Sleep Disorder Treatment Flashcards
Goals of Therapy
Promote patient’s ability to fall sleep, maintain sleep, & awaken refreshed
Meds as short a time as possible
Use minimal dose with least amount of SE
Types of Benzodiazepines
Alprazolam (Xanax) Estazolam (ProSom) Flurazepam (Dalmane) Lorazepam (Ativan) Quazepam (Doral) Temazepam (Restoril) Triazolam (Halcion)
MOA of Benzodiazepines
Facilitate the effects of GABA in the ascending reticular activating system
Examples of Short Acting Benzodiazepines
Triazolam (Halcion)
What are short acting benzodiazepines used for?
Difficulty falling asleep
Examples of Intermediate Acting Benzodiazepines
Temazepam (Restoril)
Estazolam (ProSom)
What are intermediate acting benzodiazepines used for?
Trouble maintaining or staying asleep
Examples of Long Acting Benzodiazepines
Flurazepam (Dalmane)
Quazepam (Doral)
What are long acting benzodiazepines used for?
Trouble falling asleep
Maintaining sleep
Benzodiazepine SE
Drowsiness Impaired motor function Prolonged use can lead to physical dependency Confusion Shakiness
Interactions with Benzodiazepines
Alcohol
Low-dose contraceptives: benzo’s not cleared as quickly
Contraindications of Benzodiazepines
Acute narrow-angle glaucoma
Pregnancy
Lactation
What were benzodiazepine receptor agonists developed for?
Improve the safety profile of barbiturate-type compounds
Half-life of Benzodiazepine Receptor Agonists
5 hours
Examples of Benzodiazepine Receptor Agonists
Eszopiclone (Lunesta)
Zolpidem (Ambien)
Zaleplon (Sonata)
MOA of Eszopiclone (Lunesta)
Interacts with GABA receptors located near benzodiazepine receptors
What affects the absorption of eszopiclone (Lunesta)?
High fat meals
When does eszopiclone (Lunesta) peak?
Within 1 hour
What is the half-life of eszopiclone (Lunesta)?
5-7 hours
Eszopiclone (Lunesta) SE
Headache
Dry mouth
Dizziness
Unpleasant taste in mouth
Contraindications for Eszopiclone (Lunesta)
Hypersensitivity
Pregnancy Category of Eszopiclone (Lunesta)
Pregnancy C
MOA of Zolpidem (Ambien, Ambien CR)
Modulates the GABA receptors to suppress neurons
Sedation & relaxation
Who needs a decreased dose of zolpidem (Ambien, Ambien CR)?
Elderly
Women
Half-life of Zolpidem (Ambien, Ambien CR)
2.5 hours
Onset of Zolpidem (Ambien, Ambien CR)
30 minutes
Duration of Zolpidem (Ambien, Ambien CR)
6-8 hours
Zolpidem (Ambien, Ambien CR) SE
Morning drowsiness Hangover effect Headache Dizziness Nausea
Contraindications of Zolpidem (Ambien, Ambien CR)
Hypersensitivity
Pregnancy Category of Zolpidem (Ambien, Ambien CR)
Pregnancy C
MOA of Zaleplon (Sonata)
Interacts with GABA-BZ omega 1 receptor
Sedation
Relaxation
Anti-convulsant activity
What is the 2nd line for falling asleep?
Zaleplon (Sonata)
Duration of Zaleplon (Sonata)
5 hours
Onset of Zleplon (Sonata)
Within 1 hour
Half-life of Zaleplon (Sonata)
1 hour
Zaleplon (Sonata) SE
Back or chest pain Migraine Constipation Dry mouth Nervousness
Contraindications of Zaleplon (Sonata)
Hypersensitivity
Pregnancy Category of Zaleplon (Sonata)
Pregnancy C
MOA of Diphenhydramine (Benadryl)
Acts as CNS depressant
Contraindications of Diphenhydramine (Benadryl)
Hypersensitivity
Pregnancy Category of Diphenhydramine (Benadryl)
Pregnancy B
Diphenhydramine (Benadryl) SE
Excessive daytime drowsiness Impaired psychomotor function Dry mouth Delirium Anti-cholinergic effect Constipation Urinary retention
Examples of Antidepressants Used for Insomnia
Imipramine (Tofranil)
Amitriptyline hydrochloride (Elavil)
Nortriptyline (Pamelor)
Newer Antidepressant Agents
Neazodone hydrochloride (Serzone) Venlafaxine (Effexor)
MOA of Doxepin (Silenor)
Antagonizes histamine receptor
Increases synaptic concentrations of serotonin & norepinephrine in the CNS
Doxepin (Silenor) SE
Drowsiness
Dizziness
Constipation
Blurred vision
How long after eating does one need to wait to take doxepin (Silenor)?
