Doxylamine 

Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia^[1][2][3].

Doxylamine (administered daily via diet for 7 or 15 days at doses of 40-1500 ppm) acts as a phenobarbital-type inducer of hepatic microsomal cytochrome P450 in B6C3F1 mice, with a maximum 38-fold induction of CYP2B activity; at the highest dose, it also alters thyroid hormone homeostasis by decreasing serum T₄ and increasing serum TSH^[1].
Doxylamine (1-2 mg; 4% solution (25 μL); oral administration; intravenous injection; intranasal administration; single dose) shows a bioavailability of 70.8% via intranasal delivery in male Sprague-Dawley rats, with rapid absorption and no nasal epithelial damage^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

270.37

C₁₇H₂₂N₂O

469-21-6

CC(C1=NC=CC=C1)(C2=CC=CC=C2)OCCN(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bookstaff RC, et al. Effects of doxylamine succinate on thyroid hormone balance and enzyme induction in mice. Toxicol Appl Pharmacol. 1996;141(2):584-594.

  [2]. Nuangchamnong N, et al. Doxylamine succinate-pyridoxine hydrochloride (Diclegis) for the management of nausea and vomiting in pregnancy: an overview. Int J Womens Health. 2014;6:401-409.

  [3]. Pelser A, et al. Comparative pharmacokinetics of single doses of doxylamine succinate following intranasal, oral and intravenous administration in rats. Biopharm Drug Dispos. 2002;23(6):239-244.