AZELASTINE HYDROCHLORIDE 137 ug Spray, Metered
Other active recalls for Azelastine Hydrochloride (different manufacturers) — 1 · tap to view
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Histamine-1 Receptor Antagonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Azelastine nasal spray is used to treat allergy symptoms: sneezing runny or itchy nose congestion Azelastine is in a class of medications called antihistamines. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms.
Read the full MedlinePlus article ↗- It treats two types of nasal conditions. The first is seasonal allergic rhinitis — that's hay fever, where your nose runs, you sneeze, and you feel congested because of allergens l...
- What exactly does azelastine nasal spray treat?
- It can, yes — drowsiness is one of the more common side effects. This is especially important to know before you drive or operate any machinery. Alcohol, sedatives, and tranquilize...
- That bitter taste is very common with azelastine — it's just how the medication tastes, and it's not a sign anything's wrong. A simple trick: tilt your head slightly downward while...
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII F5UM2KM3W7
Benzalkonium chloride is a chemical compound that works as a preservative and antimicrobial agent in medications. It prevents bacterial and fungal growth in liquid formulations to keep the product safe during storage and use.
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UNII 2968PHW8QP
A weak organic acid derived from citrus fruits or made through fermentation. It works as a buffer to control pH, a preservative to extend shelf life, and a flavoring agent in medications.
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UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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UNII RN3152OP35
Hypromellose is a plant-based thickener and film-former derived from cellulose. In medicines, it's used to create coatings on tablets and capsules, control how fast the drug dissolves, and improve the product's texture and stability.
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UNII 451W47IQ8X
Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
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UNII E1W4N241FO
A salt compound derived from phosphoric acid and sodium, used as a buffer to help maintain the medication's pH level and as a filler to give the tablet or capsule its proper form and size.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
7 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.277 | — |
| Medicaid paysCMS SDUD · 12 mo | $0.5614 | — |
| Medicare drug plans payPart D · Q2 2026 | $0.4445 | — |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Azelastine Hydrochloride 137 ugthis 59651-0214-30 | Aurobindo | 1 bottle | $0.277 | AB | Availability likely | — |
| Azelastine Hydrochloride 137 ug 60505-0833-05 | Apotex | 1 bottle | $0.277 | AB | Availability likely | — |
| Azelastine Hydrochloride 1 mg/mL 65162-0676-84 | Amneal | 1 bottle | $0.277 | AB | Availability likely | — |
| Azelastine 137 ug 67877-0477-50 | Ascend | 1 spray | $0.277 | AB | Availability likely | — |
| Azelastine Hydrochloride 137 ug 72603-0611-01 | NorthStar | 1 bottle | $0.277 | AB | Availability likely | — |
| Azelastine Hydrochloride 137 ug 47335-0779-91 | Sun | 1 bottle | $0.290 | — | FDA listed | +5% |
| Azelastine Hydrochloride 1 mg/mL 42291-0094-30 | AvKARE | 1 bottle | — | AB | FDA listed | — |
| Azelastine Hydrochloride 137 ug 50090-2330-00 | A-S | 1 bottle | — | AB | FDA listed | — |
| Azelastine Hydrochloride 137 ug 50090-7461-00 | A-S | 1 bottle | — | AB | FDA listed | — |
| Azelastine Hydrochloride 137 ug 68788-4056-02 | Preferred | 1 bottle | — | AB | FDA listed | — |
| Azelastine Hydrochloride 137 ug 68788-8514-02 | Preferred | 1 bottle | — | AB | FDA listed | — |
| Azelastine Hydrochloride 137 ug 71205-0449-30 | Proficient | 1 bottle | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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🗺️ Medicaid utilization & spend
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 59651-0214-30 You're viewing this | 1 BOTTLE, SPRAY in 1 CARTON (59651-214-30) / 200 SPRAY, METERED in 1 BOTTLE, SPRAY | 2020-05-08 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Azelastine hydrochloride 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. Azelastine hydrochloride Nasal Spray is an H 1 -receptor antagonist 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.
( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION For intranasal use only ( 2.3 ) Seasonal allergic rhinitis: Pediatric patients 5 to 11 years of age: 1 spray per nostril twice daily ( 2.1 ) Adults and adolescents 12 years of age and older: 1 or 2 sprays per nostril twice daily ( 2.1 ) Vasomotor rhinitis: 2 sprays per nostril twice daily in adults and adolescents 12 years of age and older ( 2.2 ) Prime Azelastine hydrochloride Nasal Spray before initial use and when it has not been used for 3 or more days ( 2.3 )
2.1Seasonal Allergic Rhinitis The recommended dosage of Azelastine hydrochloride 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 Azelastine hydrochloride Nasal Spray in pediatric patients 5 years to 11 years of age is one spray per nostril twice daily.
2.2Vasomotor Rhinitis The recommended dosage of Azelastine hydrochloride Nasal Spray in adults and adolescent patients 12 years and older with vasomotor rhinitis is two sprays per nostril twice daily.
2.3Important Administration Instructions Administer Azelastine hydrochloride Nasal Spray by the intranasal route only. Priming : Prime Azelastine hydrochloride Nasal Spray before initial use by releasing 4 sprays or until a fine mist appears. When Azelastine hydrochloride Nasal Spray has not been used for 3 or more days, reprime with 2 sprays or until a fine mist appears. Avoid spraying Azelastine hydrochloride Nasal Spray into the eyes.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 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 hydrochloride Nasal Spray: 137 mcg of azelastine hydrochloride in each 0.137 mL spray. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Somnolence: Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking Azelastine hydrochloride Nasal Spray. ( 5.1 ) Alcohol and other central nervous system (CNS) depressants: Avoid concurrent use with Azelastine hydrochloride Nasal Spray because further decreased alertness and impairment of CNS performance may occur. ( 5.1 )
5.1Somnolence in Activities Requiring Mental Alertness In clinical trials, the occurrence of somnolence has been reported in some patients taking Azelastine hydrochloride Nasal Spray [ see Adverse Reactions (6.1) ]. Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness and motor coordination such as operating machinery or driving a motor vehicle after administration of Azelastine hydrochloride Nasal Spray. Concurrent use of Azelastine hydrochloride Nasal Spray with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur [ see Drug Interactions (7.1) ].
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Use of Azelastine hydrochloride Nasal Spray has been associated with somnolence [ see Warnings and Precautions (5.1) ]. The most common adverse reactions (≥2% incidence) are: bitter taste, headache, somnolence, dysesthesia, rhinitis, nasal burning, pharyngitis, epistaxis, sinusitis, paroxysmal sneezing, nausea, dry mouth, fatigue, dizziness, and weight increase. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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 Azelastine hydrochloride Nasal Spray Two Sprays Per Nostril Twice Daily Adverse experience information for Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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 (%)] Azelastine hydrochloride 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%) Azelastine hydrochloride Nasal Spray One Spray Per Nostril Twice Daily Adverse experience information for Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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 Azelastine hydrochloride 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, g…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Central Nervous System Depressants Concurrent use of Azelastine hydrochloride Nasal Spray with alcohol or other central nervous system depressants should be avoided because reductions in alertness and impairment of central nervous system performance may occur [ see Warnings and Precautions (5.1) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Limited data from postmarketing experience over decades of use with azelastine hydrochloride in pregnant women have not identified any drug associated risks of miscarriage, birth defects, or other adverse maternal or fetal outcomes. In animal reproduction studies, there was no evidence of fetal harm at oral doses approximately 5 times the clinical daily dose. Oral administration of azelastine hydrochloride to pregnant mice, rats, and rabbits, during the period of organogenesis, produced developmental toxicity that included structural abnormalities, decreased embryo-fetal survival, and decreased fetal body weights at doses 270 times and higher than the maximum recommended human daily intranasal dose (MRHDID) of 1.096 mg.
