Azelastine is an antihistamine that blocks the histamine H-1 receptor inhibiting histamine release. It is used to treat the following conditions:

• For the relief of symptoms of perennial allergic rhinitis.

• For the relief of symptoms of allergic rhinitis and vasomotor rhinitis. 

Azelastine Dose in Adults

Dose in the treatment of Perennial allergic rhinitis:

• Astepro (0.15% solution):
  • Two sprays in each nostril two times a day.

Dose in the treatment of Seasonal allergic rhinitis: 

• Astepro (0.1% or 0.15% solution):
  • One or two sprays (0.1% solution) in each nostril two times a day or two sprays (0.15% solution) in each nostril once a day.
• Azelastine [generic] 0.1% solution:
  • One or two sprays in each nostril two times a day

Dose in the treatment of Vasomotor rhinitis:

• Azelastine [generic] 0.1% solution:
  • Two sprays in each nostril twice a day.

Azelastine Dose in Childrens

Dose in the treatment of Perennial allergic rhinitis: 

• Infants older than 6 months and Children less than 6 years:
  • 1% solution:
    • 1 spray per nostril twice a day.
• Children 6 - 12 years:
  • 1% or 0.15% solution:
    • 1 spray per nostril twice a day.
• Children older than 12 years and Adolescents:
  • 15% solution:
    • 2 sprays per nostril twice a day

Dose in the treatment of Seasonal allergic rhinitis: 

• Children 2 - 6 years:
  • 1% solution:
    • 1 spray per nostril twice a day.
• Children 6 - 12 years:
  • 1% or 0.15% solution:
    • 1 spray per nostril twice a day.
• Children older than 12 years and Adolescents:
  • 1% solution:
    • 1 or 2 sprays per nostril twice a day.
  • 15% solution:
    • 1 or 2 sprays per nostril twice a day or 2 sprays per nostril once a day.

Dose in the treatment of Vasomotor rhinitis: 

• Children older than 12 years and Adolescents:
  • 1% solution:
    • 2 sprays per nostril twice a day.

Pregnancy Risk Factor: C

• There are not many data on azelastine during pregnancy.
• It is absorbed through the nose and can cause side effects similar to those of other antihistamines.

Azelastine use during breastfeeding:

• It is unknown if the drug can be absorbed into breast milk.
• Continued treatment should be considered while breastfeeding.
• It is important to weigh the risks and benefits of continuing treatment for the mother against the potential exposure of the child to drugs 

Azelastine Dose in Renal Disease:

• Adjustment in the dose has not been recommended by the manufacturer in patients with renal disease.

Azelastine Dose in Liver Disease:

• Adjustment in the dose has not been recommended by the manufacturer in patients with liver disease.

Common Side Effects of Azelastine Include:

• Central nervous system:
  • Bitter taste
  • Headache
  • Drowsiness
• Infection:
  • Cold symptoms
• Respiratory:
  • Rhinitis
  • Cough

Less Common Side Effects of Azelastine Include:

• Central Nervous System:
  • Dysesthesia
  • Dizziness
  • Fatigue
• Dermatologic:
  • Contact Dermatitis
• Endocrine & Metabolic:
  • Weight Gain
• Gastrointestinal:
  • Dysgeusia
  • Nausea
  • Xerostomia
  • Vomiting
• Infection:
  • Upper Respiratory Tract Infection
• Neuromuscular & Skeletal:
  • Myalgia
• Ophthalmic:
  • Conjunctivitis
• Otic:
  • Otitis Media
• Respiratory:
  • Epistaxis
  • Asthma
  • Sinusitis
  • Burning Sensation Of The Nose
  • Pharyngitis
  • Nasal Discomfort
  • Sneezing
  • Sore Nose
  • Nasal Mucosa Ulcer
  • Pharyngolaryngeal Pain
• Miscellaneous:
  • Fever

Rare side effects:

• 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

Contraindication to Azelastine Include:

• The manufacturer's labeling does not contain any contraindications.

Warnings and Precautions

• CNS depression:
  • Antihistamines may cause CNS depression resulting in drowsiness.
  • Use caution when operating heavy machinery or performing tasks that require mental alertness.

Monitoring Parameters:

• None required

How to administer Azelastine?

• Intranasal administration:
  • Prime the nasal spray with 4 - 6 sprays prior to use or until a fine mist appears.
  • The spray should also be primed with 2 sprays if it has not been used for 3 or more days.
  • Clear the nostrils before use.
  • Insert the applicator into nostril keeping the bottle upright and closing the nostril.
  • Breath in and press the pump while inhaling aiming the spray tip towards the back of the nose.
  • Wipe the spray tip with a clean cloth or a tissue paper after each use.
  • Avoid spraying in the eyes or mouth.
  • After use do not tilt head back.

Mechanism of action of Azelastine:

• Azelastine competes with histamine for H-1 receptor sites on the effector cells. 
• This causes the inactivation of histamine and other mediators that mediate an allergy response.
• It stabilizes mast cells, increases motility of the bronchial epithelialcilia, and decreases hyperreactivity in the airways.

It has beenThe beginning of actionBetween 15 and 30 minutes maximum effectEasily viewed in 3 hours.

It has been aDuration of the actionapproximately 12 hours. 88% of the drug can be found inprotein-bound. 

It is primarilyMetabolizedIt is absorbed by the liver and has a bioavailability rate of around 40%.

It has been ahalf-life eliminationIt takes approximately 3 hours to get there. peak serum concentration.

International Brands of Azelastine:

• Afluon
• Allergodil
• Allergospray
• Astelin
• Astepro
• Azela
• Azelan
• Azelvin
• Azep
• Azep Nasal Spray
• Azeptin Nasal
• Azetin
• Lastin
• Lergemed
• Min Qi
• Rhinolast
• Rinalin
• Rino-Lastin
• Snizex
• Zalastin

Azelastine brands in Pakistan: