VA Class:OP300
ATC Class:S01BA13
Rimexolone is a synthetic nonfluorinated corticosteroid.
In ophthalmology, topical rimexolone is used prophylactically after ocular surgery (e.g., cataract extraction, with or without implantation of an intraocular lens) to prevent or relieve postoperative ocular inflammation. In controlled studies, topical application to the eye of rimexolone 1% was more effective than placebo in the management of postoperative anterior chamber inflammation as determined by slit-lamp biomicroscopic evaluation of number of anterior chamber cells and severity of anterior chamber flare.
In ophthalmology, topical rimexolone also is used in the treatment of anterior uveitis. Results from controlled clinical studies in patients with anterior uveitis (i.e., acute uveitis, recurrent iridocyclitis, or chronic uveitis) indicate that rimexolone 1% is as effective as prednisolone acetate 1% in reducing uveitic inflammation as determined by reductions from baseline in anterior chamber flare and anterior chamber cells.
Rimexolone is applied topically to the eye as an ophthalmic suspension. Care should be taken to avoid contamination of the suspension container. The suspension container should be shaken well immediately prior to use. The manufacturer warns that the commercially available rimexolone ophthalmic suspension is not for injection and should not be injected subconjunctivally or directly into the anterior chamber of the eye.
Safety and efficacy of rimexolone ophthalmic suspension in children have not been established.
For the prevention and relief of postoperative ocular inflammation in patients undergoing cataract extraction, the usual adult dosage of rimexolone is 1 or 2 drops of a 1% suspension in the eye(s) undergoing surgery 4 times daily beginning 24 hours after surgery. Rimexolone therapy usually is continued at this dosage for 2 weeks after surgery.
For the treatment of anterior uveitis, the usual adult dosage of rimexolone is 1 or 2 drops of a 1% suspension in the affected eye(s) every hour while awake for 7 days, then 1 drop every 2 hours while awake for an additional 7 days. Subsequent therapy should be adjusted based on severity of the disease and response to therapy. When the drug is discontinued, the dosage should be gradually tapered to avoid exacerbation of the disease. In one study, dosage was tapered to 1 or 2 drops in the affected eye(s) 4 times daily during the third week of therapy, twice daily for the subsequent 4 days, and then once daily for an additional 3 days to complete 4 weeks of therapy.
IOP should be monitored in patients receiving the drug for 10 days or longer.
Rimexolone is a synthetic nonfluorinated corticosteroid. Like fluorometholone and medrysone, rimexolone contains a methyl group at C-21. Omission of a hydroxyl group at C-21 and substitution of a methyl group at this position may reduce the risk of increased intraocular pressure (IOP) associated with topical ophthalmic corticosteroid therapy. Rimexolone occurs as a white powder. The drug has solubilities of 0.2 mcg/mL in water at 25°C and 2.96 mg/mL in methanol at 25°C.
Rimexolone ophthalmic suspension is a sterile, isotonic suspension of micronized rimexolone in a vehicle of purified water, mannitol, and carbomer 934P; sodium hydroxide and/or hydrochloric acid may be added to adjust pH to between 6-8. The commercially available suspension contains edetate disodium, polysorbate (Tweenrm) 80, benzalkonium chloride as a preservative, and sodium chloride to adjust tonicity. The ophthalmic suspension has an osmolality of 260-320 mOsm/kg.
Rimexolone ophthalmic suspension should be stored in a tight container at a temperature of 4-30°C. To prevent sedimentation in the dispensing tip, rimexolone ophthalmic suspension should be stored upright.
Additional Information
For further information on chemistry, pharmacology, pharmacokinetics, uses, cautions, and dosage and administration of rimexolone, see the EENT Corticosteroids General Statement 52:08.08.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
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