Rimexolone (Ophthalmic)

Rimexolone has been available as a corticosteroid eye drop solution for the treatment of swelling of the eyes due to injury, surgery, or anterior uveitis since 1994. Its parent company, Alcon, discontinued its availability in 2008.

Overview

Rimexolone, marketed by Alcon Pharmaceuticals as Vexol, has been available since 1994. It is supplied as a 1% eye drop solution that is applied topically to the eye. It is used primarily to treat swelling in the tissues of the eye. Its use was discontinued in 2008. Since that time, Vexol has been replaced with other similar treatment options such as prednisolone sodium phosphate or diclofenac sodium. Doctors and patients should be aware that there are fraudulent distributors claiming to offer supplies of Vexol, but this medication is no longer being produced at all under that name or in that particular formulation. Any stock of Vexol is either expired or a different formula or medication being sold as Vexol.

Rimexolone is not indicated for use of any sort of viral or bacterial infection of the eye as it does not contain any sort of antibiotic ingredient that would address the infection.

Rimexolone, or Vexol, does cause some side effects in patients. Typically, those side effects are very mild. Most common is a burning or stinging sensation upon application of the drops or a little blurry vision that corrects itself within a few minutes. However, it can occasionally have serious side effects such as changes in vision or increased risk of infections. Rarely, use of rimexolone has been linked to the onset of other illnesses such as rhinitis or pharyngitis. Prolonged use of this medication can cause the development of com/health/coma/">glaucoma or cataracts. Patients who have already had an issue with cataracts or glaucoma should use this medication only sparingly and under close medical supervision with frequent monitoring for those conditions. In very few cases, rimexolone has been linked to allergic reactions of various degrees from swelling of the eyes where applied to hives and skin rash. An allergic reaction is more likely in patients who have experienced hypersensitivity to other steroid and corticosteroid medications.

Rimexolone does interact negatively with a few medications. It should not be used in conjunction with or in proximity to the administration of any smallpox vaccine. It can worsen the gastrointestinal side effects associated with some chemotherapy and anticancer medications, especially those that treat aplastic anemia or renal cancers. Rimexolone generally should not be prescribed concomitantly with other steroid-based medications, as that can be an unsafe combination as well.

Overdose is not a really considered a danger with rimexolone. Patients would have really had to deliberately apply too much of the medication to result in any real danger to the eye itself. Chronic and prolonged use represents a far greater risk than an overdose at any given time.

Conditions Treated

  • Treatment for swelling of the eye after surgery
  • Inflammation of the eye caused by injury or infection
  • Anterior uveitis

Type Of Medication

  • Corticosteroid eye drop solution

Side Effects

Like any medication, rimexolone can cause side effects. These are usually quite mild and would not indicate that the patient needs to stop using this medication. Mild side effects include:

  • Bitter or unpleasant taste in the mouth
  • Headache
  • Sore throat
  • Dry eyes
  • Increased sensitivity to light
  • Runny nose
  • Blurry or hazy vision

Rarely, patients do experience more severe side effects that usually result in the patient going back to the doctor and changing medications. These can include:

  • Increased redness in the eyes
  • Swelling of the eyes
  • Changes in vision
  • Runny eyes that result in crusting around the eyes
  • Pain behind the eye
  • Severe pain in the eye
  • Seeing a halo effect around light

Some patients may experience an allergic reaction to rimexolone. That sort of reaction requires immediate medical attention and discontinuation of use of medication. Signs of an allergic reaction include:

  • Swelling of the lips
  • Difficult breathing
  • Swelling of the throat
  • Hives or rash
  • Swelling of the face

Dosage

The usual delivery of rimexolone is in the form of a 1% solution.

In treatment of swelling of the eye resulting from surgery, the recommended dosage protocol is one to two drops of Vexol (rimexolone) every six hours for a period of 14 days.

For treatment of anterior uveitis or injury, the standard protocol for treatment is one to two drops every hour during the waking day for one week. In the second week, the prescription is reduced to one to two drops every two hours during the day. Reduce usage from that point, applying as needed until the condition is resolved.

Overdose of rimexolone is not considered dangerous.

Interactions

While rimexolone is a relatively mild medication, it does interact with a few other medications. In terms of a moderate interaction where concomitant use is not contraindicated, the medications would include:

  • Bromfenac
  • Nepafenac
  • Diclofenac
  • Suprofen
  • Flurbiprofen
  • Ketorolac

All of these medications are ophthalmic medications as well.

