Section 10
Sleep Disorders
Neuro-Relevant Wake & Sleep Agents
23 AGENTS
Modafinil
ProvigilWake-promoting agent
- Forms
- Tab: 100, 200mg
- Dose
- 200mg qAM
- MOA
- Dopamine reuptake inhibition (weak)
Armodafinil
NuvigilWake-promoting agent
- Forms
- Tab: 50, 150, 250mg
- Dose
- 150-250mg qAM
- MOA
- Dopamine reuptake inhibition (weak)
Pitolisant
WakixH3 receptor antagonist
- Forms
- Tab: 4.45, 17.8mg
- Dose
- Titrate weekly to 17.8-35.6mg qAM
- MOA
- Blocks histamine H3 autoreceptor, ↑histamine
Solriamfetol
SunosiDopamine/NE reuptake inhibitor
- Forms
- Tab: 75, 150mg
- Dose
- 75-150mg qAM
- MOA
- Dual dopamine/norepinephrine reuptake inhibition
Sodium oxybate
Xyrem / XywavGABA-B agonist
- Forms
- Sol: 500mg/mL
- Dose
- divided dose qHS + 2.5-4h later
- MOA
- GABA-B agonism, consolidates sleep
Zolpidem
Ambien / Ambien CRNonbenzodiazepine hypnotic (Z-drug)
- Forms
- IR: 5, 10mg | CR: 6.25, 12.5mg
- Dose
- 5-10mg qHS PRN
- MOA
- Selective GABA-A α1 agonism
Eszopiclone
LunestaNonbenzodiazepine hypnotic (Z-drug)
- Forms
- Tab: 1, 2, 3mg
- Dose
- 1-3mg qHS PRN
- MOA
- GABA-A receptor agonism
Zaleplon
SonataNonbenzodiazepine hypnotic (Z-drug)
- Forms
- Cap: 5, 10mg
- Dose
- 5-10mg qHS PRN
- MOA
- Selective GABA-A α1 agonism
Ramelteon
RozeremMelatonin receptor agonist
- Forms
- Tab: 8mg
- Dose
- 8mg qHS
- MOA
- MT1/MT2 receptor agonism
Suvorexant
BelsomraOrexin receptor antagonist
- Forms
- Tab: 5, 10, 15, 20mg
- Dose
- 10-20mg qHS
- MOA
- Blocks orexin-mediated wakefulness
Lemborexant
DayvigoOrexin receptor antagonist
- Forms
- Tab: 5, 10mg
- Dose
- 5-10mg qHS
- MOA
- Blocks orexin-mediated wakefulness
Doxepin (low-dose)
SilenorTCA (low-dose H1 antagonist)
- Forms
- Tab: 3, 6mg
- Dose
- 3-6mg qHS
- MOA
- Selective H1 antagonism at low dose
Trazodone
Desyrel / genericSerotonin antagonist/reuptake inhibitor
- Forms
- Tab: 25, 50, 100, 150, 300mg
- Dose
- 25-100mg qHS
- MOA
- 5-HT2A antagonism + weak reuptake inhibition
Clonazepam
KlonopinBenzodiazepine
- Forms
- Tab: 0.5, 1, 2mg | ODT: 0.125-2mg
- Dose
- 0.5-2mg qHS (REM behavior disorder)
- MOA
- ↑GABA-A Cl- channel frequency
Pramipexole (RLS dosing)
MirapexDopamine agonist
- Forms
- Tab: 0.125, 0.25, 0.5mg
- Dose
- 0.125-0.5mg qHS (restless legs)
- MOA
- D2/D3 receptor agonism
Ropinirole (RLS dosing)
RequipDopamine agonist
- Forms
- Tab: 0.25, 0.5, 1, 2, 3, 4mg
- Dose
- 0.25-4mg qHS (restless legs)
- MOA
- D2/D3 receptor agonism
Gabapentin enacarbil
HorizantGabapentinoid (prodrug)
- Forms
- ER tab: 600mg
- Dose
- 600mg qPM (restless legs)
- MOA
- Binds α2δ Ca2+ channel subunit
Ferrous sulfate
generic onlyIron supplement
- Forms
- Tab: 325mg (65mg elemental iron)
- Dose
- 325mg once-TID (RLS w/ low ferritin)
- MOA
- Repletes iron for dopamine synthesis (RLS)
Melatonin
OTC, generic onlyHormone supplement
- Forms
- Tab/Cap: 1, 3, 5, 10mg
- Dose
- 1-10mg qHS
- MOA
- MT1/MT2 receptor agonism
Daridorexant
QuviviqOrexin receptor antagonist
- Forms
- Tab: 25, 50mg
- Dose
- 25-50mg qHS within 30 min of bed (7+ hours before waking)
- MOA
- Blocks orexin OX1R/OX2R-mediated wakefulness
Tasimelteon
HetliozMelatonin receptor agonist
- Forms
- Cap: 20mg
- Dose
- 20mg 1h before bedtime, same time nightly (Non-24-hour sleep-wake disorder)
- MOA
- MT1/MT2 receptor agonism
Sodium oxybate ER
LumryzGABA-B agonist · ER
- Forms
- ER susp packets: 4.5, 6, 7.5, 9g
- Dose
- Start 4.5g once at bedtime, increase 1.5g weekly to 6-9g
- MOA
- GABA-B / GHB receptor agonism, consolidates sleep
Methylphenidate
Ritalin / ConcertaCNS stimulant
- Forms
- Tab: 5, 10, 20mg | ER tab: 18-72mg
- Dose
- Narcolepsy: 10mg BID-TID (typical 20-60mg/day)
- MOA
- Blocks dopamine/norepinephrine reuptake