Epinastine

Epinastine is a topically active, direct H 1 -receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H 1 -receptor and has affinity for the histamine H 2 -receptor.

• Epinastine HCl ophthalmic solution is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine HCl ophthalmic solution is indicated for the prevention of itching associated with allergic conjunctivitis.ICD-10: H10.9

• None Nonecontraindicated

The recommended dosage is one drop in each eye twice a day. The recommended dosage is one drop in each eye twice a day. Treatment should be continued throughout the period of exposure (i.e., until the pollen season is over or until exposure to the offending allergen is terminated), even when symptoms are absent.

To minimize the risk of contamination, do not touch dropper tip to any surface. Keep bottle tightly closed when not in use. ( 5.1 ) Epinastine HCl should not be used to treat contact lens-related irritation. ( 5.2 ) Remove contact lenses prior to instillation of epinastine HCl.( 5.2 ) 5.1 Contamination of Tip and Solution Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to avoid contamination of the solution by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions. Bottle should be kept tightly closed when not in use. 5.2 Use with Contact Lenses Patients should be advised not to wear a contact lens if their eye is red. Epinastine HCl ophthalmic solution should not be used to treat contact lens-related irritation. The preservative in epinastine HCl, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of epinastine HCl ophthalmic solution and may be reinserted after 10 minutes following its administration. 5.3 Topical Ophthalmic Use Only Epinastine HCl ophthalmic solution is for topical ophthalmic use only and not for injection or oral use.

The most common ocular adverse reactions (incidence occurring in approximately 1% to 10% of epinastine HCl-treated eyes were burning sensation in the eye, folliculosis, hyperemia, and pruritus. The most common non-ocular adverse reactions, occurring in 10% epinastine HCl-treated eyes, were infection (cold symptoms and upper respiratory infections). To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at +1 800-417-9175 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. The most frequently reported ocular adverse reactions occurring in approximately 1 to 10% of patients were burning sensation in the eye, folliculosis, hyperemia, and pruritus. The most frequently reported non-ocular adverse reactions were infection (cold symptoms and upper respiratory infections), seen in approximately 10% of patients, and headache, rhinitis, sinusitis, increased cough, and pharyngitis, seen in approximately 1 to 3% of patients. Some of these reactions were similar to the underlying disease being studied. 6.2 Postmarketing Experience The following reactions have been identified during postmarketing use of epinastine HCl in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made.

8.1 Pregnancy: In an embryofetal developmental study in pregnant rats, maternal toxicity with no embryofetal effects was observed at an oral dose that was approximately 150,000 times the maximum recommended ocular human dose (MROHD) of 0.0014 mg/kg/day on a mg/kg basis. Total resorptions and abortion were observed in an embryofetal study in pregnant rabbits at an oral dose that was approximately 55,000 times the MROHD. In both studies, no drug-induced teratogenic effects were noted. Epinastine reduced pup body weight gain following an oral dose to pregnant rats that was approximately 90,000 times the MROHD. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, epinastine HCl ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. 8.3 Nursing Mothers A study in lactating rats revealed excretion of epinastine in the breast milk. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when epinastine HCl ophthalmic solution is administered to a nursing woman. 8.4 Pediatric Use Safety and effectiveness in pediatric patients below the age of 2 years have not been established.

Metabolism

Fourteen subjects, with allergic conjunctivitis, received one drop of epinastine HCl ophthalmic solution in each eye twice daily for seven days. On day seven, average maximum epinastine plasma concentrations of 0.04±0.014 ng/mL were reached after about two hours indicating low systemic exposure.

