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July 1983

Topically Applied OxymetazolineOcular Vasoconstrictive Activity, Pharmacokinetics, and Metabolism

Author Affiliations

From the Department of Ophthalmology, University of California at Irvine College of Medicine (Drs Duzman, Anderson, and Leopold); the Department of Ophthalmology, Jundiai (Brazil) School of Medicine (Dr Vita); and the Departments of Clinical Research (Dr Duzman) and Biostatistics (Mr Lue) and the Biochemistry Department (Drs Anderson and Chen), Allergan Pharmaceuticals, Irvine, Calif.

Arch Ophthalmol. 1983;101(7):1122-1126. doi:10.1001/archopht.1983.01040020124022

• Two double-blind, random-assignment clinical trials demonstrated the effectiveness of topical oxymetazoline hydrochloride in reducing histamine-induced hyperemia. Oxymetazoline hydrochloride at an optimum strength of 0.025% produced a marked and prolonged reduction of hyperemia, with the onset of effect occurring within one to five minutes of instillation. Safety indicators, including BP, heart rate, intraocular pressure, pupil size, and visual acuity, did not change significantly from baseline values. Oxymetazoline was absorbed slowly into the eye: only 0.006% of the original drug concentration was found in the aqueous humors of rabbits 30 minutes after instillation; the balance remained primarily in external ocular tissues. Metabolic studies in rabbits indicated that excreted amounts of unmetabolized radioactive oxymetazoline in urine following drug administration were similar (23%) for the ocular and nasal routes of application. The proportions of oxymetazoline metabolite to unchanged oxymetazoline were constant for all administration routes tested.

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