pharm Flashcards
medications contributing to insomnia
Antidepressants
Stimulants
Antihypertensives
Sedatives
Decongestants and antihistamines Analgesics
Herbal supplements
Substances of abuse
insomnia and comorbidity (i.e. GI, MSK, pscyh)
75%
sedative vs hypnotic
Sedative – A drug that reduces excitement and calms the patient. Also called anxiolytics. They do not induce sleep.
Hypnotic – A drug that results in drowsiness that promotes sleep.
benzidiapenes are what receptor agonist
GABA-A receptor agonist
what do benzodiazepines allow for in GABA channel
Chloride ion move in and enhance GABA (inhibition)
benzodiazepine effects
sedative and hypnotic
use of benzodiazepines
short term or intermittent
only long term is severe or comorbid insomnia
what not to combine benzodiapenes qith
other benzos
and alcohol or CNS depressants
most addictive and quickest onset of action benzodiazepene
high risk of abuse, dependence and rebound insomnia
triazolam
which benzodiazepen has a very long half life and should “never use”
flurazepam and nitrazepam
best benzodiaepen for insomnia according to health canada
temezapam
adverse effects of benzodiazepines
-ataxia, dizzy, withdraw, memory, abuse, next day impairment
-only use if 7-8 hours before awakening
-wait 12 hours before driving
how long can u use benzos for
24 weeks
when discontinue benzos what happens
rebound insomnia
gradual tapering helps
BENZODIAZEPINE RECEPTOR AGONISTS (Z-DRUGS) work on what
allosteric modulators of GABA-A receptors
presence of GABA does not facilitate action
enhances inhibition
Benzo receptor agonists (Z-DRUGS) vs benzodiapenzes
z drugs are allosteric modulator of GABA-A
benzos are GABA-A agonist
preferred drugs for insomnia
z-drugs
z-drugs vs benzo
similar effects on sleep
but z-drugs have: fewer adverse effects, less muscle relaxant affects, dont worsen sleep apnea and dont accumulate (less rebound on withdrawal)
z drug
zopiclone
adverse effects of z drugs
bitter/metalic taste, dry mouth, dizzy
sleep behaviours: night eating, somnambulism (sleepwalk)
impair next day activities
have is plan to sleep 7-8 hours and wait >12 hours to drive
what not to combine z drugs with
alcohol or CNS depressants
Increased risk of complex sleep behaviours in combination with other CNS-active drugs
orexin function
orexin 1 and 2 promote arousal/wakefulness
dual orexin antagonist example
lemborexant
lemborexant/ dual orexin antagonist function
reduce wakefulness and unwanted transitions between wake and sleep
for: sleep onset and sleep maintenance isnomnia
lemborexant side benefits
no withdrawal or rebound insomnia
can use for 12 months
minimal next day impairment
minimal abuse potential
lemborexant adverse effects
somnolence (drowsy), night eating, somnambulism (sleep walk)
less common: sleep paralysis, hallucinations, cataplexy
impair next day function, take if sleep fro 7-8 hours and not driving for 9 hours
cont combine with CNS depressant
contraindications for lemborexant
narcolepsy (bc possibly orexin dependent)
tricyclic antidepressant exmaple
doxepin
what receptor do TCAs work on
histamine H1 reeceptors
TCAs fro insomnia
use at low doses
high doses are for anxiety and depression
histamine receeptosr
agonist= wakeful
antagonist= sleep
health Canada indication for doxepin (TCA)
sleep-maintenance
how long can use doxepin fro
3 months
doxepin for what patient group with insomnia
elderly
bc no rebound insomnia, dependence or next day impairment
doxepin (TCA) adverse effects
since for insomnia is low dose usually no adverse
somnolence, sedation, nausea
dont combine w alcohol or CNS depressants
take within 3 hours of a meal to minimize drowsiness next day
off label agent for insomnis
sedation
- treat underlying comborditiy
centralized pain (fibromyalgia) –> anticonvulsants (i.e. gabapentin)
allergic conditions (ecemza, allergy) –> antihistamiens
mood disorders –> sedating antidepressants
insomnia in kids first line treatment
non-pharm
-
insomnia meds and kids
Although often used, over-the-counter antihistamine use is not recommended due to the risk of rapid tolerance, next-day sedation, cognitive impairment, and paradoxical reaction
insomnia and eldery
*drug interactions
-want to limit sedation, cognitive impairment bc of falls
2 best sleep meds for insomnia in elderly
Low-dose doxepin for sleep-maintenance
Lemborexant has demonstrated a favourable safety and efficacy profile in the elderly up to 6 months of use
insomnia and pregnancy
sleep apnea and restless leg are bad
non-pharm 1st
best and worst sleep medications for pregnancy
Zopiclone does not appear to be teratogenic and may be a reasonable choice if clinically justified
Benzodiazepines should be avoided, particularly in the first trimester, due to an increased risk of oral cleft; they may also cause neonatal withdrawal symptoms when used closer to term
A patient complains of a bitter taste in their mouth and dizziness following a recent prescription to help them sleep. Which of the following was most likely prescribed?
A. Doxepin
B. Lemborexant
C. Temazepam
D. Zopiclone
D. zopiclone