Suvorexant

Suvorexant
Clinical data
Trade names	Belsomra
Other names	MK-4305; MK4305
AHFS/Drugs.com	Monograph
MedlinePlus	a614046
License data	US DailyMed: Suvorexant;
Pregnancy; category	AU: B3;
Dependence; liability	Low
Addiction; liability	Low
Routes of; administration	By mouth
Drug class	Orexin receptor antagonist; Hypnotic; Sedative
ATC code	N05CJ01 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; US: Schedule IV;
Pharmacokinetic data
Bioavailability	82% (10 mg; lower at higher doses)
Protein binding	99.5%
Metabolism	Liver (CYP3A major, CYP2C19 minor)
Metabolites	Hydroxysuvorexant (inactive)
Elimination half-life	12.2 hours (8–19 hours) (40 mg)
Excretion	Feces: 66%; Urine: 23%
Identifiers
	IUPAC name [(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	1030377-33-3 ;
PubChem CID	24965990;
IUPHAR/BPS	2890;
DrugBank	DB09034 ;
ChemSpider	24662178 ;
UNII	081L192FO9;
KEGG	D10082 ;
ChEBI	CHEBI:82698;
ChEMBL	ChEMBL1083659 ;
CompTox Dashboard (EPA)	DTXSID90145616 ;
ECHA InfoCard	100.210.546
Chemical and physical data
Formula	C23H23ClN6O2
Molar mass	450.93 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl;
	InChI 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 ; Key:JYTNQNCOQXFQPK-MRXNPFEDSA-N ;
	(verify)

Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication which is 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 by mouth.

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 12 hours and a time to peak of about 2 to 3 hours. Unlike benzodiazepines and Z-drugs, suvorexant does not interact with GABA receptors, instead having a distinct mechanism of action.

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

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