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 C₂₄H₃₄O₃ and a molecular weight of 370.53. Its chemical name is 11β-Hydroxy-16α, 17α-dimethyl-17-propionylandrosta-1,4-diene-3-one. The chemical structure of rimexolone is presented below:

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.

Last updated on RxList: 11/6/2007

VEXOL® 1% (rimexolone ophthalmic suspension) is indicated for the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.

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.

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 5mL in an 8mL 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 36°-77°F (2°-25°C).

DO NOT FREEZE.

SHAKE WELL BEFORE USING.

VEXOL® is a registered trademark of N.V. Organon. ALCON LABORATORIES, INC. Fort Worth, Texas 76134. USA. FDA Rev date: 10/18/2007

Last updated on RxList: 11/6/2007

Reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.

Ocular adverse reactions occurring in 1 - 5% of patients in clinical studies of VEXOL® 1% (rimexolone ophthalmic suspension) included blurred vision, discharge, discomfort, ocular pain, increased intraocular pressure, foreign body sensation, hyperemia and pruritus.

Other ocular adverse reactions occurring in less than 1% of patients included sticky sensation, increased fibrin, dry eye, conjunctival edema, corneal staining, keratitis, tearing, photophobia, edema, irritation, corneal ulcer, browache, lid margin crusting, corneal edema, infiltrate, and corneal erosion.

Non-ocular adverse reactions occurred in less than 2% of patients. These included headache, hypotension, rhinitis, pharyngitis, and taste perversion.

No information provided.

Last updated on RxList: 11/6/2007

FOR TOPICAL OPHTHALMIC USE ONLY. Not for injection. Use in the treatment of herpes simplex infection requires great caution and frequent slit-lamp examinations. Prolonged use may result in ocular hypertension /glaucoma, damage to the optic nerve, defects in visual acuity and visual fields, and posterior subcapsular cataract formation.

Prolonged use may also result in secondary ocular infections due to suppression of host response.

Acute purulent infections of the eye may be masked or exacerbated by the presence of corticosteroid medication. In those diseases causing thinning of the cornea or sclera, perforation has been known to occur with topical steroids. It is advisable that the intraocular pressure be checked frequently.

General

Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application. Fungal invasion must be considered in any persistent corneal ulceration where a steroid has been or is in use.

For ophthalmic use only. The initial prescription and renewal of the medication order beyond 14 days should be made by a physician only after examination of the patient with the aid of magnification, such as slit lamp biomicroscopy and where appropriate, fluorescein staining. If signs and symptoms fail to improve after two days, the patient should be reevaluated. If this product is used for 10 days or longer, intraocular pressure should be monitored even though it may be difficult in children and uncooperative patients (see WARNINGS).

Carcinogenesis, mutagenesis, impairment of fertility

Rimexolone has been shown to be non-mutagenic in a battery of in vitro and in vivo mutagenicity assays.

Fertility and reproductive capability were not impaired in a study in rats with plasma levels (42 ng/mL) approximately 200 times those obtained in clinical studies after topical administration ( < 0.2 ng/mL). Long-term studies have not been conducted in animals or humans to evaluate the carcinogenic potential of rimexolone.

Pregnancy: Pregnancy Category C.

Rimexolone has been shown to be teratogenic and embryotoxic in rabbits following subcutaneous administration at the lowest dose tested (0.5 mg/kg/day, approximately 2 times the recommended human ophthalmic dose). Corticosteroids are recognized to cause fetal resorptions and malformations in animals. There are no adequate and well-controlled studies in pregnant women. VEXOL® 1% (rimexolone ophthalmic suspension) should be used in pregnant women only if the potential benefit to the mother justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human breast milk. Nevertheless, caution should be exercised when topical corticosteroids are administered to a nursing woman; a decision should be made whether to discontinue nursing or discontinue therapy, taking into consideration the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Last updated on RxList: 11/6/2007

No information provided.

VEXOL® 1% (rimexolone ophthalmic suspension) is contraindicated in epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, varicella, and most other viral diseases of the cornea and conjunctiva; mycobacterial infection of the eye; fungal diseases of the eye; acute purulent untreated infections which, like other diseases caused by microorganisms, may be masked or enhanced by the presence of the steroid; and in those persons with hypersensitivity to any component of the formulation.

Last updated on RxList: 11/6/2007

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-labelled 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.

Last updated on RxList: 11/6/2007

Do not touch dropper tip to any surface, as this may contaminate the suspension.

Last updated on RxList: 11/6/2007

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

RIMEXOLONE - OPHTHALMIC

(rih-MEX-oh-lone)

COMMON BRAND NAME(S): Vexol

USES: This medication is used to treat inflammation due to eye surgery or a certain eye condition (uveitis). It belongs to a class of drugs known as corticosteroids. Rimexolone works by relieving swelling.

HOW TO USE: To apply eye drops, wash your hands first. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface. Use as often as directed by your doctor.

If you are wearing contact lenses, remove them before using eye drops. Wait at least 15 minutes before replacing your contact lenses.

Shake this medicine well before using. Tilt your head back, look upward, and pull down the lower eyelid to make a pouch. Hold the dropper directly over your eye and place 1 drop into the pouch. Look downward and gently close your eyes for 1 to 2 minutes. Place one finger at the corner of your eye (near the nose) and apply gentle pressure. This will prevent the medication from draining out. Try not to blink and do not rub your eye. Repeat these steps for your other eye if so directed or if your dose is for more than 1 drop.

Do not rinse the dropper. Replace the dropper cap after each use.

If you are using another kind of eye medication (e.g., drops or ointments), wait at least 5 to 10 minutes before applying other medications. Use eye drops before eye ointments to allow the drops to enter the eye.

Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same times each day.

Continue using it for the full time prescribed. Do not stop using this medication without consulting your doctor. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.

Tell your doctor if your condition persists or worsens after 48 hours.

SIDE EFFECTS: Eye stinging/burning/redness, and temporary blurred vision may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Use of this medication for prolonged or repeated periods may result in a new eye infection (possibly fungal). Contact your doctor if you notice new eye symptoms (e.g., itch, yellow/green discharge).

Tell your doctor immediately if any of these unlikely but serious side effects occur: vision changes, headache, dizziness, sore throat, irritated/runny nose, new eye pain, dry eyes, change in taste.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using rimexolone, tell your doctor or pharmacist if you are allergic to it; other corticosteroids (e.g., prednisone); or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: certain eye infections caused by viruses/mycobacteria/fungus.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: cataracts, recent eye surgery, glaucoma (open-angle), diabetes, severe nearsightedness (myopia), recent heart attack.

After you apply this drug, your vision may become temporarily blurred. Use caution while driving, using machinery, or doing any other activity that requires clear vision. Limit alcoholic beverages.

If you develop a new eye condition (e.g., infection, eye surgery, eye injury) while using these eye drops, discuss with your doctor whether you should start a new bottle of eye drops.

During pregnancy, this medication should be used only when clearly needed. If you become pregnant or think you may be pregnant, tell your doctor immediately. Discuss the risks and benefits with your doctor.

It is not known if rimexolone passes into breast milk when used as an eye drop. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This medicine may be harmful if swallowed. If swallowing or overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others. Infection may spread if this bottle is used by more than one person.

Laboratory and/or medical tests (e.g., intraocular pressure) may be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store between 36-77 degrees F (2-25 degrees C) away from light and moisture. Do not freeze. Keep bottle upright and tightly closed when not in use. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.