PHARM - Anxiolytic and Hypnotic Drugs - Week 10 Flashcards
What other condition do anxiety disorders often coexist with?
Depression
What four aspects of life are anxiety disorders often associated with?
High degree of social and work impairment
Poor quality of life
Frequent relapses
Briefly describe panic disorder.
Sudden episodes of overwhelming fear with somatic symptoms
Briefly describe obsessive-compulsive disorder.
Compulsive and ritualistic behaviours as well as purposeless activities driven by irrational fears and thoughts
Briefly describe post-traumatic stress disorder.
Anxiety triggered by recall of past traumatic and stressful experiences
Briefly describe phobias.
Intense fear of objects or situations
Briefly describe generalised anxiety disorder.
A feeling of nervousness, tension, or worry not associated with a specific event, situation, or object
Briefly describe social anxiety disorder.
Fear of being with and interacting with people
Anxiety is associated with a dysregulation of what four neurotransmitter systems?
GABA
Serotonin
Noradrenaline
Dopamine
What do the most effective therapeutic agents for anxiety do (2)?
Potentiate GABA and serotonin neurotransmission
Is GABA inhibitory or excitatory?
Inhibitory
Is glutamate inhibitory or excitatory?
Excitatory
Is serotonin widely used in the CNS or only very specific parts?
Widely used
What do anxiolytics do (3)?
Relieve anxiety and tension without notably impairing consciousness
What do hypnotics do?
Produce drowsiness, encouraging the onset of a state of sleep
Is insomnia a disease entity?
No
How are insomnia and anxiety related?
Insomnia is a common clinical manifestation of anxiety
Name three non-pharmacological interventions for insomnia.
Diet
Exercise
Routine change
What two things may be responsible for insomnia?
Disease and environmental factors
What kind of drugs are benzodiazepines and what is its mechanism of action? In what way does it bind to receptors?
They are anxiolytics.
They potentiate the effects of GABA on GABAa receptors by binding allosterically.
How are benzodiazepines classified?
By the duration of their half-life.
Do benzodiazepines have predictable or unpredictable side effects?
Common and predictable
Name 5 side effects of benzodiazepines.
Confusion
Drowsiness/impaired coordination
Long-lasting hangover effects
Tolerance and dependence
Supression of REM sleep
Do benzodiazepines have a wide or narrow therapeutic margin? What does this indicate about its safety?
Wide window - good safety margin
When can benzodiazepines be lethal?
If taken in excess with alcohol or other CNS depressants like opioids and anticonvulsants
Do benzodiazepines have good absoprtion orally? What is this determined by?
Good absorption after oral administration.
Determined by lipophilicity.
What happens to benzodiazepines in the body metabolically for its clearance to occur? What system is critical for this to occur and what function should be checked as a result when administering benzodiazepines?
Transformation or biotransformation to hydrophilic metabolites.
The microsomal liver system is critical for this.
Liver function should be checked.
Many benzodiazepines have active metabolites. Are agents with or without them preferred for older patients?
Agents without active metabolites are preferred for older patients.
Are drug interactions common or rare with benzodiazepines? Give one example.
They are common
Mood stabilisers - reduce the elimination of benzodiazepines
What should benzodiazepines never be taken with and why? What can occur as a result?
Do not mix with alcohol.
It causes additive CNS depression, possibly leading to death.
Are benzodiazepines addictive? Compare it to heroin.
It is addictive - more difficult to stop than heroin.
What do benzodiazepines increase the risk of in older patients and why?
Risk of falling due to possible drowsiness.
Describe what the dosage should be like with benzodiazepines (2).
Start low and increase the dose gradually.
Decrease the dose if drowsiness and confusion occur.
Can benzodiazepines cross the placenta?
Yes, it accumulates in foetal circulation
Can benzodiazepines cross into breast milk?
Yesd
Are benzodiazepines teratogenic (2)?
Yes, cleft palate occurs
How long does it take to gain tolerance/dependence to benzodiazepines?
A couple of weeks.
What happens if sudden discontinuation of benzodiazepines occur?
Withdrawal symptoms
List 7 typical withdrawal symptoms of benzodiazepines.
Anxiety
Restlessness
Shakes
Rebound insomnia (worse than pre-treatment)
Weakness
Orthostatic hypotension
Generalised seizures
What is the recommendation to prevent benzodiazepine withdrawal symptoms?
Gradual dose reduction over 2 months.
Name a non-benzodiazepine anxiolytic and briefly describe what it does. Compare it to benzodiazepines (3).
Buspirone
Relieves anxiety without causing marked sedative/hypnotic effects
Lacks muscle relaxant and anticonvulsant properties
Briefly describe how buspirone works (2) and whether it acts on GABAa directly.
No direct effects on GABAa
Is a partial agonist of 5HT1a and some affinity for D2 receptors.
Does busiprone have abuse liability? Is there a risk of rebound anxiety or withdrawal symptoms?
Has minimal abuse liability
No rebound anxiety or withdrawal symptoms
How long does buspirone take to have an effect? Is it useful for acute anxiety states?
May take 3-4 weeks to take effect.
Not useful for acute anxiety states.
Does buspirone affect driving?
No
List 4 adverse effects of buspirone.
Less psychomotor impairment than benzodiazepines
Dizziness
Headache
GI disturbances
Does buspirone have rapid oral absorption?
Yes
Should liver function be checked when administering buspirone?
Yes
Can benzodiazepines act as a hypnotic?
Yes
How do benzodiazepines act as hypnotics?
They enhance GABA transmission.
Name three side effects of using benzodiazepines as hypnotics.
Broken sleep
Supression of REM sleep
Rebound insomnia (abrupt cessation)
Name 2 benzodiazepine-related drugs that can be used as hypnotics and describe briefly how they work.
Do they cause REM sleep suppression?
Zopiclone
Zolpidem
Increases GABA transmission by selectively binding to BZ1
Dont cause REM sleep suppression
Do antidepressants carry a risk of dependence like benzodiazepines?
No
