Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension, Ophthalmic:
Vexol: 1% (5 mL [DSC], 10 mL [DSC])
Pharmacology
Mechanism of Action
Suppresses the inflammatory response by inhibiting edema, capillary dilation, leukocyte migration and scar formation.
Pharmacokinetics/Pharmacodynamics
Absorption
Through aqueous humor
Metabolism
Hepatic for any amount of drug absorbed
Excretion
Urine and feces (>80%)
Half-Life Elimination
1 to 2 hours
Use: Labeled Indications
Ophthalmic inflammatory conditions: Treatment of postoperative inflammation following ocular surgery; treatment of anterior uveitis
Contraindications
Hypersensitivity to rimexolone or any component of the formulation; acute untreated purulent ocular infections; viral diseases of the cornea and conjunctiva (eg, epithelial herpes simplex keratitis [dendritic keratitis], vaccinia, varicella); mycobacterial or fungal infections of the eye
Documentation of allergenic cross-reactivity for corticosteroids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Dosage and Administration
Dosing: Adult
Note: Vexol has been discontinued in the United States since September 2016.
Anterior uveitis: Ophthalmic: Instill 1 to 2 drops in conjunctival sac of affected eye every hour during waking hours for the first week, then 1 drop every 2 hours during waking hours of the second week, and then taper until uveitis is resolved
Postoperative ocular inflammation: Ophthalmic: Instill 1 to 2 drops in conjunctival sac of affected eye 4 times daily beginning 24 hours after surgery and continuing through the first 2 weeks of the postoperative period
Dosing: Geriatric
Refer to adult dosing.
Administration
For topical ophthalmic use only; to avoid contamination, do not touch dropper tip to eyelids or other surfaces when placing drops in eyes. Shake well before using. The use of the same bottle for both eyes is not recommended in surgical patients.
Storage
Store upright at 2°C to 25°C (36°F to 77°F). Do not freeze.
Drug Interactions
Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Avoid combination
Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid therapy. Monitor therapy
Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Monitor therapy
Hyaluronidase: Corticosteroids may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving corticosteroids (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents (Ophthalmic): May enhance the adverse/toxic effect of Corticosteroids (Ophthalmic). Healing of ophthalmic tissue during concomitant administration of ophthalmic products may be delayed. Monitor therapy
Ritodrine: Corticosteroids may enhance the adverse/toxic effect of Ritodrine. Monitor therapy
Adverse Reactions
1% to 5%:
Central nervous system: Foreign body sensation of eye
Ophthalmic: Blurred vision, eye discharge, eye discomfort, eye pain, eye pruritus, increased intraocular pressure, ocular hyperemia
<2%:
Cardiovascular: Hypotension
Central nervous system: Headache
Gastrointestinal: Dysgeusia
Respiratory: Pharyngitis, rhinitis
Frequency not defined:
Infection: Secondary ocular infection
Ophthalmic: Cataract, eye disease (defects in visual activity), eye perforation, optic nerve damage
<1%, postmarketing, and/or case reports: Anterior chamber fibrin deposition, brow ache, conjunctival edema, corneal edema, corneal erosion, corneal infiltrates, corneal staining, corneal ulcer, crusting of eyelid, eye irritation, keratitis, lacrimation, ocular edema, photophobia, sticky sensation of eye, xerophthalmia
Warnings/Precautions
Concerns related to adverse effects:
- Cataracts: Prolonged use of corticosteroids may result in posterior subcapsular cataract formation. Use following cataract surgery may delay healing or increase the incidence of bleb formation.
- Corneal thinning: Various ophthalmic disorders, as well as prolonged use of corticosteroids, may result in corneal and scleral thinning. Continued use in a patient with thinning may result in perforation.
- Glaucoma: Prolonged use of corticosteroids may result in elevated intraocular pressure (IOP) and/or glaucoma; damage to the optic nerve; and defects in visual acuity and fields of vision. Use with caution in patients with glaucoma; monitor IOP in any patient receiving treatment for ≥10 days.
- Immunosuppression: Prolonged use of corticosteroids may increase the incidence of secondary infection (including fungal infections). Acute purulent ocular infections may be masked or exacerbated with use. Fungal infection should be suspected in any patient with persistent corneal ulceration who has received corticosteroids.
Special populations:
- Contact lens wearers: Some preparations contain benzalkonium chloride which may be adsorbed by contact lenses.
Other warnings/precautions:
- Appropriate use: Patients should be re-evaluated if symptoms fail to improve after 2 days. Initial prescription and renewal of medication should be made by healthcare provider only after examination with the aid of magnification such as slit lamp biomicroscopy or fluorescein staining (if appropriate). Corticosteroids should not be used to treat ocular herpes simplex. Use of same bottle in both eyes of postoperative patients is not recommended.
Monitoring Parameters
Intraocular pressure and periodic examination of lens (with prolonged use ≥10 days)
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events have been observed in animal reproduction studies following subcutaneous administration. The amount of rimexolone absorbed systemically following ophthalmic administration is low (<80 to 470 pg/mL).
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience foreign body sensation of eye. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, or eye discharge (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