3 hours
Contraindications of Doxepin (Silenor)
Glaucoma
Urinary retention
Constipation
Black Box Warning of Doxepin (Silenor)
Suicide thinking/behavior
Pregnancy Category of Doxepin (Silenor)
Pregnancy C
MOA of Trazodone
Inhibits repute of serotonin
Causes adrenoreceptor subsensitivity
Induces change in 5-HT presynaptic receptor adrenoreceptors
Block histamine receptors
Onset of Trazodone
1-3 hours
Half-life of Trazodone
7-9 hours
Longer in obese patients
Trazodone SE
Dizziness
Drowsiness
Blurred vision
Confusion
Contraindications of Trazodone
Use of MAOI’s
Patients receiving linezolid or IV methylene blue
Pregnancy Category of Trazodone
Pregnancy C
Black Box Warning for Trazodone
Suicidal thoughts
MOA Amitriptyline (Elavil)
Increases synaptic concentration of serotonin and/or norepinephrine in CNS
Half-life of Amitriptyline (Elavil)
13-36 hours
Amitriptyline (Elavil) SE
Sedation Dizziness Headache Weight gain Sexual SE
Contraindications of Amitriptyline (Elavil)
Hx of MI
MAOI’s
Pregnancy Category of Amitriptyline (Elavil)
Pregnancy C
Black Box Warning for Amitriptyline (Elavil)
Suicidal thoughts
MOA of Ramelteon (Rozerem)
Potent, selective agonist of melatonin receptors MT1 & MT2 within the suprachiasmic nucleus of the hypothalamus
Half-life of Ramelteon (Rozerem)
1-2 hours
Ramelteon (Rozerem) SE
Somnolence Headache Fatigue Dizziness Nausea
Contraindications for Ramelteon (Rozerem)
Fluvoxamine (Luvox)
Pregnancy Category of Ramelteon (Rozerem)
Pregnancy C
Melatonin Agonist
Ramelteon (Rozerem)
Orexin Receptor Antagonist
Suvorexant (Belsomra)
MOA of Suvorexant (Belsomra)
Blocks binding of wake-promoting neuropeptides orexin A & orexin B to receptors OZ1R & OX2R
AKA: Blocks wakening of the patient
Duration of Suvorexant (Belsomra)
7 hours
When can you not take Suvorexant (Belsomra)?
Immediately after a meal
Half-life of Suvorexant (Belsomra)
12 hours
Onset of Suvorexant (Belsomra)
30 minutes
Suvorexant (Belsomra) SE
Drowsiness Headache Abnormal dreams Lower extremity weakness Cough
Contraindications of Suvorexant (Belsomra)
Narcolepsy
Pregnancy Category of Suvorexant (Belsomra)
Pregnancy C
Medications for Insomnia
Alprazolam (Xanax) Estazolam (ProSom) Flurazepam (Dalmane) Lorazepam (Ativan) Quazepam (Doral) Temazepam (Restoril) Triazolam (Halcion) Eszopiclone (Lunesta) Zolpidem (Ambien) Zaleplon (Sonata) Imipramine (Tofranil) Amitriptyline hydrochloride (Elavil) Nortriptyline (Pamelor) Nefazodone hydrochloride (Serzone) Venlafaxine (Effexor) Doxepin (Silenor) Trazodone Ramelteon (Rozerem) Suvorexant (Belsomra)
First Line Narcolepsy Medication
Modafinil (Provigil)/Armodafinil (Nuvigil)
MOA of Modafinil (Provigil)/Armodafinil (Nuvigil)
Not well understood
May increase dopaminergic signaling
Modafinil (Provigil)/Armodafinil (Nuvigil) SE
Headache
Nausea
Nervousness
Dry mouth
Contraindications of Modafinil (Provigil)/Armodafinil (Nuvigil)
Hypersensitivity
Pregnancy Category Modafinil (Provigil)/Armodafinil (Nuvigil)
Pregnancy C
Second Line Narcolepsy Medication
Dextroamphetamine
MOA of Dextroamphetamine
Not well understood
Stimulates CNS activity
Blocks reuptake & increases release of norepinephrine & dopamine in extra neuronal space
Dextroamphetamine SE
HTN
Anorexia
Addiction
Pregnancy Category of Dextroamphetamine
Pregnancy C
Black Box of Dextroamphetamine
High abuse potential
Cardiac events
Medication for REM Sleep Behavior Disorder
Melatonin
MOA of Melatonin
Prepares the body for sleep
Melatonin SE
Abnormal heartbeat
Dizziness
Fatigue
Medications for Movement Disorders
Carbidopa-levadopa (Sinemet) Pramipexole (Mirapex) Ropinirole (Requip) Rotigotine (Neupro) Gabapentin (Neurontin)
Carbidopa-levodopa (Sinemet) SE
Sleepiness
GI problems
Examples of Dopamine Agonists for Movement Disorders
Pramipexole (Mirapex)
Ropinirole (Requip)
Rotigotine (Neupro)
MOA of Dopamine Agonists
Stimulating of postsynaptic dopamine D2-type receptors within the caudate putamen in the brain
Dopamine Agonist SE
Nausea Lightheadedness Stuffiness Edema Daytime sleepiness
Pregnancy Category of Dopamine Agonists
Pregnancy C
MOA of Gabapentin (Neurontin)
Thought to reduce presynaptic GABA release
Gabapentin (Neurontin) SE
Fatigue
Dizziness
Blurred vision
Pregnancy Category for Gabapentin (Neurontin)
Pregnancy C