30-10-23 - Sedatives anxiolytics Flashcards

1
Q

Learning outcomes

A
  • Define the terms anxiolysis and sedation
  • Outline the pharmacodynamics & pharmacokinetics of benzodiazepines & z-drugs
  • Identify other classes of drugs used in the management of anxiety
  • Define the terms tolerance, dependence & withdrawal
  • Be aware of the clinical indications to prescribe anxiolytics
  • Understand the role of B blockers in managing anxiety
  • Discuss the therapeutic role of melatonin
  • Be able to provide practical sleep hygiene advice
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2
Q

Describe the 4 levels for sedation sleep depth.

Describe their effects on the body (in picture)

A
  • 4 levels for sedation sleep depth

1) Minimal
* Also called anxiolysis
* The patient remains awake but relaxed, able to interact.

2) Moderate
* Also called conscious sedation
* The patient has depressed consciousness but will respond to verbal requests or react to touch.
* Breathing remains intact, and no support is needed.

3) Deep:
* The patient cannot be easily aroused but will respond to repeated or painful stimuli.
* Breathing may be impaired and may need to be supported.

4) Dissociative
* A trance-like state wherein the patient remains awake but unaware of the pain and retains no memory of the event.
* They can follow commands, and airway reflexes remain intact.

  • Sedation depth effects on body (in picture)
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3
Q

What can anxiolysis be used for?

A
  • Anxiolysis can be used for therapeutic procedures where the patient needs to be conscious e.g endoscopy
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4
Q

What medications can be used to treat prolonged epileptic seizures?

What is IV access is not available?

A
  • For prolonged epileptic seizures lasting longer than 5 minutes, we can use intravenous lorazepam
  • If IV access is not available consider rectal diazepam or intranasal / buccal midazolam
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5
Q

What medications are often used in the Anticipatory Care Plan (ACP) for End Of Life (EOL) care?

A
  • In the Anticipatory Care Plan (ACP) for End Of Life (EOL) care, Benzodiazepines often used in the last days or weeks of life
  • Midazolam IV is usually drug of choice in order to manage anxiety
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6
Q

NHS Fife Alcohol Withdrawal guideline

A
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7
Q

What medication used in alcohol withdrawal?

A
  • Chlordiazepoxide is often used to treat alcohol withdrawal
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8
Q

NICE Clinical Guidelines Feb 2010 Chlordiazepoxide dosing regimes in alcohol withdrawal (in picture)

A
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9
Q

What is anxiety a response to?

What 5 factors make up anxiety?

What are anxiety states?

What is the difference between ‘pathological’ and ‘normal’ state of anxiety?

A
  • Anxiety is a normal fear response to threatening stimuli:
  • 5 factors make up anxiety:
    1) Defensive behaviours
    2) Autonomic reflexes
    3) Arousal and alertness
    4) Corticosteroid secretion
    5) Negative emotions.
  • Anxiety states are reactions that occur in an anticipatory manner with no apparent stimuli.
  • Difference between ‘pathological’ and ‘normal’ state of anxiety is not clear-cut.
  • Defined at the point at which the symptoms interfere with normal productive activitie
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10
Q

What are 7 symptoms of anxiety?

A
  • 7 symptoms of anxiety:
    1) Apprehension
    2) Cued Panic Attacks
    3) Spontaneous Panic Attacks
    4) Irritability
    5) Poor sleeping
    6) Avoidance
    7) Poor concentration
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11
Q

What are 3 classifications of anxiety disorders?

A
  • 3 classifications of anxiety disorders:

1) Generalised Anxiety Disorder (GAD)
* Over-arousal, irritability, poor concentration, poor sleeping and worry over several areas most of the time

2) Panic disorder
* Intermittent episodes of panic or anxiety and taking / avoiding action to prevent these feelings.
* Panic disorder may be with or without agoraphobia (a fear of being in situations where escape might be difficult or that help wouldn’t be available if things go wrong.)
* Marked somatic symptoms, such as sweating, tachycardia, chest pains, trembling and choking

3) Other anxiety disorders
* Includes:
* Phobias (episodes of anxiety triggered by external stimuli)
* Obsessive Compulsive Disorders (distressing, intrusive thought ands and related compulsions “rituals”)
* Post Traumatic Stress Disorder (delayed and / or protracted response to a stressful event or situation).

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12
Q

What are 3 non-pharmacological treatments for anxiety?

A
  • 3 non-pharmacological treatments for anxiety?

1) Reassurance and Lifestyle Advice
* Anxiety is normal.
* No “quick fix”.

