Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

CPTP 3 > CPTP 3.5 Neuropharmacology 3 (Hypnotics and Anxiolytics) > Flashcards

CPTP 3.5 Neuropharmacology 3 (Hypnotics and Anxiolytics) Flashcards

1
Q

What are the stages of sleep?

A

First 3 hours –> ‘slow wave’ sleep

After that –> REM sleep

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What happens during each stage of sleep, and what brain region is responsible for the activity?

A

Slow wave sleep:
• Hippocampus and neocortex
• Reactivation of memories from the day

REM sleep:
• Cortex
• Consolidation of memory into long-term stores

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Recall the mechanisms of arousal

A
  • Suprachiasmatic nucleus receives messages from the retina
    • This activates the dorsomedial hypothalamic nucleus
    • This activates the arousal pathways
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Recall the ascending arousal pathways (which are activated by the dorsomedial hypothalamic nucleus)

What do they all do?

A
  • Raphe nucleus (5-HT)
    • Locus coeruleus (noradrenaline)
    • Tuberomammillary nucleus (histamine)

These project to the cortex and keep it alert by “washing over” the synapses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What structures inhibit the ascending arousal pathways?

A 
Ventrolateral preoptic nucleus
  •  GABA
  •  Galanine
Pineal gland
  •  Melatonin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the arousal and sleep-inducing neurotransmitters?

A 
Sleep inducing:
  •  GABA
  •  Galanine
  •  Melatonin
Arousal:
  •  Histamine
  •  Noradrenaline
  •  Serotonin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What happens to sleep as you age? Why?

A

Much reduced duration of sleep. You produce less melatonin as you age

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the types of insomnia?

A
  • Initial (cant get to sleep)
    • Middle (wake up in the middle of the night)
    • Early waking
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the causes of insomnia?

A 
>Stress
>Psychiatric disorders:
  •  Anxiety
  •  Depression
  •  Bipolar
  •  PTSD
>Illness
  •  Alzheimers
  •  Rheumatoid arthritis
  •  Asthma
>Medication
  •  Stimulants
  •  Antidepressants
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why does stress cause insomnia?

A

Increased HPA axis activity causes arousal pathways to be more active

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What cause of insomnia gives rise to:

1) initial insomnia?
2) terminal insomnia?

A

1) Anxiety

2) Depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What effect do bipolar disorder and PTSD have on sleep?

A

Bipolar disorder:
• Less SWS
PTSD:
• Less REM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What properties must a hypnotic have?

A
  • Short half-life
    • Inhibits ascending arousal pathways
    • Does not affect REM or SWS brain areas
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What physiological effect does anxiety have?

A 
Sympathetic NS activation:
  •  CV
  •  Hyperventilation
  •  Sweating
  •  GI (butterflies)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What ‘theme’ of core symptoms fo anxiety disorders share?

A

Fear, escape, avoidance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Name the anxiety disorders

A
  • OCD
    • PTSD
    • GAD
    • Panic disorder
    • Agoraphobia
    • Social anxiety
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What three main neurotransmitters are associated with anxiety disorders?

A

Serotonin and noradrenaline - Increased
• Increased release

GABA - Decreased
• Decreased amounts of GABA-A receptor function, so less binding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What effect do SSRIs have on 5-HT levels and anxiety?

A

Increases 5-HT in synaptic cleft, and increases anxiety

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

How are hypnotics and anxiolytics linked?

A

They both are non-specific CNS depressants that reduce levels of arousal, the difference is the dose.

(To induce sleep, a higher dose is needed than for anxiolytic effects.)

20
Q

How should hypnotics and anxiolytics half lives differ?

A

Anxiolytics - Long half life

Hypnotics - Short half life

21
Q

What are the classes of hypnotics and anxiolytics? What separates these?

A
  • Barbituates
    • Benzodiazapines
    • (Alcohol)

HYPNOTIC ONLY:
• Z-hypnotics
• Antihistamines

Therapeutic windows and pharmacokinetics

22
Q

Why are barbituates not used any more?

A
  • Interact with alcohol

* Very small therapeutic window

23
Q

Name the formulary benzodiazepines. What is the half-life and use of each?

Name the formulary Z-hypnotic

A
  • Temazepam, 10hrs, hypnotic
    • Lorazepam, 15 hrs, anxiolytic
    • Chlorodiazepoxide, 20hrs, anxiolytic
    • Diazepam, 40hrs, anxiolytic

Z-hypnotic:
• Zopiclone, 6 hours

24
Q

What other use can hypnotics and anxiolytics have?

A
  • Reduce muscle tone (i.e. in tension headaches)
    • Anticonvulsant
    • Surgical sedative
25
Q

What drug is used as a surgical sedative, what is its half life and drug class?