However, the relevance of these findings in animals to pregnant women was considered questionable based upon the high animal to human dose multiple. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In an embryo-fetal development study in mice dosed during the period of organogenesis, azelastine hydrochloride caused embryo-fetal death, structural abnormalities (cleft palate; short or absent tail; fused, absent or branched ribs), delayed ossification, and decreased fetal weight at approximately 300 times the maximum recommended human daily intranasal dose (MRHDID) in adults (on a mg/m 2 basis at a maternal oral dose of 68.6 mg/kg/day), which also caused maternal toxicity as evidenced by decreased maternal body weight.
Neither fetal nor maternal effects occurred in mice at approximately 15 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 3 mg/kg/day). In an embryo-fetal development study in pregnant rats dosed during the period of organogenesis from gestation days 7 to 17, azelastine hydrochloride caused structural abnormalities (oligo-and brachydactylia), delayed ossification, and skeletal variations, in the absence of maternal toxicity, at approximately 270 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 30 mg/kg/day).
Azelastine hydrochloride caused embryo-fetal death and decreased fetal weight and severe maternal toxicity at approximately 610 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 68.6 mg/kg/day). Neither fetal nor maternal effects occurred at approximately 20 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 2 mg/kg/day). In an embryo-fetal development study in pregnant rabbits dosed during the period of organogenesis from gestation days 6 to 18, azelastine hydrochloride caused abortion, delayed ossification and decreased fetal weight and severe maternal toxicity at approximately 530 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 30 mg/kg/day).
Neither fetal nor maternal effects occurred at approximately 5 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 0.3 mg/kg/day). In a prenatal and postnatal development study in pregnant rats dosed from late in the gestation period and through the lactation period from gestation day 17 through lactation day 21, azelastine hydrochloride produced no adverse developmental effects on pups at maternal doses up to approximately 270 times the MRHDID (on mg/m 2 basis at a maternal dose of 30 mg/kg/day).
8.2Lactation Risk Summary There are no data on the presence of azelastine hydrochloride in human milk, the effects on the breastfed infant, or the effects on milk production. Breastfed infants should be monitored for signs of milk rejection during azelastine hydrochloride use by lactating women (see Clinical Considerations). The developmental and health benef…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Limited data from postmarketing experience over decades of use with azelastine hydrochloride in pregnant women have not identified any drug associated risks of miscarriage, birth defects, or other adverse maternal or fetal outcomes. In animal reproduction studies, there was no evidence of fetal harm at oral doses approximately 5 times the clinical daily dose. Oral administration of azelastine hydrochloride to pregnant mice, rats, and rabbits, during the period of organogenesis, produced developmental toxicity that included structural abnormalities, decreased embryo-fetal survival, and decreased fetal body weights at doses 270 times and higher than the maximum recommended human daily intranasal dose (MRHDID) of 1.096 mg.
However, the relevance of these findings in animals to pregnant women was considered questionable based upon the high animal to human dose multiple. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In an embryo-fetal development study in mice dosed during the period of organogenesis, azelastine hydrochloride caused embryo-fetal death, structural abnormalities (cleft palate; short or absent tail; fused, absent or branched ribs), delayed ossification, and decreased fetal weight at approximately 300 times the maximum recommended human daily intranasal dose (MRHDID) in adults (on a mg/m 2 basis at a maternal oral dose of 68.6 mg/kg/day), which also caused maternal toxicity as evidenced by decreased maternal body weight.
Neither fetal nor maternal effects occurred in mice at approximately 15 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 3 mg/kg/day). In an embryo-fetal development study in pregnant rats dosed during the period of organogenesis from gestation days 7 to 17, azelastine hydrochloride caused structural abnormalities (oligo-and brachydactylia), delayed ossification, and skeletal variations, in the absence of maternal toxicity, at approximately 270 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 30 mg/kg/day).
Azelastine hydrochloride caused embryo-fetal death and decreased fetal weight and severe maternal toxicity at approximately 610 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 68.6 mg/kg/day). Neither fetal nor maternal effects occurred at approximately 20 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 2 mg/kg/day). In an embryo-fetal development study in pregnant rabbits dosed during the period of organogenesis from gestation days 6 to 18, azelastine hydrochloride caused abortion, delayed ossification and decreased fetal weight and severe maternal toxicity at approximately 530 times the MRHDID in adults (on a mg/m 2 basis at a maternal oral dose of 30 mg/kg/day).
