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Pharmacologic Category
Histamine H1 Antagonist; Histamine H1 Antagonist, Second Generation
Dosing: Adult
Perennial allergic rhinitis: Intranasal: Astepro (0.15% solution): Two sprays in each nostril twice daily.
Seasonal allergic rhinitis: Intranasal:
Astepro (0.1% or 0.15% solution): One or two sprays (0.1% solution) in each nostril twice daily or two sprays (0.15% solution) in each nostril once daily
Azelastine [generic] 0.1% solution: One or two sprays in each nostril twice daily
Vasomotor rhinitis: Intranasal: Azelastine [generic] 0.1% solution: Two sprays in each nostril twice daily.
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling.
Dosing: Hepatic Impairment: Adult
There are no dosage adjustments provided in the manufacturer’s labeling.
Dosing: Pediatric
Perennial allergic rhinitis: Intranasal:
Infants ≥6 months and Children <6 years: 0.1% solution: 1 spray per nostril twice daily.
Children 6 to <12 years: 0.1% or 0.15% solution: 1 spray per nostril twice daily
Children ≥12 years and Adolescents: 0.15% solution: 2 sprays per nostril twice daily
Seasonal allergic rhinitis: Intranasal:
Children 2 to <6 years: 0.1% solution: 1 spray per nostril twice daily
Children 6 to <12 years: 0.1% or 0.15% solution: 1 spray per nostril twice daily
Children ≥12 years and Adolescents:
0.1% solution: 1 or 2 sprays per nostril twice daily
0.15% solution: 1 or 2 sprays per nostril twice daily or 2 sprays per nostril once daily
Vasomotor rhinitis: Intranasal: Children ≥12 years and Adolescents: 0.1% solution: 2 sprays per nostril twice daily
Dosing: Renal Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer's labeling.
Dosing: Hepatic Impairment: Pediatric
There are no dosage adjustments provided in the manufacturer's labeling.
Use: Labeled Indications
Perennial allergic rhinitis (Astepro 0.1% and 0.15% solution only): Relief of symptoms of perennial allergic rhinitis in adults and pediatric patients ≥6 months.
Seasonal allergic rhinitis: Relief of symptoms of seasonal allergic rhinitis in adults and pediatric patients ≥2 years (Astepro 0.1% and 0.15% solution) and ≥5 years (azelastine [generic] 0.1% solution).
Vasomotor rhinitis (azelastine [generic] 0.1% solution): Relief of symptoms of vasomotor rhinitis in adults and adolescents ≥12 years.
* See Uses in AHFS Essentials for additional information.
Clinical Practice Guidelines
AAAAI and ACAAI, “Treatment of Seasonal Allergic Rhinitis,” 2017 Update
AAO-HNS, “Clinical Practice Guideline: Allergic Rhinitis,” 2015
Administration: 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. Astepro 30 mL bottles contain 200 sprays; discard bottle after 200 sprays, even if not completely empty.
Administration: Pediatric
For intranasal administration only. Before initial use, the delivery system should be primed until a fine mist appears; when 3 or more days have elapsed since the last use, the pump should be reprimed until a fine mist appears. Blow nose to clear nostrils. Remove the dust cover. Keep head tilted downward when spraying. Insert applicator into nostril, keeping bottle upright, and close off the other nostril. 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.
Storage/Stability
Store upright at 20°C to 25°C (68°F to 77°F); protect from freezing.
Medication Patient Education with HCAHPS Considerations
What is this drug used for?
• It is used to ease allergy signs.
• It is used to treat a runny nose.
Frequently reported side effects of this drug
• Nosebleed
• Fatigue
• Headache
• Cough
• Stuffy nose
• Sore throat
• Loss of strength and energy
• Nausea
• Dry mouth
• Dizziness
• Weight gain
• Sneezing
• Change in taste
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• Eye irritation
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
Contraindications
There are no contraindications listed in the manufacturer's labeling.
Warnings/Precautions
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.
* See Cautions in AHFS Essentials for additional information.
