Oxymetazoline: A Comprehensive Pharmacological and Clinical Review

1. Introduction to Oxymetazoline

Overview, Historical Context, and Therapeutic Class

Oxymetazoline is an imidazole derivative that functions as a potent, direct-acting sympathomimetic agent. Its primary pharmacological activity is as an alpha (α)-adrenergic agonist.[1] Developed in 1961 by Wolfgang Fruhstorfer and Helmut Müller-Calgan at E. Merck Darmstadt, oxymetazoline was derived from xylometazoline.[2] Therapeutically, it is classified as a vasoconstrictor and topical decongestant, initially recognized for its utility in alleviating nasal congestion.[2]

The clinical applications of oxymetazoline have expanded considerably since its introduction. It is widely available in over-the-counter (OTC) intranasal sprays for the management of nasal congestion. Furthermore, its therapeutic scope now includes prescription formulations such as topical creams for persistent facial erythema associated with rosacea and ophthalmic solutions for acquired blepharoptosis (drooping eyelids) and nonspecific ocular redness.[1] Oxymetazoline is also a constituent of a combination product, Kovanaze, used to achieve regional anesthesia in certain dental procedures.[1]

The brand Afrin, a well-known oxymetazoline nasal spray, was first marketed as a prescription medication in 1966. Its success led to its transition to an over-the-counter product in 1975.[2] This long history of use, coupled with recent FDA approvals for novel indications—Rhofade for rosacea in 2017 and Upneeq for blepharoptosis in 2020—underscores the sustained therapeutic relevance and versatility of oxymetazoline.[1]