Sleep Flashcards
Benzodiazepines
- target a1, a2-a5
- promote sleep, lessen anxiety
- most likely to produce memory disturbances such as anterograde amnesia
In what stage of sleep do night terrors occur?
Stage 3
Z Drugs
- target a1
- promote sleep
Zolpidem
- ambien , ambien CR
- Z drug used for sleep
- targets a1
- non-BDZ BDZ agonist
- reduces sleep latency
- reduces nocturnal awakenings
- reduces insomnia associated with middle of the night awakening
Alpha 1 Target
- agonist: BDZs, Z drugs
- location: cortex
- actions: sleep, anticonvulsant, amnesia, additive CNS depression
A2-A5 Targets
- agonist: BDZs
- location: limbic, brain stem
- actions: anxiolytic, myorelaxant, tolerance, dependence, addiction
“Hangover effect” is increased with drugs with:
-longer half life
Triazolam Pharmacokinetcs
- Halcion
- BDZ agonist
- rapid oral absorption
- short 1/2 life, less daytime sedation
- rebound insomnia next day due to rapid elimination
- use cautiously in elderly- dose reduction
Temazepam Pharmacokinetics
- Restoril
- BDZ agonist
- slow absorption- minimal effect on sleep latency
- intermediate 1/2 life (9-13 hrs)
Flurazepam Pharmacokinetics
- Dalmane
- BDZ agonist
- long t1/2 and active metabolite, low tolerance
- can accumulate in elderly
- impaired hepatic clearance
- daytime sedation (hangover)/overdosage
- less tolerance development than other BDZs
Zolpidem and Zaleplon Pharmacokinetics
- rapid oral absorption
- shortest durations of action and 1/2 lives
- zolpidem eliminated more slowly in females- dose recommendation halved to prevent daytime hangover
Eszopiclone Pharmacokinetics
- Lunesta
- structurally different from zolpidem or zaleplon with longer 1/2 life
- Z drug
BDZ Adverse Reactions
- daytime sedation and performance impairment
- anterograde amnesia
- rebound insomnia
- psychologic and physiologic dependence
- overall very safe
- fatal overdose very rare unless taken in combo with EtOH
Z Drug Adverse Reactions
- safety similar to BDZs
- rarely bizarre behavioral disturbances
- tolerance, dependence, withdrawal possible, but less than with BDZs
- overall very sage\
- fatal overdose very rare unless taken in combo with EtOH
Zaleplon Effectiveness
- effective for:
- dec. time to sleep onset
- NOT for reducing nocturnal awakenings
- BUT is suitable to aid sleep onset for middle of night nocturnal awakenings
Eszopiclone Effectiveness
- lunesta
- effective for:
- sleep maintenance (longest half life)
- safe for long term use
- Z drug
Triazolam
-rapid oral absorption
Trazedone
- mixed 5HT reuptake blocker and receptor antagonist
- dec. REM sleep
- ADR: oversedation, orthostasis (a1 block), priapism
- Role: antidepressant- very sedating and improves sleep continuity
- no concerns with tolerance or dependence
Ramelteon
- Melatonin Receptor Agonist (MT1 induces sleepiness)
- ADRs: dissiness, somnolence, fatigue, nausea
- Role: useful to reduce sleep latency
Melatonin
- dietary supplement
- may be best for jet lag
Diphenhydramine
- benadryl
- antagonist at CNS histamine H1 and muscarinic receptors
- most likely to cause anticholinergic effects (no pee, see, spit shit)
- ADRs: generally minimal, BUT antimuscarinic actions can be troublesome, esp in elderly
- Role: minimally effective, generally not recommended long term, can see tolerance after >10 days use
Treatment for Slow Wave Sleep
-trazedone
Adjunctive Sleep Treatment
- melatonin
- diphenhydramine
1st Line Tx of Sleep Onset
- zaleplon
- zolpidem
- ramelteon
1st Line Tx for Sleep Onset and Sleep Maintenance
- zolpidem CR
- eszopiclone
What causes homeostatic drive in sleep loss?
-likely adenosine buildup
REM Sleep
- in charge of development and memory
- rapid eye movements
- most dreams
- active brain, paralyzed body
- suppressed with EtOH
Non-REM Sleep
- in charge of brain and body regeneration
- stages N1, N2, N3 (SWS)
- sleep walking, night terrors occurs during SWS
Chronic jet lag, shift work, and sleep deprivation cause atrophy of:
-hippocampus
Epworth Sleepiness Scale
- helps sort out sleepy from fatigued
- high score= excessive daytime sleepiness
- low epworth= fatigue
Lowest core body temp:
-is 2-3 hours before spontaneous wake time
Tx for Circadian Problems
- exposure to light
- melatonin
Delayed Sleep Phase Syndrome
- night owls
- insomnia when trying to sleep at socially appropriate time
- like to stay up late
Advanced Sleep Phase Syndrome
- early birds
- like to wake up early