Geriatric Considerations
Evaluate the patient’s or caregiver’s ability to safely administer the correct dose of nasal medication. Only a small number of older subjects were included in premarketing trials. In those patients, side effects were no different than in younger patients.
Pregnancy Considerations
Azelastine is systemically absorbed following nasal inhalation and may have side effects similar to other antihistamines. However, data related to the use of azelastine in pregnancy is limited; if treatment for rhinitis in a pregnant woman is needed, other agents are preferred (Wallace 2008).
Breast-Feeding Considerations
It is not known if azelastine (nasal) is present in breast milk.
The manufacturer recommends that caution be exercised when administering azelastine (nasal) to breastfeeding women; the decision to breastfeed during therapy should consider the risk of infant exposure, benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Briggs' Drugs in Pregnancy & Lactation
Adverse Reactions
Adverse reactions may be dose-, indication-, or product-dependent:
>10%:
Central nervous system: Bitter taste (4% to 20%), headache (1% to 15%), drowsiness (≤12%)
Infection: Cold symptoms (children ≤17%)
Respiratory: Rhinitis (exacerbation; ≤17%), cough (children: 11%; infants and children: ≥2%)
2% to 10%:
Central nervous system: Dysesthesia (8%), dizziness (2%), fatigue (2%)
Dermatologic: Contact dermatitis
Endocrine & metabolic: Weight gain (2%)
Gastrointestinal: Dysgeusia (children: 2% to 4%), nausea (3%), xerostomia (3%), vomiting
Infection: Upper respiratory tract infection (children: ≥2% to 3%)
Neuromuscular & skeletal: Myalgia (≤2%)
Ophthalmic: Conjunctivitis (<2% to 5%)
Otic: Otitis media (infants & children: ≥2%)
Respiratory: Epistaxis (2% to 7%), asthma (5%), sinusitis (3% to >5%), burning sensation of the nose (4%), pharyngitis (4%), nasal discomfort (≤4%), sneezing (1% to 3%), sore nose (infants and children: ≥2%), nasal mucosa ulcer (≤2%), pharyngolaryngeal pain
Miscellaneous: Fever
<2%:
Cardiovascular: Flushing, hypertension, tachycardia
Central nervous system: Abnormality in thinking, anxiety, depersonalization, depression, hypoesthesia, malaise, nervousness, sleep disorder, vertigo
Dermatologic: Eczema, folliculitis, furunculosis
Endocrine & metabolic: Albuminuria, amenorrhea
Gastrointestinal: Abdominal pain, ageusia, aphthous stomatitis, constipation, diarrhea, gastroenteritis, glossitis, increased appetite, toothache
Genitourinary: Hematuria, mastalgia
Hepatic: Increased serum ALT
Hypersensitivity: Hypersensitivity reaction
Infection: Herpes simplex infection, viral infection
Neuromuscular & skeletal: Back pain, dislocation of temporomandibular joint, hyperkinesia, limb pain, rheumatoid arthritis
Ophthalmic: Eye pain, watery eyes
Renal: Polyuria
Respiratory: Bronchitis, bronchospasm, laryngitis, nasal congestion, paranasal sinus hypersecretion, paroxysmal nocturnal dyspnea, postnasal drip, sore throat
Miscellaneous: Laceration
<1%, postmarketing, and/or case reports: Altered sense of smell, anaphylactoid reaction, anosmia, application site irritation, atrial fibrillation, blurred vision, chest pain, confusion, drug tolerance, dyspnea, facial edema, increased serum transaminases, insomnia, muscle spasm, nasal sores, palpitations, paresthesia, pruritus, skin rash, urinary retention, visual disturbance, xerophthalmia
* See Cautions in AHFS Essentials for additional information.
