Sleep Disorders treatment Flashcards
Goals of sleep disorder tx?
- promote pt’s ability to fall asleep, maintain sleep, and awaken refreshed
- use med for as short a time as possible
- use minimal dose with lease amt of side effects
Benzos used for insomnia?
- alprazolam (Xanax)
- estazolam (Prosom)
- flurazepam (dalmane)
- lorazepam (ativan)
- quazepam (doral)
- temazepam (restoril)
- triazolam (Halcion)
MOA of Benzos?
- selectively acts on polysynaptic neuronal pathways throughout the CNS
- enhance the effects of GABA in CNS
- insomnia: facilitate the effects of GABA in ascending reticular activating system
Diff categories of benzos?
- short acting: triazolam (halcion)
- intermediate acting: temazepam (restoril), estazolam (proSom)
- long acting: flurazepam (dlamane), quazepam (doral)
Adverse effects of Benzos?
- drowsiness
- impaired motor fxn
- prolonged use: physical dependency
Interactions and CIs of Benzos?
- Interactions: caution with ETOH low dose contraceptives - CIs: acute narrow-angle glaucoma preg X lactation
What are benzodiazepine receptor agonists (BRA)?
- developed to improve the safety profile of baribturate type compounds
- have short half life: 5 hrs
- has greater receptor specificity of the GABAa BZ complex
(don’t develop tolerance, can use for longer amt of time compared to benzos, safer thean benzos)
Category of BRA’s?
- eszopiclone (lunesta)
- zolpidem (ambien)
- zaleplon (sonata)
MOA and dosage of eszopiclone (Lunesta)?
- interacts with GABA receptors located near benzo receptors
- good for sleep maintenance
- dosage:
start at 2 mg immed b/f bed, can be started or increased to 3 mg to aid in sleep maintenance - elderly:
start 1 mg to help fall asleep
2 mg for sleep maintenance
Adverse effects and CIs of eszopiclone (lunesta)?
- HA
- dry mouth
- dizziness
- CI: hypersensitivity to drug
- preg C
MOA and dosage of zolpidem (ambien, ambien CR)?
- MOA: modulates the GABA receptors to suppress neurons
- dosage:
5-10 mg PO qhs
extended release: 6.25-12.5 mg PO qhs - give lower doses in women and elderly - don’t clear drug as quickly
Adverse effects and CIs of zolpidem?
- adverse effects: morning drowsiness hangover HA - CIs: hypersensitivity - Preg C
MOA and dosage, Adverse effects, and CIs of Zaleplon (Sonata)?
- MOA: interacts with GABA-BZ omega 1 receptor = leads to sedation, muscle relaxation, anti-convulsant
- dosage:
start 10 mg PO qhs
range 5-20 mg qhs - used 2nd line for pts who have hard time falling asleep behind ambien
- adverse effects: back or chest pain, migraine, constipation
- CIs: hypersensitivity
- Preg C
Antihistamine use? Main drug used?
- most commonly used classes of OTC sleep inducing agents
- Diphenhydramine (benadryl)
MOA: unknown, acts as CNS depressant - dosage: 25-50 mg qhs
- adverse effects: excessive daytime drowsiness, impaired psychomotor fxn
- anticholinergic effects: dry mouth, caution in elderly, BPH
- category B: good to use in pregnancy
Antidepressants used for insomnia?
- imipramine (tofranil)
- amitriptyline hydrochloride (elavil)
- nortriptyline (pamelor)
- newer agents: nefazodone hydrochloride (serzone)
venlafaxine (effexor) - used off label, only antidepressant approved for insomnia is silenor
MOA, dosage, adverse effects and CI of doxepin (silenor)?
- MOA: increases synaptic concentrations of serotonin and NE in CNS
- dosage: 3-6 mg w/in 30 min of bedtime
- adverse effects: drowsiness, dizziness, constipation, blurred vision
- CI: glaucoma, urinary retention, constipation
- preg C
BBW of Doxepin (silenor)?
