Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects

Pradhan, Shilpi; Abhishek, Kumar S; Mah, Francis S.

doi:10.1517/17425250903117284

Cited by 12 publications

(9 citation statements)

References 34 publications

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“…A number of topical antihistamines are available, including azelastine, 26 emedastine, 27 epinastine, 28 and levocabastine. These medications do not affect other proinflammatory mediators, such as prostaglandins and leukotrienes, which remain uninhibited.…”

Section: Diagnosis Of Sac and Pacmentioning

confidence: 99%

Seasonal and Perennial Allergic Conjunctivitis

Freitas¹

2013

Ocular Surface Disease: Cornea, Conjunctiva and Tear Film

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Section: Diagnosis Of Sac and Pacmentioning

confidence: 99%

Seasonal and Perennial Allergic Conjunctivitis

Freitas¹

2013

Ocular Surface Disease: Cornea, Conjunctiva and Tear Film

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“…Other dual-acting agents, including Zatidor (ketotifen fumarate 0.025%; CIBA Vision, Duluth, GA) [31,32], Optivar (azelastine hydrochloride 0.05%; Muro Pharmaceutical, Tewksbury, MA) [33], and Elestat (epinastine hydrochloride 0.05%; Allergan, Irvine, CA) [34], were all FDA approved between 1999 and 2003, closely following the introduction of olopatadine. Although all of these are classified as dual-action antihistamines, each has some unique spectrum of activities.…”

Section: Dual-acting Antihistamine/mast Cell-stabilizing Moleculesmentioning

confidence: 99%

Antihistamines in Ocular Allergy: Are They All Created Equal?

Abelson

McLaughlin

Gomes

2011

Curr Allergy Asthma Rep

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Use of topical antihistamines in the treatment of allergic conjunctivitis has evolved over the past several decades as our knowledge of the nature of the underlying disease has progressed. Formulations for the eye typically employ H(1)-receptor antagonists with a dual action, both directly as competitors for histamine receptor occupancy and as mast cell-stabilizing agents. Many of these compounds also display activity against late-phase allergic symptoms. Of the newest available drugs, several have a prolonged duration of action allowing once-daily dosing. Future development is likely to focus on long-acting agents such as these and on drugs that can target additional histamine receptor subtypes.

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“…Reduction in itching and vasodilation were resulted by the competitive binding of 1 to histamine receptor sites. Furthermore, 1 acts as mast cells degranulation inhibitor by limiting the discharge of inflammatory mediators like histamine, eosinophil, and platelet‐activating factor …”

Section: Introductionmentioning

confidence: 99%

Novel Hybrid Molecules of Epinastine and Mefenamic Acid for Bioactive Assessment as Potential Anti‐inflammatory Agents

Lee

Damodar

Lee

et al. 2020

Bulletin Korean Chem Soc

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A set of novel epinastine (1) and mefenamic acid (2) hybrids (3-7) tethered via amide bond were designed and synthesized with the artistry of molecular hybridization. Then their inhibitory effect on nitric oxide (NO) production in LPS-induced RAW-264.7 macrophages and the expression levels of prostaglandin (PG) synthesis regulatory genes were evaluated in vitro. All the hybrids were found to have remarkable NO production inhibitory potential with IC 50 values ranging in between 27.69 AE 3.06 and 40.19 AE 5.52 μM without notable cytotoxicity (CC 50 ≥ 100 μM) except 6. Comparing the inhibitory effects, cytotoxicity and in vitro efficacy index (iEI), 4 (IC 50 = 32.09 AE 4.04 μM; iEI = 6.23) and 7 (IC 50 = 27.69 AE 3.06 μM; iEI = 6.40) were better suited than other hybrids as well as their parent compounds EH and MA. This outcome was further harmonized with the reduced microsomal prostaglandin E synthase-1 expression and unaltered housekeeping COX-1 expression by hybrids 4 and 7 treatment. Altogether, our findings signify that hybrids 4 and 7 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.

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Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects

Abstract: Epinastine 0.05% ophthalmic solution was found to be a safe and effective medication for the relief of symptoms of allergic conjunctivitis. Epinastine demonstrates very low CNS and cardiac toxicity.

Cited by 12 publications

References 34 publications

Seasonal and Perennial Allergic Conjunctivitis

Seasonal and Perennial Allergic Conjunctivitis

Antihistamines in Ocular Allergy: Are They All Created Equal?

Novel Hybrid Molecules of Epinastine and Mefenamic Acid for Bioactive Assessment as Potential Anti‐inflammatory Agents

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