IDT - Anxiolytics & Sedatives, Ishmael Flashcards
What do Anxiolytics do?
Reduce Anxiety
What do sedatives do?
Induce “sedation”, decrease activity, have a calming effect/reduce anxiety
What do Hypnotics do?
Induce drowsiness, cognitive performance decrease, and allow onset or allow maintenance of sleep
What is Fear?
reaction to immediate perceived threat/critical to survival
What is Conditioned fear?
Reaction to a stimulus that is associated with a threat
What is anxiety?
A normal human emotion, anticipatory response to an uncertain, potential threat
How do anxiety disorders occur?
Symptoms of anxiety interfere with normal life; no longer useful as a warning system; no focus to the fear or dread, where the scale of symptoms is not appropriate for the threat.
What region of brain is responsible for the expression of fight or flight motor response?
Striatum
Which region of the brain is responsible for the body’s autonomic response?
Brainstem
Which region of the brain produces hormonal stress response?
Hypothalamus
Which brain regions encompass the Limbic System?
Cortex, Hippocampus, Amygdala and Striatum
What is the role of GABA on arousal or sleep?
GABA deceases arousal in order to promote sleep (Inhibitory)
What Neurochemicals play a role in the regulation of sleep-wake cycles
Glutamate NE ACh 5-HT DA GABA Orexin/Hypocretin Histamine
What is circadian rhythm?
24hr cycle of physical, mental and behavioral changes
What Biological clocks control circadian rhythms?
Pineal gland - releases melatonin
Suprachiasmatic Nucleus (SCN) - master clock
Retina - light
What are the subjective features of anxiety disorders
WHARDFIA
Apprehension Worry Anticipation Fear Hypervigilance Restlessness Impaired Concentration Depression
What physiological features accompany anxiety disorders?
NGRC
Neuromuscular (tension, fatigue)
Gastrointestinal (Dry mouth, swallowing issues)
Respiratory (Hyperventilation)
Cardiovascular (palpitations)
Type of anxiety where there is excessive anxiety and worry most of the time about life?
Generalized anxiety disorder
GAD
Type of anxiety where an irrational fear interferes with normal behavior?
Phobic Anxiety Disorders
Type of anxiety where there are discrete periods of intense fear?
Panic Disorder
Type of anxiety where it mostly occurs in situational or specific circumstances?
Social Anxiety Disorder
SAD
Persistent thoughts, ideas or images that intrude into conscious awarenss
Obsession
Urges or impulses for repetitive intentional behaviors
Compulsions
Type of anxiety which recurs and is precipated by exposure to an exceptionally stressful/horrific or life threatening event.
Post-traumatic stress disorder
PTSD
Anxiety where there is a reaction to a recent identifiable stress; lasts less than six months
Acute stress disorder
Disorder where depression and anxiety occur together at the same time in the same patient (SSRIs, SNRIs)
Comorbid Depression and Anxiety
Drug where the anxiolytic effect is likely in the limbic system where high density of GABAa receptors control emotional behavior
Benzodiazepines (BZD)
Advantages of BZDs Anxiolytics
Rapid Onset of action
High therapeutic index
Highly effective in acute forms
Disadvantages of BZDs
Tolerance or Habituaton/dependence
CNS depressants/Sedative
Impair cognition/memory
additive danger w/ alcohol
Short Acting Anxiolytics
Chlorazepate
Oxazepam
Intermediate Acting Anxiolytics
Alpralozam
Lorazepam
Oxazepam
Long acting Anxiolytics
Chlordiazepoxide
Diazepam
Clonazepam
Effect of BZDs on GABA receptors
Enhance the affinity, increasing frequency of channel opening.
What other drug classes can be used as Anxiolytic drugs?
SSRIs
SNRIs
5HT1A agonist
Beta-Blockers
What is the disadvantage of SSRIs and SNRIs as anxiolytic drugs?
slow onset of action 2-6wks
What are some disadvantages of 5-HT1A agonist as axiolytic drugs?
unsuitable for acute anxiety, slow onset of action
What Beta-Blocker anxiolytic is used and how is it different than other anxiolytic medications?
Propanolol
Only treats physiological smptoms
Mechanism of action for Buspirone
5-HT1A agonist (presynaptic receptors)
attenuates serotonergic transmission
What are the primary indications of Sedative-Hypnotic drugs?
Anxiolytic Insomnia Sedation/Amnesia Anesthesia Epilepsy Muscle Relaxants Withdrawal
Which BZDs used for insomnia
QFETT
Triazolam Estazolam Temazepam Flurazepam Quazepam
What is the effect of Barbiturates on the GABA receptor?
Increase efficacy of GABA by increasing duration of opening
Ultrashort acting Barbiturates for induction of anesthesia
Methohexital
Thiopental
Short acting barbiturates for insomnia/preoperative sedation
Amobarbital
Pentobarbital
Secobarbital
Long acting barbituates for treatment of seizures
Phenobarbital
Which drug classes bind to GABAa receptors?
BZD BRB Mep ChH Z-drugs
What is the GABAa subunit composition?
2 alpha, 2 gamma, 1 beta
What is the GABAb subunit composition?
2 alpha, 2 beta, 1 gamma
What drug can be used to reverse overdose of BDZ drugs?
Flumazenil (BDZ antagonist)
no clinical effect alone
What GABAa receptor subtypes do common BDZs bind to?
alpha 1, 2, 3, 5
not 4 or 6
What GABAa subunit are Z-drugs specific for?
Alpha-1 subunit
What is defined as a state with repeated difficulty in sleep initiation, duration, consolidation and circumstances for sleep?
Insomnia
What is the most common complaint of insomnia?
Insomnia resulting in daytime impairment
What is the longest stage of sleep?
Non-REM sleep (75-80%)
How long does REM sleep generally last?
20-30min
BDZ effect on Sleep stages
Decreases sleep latency, by decreasing light sleep/dozing, and increasing time of awareness disappearance, increasing TOTAL sleep time but decreasing REM and deep sleep time.
Stages of Sleep
1 - light sleep 2 - awareness disappears 3 - slow wave sleep 4 - slowest wave sleep REM - Memorable dreaming (Cycle lasts 90-110min)
Sleeping pills/alcohol effect on sleep
perception = deep refreshing sleep
Sleep not physiologically normal
Where is the binding site for BDZ drug on GABA receptor?
between alpha and gamma subunits
An alpha2 adrenergic agonist used for sedation and analgesia in intensive care patients and some procedures
Dexmedetomidine
8 times more potent than Clonidine
Preferred over BDZ and propofol
What are the warnings/precautions of Z-drugs (Ambien)
May cause complex behaviors such as sleep-driving, or other sleep-activities
Restless Legs Syndrome effect and treatment
Impacts sleep, must be treated with newer dopamine agonists
OTC Sleep Aids action
contain antihistamine, target H1 receptor to cause sleepiness
Disadvantages of Diphenhydramine
Long half-life = daytime grogginess
Orexin receptor agonist effect on sleep
Belsomra
Bind OX1R and OX2R (GPCRs)
Improve sleep initiation and maintenance by lengthening deep sleep and REM
