Pharmacotherapy of Insomnia

Question 1

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

Answer 1

Shortest,

longer (6Hrs)

Question 2

name the 3 benzodiazapines used in in treatment of insomnia

Answer 2

Triazolam
Temazepam
Flurazepam

Question 3

which drug Can accumulate in elderly due to impaired hepatic clearance leading to daytime sedation (“hangover”)

Answer 3

Flurazepam

Question 4

which drug can cause rebound insomnia next day due to rapid elimination

Answer 4

Triazolam

Question 5

what are the common side effects of Z drugs, (zolpidem, zaleplon, Eszopiclone)

Answer 5

drowsiness, 
amnesia, 
dizziness, 
headache, 
GI complaints

Question 6

what drugs can cause sleep-walking, sleep-eating, and sleep-driving and without conscious awareness

Answer 6

Z drugs, (zolpidem, zaleplon, Eszopiclone)

Question 7

how do Z drugs (zolpidem,zaleplon,eszopiclone) induce sleeps

Answer 7

Produce sleep by facilitating the action of GABA at the GABAA receptor-chloride channel complex.

(Non-Benzodiazepine Benzodiazepine Receptor Agonists)

Question 8

what drug is effective for reducing sleep latency and nocturnal awakenings with an increase in total sleep time and efficiency

Answer 8

Zolpidem (t1/2: 2-2.5 hrs):

Question 9

what drug is Probably best suited for use as a sleep aid for middle-of-the-night awakenings.

Answer 9

Zaleplon (t1/2: 1 hr)

Question 10

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?

Answer 10

Eszopiclone (t1/2: 6 hrs)

Question 11

what is the mechanism of action for Trazodone

Answer 11

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]

Question 12

what are the Adverse Drug Reactions of trazodone

Answer 12

Oversedation and orthostasis (Orthostatic hypotension

Question 13

what are Amitriptyline, Doxepin, Nortriptyline

Answer 13

Tricyclic Antidepressants (TCADs)

Question 14

what is the Mechanism of Action for Tricyclic Antidepressants (TCADs) like Amitriptyline, Doxepin, Nortriptyline

Answer 14

Block of reuptake of serotonin and/or norepinephrine, probably also a contribution from antagonist action at histamine and muscarinic-cholinergic receptors.

Question 15

what taking Antidepressants (TCADs) for insomnia you see a _____ in REM sleep, and a ______ in slow wave sleep

Answer 15

Decrease,

Increase

Question 16

which populations are candidates for Sedating antidepressants?

Answer 16

patients who shouldn’t receive benzodiazepines, patients with depression, pain, or a risk of substance abuse.

Question 17

what is the Mechanism of Action for Ramelteon

Answer 17

Agonist at melatonin MT1 (induce sleepiness) and MT2 receptors (regulation of circadian rhythms) in suprachiasmatic nucleus of hypothalamus. Decreases mean latency to sleep

Question 18

Ramelteon is used in Treatment of ________

Answer 18

chronic or transient insomnia characterized by difficulty with sleep onset

Question 19

what is the Mechanism of Action for suvorexant?: .

Answer 19

Antagonist at orexin receptors (OX1 and OX2)

Question 20

Orexins are synthesized in neurons in the ________ that innervate all of the arousal systems and the cerebral cortex as well.

Answer 20

lateral hypothalamus

Question 21

orexin neurons play an essential role in sustaining wakefulness across the day. Orexin receptor antagonists reduce _______and increase the amounts of __________

Answer 21

sleep latency,

REM and NREM sleep.

Question 22

what is the Most common side effect of suvorexant?

Answer 22

Next-day Somnolence (alternatively “sleepiness” or “drowsiness”)

Question 23

when should suvorexant be considered for treatment

Answer 23

best considered as option when more established drugs have failed. (expensive)

Question 24

_______ 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.

Answer 24

Chloral Hydrate (Noctec)

Question 25

_________ May be effective in short-term treatment of mild insomnia. Heavily advertised, but NOT recommended for chronic use in adults.

Answer 25

Diphenhydramine & Doxylamine