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Epinastine hydrobromide
[CAS# 127786-29-2]

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Identification
ClassificationAPI >> Other chemicals
NameEpinastine hydrobromide
Synonyms(+/-)-3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine hydrobromide
Molecular StructureCAS # 127786-29-2, Epinastine hydrobromide
Molecular FormulaC16H15N3.HBr
Molecular Weight330.23
CAS Registry Number127786-29-2
EC Number821-693-3
SMILESC1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Br
Safety Data
Hazard Symbolssymbol   GHS07 Warning  Details
Risk StatementsH302  Details
Safety StatementsP264-P270-P301+P317-P330-P501  Details
Hazard Classification
up    Details
HazardClassCategory CodeHazard Statement
Acute toxicityAcute Tox.4H302
up Discovery and Applications
Epinastine hydrobromide is a chemical compound that is primarily used in the treatment of allergic conditions such as allergic rhinitis and conjunctivitis. As a second-generation antihistamine, it is designed to alleviate symptoms such as sneezing, runny nose, and itchy eyes, without causing the sedative effects typically associated with first-generation antihistamines. Its development and application have contributed significantly to the management of allergic conditions, improving the quality of life for many individuals.

The discovery of epinastine hydrobromide can be traced to the ongoing efforts in antihistamine research. Histamine, a naturally occurring substance in the body, is involved in allergic reactions by binding to histamine receptors, leading to symptoms such as inflammation and itching. The development of epinastine hydrobromide involved the design of a selective H1 receptor antagonist that could effectively block histamine activity without crossing the blood-brain barrier, which is responsible for the sedative effects of older antihistamines. This selective activity, along with the compound’s low sedative potential, made it a desirable candidate for treating allergy symptoms.

Epinastine hydrobromide works by competitively inhibiting histamine at the H1 receptor sites, preventing histamine from binding and initiating the allergic response. Unlike many other antihistamines, epinastine hydrobromide has a longer duration of action, providing extended relief from allergic symptoms. It is typically administered in oral or ocular forms, with eye drops being used to treat allergic conjunctivitis and oral tablets used for allergic rhinitis. Its use has been associated with a low incidence of central nervous system side effects, making it an attractive option for patients who require long-term treatment.

In addition to its primary use in allergic conditions, epinastine hydrobromide has also been explored for its potential applications in other areas of medicine. For example, it has shown some promise in modulating inflammation in conditions like asthma and atopic dermatitis. Research into its broader therapeutic effects continues, as scientists investigate its interactions with other biological pathways and potential roles in conditions beyond allergic responses.

Overall, epinastine hydrobromide is an important antihistamine that has significantly advanced the treatment of allergic diseases. Its development exemplifies the trend toward creating more selective and effective medications with fewer side effects, providing an improved therapeutic option for patients suffering from allergies.

References

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