VEXOL - rimexolone suspension/ drops
Alcon Laboratories, Inc
DESCRIPTION
VEXOL� 1% Ophthalmic Suspension is a sterile, multi-dose topical ophthalmic suspension containing the corticosteroid, rimexolone. Rimexolone is a white, water-insoluble powder with an empirical formula of C24 H34 O3 and a molecular weight of 370.53. Its chemical name is 11β-Hydroxy-16α,17α-dimethyl-17-propio nylandrosta-1,4-diene-3-one.
Each mL Contains: Active ingredient: rimexolone 10 mg (1%). Preservative: benzalkonium chloride 0.01%. Inactive ingredients: carbomer 974P, polysorbate 80, sodium chloride, edetate disodium, sodium hydroxide and/or hydrochloric acid (to adjust pH) and purified water.
The pH of the suspension is 6.0 to 8.0 and the tonicity is 260 to 320 mOsmol/kg.
CLINICAL PHARMACOLOGY
Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation. Placebo-controlled clinical studies demonstrated that VEXOL� 1% Ophthalmic Suspension is efficacious for the treatment of anterior chamber inflammation following cataract surgery.
In two controlled clinical trials, VEXOL� 1% Ophthalmic Suspension demonstrated clinical equivalence to 1% prednisolone acetate in reducing uveitic inflammation. In a controlled 6-week study of steroid responsive subjects, the time to raise intraocular pressure was similar for VEXOL� 1% Ophthalmic Suspension and 0.1% fluorometholone given four times daily.
As with other topically administered ophthalmic drugs, VEXOL� 1% (rimexolone ophthalmic suspension) is absorbed systemically. Studies in normal volunteers dosed bilaterally once every hour during waking hours for one week have demonstrated serum concentrations ranging from less than 80 pg/mL to 470 pg/mL. The mean serum concentrations were approximately 130 pg/mL. Serum concentrations were at or near steady state after 5 to 7 hourly doses. After decreasing the dosing frequency to once every two hours while awake during the second week of administration, mean serum concentrations were approximately 100 pg/mL.
The serum half-life of rimexolone could not be reliably estimated due to the large number of samples below the quantitation limit of the assay (80 pg/mL). However, based on the time required to reach steady-state, the half-life appears to be short (1 - 2 hours).
Based upon in vivo and in vitro preclinical metabolism studies, and on in vitro results with human liver preparations, rimexolone undergoes extensive metabolism. Following IV administration of radio-labeled rimexolone to rats, greater than 80% of the dose is excreted via the feces as rimexolone and metabolites. Metabolites have been shown to be less active than parent drug, or inactive in human glucocorticoid receptor binding assays.
INDICATIONS AND USAGE
VEXOL� 1% (rimexolone ophthalmic suspension) is indicated for the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.
DOSAGE AND ADMINISTRATION
Post-Operative Inflammation:
Apply one - two drops of VEXOL� 1% Ophthalmic Suspension into the conjunctival sac of the affected eye four times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period.
Anterior Uveitis:
Apply one - two drops of VEXOL� 1% Ophthalmic Suspension into the conjunctival sac of the affected eye every hour during waking hours for the first week, one drop every two hours during waking hours of the second week, and then taper until uveitis is resolved.
HOW SUPPLIED
5 mL and 10 mL in plastic DROP-TAINER� dispensers. VEXOL� 1% Ophthalmic Suspension is supplied in natural (clear) low density polyethylene (LDPE) bottles, with a natural LDPE dispensing plug and pink polypropylene closures. Fill volumes are 5 mL in an 8 mL bottle and 10 mL in a 10 mL bottle.
5 mL: NDC 0065-0627-07
10 mL: NDC 0065-0627-03
STORAGE: Store upright between 2�-25�C (36�-77�F).
DO NOT FREEZE.
SHAKE WELL BEFORE USING.
Rx Only
VEXOL� is a registered trademark of N.V. Organon.
ALCON LABORATORIES, INC.
Fort Worth, Texas 76134 USA
�2001, 2004, 2007, 2012 Novartis
