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85 Cards in this Set

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Treatment principles: transient insomnia
a)sleep hygiene
b)careful use of S-H
short-term insomnia
a)sleep hygiene
b)intermittent use of S-H (skip 1-2 nights of meds after 1-2 nights of good sleep)
chronic insomnia
a)reassessment of other etiologies
b)reinforce sleep hygiene
c)limit use of S-H to 1 out of 3 nights to prevent tolerance and dependence
these agents are useful in mild, transient insomnia, but less effective than BZDs
1st gen antihistamines (doxylamine, diphenhydramine)
this antihistamine is typically used for peri-operative sedation, but is occasionally used for insomnia
hydroxyzine (Vistaril or Atarax)
1st gen antihistamines adverse effects (3)
1)hangover effect
2)anticholinergic effects
3)paradoxical CNS stimulation in young children/elderly
regular use of antihistamines should be avoided because tolerance develops after how many days of continuous use?
4
diphenydramine dose
50mg HS
doxylamine dose
25mg HS
possible advantage of doxylamine over diphenhydramine
doxylamines shorter t1/2 may cause less hangover effect
BZDs MOA
binds to BZD-1 (a1-GABA-A) and BZD-2 (a2-GABA-A) receptors in brain and periphery, enhancing GABA neurotransmission
BZD adverse effects (4)
1)hangover effect
2)anterograde amnesia
3)respiratory depression
4)reduce stage 3,4 sleep and REM sleep
these long-acting BZDs are more likely to exert a hangover effect due to accumulation of active metabolites (2)
flurazepam, quazepam
If a patient presents w/ hangover sxs (daytime sedation/falls) what should you do?
a)switch to a BZD w/ shorter duration of action
b)switch to another class of S-H
Type of BZD preferred if a patient has concomitant anxiety
long-acting BZD to maintain duration throught the next day
anterograde amnesia is especially seen w/ this BZD due to its rapid onset and short t1/2
triazolam
Time to development of tolerance with short-acting BZDs and longer-acting BZDs
-1-2wks of ocntinued use
-1-3months
pregnancy category of BZDs
D or X; avoid in breastfeeding women
If a patient presents w/ hangover sxs (daytime sedation/falls) what should you do?
a)switch to a BZD w/ shorter duration of action
b)switch to another class of S-H
Type of BZD preferred if a patient has concomitant anxiety
long-acting BZD to maintain duration throught the next day
anterograde amnesia is especially seen w/ this BZD due to its rapid onset and short t1/2
triazolam
If a patient presents w/ hangover sxs (daytime sedation/falls) what should you do?
a)switch to a BZD w/ shorter duration of action
b)switch to another class of S-H
Type of BZD preferred if a patient has concomitant anxiety
long-acting BZD to maintain duration throught the next day
anterograde amnesia is especially seen w/ this BZD due to its rapid onset and short t1/2
triazolam
Time to development of tolerance with short-acting BZDs and longer-acting BZDs
-1-2wks of ocntinued use
-1-3months
Time to development of tolerance with short-acting BZDs and longer-acting BZDs
-1-2wks of ocntinued use
-1-3months
pregnancy category of BZDs
D or X; avoid in breastfeeding women
pregnancy category of BZDs
D or X; avoid in breastfeeding women
If a patient presents w/ hangover sxs (daytime sedation/falls) what should you do?
a)switch to a BZD w/ shorter duration of action
b)switch to another class of S-H
Type of BZD preferred if a patient has concomitant anxiety
long-acting BZD to maintain duration throught the next day
anterograde amnesia is especially seen w/ this BZD due to its rapid onset and short t1/2
triazolam
Time to development of tolerance with short-acting BZDs and longer-acting BZDs
-1-2wks of ocntinued use
-1-3months
pregnancy category of BZDs
D or X; avoid in breastfeeding women
These BZDs are better options for the elderly, those w/ hepatic dysfunction, and for patents w/ CYP-450 altering medications
BZDs that are conjugated (via glucoronidation)= oxazepam, temazepam, lorazepam
possible tapering option for BZDs
reduce dose 10-25% q1-2wks
if withdrawal symptoms are experienced when tapering, what should you do?
