Sedatives anxiolytics Flashcards
What are Anxiolytics ?
Used to prevent or treat anxiety symptoms or disorders. They’re sometimes called anti-anxiety medications or minor tranquilizers.
Used for minimal Sedation
When can Anxiolytics be used?
- Therapeutic procedures like endoscopy
- Managing prolonged epileptic seizures
- End of life or Anticipatory care plan
- Alcohol withdrawal
What are the features of Anxiolytics managing prolonged epileptic seizures?
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
What might we use in our end of life or anticipatory care plan?
- 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
What is the drug of choice for alcohol withdrawal ?
Chloradiazoboxide
What is anxiety ?
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
What are some anxiety symptoms?
- Apprehension
- Cued panic attacks
- Spontaneous panic attacks
- Irritability
- Poor sleeping
- Avoidance
- Poor concentration
What are the classifications of anxiety disorders ?
Classifications of anxiety disorders;
- Generalised Anxiety Disorder (GAD0
- Panic Disorder
- Other anxiety disorders
What is Generalised Anxiety Disorder (GAD)?
Generalised Anxiety Disorder (GAD);
- Over arousal
- Irritability
- Poor concentration
- Poor sleeping
- Worry over several areas most time
What is Panic Disorder?
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
What are Other Anxiety Disorders ?
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)
What are some Non-pharmacological treatments?
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
What are some Pharmacological treatments we can give for anxiety ?
1). Antidepressants
2). Benzodiazepines
3). Antiepileptics
4). 5-hydroxytryptamine (5-HT)1A - receptor agonists
5). Atypical antipsychotics
6). B-adrenoreceptor antagonists
What are the features of Antidepressants ?
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
What are Barbiturates ?
Historically ‘fashionable’ as anxiolytics (Celebs took them like Marilyn Monroe and Jimmy Hendrix)
Issues are;
- Addiction / misurse
- Fatal overdoses
Now obsolete as anxiolytics
What are the features of Benzodiazepines ?
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
Why are Benzodiazepines only prescribed for Acute Anxiety and not chronic and can they be used for mild anxiety ?
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
What are Benzodiazepines Pharmacokinetics (What do they do to the body) ?
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
How do Benzodiazepines act on receptors?
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
What is an issue with Nitrazepam?
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 !
What are the features of Anti-epileptics ?
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)
What are the features of 5-HT receptor agonist?
- Buspirone
- Effective in Generalised Anxiety Disorder
- Ineffective in the treatment of phobias or severe anxiety states
(Rarely used, only specialist)
What are the features of Atypical antipsychotics ?
- Risperidone
- Olanzapine
- Quetiapine
- Effectice in Generalised Anxiety Disorder and post-traumatic stress disorder
(Specialist use)
What are the features of B-adrenoceptor antagonists ?
- 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