Insomnia Flashcards
zolpidem (Ambien (CR)/Intermezzo)
Indication: Insomnia (Intermezzo (SL): mid. awakening (+CR))
Dose: 10mg (5mg in women); CR (12.5/6.25); SL (3.5/1.75)
Mechanism: selective GABA-A alpha-1 agonist
Advantages: does not disrupt sleep stages (like benzos)
Disadvantages: rebound insomnia; Schedule IV
ADEs: sedation, headache; complex-sleep behaviors (driving, eating, phone calls, sex)
doxepin (Silenor)
use generic
Indication: Insomnia; depression; anxiety disorders
Dose: 10mg at bedtime; Silenor at 6mg at bedtime (3mg for elderly); wait 3 hours after eating
Monitoring: EKG
Mechanism: TCA with NE and SRI and H1 antagonism
Advantages: non-habit forming; cost; non-hypnotic
Disadvantages: cardiac effects (at higher doses)
ADEs: somnolence; nausea; dry mouth; constipation; orthostasis
Off-Label: headaches; fibromyalgia; anxiety disorders
eszopiclone (Lunesta)
Indication: Insomnia
Dose: 1mg at bedtime; MAX=3mg (2mg in elderly); avoid high-fat meals (delays onset); take directly before bed
Monitoring: no routine monitoring required
Mechanism: selective GABA-A alpha-1 agonist
Advantages: does not disrupt sleep stages (like benzos)
Disadvantages: rebound insomnia; Schedule IV; high grogginess if less than eight hours between dose and awake
ADEs: somnolence; headache; unpleasant taste sensation; dizziness; dry mouth; anaphylaxis (rare); complex-sleep behaviors (driving, eating, phone calls, sex)
flurazepam (Dalmane)
Indication: Insomnia
Dose: Start at 15mg at bedtime; MAX=30mg (lower doses in elderly)
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: long half-life reduces breakthrough symptoms
Disadvantages: has active metabolites that accumulate; dependence (Schedule IV)
ADEs: somnolence; dizziness; weakness; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Other Anxiety Disorders; Acute Mania; Catatonia
Fun Facts: Marketing tagline: “One less concern for your patient with insomnia” – woman trapped in eyeball sphere trying to get out.
ramelteon (Rozerem)
Indication: Insomnia
Dose: 8mg (only dose); Avoid after high fat meal (delays onset)
Monitoring: prolactin levels; testosterone levels
Mechanism: melatonin-1 and melatonin-2 receptor agonist
Advantages: abuse and tolerance potential non-existent; lower risk of daytime grogginess
Disadvantages: not a lot different than OTC melatonin; lacks “feeling sleepy feeling,” so patients need to be informed of this—research stated that it is effective near onset, but patients report several-day lag; hormonal alterations occur with long-term use (or higher doses)
ADEs: headache; somnolence; fatigue; dizziness; nausea; SERIOUS: anaphylaxis; angioedema; complex-sleep-related behavior disorders; increased prolactin; abnormal cortisol and testosterone levels
Off-Label: Jet lag; shift-work sleep disorder; non-24-hour sleep-wake cycle
Fun Facts: another melatonin agonist has been investigated for depression but scrapped.
suvorexant (Belsomra)
Indication: Insomnia
Dose: Start at 10mg at bedtime; Take one hour after any meal (delays effect by up to 2 hours); MAX=20mg – FDA warnings at doses above this.
Monitoring: No routine monitoring required.
Mechanism: Duel orexin (OX1 and OX2) receptor antagonist (DORA) (NTs that promote wakefulness)
Advantages: Unique mechanism of action
Disadvantages: Safety concerns at higher doses; no different abuse potential
ADEs: SERIOUS: safety concerns at higher doses; impaired alertness the next day (esp. driving); sleep paralysis; hypnagogic/hypnopompic hallucinations; leg catalepsy; COMMON: Somnolence; headaches; abnormal dreams; dry mouth
temazepam (Restoril)
Indication: Insomnia
Dose: 15mg at bedtime; MAX=30mg; use lower doses in elderly; SLOW ONSET – Take 1 hr before bedtime and DO NOT repeat
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: lack of active metabolites; favored in the elderly; considered first line if benzos are preferred for insomnia
Disadvantages: Tolerance develops quickly; impacts sleep architecture; dependence (Schedule IV)
ADEs: somnolence; dizziness; weakness; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability)-primarily in elderly and pediatric populations; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: Used in DoD as a no-go pill
triazolam (Halcion)
Indication: Insomnia
Dose: 0.25mg at bedtime; MAX=0.5mg at bedtime
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: rapid onset
Disadvantages: Highest likelihood of anterograde amnesia and psychiatric disturbances (many have asked for it to be banned from US market—has been banned in the UK and Brazil); not effective for middle awakenings; tolerance develops quickly; impacts sleep architecture
ADEs: somnolence; dizziness; weakness; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability)-primarily in elderly and pediatric populations; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: Used by Dahmer to sedate his victims
zaleplon (Sonata)
Indication: Insomnia
Dose: 10mg at bedtime; MAX=20mg; avoid high-fat meals (delays onset); lower doses in the elderly
Monitoring: no routine monitoring required
Mechanism: selective GABA-A alpha-1 agonist
Advantages: does not disrupt sleep stages (like benzos); best agent for inducing sleep; fewer withdrawal effects with discontinuation; can be taken in middle of night without functional impairment (if 5+ hours of sleep, though always use caution the next day)
Disadvantages: does not help with TST or decrease number of awakenings; Schedule IV; if taken at ultra-high doses, can produce euphoria similar to benzodiazepines
ADEs: somnolence; headache; dizziness; anaphylaxis (rare); complex-sleep behaviors (driving, eating, phone calls, sex)
Fun Facts: Sonata is a musical composition with 4 movements (like stages of sleep)
Insomnia Algorithm
Non-Pharm: CBT-i; Sleep Hygiene; Blue Light Glasses; Sleep Study (r/o apnea or RLS)
Short-Term Insomnia: Zaleplon (short half-life); Zolpidem; temazepam)
Long Term (uncomplicated): diphenhydramine; melatonin; trazodone
Long Term (comorbid depression): mirtazapine; doxepin; amitriptyline; trazodone
Long Term (nightmares): clonidine; prazosin; mirtazapine
Long Term (psychosis/bipolar): quetiapine
Long Term (pain or seizures): gabapentin; pregabalin
Long Term (treatment-resistant): ramelteon; suvorexant
trazodone (Desyrel)
Indication: Major Depression
Dose: (for depression): Start at 50mg TID; increase by 50mg/d weekly; target 400mg/d; MAX=600mg/d
(for insomnia): Start 25mg at bedtime; increase by 25-50mg as needed; Max=200mg
Monitoring: No routine monitoring required
Mechanism: serotonin reuptake inhibitor; alpha-1 adrenergic antagonist; 5HT2A and hHT2C receptor antagonist
Advantages: few sexual ADEs; low weight gain; low anticholinergic or antihistaminergic effect; non-habit-forming
Disadvantages: oversedation at therapeutic doses for depression limits its use as an antidepressant; metabolite mCPP may test positive for MDMA
ADEs: drowsiness; dry mouth; dizziness; orthostatic hypotension; headache; blurred vision; nausea; vomiting; SERIOUS: priapism (which may have long-term erectile problems; syncope
Off-Label: insomnia; anxiety
