PHARM - Anxiolytic and Hypnotic Drugs - Week 10 Flashcards

1
Q

What other condition do anxiety disorders often coexist with?

A

Depression

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2
Q

What four aspects of life are anxiety disorders often associated with?

A

High degree of social and work impairment
Poor quality of life
Frequent relapses

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3
Q

Briefly describe panic disorder.

A

Sudden episodes of overwhelming fear with somatic symptoms

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4
Q

Briefly describe obsessive-compulsive disorder.

A

Compulsive and ritualistic behaviours as well as purposeless activities driven by irrational fears and thoughts

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5
Q

Briefly describe post-traumatic stress disorder.

A

Anxiety triggered by recall of past traumatic and stressful experiences

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6
Q

Briefly describe phobias.

A

Intense fear of objects or situations

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7
Q

Briefly describe generalised anxiety disorder.

A

A feeling of nervousness, tension, or worry not associated with a specific event, situation, or object

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8
Q

Briefly describe social anxiety disorder.

A

Fear of being with and interacting with people

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9
Q

Anxiety is associated with a dysregulation of what four neurotransmitter systems?

A

GABA
Serotonin
Noradrenaline
Dopamine

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10
Q

What do the most effective therapeutic agents for anxiety do (2)?

A

Potentiate GABA and serotonin neurotransmission

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11
Q

Is GABA inhibitory or excitatory?

A

Inhibitory

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12
Q

Is glutamate inhibitory or excitatory?

A

Excitatory

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13
Q

Is serotonin widely used in the CNS or only very specific parts?

A

Widely used

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14
Q

What do anxiolytics do (3)?

A

Relieve anxiety and tension without notably impairing consciousness

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15
Q

What do hypnotics do?

A

Produce drowsiness, encouraging the onset of a state of sleep

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16
Q

Is insomnia a disease entity?

A

No

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17
Q

How are insomnia and anxiety related?

A

Insomnia is a common clinical manifestation of anxiety

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18
Q

Name three non-pharmacological interventions for insomnia.

A

Diet
Exercise
Routine change

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19
Q

What two things may be responsible for insomnia?

A

Disease and environmental factors

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20
Q

What kind of drugs are benzodiazepines and what is its mechanism of action? In what way does it bind to receptors?

A

They are anxiolytics.

They potentiate the effects of GABA on GABAa receptors by binding allosterically.

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21
Q

How are benzodiazepines classified?

A

By the duration of their half-life.

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22
Q

Do benzodiazepines have predictable or unpredictable side effects?

A

Common and predictable

23
Q

Name 5 side effects of benzodiazepines.

A
Confusion
Drowsiness/impaired coordination
Long-lasting hangover effects
Tolerance and dependence
Supression of REM sleep
24
Q

Do benzodiazepines have a wide or narrow therapeutic margin? What does this indicate about its safety?

A

Wide window - good safety margin

25
Q

When can benzodiazepines be lethal?

A

If taken in excess with alcohol or other CNS depressants like opioids and anticonvulsants

26
Q

Do benzodiazepines have good absoprtion orally? What is this determined by?

A

Good absorption after oral administration.

Determined by lipophilicity.

27
Q

What happens to benzodiazepines in the body metabolically for its clearance to occur? What system is critical for this to occur and what function should be checked as a result when administering benzodiazepines?

A

Transformation or biotransformation to hydrophilic metabolites.
The microsomal liver system is critical for this.
Liver function should be checked.

28
Q

Many benzodiazepines have active metabolites. Are agents with or without them preferred for older patients?

A

Agents without active metabolites are preferred for older patients.

29
Q

Are drug interactions common or rare with benzodiazepines? Give one example.

A

They are common

Mood stabilisers - reduce the elimination of benzodiazepines

30
Q

What should benzodiazepines never be taken with and why? What can occur as a result?

A

Do not mix with alcohol.

It causes additive CNS depression, possibly leading to death.

31
Q

Are benzodiazepines addictive? Compare it to heroin.

A

It is addictive - more difficult to stop than heroin.

32
Q

What do benzodiazepines increase the risk of in older patients and why?

A

Risk of falling due to possible drowsiness.

33
Q

Describe what the dosage should be like with benzodiazepines (2).

A

Start low and increase the dose gradually.

Decrease the dose if drowsiness and confusion occur.

34
Q

Can benzodiazepines cross the placenta?

A

Yes, it accumulates in foetal circulation

35
Q

Can benzodiazepines cross into breast milk?

A

Yesd

36
Q

Are benzodiazepines teratogenic (2)?

A

Yes, cleft palate occurs

37
Q

How long does it take to gain tolerance/dependence to benzodiazepines?

A

A couple of weeks.

38
Q

What happens if sudden discontinuation of benzodiazepines occur?

A

Withdrawal symptoms

39
Q

List 7 typical withdrawal symptoms of benzodiazepines.

A
Anxiety
Restlessness
Shakes
Rebound insomnia (worse than pre-treatment)
Weakness
Orthostatic hypotension
Generalised seizures
40
Q

What is the recommendation to prevent benzodiazepine withdrawal symptoms?

A

Gradual dose reduction over 2 months.

41
Q

Name a non-benzodiazepine anxiolytic and briefly describe what it does. Compare it to benzodiazepines (3).

A

Buspirone
Relieves anxiety without causing marked sedative/hypnotic effects
Lacks muscle relaxant and anticonvulsant properties

42
Q

Briefly describe how buspirone works (2) and whether it acts on GABAa directly.

A

No direct effects on GABAa

Is a partial agonist of 5HT1a and some affinity for D2 receptors.

43
Q

Does busiprone have abuse liability? Is there a risk of rebound anxiety or withdrawal symptoms?

A

Has minimal abuse liability

No rebound anxiety or withdrawal symptoms

44
Q

How long does buspirone take to have an effect? Is it useful for acute anxiety states?

A

May take 3-4 weeks to take effect.

Not useful for acute anxiety states.

45
Q

Does buspirone affect driving?

A

No

46
Q

List 4 adverse effects of buspirone.

A

Less psychomotor impairment than benzodiazepines
Dizziness
Headache
GI disturbances

47
Q

Does buspirone have rapid oral absorption?

A

Yes

48
Q

Should liver function be checked when administering buspirone?

A

Yes

49
Q

Can benzodiazepines act as a hypnotic?

A

Yes

50
Q

How do benzodiazepines act as hypnotics?

A

They enhance GABA transmission.

51
Q

Name three side effects of using benzodiazepines as hypnotics.

A

Broken sleep
Supression of REM sleep
Rebound insomnia (abrupt cessation)

52
Q

Name 2 benzodiazepine-related drugs that can be used as hypnotics and describe briefly how they work.
Do they cause REM sleep suppression?

A

Zopiclone
Zolpidem
Increases GABA transmission by selectively binding to BZ1
Dont cause REM sleep suppression

53
Q

Do antidepressants carry a risk of dependence like benzodiazepines?

A

No