Sleep Wake- SG Flashcards
Which location of the brain and which neurotransmitter are associated w/ sleep-wake disorders?
Cannot be localized to area of brain or neurotransmitter
Numerous neurotransmitters mediate NREM sleep including ____ and _____.
- y-aminobutyric acid (GABA)
- adenosine
REM sleep is turned on by ________.
Cholinergic cells
REM sleep turned off by _________.
Noradrengeric cells
What 2 things facilitate arousal and wakefullness?
- Ascending reticular activating system
- Posterior hypothalamus
An increase in ____ has an alerting effect
A decrease in ____ promotes sleepiness
Dopamine
- Neurochemicals involved in wakefullness include _______ and _______ in the cortex
and
- ______ and ______ such as substance P and corticotropin releasing factor in the hypothalamus.
- norepinephrine & acetylcholine
- histamine & neuropeptides
- Which age group has difficulty falling asleep?
- Which 2 age groups have middle of the night awakening or early morning awakening?
- 40% of individuals w/ insomnia also have concurrent ____ _____. along w/ anxiety, depression, or substance abuse.
- Young adults
- Middle aged and elderly adults
- Psychiatric disorder
Significant percentrage of those w/ insomnia use _____ or ____ to self treat.
- Nonprescription drugs
- Alcohol
Complaint of transient / short term insomnia is usually due to what?
Recent stressors
- separation
- death in family
- job change
- college exams
Chronic insomnia is frequently comorbid w/ ____ or ______.
- psychiatric or medication conditions
3 common etiologies of insomnia
- Situational (work/financial stress)
- Medical (cardiovascular, respiratory, endocrine)
- Pscyhiatric (mood disorders, anxiety disorders, substance abuse)
What drugs interfere w/ REM sleep?
- Anticonvulsants
- Central adrengergic blockers
- Diuretics
- Selective serotonin reuptake inhibitors
- Steroids
- Stimulants
What is the goal of drug therapy for insomnia?
Lowest possible dose for shortest possible time period
2 types of medications for insomnia
Sedation & Hypnotic
- Effective sedative (anxiolytic) agent should reduce anxiety and exert a calming effect
Sedation meds for insomnia
Hypnotic drug should produce drowsiness and encourage the onset & maintenance of a state of sleep
Hypnotic meds for insomnia
3 clinical uses of Sedative-Hypnotics
- Relief of anxiety
- Insomnia
- For control of ethanol or other sedative hypnotic withdrawal states
Which sedative-hypnotics lead to coma/death?
Barbiturates / alcohol
Which sedative-hypnoticc drugs have a ceiling effect and does not work for surgical anesthesia
(no coma/death)
Benzodiazepines
Absorption/Distribution of which drug?
- lipid soluble (crosses BBB)
- absorbed well from GI tract
- good distribution to brain
Sedative-Hypnotic drugs for Insomnia
Metabolism/Excretion of which drug?
- Metabolized before elimination from body
- mainly by hepatic enzymes
- active and inactive metabolites
Sedative-Hypnotic Drugs for Insomnia
What is the most commonly used tx for insomnia?
Benzodiazepines
What are the 3 “newer” non-benzodiazepines GABA agonists which possess only sedative properties?
- Eszopiclone
- Zaleplon
- Zolpidem
What type of drugs are these?
- Estazolam
- Flurazepam
- Quazepam
- Temazepam
- Triazolam
Benzodiazepines
(most common used tx for insomnia)
Traditional benzodiazepines have which 4 properties?
- Sedative
- Anxiolytic
- Muscle relaxant
- Anticonvulsant properties
Which benzodiazepine is a “true hypnotic?”
Flurazepam
Which benzodiazepine can lead to homicidal ideation?
Triazolam
The receptors for benzodiazepines are located in which 3 areas of the brain?
- Thalamus
- Limbic structures
- Cerebral cortex
- Binding of benzodiazepines facilitates the inhibitory actions of _____.
- What does BZDRA stand for?
- GABA
- Benzodiazepine receptor agonists
What should you prescribe for:
- Acute anxiety states
- Panic attacks
- Generalized anxiety disorder
- Insomnia
- Skeletal muscle relaxation
- Seizure disorders
Benzodiazepines
PK of which drug?
- Hepatic metabolism
- Active metabolites
- Additive CNS depression w/ many drugs
- Half lives: 2-4 hrs
Benzodiazepines
3 toxicities of Benzodiazepines
- Extension of CNS depressant actions
- Tolerance
- Dependence liability
Which benzo was the 1st benzo on the market and was drug of choice for alcohol withdrawal?
Chlordiazepoxide
Which benzo is the “active metabolite?”
Oxazepam
Which benzo has active metabolites and erratic bioavailability from IM injection
Diazepam
Which benzo has active metabolites w/ long half lives?
Flurazepam
Which 3 benzos have no active metabolites?
- Lorazepam
- Oxazepam
- Zolpidem
BZDRA adverse drug events
High doses w/ long/intermediate elimination half lives have a greater potential to:
- produce daytime sedation
- psychomotor incoordination
- cognitive deficits
- half lives are shortened or prolonged in older patients?
Prolonged
- Most traditional benzodiazepines maintain hypnotic efficacy for ___ month.
- Tolerance can develop w/ time. How many days?
- 1
- 10-14 days
2 effects from BZDRA ADEs
- Anterograde amnesia
- Rebound insomnia
- What has been reported the most w/ use of BZDRAs?
- And is more likely to occur w/ short acting agents
Anterograde amnesia
(impairment of memory and recall of events occurring after the dose is taken has been reported with most )
Increased wakefulness beyond baseline amounts that last for a few nights after abrupt discontinuation
Rebound insomnia
How can you prevent / minimize rebound insomnia and avoid adverse effects on memory w/ use of BZDRAs?
Use lowest effective dose
The FDA requires BZDRA labeling to include a caution regarding what 3 things?
- anaphylaxis
- facial angioedema
- complex sleep behaviors (sleep driving, phone calls, sleep eating)
What is the most common type of drug interaction w/ sedative-hypnotics?
CNS depression
What are the 5 “interacting substances” w/ sedative-hypnotics?
- Alcohol
- Antihistamines
- Antipsychotics
- Opioid analgesics
- Tricyclic antidepressants
Overdose on BZDRAs / sedative-hypnotics can result in what 2 things?
- severe respiratory depression
- cardiovascular depression
Potentially lethal effects of BZDRAs are more likely to occur w/ what 3 substances as compared to benzodiazepines or newer hypnotics such as zolpidem?
- alcohol
- barbiturates
- carbamates
_____ may reverse CNS depressant effects of benzodiazepines, eszopiclone, zolpidem, & zaleplon
Flumazenil
_____ is a reversing agent for BZDRAs
Flumazenil
What are the 3 effects/toxicities of Flumazenil?
- Agitation
- Confusion
- Possible withdrawal syndrome
