Suvorexant

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[edit] BRAND NAMES

[edit] STRUCTURE

Suvorexant.jpg

[edit] MECHANISM OF ACTION

Suvorexant (Belsomra) is a dual orexin receptor antagonist for orexin receptors OX1R and OX2R.

Suvorexant works by turning off wakefulness rather than by inducing sleep. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.

Antagonism of orexin receptors may also underlie potential adverse effects such as signs of narcolepsy/cataplexy. Genetic mutations in the orexin system in animals result in hereditary narcolepsy; loss of orexin neurons has been reported in humans with narcolepsy.

[edit] INDICATIONS

Suvorexant is indicated for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance

[edit] DOSAGE

  • Use the lowest dose effective for the patient.
  • Recommended dose is 10 mg, no more than once per night taken within 30 minutes of going to bed, with at least 7 hours remaining before the planned time of awakening. If the 10 mg dose is well-tolerated but not effective, the dose can be increased, not to exceed 20 mg once daily.
  • Time to effect may be delayed if taken with or soon after a meal

[edit] CONTRAINDICATIONS

Do not use in patients with narcolepsy

[edit] WARNINGS AND PRECAUTIONS

  • Daytime somnolence: Risk of impaired alertness and motor coordination, including impaired driving; risk increases with dose; caution patients taking 20 mg against next-day driving and other activities requiring complete mental alertness.
  • Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment
  • Nighttime “sleep-driving” and other complex behaviors while out of bed and not fully awake. Risk increases with dose, with use of CNS depressants, and with alcohol.
  • Depression: Worsening of depression or suicidal thinking may occur. Risk increases with dose. Immediately evaluate any new behavioral changes.
  • Compromised respiratory function: Effect on respiratory function should be considered.
  • Sleep paralysis, hypnagogic/hypnopompic hallucinations, and cataplexy-like symptoms: Risk increases with dose

[edit] INTERACTIONS

  • CYP3A inhibitors: Recommended dose is 5 mg when used with moderate CYP3A inhibitors. Dose can be increased to 10 mg once daily if the 5 mg dose is not effective. Not recommended for use in patients taking strong CYP3A inhibitors.
  • Strong CYP3A inducers: Efficacy may be reduced.
  • Digoxin: Monitor digoxin concentrations

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US): There are no adequate and well-controlled studies in pregnant women. Suvorexant should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: Suvorexant and a hydroxyl-suvorexant metabolite were excreted in rat milk at levels higher (9 and 1.5

times, respectively) than that in maternal plasma. It is not known whether this drug is secreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Suvorexant is administered to a nursing woman.

[edit] SIDE EFFECTS

The most common adverse reaction (reported in 5% or more of patients treated with Suvorexant and at least twice the placebo rate) was somnolence

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Sedatives / Hypnotics / Anxiolytics
Benzodiazepines Benzodiazepines (Anxiolytics)‎ Alprazolam (Xanax)   Bromazepam (Lexotan, Lexotanil)   Chlordiazepoxide (Librium)   Clobazam (Frisium)   Clorazepate (Tranxene)   Clotiazepam (Rizen, Tienor)   Delorazepam (EN)   Diazepam (Valium)   Etizolam (Depas)   Ketazolam   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Noctamid)   Nordazepam (Nordaz)   Oxazepam (Serepax)   Prazepam (Demetrin, Lysanxia)
Benzodiazepines (Hypnotics) Brotizolam (Lendormin, Bondormin, Dormex, Sintonal, Noctilan)   Clobazam (Frisium)   Estazolam (Esilgan, ProSom)   Etizolam (Depas, Pasaden, Etilaam, Etizest)   Flunitrazepam (Rohypnol)   Flurazepam (Dalmadorm, Dalmane, Felison, Flunox, Valdorm)   Ketazolam (Anseren, Anxon)   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Loramet, Minias, Noctamid, Pronoctan, Evamyl)   Midazolam (Dormicum, Hypnovel)   Nitrazepam (Mogadon, Nitrados, Numbon, Radedorm, Alodorm)   Nordazepam (Madar, Nordaz, Stilny, Tranxilium N)   Temazepam (Normison, Restoril, Tenox, Temaze)   Triazolam (Halcion, Hypam, Rilamir)
Non-Benzodiazepine Hypnotics Eszopiclone (Lunesta)   Zolpidem (Ambien, Stilnox, Hypnogen, Sanval, Stilnoct, Zoldem, Zolsana)   Zopiclone (Imovane, Zimovane)
Melatonin agonists Melatonin (Circadin)   Ramelteon (Rozerem)
Orexin agonists Suvorexant (Belsomra)