Sleep

Question 1

Overview

Answer 1

Antihistamines: Diphenhydramine (Benadryl) and doxylamine

Sedating antidepressants:
Doxepin, amitriptyline, nortriptyline, Trazodone

Question 2

Anxiolytics/ Sedative- Hypnotics overview

Answer 2

1. Benzodiazepines : alprazolam, diazepam, lorazepam, clonazepam, oxazepam, temazepam
   if you have to put elderly on benzos= L.O.T= Lorazepam, oxazepam, temazepam
2. Barbiturates: phenobarbitol, thiopentol, pentobarbitol
3. OTHERS: BUSPIRONE, RAMELTEON, HYDROXYZINE
   4.NONBENZODIAZEPINE BENZODIAZEPINE AGONIST (NBBRA)= “Z” DRUGS: ZALEPLON (sonata), ZOLPIDEM (Ambien), ESZOPICLONE (Lunesta

Question 3

Anxiolytics/Sedative-hypnotics kinetics

Answer 3

Barbiturates and benzos-> relieve anxiety @ low doses and lead to sedation @ high doses-> some degree of anesthesia-> higher doses-> death
Most used for sleep

Question 4

Hydroxyzine (Vistaril)

Answer 4

used in primary care
2nd line agent for anxiety due to lack of efficacy for comorbid disorders
Class: Histamine (H1) antagonist
MOA: complex, competes w/ histamine for H1 receptor sites on effector cells in GI tract, bv, respiratory tract; activity on neurons may be responsible for anxiolytic effects
can cause drowsiness

Question 5

“Z” drugs

Answer 5

MC used
Zaleplon (Sonata), Zolpidem (ambien), eszopiclone (Lunesta)
MOA: benzodiazepine receptor agonists
shorten the time it takes to fall asleep and used for short term tx of insomnia

Cautions include:
ANAPHYLAXIS
FACIAL ANGIOEDEMA
COMPLEX SLEEP BEHAVIORS (sleep driving, phone calls, sleep eating)

Extra:
time to onset, half life, duration of action vary btwn drugs
Zaleplon (Sonata)= short half life used for when pts awaken in middle of the night
Generally assoc w/ less physical withdrawal, tolerance, rebound insomnia when compared to BZDs

Question 6

Ramelteon (Rozerem)

Answer 6

MOA: binds to two types of melatonin receptors in the hypothalamus to help regulate sleep and circadian rhythms-> to tx insomnia
not controlled substance= good for addicts
Effective in tx sleep onset difficulties in pts w/ obstructive sleep apnea and COPD

Question 7

Dual Orexin Receptor Antagonists (DORA)

Answer 7

Suvorexant (Belsomra) and Lemborexant (Dayvigo)
MOA: Orexin 1 and 2 receptor antagonists (orexin sustains wakefulness)
Suv helps pt fall asleep 5-10 min faster and sleep 15-25 min longer

counsel pts: sleep paralysis, cataplexy, narcolepsy-like symptoms

Caution in pt w/ depression:
CAN WORSEN MOOD AND TRIGGER SUICIDE IN DOSE DEPENDENT MANNER

Question 8

Misc.

Answer 8

Valerian: herbal sleep remedy-> American academy of sleep med-> lack of high quality evidence to support use

Melatonin: weak evidence supporting its use for tx of insomnia

Question 9

Non pharm tx for insomnia

Answer 9

Stimulus control procedures:
-regular time to wakeup and sleep even on weekends
-sleep only as much as necessary to feel rested
-go to bed only when sleepy-> avoid long periods of wakefulness in bed-> bed only for sleep or intimacy-> not reading or tv in bed
-avoid trying to force sleep-> no sleep w.in 20-30 min-> leave bed and perform relaxing activity until drowsy
-avoid blue spectrum light from tv, smart phones, tablets, mobile devices
-avoid daytime naps
-schedule worry time during day-> do not take your troubles to bed

Sleep hygiene recommendations:
-exercise routinely-> not close to bedtime bc can increase wakefulness
-create comfortable sleep environ by avoiding temp extremes, loud noises, illuminated clocks in bedroom
-dc or reduce the use of alcohol, caffeine, nicotine
-avoid drinking large quantities of liquids in evening to prevent nighttime trips to the restroom
-do something relaxing and enjoyable before bedtime