Doxylamine
First-generation antihistamine used as a short-term sedative and hypnotic (sleep aid) / From Wikipedia, the free encyclopedia
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Doxylamine, sold under the brand name Unisom among others, is an antihistamine medication which is used in the treatment of insomnia and allergies. It is also used to treat morning sickness in pregnant women in combination with pyridoxine (vitamin B6). Doxylamine is available over-the-counter, and is used in nighttime cold medicines, such as NyQuil, as well as in pain medications containing acetaminophen and codeine, to help with sleep. The medication is taken by mouth.
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Trade names | Unisom, Vicks Formula 44 (in combination with Dextromethorphan), others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682537 |
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Routes of administration | By mouth |
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Bioavailability | Oral: 24.7%[1] Intranasal: 70.8%[1] |
Metabolism | Hepatic (CYP2D6, CYP1A2, CYP2C9)[2] |
Elimination half-life | 10–12 hours (range 7–15 hours)[2][3][4] |
Excretion | Urine (60%), feces (40%)[5] |
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ECHA InfoCard | 100.006.742 |
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Formula | C17H22N2O |
Molar mass | 270.376 g·mol−1 |
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Side effects of doxylamine include dizziness, drowsiness, grogginess, and dry mouth, among others.[6][4] Doxylamine is an antihistamine—specifically an inverse agonist of the histamine H1 receptor—and to a lesser extent an anticholinergic—specifically an antagonist of the muscarinic acetylcholine receptors M1 through M5. It is a first-generation antihistamine and crosses the blood–brain barrier into the brain, thereby producing centrally mediated sedative and hypnotic effects.
Doxylamine was first described in 1948 or 1949.[7] Several of the first-generation antihistamines, including doxylamine, are the most widely used sleep medications in the world.[8] Doxylamine is also a potent anticholinergic, which means it also works as a deliriant at much higher than recommended doses as a result.[9] Its sedative and deliriant effects have led to some cases of recreational use.