Neither fetal nor maternal effects occurred at approximately 5 times the MRHDID (on a mg/m 2 basis at a maternal oral dose of 0.3 mg/kg/day). In a prenatal and postnatal development study in pregnant rats dosed from late in the gestation period and through the lactation period from gestation day 17 through lactation day 21, azelastine hydrochloride produced no adverse developmental effects on pups at maternal doses up to approximately 270 times the MRHDID (on mg/m 2 basis at a maternal dose of 30 mg/kg/day).
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of Azelastine hydrochloride Nasal Spray for the treatment of symptoms of seasonal allergic rhinitis have been established for patients 5 years and older [ see Adverse Reactions (6.1) and Clinical Studies (14.1) ]. The safety and effectiveness of Azelastine hydrochloride Nasal Spray for the treatment of vasomotor rhinitis have been established for patients 12 years and older [ see Adverse Reactions (6.1) and Clinical Studies (14.2) ]. The safety and effectiveness of Azelastine hydrochloride Nasal Spray in pediatric patients below the age of 5 years with seasonal allergic rhinitis and in pediatric patients below the age of 12 years with vasomotor rhinitis have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical trials of Azelastine hydrochloride Nasal Spray did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE There have been no reported overdosages with Azelastine hydrochloride Nasal Spray. Acute overdosage by adults with this dosage form is unlikely to result in clinically significant adverse reactions, other than increased somnolence, since one bottle of Azelastine hydrochloride Nasal Spray contains 30 mg of azelastine hydrochloride. Clinical trials in adults with single doses of the oral formulation of azelastine hydrochloride (up to 16 mg) have not resulted in increased incidence of serious adverse reactions.
General supportive measures should be employed if overdosage occurs. There is no known antidote to Azelastine hydrochloride Nasal Spray. Oral ingestion of antihistamines has the potential to cause serious adverse effects in young children.
Accordingly, Azelastine hydrochloride Nasal Spray should be kept out of the reach of children.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H 1 -receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine hydrochloride Nasal Spray is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H 1 -receptor antagonist activity.
12.2Pharmacodynamics Cardiac Electrophysiology: In a placebo-controlled study (95 subjects with allergic rhinitis), there was no evidence of an effect of Azelastine hydrochloride Nasal Spray (2 sprays per nostril twice daily for 56 days) on cardiac repolarization as represented by the corrected QT interval (QTc) of the electrocardiogram. Following multiple dose oral administration of azelastine 4 mg or 8 mg twice daily, the mean change in QTc was 7.2 msec and 3.6 msec, respectively. Interaction studies investigating the cardiac repolarization effects of concomitantly administered oral azelastine hydrochloride and erythromycin or ketoconazole were conducted.
These drugs had no effect on QTc based on analysis of serial electrocardiograms. At a dose approximately 8 times the maximum recommended dose, azelastine hydrochloride does not prolong the QTc interval to any clinically relevant extent.
12.3Pharmacokinetics Absorption: After intranasal administration, the systemic bioavailability of azelastine hydrochloride is approximately 40%. Maximum plasma concentrations (C max ) are achieved in 2 to 3 hours. Azelastine hydrochloride administered intranasally at doses above two sprays per nostril twice daily for 29 days resulted in greater than proportional increases in C max and area under the curve (AUC) for azelastine.
Distribution: Based on intravenous and oral administration, the steady-state volume of distribution is
14.5L/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: Azelastine is oxidatively metabolized to the principal active metabolite, desmethylazelastine, by the cytochrome P450 enzyme system.
The specific P450 isoforms responsible for the biotransformation of azelastine have not been identified. After intranasal dosing of azelastine hydrochloride to steady-state, plasma concentrations of desmethylazelastine range from 20 to 50% of azelastine concentrations. Limited data indicate that the metabolite profile is similar when azelastine hydrochloride is administered via the intranasal or oral route.
