Suvorexant

Suvorexant
Clinical data
Trade namesBelsomra
Other namesMK-4305; MK4305
AHFS/Drugs.comMonograph
MedlinePlusa614046
License data
Pregnancy
category
Dependence
liability		Low
Addiction
liability		Low
Routes of
administration		By mouth[2]
Drug classOrexin receptor antagonist; Hypnotic; Sedative
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability82% (10 mg; lower at higher doses)[2][5]
Protein binding99.5%[6][2]
MetabolismLiver (CYP3A major, CYP2C19 minor)[2]
MetabolitesHydroxysuvorexant (inactive)[2]
Elimination half-life12.2 hours (8–19 hours) (40 mg)[2][5][7]
ExcretionFeces: 66%[2]
Urine: 23%[2]
Identifiers
  • [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.210.546 Edit this at Wikidata
Chemical and physical data
FormulaC23H23ClN6O2
Molar mass450.93 g·mol−1
3D model (JSmol)
  • C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
  • InChI=1S/C23H23ClN6O2/c1-15-3-5-20(30-25-8-9-26-30)18(13-15)22(31)29-12-11-28(10-7-16(29)2)23-27-19-14-17(24)4-6-21(19)32-23/h3-6,8-9,13-14,16H,7,10-12H2,1-2H3/t16-/m1/s1 checkY
  • Key:JYTNQNCOQXFQPK-MRXNPFEDSA-N checkY
  (verify)

Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication which is used in the treatment of insomnia.[2][6] It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults.[2][6] Suvorexant helps with falling asleep faster, sleeping longer, being awake less in the middle of the night, and having better quality of sleep.[2][8] Its effectiveness is modest,[9] and is similar to that of other orexin antagonists, but is lower than that of benzodiazepines and Z-drugs.[10] Suvorexant is taken by mouth.[2][11][6]

Side effects of suvorexant include somnolence, daytime sleepiness and sedation, headache, dizziness, abnormal dreams, dry mouth, and impaired next-day driving ability.[2][8][12] Rarely, sleep paralysis, sleep-related hallucinations, complex sleep behaviors like sleepwalking, and suicidal ideation may occur.[2][6][9] Tolerance, dependence, withdrawal, and rebound effects do not appear to occur significantly with the medication.[2][13][14] Suvorexant is a dual orexin receptor antagonist (DORA).[6] It acts as a selective dual antagonist of the orexin OX1 and OX2 receptors.[6] The medication has an intermediate elimination half-life of 12 hours and a time to peak of about 2 to 3 hours.[2][6] Unlike benzodiazepines and Z-drugs, suvorexant does not interact with GABA receptors, instead having a distinct mechanism of action.[6][15]

Clinical development of suvorexant began in 2006[16] and it was introduced for medical use in 2014.[2][17] The medication is a schedule IV controlled substance in the United States and may have a modest potential for misuse.[18][2][19] In other places, such as Australia, suvorexant is a prescription-only medicine and is not a controlled drug.[1] Suvorexant is not available in generic formulations.[11][20][21] Besides suvorexant, other orexin receptor antagonists like lemborexant and daridorexant have also been introduced.[22][23]

  1. ^ a b Cite error: The named reference Belsomra-AU-Label was invoked but never defined (see the help page).
  2. ^ a b c d e f g h i j k l m n o p q r s "Belsomra- suvorexant tablet, film coated". DailyMed. Retrieved 30 January 2020.
  3. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  4. ^ "Regulatory Decision Summary for Belsomra". 23 October 2014.
  5. ^ a b Cite error: The named reference MerckSharpDohme2013 was invoked but never defined (see the help page).
  6. ^ a b c d e f g h i Jacobson LH, Callander GE, Hoyer D (November 2014). "Suvorexant for the treatment of insomnia". Expert Review of Clinical Pharmacology. 7 (6): 711–730. doi:10.1586/17512433.2014.966813. PMID 25318834. S2CID 41099462.
  7. ^ Cite error: The named reference DimovaBrarMen2014 was invoked but never defined (see the help page).
  8. ^ a b Cite error: The named reference pmid28365447 was invoked but never defined (see the help page).
  9. ^ a b Cite error: The named reference pmid26648692 was invoked but never defined (see the help page).
  10. ^ Cite error: The named reference pmid35843245 was invoked but never defined (see the help page).
  11. ^ a b Cite error: The named reference Drugs.com-Belsomra-Generic was invoked but never defined (see the help page).
  12. ^ Kishi T, Matsunaga S, Iwata N (2015). "Suvorexant for Primary Insomnia: A Systematic Review and Meta-Analysis of Randomized Placebo-Controlled Trials". PLOS ONE. 10 (8): e0136910. Bibcode:2015PLoSO..1036910K. doi:10.1371/journal.pone.0136910. PMC 4552781. PMID 26317363.
  13. ^ Cite error: The named reference pmid28994603 was invoked but never defined (see the help page).
  14. ^ Cite error: The named reference pmid32901578 was invoked but never defined (see the help page).
  15. ^ Atkin T, Comai S, Gobbi G (April 2018). "Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery". Pharmacological Reviews. 70 (2): 197–245. doi:10.1124/pr.117.014381. PMID 29487083. S2CID 3578916.
  16. ^ Cite error: The named reference pmid25406050 was invoked but never defined (see the help page).
  17. ^ Cite error: The named reference APDNews2014 was invoked but never defined (see the help page).
  18. ^ Cite error: The named reference FederalRegister2016 was invoked but never defined (see the help page).
  19. ^ Cite error: The named reference pmid25231363 was invoked but never defined (see the help page).
  20. ^ Cite error: The named reference pmid30092886 was invoked but never defined (see the help page).
  21. ^ Cite error: The named reference pmid26955275 was invoked but never defined (see the help page).
  22. ^ Cite error: The named reference pmid35043499 was invoked but never defined (see the help page).
  23. ^ Cite error: The named reference pmid35298826 was invoked but never defined (see the help page).