Sleep-wake disorders Flashcards
What are the 5 benzodiazepines that are FDA approved for insomnia and which is most commonly prescribed?
Temazepam is most commonly prescribed
others: estazolam, furazepam, quazepam, triazolam
all are pregnancy category X
MOA for benzodiazepines and insomnia:
nonselective binding BZ-GABA
Tolerance to benzodiazepines for insomnia develops after ____
1 month
What effect does zolpidem have on sleep stages
increase stage 2, decrease REM
no effect stage 3
MOA for nonbenzodiazepine receptor agonists is?
enhancement of GABA. selective binding to α-1->sedation
What is the big warning with using zolpidem (ambien)? What dosing should be used in females + geriatric patients?
complex sleep behaviors (walking, eating, driving)
IR->5mg. CR-> 6.25mg (decreased clearance)
What is the difference between Zolpidem IR and Zolpidem CR?
IR is labelled for short term use and the max dose is 5
CR not labelled for short term use and the max dose is 6.25
Why would a patient take Zaleplon (sonata)
take if patient wakes in the middle of night but has >4 hours before waking up for the day.
short half life (no effect on next morning)
Zaleplon (sonata) is labelled for (short/long) term use
short <1month
Eszopiclone (lunsta) use and duration of action
decrease sleep latency + number awakenings
duration of axn up to 6 hours
Eszopiclone (lunesta) is labelled for (short/long) term use
long
the choice NZBRA for chronic insomnia
What is the benefit for taking nonbenzodiazepine receptor agonist over benzodiazepines? Why is that?
- lower rates of withdrawal, tolerance, rebound insomnia, daytime sedation
- selective for α1
- no active metabolites
- reduced effect on sleep architecture
Nonbenzodiazepine receptor agonist should or should not be taken with food? How much before sleep time should it be taken?
Do not take with food-> delay absorption
Take 30 minutes before sleep time
Nonbenzodiazepine receptor agonists are metabolized by ___ with a short half life and ______
CYP3A4, no active metabolites
What are some conditions that would caution someone from being prescribed nonbenzodiazepine receptor agonists?
sleep apnea, respiratory disorders (COPD), liver disease, geriatric
better than BZ but still on Beer’s criteria
Nonbenzodiazepine receptor agonists are schedule __ and pregnancy category __?
IV (abused, avoid in SUD dependance, withdrawal)
C
need to taper to reduce
Ramelteon (rozerem) MOA is
Agonist at melatonin MT1 and MT2
NO gaba effect
Onset of effect and half life for Ramelteon?
Onset = 30 minutes
Half life = 3 hours
What are adverse effects from Ramelteon?
Really not many. Not controlled-> use in SUD Not short term Good choice for people who can't be on nonbenzodiazepine receptor agonist Preg category C
Suvorexant (Belsomra) MOA is ?
Orexin receptor antagonist
reversible at orexin 1 and 2 receptors in hypothalamus->orexin rises in AM and effect down
no gaba affinity
What are some adverse effects of suvorexant?
next day somnolence
block orexin on arousal->dampen arousal from hist, Ash, monoamines
What is the half life of orexin
12 hours-> next day sleepiness
Survorexant (is/is not) a controlled substance, used for (short/long) term use, should be taken ___ minutes before bedtime, and is pregnancy category __
Is long 30 C do not take with food
When would you use trazodone, doxepin, mitazapine for insomnia? What about quetiapine?
Comorbid depression
Comorbid anxiety, bipolar, or schizophrenia
For both: if failed other meds or contraindicated for BZ/NZBRA
What is the different between modafinil and armodafinil? (Treatments for narcolepsy)
modafinil is a racemic mix, armodafinil is the r-isomer of modafinil
What are the uses for modafinil and armodafinil?
Narcolepsy. This is excessive daytime sleepiness-> use to increase alertness and daytime performance.
What is MOA for modafinil and armodafinil?
These are schedule ___
not well understood
Increase DA by inhibit reuptake inhibitor->increase hist and orexin
increase 5HT and glutamate -> decrease gaba
IV
What is sodium oxybate (Xyrem) used for?
excessive daytime sleepiness, decrease sleep paralysis, cataplexy, hypnagogic hallucinations
MOA for sodium oxybate (Xyrem)?
not well understood; agonist at GABA-B -> effects NE, DA, 5HT, gaba
increase slove wave sleep, decrease night awakenings, increase REM
