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Chemistry

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Also known as: 87233-61-2, Emadine, Emedastine [inn], Emedastina, Emedastinum, Emedastinum [inn-latin]

Molecular Formula

C₁₇H₂₆N₄O

Molecular Weight

302.4 g/mol

InChI Key

KBUZBQVCBVDWKX-UHFFFAOYSA-N

FDA UNII

9J1H7Y9OJV

Emedastine is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Emedastine is a Histamine-1 Receptor Inhibitor. The mechanism of action of emedastine is as a Histamine H1 Receptor Antagonist.

1 2D Structure

Emedastine

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole

2.1.2 InChI

InChI=1S/C17H26N4O/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20/h4-5,7-8H,3,6,9-14H2,1-2H3

2.1.3 InChI Key

KBUZBQVCBVDWKX-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CCOCCN1C2=CC=CC=C2N=C1N3CCCN(CC3)C

2.2 Other Identifiers

2.2.1 UNII

9J1H7Y9OJV

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole Difumarate

2. Emadine

3. Emedastine Difumarate

4. Kb 2413

5. Kb-2413

6. Kg 2413

7. Kg-2413

2.3.2 Depositor-Supplied Synonyms

1. 87233-61-2

2. Emadine

3. Emedastine [inn]

4. Emedastina

5. Emedastinum

6. Emedastinum [inn-latin]

7. Emedastina [inn-spanish]

8. 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1h-benzo[d]imidazole

9. 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole

10. Emedastine (inn)

11. 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)benzimidazole

12. Emadine (tn)

13. Chembl594

14. 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole

15. 9j1h7y9ojv

16. Chebi:4779

17. 1-(2-ethoxy-ethyl)-2-(4-methyl-[1,4]diazepan-1-yl)-1h-benzoimidazole

18. 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1h-1,3-benzodiazole

19. Emedastine [inn:ban]

20. Ncgc00181341-01

21. Unii-9j1h7y9ojv

22. 1-methyl-4-(1-(2-ethoxyethyl)-1h-benzimidazo)-2-yl)(1,4)diazepane

23. Emedastine [mi]

24. Emedastine [vandf]

25. Emedastine [who-dd]

26. Schembl29770

27. Emedastine [ema Epar]

28. Gtpl7174

29. Dtxsid7048243

30. Hms3886o14

31. Amy25237

32. Bcp20085

33. Ex-a1371

34. Zinc1530912

35. 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1h-benzimidazole

36. Bdbm50019624

37. Mfcd00865647

38. S5659

39. Akos037515523

40. Ccg-267493

41. Db01084

42. 1h-benzimidazole, 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)-

43. Ac-35544

44. Bs-17691

45. Hy-108411

46. Cs-0028590

47. Ft-0693271

48. C07785

49. D07890

50. D81889

51. 233e612

52. L001093

53. Q5370305

54. Brd-k15010214-313-01-6

55. 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl) Benzimidazole

56. 1-methyl-4-(1-(2-ethoxyethyl)-1h-benzimidazol-2-yl)[1,4]diazepane

2.4 Create Date

2005-03-25

3 Chemical and Physical Properties

Molecular Formula	C₁₇H₂₆N₄O
Molecular Weight	302.4 g/mol
XLogP3	2.2
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	5
Exact Mass	302.21066147 g/mol
Monoisotopic Mass	302.21066147 g/mol
Topological Polar Surface Area	33.5 Å²
Heavy Atom Count	22
Formal Charge	0
Complexity	341
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Emadine
PubMed Health	Emedastine Difumarate (Into the eye)
Drug Classes	Ophthalmologic Agent
Drug Label	EMADINE (emedastine difumarate ophthalmic solution) 0.05% is a sterile ophthalmic solution containing emedastine, a relatively selective, H1-receptor antagonist for topical administration to the eyes. Emedastine difumarate is a white, crystalline,...
Active Ingredient	Emedastine difumarate
Dosage Form	Solution/drops
Route	Ophthalmic
Strength	0.05%
Market Status	Prescription
Company	Alcon

2 of 2
Drug Name	Emadine
PubMed Health	Emedastine Difumarate (Into the eye)
Drug Classes	Ophthalmologic Agent
Drug Label	EMADINE (emedastine difumarate ophthalmic solution) 0.05% is a sterile ophthalmic solution containing emedastine, a relatively selective, H1-receptor antagonist for topical administration to the eyes. Emedastine difumarate is a white, crystalline,...
Active Ingredient	Emedastine difumarate
Dosage Form	Solution/drops
Route	Ophthalmic
Strength	0.05%
Market Status	Prescription
Company	Alcon

4.2 Drug Indication

For the temporary relief of the signs and symptoms of allergic conjunctivitis.

FDA Label

Symptomatic treatment of seasonal allergic conjunctivitis.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Emedastine is a relatively selective H₁-receptor antagonist.

5.2 MeSH Pharmacological Classification

Anti-Allergic Agents

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)

Histamine H1 Antagonists

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

EMEDASTINE

5.3.2 FDA UNII

9J1H7Y9OJV

5.3.3 Pharmacological Classes

Established Pharmacologic Class [EPC] - Histamine-1 Receptor Inhibitor

5.4 ATC Code

S01GX06

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

S - Sensory organs

S01 - Ophthalmologicals

S01G - Decongestants and antiallergics

S01GX - Other antiallergics

S01GX06 - Emedastine

5.5 Absorption, Distribution and Excretion

Absorption

Ophthalmic use of emedastine usually does not produce measurable plasma concentrations.

Route of Elimination

Following oral administration, approximately 44% of the total dose can be recovered in the urine over the 24-hour period, with only 3.6% of the dose excreted as unchanged form. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms.

5.6 Metabolism/Metabolites

Two primary metabolites, 5-hydroxyemedastine and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. Minor metabolites include the 5'-oxoanalogs of 5-hydroxyemedastine and 6-hydroxy-emedastine and the N-oxide.

5.7 Biological Half-Life

The elimination half-life in the plasma is 3-4 hours following oral administration.

5.8 Mechanism of Action

Emedastine is a relatively selective, histamine H₁ antagonist. In vitro examinations of emedastine's affinity for histamine receptors demonstrate relative selectivity for the H₁ histamine receptor. In vivo studies have shown concentration-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration. Emedastine appears exert negligible effects on adrenergic, dopaminergic and serotonin receptors.

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