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MD4001 Week 8 > 2. Sedatives anxiolytics > Flashcards

2. Sedatives anxiolytics Flashcards

1
Q

Why were barbiturates discontinued?

A

Dependence / addiction / misuse narrow therapeutic index

Suicide easily done e.g. marylyn munroe and jimmy henricks

Also used as IV induction agents and anti convulsant

So…
Become obsolete as anxiolytics

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2
Q

Classess of sedatives and anxiolytics?

A 
• Antidepressants
• Benzodiazepines (1960s)
• Z-drugs (1990)
• B-blockers
• Other
– Melatonin
– Sedating antihistamine
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3
Q

Properties/formulation of benzodiazepine?

A

Serendipity? (librium)
Highly lipophilic: so easily absorbed
Well absorbed orally
Highly protein bound (95%) Hepatic metabolism
Active metabolites, so can last for hours
Excreted as glucoronide conjugate.

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4
Q

5 major effects of benzodiazepines?

A
  1. Anxiolytic: reduce anxiety (α2 & α3 )
  2. Hypnotic: induce sleep (α1)
  3. Reduce muscle t§one
  4. Anterograde amnesia (pros&cons)
  5. Anticonvulsant effect
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5
Q

Administration of benzodiazepines?

A

• Normally given orally or intravenously – (can be given by intranasal or rectal route)
Not advised to be given intramuscular route

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6
Q

Categorisation of benzodiazepines?

A

SHORT ACTING
Lorazepam, temazepam t1/2 8-12 hours intermediate

LONG ACTING
Diazepam t1/2 20-100

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7
Q

Structure of GABAa receptor?

A
  • Pentameric arrangement
  • Central ion channel pore
  • 18 possible subunits
  • Approx 30 forms of receptor
  • Some subunits location specific
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8
Q

Role of GABAa receptor?

A
  • Anaesthetics and benzos allosterically activate the receptor
  • Increase the frequency of opening

Act allosterically on GABAa receptors
Sedation mediated via GABAa with α1 subunit
– Anxiolysis mediated via GABAA with α2 & α3 subunits

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9
Q 
Flumazenil:
Class?
Half life?
Precipitates?
Administration?
SE?
A 
Class: Competitive benzo antagonist
Half life: Short
Precipitates: Agitation and seizures
Administration: IV in 100mcg increments
SE: N/V
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10
Q

Z drugs:
Act where?
Eg?

A

Act via benzodiazepine receptors
– Zopiclone
– Zaleplon
– Zolpidem

No benefit over z drugs and short acting benzo

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11
Q

What is tolerance

A

Is a physiological state characterized by a decrease in the effects of a drug with chronic administration.

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12
Q

Tolerance of benzo?

A

Tolerance develops quickly for sedative effects

more slowly for anxiolytic & anticonvulsant effects.

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13
Q

Mechanism for tolerance?

A
  • Neuro-adaptive process
  • Desensitisation of inhibitory GABA receptors • Sensitisation of (excitatory) NMDA receptors • Adaptions take place on different time scale
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14
Q

What is dependance?

A
  • The drug induces a rewarding experience
  • Drug taking becomes compulsive

Genetic component*

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15
Q

Two forms of dependence?

A

Psychological and physical

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16
Q

Withdrawl is a result of…

A

dependence

17
Q

Symptoms of withdrawal?

A

• Increased anxiety, onset / exacerbation of
depression
• Disturbed sleep
• Pain, stiffness , muscular aches
• Convulsions
• Can occur after relatively short courses of treatment (4 weeks)

18
Q

Clinical role of sedative and anxiolytic agents?

A 
Enable potentially uncomfortable diagnostic and therapeutic procedures to be carried out
Management of acute alcohol withdrawn
Management of insomnia
Management of generalised anxiety states
Other: Anticonvulsants
19
Q

How to manage acute alcohol withdrawl?

A

• Acute admissions to hospital
• Supply of alcohol interrupted
• Index of suspicion…
– Alcohol history
– Severity of alcohol dependence questionnaire
– Assessment of withdrawal symptoms
Chlordiazepoxide 1-2 week reducing regime

20
Q

What are the 4 questions of the CAGE questionnaire when approaching potential alcohol withdrawal cases?

A

C• Have you ever felt you should Cut down your drinking?
A• Have you ever been Annoyed by other people criticizing your drinking?
G• Have you ever felt Guilty about drinking?
E• Have you ever taken a drink in the morning to steady your nerves or ease a hangover (Eye- opener)?

21
Q

Alcohol withdrawal symptoms?

