Azelastine (Nasal Spray): Uses, Dosage, Side Effects

What Is Azelastine Nasal Spray?

Azelastine nasal spray is a commonly prescribed medication that helps relieve allergy-related nasal symptoms, including sneezing, a runny nose, and nasal congestion. It is often prescribed for individuals with seasonal allergies, such as those caused by pollen, or year-round allergies, including those triggered by dust and pet dander. This spray works quickly to make breathing easier and provide comfort from irritating nasal symptoms. Azelastine nasal spray was approved by the FDA in 1996 and has since been a trusted option for managing nasal allergies.

• How Does Azelastine Nasal Spray Work: Azelastine nasal spray works by blocking the chemicals in your body that cause allergy symptoms. When sprayed in the nose, it helps reduce sneezing, a runny nose, and nasal congestion, making it easier to breathe and feel comfortable.
• Drug Group: Azelastine nasal spray belongs to the antihistamine group of medicines.

What Is the Use of Azelastine Nasal Spray?

Azelastine nasal spray is a medication that helps relieve allergy symptoms, such as sneezing, a runny nose, and a stuffy nose. It is safe for people 12 years and older and can be used for seasonal allergies (like pollen) or year-round allergies (like dust or pets)

Dosage Forms and Available Strengths

Azelastine nasal spray is available as a nasal spray with a concentration of 0.15%. It comes in bottles designed for easy nasal use.

Warnings and Precautions

• Activities That Require Focus: Some people using Azelastine nasal spray may experience drowsiness. Avoid driving, operating machinery, or engaging in any activity that requires full attention after using it. Do not use it with alcohol or other medicines that make you sleepy, as this can make drowsiness worse.

For Patients

How to Use Azelastine Safely?

Azelastine comes as a liquid spray for your nose. You spray it in each nostril once or twice a day, precisely as the doctor tells you. Do not use more or less than the prescribed amount.

• For Children Under 12: An adult should assist them in using it.

• For Kids Under Six: Do not use the over-the-counter spray.

• Use it only in your nose; do not swallow, spray it in your eyes, or spray it in your mouth.

• Do not share your spray bottle with anyone else to prevent the spread of germs.

Steps to Use:

• Read the directions that come with your spray.

• Remove the cap and safety clip.

• Prime the pump before first use: hold the bottle upright and press the pump down 4 times until a fine mist appears. If you haven’t used it for three or more days, spray it twice to reprime.

• Blow your nose gently.

• Gently close one nostril, lean your head forward, place the spray in the other nostril, press the pump, and breathe in softly.

• Repeat for the other nostril.

• If your doctor instructed you to use two sprays per nostril, repeat the step.

• Clean the tip with a tissue, then replace the cap and safety clip.

What Are the Side Effects of Azelastine?

Common Side Effects of Nasal Azelastine

Some mild side effects may include:

• Bitter taste in the mouth.

• Burning, pain, or discomfort in the nose.

• Sneezing or a runny nose.

• Headache.

• Sore throat.

• Dry mouth.

• Nosebleeds.

• Dizziness.

• Nausea.

• Feeling tired.

Serious Side Effects of Nasal Azelastine

• Severe allergic reactions (rash, itching, swelling of the face, lips, or throat, trouble breathing).

• Severe nosebleeds.

• Extreme dizziness or fainting.

• Persistent headache or vision problems.

Even if you experience other unusual or severe symptoms, reach out to your doctor right away.

Who Is Advised to Avoid Using Azelastine Nasal Spray?

Azelastine nasal spray is not suitable for everyone. You should avoid using it if you:

• You are allergic to Azelastine or any of the ingredients in the spray.

• Have severe nose injuries or have undergone recent nasal surgery.

• If you take certain medicines that may interact with Azelastine (ask your doctor).

Always talk to your doctor before using the spray if you have any health conditions or concerns.

What Are the Things to Inform the Doctor Before Taking Azelastine?

Before you use Azelastine nasal spray, tell your doctor or pharmacist:

• If you are allergic to Azelastine, any part of this medicine, or other drugs, foods, or substances, please explain what symptoms you had.

• About all the medicines, vitamins, or herbal products you take, especially other cold or allergy medicines. Your doctor may need to adjust your doses or watch for side effects.

• If you have had nose surgery, hurt your nose, or have sores in your nose.

• Suppose you are pregnant, planning to become pregnant, or breastfeeding. Call your doctor if you become pregnant while using the spray.

Other Important Tips:

• Azelastine nasal spray may cause drowsiness. Do not drive or use machines until you know how it affects you.

• Ask your doctor about drinking alcohol while using the spray, as it can make side effects worse.

Dietary Considerations

Keep eating your usual diet unless your doctor advises a change.

Missed Dose

If you miss a dose, take it as soon as you remember. If the next dose is near, skip the missed one. Do not take two doses at the same time.

Overdose

• No overdoses have been reported with Azelastine nasal spray. Taking too much is unlikely to cause serious problems in adults, but it may cause excessive sleepiness.

• One 30 mL bottle of 0.1% spray contains approximately 30 mg of Azelastine.

• One 30 mL bottle of 0.15% spray contains approximately 45 mg of Azelastine.

• There is no antidote for an overdose. If it happens, seek medical help immediately.

• Swallowing antihistamines can be very dangerous for children, so always keep the spray out of their reach.

• In animal studies, very high doses (like 120 mg per kg in mice) caused tremors, convulsions, and death.

Storage and Handling

• Keep the spray in its original bottle, tightly closed, and out of reach of kids.

