Sleep Aids Flashcards
What class of drugs are used to treat insomnia in the short-term?
Sleep aids
What is the name for the subjective complaint of difficulty falling asleep, staying asleep, and/or experiencing restorative sleep that results in daytime impairment?
Insomnia
What are the four main classes of FDA-approved medications for the treatment of insomnia?
Benzodiazepine receptor agonists
Non-benzodiazepine receptor agonist
Tricyclic antidepressant
Melatonin receptor agonists
What about the use of over-the-counter products such as antihistamines, Valerian, and melatonin and off label use of antidepressants, antipsychotics, and anticonvulsant drugs for the treatment of insomnia?
There is limited data to support the use of these medications in insomnia
What is the mechanism of action for benzodiazepine receptor agonists?
They nonselectively bind to the alpha subunits on the gamma-aminobutyric acid type A (GABA–A) receptor complex
This results in the enhancement of GABAs inhibitory effects
Similar to benzodiazepine receptor agonists, what is the mechanism of action for non-benzodiazepine receptor agonists?
They also bind to the GABA–A receptor, but have a higher selectivity for alpha receptor subunits
What is the mechanism of action for zolpidem and zaleplon?
They also bind to the GABA–A receptor, but have a greater affinity for the alpha-1 subtype
What is the mechanism of action for eszipclone?
They also bind to the GABA–A receptor, but has a greater affinity for the alpha-2 and 3 subtypes
What advantage does the selectivity demonstrated by these medications result in?
They end up being more sedation-specific, with fewer adverse effects
Melatonin is an endogenous hormone released from which gland? What is it released in response to? From what nucleus?
The pineal gland
In response to light and dark signals
From the suprachiasmatic nucleus (SCN)
What are the three melatonin receptors in the body?
MT1, MT2, and MT3
Which two melatonin receptors regulate the wake-sleep cycle?
MT1 and MT2
What is the mechanism of action (receptor binding) for the medication Ramelteon? What endogenous hormone does it mimic?
It is a melatonin receptor agonist that binds to MT1 and MT2 receptors and;
Mimics melatonin’s sleep-promoting properties
At low doses, which tricyclic antidepressant is a selective histamine-1 antagonist that produces sedating effects?
Doxepin
What happens to doxepin, with regard to sedating effects, at higher doses? Which 3 effects does it show at higher doses?
It loses its sedating effects at higher doses
At higher doses it becomes anti-cholinergic, anti-serotonergic, and anti-adrenergic
When appropriate, what should be utilized as an initial Non-pharmacologic intervention, and is considered effective, for the management of insomnia?
Psychological and behavioral therapies
Under what 3 conditions is pharmacologic intervention indicated for insomnia?
When a patient prefers the use of a medication
When immediate symptom relief is required
When the sleep disturbance produces significant distress or impairment
Whenever possible, what should the therapeutic approach to insomnia be?
Medications should be utilized short-term in combination with non-pharmacologic strategies whenever possible
The number 3 most common adverse effects of benzodiazepine receptor agonists are?
Drowsiness, dizziness, and headache
What common adverse effect is associated with benzodiazepines with long durations of action?
Residual daytime sedation
If a benzodiazepine with a long duration of action is causing residual daytime sedation, what should be done?
Switch to a medication with an intermediate or short duration of action; this will decrease daytime drowsiness
Which adverse effect of benzodiazepine receptor agonists is considered to be dose-dependent?
What should be done if a patient complains of this specific adverse effect?
Anterograde amnesia
The dose should be lowered and the patient instructed to take the medication only at bedtime
Benzodiazepines with short durations of action tend to cause what specific type of adverse effect?
Rebound insomnia
What is rebound insomnia?
This refers to a rapid return of difficulty with sleep initiation and/or maintenance
It may be worse than before treatment
How do you prevent rebound insomnia?
Gradually taper the benzodiazepine by 10% or less at 5-to-7 day intervals
Can benzodiazepine receptor agonists cause withdrawal symptoms on discontinuation?
Yes
