Azelastine 0.1%(137mcg) Nasal-200sp
It is used to ease allergy signs.It is used to treat a runny nose.
Drug Class
Antihistamine, Nasal
Pharmacologic Class
H1-receptor antagonist; Mast cell stabilizer
Pregnancy Category
Category C
FDA Approved
Oct 1996
DEA Schedule
Not Controlled
Overview
What is this medicine?
Azelastine nasal spray is an antihistamine that helps relieve symptoms of seasonal and year-round allergies, like runny nose, sneezing, and itchy nose. It works by blocking a natural substance called histamine that your body makes during an allergic reaction.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. Continue using the medication as directed, even if your symptoms improve.
Administration
This medication is for nasal use only. Do not take it by mouth.
Avoid getting the medication in your mouth or eyes, as it may cause burning.
Before using, blow your nose to ensure proper administration.
Spray the medication up your nose, avoiding the septum (the wall between the nostrils).
If you experience a bitter taste, try tilting your head downward while using the medication.
Priming the Pump
Some products may require priming the pump before use. Follow the instructions provided by your doctor or the manufacturer.
If you haven't used the pump for a while, you may need to prime it again. Refer to the instructions or consult your doctor for guidance.
Cleaning and Maintenance
After use, clean the spray tip with a clean tissue or cloth.
If the spray tip becomes clogged, follow the cleaning instructions provided by your doctor or the manufacturer, or refer to the package insert.
Storage and Disposal
Store the medication upright at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding bathrooms and areas prone to moisture.
Store all medications in a safe location, out of reach of children and pets.
Missed Dose
If you miss a dose, use it as soon as you remember.
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 once or take extra doses to make up for a missed dose.
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. Continue using the medication as directed, even if your symptoms improve.
Administration
This medication is for nasal use only. Do not take it by mouth.
Avoid getting the medication in your mouth or eyes, as it may cause burning.
Before using, blow your nose to ensure proper administration.
Spray the medication up your nose, avoiding the septum (the wall between the nostrils).
If you experience a bitter taste, try tilting your head downward while using the medication.
Priming the Pump
Some products may require priming the pump before use. Follow the instructions provided by your doctor or the manufacturer.
If you haven't used the pump for a while, you may need to prime it again. Refer to the instructions or consult your doctor for guidance.
Cleaning and Maintenance
After use, clean the spray tip with a clean tissue or cloth.
If the spray tip becomes clogged, follow the cleaning instructions provided by your doctor or the manufacturer, or refer to the package insert.
Storage and Disposal
Store the medication upright at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding bathrooms and areas prone to moisture.
Store all medications in a safe location, out of reach of children and pets.
Missed Dose
If you miss a dose, use it as soon as you remember.
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 once or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Avoid alcohol and other medications that cause drowsiness while using azelastine, as it can increase sedation.
- Use consistently as prescribed, even if symptoms improve.
- Prime the pump before first use or if not used for several days by spraying into the air until a fine mist appears.
- Blow your nose gently before using the spray.
- Tilt your head slightly forward and insert the nozzle into one nostril, pointing slightly away from the septum. Close the other nostril. Spray while sniffing gently.
- Avoid tilting your head back after spraying to prevent the bitter taste.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
2 sprays (137 mcg/spray) per nostril twice daily
Dose Range:
274 - 548 mg
Condition-Specific Dosing:
seasonalAllergicRhinitis:
2 sprays (137 mcg/spray) per nostril twice daily
vasomotorRhinitis:
2 sprays (137 mcg/spray) per nostril twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
5 to 11 years: 1 spray (137 mcg/spray) per nostril twice daily
Adolescent:
12 years and older: 2 sprays (137 mcg/spray) per nostril twice daily
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No specific recommendations due to low systemic absorption; use with caution
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
Use with caution; systemic exposure may be increased, though data for nasal spray is limited.
Pharmacology
Mechanism of Action
Azelastine is a phthalazinone derivative that exhibits potent H1-receptor antagonist activity. It also inhibits the release of histamine and other mediators (e.g., leukotrienes, kinins) from mast cells and other inflammatory cells. It has anti-inflammatory properties and reduces capillary permeability.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 40% (systemic after nasal administration)
Tmax:
2-3 hours
FoodEffect:
Not applicable for nasal administration
Distribution:
Vd:
14.5 L/kg
ProteinBinding:
Approximately 88%
CnssPenetration:
Limited (low levels in CSF)
Elimination:
HalfLife:
Approximately 22 hours (azelastine); 54 hours (desmethylazelastine)
Clearance:
Not readily quantifiable for nasal administration due to low systemic absorption
ExcretionRoute:
Primarily feces (75%), minor renal excretion (25%)
Unchanged:
Less than 10% (renal)
Pharmacodynamics
OnsetOfAction:
Within 30 minutes (for symptomatic relief)
PeakEffect:
3-6 hours
DurationOfAction:
Up to 12 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
- Eye irritation
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor 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:
- Nose or throat irritation
- Sneezing
- Burning or stinging sensations
- Drowsiness
- Headache
- Cough
- Changes in taste
- Dry mouth
- Nosebleed
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor for medical advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
- Eye irritation
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor 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:
- Nose or throat irritation
- Sneezing
- Burning or stinging sensations
- Drowsiness
- Headache
- Cough
- Changes in taste
- Dry mouth
- Nosebleed
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor for medical advice. 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:
- Severe drowsiness or dizziness
- Nosebleeds that do not stop
- Signs of an allergic reaction (rash, itching/swelling, severe dizziness, trouble breathing)
- Worsening of nasal symptoms
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 allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is vital to verify that it is safe to take this medication with all your current medications and health conditions. Always consult your doctor before starting, stopping, or changing the dose of any medication.
