Azelastine is an antihistamine applied directly into the nose (nasal spray) to relieve allergic rhinitis symptoms — sneezing, runny nose and nasal itching. It acts locally, but part is absorbed into the circulation and can cause drowsiness, so caution is needed with alcohol and with activities requiring attention.
Also known as: Azelastina, Allergodil
No documented drug–drug interactions for this medicine.
FDA label, section 7: "Concurrent use of Azelastine HCl Nasal Spray with alcohol or other central nervous system depressants should be avoided because reductions in alertness and impairment of central nervous system performance may occur" — systemic absorption (~40%) potentiates alcohol-induced CNS depression.
Avoid alcohol during treatment with nasal azelastine; warn about the risk of reduced alertness (driving, machinery).
DailyMed/FDA (NIH/NLM) — approved Azelastine nasal spray label, section 7 Drug Interactions: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=77b20c6b-f30f-42a9-a0ef-d5d0bd3feb56
No documented disease interactions.
FDA label: limited postmarketing data over decades of use in pregnant women have not identified an associated risk of miscarriage, birth defects or other adverse maternal-fetal outcomes; no evidence of fetal harm in animal studies at oral doses ~5× the clinical daily dose.
May be used in pregnancy if the benefit justifies the risk; no risk identified in the available data.
No data on presence in human milk; monitor the breastfed infant for signs of milk rejection (related to taste alteration) during use (FDA label).
Not applicable (no specific contraception documented).
DailyMed/FDA (NIH/NLM) — approved Azelastine nasal spray label, section 8 Use in Specific Populations: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=77b20c6b-f30f-42a9-a0ef-d5d0bd3feb56
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
H1 antihistamine with selective antagonism of histamine H1 receptors; it also stabilises mast cells to a lesser degree. The clinical effect in rhinitis develops within minutes to hours after intranasal application.
Competitive, selective blockade of histamine H1 receptors in the nasal mucosa, reducing vasodilation, increased capillary permeability and the nerve-ending stimulation responsible for sneezing and itching.
Relevant systemic absorption for a topical drug: systemic bioavailability of approximately 40% after intranasal administration, with maximum plasma concentrations (Cmax) achieved in 2 to 3 hours (FDA label). This absorption profile explains the possible systemic effects (drowsiness).
Metabolised in the liver, mainly by CYP3A4, with formation of the active metabolite desmethylazelastine; the main route of elimination is renal (urinary excretion of the drug and metabolites).
Steady-state volume of distribution of 14.5 L/kg (iv/oral data); plasma protein binding of approximately 88% for azelastine and 97% for desmethylazelastine (FDA label).
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
