Sleep Agents Flashcards
What are the restorative purposes of sleep?
Energy conservation, immune function, body repair, glymphatic system
What is the information processing purposes of sleep?
Development, neurogenesis, memory consolidation, pruning
Stage one also called the drowsy period is
so light most people when awoken from this stage will say that they were not asleep
Stage two has
sleep spindles (periodic bursts of activity resulting from interactions between the thalamus and the cortex
Stage 3 nd 4 are called slow weave sleep and
are the deepest stages of sleep characterized by the development of delta waves
REM sleep is
remarkably like that of the awake state but the body or at least the major muscles are paralyzed
Non-REM sleep is characterized by
limited eye movement and a decrease in muscle tone and heart rate, metabolic rate and body temp decrease
REM sleep is characterized by
rapid, darting movements of the eyes along with paralysis of most major muscle groups. heart and respirations increase to almost the level found when awake.
REM latency
the time to the first occurrence of REM
The lose of the ability to induce muscle paralysis
REM sleep behavior disorder
Describe non-REM dreams
thoughts or person solving problems
REM dreams
illogic, bizarre, and even hallucinatory
Define sleep walking
Occurs during the first stage 4 non REM period of the night. The person will have open eyes, avoid obstacles, and have cognition clouded with no memory of the event. Best practice is to gently guide the sleepwalker back to bed.
Define Night terrors
Extreme terror and an inability to be awakened. Usually in children between ages 4 and 7 and develops in the deep stages of non-REM sleep.
Where is the Suprachiasmatic Nucleus located?
anterior hyupothalamus
What does the Suprachiasmatic Nucleus do?
It regulates circadian rhythms using solar cues from the retina
Without solar cue inputs how long is the Suprachiasmatic Nucleus cycle?
26 hours
Why are CLOCK BMAL1, PER, and CRY significant to sleep cycle?
They are believed to drive the 24 hour cycling of SCN
This specific group of neurons project to the thalamus and are responsible for awake and REM
Cholinergic
These four neurons project to the hypothalamus and cerebral cortex and are active during awake cycles.
Noradrenergic, dopaminergic, serotonergic, and histaminergic
This neurotransmitter is a key one in regulating wakefulness and is the ultimate target of many wake promoting drugs and sleep promoting drugs.
histamine
Which receptor is best known as the target of antihistamines
postysnaptic histamine 1 (H1) receptor
Stimulating the H1 receptor is likely to cause
wakefulness, normal alertness, and procognitive actions
Blocking H1 receptors is likely to cause
sedation, drowsiness or sleep
This receptor is best known for its action in gastric acid secretion and is the target of several anti-ulcer drugs and also exists in the brain
Histamine 2 (H2) receptors
This histamine receptor is still under research as a way of blocking this receptor allowing the release of histamine to act at H1 receptors
H3
The sleep/wake switch is a set of circuits located in the
hypothalamus
The on switch is known as the wake promoter and is localized within the
tuberomammillary nucleus (TMN)
The off switch is known as the sleep promoter and is localized within the
ventrolateral preoptic (VLPO) nucleus of the hypothalamus
This key neurotransmitter in the sleep/wake switch is from the TMN
histamine
This key neurotransmitter in the sleep/wake switch is from the VLPO
GABA
How does the neurotransmitter GABA affect sleep/wake cycles?
It inhibits wakefulness
What two neurons act as regulators of the sleep/wake switch
Orexin and melatonin
What neuron do those with narcolepsy have less of?
Orexin
What is the diurnal variation of depression?
worse in the morning
What is one of the most common complaints among patients with mood disorders?
Insomnia
How does effective treatment affect insomnia in those with a mood disorder
insomnia resolves
An effective, although short-lived antidepressant is
sleep deprivation
What gland secretes melatonin and is called both a clock and a calendar?
melatonin
Based on recent research on melatonin in those with SAD what does it suggest as the reason?
neural circuits that mediate season change may be impaired
In those with bipolar a lack of sleep can precede
a manic episode
Sedative-Hypnotic drugs include benzodiazepines, barbiturates and Z drugs all of which act at
GABA A receptors to enhance the action of GABA
When are benzodiazepines used for insomnia
second line hypnotics
Which benzodiazepines are utilized for insomnia
flurazepam, quazepam, triazolam, estazolam, temazepam
Why are barbiturates rarely used to treat insomnia now?
tolerance, dependence, high abuse potential, multiple drug interactions, fatal with an overdose
What barbiturates are approved to treat insomnia?
thiopental, secobarbital, phenobarbital
Barbiturates interact poorly with the antifungal
griseofulvin
Barbiturates interact poorly with the antibiotics
rifampicin and rifabutin
Barbiturates interact poorly with antileptics such as
carbamazepine, eslicarbazepine, phenytoin, phenobarbital, primidone, oxcarbazepine, topiramate
What are the signs of acute toxicity in barbiturates?
respiratory depression, coma, pinpoint pupils
How do you treat Barbiturate toxicity?
maintain body heat, support blood pressure, activated charcoal to remove barbiturate from the body, maintain adequate oxygen
What are the three Z drugs to treat insomnia?
Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)
What are the main side effects of Zolpidem (Ambien)
daytime drowsiness and dizziness
What are the main side effects of Eszopiclone (Lunesta)
bitter aftertaste, headache, somnolence, dizziness, and dry mouth
What are the main side effects of Zaleplon (Sonata)
headaches, nausea, drowsiness, dizziness, myalgia, and abdominal pain
Which antidepressant is used at lower doses as a very effective hypnotic?
Trazadone
What are the OTC antihistamines commonly used to help with insomnia?
Diphenhydramine and Doxylamine
What are the adverse effects of antihistamines for insomonia?
less effective, tolerance develops quickly, daytime drowsiness and anticholinergic effects
For those who suffer from initial insomnia and not sleep maintenance what is a good complementary therapy as well as prescription drug?
Melatonin OTC
Ramelteon (Rozerem) prescription
What is the first line treatment in those who have insomnia due to restless leg syndrome?
Dopamine agonists such as ropinirole and pramipexole
What is the second line treatment in those who have insomnia due to restless leg syndrome?
alpha-2-delta ligands such as gabapentin or pregabalin
What is the only Orexin Antagonist that is FDA approved for insomnia in adults?
Lemborexant (Dayvigo)
Modafinil and Armodafinil are both
hypersomnia and wake promoting agents
What stimulants are there that are wake-promoting agents?
Methylphenidate (Ritalin, Concerta ER), Amphetamine, Caffeine, Gamma-hyroxybutyrate (Xyrem)
