Sedatives/Anxiolytics

Question 1

What is the purpose of Sedative/Hypnotic Drugs?

Answer 1

To promote/induce sleep

Question 2

What is the purpose of Anxiolytic Drugs?

Answer 2

Anxiety relief

Question 3

Sedatives/Hypnotics can be used to treat both Anxiety and Insomnia. How do they differ?

Answer 3

Difference in dosage!
Anxiety = lower dose
Insomnia = higher dose

Question 4

Which of the following drug classes include the most commonly prescribed treatment choices for insomnia? Select all that apply

a) SSRI
b) Benzodiazepines
c) Benzodiazepine-like drugs
d) Barbituates
e) Antihistamines

Answer 4

b) Benzodiazepines

c) Benzodiazepine-like drugs

Question 5

Which two classes of drugs are used most for anxiety disorders? Select all that apply

a) Benzodiazepines
b) Barbituates
c) SSRI
d) Tricyclic antidepressants

Answer 5

a) Benzodiazepines

c) SSRI (discussed later in the semester)

Question 6

What is the DOC for Insomnia & Anxiety?

Answer 6

Benzodiazepines

Question 7

What is the main MOA of Benzodiazepines?

Answer 7

Potentiate GABA (inhibitory neurotransmitter)

Question 8

Describe what is meant by a “built-in limit” of effects Benzodiazepines can produce.

Answer 8

Only work on endogenous GABA

Question 9

How do Benzodiazepines function to treat Insomnia?

Answer 9

CNS Depression

With ↑ed doses → ↑ed progressive effects from sedation → hypnosis → stupor

Question 10

How do Benzodiazepines function to treat Anxiety?

Answer 10

Decrease anxiety through effects on the limbic system (hippocampus)

Question 11

All Benzodiazepines produce similar responses, but how do they differ? (3)

Answer 11

1) Clinical application
2) Onset
3) Duration/Accumulation

Question 12

Benzodiazepine Prototype to treat Insomnia:

Answer 12

Triazolam (Halcion)

“Hal is Tri-ying to sleep”

Question 13

Benzodiazepine Prototype(s) to treat Anxiety:

Answer 13

1) lorazepam (Ativan)
2) diazepam (Valium)
3) alprazolam (Xanax)

“Pam and Al have anxiety”

Question 14

What Drug Schedule are Benzodiazepines?

Answer 14

Schedule IV Drugs

Question 15

Benzodiazepine Routes (2)

Answer 15

1) PO

2) IV

Question 16

Benzodiazepines produce ADRs in what 3 body systems?

Answer 16

1) CNS
2) Cardiovascular (CV)
3) Respiratory system (RS)

Question 17

Benzodiazepines:
What route produces little to no effect on the CV & RS?
What’s the one exception to this?

Answer 17

PO route

EXCEPT:
PO Benzos in combo with other CNS depressants can cause significant respiratory depression

Question 18

Benzodiazepine ADRs related to CNS Effects:

Answer 18

1) Sedation/Drowsiness
2) Confusion
3) Anterograde amnesia
4) Sleep-driving

Question 19

IV Benzodiazepine ADRs related to CV system:

Answer 19

1. HYPOTENSION (profound)

2. Cardiac Arrest!

Question 20

IV Benzodiazepine ADRs related to Respiratory System (RS):

Answer 20

1. significant Respiratory DEPRESSION

Question 21

What patients shouldn’t receive IV Benzodiazepine due to ADRs related to Respiratory System (RS):

Answer 21

1. COPD
2. Obstructive Sleep apnea (OSA)
   - can worsen airway obstruction!!

Question 22

Benzodiazepines’ Major Contraindication:

Answer 22

PREGNANCY
-Category D or X
“No Benzos w/ eggos”

Question 23

Do Benzodiazepines result in Tolerance &/or Physical Dependence?

Answer 23

Yes–BOTH
Tolerance: develops slowly
Withdrawal Syndrome: can be severe with high doses

Question 24

S/S of Benzodiazepine Withdrawal Syndrome:

Answer 24

1) Panic
2) Paranoia
3) Delirium
4) HTN*
5) Muscle twitching
6) Convulsions*

Question 25

Antidote for Benzodiazepine Toxicity: What does it do? What doesn't it do? How do we administer it?

