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UM2010 Pharmacology > Anxiolytics & Hypnotics > Flashcards

Anxiolytics & Hypnotics Flashcards

1
Q

What is the definiton for anxiolytic?

A

Reduces anxiety

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2
Q

What is the definiton of hypnotic?

A

Assists sleep (also called soporifics)

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3
Q

What is the definition of relaxants?

A

Usually mean muscle relaxants

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4
Q

Minor tranquillisers are AKA

A

Sedatives

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5
Q

Major tranquillisers are AKA

A

Antipsychotics

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6
Q

What is anxiety?

A

Normal human emotional state: we have things we rationally need to worry about.

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7
Q

The difference between normal and pathological anxiety is not clear, true or false?

A

True

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8
Q

What are the two concepts of anxiety?

A

Fear

Generalised anxiety

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9
Q

What are the different types of anxiety disorders?

A
  • Panic disorder
  • Social anxiety disorder (SAD)
  • Phobias
  • Obsessive-compulsive disorder (OCD)
  • Generalised anxiety disorder (GAD)
  • Post-traumatic stress disorder
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10
Q

What part of the brain is responsible for anxiety & emotional processes ?

A

Amygdala & prefrontal cortex (PFC)

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11
Q

In anxiety disorders, what happens in the brain?

A

Dysfunctional PFC-amygdala communication

Amygdala hyperactivity

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12
Q

Amygdala hyperactivity is associated with?

A

Anxiety

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13
Q

5-HT associated with

A

Mood stability

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14
Q

What are the pharmacological strategies for Anxiolytics?

A

Increased monoaminergic / serotinergic activity:
Antidepressants, especially SSRIs
5-HT1A agonists (buspirone)
Atypical antipsychotics

Increase GABAergic (inhibitory) activity:
           GABAA receptor stimulation
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15
Q

What are the other options for anxiolytics?

A

Beta-blockers (propranolol) for physical symptoms

Pregabalin

Ketamine? Cannabidiol?

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16
Q

Main anxiolytics drugs used are?

A

Antidepressants drugs (5-HT) - Work through monoaminergic (esp. serotonergic) pathways

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17
Q

5-HT antidepressant drugs in anxiolytics are poor at dealing with?

A

Acute anxiety attacks

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18
Q

What are the preferred antidepressants as anxiolytics?

A

SSRIs preferred (e.g. sertraline, citalopram, fluoxetine)

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19
Q

Antidepressants as anxiolytics are effective against?

A

generalised anxiety, phobias, social anxiety disorder and post-traumatic stress

may also treat depression associated with anxiety

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20
Q

Buspirone, function and effect?

A

5-HT1A partial agonist

  • Used for general anxiety states; weak for panic attacks and severe anxiety. No antidepressant action.
  • Clinical effects not observed for up to 2 weeks.
  • Also binds to dopamine receptors; possible function in anxiety unclear
21
Q

Most common GABAA receptors subunit combination is?

A

a1b2g2

22
Q

In GABAA receptors, a1 subunits more associated with?

A

Hypnotic effects

23
Q

In GABAA receptors, a2/3 subunits more associated with?

A

Anxiolytics effects (amygdala)

24
Q

What are Benzodiazepines?

A

BDZs are GABAAR positive allosteric modulators; increase likelihood of channel opening

25
Q

What happens when benxodiazepines ( i.e. diazepam) binds to GABA

A

With GABA bound, receptor flits between open and closed states > more CL- enter

26
Q

GABAA receptors are ionotropic, which means?

A

Cl- channels

27
Q

Administration and use of Benzodiazepines

A

Orally active

Useful for acute anxiety; fast acting (~30 mins)

28
Q

All BDZs largely identical in side effects

True or false

A

True

29
Q

Therapeutic use of benzodiazepines are determined by duration of effect: long lasting? Medium acting? Short acting?

A

Long lasting – anticonvulsants, anxiolytics
Medium acting – anxiolytics
Short acting – anxiolytics, hypnotics

30
Q

Side effects of benzodiazepines in abuse, dependency, tolerance, overdose & toxicity

A

Abuse: calming, dream state, also + alcohol

Dependency: withdrawal rebound anxiety: hallucinations, tremor, seizures

Tolerance: downregulation of a2-containing GABAARs?

OD & toxicity: relatively safe except with alcohol. Treat with flumazenil, BDZ site antagonist

31
Q

Side effects of benzodiazepines

A

Side effects: Well tolerated; drowsiness, confusion, amnesia, loss of co-ordination, enhancement of other depressants

32
Q

Diazepam

A

Anxiolytic, muscle relaxant, anticonvulsant. ~70% of BDZ prescriptions

33
Q

Clobazam

A

Anticonvulsant only

34
Q

Clonazepam

A

Anticonvulsant – very uncommon as anxiolytic

35
Q

Midazolam

A

Ultra-short-acting, i.v. surgical sedation, i.v. anaesthesia induction (rare), i.v. anticonvulsant oral hypnotic (rare in UK)

36
Q

Some old literature may refer to “benzodiazepine receptors”. These are AKA?

A

GABAA receptors

37
Q

What is used for benzodiazepines overdose?

A

Flumazenil

38
Q

What was the preferred medication for anxiolysis before BDZs?

A

Barbiturates

39
Q

Barbiturates are very similar in MoA and effects to but more powerful?

A

Benzodiazepines

40
Q

Side effects of Barbiturates

A

Higher abuse risk
Higher addiction risk
Dangerous in OD

41
Q

What benzodiazepines drugs can be used as hypnotics?

A

“Z-drugs”: e.g. zolpidem, zopiclone & zaleplon

42
Q

moa of “Z-drugs”?

A

Structurally dissimilar, but bind to same site as BDZs
Only active at a1 subunit-containing GABAARs.
Hypnotic&raquo_space;> anxiolytic
Ultrashort duration (<4h)

43
Q

Side effects of “z drugs”

A

tolerance & dependency, abuse risk

44
Q

Which Z drug is thought to improve function after brain damage?

A

Zolpidem

45
Q

Diazepam subunit selectivity

A

a1, a2, a3, a4, a5, a6

46
Q

Flunitrazepam subunit selectivity

A

a1, a2, a5

47
Q

Midazolam subunit selectivity

A

a1, a2, a3, a4, a5, a6

48
Q

Flumazenil subunit selectivity

A

(antagonist) a1, a2, a3, a4, a5, a6

49
Q

Zolpidem subunit selectivity

A

a1

UM2010 Pharmacology (7 decks)

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