Dosing & Uses
Dosage Forms & 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
Dosage Forms & Strengths
nasal spray
- 0.1% (137mcg/spray)
- 0.15% (205.5mcg/spray)
Seasonal Allergic Rhinitis
Astelin
- <5 years: Safety and efficacy not established
- 5 to <12 years: 1 spray per nostril q12hr
- ≥12 years: 1-2 sprays per nostril q12hr
Astepro
- <2 years: Safety and efficacy not established
- 2 to <6 years: 0.1%; 1 spray per nostril q12hr
- 6-12 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 <6 years: 0.1%; 1 spray per nostril q12hr
- 6 to <12 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
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse 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 CNS depression/drowsiness; use caution when performing tasks requiring mental alertness eg, operating heavy machinery
Avoid administering concurrent CNS depressants that may add to somnolence
Caution in premature newborns and neonates
Pregnancy & Lactation
Pregnancy
Limited data from postmarketing experience over decades of use in pregnant women have not identified any drug associated risks of miscarriage, birth defects, or other adverse maternal or fetal outcomes
Animal data
- In animal reproduction studies, there was no evidence of fetal harm at oral doses approximately 5 times the clinical daily dose; oral administration to pregnant mice, rats, and rabbits, during the period of organogenesis, produced developmental toxicity that included structural abnormalities, decreased embryo-fetal survival, and decreased fetal body weights at doses 270 times and higher than maximum recommended human daily intranasal dose of 1.096 mg; relevance of these findings in animals to pregnant women considered questionable based upon high animal to human dose multiple
Lactation
There are no data on presence in human milk, effects on breastfed infant, or on milk production; breastfed infants should be monitored for signs of milk rejection during use by lactating women; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition
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
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%)
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Patient Handout
Formulary
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