Azelastine Hcl

— THERAPEUTIC CATEGORIES —
  • Rhinitis/rhinorrhea (intranasal products)
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Azelastine Hcl Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Azelastine HCl 137mcg/spray; aqueous nasal spray; contains benzalkonium chloride.

    Pharmacological Class

    Antihistamine.

    How Supplied

    Contact supplier

    Manufacturer

    Various generic manufacturers

    Mechanism of Action

    Azelastine HCl, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans.

    Azelastine Hcl Indications

    Indications

    Seasonal allergic rhinitis. Vasomotor rhinitis.

    Azelastine Hcl Dosage and Administration

    Adult

    ≥12yrs: Seasonal allergic rhinitis: 1–2 sprays in each nostril twice daily. Vasomotor rhinitis: 2 sprays in each nostril twice daily.

    Children

    Seasonal allergic rhinitis: <5yrs: not established; 5–11yrs: 1 spray in each nostril twice daily. Vasomotor rhinitis: not established.

    Azelastine Hcl Contraindications

    Not Applicable

    Azelastine Hcl Boxed Warnings

    Not Applicable

    Azelastine Hcl Warnings/Precautions

    Warnings/Precautions

    Avoid eyes. Pregnancy. Nursing mothers: monitor infants.

    Warnings/Precautions

    Somnolence inActivities Requiring Mental Alertness

    • Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking azelastine HCl nasal spray 0.1%.

    Alcohol and other CNS depressants

    • Avoid concomitant use with alcohol and other CNS depressants due to the potential risk of further decreased alertness and impairment of CNS performance.

    Pregnancy Considerations

    Risk Summary

    • Limited data from post-marketing experience over decades of use with azelastine HCl nasal spray, 0.1% in pregnant women have not identified any drug associated risks of miscarriage, birth defects, or other adverse maternal or fetal outcomes. 

    Nursing Mother Considerations

    Risk Summary

    • There are no data on the presence of azelastine HCl in human milk, the effects on the breastfed infant, or the effects on milk production. 

    • Monitor breastfed infants for signs of milk rejection.

    • Consider the developmental and health benefits of breastfeeding along with mother’s clinical need for azelastine HCl nasal spray, 0.1% and any potential adverse effects on the breastfed infant or from the underlying maternal condition.

    Clinical Considerations

    • Monitoring for Adverse Reactions: Monitor breastfed infants of lactating women treated with azelastine HCl nasal spray for possible signs of milk rejection related to the bitter taste of azelastine.

     

    Pediatric Considerations

    • Safety and effectiveness of azelastine HCl nasal spray, 0.1% 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 Considerations

    • Use caution in elderly patients, usually starting at the low end of the dosing range.

    Azelastine Hcl Pharmacokinetics

    Absorption

    • Systemic bioavailability: approximately 40%.

    • Maximum plasma concentrations are achieved in 2 to 3 hours.

    Distribution

    • Steady-state volume of distribution: 14.5 L/kg.

    • 88% plasma protein bound.

    Metabolism

    • Oxidatively metabolized by the CYP450 enzyme system.

    Elimination

    • Fecal (75%). 

    • Half-life: 22 hours.

    Azelastine Hcl Interactions

    Interactions

    Potentiates CNS depression with alcohol, other CNS depressants. Caution with other antihistamines.

    Azelastine Hcl Adverse Reactions

    Adverse Reactions

    Bitter taste, headache, somnolence, dysesthesia, nasal burning, pharyngitis, dry mouth, paroxysmal sneezing, nausea, rhinitis, fatigue, dizziness, epistaxis, weight increase, myalgia. Children: also conjunctivitis, cough, asthma.

    Azelastine Hcl Clinical Trials

    Clinical Trials

    Seasonal Allergic Rhinitis – Two Sprays Per Nostril Twice Daily

    • Approval was based on data from 3 placebo-controlled clinical trials evaluating the efficacy and safety of azelastine HCl nasal spray 0.1% in 322 patients with seasonal allergic rhinitis, including 55 pediatric patients aged 12 to 16 years. Patients received 2 sprays per nostril twice a day of either azelastine HCl nasal spray or placebo for up to 4 weeks.

    • Efficacy was based on the 12-hour reflective Total Symptom Complex (TSC) and Major Symptom Complex (MSC).

    • Azelastine HCl nasal spray showed a greater decrease in the MSC compared with placebo. In dose-ranging trials, there was a statistically significant decrease in symptoms in the azelastine arm compared with placebo within 3 hours after initial dosing and persisted over the 12-hour dosing interval.

    Seasonal Allergic Rhinitis – One Spray Per Nostril Twice Daily

    • Approval was based on data from 2 placebo-controlled clinical trials evaluating the efficacy and safety of azelastine HCl nasal spray 0.1% in 275 patient with seasonal allergic rhinitis. Patients received 1 spray per nostril twice a day of either azelastine HCl nasal spray or placebo for up to 2 weeks.

    • Efficacy was based on the 12-hour reflective Total Nasal Symptom Score (rTNSS). The primary efficacy endpoint was the change from baseline to Day 14 in rTNSS.

    • Azelastine HCl nasal spray achieved a greater mean change in rTNSS at Day 14 from baseline compared with placebo.

    Vasomotor Rhinitis

    • Approval was based on data from 2 placebo-controlled clinical trials evaluating the efficacy and safety of azelastine HCl nasal spray 0.1% in 216 patients with vasomotor rhinitis. Patients received 2 sprays per nostril twice a day of azelastine HCl nasal spray or placebo for up to 4 weeks.

    • Azelastine HCl nasal spray 0.1% achieved a significantly greater decrease in symptom complex (rhinorrhea, post nasal drip, nasal congestion, sneezing) compared with placebo.

    Azelastine Hcl Note

    Notes

    Formerly known under the brand name Astelin.

    Azelastine Hcl Patient Counseling

    See Literature

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