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3922 > 20 - Sedatives, hypnotics and anxiolytics > Flashcards

20 - Sedatives, hypnotics and anxiolytics Flashcards

1
Q

What is sedation

A

Reduction in excitement, vigilance and physiological arousal so that the person is relaxed, calm and possibly sleepy

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2
Q

What is hypnosis

A

Ability to induce drowsiness and sleep

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3
Q

What do lesions of the anterior hypothalamus cause

A

Insomnia

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4
Q

What do lesions of the posterior hypothalamus cause

A

somnolence

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5
Q

What systems are part of the ARAS

A 
NorA
5HT
ACh
DA
HA
Orexin
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6
Q

What systems are sleep promoting

A

GABA
Adenosine
Melatonin

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7
Q

What is insomnia

A

Unsatisfactory sleep onset, maintenance or early waking

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8
Q

What are some treatments for insomnia (5-6)

A 
COGNITIVE BEHAVIOURAL THERAPY
PHARMACOTHERAPY
Barbiturates
Benzodiazepines
z-drugs
Melatonin
Antihistamines
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9
Q

Why did benzodiazepines replace barbiturates

A

Lower risk of abuse, overdose and induction of liver enzymes

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10
Q

How do benzodiazepines help with insomnia

A

Promote onset of sleep and ongoing sleep

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11
Q

What are most GABAA receptors made of

A

2 a, 2b and 1 y

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12
Q

What will the y subunit be replaced with in different brain regions

A

d, e and t

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13
Q

What subunits are benzodiazepines selective for

A

a1, a2, a3, a5

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14
Q

Benzo vs barbiturate action

A

Increase affinity and no. of openings vs

Increase length opening and increase channel

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15
Q

Are benzos active without GABA

A

No, but boosts GABA response

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16
Q

What are the clinical effects of benzodiazepines

A 
Hypnotic
Sedative
Anxiolytic
Amnesic
Antiepileptic
(Produce strange sleep behaviours)
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17
Q

What are some benzodiazepine sensitive GABAA receptor brain regions

A 
Amygdala
Prefrontal cortex
Hypothalamus
Striatum
Bed nucleus of striatum
Hippocampus
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18
Q

What does the a1 subunit mediate

A

Sedation
Hypnosis
Anticonvulsion

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19
Q

What do the a2 and a3 subunits mediate

A

Anxiolysis

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20
Q

What do the a3 and a5 subunits mediate

A

Myorelaxation

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21
Q

What are z-drugs

A

Chemically not benzodiazepines but act at BZ site

22
Q

What are the effects of Z-drugs

A

Same benefits and problems of BZ

Possibly less memory/cognition side effects, shorter half life (no daytime sedation)

23
Q

Which subunit do z-drugs show some preference for

A

a1

24
Q

What are some issues with benzodiazepines

A 
Ongoing use
Tapered stopping
Dependence liability
Strange sleep behaviours
Amnesiac 
Falls in elderly
Combining with other sedatives
25
Q

How do antihistamines help with insomnia

A

Histamines are arousing

26
Q

What are first generation antihistamines

A

H1 inverse agonist

27
Q

Why do antihistamines cross the BBB

A

Lipophillic

LMW, not PGP target

28
Q

What are side effects of antihistamine

A 
Dry mouth
Constipation
Blurred vision
Urinary retention
More daytime sedation
Fog
Memory issues even when drug no longer present
29
Q

Where is endogenous melatonin synthesised

A

Pineal gland

30
Q

What reduces melatonin production

A

Light, via thalamus, reduces melatonin production

31
Q

What are the two receptors for melatonin

A

2 GPCR
MT1
MT2

32
Q

What are the two functions of the two melatonin receptors

A

MT1 - sleep onset

MT2 - circadian timing

33
Q

What is a synthetic analogue of melatonin

A

Ramelteon

34
Q

Which neurotransmitters are activating

A

NorA, 5HT, ACh, DA, HA, Orexin

35
Q

Which neurotransmitters are sleep promoting

A

GABA, adenosine and melatonin

36
Q

What is fear

A

Threatening stimulus:

State of preparation for danger and results in arousal, vigilance, increased ability to respond and negative feelings

37
Q

What is anxiety

A

State of preparation for danger and results in arousal, vigilance, increased ability to respond and negative feelings BUT NO immediate threatening stimulus

38
Q

What is the criteria for anxiety

A

Patients have to experience symptoms causing significant personal distress with associated impairment in function

39
Q

What appears to play a central role in anxiety

A

Amygdala activity up-regulated

Issues with synaptic plasticity

40
Q

What are treatments for anxiety

A 
Cognitive and behavioural therapy
Benzodiazepines
Selective serotonin reuptake inhibitors
Serotonin/noradrenaline reuptake inhibitors
Tricyclics
Pregabalin
Buspirone
41
Q

What is the first line of treatment for anxiety

A

Benzodiazepines

42
Q

What are pros and cons of benzodiazepines

A

+ act rapidly

- dependence potential, drowsiness

43
Q

Which benzodiazepines are used for anxiety

A

Alprazolam

Clonazepam

44
Q

Which drugs are not a good choice for anxiety

A

‘z drugs’

45
Q

Where is serotonin released from

A

Raphe nuclei

46
Q

What do serotonin axon projections influence

A 
Sleep
Arousal
Attention
Sensory processing in the cortex
Emotion
Mood
47
Q

What are some SSRIs for anxiety

A

Fluoxetine and paroxetine

48
Q

What is the first treatment for most anxiety disorders

A

SSRIs

49
Q

What are pros and cons of SSRIs

A 
Pros: Less side effects
May allow dual treatment for depression
Cons: Very slow to act
Sometimes side effects difficult
Have discontinuation syndrome
50
Q

What are some other anxiolytics

A

Serotonin/noradrenaline reuptake inhibitors
Other antidepressants
Pregabalin (GABA analgoue)
Buspirone (Partial 5HT1A agonist for treatment of GAD)
Alcohol

3922 (19 decks)

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