Doxylamine
- Atc Codes:R06AA09
- CAS Codes:562-10-7#469-21-6
- PHARMGKB ID:562-10-7#469-21-6
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
France: Donormyl, Lidene, Noctyl; Germany: Gittalun, Hoggar Night, Mereprine, Schlafsterne, Schlaftabs, Sedaplus, Valacordin-Doxylamin; Ireland: Doxylamine; Lithuania: Valacordin-Doxylamin; Portugal: Dormidina; Spain: Dormidina.
North America
Canada: Unisom-2; USA: Doxylamine, Unisom-Chattem.
Drug combinations
Doxylamine and Pyridoxine (Vitamin B~6~)
Doxylamine, Acetaminophen, and Dextromethorphan
Doxylamine, Acetaminophen, Dextromethorphan, and Ephedrine
Doxylamine, Acetaminophen, Dextromethorphan, and Pseudoephedrine
Chemistry
Doxylamine Succinate: C~17~H~22~N~2~O C~4~H~6~O~4~. Mw: 388.46. (1) Ethanamine, N,N-dimethyl-2-[1-phenyl-1-(2-pyridinyl)ethoxy]-, butanedioate (1:1); (2) 2-[α[2-(Dimethylamino)ethoxy]-α-methylbenzyl]pyridine succinate (1:1). CAS-562-10-7; CAS-469-21-6 (doxylamine).
Pharmacologic Category
First Generation Antihistamines; Histamine H~1~ Antagonist. Anxiolytics, Sedatives, and Hypnotics; Miscellaneous. (ATC-Code: R06AA09).
Mechanism of action
Doxylamine is an ethanolamine-derivative, first generation antihistamine. The drug competes with histamine for H~1~-receptor sites on effector cells. Blocks chemoreceptor trigger zone, diminishes vestibular stimulation, and depresses labyrinthine function through its central anticholinergic activity.
Therapeutic use
Due to its sedative effect, it is used in the short-term management of insomnia. The drug is also used in combination with antitussives and decongestants for the temporary relief of cold and cough symptoms.
Pregnancy and lactiation implications
Approved for use in pregnancy-associated nausea and vomiting. Doxylamine may be excreted in breast milk, potentially resulting in sedative effects in nursing infants.
Unlabeled use
Contraindications
Hypersensitivity to doxylamine or any component of the formulation.
Warnings and precautions
May cause CNS depression. Use with caution in cardiovascular disease (including hypertension and ischemic heart disease). Use with caution, if at all, in angle-closure glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction. Use with caution in patients who have a breathing problem (e.g. emphysema, chronic bronchitis). Use generally not recommended in asthmatics who previously experienced a serious antihistamine-induced adverse bronchopulmonary effect. Risk of marked drowsiness. Possible excitability (especially in children). Some preparations may contain the dye tartrazine (possible allergic reactions in susceptible individuals (e.g. those sensitive to aspirin)). Should not be used in premature or full-term neonates (may experience CNS stimulation rather than sedation). Use of the drug in children younger than 2 years of age is not recommended. Use as an antihistamine only under the direction of a clinician in children 2 to <6 years of age. Possible increased risk of dizziness, sedation, and hypotension if used in the elderly.