Elimination: Based on intravenous and oral administration, the elimination half-life and plasma clearance are 22 hours and
0.5L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Special Populations: Hepatic Impairment: Following oral administration, pharmacokinetic parameters were not influenced by hepatic impairment.
Renal Impairment: Based on oral, single-dose studies, renal insufficiency (creatinine clearance <50 mL/min) resulted in a 70 to 75% higher C max and AUC compared to normal subjects. Time to maximum concentration was unchanged. Age: Following oral administration, pharmacokinetic parameters were not influenced by age.
Gender: Following oral administration, pharmacokinetic parameters were not influenced by gender. Race: The effect of race has not been evaluated. Drug-Drug Interactions: Erythromycin: No significant pharmacokinetic interaction was observed with the co-administration of orally administered azelastine (4 mg twice daily) with erythromycin (500 mg three times daily for 7 days).
In this study, co-administration of orally administered azelastine with erythromycin resulted in C max of 5.36 ± 2.6 ng/mL and AUC of 49.7 ± 24 ng•h/mL for azelastine, whereas, administration of azelastine alone resulte…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H 1 -receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine hydrochloride Nasal Spray is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H 1 -receptor antagonist activity.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Azelastine Hydrochloride Nasal Spray, 137 mcg is supplied as a 30 mL package (NDC 59651-214-30) 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 white safety clip and a transparent 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. Azelastine Hydrochloride Nasal Spray should not be used after the expiration date “EXP” printed on the medicine label and carton. Storage: Store upright at controlled room temperature 20° to 25°C (68° to 77°F).
Protect from freezing.
📋 Description ▾
11 DESCRIPTION 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 C 22 H 24 ClN 3 O•HCl with the following chemical structure: Azelastine hydrochloride Nasal Spray contains 0.1% azelastine hydrochloride USP in an aqueous solution at pH 6.8 ± 0.3. It also contains benzalkonium chloride (125 mcg/mL), citric acid monohydrate, disodium hydrogen phosphate dodecahydrate, edetate disodium, hypromellose, purified water, and sodium chloride. After priming [ see Dosage and Administration (2.3) ], each metered spray delivers a 0.137 mL mean volume containing 137 mcg of azelastine hydrochloride USP (equivalent to 125 mcg of azelastine base).
The bottle can deliver 200 metered sprays. Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA-approved patient labeling (Patient Information and Instructions for Use). Activities Requiring Mental Alertness Somnolence has been reported in some patients taking Azelastine hydrochloride Nasal Spray. Caution patients against engaging in hazardous occupations requiring complete mental alertness and motor coordination such as driving or operating machinery after administration of Azelastine hydrochloride Nasal Spray [ see Warnings and Precautions (5.1) ].
Concurrent Use of Alcohol and other Central Nervous System Depressants Instruct patients to avoid concurrent use of Azelastine hydrochloride Nasal Spray with alcohol or other central nervous system depressants because additional reductions in alertness and additional impairment of central nervous system performance may occur [ see Warnings and Precautions (5.1) ]. Common Adverse Reactions Inform patients that the treatment with Azelastine hydrochloride Nasal Spray may lead to adverse reactions, which include bitter taste, headache, somnolence, dysesthesia, rhinitis, nasal burning, pharyngitis, epistaxis, sinusitis, paroxysmal sneezing, nausea, dry mouth, fatigue, dizziness, and weight increase [ see Adverse Reactions (6.1) ].
Priming Instruct patients to prime the pump before initial use and when Azelastine hydrochloride Nasal Spray has not been used for 3 or more days [ see Dosage and Administration (2.3) ]. Keep Spray Out of Eyes Instruct patients to avoid spraying Azelastine hydrochloride Nasal Spray into their eyes. Keep Out of Children’s Reach Instruct patients to keep Azelastine hydrochloride Nasal Spray out of the reach of children.
If a child accidentally ingests Azelastine hydrochloride Nasal Spray, seek medical help or call a poison control center immediately. Distributed by: Aurobindo Pharma USA, Inc. 279 Princeton-Hightstown Road East Windsor, NJ 08520 Manufactured by: Aurobindo Pharma Limited Hyderabad-500 038, India Revised: 11/2020