Answer 25

Flumazenil (Romazicon)--1 hr duration DOES reverse sedative effects DOESN'T reverse respiratory depression! Administration: IV over 15 seconds Repeat doses q1 minute

Question 26

What major patient teaching do we need to provide related to benzodiazepines + withdrawal?

Answer 26

NEED TO WEAN! "reduce benzoooos slooooowly"

Question 27

What patient teaching would we provide related to Benzodiazepine ADRs Sedation/Psychomotor depression?

Answer 27

1) Avoid hazardous activities (driving) while adjusting 2) These ADRs should lessen after ~1 week or so. 3) Avoid other CNS depressants (ETOH)

Question 28

Benzodiazepine-like Drug Prototype(s) to treat Insomnia:

Answer 28

1) zolpidem (Ambien)** 2) zaleplon (Sonata) 3) eszopiclone (Lunesta) "Eszter 'likes' to take away "Zoom-Zoom" in her sleep"

Question 29

Prototype & Drug Schedule for Benzodiazepine-like Drugs to treat insomnia:

Answer 29

zolpidem (Ambien) | Schedule IV

Question 30

zolpidem (Ambien) MOA:

Answer 30

Act as agonists at the benzodiazepine receptor site on the GABA receptor-chloride channel

Question 31

How does zolpidem (Ambien) aid with insomnia?

Answer 31

Helpful with *falling* asleep XR: helps with *staying* asleep

Question 32

zolpidem (Ambien) ADRs:

Answer 32

1) Daytime Sedation/Drowsiness - "Hang-over Effect" --> *MOST COMMON SE* 2) Sleep-driving

Question 33

Does zolpidem (Ambien) result in Tolerance &/or Physical Dependence?

Answer 33

Nope

Question 34

zolpidem (Ambien) Patient Teaching:

Answer 34

1) Avoid hazardous activities (driving) while adjusting 2) Avoid other CNS depressants (ETOH) 3) Teach family about sleep-driving risk

Question 35

Name the 2 Non-Benzo/Non-Barbituates used to treat Anxiety:

Answer 35

1) buspirone (BuSpar) | 2) hydroxyzine

Question 36

buspirone (BuSpar) is not a 1) ___ __________ and is not used 2) ___.

Answer 36

1) CNS depressants | 2) PRN

Question 37

What are some other benefits of buspirone (BuSpar)?

Answer 37

NO abuse potential NO suicide risk NO increased CNS effecrs with other drugs (ETOH, benzos, etc.)

Question 38

Why can't we use buspirone (BuSpar) PRN?

Answer 38

Takes weeks to develop peak effects! | -May require a PRN Anxiolytic while therapeutic effects develop

Question 39

What is the major Contraindication with buspirone (BuSpar)?

Answer 39

GRAPEFRUIT!

Question 40

How do we switch from a Benzodiazepine to buspirone (BuSpar)?

Answer 40

``` Give buspirone (BuSpar) 2-4 wks before stopping the benzo -Need to Wean Benzo slowly!! ```

Question 41

Does buspirone (BuSpar) result in Tolerance &/or Physical Dependence?

Answer 41

Nope

Question 42

What class of drug is Hydroxyzine?

Answer 42

Antihistamine

Question 43

What can we use Hydroxyzine for?

Answer 43

1) Anxiety (effects on serotonin) | 2) Insomnia (anticholinergic effect)

Question 44

Is Hydroxyzine a Scheduled Drug?

Answer 44

Nope

Question 45

Hydroxyzine route and dosing:

Answer 45

1) PO Dosing: 1) Routine: anxiety QID (4x/day) 2) PRN: insomnia

Question 46

Hydroxyzine SEs:

Answer 46

ANTICHOLINERGIC SEs!! 1) Dry mouth 2) Constipation 3) Confusion 4) Dizziness 5) Headache 6) Fatigue

Question 47

What serious ADR can occur with prolonged use of Hydroxyzine?

Answer 47

Prolonged QT-Interval!

Question 48

Does Hydroxyzine result in Tolerance &/or Physical Dependence?

Answer 48

Nope