Azelastine

What is azelastine?

Azelastine is a histamine-1 receptor antagonist, otherwise known as an antihistamine. This means the medication reduces histamine levels when sprayed into the nose, mitigating allergy symptoms such as sneezing, itching, and rhinitis (runny nose).¹

What is azelastine nasal spray used to treat?

Azelastine is approved by the Food and Drug Administration (FDA) to treat allergic rhinitis in people aged five years and older. Allergic rhinitis is otherwise known as allergies or hay fever. It can be caused by seasonal allergens or experienced all year round.

The nasal spray is also used to treat vasomotor rhinitis — a non-allergic runny nose — in adults and children aged 12 years and above.²

Dosage forms and strengths

Azelastine nasal spray is available in two strengths:

• 0.1% delivers 137mcg per spray (Astelin — prescription only)² ³

• 0.15% delivers 205.5mcg per spray (Astepro — available over the counter for patients six years and older)⁴ ⁵

How do you take azelastine?

Azelastine is taken as an intranasal spray.

Depending on your age and condition, you will be instructed to use 1–2 sprays in each nostril 1–2 times a day. Carefully follow the usage instructions given to you by your doctor or pharmacist and printed on the medication’s packaging.⁶

Before using the spray for the first time, prime it with four sprays or until a fine mist appears. If you have not used the spray for three days or more, the pump will need to be reprimed, typically with two sprays.

Seeing results

Azelastine has a rapid onset of action and typically relieves symptoms faster than corticosteroids. You should begin to feel symptomatic relief almost immediately, usually after about 15 minutes.

Who should not take azelastine?

People who are allergic to azelastine and its components should not use the medication.

Potential side effects of azelastine

Azelastine use can cause side effects that range from mild to severe.⁷

Common side effects

• Drowsiness

• Bitter taste

• Headache

• Cold symptoms

• Cough

Less common side effects

• Burning sensation in the nose

• Sneezing

• Dry nose, eyes, or mouth

• Nasal irritation

• Fatigue

• Muscle aches

• Nausea

• Dizziness

• Weight gain

Rare or more severe adverse effects

• Hypertension

• Flushing

• Rapid heart rate, palpitations

• Contact dermatitis

• Constipation

• Swollen, inflamed tongue

• Hyperkinesia

• Vertigo

• Vomiting

• Bronchospasm

• Loss of smell or taste

• Urinary retention

• Albuminuria

• Amenorrhea

• Confusion

When to seek medical attention

It’s important to talk to your doctor about any side effects you are experiencing.

Seek urgent medical attention if you have:

• Any signs of an allergic reaction to azelastine

• Any of the severe side effects listed above

Overdose

While no overdoses have been reported with azelastine nasal spray, it is theoretically possible to take too much.²

There are no serious clinical signs associated with overdose other than drowsiness since the concentrations of the drug used are very small. However, there is a potential for serious side effects if a child takes the medicine by mouth.

Allergy information

Azelastine can sometimes trigger allergic reactions. However, this is rare.

Stop taking azelastine and talk to your doctor if your allergy symptoms worsen after taking the drug.

Symptoms of an allergic reaction to the drug include the following:

• Rash

• Itching/swelling (especially of the face, tongue, or throat)

• Dizziness

• Vomiting

• Trouble breathing

Seek emergency medical assistance if your reaction is severe.

Long-term use of azelastine

Using azelastine for extended periods or using it consistently for perennial allergic rhinitis causes no specific problems.

Pregnancy category

The FDA has designated azelastine a pregnancy category C medication, meaning the risks of taking the drug during pregnancy cannot be ruled out.⁴

There are no satisfactory studies on pregnant women, but animal studies show risk to the fetus.

Azelastine should only be used during pregnancy if the benefits outweigh the risks.

Azelastine and pregnancy

Azelastine hydrochloride has been shown to cause toxicity in rabbits, mice, and rats while pregnant. It is associated with fetal death and malformations in these animals, such as cleft palate, delayed bone development, and decreased fetal weight.⁴

Although these studies used a much higher dose than is typically used by humans, your doctor will most likely recommend discontinuing azelastine during pregnancy unless the benefits clearly outweigh the potential risks.

