Sedatives anxiolytics Flashcards

1
Q

What are Anxiolytics ?

A

Used to prevent or treat anxiety symptoms or disorders. They’re sometimes called anti-anxiety medications or minor tranquilizers.

Used for minimal Sedation

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2
Q

When can Anxiolytics be used?

A
  • Therapeutic procedures like endoscopy
  • Managing prolonged epileptic seizures
  • End of life or Anticipatory care plan
  • Alcohol withdrawal
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3
Q

What are the features of Anxiolytics managing prolonged epileptic seizures?

A

Anxiolytics managing prolonged epileptic seizures;
- Is seizure lasts longer than 5 minutes = Intravenous Lorazepam
- Intravenous access not available consider rectal diazepam or intranasal / buccal midazolam

Relax and sedate as well as anticonvulsive effect

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4
Q

What might we use in our end of life or anticipatory care plan?

A
  • Benzodiazepines often used in last days or weeks of life (offer as just in case meds)
  • Management of anxiety
  • Agitated delirium
  • Massive terminal haemorrhage
  • Breathlessness or respiratory distress (alongside opioid)
  • Midazolam IV is usually drug of choice
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5
Q

What is the drug of choice for alcohol withdrawal ?

A

Chloradiazoboxide

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6
Q

What is anxiety ?

A

A normal fear response to threatening stimuli;
- Defence behavioural, autonomic reflexes, arousal and alertness, corticosteroid secretion and negative emotions

Anxiety ‘states’ - 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 activities

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7
Q

What are some anxiety symptoms?

A
  • Apprehension
  • Cued panic attacks
  • Spontaneous panic attacks
  • Irritability
  • Poor sleeping
  • Avoidance
  • Poor concentration
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8
Q

What are the classifications of anxiety disorders ?

A

Classifications of anxiety disorders;
- Generalised Anxiety Disorder (GAD0
- Panic Disorder
- Other anxiety disorders

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9
Q

What is Generalised Anxiety Disorder (GAD)?

A

Generalised Anxiety Disorder (GAD);
- Over arousal
- Irritability
- Poor concentration
- Poor sleeping
- Worry over several areas most time

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10
Q

What is Panic Disorder?

A

Panic Disorder;
- Intermittent episodes of panic or anxiety and taking / avoiding action to prevent these feelings.
- Panic disorder may be with or without agoraphobia (fear of going into crowded places / leaving home).
- Marked somatic symptoms such as sweating, tachycardia, chest pains, trembling and choking

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11
Q

What are Other Anxiety Disorders ?

A

Other Anxiety Disorders;
- Phobias (episodes of anxiety triggered by external stimuli)
- Obsessive Compulsive Disorders (distressing, intrusive thought 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 some Non-pharmacological treatments?

A

1st line: Reassurance and lifestyle advice;
- Anxiety is normal
- No “quick fix”

2nd line: Guided self help;
- Mantras, mindfulness, worry time
- Refer to mood cafe

3rd line: Psychological therapy;
- Cognitive behaviour therapy

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13
Q

What are some Pharmacological treatments we can give for anxiety ?

A

1). Antidepressants
2). Benzodiazepines
3). Antiepileptics
4). 5-hydroxytryptamine (5-HT)1A - receptor agonists
5). Atypical antipsychotics
6). B-adrenoreceptor antagonists

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14
Q

What are the features of Antidepressants ?

A

Antidepressants;
- Selective serotonin (5-HT) reuptake inhibitors (SSRIs); e.g Escitalopram, Sertraline and Paroxetine)
- Serotonin / noradrenaline reuptake inhibitors (SNRIs; e.g Venlafaxine and Duloxetine)
- Older antidepressants - tricyclic anti depressants e.g amitriptyline and monoamine oxidase inhibitors (MAOIs) are also effective

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15
Q

What are Barbiturates ?

A

Historically ‘fashionable’ as anxiolytics (Celebs took them like Marilyn Monroe and Jimmy Hendrix)

Issues are;
- Addiction / misurse
- Fatal overdoses

Now obsolete as anxiolytics

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16
Q

What are the features of Benzodiazepines ?

A

Benzodiazepines;
- Diazepam, lorazepam, temazepam
- Chloradiazepoxide / Librium (Alcohol withdrawl)
- Effective anxiolytic drugs
- Unwanted side effects e.g Amnesia (can be useful for patient, e.g endoscopy patient)
- Induce tolerance
- Dependence - both physical and psychological
- Drugs of abuse
- Act within 30 minutes - useful for patients who need acute treatments and can be taken on an ‘as needed’ basis

17
Q

Why are Benzodiazepines only prescribed for Acute Anxiety and not chronic and can they be used for mild 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

18
Q

What are Benzodiazepines Pharmacokinetics (What do they do to the body) ?

A

Benzodiazepines Pharmacokinetics;
- Well absorbed orally: peak effects 30 mins - 2 hours
- Highly lipophilic: absorbed fast and enter CNS quickly
- Highly protein bound: big reservoir tend to be long acting
- Duration of action: redistribution
- Many have active metabolites
- Renal excretion in urine

Have 5 major effects;
- Anxiolytic - reduce anxiety (a2 & a3)
- Hypnotic - induce sleep (a1)
- Reduce muscle tone
- Anterograde amnesia (pros and cons)
- Anti-convulsive effect

Large number of benzodiazepine - all similar actions, main difference duration of action

Act on GABA Receptors

19
Q

How do Benzodiazepines act on receptors?