2) Guided self help
* Mantras, mindfulness, worry time
* www.moodcafe.co.uk

3) Psychological Therapy
* Cognitive behaviour therapy

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13
Q

What are 6 types of Pharmacological treatments for anxiety?

A
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14
Q

What are 3 types of anti-depressants? What are examples of each?

A
  • 3 types of anti-depressants? What are examples of each:

1) Selective serotonin (5-HT) reuptake inhibitors (SSRIs)
* e.g. escitalopram , sertraline and paroxetine )

2) Serotonin/noradrenaline reuptake inhibitors (SNRIs
* e.g. venlafaxine and duloxetine

3) Older antidepressants
* Tricyclic antidepressants e.g. amitriptyline
* Monoamine oxidase inhibitors (MAOIs) are also effective

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15
Q

What are 3 examples of benzodiazepines?

What are they effective for?

How quickly do they act?

Describe the tolerance and dependence of benzodiazepines?

What is a potential adverse effect of benzodiazepines?

A
  • 3 examples of benzodiazepines:
    1) Diazepam
    2) Lorazepam
    3) Temazepam
  • Benzodiazepines are effective anxiolytic drugs
  • Act within 30 minutes, - useful for patients who need acute treatment, and can be taken on an ‘as needed’ basis.
  • Induce tolerance
  • Dependence – both physical and psychological
  • Benzodiazepines can be drugs of abuse and can also have unwanted side effects e.g. amnesia
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16
Q

When can benzodiazepines be used for anxiety?

A
  • The use of benzodiazepines to treat short term ‘mild’ anxiety is inappropriate
  • 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
17
Q

What is one of the fist benzodiazepines?

What was it used for?

A
  • Chlordiazepoxide/Librium is one of the first benzodiazepines
  • It is used in the treatment of alcohol withdrawal
18
Q

Where are benzodiazepines well absorbed?

How long does it take until their peak effects?

What are chemical properties of benzodiazepines?

How are they metabolised?

How are they secreted?

A
  • Benzodiazepines are well absorbed orally
  • Peak effects 30mins – 2 hours
  • Beznodiaepines are Highly lipophilic (absorbed fast and enter CNS quickly) and Highly protein bound (Big reservoir tend to be long acting)
  • Hepatic metabolism (cytochrome p450)
  • Renal excretion in urine
19
Q

Benzodiazepines Pharmacodynamics (what the drug does to the body)

What are 5 major effects of benzodiazepines?

How many benzodiazepines are there?

A
  • Benzodiazepines Pharmacodynamics (what the drug does to the body)
  • 5 major effects of benzodiazepines:
    1) Anxiolytic - reduce anxiety (α2 & α3 )
    2) Hypnotic - induce sleep (α1)
    3) Reduce muscle tone
    4) Anterograde amnesia (pros & cons)
    5) Anticonvulsant effect
  • Large number of benzodiazepine - all similar actions, main difference duration of action.
20
Q

What receptors do benzodiazepines affect?

How is sedation and anxiolysis mediates through GABAA receptors?

A
  • Benzodiazepines act allosterically on GABAA receptors
  • Allosteric binding is the process of an effector binding to an enzyme to modify its activity
  • Sedation mediated via GABAA with α1 subunit
  • Anxiolysis mediated via GABAA with α2 & α3 subun
21
Q

Benzodiazepines half-life, speed of onset, and use (in picture)

A
22
Q

What are 2 examples of antiepileptics?

What are they used to treat?

What other antiepileptics might be used for generalised anxiety disorder.?

A
  • 2 examples of antiepileptics:
    1) Gabapentin
    2) Pregabalin
  • These antiepileptics are used to treat general anxiety disorder, although trial data on gabapentin are limited.
  • Other antiepileptic drugs such as tiagabine, valproate and levetiracetam, may also be effective in treating generalised anxiety disorder
23
Q

What is an example of a 5-HT 1A receptor agonist?

What is it effective and ineffective in treating?

A
  • Buspirone is a 5-HT 1A receptor agonist
  • It is effective in Generalised Anxiety Disorder
  • Ineffective in the treatment of phobias or severe anxiety states.
24
Q

What are 3 examples of atypical antipsychotics?

What are they effective in treating?

A
  • 3 examples of atypical antipsychotics:
    1) Olanzapine
    2) Risperidone
    3) Quetiapine
  • They are effective in Generalised Anxiety Disorder and posttraumatic stress disorder
25
Q

What is an example of β-Adrenoceptor antagonists?

What groups of people is it used by?

What does the effectiveness of the block depend on?

A
  • Propranolol is a β-Adrenoceptor antagonists (beta-blocker)
  • Sometimes used by actors and musicians to reduce the symptoms of stage fright, but their use by snooker players to minimise tremor is banned as unsportsmanlike
  • Effectiveness depends on block of peripheral sympathetic responses rather than on any central effects
26
Q

What is tolerance?

