Azelastine 0.05% Ophth Solution 6ml
It is used to ease allergy signs in the eye.
Drug Class
Ophthalmic Antihistamine; Ophthalmic Mast Cell Stabilizer
Pharmacologic Class
H1-receptor antagonist; Mast cell stabilizer
Pregnancy Category
Category C
FDA Approved
Oct 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Azelastine ophthalmic solution is an eye drop used to relieve itchy, red, and watery eyes caused by allergies. It works by blocking substances in your body that cause allergic reactions 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. This medication is for eye use only.
Before Using
1. Wash your hands thoroughly before handling the medication.
2. Remove your contact lenses before applying the medication. You can put them back in 10 minutes after use, unless your eyes are irritated or infected.
Applying the Medication
1. Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
2. Tilt your head back and gently drop the medication into your eye.
3. After applying the medication, keep your eyes closed and apply gentle pressure to the inside corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
Storage and Disposal
Store the medication at room temperature or in the refrigerator. Do not freeze. Keep the container upright with the cap on and the lid tightly closed.
Missed Dose
If you miss a dose, use it as soon as you remember. However, if it's 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. This medication is for eye use only.
Before Using
1. Wash your hands thoroughly before handling the medication.
2. Remove your contact lenses before applying the medication. You can put them back in 10 minutes after use, unless your eyes are irritated or infected.
Applying the Medication
1. Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
2. Tilt your head back and gently drop the medication into your eye.
3. After applying the medication, keep your eyes closed and apply gentle pressure to the inside corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
Storage and Disposal
Store the medication at room temperature or in the refrigerator. Do not freeze. Keep the container upright with the cap on and the lid tightly closed.
Missed Dose
If you miss a dose, use it as soon as you remember. However, if it's 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 touching the dropper tip to your eye or any other surface to prevent contamination.
- Remove contact lenses before administering the drops and wait at least 10 minutes before reinserting them.
- Do not wear contact lenses if your eyes are red.
- If using other eye drops, wait at least 10 minutes between applications.
- Avoid known allergens (e.g., pollen, pet dander, dust mites) as much as possible.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
1 drop in each affected eye twice daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
seasonal allergic conjunctivitis:
1 drop in each affected eye twice daily, may be increased to 4 times daily if needed
perennial allergic conjunctivitis:
1 drop in each affected eye twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
3 years to 11 years: 1 drop in each affected eye twice daily
Adolescent:
12 years and older: 1 drop in each affected eye twice daily, may be increased to 4 times daily if needed
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed due to minimal systemic absorption
Moderate:
No adjustment needed due to minimal systemic absorption
Severe:
No adjustment needed due to minimal systemic absorption
Dialysis:
No specific considerations due to minimal systemic absorption
Hepatic Impairment:
Mild:
No adjustment needed due to minimal systemic absorption
Moderate:
No adjustment needed due to minimal systemic absorption
Severe:
No adjustment needed due to minimal systemic absorption
Pharmacology
Mechanism of Action
Azelastine is a phthalazinone derivative that exhibits H1-receptor antagonist activity and mast cell stabilizing effects. It inhibits the release of histamine and other mediators (e.g., leukotrienes, platelet-activating factor) from mast cells and other cells involved in the allergic response. It also reduces chemotaxis and activation of eosinophils and neutrophils.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption after ophthalmic administration. Peak plasma concentrations are typically in the picogram/mL range.
Tmax:
Not precisely quantifiable for ophthalmic use due to minimal systemic absorption; systemic Tmax for oral azelastine is 2-3 hours.
FoodEffect:
Not applicable for ophthalmic solution
Distribution:
Vd:
Approximately 14.5 L/kg (systemic, from oral data)
ProteinBinding:
Approximately 90% (systemic)
CnssPenetration:
Limited (for ophthalmic use, due to minimal systemic absorption)
Elimination:
HalfLife:
Approximately 22 hours (azelastine) and 54 hours (desmethylazelastine) after systemic administration; less relevant for ophthalmic use due to minimal systemic exposure.
Clearance:
Not precisely quantifiable for ophthalmic use due to minimal systemic absorption.
ExcretionRoute:
Primarily fecal (75%) and renal (25%) after systemic administration.