- Suicide thinking/behavior
MOA, dosage, adverse effects, CI of trazodone? BBW?
- SARI: inhibits reuptake of serotonin, causes adrenoreceptor subsensitivity, induces change in 5-HT pressynaptic receptor adrenoreceptorys
- dosage: 5-100 mg b/f bedtime
- adverse effects: dizziness, drowsiness
- CI: use of MAOIs, pts receiving linezolid or IV methylene blue
- preg C
- BBW: suicidal thoughts
MOA, dosage, adverse effects, CI of amitriptyline ?
- MOA: increases synaptic concentration of serotonin and or NE in CNS
- dosage: 25-50 mg at bedtime
- adverse effects: sedation, dizziness, HA, constipation, wt gain
- half life: 13-36 hrs
- CI: hx of MI, MAOIs
- preg C
- BBW: suicidal thoughts
MOA, dosage, adverse effects, CI, preg of Ramelteon (rozerem)?
- MOA: potent, selective agonist of melatonin receptors MT1, and MT2 within the suprachiasmic nucleus of the hypothalamus
- dosage: 8 mg daily w/in 30 min of bedtime
- adverse effects: somnolence. HA, fatigue, nausea
- CI: fluvoxamine (luvox) SSRI
- preg C
What is suvorexant (belsomra)? MOA, dosage, adverse effects, CIs, preg?
- orexin receptor antagonist
- MOA: blocks binding of wake promoting neuropeptides orexin A and B to receptors OZ1R and OX2R - suppresses wake drive
- dosage: 10 mg once daily w/in 30 min of bedtime (max 20 mg)
- don’t take immed after meal, need 7 hrs of planned sleep
- adverse effects: drowsiness, HA, abnormal dreams
- CI: narcolepsy
- preg C
First line tx for narcolepsy? MOA, dose, adverse effects, preg?
- modafinil (Provigil)/armodafinil (nuvigil):
MOA: not well understood, but may increase dopaminergic signaling - dose: modafinil - 100mg qAM, can titrate up to 300-400 mg
armodafinil: 150 mg q AM, titrate up to 250 mg - adverse effects: HA, nausea, nervousness, dry mouth
- preg C
2nd line tx for narcolepsy? MOA, dose, side effects, preg, BBW?
- dextroamphetamine
- MOA: not well understood, but stimulates CNS activity, blocks reuptake and icnreases release of NE and dopamine in extraneuronal space (sympathomimetic)
- dose: 10 mg daily
- SE: HTN, anorexia, addiction
- preg C
- BBW: high abuse potential, cardiac events
- don’t take in evening - insomnia
First line therapy for REM sleep behavior disorder?
- melatonin
- MOA: prepares body for sleep
- doses: 0.5 - 10 mg PO qhs
- SEs:
abnormal heartbeat, dizziness, fatigue
Movement disorders?
- RLS
- periodic limb movement disorders
Dopaminergic agent used in movement disorders?
- carbidopa-levodpa (sinemet)
- dosage: carbidopa 25 mg/levodopa 100mg (0.5-1 tab)
- adverse effects:
sleepiness, GI probs
Dopamine agonists used in movement disorders? MOA?
- pramipexole (mirapex)
- ropinirole (requip)
- rotigotine (neupro)
- MOA: stimulation of postsynaptic dopamine D2 type receptors within caudate putamen in the brain
Dosage of dopamine agonists in movement disorders? Adverse effects, preg?
- pramipexole: initial 0.125 mg once daily 2-3 hrs b/f bef
- ropinirole (requip): inital 0.25 mg daily 1-3 hrs b/f bed
- rotigotine: apply 1 mg pathc daily
- adverse effects: Nausea, lightheadedness
- preg C
Anticonvulsants used in movement disorders?
- gabapentin (neurontin)
- MOA: thought to reduce presynaptic GABA release
- dosage: initial 300 mg daily 2 hrs b/f bed
- adverse events:
fatigue, dizziness, blurred vision - preg C
- used off label for RLS
