Sedative- Hypnotics (Anxiolytics) Flashcards
What are the Benzodiazepines
Alprazolam, Chlordiazepoxide, Clonazepam, Clorazepate, Diazepam, Lorazepam, Oxazepam, Prazepam
What are the non-benzodiazepine anxiolytics
Buspirone, Propanolol
What is the mechanism of action of Benzodiazepines
They act as allosteric agonists, they do not activate the receptor independently of the natural ligand. They potentiate effects of GABA
What is Flumazenil and what does it do/used for
Flumazenil is a competitive antagonist that blocks the effects of benzodiazepines
Which drugs are metabolized to N-desmethyldiezapam (nordiazepam)
Clorazepate Diazepam Chlordiazepoxide Prazepam Halazepam
Of the drugs that are metabolized to nordiazepam, which is not directly metabolized to this but must first undergo other phases of metabolism?
Chlordiazepoxide
What are the active metabolites of Chlordiazepoxide?
N-desmethylchlordiazepoxide
Demoxepam
Nordiazepam
What is N-desmethyldiazepam (nordiazepam) metabolized to, and by what process does this occur?
Oxazepam via Hydroxylation
Which Benzodiazepines are not metabolized to Oxazepam?
Alprazolam and Lorazepam
What is the active metabolite of Alprazolam?
a-hydroxyalprazolam
Which drug is converted directly to a Glucuronide conjugate?
Lorazepam
Are benzodiazepines safe for pregnancy? What Pregnency catagory are they in?
No. Catagory D
Which Benzodiazepines have a Rapid onset of action?
Clorazepate
Diazepam
Flurazepam
Triazolam
Which Fast acting Benzo has the shortest half life?
Triazolam (It is the only Rapid onset Benzo with a short t1/2, all others have long t1/2)
Which Benzos have a slow onset of action?
Oxazepam
Prazepam
Temazepam
Which slow acting Benzo has a short half life?
Oxazepam
Which slow acting Benzo has a long half life?
Prazepam
Withdrawal reactions occur after abrupt discontinuation of Benzos. Which benzos should be tapered?
Short half life benzos should be tapered.
Triazolobenzodiazepines (Alprazolam, Estazolam, and Triazolam)
Which Benzo is most used for panic attacks? Why?
Alprazolam because it also has antidepressant effects similar to TCAs.
Which Benzo produces muscle relaxation in clinical doses?
Diazepam
Which Benzos are used to treat Alcohol withdrawal?
Chlordiazepoxide
Diazepam
Lorazepam
Which Benzo do you use to treat Alcohol withdrawal in a person with hepatic impairment?
Lorazepam because it undergoes Renal metabolism as well
Which subunits on the GABA receptor do Benzos bind to, to enhance inhibitory action of GABA?
a1, a2, a3 or a5 AND y subunit
What is the chronological order in which the tolerance to benzos develop
- Sedative and Hypnotic effect
- Anticonvulsant effect
- RARELY IF EVER TO ANXIOLYTIC EFFECT
(the time which tolerance develops varies by drug)
What is the mechanism for tolerance to Benzos
- Receptor uncoupling
- Receptor sub-unit down-regulation
- Sensitization of glutamatergic system
- Crosstalk from other G-protein receptor systems
Which Benzos can be administered by injection?
Diazepam
Lorazepam
What patient populations do you need to be careful prescribing Benzos to? Why?
Older patients, especially those with COPD because Benzos cause respiratory depression
In a patient who is experiencing respiratory depression from Benzos, what drug do you give to offset the effects?
Flumazenil
What is the mechanism of action of Buspirone?
Supresses seretonergic while enhancing noradrenergic and dopaminergic activities
What is Buspirone used for?
Equally effective as Benzos as anxiolyitc
Has no anticonvulsant, muscle relaxant, or sedative effect
What is propanolol used for (not cardio)
performance anxiety or stage fright
What is the problem with using buspirone?
It has a VERY slow onset, and takes weeks to see clinical effect
Describe mechanism of Propanolol to reduce stage fright (not mechanism of action)
supresses somatic and autonomic symptoms of anxiety but does not alter emotional symptoms
