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Topically applied oxymetazoline. Ocular vasoconstrictive activity, pharmacokinetics, and metabolism
Archives of Ophthalmology (Chicago, Ill. : 1960)
|July 1, 1983
Summary
Topical oxymetazoline hydrochloride effectively reduces eye redness (hyperemia) within minutes. This 0.025% solution showed no significant safety concerns in clinical trials, making it a promising treatment.
Area of Science:
- Ophthalmology
- Pharmacology
Background:
- Histamine-induced hyperemia is a common ocular condition.
- Effective and safe treatments for ocular hyperemia are needed.
Purpose of the Study:
- To evaluate the efficacy and safety of topical oxymetazoline hydrochloride for reducing histamine-induced hyperemia.
- To determine the optimal concentration and onset of action.
Main Methods:
- Two double-blind, random-assignment clinical trials were conducted.
- Oxymetazoline hydrochloride at 0.025% was instilled topically.
- Safety indicators including BP, heart rate, IOP, pupil size, and visual acuity were monitored.
Main Results:
- Oxymetazoline hydrochloride (0.025%) significantly reduced hyperemia within 1-5 minutes.
- No significant changes in safety indicators were observed.
- Slow ocular absorption and consistent metabolism across administration routes were noted in rabbit studies.
Conclusions:
- Topical oxymetazoline hydrochloride (0.025%) is effective and safe for reducing histamine-induced hyperemia.
- The drug demonstrates rapid onset and prolonged action with minimal systemic absorption.