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 allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.
To ensure your safety, it is vital to verify that it is safe to take this medication with all your current medications and health conditions. Always consult your doctor before starting, stopping, or changing the dose of any medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you. If you have recently undergone nose surgery, experienced a nose injury, or have nose ulcers or sores, consult with your doctor. While taking this medication, refrain from consuming alcohol. Prior to using marijuana, other cannabis products, or prescription or over-the-counter drugs that may cause drowsiness, discuss the potential risks with your doctor. If you accidentally ingest this medication orally, immediately seek medical attention or contact a poison control center. If you are pregnant, planning to become pregnant, or are breast-feeding, inform your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Drowsiness
- Dizziness
- Confusion
- Tachycardia (fast heart rate)
- Hypotension (low blood pressure)
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is generally supportive and symptomatic.
Drug Interactions
Moderate Interactions
- CNS depressants (e.g., alcohol, sedatives, hypnotics, anxiolytics, other antihistamines): May cause additive CNS depression (drowsiness, impaired performance).
- Cimetidine: May increase azelastine plasma concentrations due to inhibition of CYP450 enzymes.
Monitoring
Routine Monitoring
Symptom relief (nasal congestion, rhinorrhea, sneezing, itching)
Frequency: Regularly throughout treatment
Target: Reduction or resolution of symptoms
Action Threshold: Lack of improvement or worsening of symptoms after appropriate trial period
Adverse effects (e.g., bitter taste, epistaxis, somnolence, headache)
Frequency: Regularly, especially during initial treatment
Target: Absence or tolerability of side effects
Action Threshold: Intolerable side effects or signs of significant CNS depression
Symptom Monitoring
- Nasal congestion
- Rhinorrhea (runny nose)
- Sneezing
- Nasal itching
- Post-nasal drip
- Headache
- Drowsiness/Somnolence
- Bitter taste
- Epistaxis (nosebleed)
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show developmental toxicity at high doses.
Second Trimester:
Limited human data; animal studies show developmental toxicity at high doses.
Third Trimester:
Limited human data; animal studies show developmental toxicity at high doses.
Lactation
Azelastine is excreted in breast milk in animals. Caution should be exercised when azelastine nasal spray is administered to a nursing mother. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for azelastine and any potential adverse effects on the breastfed infant.
Infant Risk:
Low to moderate risk (L3). Potential for infant drowsiness or irritability, though systemic absorption from nasal spray is low.
Pediatric Use
Approved for children 5 years and older for seasonal allergic rhinitis and 12 years and older for vasomotor rhinitis. Dosing varies by age group. Safety and efficacy not established in children younger than 5 years.
Geriatric Use
No specific dose adjustment is generally needed. However, elderly patients may be more susceptible to the sedative effects of antihistamines; monitor for drowsiness and falls.
Clinical Information
Clinical Pearls
- Azelastine nasal spray can cause a bitter taste, which is a common reason for non-adherence. Proper administration technique (tilting head slightly forward, not sniffing too hard) can help minimize this.
- While systemic absorption is low, azelastine can still cause drowsiness, especially when combined with alcohol or other CNS depressants.
- It has a relatively rapid onset of action (within 30 minutes) compared to some other allergy medications.
- Unlike nasal corticosteroids, azelastine is not indicated for non-allergic rhinitis (unless specifically vasomotor rhinitis).
- Patients should be advised to prime the pump before first use or if it hasn't been used for several days to ensure a consistent spray.
Alternative Therapies
- Other nasal antihistamines (e.g., Olopatadine nasal spray)
- Nasal corticosteroids (e.g., Fluticasone, Mometasone, Budesonide)
- Oral antihistamines (e.g., Loratadine, Fexofenadine, Cetirizine)
- Mast cell stabilizers (e.g., Cromolyn sodium nasal spray)
- Leukotriene receptor antagonists (e.g., Montelukast)
- Immunotherapy (allergy shots/sublingual tablets)
Cost & Coverage
Average Cost:
Varies, typically $50-$150 per 30.5 mL (200 sprays) bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (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 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.