Azelastine

Selected Rx 0.1% treats seasonal allergic-rhinitis symptoms from age 5 and vasomotor-rhinitis symptoms from age 12. Selected Rx 0.15% treats seasonal and perennial allergic rhinitis from age 6. OTC Astepro Allergy temporarily relieves nasal congestion, runny nose, sneezing and itchy nose due to hay fever/other upper-respiratory allergies from age 6; it is not an inferred treatment for a viral cold.

Selected 0.05% eye drops treat eye itching associated with allergic conjunctivitis; safety/effectiveness below age 3 have not been established. They do not treat contact-lens-related irritation. Combination nasal products containing another ingredient have their own label and are outside this single-ingredient dosing summary.

Apotex Rx 0.1%: prime with 4 sprays or until a fine mist. Selected Rx 0.15% and manufacturer Astepro instructions: 6 sprays or until a fine mist. After≥ 3 days without use, selected nasal instructions require reprime with 2 sprays or until fine mist. Prime away from the face. Blow the nose, keep head forward/down and bottle upright, insert the tip gently, spray while sniffing gently and alternate nostrils. Do not tilt back immediately or inhale forcefully; this helps avoid bitter drainage. Clean/wipe as directed and replace clip/cap. Use the exact bottle’s leaflet if device differs.

Instill 1 drop into each affected eye twice daily. Use only in the eyes; wash hands and keep the dropper from contacting eye/lids/other surfaces. Do not wear contacts when eyes are red and do not treat contact-lens irritation with these drops. For soft-lens users whose eyes are not red, remove lenses and wait at least 10 minutes after instillation before reinsertion because benzalkonium chloride can be absorbed by the lens.

No fixed renal/hepatic dose-adjustment schedule is supplied in these selected labels. The selected Rx 0.15% full PI specifies age≥ 6, while its appended patient information says safety/effectiveness unknown below 6 months. This conflicting leaflet wording does not authorize infant treatment; follow verified exact-product prescribing information and ask a pharmacist/prescriber before treating younger children.

Selected Rx nasal PI sections 4 state none; this is not proof that allergy is safe. OTC Astepro says do not use with a prior allergic reaction to the product/ingredients. Eye drops are contraindicated for known or suspected component hypersensitivity. Review the exact product’s excipients and previous reactions.

The selected nasal and ophthalmic labels have no boxed warning. Nasal sedation, route-specific precautions and OTC age restrictions still apply.

Nasal effects include bitter taste, headache, somnolence, burning/irritation, sneezing, dry mouth and epistaxis; rates vary by regimen. Serious postmarketing reports include allergy and other systemic effects without reliably established frequency. Eye drops can cause transient burning/stinging, headache, bitter taste or temporary blur; assess significant pain or persistent visual change. Overdose/ingestion needs immediate medical/Poison Help advice, particularly for a child; supportive care is used and no nasal azelastine antidote is known. Do not assume low routine ocular absorption makes ingestion harmless.

Avoid concurrent alcohol or other CNS depressants with nasal azelastine because alertness and CNS performance may worsen. Discuss other sedating antihistamines, sleep medicines or tranquilizers before combining them.

Cimetidine increased orally administered azelastine exposure by about 65% in a study; this is not an intranasal or ocular dose-adjustment algorithm. Oral erythromycin studies did not show a significant pharmacokinetic/QTc effect; ketoconazole interfered with the assay, so unchanged drug exposure cannot be inferred. No universal CYP-specific adjustment or no-interactions claim is supported. The selected eye label supplies no dedicated interaction study/regimen.

Selected 0.1% nasal seasonal use begins at 5, vasomotor at 12; selected 0.15% Rx/OTC nasal use begins at 6; eye-drop data below 3 are lacking. Do not extrapolate across brands or from contradictory Rx 0.15% leaflet text. Nasal geriatric trials were limited, so start cautiously based on organ function/co-medication; eye labeling observed no overall older-versus-younger difference.