A

They allosterically bind on GABA receptors

Mediate and promote, increase GABA binding resulting in increase chlorine moving across gap

Sedation mediated via GABA with a1 subunit
- Anxiolysis mediated via GABA with a2 and a3 subunits

20
Q

What is an issue with Nitrazepam?

A

It has a long half life of 18 - 25 hours so if taken too late in day can give hangover effect so may be more detrimental than helpful !

21
Q

What are the features of Anti-epileptics ?

A

Anti-epileptics;
- Pregabalin (better one) and Gabapentin
- Treat general anxiety disorder, although trial data on gabapentin are limited
- Other anti epileptic drugs such as Tiagabine, Valproate and Levetiracetam, may also be effective in treating generalised anxiety disorder (Side effect profile can limit good can get from it)

22
Q

What are the features of 5-HT receptor agonist?

A
  • Buspirone
  • Effective in Generalised Anxiety Disorder
  • Ineffective in the treatment of phobias or severe anxiety states
    (Rarely used, only specialist)
23
Q

What are the features of Atypical antipsychotics ?

A
  • Risperidone
  • Olanzapine
  • Quetiapine
  • Effectice in Generalised Anxiety Disorder and post-traumatic stress disorder
    (Specialist use)
24
Q

What are the features of B-adrenoceptor antagonists ?

A
  • Propanaolol (\0)
  • 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
25
Q

What is Tolerance and what drugs do we see this in?

A

Tolerance is a Physiological reaction (neuroadaption) characterised by a decrease in the effects of a drug with chronic administration requiring dose to attain same effect
- (Have to use more of drug for same effect)

Benzodiazepines;
- Tolerance develops quickly for sedative effects
- More slowly for anxiolytic & anticonvulsant effects
- Neuroadaptive due to desensitisation of inhibitory GABA receptors
- Sensitisation of (excitatory) NMDA receptors

26
Q

What is dependence ?

A

To be considered as dependent a patient must of 3 of the 6 criteria in the last 12 months;

2 drug-related criteria;
- Compulsion / cravings to take benzodiazepines
- Difficulties in controlling benzodiazepine use

2 consequence of use criteria;
- Progressive neglect of alternative pleasures / interests due to benzodiazepine use
- Persistent use despite harmful consequences

2 physiological criteria;
- Characteristic benzodiazepine withdrawal state
- Evidence of tolerance to benzodiazepines

More features;
- This drug induces a rewarding experience
- Drug taking becomes compulsive
- Psychological dependence
- Physical dependence
- Genetic factors

27
Q

What are the features of Withdrawl ?

A

Withdrawl;
- A result of physical dependence
- Increased anxiety, onset / exacerbation of depression
- Disturbed sleep
- Pain, stiffness, muscular aches
- Convulsions
- Can occur after relatively short courses of treatments (4 weeks)

28
Q

What are the signs of drug abuse?

A

Abuse;
- Common drugs of misuse / abuse
- Usually part of polydrug misuse
- Enhances “highs”
- Attenuates “crashes”
- In part iatrogenically (cause of disease) driven

29
Q

How should you manage Insomnia ?

A

Insomnia makes a significant impact on a persons daytime functioning

Insomnia Management;
- Difficulty getting off to sleep or waking up ?
- Assessment ? Pain / breathlessness
- Good sleep hygiene
- Hypnotics revered for the acutely distressed

Caution in elderly;
- Confusion
- Falls
- Slower metabolism

If you must prescribe;
- Short acting benzo or z-drug
- Lowest effective dose for shortest time
- Inform patient no repeat prescriptions & explain why (Effect will reduce over time, must have a plan to stop)

30
Q

What is sleep hygiene and how can we improve it ?

A

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

Ways to improve;
- Establish a regular pattern of going to bed & getting up
- Get regular exercise preferably in the morning but not within 4 hours of going to bed
- Keep your bedroom cool, dark & quiet
- Don’t have caffeine, alcohol or smoke within 6 hours of bedtime
- Avoid screen time for at least 30 mins before bed
- Avoid naps during the day

31
Q

What are Z drugs?

A

Zopiclone, Zolpidem and Zaleplon
- Act via benzodiazepine receptors
- Structurally different
- Very similar pharmacodynamic profile
- Consider in elderly shorter half life means less hangover
- Consider if risk of misuse
- Falls risk

32
Q

What is the Therapeutic role of Melatonin ?

A

Melatonin;
- Naturally occurring hormones
- Synthesised in pineal gland
- High levels at night, low during day
- Licensed for insomnia > 55 years not SMC approved, lack if evidence ?
- Specialists use in children with sleep disturbance

33
Q

What is the law on driving (October 2019) in relation to prescriptions ?

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

If above the specified limit, not commit the new offence if your driving is not impaired and you are taking your medicine in accordance with the advice of a healthcare professional

Benzodiazepines, opioids and amphetamines