Anxiolytic and hypnotic drugs Flashcards
chloradiazepoxide lorazepam midaxolam temazepam are all examples of
Benzodiazepines
Benzodiazepines have a …..effect?
Anxiolytic and hypnotic
Barbiturates have a …..effect?
Anxiolytic and hypnotic
Busipirone is a…
5-HT1a agonist
propranolol is a
B antagonist
escitalopram is a
SSRI
What is the benefit of using B antagonists for anxiety?
They reduce the physical symptoms and reduce feedback loop for continued anxiety
- no impact on psychological experience
How does lorazepam impact sleep?
A benzo
- reduced the time taken to fall asleep and increases duration
- less REM sleep
Side effect of benzos?
Tolerance develops
stop Benzol -rebound increase in REM sleep
What impact to Benzes have on muscle?
Reduce muscle tone and coordination
T or F Benzo’s have anti-convulsant activity?
True
Anterograde amnesia is associated with what drug?
Benzodiazepines
- endoscopy
- dental procedures
- date rape drug
MOA of benzodiazepines
Enhance GABA activity at GABAa receptors
bind to an accessory site on the receptor, induces conformational change
to enhance GABA binding + activity
How does GABA cause inhibition
Increases Cl- by increasing the frequency of channel openings
MOA of benzodiazepine inverse agonists e.g. B carbolines
Bind to receptor at BZ accessory site and produce increased anxiety and convulsions
What do BZ antagonists do?
Competively inhibit the action of BZ ( agonists ) and BZ inverse agonists
They bind passively, no direct effect, they just block the others from acting
Where do BZs bind, accumulate and how are they metabolised?
bind to plasma proteins
accumulate in fat
excreted as glucuronide conjugates
Noradazepam is a long-lasting, pharm active metabolite of some BZs
What consideration must be made when prescribing BZs to elderly patients?
The half life is increased in elderly
Which type of BZ is used for sleep disorders and anxiety?
Short and medium
lorazepam ad alprazolam
What are the uses and give an example of a long acting BZ?
Used for anxiety and epilepsy
not hypnosis
e.g. diazepam
T or F triazolam is used for anxiety?
F
it is ultra short < 6hrs
only hypnotic
T or F alprazolam is used for anxiety?
True 24hrs medium BZ
What can be used to reverse the acute toxicity caused by BZs?
How does the acute toxicity present?
Flumazenil
respiratory depression esp when combined with alcohol
What type of drug is zolpidem
a non-BZ hypnotic
What are the advantages of using zolpidem vs BZ
No hanger
rapid onset of action
not myorelaxant, anticonvulsant or anxyiolytic
Buspirone, isapirone and gepirone are all examples of
5-HT1a receptor agonists
Use of 5-HT1a receptor agonists ?
Anxiolytic
takes days or weeks
Which is not a side effect of 5-HT1a receptor agonists ?
- Dizziness
- headache
- sedation
- loss of balance
- loss of coordination
- withdrawal
- nausea
- addiction
Sedation is not a side effect of 5-HT1a receptor agonists
addiction not listed
Pentobarbital ……the actions of GABA
Enhances the actions of GABA
T or F
tolerance and dependence are side effects of barbiturates
True
What is the first line therapy for anxiety disorders
give examples
SSRI
e.g. fluoxetine / prozac
escitalopram / lexapro
Fluoxetine is a
SSRI
