Sedatives/Anxiolytics Flashcards
What is the purpose of Sedative/Hypnotic Drugs?
To promote/induce sleep
What is the purpose of Anxiolytic Drugs?
Anxiety relief
Sedatives/Hypnotics can be used to treat both Anxiety and Insomnia. How do they differ?
Difference in dosage!
Anxiety = lower dose
Insomnia = higher dose
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
b) Benzodiazepines
c) Benzodiazepine-like drugs
Which two classes of drugs are used most for anxiety disorders? Select all that apply
a) Benzodiazepines
b) Barbituates
c) SSRI
d) Tricyclic antidepressants
a) Benzodiazepines
c) SSRI (discussed later in the semester)
What is the DOC for Insomnia & Anxiety?
Benzodiazepines
What is the main MOA of Benzodiazepines?
Potentiate GABA (inhibitory neurotransmitter)
Describe what is meant by a “built-in limit” of effects Benzodiazepines can produce.
Only work on endogenous GABA
How do Benzodiazepines function to treat Insomnia?
CNS Depression
With ↑ed doses → ↑ed progressive effects from sedation → hypnosis → stupor
How do Benzodiazepines function to treat Anxiety?
Decrease anxiety through effects on the limbic system (hippocampus)
All Benzodiazepines produce similar responses, but how do they differ? (3)
1) Clinical application
2) Onset
3) Duration/Accumulation
Benzodiazepine Prototype to treat Insomnia:
Triazolam (Halcion)
“Hal is Tri-ying to sleep”
Benzodiazepine Prototype(s) to treat Anxiety:
1) lorazepam (Ativan)
2) diazepam (Valium)
3) alprazolam (Xanax)
“Pam and Al have anxiety”
What Drug Schedule are Benzodiazepines?
Schedule IV Drugs
Benzodiazepine Routes (2)
1) PO
2) IV
Benzodiazepines produce ADRs in what 3 body systems?
1) CNS
2) Cardiovascular (CV)
3) Respiratory system (RS)
Benzodiazepines:
What route produces little to no effect on the CV & RS?
What’s the one exception to this?
PO route
EXCEPT:
PO Benzos in combo with other CNS depressants can cause significant respiratory depression
Benzodiazepine ADRs related to CNS Effects:
1) Sedation/Drowsiness
2) Confusion
3) Anterograde amnesia
4) Sleep-driving
IV Benzodiazepine ADRs related to CV system:
- HYPOTENSION (profound)
2. Cardiac Arrest!
IV Benzodiazepine ADRs related to Respiratory System (RS):
- significant Respiratory DEPRESSION
What patients shouldn’t receive IV Benzodiazepine due to ADRs related to Respiratory System (RS):
- COPD
- Obstructive Sleep apnea (OSA)
- can worsen airway obstruction!!
Benzodiazepines’ Major Contraindication:
PREGNANCY
-Category D or X
“No Benzos w/ eggos”
Do Benzodiazepines result in Tolerance &/or Physical Dependence?
Yes–BOTH
Tolerance: develops slowly
Withdrawal Syndrome: can be severe with high doses
S/S of Benzodiazepine Withdrawal Syndrome:
1) Panic
2) Paranoia
3) Delirium
4) HTN*
5) Muscle twitching
6) Convulsions*
Antidote for Benzodiazepine Toxicity:
What does it do? What doesn’t it do?
How do we administer it?
Flumazenil (Romazicon)–1 hr duration
DOES reverse sedative effects
DOESN’T reverse respiratory depression!
Administration:
IV over 15 seconds
Repeat doses q1 minute
What major patient teaching do we need to provide related to benzodiazepines + withdrawal?
NEED TO WEAN!
“reduce benzoooos slooooowly”
What patient teaching would we provide related to Benzodiazepine ADRs Sedation/Psychomotor depression?
1) Avoid hazardous activities (driving) while adjusting
2) These ADRs should lessen after ~1 week or so.
3) Avoid other CNS depressants (ETOH)
Benzodiazepine-like Drug Prototype(s) to treat Insomnia:
1) zolpidem (Ambien)**
2) zaleplon (Sonata)
3) eszopiclone (Lunesta)
“Eszter ‘likes’ to take away “Zoom-Zoom” in her sleep”
Prototype & Drug Schedule for Benzodiazepine-like Drugs to treat insomnia:
zolpidem (Ambien)
Schedule IV
zolpidem (Ambien) MOA:
Act as agonists at the benzodiazepine receptor site on the GABA receptor-chloride channel
How does zolpidem (Ambien) aid with insomnia?
Helpful with falling asleep
XR: helps with staying asleep
zolpidem (Ambien) ADRs:
1) Daytime Sedation/Drowsiness
- “Hang-over Effect” –> MOST COMMON SE
2) Sleep-driving
Does zolpidem (Ambien) result in Tolerance &/or Physical Dependence?
Nope
zolpidem (Ambien) Patient Teaching:
1) Avoid hazardous activities (driving) while adjusting
2) Avoid other CNS depressants (ETOH)
3) Teach family about sleep-driving risk
Name the 2 Non-Benzo/Non-Barbituates used to treat Anxiety:
1) buspirone (BuSpar)
2) hydroxyzine
buspirone (BuSpar) is not a 1) ___ __________ and is not used 2) ___.
1) CNS depressants
2) PRN
What are some other benefits of buspirone (BuSpar)?
NO abuse potential
NO suicide risk
NO increased CNS effecrs with other drugs (ETOH, benzos, etc.)
Why can’t we use buspirone (BuSpar) PRN?
Takes weeks to develop peak effects!
-May require a PRN Anxiolytic while therapeutic effects develop
What is the major Contraindication with buspirone (BuSpar)?
GRAPEFRUIT!
How do we switch from a Benzodiazepine to buspirone (BuSpar)?
Give buspirone (BuSpar) 2-4 wks before stopping the benzo -Need to Wean Benzo slowly!!
Does buspirone (BuSpar) result in Tolerance &/or Physical Dependence?
Nope
What class of drug is Hydroxyzine?
Antihistamine
What can we use Hydroxyzine for?
1) Anxiety (effects on serotonin)
2) Insomnia (anticholinergic effect)
Is Hydroxyzine a Scheduled Drug?
Nope
Hydroxyzine route and dosing:
1) PO
Dosing:
1) Routine: anxiety QID (4x/day)
2) PRN: insomnia
Hydroxyzine SEs:
ANTICHOLINERGIC SEs!!
1) Dry mouth
2) Constipation
3) Confusion
4) Dizziness
5) Headache
6) Fatigue
What serious ADR can occur with prolonged use of Hydroxyzine?
Prolonged QT-Interval!
Does Hydroxyzine result in Tolerance &/or Physical Dependence?
Nope
