ASTEPRO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ASTEPRO (ASTEPRO).
Selective histamine H1 receptor antagonist; inhibits histamine release from mast cells and basophils, thereby reducing allergic symptoms.
| Metabolism | Hepatic via CYP3A4; active metabolite desmethylazelastine. |
| Excretion | Primarily renal elimination: approximately 70% of an oral dose is excreted unchanged in urine, with <10% as metabolites. Fecal elimination accounts for <20%. |
| Half-life | Terminal elimination half-life is approximately 28–36 hours. Clinical context: supports once-daily dosing; steady state reached after 5–7 days. |
| Protein binding | Approximately 88–90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 50 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intranasal bioavailability is approximately 70% (systemic exposure relative to intravenous). Oral bioavailability is <10% due to extensive first-pass metabolism. |
| Onset of Action | Intranasal: Onset within 30–60 minutes; significant symptom relief by 2 hours. |
| Duration of Action | Duration of action for symptom relief is approximately 24 hours, consistent with once-daily dosing. |
One 0.15% ophthalmic solution drop instilled into the affected eye(s) twice daily (approximately every 8 to 12 hours).
| Dosage form | SPRAY, METERED |
| Renal impairment | No dosage adjustment required for renal impairment based on available data; monitor for adverse effects in severe impairment (CrCl < 30 mL/min). |
| Liver impairment | No dosage adjustment recommended for hepatic impairment; use caution in severe impairment due to lack of data. |
| Pediatric use | For children 3 years and older: administer one drop in each affected eye twice daily. Safety and efficacy for ages <3 years have not been established. |
| Geriatric use | No specific dose adjustment needed; monitor for ocular adverse effects as elderly may have increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ASTEPRO (ASTEPRO).
| Breastfeeding | Unknown if azelastine is excreted in human milk; however, other antihistamines (e.g., chlorpheniramine) are excreted. M/P ratio not determined. Caution advised. Consider risk/benefit; prefer alternative agents when possible. |
| Teratogenic Risk | Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, azelastine (active ingredient) produced fetal abnormalities (skeletal malformations, omphalocele) at doses > 7 times the maximum recommended human daily inhalation dose. Risk cannot be ruled out. Use only if potential benefit justifies potential risk to fetus. Not recommended in first trimester due to theoretical risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to azelastine or any component of the formulation"]
| Precautions | ["Drowsiness; avoid driving or operating machinery","Avoid alcohol or CNS depressants","Use with caution in patients with renal impairment","Not recommended for children under 6 years"] |
| Food/Dietary | No significant food interactions. Alcohol may increase drowsiness; caution with concurrent use. |
| Clinical Pearls | ASTEPRO (azelastine hydrochloride) is a topical antihistamine nasal spray used for allergic rhinitis. Onset of action is within 30 minutes; maximal effect in 2-3 weeks. Bitter taste is common; advise patients to avoid sniffing deeply after administration. Not for acute exacerbations of asthma. |
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| Fetal Monitoring | Monitor for maternal adverse effects: sedation, dizziness, headache, bitter taste. Fetal monitoring: ultrasound for fetal development if used long-term or at high doses. No specific monitoring required if used as directed. |
| Fertility Effects | No specific human fertility studies. In animal studies, azelastine did not impair fertility at doses up to 20 mg/kg/day (approximately 20 times MRHDID). Effects on human fertility are unknown; unlikely to cause significant impairment. |
| Patient Advice | Prime the pump by spraying 4 times into the air before first use or if not used for 2 days. · Blow nose gently before use. Tilt head forward, insert nozzle into nostril, spray while breathing in gently. · Avoid sniffing deeply after spraying to reduce bitter taste. Rinse mouth if bitter taste occurs. · Use regularly for full effect; not for immediate relief of acute symptoms. · Inform your doctor if pregnant, planning to become pregnant, or breastfeeding. |