ASTEPRO ALLERGY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ASTEPRO ALLERGY (ASTEPRO ALLERGY).
Antihistamine; selectively antagonizes histamine H1 receptors, preventing histamine-mediated allergic responses.
| Metabolism | Hepatic via CYP3A4, with some contribution from CYP2D6; undergoes extensive first-pass metabolism. |
| Excretion | Primarily renal excretion; approximately 70-80% of a dose is excreted as unchanged drug in urine, with the remainder as metabolites. Fecal elimination accounts for <10%. |
| Half-life | Terminal elimination half-life is 22-26 hours. Clinical context: supports once-daily dosing; steady state achieved within ~5 days. |
| Protein binding | Approximately 88% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 3.1 L/kg; indicates extensive tissue distribution beyond plasma volume. |
| Bioavailability | Intranasal: approximately 1% due to local administration and minimal systemic absorption. |
| Onset of Action | Intranasal: within 30 minutes for relief of allergic rhinitis symptoms. |
| Duration of Action | 12 hours following intranasal administration; clinical efficacy supports twice-daily dosing (every 12 hours). |
| Molecular Weight | 307.8 |
One spray (205.5 mcg azelastine hydrochloride and 137 mcg fluticasone propionate) per nostril twice daily.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (CrCl <15 mL/min). |
| Liver impairment | For Child-Pugh class A or B: no adjustment. For Child-Pugh class C: avoid use due to lack of data. |
| Pediatric use | Children 6-11 years: one spray per nostril twice daily. Children ≥12 years: same as adult dose. |
| Geriatric use | No specific adjustment required, but monitor for increased systemic exposure and adverse effects. Use caution due to potential comorbidities and concomitant medications. |
| 1st trimester | Avoid due to lack of safety data and potential teratogenic risk. |
| 2nd trimester | Use only if clearly needed; no adequate well-controlled studies. |
| 3rd trimester | Use only if clearly needed; may cause neonatal adverse effects. |
Clinical note
Comprehensive clinical and safety monograph for ASTEPRO ALLERGY (ASTEPRO ALLERGY).
| Placental transfer | Not studied; expected to cross due to low molecular weight. |
| Breastfeeding | No data on excretion in human milk; manufacturer recommends caution. |
| Lactation Rating | L3 (Moderately Safe) |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to any componentSevere hepatic impairment
| Precautions | May cause drowsiness; avoid alcohol and CNS depressants. Use with caution in renal impairment (CrCl <30 mL/min) and hepatic impairment. Not recommended for severe hepatic impairment. |
| Food/Dietary | No significant food interactions. Grapefruit juice does not affect azelastine metabolism. Avoid alcohol due to additive sedative effects. |
| Clinical Pearls | ASTEPRO ALLERGY (azelastine hydrochloride 0.15% nasal spray) is a second-generation antihistamine. Onset of action is within 30 minutes. Bitter taste may occur; instruct patients to tilt head forward after spraying to minimize postnasal drip. Contains benzalkonium chloride; avoid in patients with nasal ulcers or recent nasal surgery. Not recommended for children under 6 years. |
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| Teratogenic Risk | ASTEPRO ALLERGY contains azelastine, a histamine H1-receptor antagonist. In animal studies, no teratogenic effects were observed at doses up to 7 times the maximum recommended human intranasal dose. There are no adequate and well-controlled studies in pregnant women. Risk cannot be ruled out; first trimester: consider benefit vs risk; second and third trimesters: no known specific fetal risks, but use caution. |
| Fetal Monitoring | No specific maternal or fetal monitoring required beyond standard prenatal care. Observe for maternal sedation or other CNS effects if used systemically. |
| Fertility Effects | Animal studies with azelastine showed no impairment of fertility at doses up to 7 times the maximum recommended human intranasal dose. No human data available. |
| Patient Advice | Prime pump by spraying 4 times or until a fine mist appears before first use and if not used for 3 or more days. · Tilt head slightly forward and spray away from the nasal septum to reduce risk of bleeding and bitter taste. · Do not exceed recommended dose (2 sprays per nostril twice daily). · Bitter taste is common; drinking a beverage afterward may help. · Avoid alcohol and other CNS depressants as they may increase drowsiness. · Inform your doctor if you have kidney disease, as dose adjustment may be needed. |