A medication that interacts negatively and should not be used in conjunction with rimexolone is the smallpox vaccine, either in the brand name form of ACAM2000 or Dryvax. It is also contraindicated for patients taking the cancer medication Aldesleukin. Ceritinib and rimexolone taken in combination can cause an increased risk of hyperglycemia. Patients taking the iron chelator deferasirox for treatment of various anemias should add rimexolone with caution, as it has been shown to exacerbate the digestive issues that sometimes accompany use of deferasirox (i.e. bleeding of the gastrointestinal tract or ulceration of the GI tract).

Warnings

Patients who use rimexolone over an extended period of time are more likely to develop a fungal infection of the cornea. This should be monitored if the patient is using the eye drops for more than one round of treatment.

For patients suffering from viral infections of the eye, use of Vexol is contraindicated. Examples of these sorts of infections include conditions such as vaccinia, mycobacterial infection, varicella and epithelial herpes simplex keratitis. Use of Vexol (rimexolone) may extend the length of the infection or exacerbate the symptoms it causes.

Use of corticosteroids such as rimexolone can cause thinning of the sclera and/or the cornea. It may also compromise the patient's immune system, making infection more likely.

Extended use of Vexol has been linked to the development of glaucoma, cataracts and other forms of damage to the optic nerve. For patients with a history of cataracts or glaucoma, use of rimexolone should be approached cautiously and with medical supervision. It can also cause an increase in intraocular pressure, which may result in damage to the optic nerve or cornea and ultimately damage the vision of the patient.

Rimexolone should not be prescribed to patients who have shown hypersensitivity or an allergic response to steroids.

One danger of Vexol, particularly in prolonged use, is the masking of infection and other symptoms. It may also damage visual acuity, especially peripheral fields of vision.

Vexol ophthalmic solution is for topical use only. It should not be injected. The dropper that comes with the solution should not come in direct contact with the eye or any other surface as that can lead to contamination of the solution.

Patients should not use any other solutions or topical eye medications in conjunction with Vexol, unless prescribed by their physician.

Patients who wear contact lenses should discuss this with their doctor and whether or not these can be worn while using rimexolone.

There has been no indication that use of rimexolone while pregnant represents any danger to the fetus. This is also true for nursing mothers and infants, but patients in either situation should proceed with caution.

Patients should share with their physician any other medications they are taking, both prescription and over the counter. This is especially true if they take inhaled nasal steroids on a regular basis. While rimexolone does not interact adversely with many medications, patients respond differently to various combinations of medication. If the patient's condition does not improve within a few days of beginning treatment, the physician should consider alternative therapies.

In less than 2% of cases, use of rimexolone has been linked to the onset of chronic headache, pharyngitis, hypotension, dysgeusia, and rhinitis.

Rimexolone has not been studied in pediatric patients and is not recommended for use in children.

Storage

Vexol (rimexolone) is delivered as a 1% solution in a vial with an eye dropper. It should be stored upright and at room temperature. The bottle should remain tightly closed and stored away from direct sunlight and excessive moisture. It should be kept out of the reach of children and pets. This medication is only viable for four weeks after it has been opened. Patients should dispose of medication once they have completed their course of treatment, even if some of the solution remains.

Summary

Rimexolone, brand name Vexol, is a corticosteroid ophthalmic solution for use in the treatment of certain eye conditions linked to inflammation, swelling and pain in the eye caused by injury, surgery or other non-infectious cause. It is not indicated for treatment of viral or bacterial eye infection. It is also not approved for use with pediatric patients.

RImexolone is prescribed as a 1% solution and is a relatively mild medication that has limited interaction with other families and classes of drugs. Its major interactions are with certain anticancer and chemotherapy drugs and with the small pox vaccine. It is also not recommended as a first line of treatment for patients with a history of glaucoma or cataracts as prolonged use of Vexol may cause a recurrence of these conditions.

Prescribed dosages are usually one to two drops every couple of hours for seven days with a reduction in application times in the second week of treatment. If the patient's condition has not improved within 14 days of use of Vexol, the prescribing physician should reevaluate and explore other treatment options.

Production of Vexol was discontinued in 2008 and is no longer available for prescription or treatment. Other similar medications are available, including flurbiprofen sodium and bromfenac, that have a similar mechanism of action.