Epinastine 0.05% Ophth Sol 5ml
It is used to treat eye irritation due to allergies.
Drug Class
Ophthalmic Antihistamine
Pharmacologic Class
H1-receptor antagonist; Mast cell stabilizer
Pregnancy Category
Category C
FDA Approved
Sep 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Epinastine is an eye drop used to relieve itchy, red, and watery eyes caused by allergies. It works by blocking natural substances (histamine) in your body that cause allergic symptoms and by stabilizing cells that release these substances.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Use the medication as directed, even if your symptoms improve.
Administration
Apply this medication to your eyes only.
Remove your contact lenses before using the medication. You can put them back in 10 minutes after application, unless your eyes are irritated or infected.
Wash your hands before and after using the medication.
Avoid touching the container tip to your eye, lid, or other skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
Tilt your head back and gently drop the medication into your eye.
After application, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Do not use the medication if the solution has changed color.
Storage and Disposal
Store the medication at room temperature with the lid tightly closed.
Keep all medications in a safe place, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on the best disposal method, and consider participating in local drug take-back programs.
Missed Dose
If you miss a dose, use it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
* Do not use two doses at the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Use the medication as directed, even if your symptoms improve.
Administration
Apply this medication to your eyes only.
Remove your contact lenses before using the medication. You can put them back in 10 minutes after application, unless your eyes are irritated or infected.
Wash your hands before and after using the medication.
Avoid touching the container tip to your eye, lid, or other skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
Tilt your head back and gently drop the medication into your eye.
After application, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Do not use the medication if the solution has changed color.
Storage and Disposal
Store the medication at room temperature with the lid tightly closed.
Keep all medications in a safe place, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on the best disposal method, and consider participating in local drug take-back programs.
Missed Dose
If you miss a dose, use it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
* Do not use two doses at the same time or take extra doses.
Lifestyle & Tips
- Avoid rubbing your eyes, as this can worsen irritation and symptoms.
- Avoid known allergens (e.g., pollen, pet dander, dust mites) as much as possible.
- Remove contact lenses before applying the eye drops and wait at least 10 minutes before reinserting them.
- Do not touch the dropper tip to your eye or any other surface to prevent contamination.
- If using other eye drops, wait at least 5 minutes between applications.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
1 drop in each affected eye twice daily
Condition-Specific Dosing:
allergicConjunctivitis:
1 drop in each affected eye twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
1 drop in each affected eye twice daily (2 years of age and older)
Adolescent:
1 drop in each affected eye twice daily
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed (minimal systemic absorption)
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Pharmacology
Mechanism of Action
Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of histamine release from mast cells. It exhibits high selectivity for the H1-receptor and has no activity at alpha-1, alpha-2, or dopamine receptors. It also has low affinity for H2-receptors and muscarinic cholinergic receptors.
Pharmacokinetics
Absorption:
Bioavailability:
Not quantifiable (minimal systemic absorption)
Tmax:
Not applicable (minimal systemic absorption)
FoodEffect:
Not applicable
Distribution:
Vd:
Not applicable (minimal systemic absorption)
ProteinBinding:
Not applicable (minimal systemic absorption)
CnssPenetration:
Limited (minimal systemic absorption)
Elimination:
HalfLife:
Not applicable (minimal systemic absorption)
Clearance:
Not applicable (minimal systemic absorption)
ExcretionRoute:
Not applicable (minimal systemic absorption)
Unchanged:
Not applicable (minimal systemic absorption)
Pharmacodynamics
OnsetOfAction:
Within minutes
PeakEffect:
3-5 minutes
DurationOfAction:
Up to 12 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
- Changes in vision, eye pain, or severe eye irritation
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
- Burning sensation
- Excessive tearing
- Symptoms of a common cold
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
- Changes in vision, eye pain, or severe eye irritation
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
- Burning sensation
- Excessive tearing
- Symptoms of a common cold
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Worsening eye irritation or pain
- Changes in vision
- Signs of eye infection (e.g., pus, severe redness, swelling)
- Persistent or severe headache (rare, but reported)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor assess potential interactions between this medication and other substances.
* Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your other medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor assess potential interactions between this medication and other substances.
* Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is crucial to verify that this medication can be taken safely with all your other medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Do not use this medication to treat irritation or discomfort associated with contact lens use. Additionally, avoid wearing contact lenses if you have red eyes, as this may exacerbate the condition.
If you are pregnant, planning to become pregnant, or are currently breast-feeding, it is crucial to discuss this with your doctor. Your healthcare provider will need to weigh the benefits and risks of using this medication during this time to ensure the best possible outcome for both you and your baby.
Do not use this medication to treat irritation or discomfort associated with contact lens use. Additionally, avoid wearing contact lenses if you have red eyes, as this may exacerbate the condition.
If you are pregnant, planning to become pregnant, or are currently breast-feeding, it is crucial to discuss this with your doctor. Your healthcare provider will need to weigh the benefits and risks of using this medication during this time to ensure the best possible outcome for both you and your baby.
Overdose Information
Overdose Symptoms:
- Unlikely with ophthalmic use due to minimal systemic absorption.
- Possible local irritation, redness, or discomfort if excessive drops are used.
What to Do:
If an overdose is suspected, rinse the eye with lukewarm water. If swallowed, contact a poison control center (e.g., 1-800-222-1222) or seek medical attention immediately, though systemic toxicity is highly unlikely.
Drug Interactions
Monitoring
Baseline Monitoring
Ocular examination
Rationale: To assess baseline severity of allergic conjunctivitis symptoms (redness, itching, swelling, discharge).
Timing: Prior to initiation of therapy
Routine Monitoring
Symptom relief (ocular itching, redness)
Frequency: Daily or as needed
Target: Reduction or resolution of symptoms
Action Threshold: If symptoms worsen or do not improve after several days of use, re-evaluate diagnosis or treatment.
Ocular irritation/discomfort
Frequency: Daily or as needed
Target: Minimal to no irritation
Action Threshold: Discontinue if severe or persistent irritation occurs.
Symptom Monitoring
- Ocular itching
- Ocular redness
- Ocular swelling
- Ocular discharge
- Foreign body sensation
- Blurred vision (rare)
Special Patient Groups
Pregnancy
Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption following ophthalmic administration is minimal.
Trimester-Specific Risks:
First Trimester:
Risk cannot be ruled out; minimal systemic exposure suggests low risk.
Second Trimester:
Risk cannot be ruled out; minimal systemic exposure suggests low risk.
Third Trimester:
Risk cannot be ruled out; minimal systemic exposure suggests low risk.
Lactation
L3 (Moderately safe). It is not known whether epinastine is excreted in human milk. However, systemic absorption is minimal, making infant exposure unlikely to be significant. Use with caution.
Infant Risk:
Low risk due to minimal systemic absorption in the mother.
Pediatric Use
Safety and efficacy have been established in pediatric patients 2 years of age and older. Not recommended for use in children younger than 2 years.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. No specific dose adjustment is required.
Clinical Information
Clinical Pearls
- Epinastine is a dual-acting agent, providing both antihistaminic and mast cell stabilizing effects, which can offer rapid relief and sustained control of allergic conjunctivitis symptoms.
- Patients should be instructed on proper instillation technique to avoid contamination of the dropper tip and to ensure optimal drug delivery.
- Advise patients to remove soft contact lenses prior to instillation and wait at least 10 minutes before reinserting them, as the preservative (benzalkonium chloride) can be absorbed by soft lenses.
- While generally well-tolerated, transient burning or stinging upon instillation is a common side effect.
Alternative Therapies
- Olopatadine ophthalmic (e.g., Pataday, Patanol)
- Azelastine ophthalmic (e.g., Optivar)
- Ketotifen ophthalmic (e.g., Zaditor)
- Cromolyn sodium ophthalmic (e.g., Crolom)
- Nedocromil sodium ophthalmic (e.g., Alocril)
- Bepotastine ophthalmic (e.g., Bepreve)
- Alcaftadine ophthalmic (e.g., Lastacaft)
- Topical ophthalmic NSAIDs (e.g., ketorolac) for inflammation
- Oral antihistamines (for systemic allergy symptoms)
Cost & Coverage
Average Cost:
Variable, typically $30-$100 for generic 5ml bottle per 5ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic formulations; Tier 3 or higher for brand-name
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about your medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.