Doxylamine Succinate

(BANM, rINNM)
Doxylamine Succinate Chemical formula
Synonyms: Doksilamin Süksinat; Doksilamino-vandenilio sukcinatas; Doksylamiinivetysuksinaatti; Doxilamin-hidrogén-szukcinát; Doxylamine Hydrogen Succinate; Doxylamine, hydrogénosuccinate de; Doxylamine, Succinate de; Doxylamin-hydrogen-sukcinát; Doxylamini hydrogenosuccinas; Doxylamini Succinas; Doxylaminium Succinate; Doxylaminvätesuccinat; Histadoxylamine Succinate; Succinato de doxilamina. NN-Dimethyl-2-[
Cyrillic synonym: Доксиламина Суксинат.

💊 Chemical information

Chemical formula: C17H22N2O,C4H6O4 = 388.5.
CAS — 469-21-6 (doxylamine); 562-10-7 (doxylamine succinate).
ATC — R06AA09.
ATC Vet — QR06AA09.

Pharmacopoeias.

In Eur. and US.

Ph. Eur. 6.2

(Doxylamine Hydrogen Succinate; Doxylamine Succinate BP 2008). A white or almost white powder. Very soluble in water; freely soluble in alcohol.

USP 31

(Doxylamine Succinate). A white or creamy-white powder having a characteristic odour. Soluble 1 in 1 of water, 1 in 2 of alcohol and of chloroform, and 1 in 370 of ether; very slightly soluble in benzene. Protect from light.

💊 Adverse Effects and Precautions

Overdosage.

In an evaluation of 109 cases of intoxication with doxylamine,1 no correlation was found between the amount ingested or plasma concentration and the frequency or extent of symptoms. The most common symptom was impaired consciousness. Psychotic behaviour, seizures, and antimuscarinic symptoms such as tachycardia and mydriasis were also observed. Rhabdomyolysis occurred in one patient and was accompanied by transient impairment of renal function. The same group commented2 that rhabdomyolysis had been noted in 7 of 442 cases of doxylamine overdosage, with an associated rise in plasma creatine kinase and myoglobinuria, and suggested that doxylamine has a direct toxic effect on striated muscle.
1. Köppel C, et al. Poisoning with over-the-counter doxylamine preparations: an evaluation of 109 cases. Hum Toxicol 1987; 6: 355–9
2. Köppel C, et al. Rhabdomyolysis in doxylamine overdose. Lancet 1987; i: 442–3.

💊 Pharmacokinetics

After oral doses of doxylamine succinate peak plasma concentrations occur after 2 to 3 hours. An elimination half-life of about 10 hours has been reported.
1. Friedman H, et al. Clearance of the antihistamine doxylamine: reduced in elderly men but not in elderly women. Clin Pharmacokinet 1989; 16: 312–16.

💊 Uses and Administration

Doxylamine succinate, a monoethanolamine derivative, is a sedating antihistamine with antimuscarinic and pronounced sedative effects. Doxylamine succinate is given for the symptomatic relief of hypersensitivity reactions, in pruritic skin disorders, as a hypnotic in the short-term treatment of insomnia, and as an ingredient of compound preparations for symptomatic treatment of coughs and the common cold. In general it is no longer used in the management of nausea and vomiting of early pregnancy. Oral doses of up to 25 mg of doxylamine succinate have been given every 4 to 6 hours to a maximum of 150 mg daily. The usual hypnotic dose is 25 mg orally at night.

💊 Preparations

USP 31: Acetaminophen, Dextromethorphan Hydrobromide, Doxylamine Succinate, and Pseudoephedrine Hydrochloride Oral Solution; Doxylamine Succinate Syrup; Doxylamine Succinate Tablets.

Proprietary Preparations

Austral.: Dozile; Restavit; Canad.: Unisom-2; Chile: Calmex; Dorminoctil; Nocpaz; Trimepaz†; Zarcop; Cz.: Hoggar N†; Fr.: Donormyl; Lidene; Noctyl; Ger.: Gittalun; Hewedormir doxyl intens†; Hoggar Night; Mereprine; Munleit†; SchlafTabs; Sedaplus; India: Rest-Aid; Israel: Sleep Aid; Unisom; NZ: Dozile; Philipp.: Unisom; Port.: Dormidina; S.Afr.: Equi-Sleep†; Restwel; Somnil; Spain: Dormidina; Switz.: Sanalepsi N; Turk.: Unisom; USA: Aldex AN; Unisom SleepTabs. Multi-ingredient: Austral.: Analgesic/Calmative; Codalgin Plus; Dimetapp Cold, Cough & Flu; Dolased Analgesic Calmative; Dolased Day/Night Pain Relief; Fiorinal; Mersyndol; Ordov Migradol†; Panadeine Plus; Panalgesic; Austria: Wick Erkaltungs-Saft fur die Nacht; Wick Hustensaft; Belg.: Pholco-Mereprine; Braz.: Broncolex†; EMS Expectorante; Hytos Plus; Revenil; Revenil Dospan; Revenil Expectorante; Silencium; Silomat Plus†; Canad.: Dalmacol; Diclectin; Mersyndol with Codeine; Neo Citran Cold & Flu†; Nighttime; Nighttime Cold & Flu; Nyquil Sinus; NyQuil†; ratioCalmydone; Regular Strength Sinus Medication; Tylenol Sinus (Nighttime Relief); Vicks Nyquil Cold & Flu; Cz.: Wick Medinait†; Fr.: DolirhumePro; Ger.: Paedisup; Wick Medinait; India: Doxinate; Vominate; Indon.: Dexmolex; Siladex; Irl.: Syndol; Ital.: Vicks Medinait; NZ: Dimetapp Cold, Cough & Flu Day & Night†; Mersyndol; Pryndette†; Pol.: Tabcin Impakt; Port.: Nausefe; S.Afr.: Abflex; Acurate; Adco-Dol; Asic; B-Dol; Betapyn; Cepacol; Codoxol; Doxsyn; Forpyn†; Lenapain; Nethaprin Dospan; Nethaprin Expectorant; Nomopain; Paxidal; Pynclear†; Pynstop; Sedapain; Sedi nol; Syndol; Tensopyn; Vicks Medinite; Xerotens†; Spain: Cariban; Medinait; Vicks Medinait†; Switz.: Vicks Medinait; Turk.: Vicks MediNait; UK: Painex; Propain Plus; Syndol; Vicks Medinite; USA: Alka-Seltzer Plus NightTime Cold; All-Nite Cold Formula; Genite; Night Time Cold/Flu Relief; Nite Time Cold Formula; NyQuil Hot Therapy; NyQuil Nighttime Cold/Flu; Nytcold Medicine; Vicks NyQuil LiquiCaps; Vicks NyQuil Multi-Symptom Cold Flu Relief; Vicks NyQuil Sinus; Venez.: Mercindol.
Published December 09, 2018.