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Psychiatry > Pharmacology of Anxiolytic Drugs > Flashcards

Pharmacology of Anxiolytic Drugs Flashcards

1
Q

Give some examples of benzodiazepines.

A

Midazolam (Hypnovel)
Lorazepam (Ativan)
Loprazolam
Oxazepam

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2
Q

What are the pharmacological effects of benzodiazepines?

A
  • Reduce anxiety and aggression.
  • Hypnosis/sedation.
  • Muscle relaxation.
  • Anticonvulsant effect.
  • Anterograde amnesia (loss of ability to form new memories).
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3
Q

What is the choice of benzodiazepine determined by?

A

Duration of action

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4
Q

How do all benzodiazepines act?

A

By increasing GABA-mediated inhibition

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5
Q

What is GABA (in the brain)?

A

The main inhibitory transmitter in the brain

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6
Q

What does GABA stand for?

A

Gamma Amino Butyric Acid

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7
Q

GABA has a __________ distribution

A

WIDESPREAD

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8
Q

Where is glycine restricted to?

A

The spinal cord and brain stem.

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9
Q

What does GABA cause in target cells?

A

Hyperpolarisation

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10
Q

Describe the action of benzodiazepines.

A 
Act by enhancing the action of GABA at the
GABAA receptor (increased inhibition)
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11
Q

Is the GABA binding site and the benzodiazepine binding site the same?

A

NO

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12
Q

NICE say that use of benzodiazepines should not exceed what?

A

4 weeks

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13
Q

Give 3 examples of substances which exhibit anxiolytic properties in humans +/or some animal tests of anxiety.

A

Ethanol, neurosteroids and barbiturates

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14
Q

What have anxiogenic properties?

A

Inverse BDZ agonists ie. β-carbolines

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15
Q

Name a drug that can increase anxiety.

A

Flumazenil (antagonist).

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16
Q

In behavioural tests, drugs which do what have been shown to be weak anxiolytics?

A

Drugs which increase GABA concentration in the brain, or act directly on GABAA receptors.

17
Q

Benzodiazepines are fairly safe in overdose. Explain this.

A

Alone, they are unlikely to cause respiratory depression

18
Q

Name a benzodiazepine antagonist.

A

Flumazenil.

19
Q

What happens of withdrawal of benzodiazepines?

A

Rebound anxiety and sometimes physical symptoms

20
Q

Outline 3 specific problems with benzodiazepines.

A
  • Cause paradoxical aggression – due to disinhibition.
  • anterograde amnesia and impaired co-ordination (beware rohypnol).
  • Cause tolerance and dependence.
21
Q

Benzodiazepines should be used for a max of ____ weeks

A

FOUR

22
Q

What may rapid withdrawal of benzodiazepines cause?

A

Confusion, toxic psychosis and even convulsions

ALSO- insomnia, subjective anxiety, insomnia, loss of appetite and body weight, tremor, perspiration, tinnitus, and perceptual disturbances

23
Q

Aside from rapid withdrawal of benzodiazepines, what can also cause withdrawal symptoms?

A

Neuroadaptation of the GABA response:
Chronic treatment causes decreased response to GABA, so withdrawal results in anxiety/convulsions possibly due to decreased density of BZ receptors.

24
Q

Outline how a patient should safely be withdrawn from benzodiazepines.

A
  1. Transfer patient to equivalent daily dose of diazepam/chlordiazepoxide, preferably taken at night.
  2. Reduce dose every 2–3 weeks in steps of 2 or 2.5 mg; if withdrawal symptoms occur, maintain this dose until symptoms improve.
  3. Reduce dose further, if necessary in smaller steps; it is better to reduce too slowly rather than too quickly.
  4. Stop completely; time needed for withdrawal can vary from about 4 weeks to a year or more.
25
Q

What should you do if a patient starts to experience withdrawal symptoms?

A

Keep dose the same until symptoms improve

26
Q

Name 4 antidepressants which can be used in the treatment of anxiety.

A

SSRI’s
Tricyclics.
Venlafaxine.
Moclobemide.

27
Q

What are SSRI’s used first line for?

A

Panic disorder.
OCD.
PTSD.
Phobias.

28
Q

Give 2 examples of tricyclics.

A

Clomipramine.

Imipramine.

29
Q

What anxiety disorders are tricyclics used in the treatment of?

A

2nd line for panic disorder (unlicensed), OCD.

30
Q

What anxiety disorder can venlafaxine be used to treat?

A

GAD

31
Q

What anxiety disorder can moclobemide be used to treat?

A

Social anxiety disorder

32
Q

Outline the 2 modes of action of pregabalin.

A
  1. Ca2+ channel blocker

2. GABA enhancer

33
Q

When is pregabalin considered for the treatment of anxiety?

A

If patient is not responsive to other treatments

34
Q

Give an example of a beta blocker and what they are used in the treatment of.

A

Propanolol

  • Somatic symptoms ie. palpitation, tremor
35
Q

Outline the 4 modes of action of Busiprone.

A
  1. 5-HT1A receptor partial agonist.
  2. Presynaptic dopamine antagonist at the D2, D3 and D4 receptors.
  3. Partial α1 receptor agonist.
  4. Overall suppresses serotonergic activity while noradrenergic and dopaminergic cell firing is enhanced.
36
Q

How long does the effects of Busiprone take to develop?

A

Possibly weeks

37
Q

What is Busiprone sometimes prescribed with? Why?

A

With an SSRI, in order to modify SSRI effects on libido

Psychiatry (31 decks)

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