Allergy and Idiosyncratic Reactions
Toxicology
Metabolism/Transport Effects
Substrate of CYP1A2 (minor), CYP2C19 (minor), CYP2D6 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions Open Interactions
Alcohol (Ethyl): May enhance the CNS depressant effect of Azelastine (Nasal). Risk X: Avoid combination
CNS Depressants: May enhance the CNS depressant effect of Azelastine (Nasal). Risk X: Avoid combination
Genes of Interest
Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Nasal, as hydrochloride:
Astepro: 0.15% (30 mL) [contains benzalkonium chloride, edetate disodium]
Generic: 137 mcg/spray (30 mL); 0.1% (30 mL); 0.15% (30 mL)
Anatomic Therapeutic Chemical (ATC) Classification
- R01AC03
Generic Available (US)
Yes
Pricing: US
Solution (Azelastine HCl Nasal)
0.1% (per mL): $3.51
0.15% (per mL): $2.23 - $5.81
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Mechanism of Action
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
Pharmacodynamics/Kinetics
Onset of action: 15 to 30 minutes (Wallace 2008); maximum effect: 3 hours
Duration: 12 hours
Distribution: Vd: 14.5 L/kg
Protein binding: Azelastine: ~88%; Desmethylazelastine: ~97%
Metabolism: Hepatic via CYP; active metabolite, desmethylazelastine
Bioavailability: ~40%
Half-life elimination: Azelastine: 22 hours (0.1% solution), 25 hours (0.15% solution) to 25 hours; Desmethylazelastine: 52 hours (0.1% solution), 57 hours (0.15% solution)
Time to peak, serum: 2 to 3 hours (Azelastine [generic] 0.1% solution); 3 to 4 hours (Astepro)
Excretion: Feces (~75%, <10% as unchanged drug)
Clearance: 0.5 L/hour/kg
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Bitter taste, xerostomia (normal salivary flow resumes upon discontinuation), aphthous stomatitis, glossitis, and burning sensation in throat. Chronic use of antihistamines will inhibit salivary flow, particularly in elderly patients. May contribute to periodontal disease and oral discomfort.
Effects on Bleeding
No information available to require special precautions
Index Terms
Azelastine HCl; Azelastine Hydrochloride
FDA Approval Date
November 01, 1996
References
Astelin nasal spray (azelastine) [prescribing information]. Somerset, NJ: MEDA Pharmaceuticals; October 2014.
Astepro (azelastine) [package insert]. Somerset, NJ: Meda Pharmaceuticals Inc; September 2018.
Azelastine [prescribing information]. Bridgewater, NJ: Amneal Pharmaceuticals LLC; October 2018.
Azelastine spray [prescribing information]. Toronto, Ontario: Apotex Corp; December 2014.
Dykewicz MS, Fineman S, Nicklas R, et al, “Diagnosis and Management of Rhinitis: Complete Guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology. American Academy of Allergy, Asthma, and Immunology,” Ann Allergy Asthma Immunol, 1998, 81(5 Pt 2):478-518.[PubMed 9860027]
Wallace DV, Dykewicz MS, Bernstein DI, et al, “The Diagnosis and Management of Rhinitis: An Updated Practice Parameter,” J Allergy Clin Immunol, 2008, 122(2 Suppl):1-84.[PubMed 18662584]
Brand Names: International
Afluon (ES, GR, TR); Allergodil (AE, AT, BE, BG, BH, CH, CZ, DE, DK, EE, FR, HN, IT, JO, KW, LB, LT, LU, NL, PL, PT, QA, RO, RU, SA, SI, SK, TR, UA, VE); Allergospray (AT); Astelin (PK); Astepro (DK, IT, NL); Aze-Air (VN); Azela (PH, TW); Azelan (KR); Azelvin (SE); Azep (CN, IN, NZ, SG); Azep Nasal Spray (AU, HK, NZ); Azeptin Nasal (KR); Azetin (HK, TW); Lastin (FI, SE); Lergemed (EG); Min Qi (CN); Rhinolast (IE, IL, MT, PK); Rinalin (DO, GT, NI, PA, SV); Rino-Lastin (BR); Snizex (LK); Zalastin (EG, LB)
Last Updated 5/1/20
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