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PR3136 > ANXIOLYTIC > Flashcards

ANXIOLYTIC Flashcards

1
Q

Psychological component of anxiety state

A

Insomnia
Arousal
Lack of concentration
Negative emotions (worry, nervousness, unease)

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2
Q

Physical component of anxiety state

A 
Tachycardia
Shortness of breath
Nausea
Gastric acid hypersecretion
Trembling
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3
Q

Generalised Anxiety Disorder (GAD)

A
  • at least 6 months
  • excessive and uncontrolled worry over everyday matters
  • interferes with daily functioning
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4
Q

Anxiolytic and sedative benzodiazepines

A
  1. Diazepam

2. Lorazepam

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5
Q

Hypnotic benzodiazepines

A
  1. Diazepam
  2. Triazolam
  3. Temazepam
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6
Q

Pre-anaesthetic benzodiazepines

A
  1. Diazepam

2. Midazolam

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7
Q

3 categories of benzodiazepines according to their onset of action

A
  1. Short acting
    - few hours (3-8h)
    - Triazolam (insomnia) & Midazolam (general anaesthesia)
  2. Intermediate acting
    - several hours (10-20h)
    - Temazepam (insomnia) & Lorazepam (insomnia & status epilepticus)
  3. Long acting
    - days
    - Diazepam (epilepsy, status epilepticus & refractory seizures)
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8
Q

MOA of benzodiazepines

A

Benzodiazepines bind to benzodiazepine binding site on GABA receptor.
This enhance and promote the binding of GABA to its binding site which then opens the Cl- channel to allow influx of negatively charged Cl- into the cell, causing neuronal membrane to be hyperpolarised.
Hence, it is harder for the neuron to be depolarised and fired.

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9
Q

Can benzodiazepines work without GABA agonists?

A

No.

Benzodiazepines potentiate GABA action by increasing the frequency of GABA-induced channel opening.

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10
Q

Side effects of benzodiazepines

A
  1. Severe respiratory depression, especially with alcohol use
  2. Confusion, amnesia and drowsiness
  3. Impaired muscle coordination
  4. High risk of dependency development
    - withdrawal effects (disturbed sleep, rebound anxiety, tremors and convulsion)
  5. High risk of tolerance development (req higher dose to exhibit same therapeutic effect)
    - depends on the frequency of use
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11
Q

Treatment for overdosage of benzodiazepines

A

Flumazenil, benzodiazepine-site antagonist

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12
Q

Non-benzodiazepines (6)

A
  1. Zolpidem
  2. Buspirone
  3. Barbiturates
  4. Pregabalin (GABA analogue)
  5. Hydroxyzine
  6. Propranolol
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13
Q

MOA of Zolpidem

A
  • binds to benzodiazepine-binding site to potentiate GABA binding to its receptor
  • primarily used to treat insomnia (NO ANXIOLYTIC EFFECT)
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14
Q

MOA of Buspirone

A
  • partial 5-HT receptor agonist & dopamine receptor angonist
  • for GAD but onset takes 1-2 weeks
  • lack muscle relaxant and anti-convulsant properties
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15
Q

MOA of Barbiturates

A
  • bind to barbital binding site on GABA receptor
  • higher tendency for dependence and tolerance
  • severe withdrawal symptoms
  • at anaesthetic doses, it can directly open Cl- channels and block Na+ channels
  • CANNOT use flumazenil for overdosage treatment
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16
Q

MOA of Pregabalin

A
  • GABA agonist analogue which increase synaptic GABA agonists
  • also act on voltage-gated Ca2+ channels
  • for GAD and anti-convulsant effect
  • risk of suicidal thoughts
17
Q

MOA of Hydroxyzine

A
  • antihistamines with activities on serotonergic and alpha-adrenergic receptors
  • anxiolytic effect due to 5-HT receptors activities
  • low addictive potential compared to benzodiazepines and barbiturates
  • helps with itching
18
Q

MOA of Propranolol

A
  • beta-adrenergic receptor antagonist
  • for performance anxiety and social phobias
  • reduce physical symptoms
  • CI in asthma and heart diseases
19
Q

3 categories of barbiturates according to their onset of action

A
  1. Ultra-short acting
    - mins
    - thiopental (IV anaesthesia)
  2. Short acting (sedative & hypnotic)
    - 3-8h
    - pentobarbital & amobarbital
  3. Long acting
    - days
    - phenobarbital
20
Q

Anti-depressants as anxiolytics (4)

A
  1. NaSSA : Mirtazapine
  2. TCA : Clomipramine
  3. SSRI : Fluoxetine, citalopram, sertraline and paroxetine
  4. SNRI : Venlafaxine and duloxetine

serotonergic agents

21
Q

Buspirone vs Buproprion

A

Buspirone

  • partial 5-HT agonist
  • activities on dopamine receptors

Buproprion
- NDRI

22
Q

ADR of Pregabalin

A

Suicidal tendency

PR3136 (19 decks)

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