DOXYLAMINE — Wikipedia

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Doxylamine
Image illustrative de l’article Doxylamine
Enantiomer r from doxylamine (left) and S-Doxylamine (right)
Identification
UICPA name ( RS )- N , N -Dimethyl-2- (1-phenyl-1-pyridin-2-yl-ethoxy) -Tethanamine
N O CAS 469-21-6 (Racemic)
76210-49-6 (+)
76210-47-4 ( -)
N O Echa 100.006.742
N O THIS 207-414-2
Code ATC R06 AA09
DrugBank DB00366
Pubchem 3162
SMILES
Inches
Chemicals
Formula C 17 H 22 N 2 O [Isomers]
Molar mass [ first ] 270.369 4 ± 0.015 8 g/mol
C 75,52 %, H 8,2 %, N 10,36 %, O 5,92 %,
Physical properties
T° fusion 25 °C [ 2 ]
Ecotoxicology
DL 50 470 mg · kg -first (mouse, oral)
62 mg · kg -first (mouse, i.v.)
460 mg · kg -first (mouse, s.c.) [ 2 ]
Pharmacokinetic data
Half-life of élim. 10h
Excretion
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essentially urinary

Therapeutic considerations
Therapeutic class Antihistamine h first for systemic use • sedative
Car driving prohibited (level 3)
Psychotropic character
Category sedative
Way of consuming

Oral

Risk of dependence Weak
IS units and CNTP , unless otherwise stated.
modifier Consultez la documentation du modèle

The doxylamine is an antihistamine h first (Histamine H1 receptor  (in) ) first generation; It is used for the treatment of allergies, light insomnia as well as nausea induced by pregnancy [ 3 ] (considered outside the AMM in France).

Today first -generation antihistamines are no longer used in first intention to treat allergies, they are preferred to antihistamines of second and third generation specific hints of receptors first peripherals thus eliminating the sedative effect generally unwanted when processing allergies. This is why doxylamine is only indicated in treatment of occasional insomnia. Doxylamine, with significant sedative properties, reduces the sleeping time and avoids night awakenings.

Its anti-emotional properties also allow it to be prescribed as anti-nausea. It is used in pyridoxin/doxylamine combination to treat nausea and vomiting of pregnancy [ 4 ] .

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A treatment based on doxylamine does not require any prescription, however an extension of treatment beyond five days requires the advice of a doctor. The intake of doxylamine alters the level of vigilance and increases the risk of falling. It makes you unfit for domestic and professional work, as well as to the driving of any vehicle.

Doxylamine is classified “A” in terms of its fetal safety by the reference guide Briggs on fetal and neonatal risk [ 5 ] .

Although it is customary to say that doxylamine causes no dependence or addiction, it can be nuanced [ 6 ] .

Antihistamines h first , or reverse agonist of H receptors first (in) , reduce the effects of histamine. First generation antihistamines are not specific to peripheral receptors, they therefore also act on H receptors first of the central nervous system.

  1. ↑ Molar mass calculated after ‘ Atomic weights of the elements 2007 » , on www.chem.qmul.ac.uk .
  2. ↑ a et b (in) ‘ Doxylamine » , on Chedplus , consulted on July 29, 2009
  3. ↑ ‘ https://www.ncbi.nlm.nih.gov/pmc/articles/pmc4030125/ » , on lecrat.fr (consulted the )
  4. ↑ (in) Svetlana Madjunk , Caroline Maltepe you gideon Koren , ‘ The Delayed-Release Combination of Doxylamine and Pyridoxine (Diclegis®/Diclectin®) for the Treatment of Nausea and Vomiting of Pregnancy » , Pediatric Drugs , vol. 16, n O 3, , p. 199–211 (ISSN  1174-5878And 1179-2019, DOI  10.1007/s40272-014-0065-5, read online , consulted the )
  5. ↑ (in) Briggs GG, Freeman RK, Yaffe SJ. Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk , 8th edition. 2008. Published by: Lippincott Williams & Wilkins.
  6. ↑ “Dependence is set up (…) with many users. This poses several problems. First, the effectiveness of sedative antihistamines was evaluated in the short term and nothing guarantees their effectiveness beyond a few days or a few weeks, “said Professor Anne Roussin. [Drugs without a prescription, user manual] on Slate.fr of November 12, 2013

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