Azelastine nasal spray – Use, Dosage, Side Effects, OTC Price Reviews

Azelastine - Side Effects, Uses, Dosage, Overdose, Pregnancy

What is Azelastine nasal spray?

Azelastine nasal spray is an intranasal spray that contains Azelastine. Azelastine is an antihistamine that works by inhibiting the effect of histamine. Our body produces a substance called histamine that is responsible for allergies resulting in itching, sneezing, runny nose and watery eyes. Azelastine nasal spray is beneficial in providing relief from the symptoms associated with seasonal or perennial rhinitis and vasomotor rhinitis. The symptoms include the stuffy or a runny nose, itching, sneezing and watery eyes. Azelastine is available in Nasal Spray form and you should take it with doctor’s prescription only.

Azelastine Nasal : Uses, Side Effects, Interactions, Pictures, Warnings

What is Azelastine prescribed for?

Your doctor prescribes Azelastine nasal spray for treating symptoms of allergic rhinitis such as itching, sneezing, runny nose and watery eyes.

What are some other brands of Azelastine?

Some common brand names of Azelastine are:

  • Astelin
  • Azellastina
  • Azelastinum
  • Optivar
  • Allergodil
  • Lastin
  • Afluon
  • Meda AB

How Azelastine nasal spray works?

Azelastine nasal spray contains Azelastine, which is a phthalazinone derivative that exhibits a histamine H1-receptor antagonist activity.  Being an antihistamine antagonist, Azelastine blocks the action of histamine thereby reducing the inflammatory action of histamine (It is a substance that our body produces which causes inflammation). This results in the opening of airway and narrowing of blood vessels. Azelastine also known to reduce the effect on nerves that are present inside the nose to stop sneezing and itching.

Azelastine nasal spray indications

The indications for Azelastine nasal spray includes:

  1. Symptoms of seasonal allergic rhinitis such as:
    • Rhinorrhea
    • Pruritis
    • Sneezing
  2. Perennial Allergies
  3. Vasomotor Allergies includes:
    • Nasal congestion
    • Postnasal drip

Azelastine nasal spray use for allergy rhinitis

Azelastine is more than just an antihistamine. It shows fast and long acting effects based on the triple mode of action. Its triple mode of action includes anti-inflammatory action, mast cell stabilizing properties, and anti-allergic effects.

Azelastine nasal spray has a faster onset of action and a better safety profile as compared to other intranasal corticosteroids. Azelastine in allergic rhinitis:

  1. Acts by Reducing the
  • Concentration of leukotrienes, kinins, and platelet activating factor and
  • Inflammatory cell migration in rhinitis patients
  1. Effective at lower dose of 1 spray as well at a dose of 2 sprays per nostril twice daily
  2. Have faster onset of action and a better safety profile.
  3. It shows comparable efficacy with Fluticasone propionate as well as mometasone furoate.
  4. It demonstrates good tolerability profile in both adults and children.
  5. Incorrect dosing technique can lead to the bitter taste of the medication, therefore; you should adopt correct dosing technique.

How long should be Azelastine nasal spray use for allergy rhinitis?

Azelastine is a first line treatment of symptoms associated with allergic rhinitis or hay fever. If you are suffering from allergic rhinitis or hay fever, use Azelastine nasal spray, because it treats a runny nose, blocked nose, itching of the nose, and sneezing within 15 minutes of administration. You can take this medication as soon as you need it.

How long can you use azelastine?

How long does it take Azelastine to work?

Once you take Azelastine nasal spray for the treatment of rhinitis, it will start working within 15 minutes and it will settle the symptoms as soon as its action begins.

Pharmacokinetics and metabolism of Azelastine

Absorption:

Azelastine nasal spray shows 40% of systemic bioavailability after nasal administration. It achieves maximum plasma concentration within 2 to 3 hours.

The administration of Azelastine by intranasal route at a dose of two sprays per nostril twice daily shows greater Cmax (maximum plasma concentration) and AUC (area under curve) for Azelastine.