• Oct 31, 2011ANDAANDA090951Somerset Theraps Llc

1. 1Treatment Failure31729%
2. 2Pyrexia635.7%
3. 3Drug Ineffective544.9%
4. 4Diarrhoea494.4%
5. 5Pneumonia474.2%
6. 6Decreased Appetite464.1%
7. 7Anaemia373.3%
8. 8Rash373.3%
9. 9Malaise363.2%
10. 10Off Label Use333.0%
11. 11Hepatic Function Abnormal322.9%
12. 12Nausea282.5%
13. 13Platelet Count Decreased272.4%
14. 14Erythema262.3%
15. 15Drug Eruption252.3%

The 10 most recently updated of 20 ClinicalTrials.gov registrations naming Epinastine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Evaluate the Efficacy and Safety of Epinastine Hydrochloride Eye Drops in the Treatment of Chinese Seasonal Allergic Conjunctivitis Patients
  Completed · Phase 3 · Interventional · 266 enrolled · Zhaoke (Guangzhou) Ophthalmology Pharmaceutical Ltd.
  NCT06212973updated 2024-01-19
• Non-Pharmaceutical Treatment of Seasonal Allergic Conjunctivitis
  Completed · Phase 4 · Interventional · 18 enrolled · Aston University
  NCT01569191updated 2018-02-05
• Safety and Efficacy Study of Epinastine Nasal Spray in Subjects With Seasonal Allergic Rhinitis (P08648)
  Completed · Phase 3 · Interventional · 798 enrolled · Merck Sharp & Dohme LLC
  NCT00564421updated 2017-03-24
• Two Formulations and Concentrations of Epinastine Nasal Spray Versus Azelastine Nasal Solution for Allergic Rhinitis
  Completed · Phase 2 · Interventional · 131 enrolled · Merck Sharp & Dohme LLC
  NCT01382654updated 2015-11-02
• A Study of Epinastine Nasal Spray in Subjects With Seasonal Allergic Rhinitis
  Completed · Phase 2 · Interventional · 571 enrolled · Merck Sharp & Dohme LLC
  NCT00407927updated 2015-10-12
• Effectiveness of Olopatadine HCl Ophthalmic Solution for the Treatment of Allergic Conjunctivitis in Japan
  Completed · Phase 4 · Interventional · 50 enrolled · Alcon Research
  NCT02251613updated 2015-10-07
• Study of Two Marketed Ocular Anti-Allergy Medications in Subjects With Allergic Conjunctivitis
  Completed · Phase 4 · Interventional · 79 enrolled · Merck Sharp & Dohme LLC
  NCT00534794updated 2015-05-13
• Study of DE-114 Ophthalmic Solution in Patients With Allergic Conjunctivitis
  Completed · Phase 3 · Interventional · 87 enrolled · Santen Pharmaceutical Co., Ltd.
  NCT01363700updated 2014-11-19
• Dose Tolerance Study in Healthy Male Volunteers After Intranasal Application of Epinastine Nasal
  Completed · Phase 1 · Interventional · 39 enrolled · Boehringer Ingelheim
  NCT02260037updated 2014-10-09
• Bioequivalence of the New Formulation of WAL 801 CL Dry Syrup Compared to the Conventional Formulation of WAL 801 CL Dry Syrup in Healthy Male Volunteers
  Completed · Phase 1 · Interventional · 34 enrolled · Boehringer Ingelheim
  NCT02260050updated 2014-10-09

Frequently asked questions

How does Epinastine work?

Epinastine is a topically active, direct H 1 -receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H 1 -receptor and has affinity for the histamine H 2 -receptor.

What is Epinastine used for?

According to FDA labeling, Epinastine carries indications including: Epinastine HCl ophthalmic solution is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine HCl ophthalmic solution is indicated for the prevention of itching associated with allergic conjunctivitis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Epinastine?

Epinastine is classified as Other antiallergics, Other antihistamines for systemic use, Adrenergic Receptor Agonist, Histamine-1 Receptor Inhibitor, Adrenergic Agonists, Adrenergic alpha-Agonists, Histamine H1 Receptor Antagonists, Decreased Histamine Activity, Decreased Histamine Release.

What are the contraindications for Epinastine?

Epinastine labeling lists contraindications including: None None. Always consult the full prescribing information and a clinician.