Sleep Disorders treatment

Question 1

Goals of sleep disorder tx?

Answer 1

• 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

Question 2

Benzos used for insomnia?

Answer 2

• alprazolam (Xanax)
• estazolam (Prosom)
• flurazepam (dalmane)
• lorazepam (ativan)
• quazepam (doral)
• temazepam (restoril)
• triazolam (Halcion)

Question 3

MOA of Benzos?

Answer 3

• 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

Question 4

Diff categories of benzos?

Answer 4

• short acting: triazolam (halcion)
• intermediate acting: temazepam (restoril), estazolam (proSom)
• long acting: flurazepam (dlamane), quazepam (doral)

Question 5

Adverse effects of Benzos?

Answer 5

• drowsiness
• impaired motor fxn
• prolonged use: physical dependency

Question 6

Interactions and CIs of Benzos?

Answer 6

- Interactions: 
caution with ETOH
low dose contraceptives
- CIs:
acute narrow-angle glaucoma
preg X
lactation

Question 7

What are benzodiazepine receptor agonists (BRA)?

Answer 7

• 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)

Question 8

Category of BRA’s?

Answer 8

• eszopiclone (lunesta)
• zolpidem (ambien)
• zaleplon (sonata)

Question 9

MOA and dosage of eszopiclone (Lunesta)?

Answer 9

• 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

Question 10

Adverse effects and CIs of eszopiclone (lunesta)?

Answer 10

• HA
• dry mouth
• dizziness
• CI: hypersensitivity to drug
• preg C

Question 11

MOA and dosage of zolpidem (ambien, ambien CR)?

Answer 11

• 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

Question 12

Adverse effects and CIs of zolpidem?

Answer 12

- adverse effects:
morning drowsiness
hangover
HA
- CIs:
hypersensitivity
- Preg C

Question 13

MOA and dosage, Adverse effects, and CIs of Zaleplon (Sonata)?

Answer 13

• 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

Question 14

Antihistamine use? Main drug used?

Answer 14

• 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

Question 15

Antidepressants used for insomnia?

Answer 15

• imipramine (tofranil)
• amitriptyline hydrochloride (elavil)
• nortriptyline (pamelor)
• newer agents: nefazodone hydrochloride (serzone)
  venlafaxine (effexor)
• used off label, only antidepressant approved for insomnia is silenor

Question 16

MOA, dosage, adverse effects and CI of doxepin (silenor)?

Answer 16

• 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

Question 17

BBW of Doxepin (silenor)?

Answer 17

• Suicide thinking/behavior

Question 18

MOA, dosage, adverse effects, CI of trazodone? BBW?

Answer 18

• 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

Question 19

MOA, dosage, adverse effects, CI of amitriptyline ?

Answer 19

• 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

Question 20

MOA, dosage, adverse effects, CI, preg of Ramelteon (rozerem)?

Answer 20

• 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

Question 21

What is suvorexant (belsomra)? MOA, dosage, adverse effects, CIs, preg?

Answer 21

• 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

Question 22

First line tx for narcolepsy? MOA, dose, adverse effects, preg?

Answer 22

• 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

Question 23

2nd line tx for narcolepsy? MOA, dose, side effects, preg, BBW?

Answer 23

• 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

Question 24

First line therapy for REM sleep behavior disorder?

Answer 24

• melatonin
• MOA: prepares body for sleep
• doses: 0.5 - 10 mg PO qhs
• SEs:
  abnormal heartbeat, dizziness, fatigue

Question 25

Movement disorders?

Answer 25

- RLS | - periodic limb movement disorders

Question 26

Dopaminergic agent used in movement disorders?

Answer 26

- carbidopa-levodpa (sinemet) - dosage: carbidopa 25 mg/levodopa 100mg (0.5-1 tab) - adverse effects: sleepiness, GI probs

Question 27

Dopamine agonists used in movement disorders? MOA?

Answer 27

- pramipexole (mirapex) - ropinirole (requip) - rotigotine (neupro) - MOA: stimulation of postsynaptic dopamine D2 type receptors within caudate putamen in the brain

Question 28

Dosage of dopamine agonists in movement disorders? Adverse effects, preg?

Answer 28

- 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

Question 29

Anticonvulsants used in movement disorders?

Answer 29

- 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