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suvorexant

Structure via PubChem · Public domain (PubChem)

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suvorexant

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Also known as Belsomra®, DORA-analogue, MK 4305, MK-4305, MK4305, Belsomra

Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults. Suvorexant helps with falling asleep faster, sleeping longer, being awake less in the middle of the night, and having better quality of sleep. Its effectiveness is modest, and is similar to that of other orexin antagonists, but is lower than that of benzodiazepines and Z-drugs. Suvorexant is taken orally.

Key facts

Drug.Verifiedfields
verified
Drug.Watchedfields
verified
Drug.verifiedrevid
458281672
Drug.image
Suvorexant.svg
Drug.image_class
skin-invert-image
Drug.image2
Suvorexant-from-xtal-Mercury-3D-bs.png
Drug.width
250px
Drug.image_class2
bg-transparent
Drug.width2
250px
Drug.tradename
Belsomra
Drug.MedlinePlus
a614046
Drug.DailyMedID
Suvorexant
Drug.pregnancy_AU
B3
Drug.dependency_liability
Low
Drug.addiction_liability
Low
Drug.routes_of_administration
Oral
Drug.class
Orexin receptor antagonist; Hypnotic; Sedative
Drug.ATC_prefix
N05

via Wikipedia infobox

Chemical data

Formula
C23H23ClN6O2
Molecular weight
450.9 g/mol
IUPAC name
[(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone
SMILES
C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
InChIKey
JYTNQNCOQXFQPK-MRXNPFEDSA-N
XLogP
4.9
Polar surface area
80.3 Ų
H-bond donors
0
H-bond acceptors
6
Formal charge
0

via PubChem

~35 min read

Encyclopedic overview

31 sections
Contents
  • Medical uses
  • Available forms
  • Contraindications
  • Side effects
  • Overdose
  • Interactions
  • Pharmacology
  • Pharmacodynamics
  • Mechanism of action
  • Pharmacokinetics
  • Absorption
  • Distribution
  • Metabolism
  • Elimination
  • Specific populations
  • Miscellaneous
  • Chemistry
  • History
  • Society and culture
  • Names
  • Availability
  • Legal status
  • Controversy
  • Research
  • Delirium
  • Psychiatry
  • Alzheimer's disease
  • Diabetes
  • References
  • Further reading
  • External links

Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults. Suvorexant helps with falling asleep faster, sleeping longer, being awake less in the middle of the night, and having better quality of sleep. Its effectiveness is modest, and is similar to that of other orexin antagonists, but is lower than that of benzodiazepines and Z-drugs. Suvorexant is taken orally.

Side effects of suvorexant include somnolence, daytime sleepiness and sedation, headache, dizziness, abnormal dreams, dry mouth, and impaired next-day driving ability. Rarely, sleep paralysis, sleep-related hallucinations, complex sleep behaviors like sleepwalking, and suicidal ideation may occur. Tolerance, dependence, withdrawal, and rebound effects do not appear to occur significantly with the medication. Suvorexant is a dual orexin receptor antagonist (DORA). It acts as a selective dual antagonist of the orexin OX1 and OX2 receptors. The medication has an intermediate elimination half-life of 12hours and a time to peak of about 2 to 3hours. Unlike benzodiazepines and Z-drugs, suvorexant does not interact with GABA receptors, instead having a distinct mechanism of action.

Excerpted from Wikipedia’s “suvorexant” article, available under the CC BY-SA 4.0 licence.

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