Astelin

Name: Astelin

What is azelastine, and how does it work (mechanism of action)?

Azelastine is an antihistamine, a chemical that blocks the effects of histamine, another chemical that is responsible for some of the symptoms in allergic reactions. Azelastine is chemically different from other antihistamines and is used only as a nasal inhaler for the treatment of symptoms of seasonal allergic rhinitis, such as runny nose, sneezing, and nasal itching in adults and children 12 years of age and older. Azelastine was approved by the FDA in 1996.

Notes

Do not share this medication with others.

Uses of Astelin

Astelin is a prescription medication used to treat allergy symptoms of the nose such as runny or stuffy nose, sneezing, and itching.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Astelin and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if Astelin is excreted in human breast milk or if it will harm your nursing baby.

What happens if I miss a dose?

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

What should I avoid while taking azelastine nasal?

This medicine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Drinking alcohol with this medicine can cause side effects.

What other drugs will affect azelastine nasal?

Using this medicine with other drugs that make you sleepy can worsen this effect. Ask your doctor before using a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety, depression, or seizures.

Other drugs may interact with azelastine nasal, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Indications and Usage for Astelin

Astelin Nasal Spray is indicated for the treatment of the symptoms of seasonal allergic rhinitis in adults and pediatric patients 5 years and older, and for the treatment of the symptoms of vasomotor rhinitis in adults and adolescent patients 12 years and older.

Astelin Dosage and Administration

Seasonal Allergic Rhinitis

The recommended dosage of Astelin Nasal Spray in adults and adolescent patients 12 years and older with seasonal allergic rhinitis is one or two sprays per nostril twice daily. The recommended dosage of Astelin Nasal Spray in pediatric patients 5 years to 11 years of age is one spray per nostril twice daily.

Vasomotor Rhinitis

The recommended dosage of Astelin Nasal Spray in adults and adolescent patients 12 years and older with vasomotor rhinitis is two sprays per nostril twice daily.

Important Administration Instructions

Administer Astelin Nasal Spray by the intranasal route only.

Priming:  Prime Astelin Nasal Spray before initial use by releasing 4 sprays or until a fine mist appears. When Astelin Nasal Spray has not been used for 3 or more days, reprime with 2 sprays or until a fine mist appears. Avoid spraying Astelin Nasal Spray into the eyes.

Dosage Forms and Strengths

Astelin Nasal Spray is a nasal spray solution. Each spray of Astelin Nasal Spray delivers a volume of 0.137 mL solution containing 137 mcg of azelastine hydrochloride.

Adverse Reactions

Use of Astelin Nasal Spray has been associated with somnolence [see Warnings and Precautions (5.1)].

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect rates observed in practice.

Seasonal Allergic Rhinitis

      Astelin Nasal Spray Two Sprays Per Nostril Twice Daily

Adverse experience information for Astelin Nasal Spray is derived from six placebo- and active-controlled, 2-day to 8-week clinical trials which included 391 patients, 12 years of age and older, with seasonal allergic rhinitis who received Astelin Nasal Spray at a dose of 2 sprays per nostril twice daily. In placebo-controlled efficacy trials, the incidence of discontinuation due to adverse reactions in patients receiving Astelin Nasal Spray and vehicle placebo was 2.2% and 2.8%, respectively.

Table 1 contains adverse reactions that were reported with frequencies ≥2% in the Astelin Nasal Spray 2 sprays per nostril twice daily treatment group and more frequently than placebo.

Table 1: Adverse Reactions Reported in ≥2% Incidence in Placebo-Controlled
Trials in Patients with Seasonal Allergic Rhinitis [n (%)]
Astelin
Nasal Spray
N = 391
Vehicle
Placebo
N = 353
Bitter Taste 77 (19.7%) 2 (0.6%)
Headache 58 (14.8%) 45 (12.7%)
Somnolence 45 (11.5%) 19 (5.4%)
Nasal Burning 16 (4.1%) 6 (1.7%)
Pharyngitis 15 (3.8%) 10 (2.8%)
Paroxysmal Sneezing 12 (3.1%) 4 (1.1%)
Dry Mouth 11 (2.8%) 6 (1.7%)
Nausea 11 (2.8%) 4 (1.1%)
Rhinitis 9 (2.3%) 5 (1.4%)
Fatigue 9 (2.3%) 5 (1.4%)
Dizziness 8 (2.0%) 5 (1.4%)
Epistaxis 8 (2.0%) 5 (1.4%)
Weight Increase 8 (2.0%) 0 (0.0%)

      Astelin Nasal Spray One Spray Per Nostril Twice Daily

Adverse experience information for Astelin Nasal Spray at a dose of one spray per nostril twice daily is derived from two placebo-controlled 2-week clinical studies which included 276 patients 12 years of age and older with seasonal allergic rhinitis. The incidence of discontinuation due to adverse reactions in patients receiving Astelin Nasal Spray and vehicle placebo was 0.0% and 0.8%, respectively. Bitter taste was reported in 8.3% of patients compared to none in the placebo group. Somnolence was reported in 0.4% of patients compared to none in the placebo group.

A total of 176 patients 5 to 11 years of age were exposed to Astelin Nasal Spray at a dose of 1 spray each nostril twice daily in 3 placebo-controlled studies. In these studies, adverse reactions that occurred more frequently in patients treated with Astelin Nasal Spray than with placebo, and that were not represented in the adult adverse reactions table above include rhinitis/cold symptoms (17.0% vs. 9.5%), cough (11.4% vs. 8.3%), conjunctivitis (5.1% vs. 1.8%), and asthma (4.5% vs. 4.1%).

      Adverse Reactions <2% in Astelin Nasal Spray One or Two Sprays Per Nostril Twice Daily

The following reactions were observed infrequently (<2% and exceeding placebo incidence) in patients who received Astelin Nasal Spray dosed at 1 or 2 sprays per nostril twice daily in U.S. clinical trials.

Cardiovascular: flushing, hypertension, tachycardia.

Dermatological: contact dermatitis, eczema, hair and follicle infection, furunculosis, skin laceration.

Digestive: constipation, gastroenteritis, glossitis, ulcerative stomatitis, vomiting, increased SGPT, aphthous stomatitis, diarrhea, toothache.

Metabolic and Nutritional: increased appetite.

Musculoskeletal: myalgia, temporomandibular dislocation, rheumatoid arthritis.

Neurological: hyperkinesia, hypoesthesia, vertigo.

Psychological: anxiety, depersonalization, depression, nervousness, sleep disorder, thinking abnormal.

Respiratory: bronchospasm, coughing, throat burning, laryngitis, bronchitis, dry throat, nocturnal dyspnea, nasopharyngitis, nasal congestion, pharyngolaryngeal pain, sinusitis, nasal dryness, paranasal sinus hypersecretion, post nasal drip.

Special Senses: conjunctivitis, eye abnormality, eye pain, watery eyes, taste loss.

Urogenital: albuminuria, amenorrhea, breast pain, hematuria, increased urinary frequency.

Whole Body: allergic reaction, back pain, herpes simplex, viral infection, malaise, pain in extremities, abdominal pain, pyrexia.

Vasomotor Rhinitis

Adverse experience information for Astelin Nasal Spray is derived from two placebo-controlled clinical studies which included 216 patients 12 years and older with vasomotor rhinitis who received Astelin Nasal Spray at a dose of 2 sprays per nostril twice daily for up to 28 days. The incidence of discontinuation due to adverse reactions in patients receiving Astelin Nasal Spray and vehicle placebo was 2.8% and 2.9%, respectively.

The following adverse reactions were reported with frequencies ≥ 2% in the Astelin Nasal Spray treatment group and more frequently than placebo.

Table 2: Adverse Reactions Reported in ≥2% Incidence in Placebo-Controlled
Trials in Patients with Vasomotor Rhinitis [n (%)]
Astelin
Nasal Spray
N = 216
Vehicle
Placebo
N = 210
Bitter Taste 42 (19.4%) 5 (2.4%)
Headache 17 (7.9%) 16 (7.6%)
Dysesthesia 17 (7.9%) 7 (3.3%)
Rhinitis 12 (5.6%) 5 (2.4%)
Epistaxis 7 (3.2%) 5 (2.4%)
Sinusitis 7 (3.2%) 4 (1.9%)
Somnolence 7 (3.2%) 2 (1.0%)

Reactions observed infrequently (<2% and exceeding placebo incidence) in patients who received Astelin Nasal Spray (2 sprays/nostril twice daily) in U.S. clinical trials in vasomotor rhinitis were similar to those observed in U.S. clinical trials in seasonal allergic rhinitis.

In controlled trials involving nasal and oral azelastine hydrochloride formulations, there were infrequent occurrences of hepatic transaminase elevations.

Postmarketing Experience

During the post approval use of Astelin Nasal Spray, the following adverse reactions have been identified. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Adverse reactions reported include: anaphylaxis, application site irritation, atrial fibrillation, chest pain, confusion, dyspnea, facial edema, involuntary muscle contractions, nasal sores, palpitations, paresthesia, parosmia, pruritus, rash, disturbance or loss of sense of smell and/or taste, tolerance, urinary retention, vision abnormal and xerophthalmia.

How Supplied/Storage and Handling

Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg is supplied as a 30-mL package (NDC 0037-0241-30) delivering 200 metered sprays in a high-density polyethylene (HDPE) bottle fitted with a metered-dose spray pump unit. The spray pump unit consists of a nasal spray pump fitted with a blue safety clip and a blue plastic dust cover. The net content of the bottle is 30 mL (net weight 30 gm of solution). Each bottle contains 30 mg (1 mg/mL) of azelastine hydrochloride. After priming [see Dosage and Administration (2.3)], each spray delivers a fine mist containing a mean volume of 0.137 mL solution containing 137 mcg of azelastine hydrochloride. The correct amount of medication in each spray cannot be assured before the initial priming and after 200 sprays have been used, even though the bottle is not completely empty. The bottle should be discarded after 200 sprays have been used. Astelin Nasal Spray should not be used after the expiration date "EXP" printed on the medicine label and carton.

Storage:

Store at controlled room temperature 20° to 25°C (68° to 77°F). Protect from freezing.

In Summary

Common side effects of Astelin include: drowsiness, bitter taste, and dysgeusia. Other side effects include: epistaxis. See below for a comprehensive list of adverse effects.

For the Consumer

Applies to azelastine nasal: nasal spray

Along with its needed effects, azelastine nasal (the active ingredient contained in Astelin) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking azelastine nasal:

Rare
  • 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 side effects of azelastine nasal may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Bitter taste in the mouth
  • drowsiness or sleepiness
Less common
  • Bloody mucus or unexplained nosebleeds
  • 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

Azelastine nasal Pregnancy Warnings

Animal studies have shown that this drug causes developmental toxicity in mice, rats, and rabbits at doses more than 15 times the equivalent human dose. Neither fetal nor maternal effects occurred at approximately 15 times the human dose or less. There are no adequate and well-controlled studies in pregnant women. US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

This drug should be used during pregnancy only if the benefit outweighs the risk to the fetus. US FDA pregnancy category: C

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