Describe the 4 parts in development of tolerance for benzodiazepines?

A
  • Tolerance is a physiological reaction (neuroadaption) characterised by a decrease in the effects of a drug with chronic administration requiring increasing dose to attain same effect.
  • 4 parts in development of tolerance for benzodiazepines:

1) Tolerance develops quickly for sedative effects

2) More slowly for anxiolytic & anticonvulsant effects

3) Neuroadaptive due to desensitisation of inhibitory GABA receptors

4) Sensitisation of (excitatory) NMDA receptors

27
Q

How does drug dependence develop?

What are the 2 types of dependence?

What can influence dependence?

Describe the criteria for dependence (in picture)

A
  • Drug dependence develops when a drug induces a rewarding experience, leading to drug taking becomes compulsive
  • There is psychological and physical dependence
  • Genetic factors can influence dependence
  • Criteria for dependence (in picture)
28
Q

What is withdrawal a result of?

How quickly can it occur?

What are 5 symptoms/signs of withdrawal?

A
  • Withdrawal is a result of physical dependence
  • It can occur after relatively short courses of treatment (4 weeks)
  • 5 Symptoms/signs of withdrawal:
    1) Increased anxiety
    2) Onset / exacerbation of depression
    3) Disturbed sleep
    4) Pain, stiffness, muscular aches
    5) Convulsions (seizures)
29
Q

What drugs are commonly used in abuse?

How does it alter highs and crashes?

How can it be driven?

A
  • Common drugs of misuse / abuse e.g Rohypnol
  • Usually, part of polydrug misuse
  • Enhances “highs”
  • Attenuates (reduces) “crashes”
  • In part, drug abuse is iatrogenically driven (induced unintentionally by a physician or surgeon or by medical treatment or diagnostic procedures)
30
Q

What is insomnia?

Why is assessment surrounding insomnia important?

What is important in avoiding insomnia?

What group are hypnotics reserved for?

What group should be cautious using hypnotics?

A
  • Insomnia is difficulty getting to sleep or staying asleep for long enough to feel refreshed the next morning
  • Assessment around insomnia is important, as factors such as pain/breathlessness that cause insomnia should be treated instead of using a sleeping tablet
  • Good sleep hygiene is important in avoiding insomnia
  • Hypnotics reserved for the acutely distressed
  • Caution in the elderly for hypnotics:
    1) Confusion
    2) Falls
    3) Slower metabolism
31
Q

What are 3 rules for prescribing in insomnia if we must prescribe?

A
  • 3 rules for prescribing in insomnia if we must prescribe:

1) Short acting benzo or z-drug

2) Lowest effective dose for shortest time

3) Inform patient no repeat prescriptions & explain why
* With benzodiazepines, tolerances develop, and drugs stop working

32
Q

What is the aim of sleep hygiene?

What are 6 parts of good sleep hygiene?

A
  • 6 parts of good sleep hygiene:

1) Establish a regular pattern of going to bed & getting up

2) Get regular exercise preferably in the morning but not within 4 hours of going to bed

3) Keep your bedroom cool, dark & quiet

4) Don’t have caffeine, alcohol or smoke within 6 hours of bedtime

5) Avoid screen time for at least 30mins before bed

6) Avoid naps during the day

33
Q

What are 3 examples of Z drugs?

What is their mechanism of action?

How do they compare to benzodiazepines?

When should we consider Z drugs?

What is their a risk of?

A
  • 3 examples of Z drugs:
    1) Zopiclone
    2) Zolpidem
    3) Zaleplon
  • Z drugs act via benzodiazepine receptors (GABAA receptors)
  • Z drugs are structurally different, but have a very similar pharmacodynamic profile to benzodiazepines
  • Consider in elderly shorter half-life means less hangover
  • Consider if risk of misuse
  • With Z drugs, there is a fall risk
34
Q

What is melatonin?

What is it synthesised by?

When are melatonin levels high and low?

What conditions it is licensed for?

A
  • Melatonin is a naturally occurring hormone
  • It is synthesized in pineal gland
  • There are high levels at night, low during day
  • Serotonin is licensed for insomnia > 55yrs – not SMC (Scottish medical consortium) approved, lack of evidence?
  • Can have specialists use it in children with sleep disturbance.
35
Q

Describe the Law on driving (October 2019).

What 3 types of medications does this law cover?

A
  • Law on driving (October 2019)
  • 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
  • This law covers:
    1) Benzodiazepines
    2) Opioids
    3) Amphetamines