Roidipedia.Compound reference & reporting
06 AUG 2026
CompoundsOther Doxylamine
OtherOTC sleep aidFirst-generation antihistamineAnticholinergic

Doxylamine

Also known as Unisom SleepTabs · Restavit · Diclegis/Diclectin component (with pyridoxine)

First-generation sedating antihistamine sold OTC for insomnia (Unisom SleepTabs) and, with pyridoxine, for pregnancy nausea. Longer-acting and more sedating than diphenhydramine, with the same anticholinergic drawbacks and rapid tolerance.

01 Overview

Doxylamine is a first-generation ethanolamine H1 antihistamine widely used as an OTC hypnotic (brand Unisom SleepTabs). It is also combined with vitamin B6 (pyridoxine) in prescription products for nausea and vomiting of pregnancy, one of the few sleep-adjacent agents considered safe in pregnancy.

As a sleep aid it is at least as sedating as diphenhydramine and has a longer half-life, which increases both efficacy for occasional use and the likelihood of next-morning hangover. As with all sedating antihistamines, tolerance to the hypnotic effect develops within days, and its anticholinergic profile makes it unsuitable for regular use or for older adults.

02 Mechanism

Central histamine H1 receptor antagonism suppresses histaminergic arousal; substantial muscarinic antagonism accounts for anticholinergic effects.

03 Dosing

TierDoseRouteNotes
Sleep aid25 mgOral25 mg ~30 min before bed; for short-term occasional use.

04 Effects

EffectMagnitudeEvidence
Sedation / reduced sleep onset latencyStrongly sedating; shortens time to fall asleep for occasional use.Clinical
Antiemetic effect (with pyridoxine)Combined with vitamin B6 it reduces nausea and vomiting of pregnancy, a distinct approved use.Clinical

05 Side effects

EffectSeverityFrequencyEvidenceCountermeasures
Rapid toleranceHypnotic effect fades within several nights of continuous use.MildNearly universal with nightly useClinical
Prolonged next-day sedation (hangover)Long half-life produces marked next-morning drowsiness and impaired alertness.ModerateCommonClinical
Anticholinergic effectsDry mouth, constipation, blurred vision, and urinary retention.ModerateCommonClinical

07 References

Doxylamine succinate as a nighttime sleep aid: efficacy reviewCurr Med Res Opin, 1990s review
American Geriatrics Society Beers Criteria (anticholinergics)J Am Geriatr Soc, 2023 update

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.