Distribution:

Based on intravenous and oral administration, the steady-state volume of distribution is 14.5 L/kg. In vitro studies with human plasma indicate that the plasma protein binding of Azelastine and its metabolite, desmethylAzelastine, are approximately 88% and 97%, respectively.

Metabolism:

DesmethylAzelastine is an oxidative metabolite of Azelastine. The metabolism of Azelastine carried out with the help of cytochrome P450 enzyme whereas isoforms of P450 responsible for this biotransformation is not identified.

After intranasal dosing of Azelastine hydrochloride, plasma concentrations of desmethylAzelastine range from 20% to 50% of Azelastine concentrations. When Azelastine hydrochloride is administered via the intranasal or oral route, metabolite profile has limited data.

Elimination:

The elimination half-life and plasma clearance of Azelastine via intravenous and oral administration are 22 hours and 0.5L/h/kg respectively. When administered orally, 75% of the Azelastine was excreted in the feces.

Azelastine nasal spray dosage

Azelastine hydrochloride nasal spray is a nasal spray solution. Each spray of Azelastine hydrochloride nasal spray delivers a volume of 0.137 ml solution containing 137 mcg of Azelastine hydrochloride.

Azelastine nasal spray proper use

Azelastine nasal spray box usually contains a patient information leaflet. Before using, read the instructions carefully and follow them accordingly. You should use this medicine only as directed by your doctor. Do not use this medication more than recommendations in order to avoid any chance of side effects. The Azelastine nasal spray is for use only in the nose. You should use the right mode (intranasal) of administration. It should administer by the nose and by avoiding your mouth and eyes area. If it does get into these areas, wash it off with normal water. If you have any nose problem or nose injury, ask your doctor before taking this medicine. Consult your pharmacist for any questions and confusions about this medication.

What is azelastine hydrochloride nasal spray used for?

To use the spray:

  1. If you are a first time user of Azelastine nasal spray, prime the spray before use. Press the top of the pump at least 6 times or press it until a fine spray comes out.
  2. If you have not used this spray for more than 3 days, Prime again with two sprays.
  3. Clean your nose before using the spray.
  4. Tilt your head back and insert the tip of the nosepiece of nasal spray into your nostril.
  5. Close the other nostril with your finger. Release one spray at one time; breathe in the medicine through the nostril.
  6. Hold on for few seconds and breathe out through your mouth.
  7. Use the same technique while spraying into the other nostril.
  8. Do not blow your nose after administration of the medicine.
  9. Clean the tip of the nosepiece gently with a dry tissue or cloth and close the spray with a cap.
  10. This nasal spray contains 200 sprays; therefore, do not use it after 200 sprays.

Can Azelastine nasal spray be used during pregnancy?

Azelastine shows neither fetal nor maternal effects occurred even at 15 times doses of human dose in animal studies. There are no adequate and well-controlled studies in pregnant women. USFDA category for pregnancy risk is “C”.

One should take this medication in emergency and only after the recommendation of the doctor. The pregnant women can use Azelastine nasal spray only if the benefit outweighs the risk to the fetus.

Can Azelastine nasal spray be used during breastfeeding?

Nursing mothers can take this medicine only in emergency conditions and only if benefits outweigh the risk to the infant. Azelastine uses to excrete in human milk in small amounts. Therefore, the nursing mother should be cautious while taking this medicine. Any side effect in the nursing infant is unknown.

Azelastine nasal spray side effects:

Azelastine may cause some side effects that do not need medical attention as they disappear during treatment. Your healthcare provider will also inform you regarding some common side effects of this medicine and will tell you about the prevention and control of those side effects. If you find any other troublesome side effect in your body after taking this medicine, consult your doctor immediately.

You may need medical attention if you see any of these side effects of Azelastine nasal spray.

  1. The most common side effects of Azelastine are Bitter taste in mouth and Drowsiness
  2. Less common side effects are:
  • Bloody mucus or unexplained nosebleed
  • burning inside the nose
  • dizziness
  • dryness of the mouth
  • headache
  • muscle aches or pain
  • nausea
  • sore throat
  • sudden outbursts of sneezing
  • unusual tiredness or weakness
  • weight gain
  1. Some rare side effects are:
  • Blood in the urine
  • blurred vision or other change in vision
  • cough
  • eye pain
  • eye redness
  • hives, itching, or skin rash
  • rapid heartbeat
  • sores in the mouth or on the lips
  • tightness in the chest
  • troubled breathing

Some patients may feel other side effects that are not mentioned in the list. You should consult your doctor if you see any other side effect apart from the list.

