Overview
Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Indication
For the prevention of itching associated with allergic conjunctivitis.
Associated Conditions
- Allergic Conjunctivitis (AC)
Research Report
Epinastine: A Comprehensive Pharmacological and Clinical Monograph
1.0 Abstract
Epinastine is a second-generation, topically active antihistamine and mast cell stabilizer classified as a small molecule drug. It is distinguished by a multi-faceted mechanism of action that includes potent, direct antagonism of the histamine H1-receptor and inhibition of histamine release from mast cells. This dual activity provides both immediate and sustained relief from allergic symptoms. While it possesses affinity for other receptors, including H2, adrenergic, and serotonergic sites, its physicochemical properties prevent it from crossing the blood-brain barrier, resulting in a non-sedating profile that is a hallmark of its class. The primary approved therapeutic indication for its ophthalmic formulation is the prevention of ocular itching associated with allergic conjunctivitis. Clinical studies have demonstrated a rapid onset of action and a duration of effect that supports a convenient twice-daily dosing regimen. Pharmacokinetically, topical administration leads to high local concentrations in the tear film with minimal systemic absorption, which, combined with its limited metabolism, results in a favorable safety profile with a very low risk of systemic side effects or drug-drug interactions. Epinastine is generally well-tolerated, with the most common adverse events being localized ocular effects. It is available globally under various brand names, and in the United States, generic formulations are marketed following the discontinuation of the original brand, Elestat®.
2.0 Chemical Identity and Physicochemical Properties
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2024/01/19 | Phase 3 | Completed | Zhaoke (Guangzhou) Ophthalmology Pharmaceutical Ltd. | ||
2014/10/09 | Phase 1 | Completed | |||
2014/10/09 | Phase 1 | Completed | |||
2014/09/29 | Phase 4 | Completed | |||
2014/07/08 | Phase 1 | Completed | |||
2014/07/08 | Phase 3 | Completed | |||
2011/06/27 | Phase 2 | Completed | |||
2007/11/28 | Phase 3 | Completed | |||
2007/09/26 | Phase 4 | Completed | |||
2007/06/21 | Phase 4 | Withdrawn | Hom, Milton M., OD, FAAO |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Somerset Therapeutics, LLC | 70069-008 | OPHTHALMIC | 0.5 mg in 1 mL | 11/9/2023 | |
Breckenridge Pharmaceutical, Inc. | 51991-836 | OPHTHALMIC | 0.5 mg in 1 mL | 11/1/2021 | |
Sun Pharmaceutical Industries, Inc. | 62756-329 | OPHTHALMIC | 0.5 mg in 1 mL | 10/24/2018 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
No EMA approvals found for this drug. |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
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No HSA approvals found for this drug. |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
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No NMPA approvals found for this drug. |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
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No PPB approvals found for this drug. |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
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No TGA approvals found for this drug. |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
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No Health Canada approvals found for this drug. |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
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No CIMA AEMPS (Spain) approvals found for this drug. |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Philippines FDA approvals found for this drug. |
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Saudi SFDA approvals found for this drug. |
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Malaysia NPRA approvals found for this drug. |
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
---|---|---|---|---|---|
No UK EMC drug information found for this drug. |
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