Pharmacokinetic and Tolerability Comparison Between Over-the-Counter and Prescription Azelastine Hydrochloride Nasal Spray for Allergic Rhinitis Management

Allergic rhinitis (AR) is an inflammatory condition that affects millions worldwide, causing significant healthcare costs and impairment in quality of life. While clinical guidelines recommend intranasal antihistamines as a first-line treatment for AR, current prescription azelastine hydrochloride 0.1% (HCl) nasal sprays have limitations in accessibility and strength. Additionally, palatability and dosing regimen have also been reported as factors associated with suboptimal adherence to nasal spray therapy. This review examines how over-the-counter (OTC) azelastine HCl available in the United State (US) compares with the prescription version with respect to accessibility, formulation characteristics, and dosing. The US Food and Drug Administration approved 0.15% azelastine HCl for OTC use in 2021. A newly published pharmacokinetic study reveals that OTC azelastine HCl provides greater drug exposure than its prescription counterpart (0.10% azelastine HCl) without significantly altering the drug’s pharmacokinetic or safety profile. Furthermore, OTC azelastine HCl can be administered once daily, as opposed to twice daily, and it moderates the drug’s bitter taste. The OTC 0.15% azelastine HCl formulation demonstrates a higher concentration of the active compound compared to the 0.10% prescription form, as well as flexible dosing and increased palatability. This review suggests that the OTC formulation may facilitate greater systemic exposure while maintaining a similar safety profile compared to the prescription formulation, providing an accessible management strategy for appropriate patients with AR.