• Store it at room temperature (20 to 25°C or 68 to 77°F), away from heat, moisture, and sunlight (don’t keep it in the bathroom).

• Always lock the cap and store it in a high, out-of-sight location.

• Throw away safely. Don’t flush it down the toilet. Take unused spray to a medicine take-back program.

For Doctors

Dose:

Recommended Dosage for Seasonal Allergic Rhinitis

• Children 6 to 11 Years: 1 spray per nostril twice a day.

• Adults and Adolescents 12 years and Older: 1 or 2 sprays per nostril twice a day, or 2 sprays per nostril once a day.

Recommended Dosage for Perennial Allergic Rhinitis

• Children 6 to 11 Years: 1 spray per nostril twice a day.

• Adults and Adolescents 12 years and Older: 2 sprays per nostril twice a day.

What Are the Pharmacological Actions of Azelastine?

Pharmacodynamics:

Azelastine nasal spray works by reducing allergy symptoms such as sneezing, a runny nose, and nasal congestion. Studies show that when used as directed, it does not affect heart rhythm (QT interval) and is generally safe for adults and children. Its active metabolite, desmethylazelastine, also contributes to the control of allergy symptoms.

Mechanism of Action:

Azelastine nasal spray is an antihistamine. It works by blocking histamine (a chemical that causes allergy symptoms) in the body. Its main breakdown product, desmethylazelastine, also helps stop allergy symptoms.

Pharmacokinetics:

• Absorption: After being sprayed into the nose, Azelastine enters the bloodstream slowly. For the 0.1% spray, peak levels appear in approximately 3 hours, and for the 0.15% spray, in approximately 4 hours. Approximately 40% of the medicine enters the bloodstream.

• Metabolism: The body breaks down Azelastine into an active substance called Desmethylazelastine, which also helps alleviate allergy symptoms.

• Elimination: Azelastine is eliminated from the body slowly, with a half-life of 22–25 hours, and Desmethylazelastine has a half-life of 52–57 hours. Most of it is excreted in feces.

• Special Groups: Liver problems, age, and gender do not significantly change how the spray works, but kidney problems can increase blood levels.

Toxicity

• Cancer Risk: Long-term studies in rats and mice have shown that azelastine does not cause cancer, even at doses significantly higher than the typical human dose.

• Genetic Safety: Tests have shown that Azelastine does not damage DNA or cause mutations.

• Fertility: Normal fertility was observed in rats at doses up to 150 times the human dose. Extremely high Azelastine doses reduced pregnancies and affected reproductive cycles.

• Pregnancy and Fetal Development: Very high doses in mice, rats, and rabbits caused birth defects, embryo-fetal death, or low fetal weight, but Azelastine doses closer to human use did not affect mothers or babies.

What Are the Drug Interactions of Azelastine?

• Alcohol and CNS Depressants: Avoid using Azelastine nasal spray with alcohol or other sedating drugs because it can make you drowsy and reduce alertness.

• Erythromycin and Ketoconazole: Taking these antibiotics with Azelastine does not affect heart rhythm. Ketoconazole may slightly alter blood levels, but this is not considered harmful.

• Cimetidine: This medicine can increase Azelastine levels in the blood by about 65 %, so your doctor may need to watch for side effects.

Clinical Studies

Seasonal Allergic Rhinitis (SAR):

• Azelastine 0.1 %: Nasal spray for allergic rhinitis tested in 834 patients aged 12 to 83 for 2 weeks. Using two sprays per nostril twice daily reduced allergy symptoms (sneezing, runny nose, congestion, itching) more than a placebo. One spray twice daily also helped but was slightly less effective.

• Azelastine 0.15 %: Tested in 2,499 patients in multiple 2-week trials. 2 sprays twice daily or two sprays once daily significantly reduced allergy symptoms compared to placebo. Effects were measured using total nasal symptom scores (TNSS).

Perennial Allergic Rhinitis (PAR):

• Azelastine 0.15 %: Tested in 578 patients for 4 weeks. 2 sprays per nostril twice daily reduced allergy symptoms more than placebo, showing it is effective for year-round allergies.

Use in Specific Populations

• Pregnancy: Azelastine nasal spray should be used only if the benefits outweigh the risks. High doses in animals caused birth defects and fetal death, but doses close to human use were safe.

• Nursing Mothers: The safety of Azelastine for use during breastfeeding is unknown, so caution is advised when using it while breastfeeding.

• Children: The safety and effectiveness in children under 12 years have not been established.

• Older Adults: Older adults usually respond similarly to younger adults, but doctors typically start with a lower dose to be cautious, as their kidneys, liver, or heart may be weaker.

Conclusion:

Azelastine nasal spray is a helpful medicine for people with allergies. It helps alleviate sneezing, a runny nose, nasal itching, and congestion. Using it correctly and following safety precautions ensures its effectiveness and safety. Paying attention to potential side effects and consulting a doctor when necessary helps achieve the best results.

Key Takeaways:

• Azelastine nasal spray is typically used as 1–2 sprays per nostril, 1–2 times a day, as directed by the doctor and age.

• Spray only in the nose; do not swallow or spray into the eyes. Prime the pump before first use.

• Common side effects include bitter taste, nasal irritation, headache, or tiredness.

• Avoid alcohol or sedating drugs, and use caution during pregnancy or breastfeeding. Children under 12 should use it under adult supervision.

If you experience severe allergy symptoms or unusual reactions, consult our doctor online for timely care and guidance.