Insomnia Flashcards
what NT keep you alert
NE
Ach
dopamine
histamine
hypocretin/orexin
what NT make you sleepy
adenosine
GABA
what drugs make you sleepy
anticholinergic
antihistamines
benzos
suvorexant
what meds keep you awake
amphetamines
adenosine antagonists
order of tx for insomnia
- address underlying causes
- assess for stimulating drugs
- CBT
- drugs
underlying causes of insomnia
sleep apnea
pain
RLS
anxiety/dpn
stimulating meds that might cause insomnia
caffeine
decongestants
stimulants
SSRIs
diuretics
preferred tx for insomnia
CBT
first line pharm for insomnia
nonbenzos → zolpidem, rameleton
short acting benzos → tamezepam
ability of drug to rapidly induce sleep is influenced by
rate of absorption
ability to maintain sleep is influenced by
t½
rebound insomnia is caused by __
and influenced by __
abrupt d/c
t½
what drug is first line for insomnia
zolpidem - ambien → “z drug”
3 z drugs to know
zolpidem → ambien
eszopiclone → lunesta
zaleplon → sonata
4 other drug agents for insomnia besides z drugs
benzos
orexin antagonists
melatonin agonists
1st gen antihistamines
2 benzos used for insomnia
temazepam → restoril
triazolam → halcion
orexin antagonist to know
suvorexant → belsomra
melatonin agonist to know
ramelteon → rozerem
2 1st gen antihistamines to know
diphenhydramine
doxylamine → Nyquil
t/f: there is no receptor for benzos
T!
where do benzos bind
binding site on GABA chloride channel
which drugs bind to alpha 1 subunit
benzos
z drugs
alpha 1 is located in the __
and has __ therapeutic action (2)
cortex
sleep/anticonvulsant
negative effects associated w. alpha 1 activation (benzos and z drugs)
amnesia
additive CNS dpn
which drug binds to alpha2 and alpha5 subunits
benzos
alpha 2 and 5 subunits are located in the (2)
and have __ therapeutic actions (2)
limbic system/brain stem
anxiolytic myorelaxant
negative effects related to alpha 2 and 5 subunit activation (benzos)
motor incoordination
tolerance/dependence
addiction
decreased REM
which chloride subunit do both benzos AND z drugs bind to
alpha 1
z drugs bind only to __ Cl subunit
benzos bind to __ subunits (3)
z drugs: alpha 1
benzos: alpha1, alpha2, alpha5
tolerance to benzos occurs if used > __
1 week
benzos, etoh, and barbs all negatively affect which stage of sleep
REM
z drugs are rapidly absorbed and eliminated via __ meatbolism
hepatic
which sleep drug has the longest t½
escopiclone → lunesta
most widely prescribed agent for insomnia
zolpidem → ambien
immediate release ambien is used to
reduce sleep latency
sustained release ambien (CR) is used to
reduce nocturnal awakenings
low dose sublingual ambien (intermezzo) is used for
middle of the night awakening
which z drug is safe for long term use
and used for sleep maintenance
escopiclone → lunesta
which z drug has minor role in insomnia, but is used to decrease time to sleep onset
zalepon → sonata
rapid oral onset
common s.e of z drugs
drowsiness
amnesia
HA
GI
rarely bizarre behavioral disturbances
what class are Z drugs
IV
is dependence-withdrawal likely w. z drugs
yes, but unlikely
fatal overdoses are rare w. z drugs and benzos, unless
taken in combo w. other CNS depressants
what 2 benzos are used for insomnia
triazolam → halcion
temazepam → restoril
t½ of:
triazolam:
temazepam:
trazolam: short
temazepam: intermediate
which benzo used for insomnia can cause rebound insomnia
triazolam (halcion)
d.t rapid elimination
which benzo has minimal effect on sleep latency
temazepam
dt longer t½
triazolam has less __
but more __
daytime sedation
rebound insomnia
dt short t½
benzos have declining use for insomnia due to
daytime sedation/performance impairment
rebound insomnia
anterograde amnesia
psychologic and physiologic dependence
4 insomnia drugs w. non GABA benzo binding site mechanisms
suvorexant
ramelteon
antidepressants
antihistamines
hypothalamic neuropeptides that innervate all arousal systems and fxn to maintain wakefulness
orexins
what insomnia drug is an orexin antagonist
suvorexant
ADR of suvorexant
dose related next-day somnolence
what class is suvorexant
IV → abuse liability
suvorexant is FDA approved for __
but is really only used when __
sleep-onset/maintenance
first line drugs have failed
what insomnia drug is an agonist a melatonin receptors
ramelteon
MT1 receptor fxn:
MT2 receptor fxn:
MT1: induces sleep
MT2: regulates circadian rhythms
ADRs of ramelteon
dizziness
somnolence
fatigue
nausea
ramelteon is used for:
but melatonin may be better for:
reducing sleep latency
jet lag
what insomnia drug is a serotonin receptor antagonist and reuptake blocker
trazodone
ADRs of trazodone
oversedation
orthostasis
priapism
what class of drug is trazodone
antidepressant → SARI
pro of trazodone
no concerns w. tolerance or dependence
what insomnia drug is an antagonist at CNS histamine H-1 and muscarinic receptors
diphenhydramine - doxylamine
diphenhydramine/doxylamine might not be best for elderly due to what ADR
antimuscarinic
3 first line drugs for sleep onset
zeleplon → z drug
zolpidem → z drug
ramelton → melatonin receptor agonist
1st line for sleep onset and maintenance
zolpidem CR (extended release) → z drug
eszopiclone → z drug
2nd line for insomnia:
adjunctive for insomnia:
2nd line: trazodone → antidepressant
+/- temazepam
adjunctive: melatonin, diphenhydramine → antihistamine