azelastine (Astelin Nasal Spray, Astepro, Azelastine HCl, Rhinolast)
Dosing and uses of Astelin Nasal Spray, Astepro (azelastine)
Adult dosage forms and strengths
nasal spray
- 0.1% (137mcg/spray)
- 0.15% (205.5mcg/spray)
Seasonal Allergic Rhinitis
Astelin 0.1%: 1-2 sprays per nostril q12hr, Or
Astepro 0.15%: 2 sprays per nostril qDay
Perennial Allergic Rhinitis
Astepro 0.15%: 2 sprays per nostril q12hr
Vasomotor Rhinitis
Astelin 0.1%: 2 sprays per nostril q12hr
Administration
Prime with 4 sprays before initial use; if idle for 3 days, reprime with 2 sprays
Pediatric dosage forms and strengths
nasal spray
- 0.1% (137mcg/spray)
- 0.15% (205.5mcg/spray)
Seasonal Allergic Rhinitis
Astelin
- <6 years: Safety and efficacy not established
- 6-11 years: 1 spray per nostril q12hr
- ≥12 years: 1-2 sprays per nostril q12hr
Astepro
- <2 years: Safety and efficacy not established
- 2-5 years: 0.1%; 1 spray per nostril q12hr
- 6-11 years: 0.1% or 0.15%; 1 spray per nostril q12hr
- ≥12 years
- 0.1% or 0.15%: 1 or 2 sprays per nostril q12hr, or
- 0.15%: 2 sprays per nostril qDay
Perennial Allergic Rhinitis
Astepro
- <6 months: Safety and efficacy not established
- 6 months through 5 years: 0.1%; 1 spray per nostril q12hr
- 6-11 years: 0.1% or 0.15%; 1 spray per nostril q12hr
- ≥12 years: 0.15%; 2 sprays per nostril q12hr
Vasomotor Rhinitis
Astelin
- <12 years: Safety and efficacy not established
- ≥12 years: 2 sprays per nostril q12hr
Administration
Prime with 4 sprays before initial use; if idle for 3 days, reprime with 2 sprays
Astelin Nasal Spray, Astepro (azelastine) adverse (side) effects
>10%
Bitter taste (8-19.7%)
Headache (8-14.8%)
Somnolence (1-11.5%)
Cold symptoms/rhinitis (2-17%)
Cough (11%)
1-10%
Nasal burning (4.1%)
Sneezing (3.1%)
Dry mouth (2.8%)
Nausea (2.8%)
Conjunctivitis (2-5%)
Asthma (5%)
Fatigue (2.3%)
Rhinitis (2.3%)
Pharyngitis (4%)
Dizziness (2%)
Weight increase (2%)
Myalgia (<2%)
<1%
Amenorrhea
Breast pain
Constipation
Contact dermatitis
Eczema
Flushing
Glossitis
Hyperkinesia
Hypertension
Tachycardia
Vertigo
Vomiting
Postmarketing Reports
Anaphylactoid reaction
Application site irritation
Atrial fibrillation
Chest pain
Confusion
Dyspnea
Facial edema
Involuntary muscle contractions
Nasal sores
Palpitations
Paresthesia
Parosmia
Pruritus
Rash
Disturbance or loss of sense of smell and/or taste
Tolerance
Urinary retention
Vision abnormaL
Xerophthalmia
Warnings
Contraindications
Documented hypersensitivity
Cautions
May cause drowsiness
Caution in narrow angle glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction
Avoid concurrent CNS depressants that may add to somnolence
Caution in premature newborns and neonates
Caution in nursing women
Pregnancy and lactation
Pregnancy category: C
Lactation: Not known if excreted in breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Astelin Nasal Spray, Astepro (azelastine)
Mechanism of action
H1-receptor antagonist; inhibits release of histamine and other mediators involved in allergic response; may reduce hyperactivity of airways if used intranasally
Absorption
Bioavailability: 40%
Onset: 1-3 hr
Duration: 12 hr
Peak serum time: 2-4 hr
Distribution
Protein bound: 88%
Vd: 14.5 L/kg
Metabolism
Metabolized by hepatic P450
Metabolites: Desmethylazelastine
Elimination
Half-life: 22 hr
Clearance: 0.5 L/hr/kg
Excretion: Feces (75%)
