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PHARM L19: Sedatives and Hypnotics

Terms in this set (44)

Which of the following is NOT true about GABA-A receptors?
A) inhibitory, post-synaptic
B) powerful and rapid enhancement of excitation
C) composed of 5 subunits: two α, two β and 1 γ
D) great enhances precision of excitatory synaptic transmission
E) Involves Cl- channel
B) powerful and rapid enhancement of excitation
*SUPPRESSION
Which subunit is necessary for benzodiazepine binding at the GABA-A receptor?
γ
*diazepam (valium), chlordiazepoxide (librium), Seresta
Which of the following is NOT true about allosteric modulation of GABA receptors?
A) GABA agonists activate Cl- channels
B) Barbiturates and BZDs do not bind to the GABA site
C) There are specific binding sites for each class
D) Barbiturates can indirectly modulate GABA receptor activity
E) BZDs directly increase Cl- flux, but barbiturates do not
E) BZDs directly increase Cl- flux, but barbiturates do not

*Barbiturates directly increase Cl- flux, BZDs do not
*Indirectly facilitate effects of GABA or direct agonists
Which of the following statements about dimensionality of sedatives is TRUE?
A) Increasing dose leads to greater CNS depression
B) Barbiturates had more predictable dose-response effects, but retained the CNS depression
C) BZDs were developed to minimize depth of CNS depression
D) Classic GABA drugs such as chloral hydrate were highly lethal
E) All are true
E) All are true
What are benzodiazepines used for?
- Anxiety
- Sleep disorders
- Seizure disorders
- Anesthesia adjunct (amnesia, reduce post-op pain)
- Withdrawal (alcohol, BZDs, barbiturates)
Which of the following is NOT true about benzodiazepines?
A) good therapeutic ratio
B) causes motor incoordination and cognitive slowing
C) can lead to tolerance and dependence
D) often short-acting, so less risk of drug interaction
E) can cause respiratory depression in combination with other sedatives
E)
D) often short-acting, so less risk of drug interaction
*LONG-lasting, greater risk of drug interactions (especially alcohol)
List the BZD agonists
DIAZEPAM
CHLORDIAZEPOXIDE
MIDAZOLAM
Which BZD agonist has a wide range of actions and is long-lasting?
A) flumazenil
B) phenobarbital
C) chlordiazepoxide
D) diazepam
E) all of the above
D) diazepam
Which BZD agonist is water soluble and largely replaced by midazolam?
A) flumazenil
B) phenobarbital
C) chlordiazepoxide
D) diazepam
E) all of the above
C) chlordiazepoxide
Which of the following is a BZD antagonist?
A) zaleplon
B) midazolam
C) flumazenil
D) diazepam
E) chlordiazepoxide
C) flumazenil
*blocks the effects of BZDs
*will precipitate withdrawal in BZD-dependent subjects
Name 2 non-BZDs/non-barbiturates that have GABA-A activity but different structures
ZOLPIDEM
ZALEPLON
What is zolpidem used for?
What is zaleplon used for?
- sleep
- sleep, short-acting
*Non-BZDs, Non-barbiturates
What are pentobarbital and amobarbital used for?

What is phenobarbital used for?

What is thiopental used for?
sleep

seizure disorders

induce anesthesia
Compounds that increase drowsiness and sleep are ___________.

Compounds that reduce anxiety and increase calm (decrease activity) are _____________.
hypnotics

sedatives
Which of the following is a melatonin drug?
A) ramelteon
B) diphenhydramine
C) zaleplon
D) flumazenil
E) none of the above
A) ramelteon
Which of the following is an antihistamine?
A) ramelteon
B) diphenhydramine
C) zaleplon
D) flumazenil
E) all of the above
B) diphenhydramine
Which of the following is NOT a characteristic of anxiety?
A) tension and poor concentration
B) muscle tension
C) fatigue
D) autonomic depression
E) glucocorticoid release
D) autonomic depression
*autonomic hyperexcitability
Describe the criteria for pathological anxiety (3)
• absence of a threat
• out of proportion to the threat
• AND impair the individual's ability to function
The following characteristics describes which anxiety disorder?
• chronic, non-reactive
• motor tension (trembling, twitching)
• autonomic arousal (↑ respiration, ↑ HR, sweat, nausea)
• vigilance (↑startle, irritable, difficulty concentrating)
Generalized anxiety disorder
The following characteristics describes which anxiety disorder?
• recurrent, non-reactive
• feelings of terror or doom
panic disorder
The following characteristics describes which anxiety disorder?
• Fears of specific objects
• May be reactive, but response is out of proportion to threat and impairs ability to function
• Increasingly treated with drugs
Phobias
The following characteristics describes which anxiety disorder?
• Recurrent
• Persistent ideas, thoughts, actions
• Repetitive, stereotypic, purposive and intentional behaviors • Performing behavior relieves tension
Obsessive-Compulsive Disorder
The following characteristics describes which anxiety disorder?
• Acute or chronic reaction to severe event
• Does not respond well to current treatments
Acute/Post-traumatic Stress Disorder
How do GABA agonists affect anxiety? GABA antagonists?
• Agonists decrease anxiety
• Antagonists induce anxiety and panic
What is the effect of increased serotonin on levels of anxiety?
• ↑ levels related to ↑ increased anxiety
• ↓ levels related to ↓ anxiety
Which drugs are most effective treatments for GAD?
BZDs
- short-term use only bc risk of dependence
- not effective with panic, OCD, PTSD
- not best for social anxiety
Describe the acute uses for GABA
surgical/dental sedation, severe acute panic attacks
List the serotonin drugs used to treat anxiety
BUSPIRONE
FLUOXETINE
CLOMIPRAMINE
hallucinogens: psilocybin

*high doses can exacerbate anxiety
*not useful for social anxiety disorder
List the disorders associated with the following drugs.
• Buspirone
• Fluoxetine
• Clomipramine
• Psilocybin
• Buspirone: mild-moderate GAD
• Fluoxetine: panic disorder, OCD
• Clomipramine: OCD
• Psilocybin: PTSD, other severe anxiety disorders
JM is a 29 year-old male who reports he feels stressed and exhausted all the time. He reports persistent worries about potential layoffs at work and events outside work and has taken sick days off work due to these worries.

Which disorder does he likely have?
A. generalized anxiety disorder
B. panic attacks
C. obsessive-compulsive disorder
D. phobias
E.post-traumatic stress disorder

Which drug should be prescribed?
A. Zolpidem
B. Flumazenil
C. Pentobarbital
D. Fluoxetine
E. Midazolam
A. generalized anxiety disorder

E. Midazolam
Describe each type of insomnia.
• Onset
• Maintenance
• Termination
O: trouble falling asleep

M: wake frequently during the night (NOT due to stimulation, bladder, etc.)

T: can't go back to sleep
Which of the following is/are characteristics of onset insomnia? Select all that apply.
A) body temperature still falling at normal sleep time so can't fall asleep right away
B) wake frequently during the night
C) body temperature rises at normal sleep time so wake up sooner and can't go back to sleep
D) depends on levels of adenosine, melatonin, serotonin, adrenaline
A) body temperature still falling at normal sleep time so can't fall asleep right away
D) depends on levels of adenosine, melatonin, serotonin, adrenaline

B: maintenance insomnia
C: termination insomnia
Which of the following is/are characteristics of maintenance insomnia? Select all that apply.
A) body temperature still falling at normal sleep time so can't fall asleep right away
B) wake frequently during the night
C) body temperature rises at normal sleep time so wake up sooner and can't go back to sleep
D) rapid entry into REM sleep, ahead of regular onset
C) body temperature rises at normal sleep time so wake up sooner and can't go back to sleep
D) rapid entry into REM sleep, ahead of regular onset
Describe the behavioral treatments for insomnia
• Decrease stimulation
• Use bed only for sleeping
• Light therapy (or timing): SCN sensitive to blue/green light, not red
• Scheduled meals
• Scheduled exercise (mid-day, evening best)
There are 4 stages of sleep.
Which stages are more prevalent in the early evening?
Which are more prevalent in the late evening?
3-4
(less in REM)

REM
(less stages 3-4)
Stage 1 of sleep is associated with:
A) sleep spindles and K complexes
B) mostly slow waves
C) high voltage and high frequency
D) low voltage and mixed frequency
E) A and D
D) low voltage and mixed frequency
What is the role of the reticular formation of the brain?
Which NT is associated with this?

Role of basal forebrain? NT?
Maintain arousal
ACh

- Increases arousal, learning and attention: ACh
- Inhibits thalamus & cortex: GABA (triggered by adenosine accumulation)
Which NT is associated with the pathway for stimulating arousal in the hypothalamus?

Which NT is associated with the pathway for promoting sleep in the hypothalamus?
histamine

GABA
What is the role of ACh and histamine in the chemical mechanisms for sleep?

What is the role of GABA, adenosine, and blockade of Glu and histamine?
excitation and arousal
• ACh - nicotine
• blockage of adenosine - caffeine

inhibition and drowsiness
- GABA: sedative hypnotics, general anesthetics, alcohol
- Adenosine: triggers sleep cascade in basal forebrain
- Block: antihistamines - drowsiness; Glu blockers - loss of consciousness, bizarre dreams
Which drugs are preferred for treatment of insomnia?
newer, short-acting compounds
"Non-BZDs" - ZOLPIDEM, ZALEPLON
• short-acting, fewer adverse effects
• less tolerance, dependence, rebound insomnia
Which of the following statements regarding Ramelteon is TRUE?
A) effective for long-term use
B) melatonin receptor antagonist
C) decreases latency to sleep without rebound insomnia
D) long-acting compound preferred for treatment of insomnia
E) for maintenance insomnia only
C) decreases latency to sleep without rebound insomnia
*NOT effective for short-term use
*melatonin receptor AGONIST
*ONSET insomnia only
What primarily resets the biological clock?

Which gland releases melatonin?

What is the function of melatonin?
Clinical uses?
Risks?
light

pineal gland

- released 2 hrs before bedtime, doses at other times resets cycle & sleepier earlier
- helps prevent jet lag, changing shifts
- long-term use alters fertility and worsens movement disorders
- causes birth defects if taken during pregnancy
Jeanette visits her PCC for a regularly scheduled checkup. She is perimenopausal, has a BMI of 27, is diabetic, and was diagnosed with an anxiety disorder while in her mid-20s. She is currently stable and continues to take paroxetine for anxiety. She has been very tired during the day and she has had increasing trouble trying to sleep. She usually doesn't have much trouble falling asleep, but awakens several times every night, and often has difficulty getting back to sleep. Jeanette agrees to take a medication to treat sleep maintenance symptoms of insomnia.
It is most likely:
A. Zolpidem
B. Ramelteon
C. Pentobarbital
D. Fluoxetine
E. Midazolam
A. Zolpidem
*long-acting
Why does Benadryl knock me out, but Claritin and Allegra don't?
A. diphenhydramine (Benadryl) acts at H1 receptors and loratadine (Claritin) acts at H2
B. diphenhydramine acts at H3 receptors and loratadine acts at H1
C. diphenhydramine acts at H2 receptors and loratadine acts at H4
D. diphenhydramine and loratadine have different affinities for mast cells
E. diphenhydramine penetrates into the brain, but loratadine penetrates poorly
E. diphenhydramine penetrates into the brain, but loratadine penetrates poorly
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