A

**May start 8 hours after drop in alcohol levels (peak day 2) **
Insomnia / anxiety/ restlessness/ agitation
Tremor
Nausea & vomiting
Sweating
Palpitations
Hallucinations auditory / visual/tactile
Seizures

22
Q

Investigation results that suggest chronic alcohol consumption?

A 
• Raised MCV
• Pancytopenia (result of alcohol induced bone
marrow suppression
• Folate deficiency
• Prolonged prothrombin time
23
Q

How to treat alcohol withdrawl?

A

Chlordiazepoxide dosing regimes in alcohol withdrawal

24
Q

How to manage insomnia?

A

Try not to lol

Assess the source FIRST
Hypnotics reserved for the acutely distressed

Avoid benzo administration for insomnia in elderly bc

  1. Confusion
  2. Falls
  3. Slower metabolism
25
Q

What is sleep hygiene?

A

Sleep hygiene aims to make people more aware of behavioural, environmental & temporal factors that may be detrimental or beneficial to sleep

26
Q

How to encourage good sleep hygiene?

A

Get into routine
Exercise in morning, not within 4 hrs of sleep
Bedroom = cool, dark, quiet
No caffiene, alcohol or smoke within 6 hrs
Screen time not 30 mins before bed
No day naps

27
Q

Drug treatment for insomnia?

A

TO BE AVOIDED
Short acting benzo or z-drug
Lowest dose for shortest period
no repeat prescriptions. Explain? Tolerance makes it ineffective

28
Q

Considerations when managing prolonged seizures?

A

DO IT, need to protect patient from injury

Provide 02 is available
Consider/exclude hypoglycaemia

Lorazapam: For seizures 5 mins ++
Route: IV access. If not possibile, then rector diazepam or intranasal/buccal midazolam

29
Q 
Minimal sedation (anxiolysis) definition?
Responsiveness
Airway
Spontaneous ventilation
CV function
A

Responsiveness: Normal response to verbal stimulation
Airway: Unaffected
Spontaneous ventilation: Unaffected
CV function: Unaffected

30
Q 
Moderate sedation/analgesia (conscious sedation) definition?
Responsiveness
Airway
Spontaneous ventilation
CV function
A

Responsiveness: Purposeful* response to verbal or tactile stimulation
Airway: No intervention required
Spontaneous ventilation: Adequate
CV function: Usually maintained

31
Q 
Deep sedation/analgesia?
Responsiveness
Airway
Spontaneous ventilation
CV function
A

Responsiveness: Purposeful response after repeated or painful stimulation
Airway: Intervention may be required
Spontaneous ventilation: May be inadequate
CV function: Usually maintained

32
Q 
General analgesia?
Responsiveness
Airway
Spontaneous ventilation
CV function
A

Responsiveness: Unarousable, even w/painful stimulus
Airway: Intervention often required
Spontaneous ventilation: Frequently inadequate
CV function: May be impaired

33
Q

Acute anxiety management?

A

Anxiety is a normal. It becomes a problem if it starts to interfere with your everyday life.
No “quick fix”

Guided self help:
• reduce caffeine, reduce alcohol
• Mantras, mindfulness, worrytime
Cognitive behaviour therapy

34
Q

Use of benzo in acute anxiety management?

A

Just don’t!
“Benzodiazepines are indicated for the short-term relief (two to four weeks only) of anxiety that is severe, disabling, or causing the patient unacceptable distress, occurring alone or in association with insomnia or short-term psychosomatic, organic, or psychotic illness.”

35
Q

Use of b-blockers in acute anxiety treatment?

A

Helps with tachycardia, palpitations, tremor and sweating

Blocks sympathetic system

Usually: Propranolol
Advantages: non-sedative, no dependence or abuse

36
Q

SSRI withdrawal profile?

A

– Nausea / diarrhoea
– Insomnia
– Sexual dysfunction
– Suicidal behaviour (is it toxic in OD)

37
Q

Use of gabapentin and pregabalin?

A

Management of chronic pain

38
Q

Melatonin:
What is it?
Fluctuation of level?
Use?

A

What is it?
Naturally occurring hormone
Synthesized in pineal gland
Secreted in response to input from retina.

Level change:
High levels at night, low during day

Use:
Clinically often used in children with sleep disturbance.

39
Q

Law on driving (March 2015)

A
  • This law states that it is an offence to drive with certain drugs above specified levels in the body, whether your driving is impaired or not
  • If you are taking these medicines as directed and your driving is not impaired, then you are not breaking the law
  • Benzos, opioids, amphetamines

MD4001 Week 8 (7 decks)

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