Azelastine and breastfeeding

It is not known whether azelastine hydrochloride is excreted in breast milk. Caution is generally advised if you choose to take the drug while breastfeeding.⁷

Missed doses

If you miss a dose of this medication, take it as soon as you realize it. If it is very close to the time for your next dose, skip the missed dose.

Taking too high a dose of azelastine can cause drowsiness and affect your ability to do normal activities.

Drug interactions

Azelastine nasal spray is not known to interact with other drugs. However, you should avoid using azelastine while taking other drugs that can cause drowsiness (e.g., sedatives) due to the risk of cumulative effects.

Can I drink alcohol while taking azelastine?

It is generally not advisable to drink alcohol while taking azelastine. Alcohol can also cause drowsiness as it is a central nervous system depressant. Combining it with azelastine can result in impaired alertness.²

Review with your doctor whether you should avoid alcohol completely while taking the drug.

What to discuss with your doctor before starting azelastine

Before you start using azelastine nasal spray, you should discuss the following things with your doctor:

• If your doctor recommends azelastine, share a list of all medications you are taking, including supplements and herbs.

• Inform your doctor of any allergies to medicines you have experienced in the past.

• If you are planning a pregnancy, it is wise to discuss alternatives. Azelastine has been associated with birth defects in animal studies. The risk to humans is unknown, so your doctor will review your situation to determine if the benefits of using the drug outweigh the risks in your case.

• Azelastine can cause drowsiness. You should not drive or operate machinery until you know how the drug affects you. If this is part of your work or lifestyle, speak to your doctor about how you can use this medication safely.

• If you are using over-the-counter Astepro, ensure that your doctor knows you are taking it — even if you only take it occasionally. It is generally wise to inform your doctor of all over-the-counter medications you use, whether on occasion or regularly.

Stopping azelastine

Azelastine is not addictive and has no withdrawal symptoms. Note that your allergy symptoms may return if you stop taking it.

Drug approval history

Azelastine was approved by the FDA to be sold under the brand name Astelin in 1996. It was initially approved to treat seasonal allergic rhinitis and was later approved to treat vasomotor rhinitis in 1999.⁸

Astepro was approved for non-prescription use in 2021.⁵

Tips for using azelastine nasal spray

Following these tips will help you use azelastine nasal spray safely and get the best results:

• Each nasal spray bottle has the capacity to deliver a specific number of doses. The spray must be primed before use and reprimed if not used in some time. Don’t continue using the bottle after the stated number of sprays have been used as this can affect the dosage.

• Azelastine can cause drowsiness. It should not be mixed with alcohol or other sedatives, and you should not drive or operate machinery when first taking the drug. Talk to your doctor about alternatives if drowsiness is a problem for you.

• Tell your doctor or dentist that you are using azelastine nasal spray before surgery. This is because the medication can increase the effect of sedatives. They may recommend you do not take it on the day of your surgery or adjust the sedative dosage to compensate.

• Talk to your doctor if you become pregnant while using this drug.

• Do not store azelastine in the bathroom as it is negatively affected by excess heat and moisture.

• Keep azelastine nasal spray upright at temperatures of 68–77°F. Do not use azelastine that has frozen.

• It is vitally important to keep azelastine out of the reach of young children as it can be toxic to them if taken orally. The nasal spray is not child resistant, so it should be kept well out of their reach and sight.

Frequently asked questions

Is azelastine the same as Flonase?

No. Flonase is fluticasone, a steroid medication. Azelastine is an antihistamine.⁹

How many times a day can you use azelastine nasal spray?

Depending on your doctor’s or pharmacist’s directions, you can use two sprays in each nostril once a day or 1–2 sprays in each nostril every 12 hours. Do not use more than four sprays in each nostril per day. If you obtained the drug over the counter, follow the directions and age specifications on the label.

How long does it take for azelastine to start working?

Azelastine starts working very quickly. Symptomatic relief is typically experienced after about 15 minutes.

Does azelastine affect sleep?

:Azelastine can cause somnolence (drowsiness) in some people. Because of this, taking it at night might help with sleep, but it can make you drowsy in the morning.