temporarily increase dose and start a less aggressive taper
BZDs indicaton
transient and short-term insomnia
Types of BZDs for sleep onset problems and sleep maintenance problems
-shorter acting agents
-longer acting agents
flurazepam dose
15-30mg
temazepam dose
15-30mg
triazolam dose
0.125-0.25mg
BZD-1 selective agents (3)
-zolpidem
-zaleplon (Sonata)
-eszopiclone (Lunesta)
BZD-1 selective agents MOA
selectively acts on a1-GABA-A receptors w/ little anxiolytic, anticonvulsant, or muscle relaxant activity
zolpidem/zolipdem CR adverse effects
1)min tolerance/rebound effects compared to BZDs (case reports)
2)drowsiness, amnesia, HA, GI complaints
zolpidem effectiveness
-comparable to BZDs for reducing sleep latency
-increases both total sleep time and efficiency
-does not disturb sleep architecture
zaleplon adverse effects
1)no significant reports of tolerance, withdrawal, or hangover (short t1/2)
2)dizziness, HA, somnolence
zaleplon effectiveness
-useful in reducing sleep latency, but not for reducing nocturnal awakenings or increasing total sleep time (due to short t1/2 and fast onset)
-does not distur sleep architecture
eszopliclone adverse effects
1)no significant reports of tolerance, withdrawal, or hangover
2)HA, somnolence, unpleasant taste
eszoplicone effectiveness
-reduces sleep latency and improves sleep maintenance
-does not disturb sleep architecture
this agent may be used when a person wakes up in the middle of the night and 4hrs of sleep may be achieved
zaleplon
zolpidem dose
5-10mg HS
zolpidem CR dose
6.25-12.5mg HS
zaleplon dose
5-20mg HS
eszopiclone dose
1-3mg HS
ramelteon MOA
agonist at both MT1 and MT2 receptors and is thought to be useful for sleep initiation
ramelteon C/I
-severe hepatic insufficiency
ramelteon adverse effects
1)no evidence for w/drawal or tolerance
2)dizziness
remaleteon drug interaction
fluvoxamine can increase serum concentrations dramatically (Cmax inc 70fold)
ramelteon effectiveness
a)useful for pts w/ prolonged sleep latencies
b)long-term and is not controlled
c)substance abusers w/ insomnia
this agents use is limited to transient insomnia and it may cause hyperbilirubinemia
chloral hydrate
these agents have a higher risk of CNS and respiratory depression as compared to BZDs w/o offering significant advantages
barbiturates
these agents are not recommended unless patient has insomnia and cannot take a BZD
antidepressants
these agents may be useful in patients w/ depression or neuropathic pain as co-morbidities
tricyclic antidepressants
TCA MOA
inhibit reuptake of NE and 5-HT
TCA adverse effects (4)
1)hangover
2)falls in elderly
3)anticholinergic
4)cardiac conduction abnormalities (dangerous in pts w/ hx of suicide attempts)
this agent has been shown to increase total sleep in pts w/ depression and it has a very low propensity for drug abuse
trazodone
trazodone MOA
SSRI w/ mixed agonist/antagonist effects at serotonergic receptors
trazodone adverse effects (3)
1)serotonin syndrome
2)orthostatic effects from alpha adrenergic blockade
3)priapism
a sedating SSRI
paroxetine (sertraline, fluoxetine, etc can cause insomnia)
agent that may decrease sleep latency, but results in fragmented, unfruitful sleep
ethanol
herbal melatonin should be used cautiously in what kind of patients (3)
1)vascular d/o (can cause vasoconstriction)
2)immunosuppressive therapy (enhance immune function)
3)pregnant/lactating females
herbal melatonin is most commonly used for?
children or jet lag
valerian root adverse effects (4)
1)HA
2)cardiac disturbances
3)uterine contractions (no to pregnant pts)
4)hepatotoxicity
pharmacological therapy for patients with circadian rhythm sleep d/o
a)zaleplon, zolpidem (preferred to to lack of hangover effects)
b)short-acting BZDs
c)ramelteon
d)melatonin (herbal)
pharmacological therapy for patients with breathing-related sleep d/o and its general indication
modafinil (Provigil) (indicated for use in pts w/ daytime sleepiness despite treatment w/ CPAP)
modafinil MOA
CNS stimulant which lacks many adverse effects of traditional stimulants (tachycardia, HTN)
modafinil adverse effects (3)
1)HA
2)nausea
3)nervousness
treatment of breathing-related sleep d/o with these agents may be lethal
CNS depressants (BZD, opiods, etc)
standard pharmacological treatment in pts w/ narcolepsy who have excessive daytime sleepiness (EDS)
modafanil
pharmacological treatment in pts w/ narcolepsy who have cataplexy (sudden loss of muscle tone)(3)
-TCAs
-fluoxetine
-sodium oxybate (GHB)
this agent for cateplexy is considered 2nd line eventhough it appears to be more effective in treating cataplexy than other agents
sodium oxybate
sodium oxybate MOA
binds to GABA-B receptors and sodium oxybate specific receptors and has mamy effects on other neurotransmitters
sodium oxybate effectiveness
-improves sleep architecture while reducing EDS, sleep paralysis, cataplexy, and hypnagogic hallucinations
pharmacological therapy for patients w/ restless leg syndrome (RLS)
a)mild=BZD may be 1st line
b)opiates (concerns w/ tolerance)
c)dopamine agonists (ropinirole, pramipexole, pergolide)=titrate slow to avoid nausea
d)gabapentin
Use of these agents in RLS may exacerbate insomnia
dopamine agonists