYP and MAO inhibitors

38
Q

Thought to increase the presynaptic release of GABA by binding to voltage-gated Ca2+ channels and altering Ca2+ influx

A

Pregabalin

39
Q

Pregabalin also increases GABA biosynthesis by modulating the actions of which two enzymes?

A

Glutamate decarboxylase and Branched-chain aminotransferase

40
Q

Is also GABAergic, though it does not bind the GABA receptor like BZs

A

Pregabalin

41
Q

Produces anxiolytics effects similar to the BZs and antidepressants

A

Pregabalin

42
Q

A prototypical tricyclic antidepressant that acts like an SNRI

A

Imipramine

43
Q

Although effective in the treatment of GAD, it is considered a second-line agent due to higher toxicity and adverse effect rates than the newer antidepressants

A

Imipramine

44
Q

Has antiadrenergic, anticholinergic, and antihistamine properties

A

Imipramine

45
Q

A potent H1 antihistamine that also acts as a strong antagonist t 5-HT receptors

A

Hydroxyzine

46
Q

The anxiolytic properties of Hydroxyzine are from its

A

Antiserotonergic effects

47
Q

Adverse effects are related to antihistamine, anticholinergic, and anti dopaminergic properties, and include dry mouth, GI disturbances, and blurred/double vision

A

Hydroxyzine

48
Q

An atypical antipsychotic with antagonist activity at 5-HT receptors

A

Quetiapine XR

49
Q

Classified as an alternative agent due to numerous adverse effects that are related to blockade of muscarinic, a-adrenergic, and dopamine receptors

A

Quetiapine XR

50
Q

Drugs used to treat insomnia

A

Hypnotics

51
Q

GABAergic drugs can also be used as

A

Hypnotic Agents

52
Q

At hypnotic doses, increase total sleep time and decrease sleep latency and the number of awakenings

A

BZs

53
Q

Bind to the same sight on the GABA-A receptor as the BZs and exhibit similar GABAergic effects

A

Non-BZ hypnotics

54
Q

More selective in their binding than the BZs

-All decreases time to persistent sleep

A

Non-BZ Hypnotics

55
Q

Non-BZ hypnotics that increase total sleep time

A

Zolpidem and eszopiclone

56
Q

Non-BZ Hypnotic that does NOT increase total sleep time

A

Zaleplon

57
Q

Occurs with both zolpidem and zaleplon if used at higher doses

A

Rebound insomnia

58
Q

Unlike certain BZs, ALL lack anticonvulsant and muscle relaxing activities

A

Non-BZ Hypnotics

59
Q

Both act as agonists at melatonin receptors in the brain and have NO GABAergic effects in the CNS

A

Ramelteon and Tasimelteon

60
Q

Decreases sleep latency and increases sleep periods with no rebound insomnia or risk of dependence

A

Non-GABAergic Hypnotics (Ramelteon and Tasimelteon)

61
Q

Approved for non-24 hour sleep-wake disorder

A

Tasimelteon

62
Q

Can cause decreased testosterone and increased prolactin

A

Ramelteon

63
Q

A neurotransmitter in the wake pathway that acts as a central promoter of wakefulness

A

Orexin (OX)

64
Q

Acts as an antagonist at OX1 and OX2 receptors in the brain with no GABAergic CNS effects

A

Suvorexant

65
Q

Decreases sleep latency and increases sleep periods, but is associated with a risk of abuse or dependence

A

Suvorexant

66
Q

Sedation and somnolence are what type of effects?

A

Antihistamine

67
Q

Dry mouth, constipation, blurred/double vision, and tachycardia are what type of effects?

A

Anticholinergic effects

68
Q

Orthostatic hypotension is which type of effect?

A

Antiadrenergic

NBB 2 (21 decks)

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