Azelastine

Name: Azelastine

Azelastine Brand Names

Azelastine may be found in some form under the following brand names:

  • Astelin

  • Astepro

  • Dymista

  • Optivar

Side Effects of Azelastine

Side effects of azelastine nasal spray include:

  • unusual taste (bitter or sweet)
  • nose pain or discomfort
  • nosebleeds
  • headache
  • fatigue
  • sleepiness
  • sneezing

Side effects of azelastine eye drops include:

  • unusual taste (bitter or sweet)
  • eye irritation/stinging
  • headache
  • temporary blurring of vision
  • flu-like symptoms

Talk to your doctor about any side effect that is bothersome or that does not go away. 

This is not a complete list of azelastine side effects. Ask your doctor or pharmacist for more information.

Indications and Usage for Azelastine

Azelastine hydrochloride (HCl) nasal spray, 0.1% 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 Description

Azelastine HCl nasal spray, 0.1%, 137 micrograms (mcg), is an antihistamine formulated as a metered-spray solution for intranasal administration. Azelastine HCl, USP 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 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 C22H24ClN3O•HCl with the following chemical structure:

Azelastine HCl nasal spray, 0.1% contains 0.1% Azelastine HCl, USP in an aqueous solution at pH 6.8 ± 0.3. It also contains benzalkonium chloride (125 mcg/mL), citric acid, dibasic sodium phosphate, edetate disodium, hypromellose, purified water (pH 6.8) 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 HCl, USP (equivalent to 125 mcg of Azelastine base). The bottle can deliver 200 metered sprays.

Clinical Studies

14.1 Seasonal Allergic Rhinitis

Two Sprays Per Nostril Twice Daily

The efficacy and safety of Azelastine HCl nasal spray, 0.1% were evaluated in three placebo-controlled clinical trials of Azelastine HCl nasal spray, 0.1% including 322 patients with seasonal allergic rhinitis who received two sprays per nostril twice a day for up to 4 weeks. These trials included 55 pediatric patients ages 12 to 16 years. Assessment of efficacy was based on the 12-hour reflective Total Symptom Complex (TSC) and Major Symptom Complex (MSC). The MSC was calculated as the average of individual symptoms of nose blows, sneezes, runny nose/sniffles, itchy nose, and watery eyes as assessed by patients on a 0 to 5 categorical scale. Azelastine HCl nasal spray, 0.1% two sprays per nostril twice daily demonstrated a greater decrease in the MSC than placebo (Table 3).

Table 3: Mean Change from Baseline in Reflective MSC* in Adults and Adolescents ≥12 Years with Seasonal Allergic Rhinitis Treated with Azelastine HCl Nasal Spray, 0.1% Two Sprays Per Nostril Twice Daily Versus Placebo

Treatment

N

Baseline LS Mean (SD)

Change from Baseline (SD)

Treatment Difference

P-value

Trial 1: 12 Hour AM and PM Reflective MSC

Azelastine HCl Nasal Spray, 0.1%

63

11.48 (4.13)

-3.05 (3.51)

1.98

<0.01

Placebo Nasal Spray

60

10.84 (4.53)

-1.07 (3.52)

Trial 2: 12 Hour AM and PM Reflective MSC

Azelastine HCl Nasal Spray, 0.1%

63

12.50 (4.5)

-4.10 (3.46)

2.03

<0.01

Placebo Nasal Spray

63

12.18 (4.64)

-2.07 (4.01)

Trial 3: 12 Hour AM and PM Reflective MSC

Azelastine HCl Nasal Spray, 0.1%

66

12.04 (4.03)

-3.31 (3.74)

1.35

0.04

Placebo Nasal Spray

66

11.66 (3.96)

-1.96 (3.57)

* Major Symptom Complex (MSC): Average of individual symptoms of nose blows, sneezes, runny nose/sniffles, itchy nose, and watery eyes as assessed by patients on a 0 to 5 categorical scale.

In dose-ranging trials, administration of Azelastine HCl nasal spray, 0.1% two sprays per nostril twice daily resulted in a statistically significant decrease in symptoms compared to saline placebo within 3 hours after initial dosing and persisted over the 12-hour dosing interval.

One Spray Per Nostril Twice Daily

The efficacy and safety of Azelastine HCl nasal spray, 0.1% were evaluated in two placebo-controlled clinical trials of Azelastine HCl nasal spray, 0.1% including 275 patients with seasonal allergic rhinitis who received one spray per nostril twice a day for up to 2 weeks. Assessment of efficacy was based on the 12-hour reflective Total Nasal Symptom Score [rTNSS]. rTNSS is calculated as the sum of the patients scoring of four individual nasal symptoms (runny nose, sneezing, itchy nose, and nasal congestion) as assessed by patients on a 0 to 3 categorical scale. The primary efficacy endpoint was the change from Baseline to Day 14 in rTNSS. The mean change from baseline in rTNSS was greater in patients receiving Azelastine HCl nasal spray, 0.1% one spray per nostril twice daily than those receiving placebo (Table 4).

Table 4: Mean Change from Baseline in Reflective TNSS* in Adults and Adolescents ≥12 years with Seasonal Allergic Rhinitis Treated with Azelastine HCl Nasal Spray, 0.1% One Spray Per Nostril Twice Daily Versus Placebo

Treatment

N

Baseline LS Mean (SD)

Change from Baseline (SD)

Treatment Difference

P-value

Trial 4: 12 Hour AM and PM Reflective TNSS

Azelastine HCl Nasal Spray, 0.1%

138

16.34 (4.22)

-2.69 (4.79)

1.38

0.01

Placebo Nasal Spray

141

17.21 (4.32)

-1.31 (4.29)

Trial 5: 12 Hour AM and PM Reflective TNSS

Azelastine HCl Nasal Spray, 0.1%

137

16.62 (4.20)

-3.68 (4.16)

1.18

0.02

Placebo Nasal Spray

136

16.84 (4.77)

-2.50 (4.01)

* Total Nasal Symptom Score (TNSS): Average of individual symptoms of runny nose, sneezing, itchy nose, and nasal congestion as assessed by patients on a 0 to 3 categorical scale.

Two-week studies comparing the efficacy (and safety) of Azelastine HCl nasal spray, 0.1% two sprays per nostril twice daily versus one spray per nostril twice daily were not conducted.

14.2 Vasomotor Rhinitis

The efficacy and safety of Azelastine HCl nasal spray, 0.1% were evaluated in two placebo-controlled clinical trials of Azelastine HCl nasal spray, 0.1% including 216 patients with vasomotor rhinitis who received two sprays per nostril twice a day for up to 4 weeks. These patients had vasomotor rhinitis for at least one year, negative skin tests to indoor and outdoor aeroallergens, negative nasal smears for eosinophils, and negative sinus X-rays. Azelastine HCl nasal spray, 0.1% demonstrated a significantly greater decrease in a symptom complex comprised of rhinorrhea, post nasal drip, nasal congestion, and sneezing compared to placebo.

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