Unchanged:
Less than 10% (systemic)
Pharmacodynamics
OnsetOfAction:
Within minutes (typically 2-3 minutes)
PeakEffect:
2-3 minutes
DurationOfAction:
Up to 12 hours
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
If you experience any of the following severe side effects, contact your doctor immediately or seek emergency medical attention. Although rare, some individuals may be at risk for life-threatening reactions. Be aware of the following signs and symptoms:
Allergic reactions, which may include:
+ 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
As with any medication, side effects can occur. While many people may not experience any side effects or only minor ones, it's essential to be aware of the following:
Headache
Burning or stinging sensations
* Bad taste in your mouth
If any of these side effects or any others bother you or persist, contact your doctor for guidance. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects
To report side effects, you can contact your doctor or the FDA at 1-800-332-1088. You can also submit reports online at https://www.fda.gov/medwatch.
If you experience any of the following severe side effects, contact your doctor immediately or seek emergency medical attention. Although rare, some individuals may be at risk for life-threatening reactions. Be aware of the following signs and symptoms:
Allergic reactions, which may include:
+ 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
As with any medication, side effects can occur. While many people may not experience any side effects or only minor ones, it's essential to be aware of the following:
Headache
Burning or stinging sensations
* Bad taste in your mouth
If any of these side effects or any others bother you or persist, contact your doctor for guidance. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects
To report side effects, you can contact your doctor or the FDA at 1-800-332-1088. You can also submit reports online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Persistent or worsening eye irritation
- Eye pain
- Changes in vision
- Signs of eye infection (e.g., discharge, swelling, increased redness)
- Severe allergic reaction (e.g., rash, itching/swelling, severe dizziness, trouble breathing) - seek immediate medical attention.
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 and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting 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 and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. When taking this drug, exercise caution when driving or performing tasks that require clear vision to ensure your safety. This medication is not intended to treat irritation caused by contact lenses. If your eyes are red, avoid wearing contact lenses to prevent further irritation. If you are pregnant, planning to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Unlikely with ophthalmic use due to minimal systemic absorption.
- If accidentally ingested, symptoms may include drowsiness, confusion, lethargy, rapid heart rate, and low blood pressure.
What to Do:
If accidental ingestion occurs, especially in children, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention. Treatment is supportive.
Drug Interactions
Monitoring
Symptom Monitoring
- Ocular itching
- Ocular redness
- Tearing
- Foreign body sensation
- Photophobia
- Vision changes (report immediately)
- Eye pain (report immediately)
- Signs of infection (e.g., discharge, swelling, increased pain)
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Minimal systemic absorption is expected after ophthalmic administration.
Trimester-Specific Risks:
First Trimester:
Limited human data. Animal studies show adverse effects at high systemic doses. Minimal systemic absorption from ophthalmic use reduces risk.
Second Trimester:
Limited human data. Minimal systemic absorption from ophthalmic use reduces risk.
Third Trimester:
Limited human data. Minimal systemic absorption from ophthalmic use reduces risk.
Lactation
Considered low risk. Azelastine is excreted in breast milk after systemic administration, but systemic exposure from ophthalmic use is minimal, making infant exposure unlikely to be significant.
Infant Risk:
Low risk of adverse effects to the breastfed infant due to minimal systemic absorption by the mother.
Pediatric Use
Approved for use in children 3 years of age and older. Safety and efficacy in children younger than 3 years have not been established.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. No specific dosage adjustment is needed.
Clinical Information
Clinical Pearls
- Azelastine ophthalmic solution is a dual-acting agent, providing both antihistamine and mast cell stabilizing effects, which can lead to rapid onset of action and sustained relief.
- Patients should be instructed on proper instillation technique to maximize efficacy and minimize contamination.
- Advise patients not to wear contact lenses if their eyes are red, and to remove contact lenses before instilling azelastine, waiting at least 10 minutes before reinserting.
- While generally well-tolerated, some patients may experience transient burning or stinging upon instillation.
Alternative Therapies
- Other ophthalmic antihistamines (e.g., pheniramine/naphazoline)
- Ophthalmic mast cell stabilizers (e.g., cromolyn sodium, lodoxamide)
- Ophthalmic NSAIDs (e.g., ketorolac)
- Ophthalmic corticosteroids (for severe cases, short-term use)
- Oral antihistamines (e.g., loratadine, cetirizine, fexofenadine)
- Allergen avoidance strategies
Cost & Coverage
Average Cost:
Varies widely, typically $30-$100+ per 6ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (preferred or non-preferred brand/generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to 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 details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.