Sleep Disorders Flashcards
What are the effects of a sedative drug
- decreases activity
- calming effect
- moderates excitement
What is a hypnotic drug?
- produces drowsiness
- imitates the natural sleep pattern
What is insomnia?
sleep disorder; you have difficulty falling or staying asleep
What are the three different types of insomnia?
- Transient insomnia
- Acute insomnia
- Chronic insomnia
What is transient insomnia?
a type of insomnia that can be brought on by many things and usually lasts for a few days
What is acute insomnia?
a type of insomnia that is caused by many types of stresses or a traumatic event and this usually lasts for a few days or weeks
What is chronic insomnia?
a type of insomnia that is caused by an underlying disorder and can last from months to years
How many stages of sleep are there?
5 stages
What is stage is REM sleep in?
Stage 5
Where does non-REM sleep occur?
Stages 1 - 4
What is Stage 1 sleep?
light sleep, muscle activity slows, slight muscle twitching
What is Stage 2 sleep?
slight decrease in body temperature, breathing and heart rate slows
What is Stage 3 sleep?
deep sleep begins, brain generates delta waves
What is Stage 4 sleep?
deep sleep begins; delta waves are produced; limited muscle activity
What is Stage 5 sleep?
REM sleep; dreaming occurs; muscles relax and heart rate increases; breathing is rapid and shallow
What are the ideal hypnotic pharmacokinetic properties?
- rapid absorption
- no active metabolites
- optimal half- life
What are the ideal hypnotic pharmacokinetic effects?
- rapid onset of action
- other mechanisms besides CNS depression
- sleep maintenance
- improved daytime function
- no “hangover effect” in the morning
Why were barbiturates replaced as the mainstay treatment to induce sleep with BZDs? (4 reasons)
- induce tolerance
- physical dependence
- severe withdrawal symptoms
- induce drug-metabolizing enzymes
What is the onset of action of barbiturates?
20 - 60 minutes
What is the duration of action of barbiturates?
15 - 50 hours
What are two examples of barbiturates?
pentobarbital, amobarbital
What is the CNS effect of barbiturates?
induced coma with toxic doses
What is the mechanism of action of barbiturates?
bind to GABA (a) receptors and then potentiate GABA actions which causes a prolonged entry of chloride through the chloride channel in the GABA receptor
What is the mechanism of action of benzodiazepines?
enhances the GABA induced ionic currents by causing hyper-polarization and causing increased inhibitory effects
What are the actions of benzodiazepines?
- sedative-hypnotic
- muscle relaxant
- anxiolytic
- anticonvulsant
Do benzodiazepines have a general anesthetic effect?
No
As the dosage of benzodiazepines increases what happens?
hypnosis then leads to unconsciousness
How do benzodiazepines affect sleep?
benzodiazepines decrease the amount of time that it takes for you to fall asleep, which will increase the amount of time that you are asleep
What is an FDA approved drug that helps with insomnia?
Temazepam (Restoril)
What is the effect that benzodiazpines have at hypnotic doses?
- no effect on respiration
- no effect on cardiovascular effects
- obstructive sleep apnea
What is the effect that benzodiazepines have at anesthetic doses?
- slight depression of alveolar ventilation
- decreases blood pressure and increases heart rate
What type of drugs are the first line therapy for insomnia?
“Z-drugs”
Do “Z-drugs” have a high or low potential for abuse?
low potential for abuse
What is the effect that Z-drugs have on benzodiazepines?
agonistic effects at the benzodiazepine site on the GABA receptor
What class of drugs are ideal for elderly patients?
Z-drugs
What are the advantages of using Z-drugs? (6)
- no rebound insomnia
- less hangover
- no withdrawal
- no active metabolites
- less effect on the sleep cycle
- dependency is only expected after long term use
What is the mechanism of action for Zaleplon (Sonata)?
agonist at GABA receptors (alpha-1 receptor unit)
What is the sleep onset of Zaleplon (Sonata)
1 hour
When is the ideal time that you would need to take Zaleplon (Sonata)
directly at bedtime or before bedtime
Is Zolpidem (Ambien)for long term or short term treatment of insomnia?
short term treatment of insomnia
When would you have to adjust the dose of Zolpidem (Ambien)
for elderly patients and cirrhosis patients
What drug has a sex-gap?
Zolpidam
What formulations does Zolpidem come in?
Controlled and Immediate release
Does Ambien emulate normal sleep cycle?
yes
Is Eszopiclone (Lunesta) for short term or long term treatment of insomnia?
long term
What are some side effects of Eszopiclone (Lunesta)?
may cause abnormal thinking, behavior, aggression, agitation and hallucinations
What is the mechanism of action for antihistamines?
Histamine Receptor Antagonists
What are two examples of antihistamines?
Diphenhydraminen (Zyquil) and Doxylamine
What is a side effect of antihistamine use?
dry mouth, dry eyes, urinary retention, blurred vision, and constipation
What is the mechanism of action for Doxepin (Silenor)?
H1-receptor (Higher affinity)
What is Doxepin (Silenor)?
tricyclic antidepressant that has antihistamine effects
Doxepin (Silenor) improves sleep maintenance, but not ______?
latency
What do you need to be cautious of when taking Doxepin (Silenor)?
do not use when taking MAO inhibitor in the past 14 days
What drug is an orexin receptor antagonist?
Suvorexant
What is the indication for Suvorexant?
it treats difficulty in falling or staying asleep
What is the mechanism of action for Suvorexant?
Highly selective dual antagonist for orexin receptors OX1R and OX2R
What is the main difference between Orexin Receptor Antagonist and other drugs that treat sleep disorders?
it does not disrupt cognition
What is melatonin?
Hormone produced naturally by the pineal gland in response to darkness; helps manage sleep and wake cycles
What is the mechanism of action of melatonin?
MT1and MT2receptor agonist
Where is melatonin likely the most effective?
delayed sleep phase syndrome
What can melatonin also be used for even though it is not FDA approved?
dietary supplement
What is the mechanism of action for Ramelteon (Rozerem)?
melatonin receptor agonist that has a high affinity for M1 and M2
What is Ramelteon (Rozerem)?
Synthetic melatonin analog
What are the advantages of Ramelteon (Rozerem)? (4)
- no rebound insomnia
- no CNS depression
- no abuse potential, tolerance, or withdrawal
You are the medication specialist as part of an interprofessional team at a local hospital. A.D. is a 79-year old female who was diagnosed with Parkinson’s disease 2 years ago. She complains about having difficulty falling asleep. You are asked for a therapeutic recommendation. Patient currently takes lovastatin and a MAO inhibitor. Which of the following medications would be useful for A.D.?
Eszopiclone
