Comparative Pharmacology
Head-to-head clinical analysis: DOXYLAMINE versus DOXYLAMINE SUCCINATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOXYLAMINE versus DOXYLAMINE SUCCINATE.
Doxylamine vs DOXYLAMINE SUCCINATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Doxylamine is a first-generation antihistamine with sedative properties. It acts as a competitive antagonist at histamine H1 receptors, thereby blocking the effects of histamine. It also possesses anticholinergic activity.
Antagonist at histamine H1 receptors, producing sedative and antihistaminic effects; also possesses anticholinergic properties.
12.5–25 mg orally at bedtime for insomnia; 25 mg orally every 4–6 hours as needed for allergies (max 150 mg/day).
6.25 to 25 mg orally every 4 to 6 hours as needed, not to exceed 150 mg per day.
None Documented
None Documented
10-12 hours; prolonged in elderly and hepatic impairment.
Clinical Note
moderateDoxylamine + Venlafaxine
"The risk or severity of adverse effects can be increased when Doxylamine is combined with Venlafaxine."
Clinical Note
moderateDoxylamine + Nefazodone
"The risk or severity of adverse effects can be increased when Doxylamine is combined with Nefazodone."
Clinical Note
moderateDoxylamine + Tranylcypromine
"Doxylamine may increase the anticholinergic activities of Tranylcypromine."
Clinical Note
moderateDoxylamine + Sertraline
Terminal elimination half-life ranges from 10 to 12 hours in adults. In elderly patients, half-life may be prolonged (up to 15-18 hours) due to reduced renal clearance.
Renal (approximately 60% as unchanged drug and metabolites, primarily as N-desmethyldoxylamine and other metabolites); biliary/fecal (minor).
Renal excretion of metabolites (30-60% as conjugated metabolites, <5% unchanged). Fecal elimination is minor (<10%).
Category A/B
Category C
Antihistamine (Sedating)
Antihistamine (Sedating)
"The risk or severity of adverse effects can be increased when Doxylamine is combined with Sertraline."