Pharmacologic Substance
doxylamine
Brand Names:
Aldex AN; Bonjesta; Diclegis; Nocto; Unisom; Wal-Som (doxylamine); Zzzquil Ultra
Effect:
Decreased Histamine Activity
May Treat:
Headache; Rhinitis, Allergic, Perennial; Sleep Initiation and Maintenance Disorders
More Information:
ChemID; DrugBank; DailyMed; DrugInfo; PDR
Definitions related to doxylamine:
  • A first generation ethanolamine with antiinflammatory, sedative and antihistamine properties. Doxylamine competitively inhibits the histamine 1 (H1) receptor, thereby preventing the action of endogenous histamine as well as the subsequent release of pro-inflammatory mediators from basophils and mast cells. This agent acts as an inverse agonist that combines with, and stabilizes the inactive form of the H1-receptor, shifting the H1 receptor equilibrium toward the inactive state. This results in downregulation of nuclear factor-kappaB (NF-kappaB) and NF-kappaB dependent antigen presentation, chemotaxis, as well as expression of cell-adhesion molecules and pro-inflammatory cytokines.
    NCI Thesaurus
    U.S. National Cancer Institute, 2021
  • Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM.
    NLM Medical Subject Headings
    U.S. National Library of Medicine, 2021
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