Elestat 0.05% Ophth Solution 5ml
It is used to treat eye irritation due to allergies.
Drug Class
Antihistamine, Ophthalmic
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 eyes caused by allergies. It works by blocking a natural substance called histamine that causes allergic symptoms, and also helps to stabilize cells that release histamine.
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 Instructions
Apply this medication to your eyes only.
Remove contact lenses before using the medication. You can put them back in 10 minutes after application, but avoid doing so if your eyes are irritated or infected.
Wash your hands before and after using the medication.
To prevent contamination, avoid touching the container tip to your eye, lid, or other skin, as this can lead to bacterial infection and potentially 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. This helps the medication stay in your eye.
Important Safety Precautions
Do not use the medication if the solution changes 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 Instructions
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 Instructions
Apply this medication to your eyes only.
Remove contact lenses before using the medication. You can put them back in 10 minutes after application, but avoid doing so if your eyes are irritated or infected.
Wash your hands before and after using the medication.
To prevent contamination, avoid touching the container tip to your eye, lid, or other skin, as this can lead to bacterial infection and potentially 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. This helps the medication stay in your eye.
Important Safety Precautions
Do not use the medication if the solution changes 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 Instructions
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
- Do not wear contact lenses if your eyes are red. If you wear soft contact lenses, remove them before applying the drops and wait at least 10 minutes before reinserting them.
- Avoid touching the dropper tip to any surface to prevent contamination.
- If using other eye drops, wait at least 5 minutes between applications.
- Store at room temperature, away from light and moisture.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
One drop in each affected eye twice daily
Condition-Specific Dosing:
allergicConjunctivitis:
One drop in each affected eye twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established (safety and efficacy not established in children under 2 years of age)
Child:
One drop in each affected eye twice daily (âĨ2 years of age)
Adolescent:
One drop in each affected eye twice daily
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Dialysis:
No adjustment needed (minimal systemic absorption)
Hepatic Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Pharmacology
Mechanism of Action
Epinastine is a topically active, direct H1-receptor antagonist and mast cell stabilizer. It inhibits histamine release from mast cells and blocks H1 receptors, thereby preventing the effects of histamine on conjunctival blood vessels and nerve endings, which are responsible for the itching associated with allergic conjunctivitis.
Pharmacokinetics
Absorption:
Bioavailability:
Not applicable (topical ophthalmic, minimal systemic absorption)
Tmax:
Not quantifiable (plasma concentrations generally below limit of quantification)
FoodEffect:
Not applicable
Distribution:
Vd:
Not quantifiable (minimal systemic absorption)
ProteinBinding:
Not quantifiable (minimal systemic absorption)
CnssPenetration:
Limited (minimal systemic absorption)
Elimination:
HalfLife:
Not quantifiable (plasma concentrations generally below limit of quantification)
Clearance:
Not quantifiable (minimal systemic absorption)
ExcretionRoute:
Primarily renal (for systemically absorbed drug, but minimal absorption)
Unchanged:
Not quantifiable (minimal systemic absorption)
Pharmacodynamics
OnsetOfAction:
Within minutes to 30 minutes
PeakEffect:
Within 3-6 hours
DurationOfAction:
Up to 12 hours (allows for twice-daily dosing)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. Immediately contact your doctor or seek medical attention if you notice any of the following symptoms, which could indicate a serious reaction:
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
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in eyesight, 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 side effects or only have mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they persist or bother you:
Burning sensation
Excessive tearing
* Symptoms of a common cold
Important Note
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor for guidance. 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. Immediately contact your doctor or seek medical attention if you notice any of the following symptoms, which could indicate a serious reaction:
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
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in eyesight, 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 side effects or only have mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they persist or bother you:
Burning sensation
Excessive tearing
* Symptoms of a common cold
Important Note
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor for guidance. 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:
- Persistent or worsening eye irritation or pain
- Changes in vision
- New eye infections or discharge
- Severe allergic reactions (e.g., rash, itching/swelling, severe dizziness, trouble breathing) - though rare with ophthalmic use.
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 is crucial to ensure safe use and avoid potential interactions.
* Any existing health problems, as this medication may interact with other medical conditions.
To guarantee your safety, carefully review all your medications and health issues with your doctor and pharmacist. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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 is crucial to ensure safe use and avoid potential interactions.
* Any existing health problems, as this medication may interact with other medical conditions.
To guarantee your safety, carefully review all your medications and health issues with your doctor and pharmacist. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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 caused by contact lenses. 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 doctor will help you weigh the benefits and risks of using this medication during this time, considering both your health and the health of your baby.
Do not use this medication to treat irritation caused by contact lenses. 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 doctor will help you weigh the benefits and risks of using this medication during this time, considering both your health and the health of your baby.
Overdose Information
Overdose Symptoms:
- Unlikely to occur with ophthalmic use due to minimal systemic absorption. If accidentally ingested, symptoms might include drowsiness, dry mouth, or gastrointestinal upset, but severe toxicity is not expected.
What to Do:
If accidental ingestion occurs, contact a poison control center or seek medical attention. For ocular overdose, flush eyes with water. Call 1-800-222-1222
Drug Interactions
Monitoring
Routine Monitoring
Ocular symptoms (itching, redness)
Frequency: Regularly during treatment
Target: Reduction or resolution of symptoms
Action Threshold: Persistent or worsening symptoms, or new ocular irritation
Ocular irritation/discomfort
Frequency: Regularly during treatment
Target: Absence or mild, transient irritation
Action Threshold: Severe or persistent irritation, pain, or vision changes
Symptom Monitoring
- Ocular itching
- Ocular redness
- Ocular burning/stinging
- Foreign body sensation
- Tearing
- Blurred vision
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high systemic doses, but human data are limited and systemic absorption from ophthalmic use is minimal.
Trimester-Specific Risks:
First Trimester:
Limited data, minimal systemic absorption suggests low risk.
Second Trimester:
Limited data, minimal systemic absorption suggests low risk.
Third Trimester:
Limited data, minimal systemic absorption suggests low risk.
Lactation
Caution should be exercised when epinastine ophthalmic solution is administered to a nursing woman. It is unknown whether epinastine is excreted in human milk, but systemic absorption is minimal, suggesting low infant exposure.
Infant Risk:
Low risk (L3 - Moderately safe, but monitor infant for potential effects like drowsiness, though unlikely due to minimal systemic absorption).
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 of age.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. Dosage adjustment is generally not necessary.
Clinical Information
Clinical Pearls
- Epinastine offers a dual mechanism of action (antihistamine and mast cell stabilizer), providing both rapid relief and sustained control of allergic conjunctivitis symptoms.
- Patients should be instructed on proper eye drop instillation technique to maximize efficacy and minimize contamination.
- Due to its minimal systemic absorption, epinastine ophthalmic solution has a favorable systemic safety profile and is unlikely to cause systemic side effects or drug interactions.
- It is a good option for patients seeking a twice-daily dosing regimen for allergic conjunctivitis.
Alternative Therapies
- Olopatadine ophthalmic (e.g., Pataday, Patanol)
- Azelastine ophthalmic (e.g., Optivar)
- Ketotifen ophthalmic (e.g., Zaditor, Alaway)
- Cromolyn sodium ophthalmic (e.g., Crolom)
- Nedocromil sodium ophthalmic (e.g., Alocril)
- Bepotastine ophthalmic (e.g., Bepreve)
- Alcaftadine ophthalmic (e.g., Lastacaft)
Cost & Coverage
Average Cost:
$50 - $150 per 5ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (for brand), Tier 1 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, 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 this 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 seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.