Sedative- Hypnotics (Anxiolytics)

Question 1

What are the Benzodiazepines

Answer 1

Alprazolam, Chlordiazepoxide, Clonazepam, Clorazepate, Diazepam, Lorazepam, Oxazepam, Prazepam

Question 2

What are the non-benzodiazepine anxiolytics

Answer 2

Buspirone, Propanolol

Question 3

What is the mechanism of action of Benzodiazepines

Answer 3

They act as allosteric agonists, they do not activate the receptor independently of the natural ligand. They potentiate effects of GABA

Question 4

What is Flumazenil and what does it do/used for

Answer 4

Flumazenil is a competitive antagonist that blocks the effects of benzodiazepines

Question 5

Which drugs are metabolized to N-desmethyldiezapam (nordiazepam)

Answer 5

Clorazepate
Diazepam
Chlordiazepoxide
Prazepam
Halazepam

Question 6

Of the drugs that are metabolized to nordiazepam, which is not directly metabolized to this but must first undergo other phases of metabolism?

Answer 6

Chlordiazepoxide

Question 7

What are the active metabolites of Chlordiazepoxide?

Answer 7

N-desmethylchlordiazepoxide
Demoxepam
Nordiazepam

Question 8

What is N-desmethyldiazepam (nordiazepam) metabolized to, and by what process does this occur?

Answer 8

Oxazepam via Hydroxylation

Question 9

Which Benzodiazepines are not metabolized to Oxazepam?

Answer 9

Alprazolam and Lorazepam

Question 10

What is the active metabolite of Alprazolam?

Answer 10

a-hydroxyalprazolam

Question 11

Which drug is converted directly to a Glucuronide conjugate?

Answer 11

Lorazepam

Question 12

Are benzodiazepines safe for pregnancy? What Pregnency catagory are they in?

Answer 12

No. Catagory D

Question 13

Which Benzodiazepines have a Rapid onset of action?

Answer 13

Clorazepate
Diazepam
Flurazepam
Triazolam

Question 14

Which Fast acting Benzo has the shortest half life?

Answer 14

Triazolam (It is the only Rapid onset Benzo with a short t1/2, all others have long t1/2)

Question 15

Which Benzos have a slow onset of action?

Answer 15

Oxazepam
Prazepam
Temazepam

Question 16

Which slow acting Benzo has a short half life?

Answer 16

Oxazepam

Question 17

Which slow acting Benzo has a long half life?

Answer 17

Prazepam

Question 18

Withdrawal reactions occur after abrupt discontinuation of Benzos. Which benzos should be tapered?

Answer 18

Short half life benzos should be tapered.

Triazolobenzodiazepines (Alprazolam, Estazolam, and Triazolam)

Question 19

Which Benzo is most used for panic attacks? Why?

Answer 19

Alprazolam because it also has antidepressant effects similar to TCAs.

Question 20

Which Benzo produces muscle relaxation in clinical doses?

Answer 20

Diazepam

Question 21

Which Benzos are used to treat Alcohol withdrawal?

Answer 21

Chlordiazepoxide
Diazepam
Lorazepam

Question 22

Which Benzo do you use to treat Alcohol withdrawal in a person with hepatic impairment?

Answer 22

Lorazepam because it undergoes Renal metabolism as well

Question 23

Which subunits on the GABA receptor do Benzos bind to, to enhance inhibitory action of GABA?

Answer 23

a1, a2, a3 or a5 AND y subunit

Question 24

What is the chronological order in which the tolerance to benzos develop

Answer 24

1. Sedative and Hypnotic effect
2. Anticonvulsant effect
3. RARELY IF EVER TO ANXIOLYTIC EFFECT
   (the time which tolerance develops varies by drug)

Question 25

What is the mechanism for tolerance to Benzos

Answer 25

1. Receptor uncoupling 2. Receptor sub-unit down-regulation 3. Sensitization of glutamatergic system 4. Crosstalk from other G-protein receptor systems

Question 26

Which Benzos can be administered by injection?

Answer 26

Diazepam | Lorazepam

Question 27

What patient populations do you need to be careful prescribing Benzos to? Why?

Answer 27

Older patients, especially those with COPD because Benzos cause respiratory depression

Question 28

In a patient who is experiencing respiratory depression from Benzos, what drug do you give to offset the effects?

Answer 28

Flumazenil

Question 29

What is the mechanism of action of Buspirone?

Answer 29

Supresses seretonergic while enhancing noradrenergic and dopaminergic activities

Question 30

What is Buspirone used for?

Answer 30

Equally effective as Benzos as anxiolyitc | Has no anticonvulsant, muscle relaxant, or sedative effect

Question 31

What is propanolol used for (not cardio)

Answer 31

performance anxiety or stage fright

Question 32

What is the problem with using buspirone?

Answer 32

It has a VERY slow onset, and takes weeks to see clinical effect

Question 33

Describe mechanism of Propanolol to reduce stage fright (not mechanism of action)

Answer 33

supresses somatic and autonomic symptoms of anxiety but does not alter emotional symptoms