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Suvorexant
Medication used to treat insomnia / From Wikipedia, the free encyclopedia
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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]
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Trade names | Belsomra |
Other names | MK-4305; MK4305 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a614046 |
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Dependence liability | Low |
Addiction liability | Low |
Routes of administration | By mouth[2] |
Drug class | Orexin receptor antagonist; Hypnotic; Sedative |
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Bioavailability | 82% (10 mg; lower at higher doses)[2][5] |
Protein binding | 99.5%[6][2] |
Metabolism | Liver (CYP3A major, CYP2C19 minor)[2] |
Metabolites | Hydroxysuvorexant (inactive)[2] |
Elimination half-life | 12.2 hours (8–19 hours) (40 mg)[2][5][7] |
Excretion | Feces: 66%[2] Urine: 23%[2] |
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ECHA InfoCard | 100.210.546 ![]() |
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Formula | C23H23ClN6O2 |
Molar mass | 450.93 g·mol−1 |
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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]