Sedative Hypnotic Agents

Question 1

Reduces anxiety and exerts a calming effect

Answer 1

Sedative (anxiolytics)

Question 2

Promotes drowsiness and encourages the onset and maintenance of sleep

Answer 2

Hypnotic drug

Question 3

Indicated for patients experiencing symptoms severe enough to produce functional disability

Answer 3

Anxiolytic medication

Question 4

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

Answer 4

Benzodiazepines (BZs)

Question 5

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

Answer 5

Lipophilicity

Question 6

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

Answer 6

BZs

Question 7

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

Answer 7

Multiple doses

Question 8

The BZs bind to the molecular components of the

Answer 8

GABA-A receptor

Question 9

Functions as a Cl- ion channel

Answer 9

GABA-A receptor

Question 10

A heteropentameric glycoprotein assembled from 5 subunits

Answer 10

GABA-A receptor

Question 11

All neuropharmacological agents are usually very

Answer 11

Lipophilic

Question 12

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

Answer 12

GABA

Question 13

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

-BZ antagonists also target here

Answer 13

Alpha and gamma subunits

Question 14

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

Answer 14

BZs

Question 15

Which BZ has the fastest time to peak blood level?

Answer 15

Midazolam

Question 16

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

Answer 16

BZs

Question 17

There is little justification for long-term therapy of

Answer 17

BZs

Question 18

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

Answer 18

1/2

Question 19

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

Answer 19

BZs

Question 20

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

-Labeled for sedation prior to medical or surgical procedures

Answer 20

Midazolam

Question 21

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

Answer 21

BZs

Question 22

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

Answer 22

BZ toxicity

Question 23

Tolerance, psychological dependence, and physiologic dependence can result from

Answer 23

Prolonged BZ use

Question 24

The drugs most frequently involved in deliberate overdoses

Answer 24

Sedative-hypnotics

Question 25

Increase the frequency at which the Cl- channel opens

Answer 25

BZs

Question 26

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

Answer 26

BZs

Question 27

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

Answer 27

Flumazenil (Romazicon)

Question 28

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

Answer 28

Flumazenil (Romazicon)

Question 29

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

Answer 29

Flumazenil

Question 30

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

Answer 30

SSRIs and SNRIs

Question 31

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

Answer 31

SSRI’s and SNRI’s

Question 32

The anti-anxiety response of antidepressants requires

Answer 32

2-4 weeks or longer

Question 33

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

Answer 33

Buspirone

Question 34

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

Answer 34

Buspirone

Question 35

Also has affinity for brain dopamine D2 receptors

Answer 35

Buspirone

Question 36

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

Answer 36

Buspirone

Question 37

Buspirone interacts with

Answer 37

Inducers and inhibitors of CYP and MAO inhibitors

Question 38

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

Answer 38

Pregabalin

Question 39

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

Answer 39

Glutamate decarboxylase and Branched-chain aminotransferase

Question 40

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

Answer 40

Pregabalin

Question 41

Produces anxiolytics effects similar to the BZs and antidepressants

Answer 41

Pregabalin

Question 42

A prototypical tricyclic antidepressant that acts like an SNRI

Answer 42

Imipramine

Question 43

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

Answer 43

Imipramine

Question 44

Has antiadrenergic, anticholinergic, and antihistamine properties

Answer 44

Imipramine

Question 45

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

Answer 45

Hydroxyzine

Question 46

The anxiolytic properties of Hydroxyzine are from its

Answer 46

Antiserotonergic effects

Question 47

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

Answer 47

Hydroxyzine

Question 48

An atypical antipsychotic with antagonist activity at 5-HT receptors

Answer 48

Quetiapine XR

Question 49

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

Answer 49

Quetiapine XR

Question 50

Drugs used to treat insomnia

Answer 50

Hypnotics

Question 51

GABAergic drugs can also be used as

Answer 51

Hypnotic Agents

Question 52

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

Answer 52

BZs

Question 53

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

Answer 53

Non-BZ hypnotics

Question 54

More selective in their binding than the BZs -All decreases time to persistent sleep

Answer 54

Non-BZ Hypnotics

Question 55

Non-BZ hypnotics that increase total sleep time

Answer 55

Zolpidem and eszopiclone

Question 56

Non-BZ Hypnotic that does NOT increase total sleep time

Answer 56

Zaleplon

Question 57

Occurs with both zolpidem and zaleplon if used at higher doses

Answer 57

Rebound insomnia

Question 58

Unlike certain BZs, ALL lack anticonvulsant and muscle relaxing activities

Answer 58

Non-BZ Hypnotics

Question 59

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

Answer 59

Ramelteon and Tasimelteon

Question 60

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

Answer 60

Non-GABAergic Hypnotics (Ramelteon and Tasimelteon)

Question 61

Approved for non-24 hour sleep-wake disorder

Answer 61

Tasimelteon

Question 62

Can cause decreased testosterone and increased prolactin

Answer 62

Ramelteon

Question 63

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

Answer 63

Orexin (OX)

Question 64

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

Answer 64

Suvorexant

Question 65

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

Answer 65

Suvorexant

Question 66

Sedation and somnolence are what type of effects?

Answer 66

Antihistamine

Question 67

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

Answer 67

Anticholinergic effects

Question 68

Orthostatic hypotension is which type of effect?

Answer 68

Antiadrenergic