Pharm: Sedative Hypnotics Flashcards
How do benzodiazepines distribute through the body and how are they metabolized?
- Widely distributed throughout body: CNS, placenta, breast-milk
- Hepatic metabolism (CYP3A4) and excretion via kidney
What are the benefits of using benzodiazepines for anxiety states?
- High therapeutic index; antagonist available for OD (flumazenil)
- Low-risk of drug-drug interactions
- Minimal effect of cardiovascular or autonomic function
Which benzodiazepine has the fastest rate of onset?
Diazepam
How does Diazepam differ from Alprazolam in terms of half-life, active metabolites and rate of onset?
- Diazepam: long half-life (>100 hr); has active metabolite; very fast onset
- Alprazolam: short half-life (12-15); no active metabolite; fast onset
Which benzodiazepine has a short half-life (5-14 hr), no active metabolite, and the slowest rate of onset?
Oxazepam
Which 2 benzodiazepines have the shortest half-lifes?
Triazolam and Midazolam
Which 4 benzodiazepines have the longest half-lives all >100 hr and all have active metabolites?
- Chlordiazepoxide
- Clorazepate
- Diazepam
- Flurazepam
List 5 benzodiazepines that are short to intermediate acting?
- Alprazolam
- Temazepam
- Triazolam
- Oxazepam
- Midazolam
What is the effect of barbituates on CYP450 enzymes?
Can induce CYP450 enzymes
What is the prototype ultra-short acting barbituate used in anesthesia?
Thiopental
What is the prototype short-acting barbituate that is used for insomnia?
Secobarbital
What is the prototype long-acting barbituate that is used for seizures?
Phenobarbital
What are 3 of the newer sedative hypnotics that are used as sleep aids?
- Eszopiclone (Lunesta)
- Zolpidem (Ambien)
- Zaleplon (Sonata)
Which newer sedative hypnotic has the advantage of coming in a biphasic release formulation for sustained sleep maintenance?
Zolpidem (Ambien)
Which newer sedative hypnotic has the longest half-life?
Eszopiclone (Lunesta)
What are 4 AE’s associated with the sedative drug, Ramelteon?
- Dizziness
- Somnolence
- Fatigue
- Endocrine changes –> ↓ testosterone and ↑ prolactin
What is Buspirone used for and what must you keep in mind when prescribing this drug?
- Approved for tx of generalized anxiety disorder
- Anxiolytic effects may take more than a week to become established (less effective in acute panic disorders)
