Azelastine Nasal

Competes with histamine for H1-receptor sites on effector cells and inhibits the release of histamine and other mediators involved in the allergic response; when used intranasally, reduces hyper-reactivity of the airways; increases the motility of bronchial epithelial cilia, improving mucociliary transport

Distribution

Vd: 14.5 L/kg

Metabolism

Hepatic via CYP; active metabolite, desmethylazelastine

Excretion

Feces (75%, <10% as unchanged drug)

Clearance: 0.5 L/hour/kg

12 hours

Half-Life Elimination

Azelastine: 22 hours (0.1% solution), 25 hours (0.15% solution); Desmethylazelastine: 52 hours (0.1% solution), 57 hours (0.15% solution)

Protein Binding

Azelastine: ~88%; Desmethylazelastine: ~97%

Intranasal: Before initial use of the nasal spray, the delivery system should be primed with 4 sprays (azelastine [generic] 0.1% solution) or 6 sprays (Astepro), or until a fine mist appears. If 3 or more days have elapsed since last use, the delivery system should be reprimed with 2 sprays or until a fine mist appears. Blow nose to clear nostrils. Keep head tilted downward when spraying. Insert applicator into nostril, keeping bottle upright, and close off the other nostril. Aim the spray tip toward the back of nose. Breathe in through nose. While inhaling, press pump to release spray. Alternate sprays between nostrils. After each use, wipe the spray tip with a clean tissue or cloth. Avoid spraying in eyes or mouth. Do not tilt head back after use.

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

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.

A bitter taste in the mouth, drowsiness, a burning feeling inside the nose, sneezing fits, cough, nose bleeds, runny nose, nausea, dry mouth, headache, weight gain, muscle aches, or red eyes may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Applies to azelastine nasal: nasal spray

General

The most commonly reported adverse reactions were headache, bitter taste, sinusitis, and epistaxis.[Ref]

Respiratory

Common (1% to 10%): Epistaxis, nasal discomfort, upper respiratory infection, sneezing, nasal mucosal ulceration, sinusitis
Postmarketing reports: Nasal burning, throat irritation, dyspnea, paroxysmal sneezing[Ref]

Hypersensitivity

Postmarketing reports: Anaphylactoid reaction[Ref]

Local

Postmarketing reports: Application site irritation[Ref]

Nervous system

Very common (10% or more): Bitter taste (10%)
Common (1% to 10%): Headache, somnolence, dysgeusia
Postmarketing reports: Sweet taste, confusion, dizziness, nervousness, paraesthesia, parosmia, involuntary muscle contractions, disturbance or loss of sense of smell and/or taste[Ref]

Cardiovascular

Postmarketing reports: Atrial fibrillation, chest pain, hypertension, palpitations, tachycardia[Ref]

Dermatologic

Very rare (less than 0.01%): Urticaria, pruritus, rash[Ref]

Gastrointestinal

Postmarketing reports: Abdominal pain, nausea[Ref]

Other

Common (1% to 10%): Fatigue
Postmarketing reports: Facial edema, tolerance[Ref]

Ocular

Postmarketing reports: Blurred vision, xerophthalmia[Ref]

Genitourinary

Postmarketing reports: Urinary retention[Ref]

Some side effects of azelastine nasal may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

2 to 5 years:
0.1% spray: 1 spray in each nostril twice a day
6 to 11 years:
0.1% spray and 0.15% spray: 1 spray in each nostril twice a day

Use: Seasonal allergic rhinitis

6 months to 5 years:
0.1% spray: 1 spray in each nostril twice a day
6 to 11 years:
0.1% spray and 0.15% spray: 1 spray in each nostril twice a day

Use: Perennial allergic rhinitis

Safety and efficacy have not been established in patients younger than 6 months.

Consult WARNING section for additional precautions.

Data not available