Sedatives-Hypnotics-Kisby Flashcards
What is the tx for transient insomnia?
Hypnotics - low dose for 2-3 nights
What is the tx for short-term insomnia?
Hypnotics used intermittently during this time (3 days - 3 weeks)
Which drugs are Benzodiazepines? (5)
- Estazolam
- Triazolam
- Flurazepam
- Temazepam
- Quazepam
Which drugs are selective Benzodiazepine receptor agonists (aka Z compounds)? (3)
- Zolpidem
- Zalepion
- Eszopiclone
Which drugs are Barbituates? (6)
- Phenobarbital
- Pentobarbital
- Thiopental
- Amobarbital
- Secobarbital
- Mephobarbital
Which drugs are melatonin receptor agonists? (2)
- Ramelteon
2. Tasimelteon
Why are Benzos used more than Barbs for sleep?
Safer! Less tolerance too.
Estazolam
- Sleep maintenance
- Half-life: 8-28hrs
Flurazepam
- Sleep onset & sleep maintenance
- Half-life: 2-3hrs
Quazepam
- Sleep maintenance
- Half-life: 41hrs
Temazepam
- Sleep maintenance
- Half-life: 3-18hrs
Triazolam
- Sleep onset
- Half-life: 2-6hrs
What is the MOA of Benzos?
Allosterically bind to a1 and y subunit of GABAa receptor complex leading to sedation
What do Benzos affect that Z compounds don’t?
REM sleep
Zolipidem
- Sleep maintenance
- Half-life: 5-7hrs
- SE: unpleasant taste, dry mouth
Zaleplon
- Sleep onset
- Half-life: 5-10hrs
Eszopiclone
- Sleep onset or sleep maintenance
- Half-life: 5-10hrs
What do all Z compounds interact with?
CYP3A4 & ETOH
What can abrupt Benzo withdrawal lead to?
Rebound insomnia
What is the MOA of Barbs?
Selectively bind GABAa receptor at an allosteric a and B subunit site
What is the MOA of Melatonin receptor agonists?
- Selectively bind to MT1 & MT2 receptors in SCN
- MT1 regulates sleepiness
- MT2 regulates phase shifting
Ramelteon
- Sleep onset
- Half-life: 1-3hrs
- SE: infertility, somnolence
Tasimelteon
- Sleep onset & sleep maintenance
- Half-life: .5-3hrs
- Use: Non-24 hour sleep disorder
