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Azelastine Hydrochloride
Overview
What is Astelin?
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 CHCINO•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, 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.
What does Astelin look like?
What are the available doses of Astelin?
Sorry No records found.
What should I talk to my health care provider before I take Astelin?
Sorry No records found
How should I use Astelin?
Astelin Nasal Spray is indicated for the treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in adults and children 5 years and older, and for the treatment of the symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion and postnasal drip in adults and children 12 years and older.
The recommended dose of Astelin Nasal Spray in adults and children 12 years and older with seasonal allergic rhinitis is one or two sprays per nostril twice daily. The recommended dose of Astelin Nasal Spray in children 5 years to 11 years of age is one spray per nostril twice daily.
What interacts with Astelin?
Astelin Nasal Spray is contraindicated in patients with a known hypersensitivity to azelastine hydrochloride or any of its components.
What are the warnings of Astelin?
Sorry No Records found
What are the precautions of Astelin?
Activities Requiring Mental Alertness:
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Nursing Mothers:
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Pediatric Use:
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Geriatric Use:
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What are the side effects of Astelin?
To report SUSPECTED ADVERSE REACTIONS, contact Meda Pharmaceuticals Inc. at 1-800-526-3840 or FDA at 1-800-FDA-1088 or .
Seasonal Allergic Rhinitis
| ADVERSE EVENT | Astelin Nasal Sprayn = 391 | VehiclePlacebon = 353 |
| Bitter Taste | 19.7 | 0.6 |
| Headache | 14.8 | 12.7 |
| Somnolence | 11.5 | 5.4 |
| Nasal Burning | 4.1 | 1.7 |
| Pharyngitis | 3.8 | 2.8 |
| Dry Mouth | 2.8 | 1.7 |
| Paroxysmal Sneezing | 3.1 | 1.1 |
| Nausea | 2.8 | 1.1 |
| Rhinitis | 2.3 | 1.4 |
| Fatigue | 2.3 | 1.4 |
| Dizziness | 2.0 | 1.4 |
| Epistaxis | 2.0 | 1.4 |
| Weight Increase | 2.0 | 0.0 |
ADVERSE REACTIONS
| ADVERSE EVENT | Astelin Nasal Sprayn = 216 | VehiclePlacebon = 210 |
| Bitter Taste | 19.4 | 2.4 |
| Headache | 7.9 | 7.6 |
| Dysesthesia | 7.9 | 3.3 |
| Rhinitis | 5.6 | 2.4 |
| Epistaxis | 3.2 | 2.4 |
| Sinusitis | 3.2 | 1.9 |
| Somnolence | 3.2 | 1.0 |
What should I look out for while using Astelin?
Astelin Nasal Spray is contraindicated in patients with a known hypersensitivity to azelastine hydrochloride or any of its components.
What might happen if I take too much Astelin?
There have been no reported overdosages with Astelin Nasal Spray. Acute overdosage by adults with this dosage form is unlikely to result in clinically significant adverse events, other than increased somnolence, since one bottle of Astelin Nasal Spray contains 30 mg of azelastine hydrochloride. Clinical studies 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 events. General supportive measures should be employed if overdosage occurs. There is no known antidote to Astelin Nasal Spray. Oral ingestion of antihistamines has the potential to cause serious adverse effects in young children. Accordingly, Astelin Nasal Spray should be kept out of the reach of children. Oral doses of 120 mg/kg and greater (approximately 460 times the maximum recommended daily intranasal dose in adults and children on a mg/m basis) were lethal in mice. Responses seen prior to death were tremor, convulsions, decreased muscle tone, and salivation. In dogs, single oral doses as high as 10 mg/kg (approximately 260 times the maximum recommended daily intranasal dose in adults and children on a mg/m basis) were well tolerated, but single oral doses of 20 mg/kg were lethal.
How should I store and handle Astelin?
