Sedative - Hypnotics

Question 1

Anxiolytics usage of BNZs to treat anxiety

Answer 1

• use drugs w/ long half lives

- allosteric agonists at GABA receptor, increase potency of endogenous GABA

Question 2

What BNZs are metabolized to nordiazepam

Answer 2

Cloraepate, diazepam, chlordizepoxie, prazepam, halazepam

- has long half life

Question 3

What BNZs have a shorter half life and why?

Answer 3

• Lorazepam and alprazolam b/c of simpler metabolism being rapdily conjugated and eliminated in urine

Question 4

Who BNZs don’t under hepatic metabolism

Answer 4

• lorazepam

Question 5

What BNZs have a rapid or slow onset of action?

Answer 5

1. Rapid = diazepam, flurazepam, triazolam
2. Slow = prazepam
   - onset is determined by dissolution rate and speed of absorption from the GIT

Question 6

What BNZs have a long or slow half life?

Answer 6

1. long = chlordiazepoxide, diazepam, flurazepam, prazepam

2. short = clonazepam, traizolam

Question 7

BNZ withdrawal problems

Answer 7

• occurs w/ abrupt discontinuation, especially a problem if drug has short half life
• alprazolam and triazolam = more severe reactions
• take care to taper drug

Question 8

What are the symptoms of BNZ withdrawal

Answer 8

generally autonomic - tremor, sweating, insomnia, abdominal discomfort, tachycardia, systolic HTN, muscle twitching, and photo/audio sensitivity

• rebound anxiety and insomnia
• convulsions possible after protracted high doses

Question 9

What is commonly used to treat anxiety?

Answer 9

alprazolam, lorazepam, clonazepam

Question 10

What is commonly used to treat panic attacks

Answer 10

alprazolam b/c has antidepressant activity like TCAs

Question 11

What BNZ leads to muscular relaxation

Answer 11

diazepam inhibits monosynpatic reflexes in spinal cord

Question 12

What is commonly used in EtOH withdrawal

Answer 12

• chlordiazepoxide and diazepam

- lorazepam is hepatic impairment

Question 13

How does tolerance develop w/ BNZs

Answer 13

1st to sedative and hypnotic effects
2nd to anticonvulsant effects
- rarely if ever to anxiolytic effects
- absolute time varies by drug

Question 14

what is thought to be the mechanism of tolerance w/ BNZs

Answer 14

1. receptor uncoupling
2. receptor subunit downregulation
3. sensitization of glutamatergic system
4. crosstalk from other GPCRs

Question 15

what receptor subunits do BNZs interact with?

Answer 15

by drug interaction w/ GABA receptors in various locations in the brain. being btw Alpha 1, 2, 3, or 5 subunit and gamma subunit

Question 16

ADE of BNZs

Answer 16

1. avoid activities requiring mental alertness until drug effects are realized
2. may cause nausea, xerostomia, confusion, headache, of feeling of indifference
3. may see excessive sedation or respiratory depression
4. avoid concomitant use of EtOH or other CNS depressants

Question 17

MOA of buspirone

Answer 17

• not clear but my suppress serotonergic while enhancing noradrenergic and dopaminergic activities
• but slow onset but just as effective as BNZ
• no anticonvulsants, muscle relaxant, or sedative effects

Question 18

MOA of propranolol

Answer 18

B adrenergic receptor blocker

- performance anxiety