Oral single-dose studies found higher azelastine exposure with CrCl< 50 mL/min; oral hepatic-impairment studies found no PK influence. These observations do not establish universal nasal/ocular safety or a fixed adjustment schedule. Assess sedation and comorbidity and use the exact product’s regimen; no selected eye-label impairment algorithm is provided.

Nasal-label limited postmarketing pregnancy experience has not identified a drug-associated adverse outcome signal; this does not establish absence of risk. Selected eye label lacks adequate controlled pregnancy studies and advises use when benefit justifies risk. Human milk/infant/milk-production data are lacking; nasal 0.1% labeling advises watching for infant milk rejection potentially related to bitterness. OTC requires health-professional advice in pregnancy/breastfeeding. Weigh maternal need and feeding benefits rather than assigning obsolete letter categories.

Azelastine is a relatively selective H1 antagonist. Experimental effects also include suppression of histamine/other mediator release; these findings do not make it a corticosteroid or establish treatment for every inflammatory eye/nasal condition.

Nasal absorption

Systemic bioavailability about 40%. Selected 0.1% peak 2–3 hours; selected 0.15% median peak 4 hours after the studied dose.

Ocular exposure

Low systemic levels after ocular treatment; these measurements do not apply to swallowed bottle contents.

Metabolism / binding

Oxidative CYP metabolism to active desmethylazelastine; specific responsible isoforms not identified. Approximate binding 88% parent,97% metabolite.

Half-life distinctions

Selected 0.15% intranasal study: parent 25 hours, metabolite 57 hours. The 22-hour value in other labeling is based on oral/IV administration, not an interchangeable route measurement.

Elimination

About 75% of an oral radiolabeled dose recovered in feces; this mass-balance route is distinct from topical administration.

Assess symptom response, adherence and exact device/drop technique; review sedation, alcohol/sedatives, epistaxis/nasal injury and eye discomfort/blur or allergic symptoms. Confirm ages and OTC restrictions. No routine laboratory monitoring interval or drug-level target is specified by these labels.

Keep nasal head position downward and sniff gently; do not share spray or use in eyes. Prime the correct bottle and count labeled sprays; liquid remaining after the metered limit may not deliver a reliable dose. For a clogged selected spray, remove and soak the pump unit in warm water, pump to clear, air-dry, reassemble and reprime; never use a pin. Use eye drops with clean technique and lens precautions. Keep products away from children and contact Poison Help for ingestion.

Ingredient / route

Azelastine HCl 1 mg/mL (0.1%) · intranasal.

Delivered dose

137 mcg azelastine HCl in 0.137 mL per spray after priming.

Labeler / example NDC

Apotex · 60505-0833-5,200-metered-spray bottle.

U.S. status

Prescription ANDA product; no DEA schedule.

Selected Rx 0.1% nasal

137 mcg HCl per metered spray; 30 mg HCl in bottle.

Selected Rx 0.15% nasal

205.5 mcg HCl per 0.137 mL spray; 30 mL/200 sprays,45 mg HCl. Selected repack NDC 68071-2498-3; underlying Apotex ANDA labeling.

OTC Astepro Allergy

0.15%,205.5 mcg HCl (187.6 mcg azelastine base) per spray; Bayer NDA OTC product, ages≥ 6. Bottle counts/sizes vary; read package.

Selected ophthalmic 0.05%

0.5 mg/mL HCl (0.457 mg/mL base); Gland 6 mL bottle NDC 68083-287-01. Benzalkonium chloride 0.125 mg/mL preservative.

Product scope

No azelastine/fluticasone combination dose, non-U.S. oral product or exhaustive brand-stock claim is inferred.

Selected Rx nasal sprays: upright 20–25°C, protect from freezing, close cap; discard after 200 metered sprays even if liquid remains, and respect EXP. OTC Astepro: 20–25°C, protect from freezing; retain carton and User Guide and follow its count/expiry. Selected eye drops: upright 2–25°C, cap tightly and avoid tip contamination. Do not apply one product’s storage temperature or an invented after-opening discard interval to every brand.