Pharm: Sedative Hypnotics

Question 1

How do benzodiazepines distribute through the body and how are they metabolized?

Answer 1

• Widely distributed throughout body: CNS, placenta, breast-milk
• Hepatic metabolism (CYP3A4) and excretion via kidney

Question 2

What are the benefits of using benzodiazepines for anxiety states?

Answer 2

• High therapeutic index; antagonist available for OD (flumazenil)
• Low-risk of drug-drug interactions
• Minimal effect of cardiovascular or autonomic function

Question 3

Which benzodiazepine has the fastest rate of onset?

Answer 3

Diazepam

Question 4

How does Diazepam differ from Alprazolam in terms of half-life, active metabolites and rate of onset?

Answer 4

• Diazepam: long half-life (>100 hr); has active metabolite; very fast onset
• Alprazolam: short half-life (12-15); no active metabolite; fast onset

Question 5

Which benzodiazepine has a short half-life (5-14 hr), no active metabolite, and the slowest rate of onset?

Answer 5

Oxazepam

Question 6

Which 2 benzodiazepines have the shortest half-lifes?

Answer 6

Triazolam and Midazolam

Question 7

Which 4 benzodiazepines have the longest half-lives all >100 hr and all have active metabolites?

Answer 7

• Chlordiazepoxide
• Clorazepate
• Diazepam
• Flurazepam

Question 8

List 5 benzodiazepines that are short to intermediate acting?

Answer 8

• Alprazolam
• Temazepam
• Triazolam
• Oxazepam
• Midazolam

Question 9

What is the effect of barbituates on CYP450 enzymes?

Answer 9

Can induce CYP450 enzymes

Question 10

What is the prototype ultra-short acting barbituate used in anesthesia?

Answer 10

Thiopental

Question 11

What is the prototype short-acting barbituate that is used for insomnia?

Answer 11

Secobarbital

Question 12

What is the prototype long-acting barbituate that is used for seizures?

Answer 12

Phenobarbital

Question 13

What are 3 of the newer sedative hypnotics that are used as sleep aids?

Answer 13

• Eszopiclone (Lunesta)
• Zolpidem (Ambien)
• Zaleplon (Sonata)

Question 14

Which newer sedative hypnotic has the advantage of coming in a biphasic release formulation for sustained sleep maintenance?

Answer 14

Zolpidem (Ambien)

Question 15

Which newer sedative hypnotic has the longest half-life?

Answer 15

Eszopiclone (Lunesta)

Question 16

What are 4 AE’s associated with the sedative drug, Ramelteon?

Answer 16

• Dizziness
• Somnolence
• Fatigue
• Endocrine changes –> ↓ testosterone and ↑ prolactin

Question 17

What is Buspirone used for and what must you keep in mind when prescribing this drug?

Answer 17

• Approved for tx of generalized anxiety disorder
• Anxiolytic effects may take more than a week to become established (less effective in acute panic disorders)