Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMKOXFE)

Drug Name

Doxylamine Drug Info

Synonyms

Dossilamina; Doxilamina; Doxilminio; Doxylaminum; Dossilamina [DCIT]; Diclectin (TN); Dolased (TN); Donormyl (TN); Dormidina (TN); Doxilminio [INN-Spanish]; Doxylamine (INN); Doxylamine [INN:BAN]; Doxylaminum [INN-Latin]; Dozile (TN); Evanorm (TN); Mersyndol (TN); Restavit (TN); Somnil (TN); Syndol (TN); Unisom-2 (TN); Phenyl-2-pyridylmethyl-beta-N,N-dimethylaminoethyl ether; N,N-Dimethyl-2-(1-phenyl-1-(2-pyridinyl)ethoxy)ethanamine; N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine; N,N-dimethyl-2-[(1-phenyl-1-pyridin-2-ylethyl)oxy]ethanamine; N,N-dimethyl-2-[1-phenyl-1-(pyridin-2-yl)ethoxy]ethanamine; 2-(alpha-(2-(Dimethylamino)ethoxy)-alpha-methylbenzyl)pyridine; 2-Dimethylaminoethoxyphenylmethyl-2-picoline

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Approved	[1]
Common cold	CA00	Approved	[1]
Morning sickness	SC00	Approved	[2]
Seasonal allergic rhinitis	CA08.01	Approved	[1]
Urticaria	EB00-EB05	Approved	[1]
Vasomotor/allergic rhinitis	CA08	Approved	[1]
Pruritus	EC90	Investigative	[1]

Therapeutic Class

Hypnotics and Sedatives

Cross-matching ID

PubChem CID: 3162
ChEBI ID: CHEBI:51380
CAS Number: CAS 469-21-6
TTD Drug ID: DMKOXFE
ACDINA Drug ID: D00216

Molecule-Related Drug Atlas

Molecule Type:

DTT

DOT

Drug Status:

Approved Drug(s)

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Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[5]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[6]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[7]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[8]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[9]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[7]
Doxepin	DMPI98T	Anxiety		Approved	[10]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[7]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[11]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[12]
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Drug(s) Affected By Phosphatidylcholine translocator ABCB4 (ABCB4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Paclitaxel	DMLB81S	Breast carcinoma		Approved	[13]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[14]
Methysergide	DM1EF73	Migraine	8A80	Approved	[4]
Clavulanate	DM2FGRT	Bacteremia	1A73	Approved	[15]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[16]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[4]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[17]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[18]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[19]
Omeprazole	DM471KJ	Cystic fibrosis	CA25	Approved	[20]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Antagonist	[3]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Phosphatidylcholine translocator ABCB4 (ABCB4)	OTE6PY83	MDR3_HUMAN	Gene/Protein Processing	[4]

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References

1	Doxylamine FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7171).
3	First-generation H1 antihistamines found in pilot fatalities of civil aviation accidents, 1990-2005. Aviat Space Environ Med. 2007 May;78(5):514-22.
4	Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
5	Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
6	Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
7	Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
8	Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
9	Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
10	Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
11	Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
12	Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
13	[Reversal effect of MDR1 and MDR3 gene silencing on resistance of A2780/taxol cells to paclitaxel]. Zhonghua Fu Chan Ke Za Zhi. 2007 Jun;42(6):412-6.
14	8-Methoxypsoralen disrupts MDR3-mediated phospholipids efflux and bile acid homeostasis and its relevance to hepatotoxicity. Toxicology. 2017 Jul 1;386:40-48. doi: 10.1016/j.tox.2017.05.011. Epub 2017 May 24.
15	Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
16	Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
17	Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
18	Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
19	Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
20	Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.