Clinical medicine profile
Epinastine
Therapeutic agent (verify pharmacological class)
- Route
- OPHTHALMIC
- Schedule
- POM
- ATC
- Not assigned
- PPB status
- registered
Safety essentials
The information most likely to change a prescribing or dispensing decision.
Contraindications
- Hypersensitivity to the active substance or excipients.
- Additional absolute contraindications are indication- and product-specific — consult SmPC.
Precautions
- 5 WARNINGS AND PRECAUTIONS 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.
Dosing matrix
Population and organ-function guidance, shown together for faster comparison.
2 DOSAGE AND ADMINISTRATION 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.
8.4 Pediatric Use Safety and effectiveness in pediatric patients below the age of 2 years have not been established.
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Use, effects & interactions
Indications
- 1 INDICATIONS AND USAGE 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.
Adverse effects
- (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.
- The reactions, which have been chosen for inclusion due to either their seriousness, frequency of reporting, possible causal connection to epinastine HCl, or a combination of these factors, include: lacrimation increased.
Drug interactions
Open multi-drug checker ↗- Professional use: confirm indication, dose, duration, monitoring and patient counselling points against current Kenya STG / EML and the product SmPC.
- Document allergy status and key interactions.
Mechanism & disposition
12.
Read complete mechanism
12.1 Mechanism of Action 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 also possesses affinity for the ɑ 1 , ɑ 2 -, and 5-HT 2 -receptors.
Product-specific
Product-specific
OPHTHALMIC
with multiple dosing. Epinastine is 64% bound to plasma proteins. The total systemic clearance is approximately 56 L/hr and the terminal plasma
half-life is about 12 hours. Epinastine is mainly excreted unchanged. About 55% of an intravenous dose is recovered unchanged in the urine with about 30% in feces. Less than 10% is metabolized. The renal elimination is mainly via active tubular secretion.
is about 12 hours. Epinastine is mainly excreted unchanged. About 55% of an intravenous dose is recovered unchanged in the urine with about 30% in feces. Less than 10% is metabolized. The renal
Pregnancy, lactation & diet
8 USE IN SPECIFIC POPULATIONS 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. 8.5 Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients.
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.
Brands & loaded prices
| Brand | Manufacturer | Pack | Observed price |
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| No reviewed brand listings are linked yet. | |||
Sources & review state
Decision support only. Confirm patient-specific decisions against the current product SmPC, Kenya STG/EML, and professional judgement.