Sleep Disorders Flashcards
Benzodiazepine MOA, SE, and CI
MOA: selectively act of polysynaptic CNS neuronal pathways
-Enhance GABA (inhibitory) effects - block arousal
SE: Drowsiness, impaired motor function, physical dependency with prolonged use
CI: Acute narrow-angle glaucoma, Pregnancy (X), Lactation
DI: ETOH caution, OCP decrease clearance
Short Term Benzodiazepines
Triazolam (Halcion)
For difficulties falling asleep
Intermediate-acting Benzodiazepines
Temazepam (Restoril)
Estazolam (ProSam)
Used for trouble maintaining sleep
Long-acting Benzodiazepines
Flurazepam (Dalmane)
Quazepam (Doral)
Rapid onset and last longer
Used for help falling asleep and maintaining sleep
Benzodiazepine Receptor Agonists (BRA)
Help eliminate benzo use
Shorter 1/2 life - less groggy
All are Prego C and only CI is hypersensitivity
Eszopiclone (Lunesta)
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)
MOA: Interacts with GABA receptors near Benzo receptors
For sleep maintenance
Lower dose in elderly; 1/2 life 5-7 hours; peak serum in 1 hour
SE: HA, dizziness, dry mouth, unpleasant taste in mouth
Zolpidem (Ambien)
MOA: modulates GABA receptors to suppress neurons - relaxation and sedations
1st line for trouble falling asleep - Have to take w/ 6-8 hrs before wakeup
Lower dose w/ elderly and women; 1/2 2.5 hours; 30 min response
SE: Morning drowsiness, hangover, HA
Zaleplon (Sonata)
MAO: Interacts with GABA-BZ omega 1 receptor
2nd line for difficulty falling asleep - 5 hours of sleep needed
also mild anticonvulsant activity
Onset and 1/2 life w/in 1 hour
SE: Back/chest pain, migraine, constipation
Antihistamine
Most common OTC sleep inducing agent - Benadryl
CNS depressant, non-addictive
SE: excessive daytime drowsiness (long 1/2 life), impaired psychomotor function, anticholinergic SE
Pregnancy B
Antidepressants
Used off-label or with anxiety/pain subcomponent to insomnia
Only Doxepin FDA labelled for insomnia
Doxepin (Silenor)
Trazodone
Amitriptyline (Elavil)
All have BBW for suicidal thoughts
All are pregnancy C
Doxepin (Silenor)
Only antidepressant labelled for use in insomnia
Used to maintain sleep
MOA: Increases serotonin and norepinephrine concentration in the synapse
Cannot take w/in 3 hours of eating, really bad w/ concomitant constipation
CI: glaucoma, urinary retention
Trazodone
Serotonin antagonist and reuptake inhibitor
MOA: changes serotonin receptor and inhibits serotonin reuptake
CI: MAOI, linezolid, IV methylene blue
Amitriptyline (Elavil)
Commonly used for insomnia
MOA: Increases synaptic concentrations of serotonin and/or norepinephrine
Half-life: 13-36 hours
CI: History of MI, MAOI
Melatonin Agonist
Ramelteon (Rozerem)
Good for sleep onset insomnia
MOA: selective agonist of MT1 and MT@ within suprachiasmatic nucleus
Take w/in 30 minutes, half-life 1-2 hours
CIL Fluvoxamine (Luvox) - SSRI
Orexin Receptor Antagonist
Suvorexant (Belsomra)
Used for sleep onset or maintenance - suppresses wake drive
MOA: block binding to wake-promoting neuropeptides (Orexin A&B) to receptors OZ1R and OX2R
Need 7 hours of sleep, take 30 minutes before bed
CI: Narcolepsy