Store at 20 - 25° C (68 - 77° F) [See USP Controlled Room Temperature].See the FDA-approved Medication Guide.Store at 20 - 25° C (68 - 77° F) [See USP Controlled Room Temperature].See the FDA-approved Medication Guide.Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, () is supplied as a package containing 200 metered sprays in a high-density polyethylene (HDPE) bottle fitted with a metered-dose spray pump unit. Patient instructions are also provided. The spray pump unit consists of a nasal spray pump fitted with a blue safety clip and a blue plastic dust cover.The Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, bottle contains 30 mg (1 mg/mL) of azelastine hydrochloride. The bottle can deliver 200 metered sprays. Each spray delivers a mean of 0.137 mL solution containing 137 mcg of azelastine hydrochloride.Storage:U.S. Patents 5,164,194; D447,419.Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, () is supplied as a package containing 200 metered sprays in a high-density polyethylene (HDPE) bottle fitted with a metered-dose spray pump unit. Patient instructions are also provided. The spray pump unit consists of a nasal spray pump fitted with a blue safety clip and a blue plastic dust cover.The Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, bottle contains 30 mg (1 mg/mL) of azelastine hydrochloride. The bottle can deliver 200 metered sprays. Each spray delivers a mean of 0.137 mL solution containing 137 mcg of azelastine hydrochloride.Storage:U.S. Patents 5,164,194; D447,419.Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, () is supplied as a package containing 200 metered sprays in a high-density polyethylene (HDPE) bottle fitted with a metered-dose spray pump unit. Patient instructions are also provided. The spray pump unit consists of a nasal spray pump fitted with a blue safety clip and a blue plastic dust cover.The Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, bottle contains 30 mg (1 mg/mL) of azelastine hydrochloride. The bottle can deliver 200 metered sprays. Each spray delivers a mean of 0.137 mL solution containing 137 mcg of azelastine hydrochloride.Storage:U.S. Patents 5,164,194; D447,419.Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, () is supplied as a package containing 200 metered sprays in a high-density polyethylene (HDPE) bottle fitted with a metered-dose spray pump unit. Patient instructions are also provided. The spray pump unit consists of a nasal spray pump fitted with a blue safety clip and a blue plastic dust cover.The Astelin (azelastine hydrochloride) Nasal Spray, 137 mcg, bottle contains 30 mg (1 mg/mL) of azelastine hydrochloride. The bottle can deliver 200 metered sprays. Each spray delivers a mean of 0.137 mL solution containing 137 mcg of azelastine hydrochloride.Storage:U.S. Patents 5,164,194; D447,419.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
After intranasal administration, the systemic bioavailability of azelastine hydrochloride is approximately 40%. Maximum plasma concentrations (Cmax) are achieved in 2-3 hours. Based on intravenous and oral administration, the elimination half-life, steady-state volume of distribution, and plasma clearance are 22 hours, 14.5 L/kg, and 0.5 L/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. 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; however, clinical interaction studies with the known CYP3A4 inhibitor erythromycin failed to demonstrate a pharmacokinetic interaction. In a multiple-dose, steady-state drug interaction study in normal volunteers, cimetidine (400 mg twice daily), a nonspecific P450 inhibitor, raised orally administered mean azelastine (4 mg twice daily) concentrations by approximately 65%.
The major active metabolite, desmethylazelastine, was not measurable (below assay limits) after single-dose intranasal administration of azelastine hydrochloride. After intranasal dosing of azelastine hydrochloride to steady-state, plasma concentrations of desmethylazelastine range from 20-50% of azelastine concentrations. When azelastine hydrochloride is administered orally, desmethylazelastine has an elimination half-life of 54 hours. Limited data indicate that the metabolite profile is similar when azelastine hydrochloride is administered via the intranasal or oral route.
In vitro
Azelastine hydrochloride administered intranasally at doses above two sprays per nostril twice daily for 29 days resulted in greater than proportional increases in Cmax and area under the curve (AUC) for azelastine.
Studies in healthy subjects administered oral doses of azelastine hydrochloride demonstrated linear responses in Cmax and AUC.
Non-Clinical Toxicology
Astelin Nasal Spray is contraindicated in patients with a known hypersensitivity to azelastine hydrochloride or any of its components.Drug Interactions:
Cimetidine (400 mg twice daily) increased the mean Cmax and AUC of orally administered azelastine hydrochloride (4 mg twice daily) by approximately 65%. Ranitidine hydrochloride (150 mg twice daily) had no effect on azelastine pharmacokinetics.
Interaction studies investigating the cardiac effects, as measured by the corrected QT interval (QTc), of concomitantly administered oral azelastine hydrochloride and erythromycin or ketoconazole were conducted. Oral erythromycin (500 mg three times daily for seven days) had no effect on azelastine pharmacokinetics or QTc based on analyses of serial electrocardiograms. Ketoconazole (200 mg twice daily for seven days) interfered with the measurement of azelastine plasma concentrations; however, no effects on QTc were observed.
No significant pharmacokinetic interaction was observed with the coadministration of an oral 4 mg dose of azelastine hydrochloride twice daily and theophylline 300 mg or 400 mg twice daily.
Activities Requiring Mental Alertness:
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To report SUSPECTED ADVERSE REACTIONS, contact Meda Pharmaceuticals Inc. at 1-800-526-3840 or FDA at 1-800-FDA-1088 or .
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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