Anxiolytics, Hypnotics & Sedatives Flashcards
What are the major mediators of the symptoms of anxiety disorders?
gamma-aminobutyric acid (GABA), norepinephrine, serotonin, and dopamine.
Why are BDZ’s used for anxiety disorders?
Benzodiazepines (BDZs) have been used extensively for anxiety disorders
due to their anxiolytic, hypnotic, muscle relaxant, anticonvulsant and amnesic
action.
Why are anxiolytics used for sleeping disorders?
Anxiolytics may be clinically used for sleep disorders (e.g. insomnia) due to
their sedative and hypnotic (sleep-inducing) effects.
Anxiety meaning?
Disorders are characterised by a feeling of apprehension,
uncertainty and fear without any apparent stimulus.
Anxiety disorders?
Disorders:
*Generalised Anxiety Disorder (GAD)
*Phobias
*Panic Disorder (PD)
*PTSD
*OCD
Anxiety disorders symptoms?
STOMACH
Sweating/Sleeping disorder
Tremor/Tachycardia
Organic Causes to be ruled out
Motor Tension
Arrthymias
C
Hyperventilation
Anxiety goals for treatment?
-Fear extinction
-Blocking reconsolidating of fear memories
Drugs treatment for anxiety?
- Benzodiazepines
- Barbiturates
*SSRIs
What are GABA-gated channels targets for?
*Benzodiazepines
*Barbiturates
*Alcohol
*Cannabis
These drugs act at different sites to increase opening of the channel
and thus enhance inhibitory synaptic transmission (note: presence
of any of the 4 influences the binding of the others)
Why are benzodiazepines most commonly used?
due to their superiority regarding safety and effectiveness compared to barbiturates
Benzodiazepines MOA?
Bind to a specific regulatory receptor site on the GABAA receptor →
enhance inhibitory effect of GABA →
Allosteric enhancement of Cl conduction→ increase frequency of
channel opening; hyperpolarisation
Results:
anxiolysis, sedation and
hypnosis, muscle relaxation, suppression of convulsions.
Benzodiazepines pharmacological Effects?
STOMACH
Sedation
Tremor
O
M
Anxiolytic/Anaesthetic/Awareness(Hyponsis
Coma/Death
Hypnosis
Classifications of Benzodiazepines?
- Sedative hypnotics
- Anxiolytixs
What are the short acting/sedative drugs?
Usually short acting and ultra-short acting
AT(2)OM
‘A’ stands for alprazolam
T’ stands for triazolam and Temezapam
‘O’ stands for oxazepam
‘M’ stands for midazolam.
What are the anxiolytics drugs?
Usually long and intermediate acting
Long drugs feel calming
Lorazepam
Diazepam
Flunitrazepam
Chlordiazepoxide
Which BDZ’s are safe to use for patients in liver disease?
Outside the liver
Oxazepam
Temazapam
Lorazepam
What are the antidote for BDZ overdose?
Ben Is off with FLU
Flumazenil
Lithium
What are the contraindications of Flumazenil?
Dependence
Mixed doese with CVS
CNS toxic(TCA)
Benzodiazepines drugs for insomnia?
Dreams Terrify
Familys
Temazepam
Flurazepam
Which BDZ drugs is used for anxiety an delirium?
Drugs are Calming
Chlordiazepoxide
Diazepam
Benzodiazepines drugs for sedation?
Keep some on the DL-sedated
Diazepam
Lorazepam
Benzodiazepines side effects?
Sedation
Depression
Hyper excitability in children
What is the main neurotransmitter that innervates the amygdala?
Serotonin
Which accessory organ plays a function in the experience of fear and anxiety?
amygdala
What are the Selective Serotonin Re-uptake Inhibitors(SSRIs)?
FESC (FUSEK FEELINGS)
Fluxoxetine
Escitalopram
Sertraline
Paroxetine
SSRI’s MOA?
prevent the presynaptic reuptake of 5-HT → more 5-HT to
stimulate postsynaptic 5-HT receptors (5-HT1; antidepressant and
anxiolytic effects)
SSRI’s S/E?
BAD SSRI
Body weight increase
Anorexia
Dizziness
Suicidal Thoughts
Serotonin Syndrome
Reproductive-Sexual Dysfunction
Insomnia
SSRI’s drug interactions?
do not use with MAOIs; fluoxetinecan inhibit cytochrome P-450
isoenzymes and thus the metabolism of certain β-blockers including
propranolol and metoprolol → hypotension, bradycardia
SSRI drugs and functions?
Effective for Sadness, panic and compulsions?
Escitalopram
Fluxoxetine
Sertraline
Paroxetine
Serotonin Syndrome components side effects?
HARM
Hyperthermia
Autonomic Instability(Delirium)
Rigidity
Myoclonus
Which drugs cause Serotonin Overdose ?
MAO-1
Lithium
Methampetamine
TCA’s
Other hypnotic agents MAO?
-None Benzodiazepine but selectively bind to BDZ-1 receptors .
Other hypnotic drugs?
Z3-The Z drugs
Zopiclone
Zolpidem
Zalepron
Other hypnotic drugs half-life duration?
Shorter half-life than BDZ-1
What are the benefits of this short life of BDZ?
Have reduced propensity to cause tolerance and have less abuse liability
Which other hypnotic dug has the shortest half-life and what is the benefit of that?
Zalepron
Zalepronhas such a short half-life that it can be used to treat
midle-of-the-night insomnia as long as 5hrs elapses before
driving or operating machinery
What other hypnotic drugs are used for antihistamines?
Antihistamines:
Diphenhydramine, Hydroxyzine
What other hypnotic drugs are used for antidepressants ?
Doxapen