Azelastine nasal spray contraindication

There is no reported contraindication of Azelastine Nasal Spray.

Azelastine nasal spray interactions

If you are taking Azelastine under the guidance of your doctor, he may already know the possible interactions of this medication and may be monitoring you for it. Discuss with your doctor, if you are taking any prescription, non-prescription, herbal products, and over the counter products. Tell your doctor if you are taking:

  • Other antihistamines (e.g. Diphenhydramine)
  • Anti-anxiety drugs (e.g. Diazepam)
  • Anti-seizure drugs (e.g. Phenobarbital)
  • Medicines for sleep (e.g. Zolpidem)
  • Muscle relaxants
  • Narcotic pain relievers (e.g. codeine)
  • Psychiatric medicines (e.g. phenothiazines such as chlorpromazine or amitryptaline)
  • Tranquilizers
  • Drowsiness causing agents such as cold and cough medicines

Not all interactions mentioned here therefore you should make a list of all medicines that you are taking. Do check this list with your doctor before taking Azelastine nasal spray.

What should I do if I forget a dose?

Whenever you missed a dose of Azelastine nasal spray, take the missed dose as soon as you remember it. However, if you remember the missed dose at the time of next dose then skip the missed dose and continue with your regular dosing schedule. Avoid “doubling up” the dose for making the missed one.

Can I drink alcohol while taking Azelastine?

One should not take alcohol with this medicine because this medicine will add to the effects of alcohol and other CNS depressants (sedative, tranquilizers, sleep medicines and antihistamines). This can cause excessive drowsiness and lack of alertness.

Azelastine nasal spray precautions and warnings

  • If you see any unwanted effect of this medicine, you should check it with your doctor. If you see any symptoms that do not improve within a few days or if it becomes worse, check with your doctor.
  • One should not take alcohol with this medicine because this medicine will add to the effects of alcohol and other CNS depressants. This can cause excessive drowsiness and lack of alertness.
  • Some medicines that can cause CNS depression are antihistamines or medicine for hay fever, other allergies, or colds, sedatives, tranquilizers, or sleeping medicine, prescription pain medicine or narcotics, medicine for seizures, muscle relaxants, or anesthetics, including some dental anesthetics. Consult your doctor or pharmacist about above-mentioned medicines, before using Azelastine nasal spray.
  • One of the side effects of this medicine is drowsiness due to which a person can become dizzy, drowsy, or less alert than they are normally. Azelastine may cause some people to feel drowsy or less alert on awakening, even if you used it at bedtime.  You should avoid driving, use of heavy machines or stop doing anything that is dangerous after taking this medicine.
  • Azelastine nasal spray is an intranasal spray and you should administer this only by nasal route. You should avoid your eyes area while taking this medicine because this medicine may cause irritation in the eyes or blurred vision. Rinse your eyes immediately with water, if this medicine entered in your eyes accidentally. You can also keep your eyes close before putting this medicine into your nostril; this will help you to prevent its exposure from your eyes.
  • If you are taking any other medicines such as herbal supplements, vitamins or OTC products, do not forget to discuss it with your doctor before taking this medicine. Avoid taking this medicine without the recommendation of the doctor.

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About Miljan Krcobic 239 Articles
My name is Miljan Krčobić. I was born on 14th of November 1989. in Negotin, Serbia, where I finished elementary and high school. In June 2015 I graduated from the Faculty of Pharmacy in Belgrade and thus acquired the title Master of Pharmacy. From the July of 2015 to January 2016 I worked in a pharmaceutical company Hemofarm a.d.(Member of STADA group) based in Vrsac, Serbia, as an expert associate for GMP compliance within the sector Quality Assurance. I am currently working in a pharmacy called Zivkovic in Negotin. As a freelancer I write medical articles on Elance and Upwork.