A

Midazolam
• t(1/2) = 1-4 hours
• benzodiazapine

26
Q

Why do chlorodiezepoxide and diezepam have such long half-lives?

A

Their metabolites are biologically active

27
Q

What are the adverse effects associated with hypnotics and anxiolytics?

What causes many of these?

A
  • Interaction with alcohol
    • Poor motor co-ordination
    • Poor memory (this is why roofies, a benzo, causes the victim to not remember)
    • Decreased REM sleep
    • Tolerance, dependence and withdrawal syndrome

Neurological side effects caused by non-selective CNS suppression

28
Q

What are the modes of action of the hypnotics and anxiolytics classes?

A

Barbituates:
• Non-selective depressant activity, reduces Na+ channels preventing action potentials
• GABA-A receptor has barbiturate site which can activate it in absence of GABA, by opening the Cl- channel

Alcohol:
• Allosteric modulator of GABA-A receptor (enhance effect of GABA)

Benzodiazepines:
• Allosteric modulator of GABA-A receptor (enhance effect of GABA)

Z-hypnotics:
• Allosteric modulator of GABA-A receptor (enhance effect of GABA)

29
Q

Why do barbiturates have a smaller therapeutic window and less safe in overdose?

A

They activate GABA-A, rather than modulate it, thus GABA does not need to be present, making it much more potent. (endogenous GABA cannot act as a rate-limiting step)

30
Q

What is the nature of the interaction between alcohol and the hypnotic/anxiolytic drug classes?

A

They potentiate each other.

31
Q

How many subunits are in each GABA-A receptor, and what types?

A
  • Two alphas
    • Two betas
    • One ‘other’ –> USUALLY gamma-2 in the brain
32
Q

Why are benzodiazepines described as ‘non-selective’?

A

They are selective for GABA-A receptors whose fifth subunit is gamma-2, which accounts for most GABA-A receptors in the brain

33
Q

Where are the targetted GABA-A receptors?

A

In the ascending arousal pathways

NB: endogenous GABA pathway terminating here is the ventrolateral preoptic nucleus

34
Q

Why are benzodiazepenes not recommended for chronic use?

A

Rebound anxiety:

  • Patient with anxiety has reduced GABA function
  • Benzodiazepines are administered, and GABA function is increased, anxiety decreases
  • GABA receptors begin to adapt to the benzo therapy, slowly reducing the GABA function due to tolerance
  • When benzo therapy is removed, this adaptation remains, so brain GABA function is even lower than on day 0
  • This causes even more severe anxiety after removal of therapy
35
Q

How do Z-hypnotics compare to benzodiazepines?

A

They bind to the same site, but do not share the same structure.

Z-hypnotics are more selective, as they are selective for a-1 subunit-containing pentamers (as the fifth subunit), rather than the gamma-2

36
Q

Why should hypnotics have a shorter half life?

A

To reduce hangover

37
Q

How do antihistamines work as hypnotics?

A

H1 antagonists, inhibit histamine excitatory pathways from the tuberomammillary nucleus

Must be “drowsy” antihistamines (first generation)

38
Q

What are the side effects of antihistamines used as hypnotics?

A
  • Weight gain with long-term use

* Anticholinergic effects (dry mouth, constipation, etc.)

39
Q

Do Z-hypnotics cause dependence?

A

Yes

40
Q

What is NICE guidance on prescribing for insomnia?

A

If severe, prescribe benzos or Z-hypnotics for short periods

41
Q

What should be prescribed for depression/anxiety co-morbid patients?

A

SSRIs, which are active on most anxiety disorders, therefore 2 birds with one stone

42
Q

Which antidepressants can be used as anxiolytics, what neurotransmitter do these focus on?

A

Focuses on 5-HT neurotransmission:

SSRIs
• For comorbid depression and (any) anxiety disorder

SNRIs
• GAD

TCAs
• Panic disorder
• GAD

MAOs
• Panic disorder
• Agoraphobia
• Social Phobia

43
Q

What does each antidepressant class inhibit?

A

Serotonin reuptake transporter on presynaptic membrane
• SSRIs
• SNRIs
• TCAs

Monoamine oxidase underneath that membrane
• MAOIs

44
Q

But wait, antidepressants increase 5-HT, which is excitatory, but it still treats anxiety? What gives?

A

Initially, an increase in anxiety is seen (anxiogenesis stage) due to the increase in 5-HT.

Eventually, tolerance occurs, and 5-HT2A receptors are downregulated, and 5-HT1A receptors are upregulated (anxiolysis)

Takes time because changes in protein expression are needed

45
Q

Should you use benzos or SSRIs for anxiolysis

A

SSRIs
• Benzos cause withdrawal symptoms
• Benzos do not treat depression

Do not use benzos for anxiety disorders over a long period of time

CPTP 3 (21 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions