Astelin

Use of Astelin Nasal Spray has been associated with somnolence [see WARNINGS AND PRECAUTIONS].

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

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 (%)]

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%).

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.

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 (%)]

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.

• Meda Pharmaceuticals, Inc.

Astelin is part of the drug class:

• Other antiallergics

Do not use Astelin if you are allergic to any ingredient in it. 

Astelin can cause drowsiness. Do not drive or operate heavy machinery until you know how this medicine affects you.

Alcohol can worsen drowsiness. Avoid alcohol use with Astelin nasal spray.

Before receiving Astelin, tell your doctor:

• about all of your medical conditions
• if you are allergic to any ingredient in Astelin.
• if you are pregnant or breastfeeding

Tell your doctor about all of the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Azelastine is an antihistamine that reduces the effects of natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.

Azelastine nasal (for the nose) prevents sneezing, itching, runny nose, and other nasal symptoms of allergies. This medicine is for seasonal allergies in adults and children who are at least 2 years old, and for year-round allergies in adults and children as young as 6 months old.

Azelastine nasal may also be used for purposes not listed in this medication guide.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of azelastine nasal spray in children. However, safety and efficacy of azelastine nasal have not been established to treat seasonal allergic rhinitis in children younger than 2 years of age and perennial allergic rhinitis in children younger than 6 months of age.

Geriatric

Although appropriate studies on the relationship of age to the effects of azelastine nasal spray have not been performed in the geriatric population, no geriatric-specific problems have been documented to date. However, elderly patients are more likely to have age-related kidney, liver, or heart problems, which may require caution and an adjustment in the dose for patients receiving azelastine nasal spray.

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Bupropion
• Donepezil

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Cimetidine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Kidney disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

• It is used to ease allergy signs.
• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Feeling sleepy.
• Headache.
• Cough.
• Runny nose.
• Sneezing.
• Nose pain or irritation.
• Burning.
• Change in taste.
• Feeling tired or weak.
• Fever.
• Nosebleed.
• Sore throat.
• Upset stomach or throwing up.
• Dry mouth.
• Dizziness.
• Weight gain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Astelin (azelastine hydrochloride) Nasal Spray, 137 micrograms (mcg), is an antihistamine formulated as a metered-spray solution for intranasal administration. Azelastine hydrochloride occurs as a white, almost odorless, crystalline powder with a bitter taste. It has a molecular weight of 418.37. It is sparingly soluble in water, methanol, and propylene glycol and slightly soluble in ethanol, octanol, and glycerine. It has a melting point of about 225°C and the pH of a saturated solution is between 5.0 and 5.4. Its chemical name is (±)-1-(2H)-phthalazinone,4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride. Its molecular formula is C22H24ClN3O•HCl with the following chemical structure:

Astelin Nasal Spray contains 0.1% azelastine hydrochloride in an aqueous solution at pH 6.8 ± 0.3. It also contains benzalkonium chloride (125 mcg/mL), edetate disodium, hypromellose, citric acid, dibasic sodium phosphate, sodium chloride, and purified water.

After priming [see Dosage and Administration (2.3)], each metered spray delivers a 0.137 mL mean volume containing 137 mcg of azelastine hydrochloride (equivalent to 125 mcg of azelastine base). The bottle can deliver 200 metered sprays.

Before using azelastine nasal, tell your doctor about all of your medical conditions.

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

Before using azelastine, tell your doctor if you regularly use other medicines that make you sleepy (such as cold or allergy medicine, sedatives, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by azelastine.

Drinking alcohol can increase certain side effects of azelastine.

Call your doctor if your symptoms do not improve, or if they get worse while using azelastine.

Stop using azelastine and call your doctor at once if you have fast or uneven heartbeats, tightness in your chest, or if you feel short of breath.

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.

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.

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.

Substance Name

Azelastine

CAS Registry Number

58581-89-8

Drug Class

Antihistamines