Pharmacotherapy of Insomnia Flashcards
Zolpidem and Zaleplon have the ______ durations of action (6-8 hours) and half-lives of available agents (zolpidem: 2-2.5 hrs; zaleplon: 1 hr). Eszopiclone is Structurally different from zolpidem or zaleplon with _____ t1/2
Shortest,
longer (6Hrs)
name the 3 benzodiazapines used in in treatment of insomnia
Triazolam
Temazepam
Flurazepam
which drug Can accumulate in elderly due to impaired hepatic clearance leading to daytime sedation (“hangover”)
Flurazepam
which drug can cause rebound insomnia next day due to rapid elimination
Triazolam
what are the common side effects of Z drugs, (zolpidem, zaleplon, Eszopiclone)
drowsiness, amnesia, dizziness, headache, GI complaints
what drugs can cause sleep-walking, sleep-eating, and sleep-driving and without conscious awareness
Z drugs, (zolpidem, zaleplon, Eszopiclone)
how do Z drugs (zolpidem,zaleplon,eszopiclone) induce sleeps
Produce sleep by facilitating the action of GABA at the GABAA receptor-chloride channel complex.
(Non-Benzodiazepine Benzodiazepine Receptor Agonists)
what drug is effective for reducing sleep latency and nocturnal awakenings with an increase in total sleep time and efficiency
Zolpidem (t1/2: 2-2.5 hrs):
what drug is Probably best suited for use as a sleep aid for middle-of-the-night awakenings.
Zaleplon (t1/2: 1 hr)
What drug is safest for long term use with little or no suggestion for development of tolerance, dependence, or abuse in the treatment of Insomnia?
Eszopiclone (t1/2: 6 hrs)
what is the mechanism of action for Trazodone
Complex effects on 5HT neurons, including weak but specific inhibition of reuptake and both agonist and antagonist receptor actions. [decrease in REM sleep, increase / no change in SWS]
what are the Adverse Drug Reactions of trazodone
Oversedation and orthostasis (Orthostatic hypotension
what are Amitriptyline, Doxepin, Nortriptyline
Tricyclic Antidepressants (TCADs)
what is the Mechanism of Action for Tricyclic Antidepressants (TCADs) like Amitriptyline, Doxepin, Nortriptyline
Block of reuptake of serotonin and/or norepinephrine, probably also a contribution from antagonist action at histamine and muscarinic-cholinergic receptors.
what taking Antidepressants (TCADs) for insomnia you see a _____ in REM sleep, and a ______ in slow wave sleep
Decrease,
Increase
which populations are candidates for Sedating antidepressants?
patients who shouldn’t receive benzodiazepines, patients with depression, pain, or a risk of substance abuse.
what is the Mechanism of Action for Ramelteon
Agonist at melatonin MT1 (induce sleepiness) and MT2 receptors (regulation of circadian rhythms) in suprachiasmatic nucleus of hypothalamus. Decreases mean latency to sleep
Ramelteon is used in Treatment of ________
chronic or transient insomnia characterized by difficulty with sleep onset
what is the Mechanism of Action for suvorexant?: .
Antagonist at orexin receptors (OX1 and OX2)
Orexins are synthesized in neurons in the ________ that innervate all of the arousal systems and the cerebral cortex as well.
lateral hypothalamus
orexin neurons play an essential role in sustaining wakefulness across the day. Orexin receptor antagonists reduce _______and increase the amounts of __________
sleep latency,
REM and NREM sleep.
what is the Most common side effect of suvorexant?
Next-day Somnolence (alternatively “sleepiness” or “drowsiness”)
when should suvorexant be considered for treatment
best considered as option when more established drugs have failed. (expensive)
_______ is an Old drug (1800’s), that may be an effective hypnotic for a few nights for transient insomnia. Continued use often leads to physical dependence.
Chloral Hydrate (Noctec)
_________ May be effective in short-term treatment of mild insomnia. Heavily advertised, but NOT recommended for chronic use in adults.
Diphenhydramine & Doxylamine
