Vexol
Classes
Ophthalmological Corticosteroids
Administration
Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.
Intra-articular Administration
Rimexolone is not approved by the FDA for intra-articular injection.
Inject intra-articularly into the knee joint.
For ophthalmic use only. Shake well before use.
Instruct patient on proper instillation of eye solution (see Patient Information).
Do not to touch the tip of the dropper to the eye, fingertips, or other surface.
Adverse Reactions
ocular hypertension / Delayed / 1.0-5.0
corneal erosion / Delayed / 0-1.0
keratitis / Delayed / 0-1.0
visual impairment / Early / Incidence not known
hyperemia / Delayed / 1.0-5.0
blurred vision / Early / 1.0-5.0
hypotension / Rapid / 0-2.0
corneal edema / Early / 0-1.0
photophobia / Early / 0-1.0
cataracts / Delayed / Incidence not known
ocular infection / Delayed / Incidence not known
ocular irritation / Rapid / 1.0-5.0
ocular discharge / Delayed / 1.0-5.0
ocular pain / Early / 1.0-5.0
foreign body sensation / Rapid / 1.0-5.0
ocular pruritus / Rapid / 1.0-5.0
dysgeusia / Early / 0-2.0
rhinitis / Early / 0-2.0
headache / Early / 0-2.0
pharyngitis / Delayed / 0-2.0
xerophthalmia / Early / 0-1.0
Common Brand Names
Vexol
Dea Class
Rx
Description
Ophthalmic corticosteroid
Used for postoperative ocular inflammation or anterior uveitis
Clinically equivalent to 1% prednisolone in reducing uveitic inflammation
Dosage And Indications
Apply 1—2 drops into the conjunctival sac of the affected eye four times daily, beginning 24 hours after surgery and continuing through the first 2 weeks of the post-operative period.
Apply 1—2 drops into the conjunctival sac of the affected eye every hour during waking hours for the first week, 1 drop every 2 hours during waking hours of the second week and then taper until uveitis is resolved.
Apply 1—2 drops into the conjunctival sac of the affected eye four times daily.
In a study of several doses, a single intra-articular injection of 40 mg into the affected knee joint provided significant pain relief, improvement in stiffness, tenderness and mobility for 8—12 weeks. Clinical improvement was noted at doses of 10 or 20 mg, but a dose of 40 mg gave the longest duration of improvement.
†Indicates off-label use
Dosing Considerations
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
Renal ImpairmentSpecific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Drug Interactions
There are no drug interactions associated with Rimexolone products.
Maximum Dosage
2 drops/eye every hour while awake for up to 1 week.
Elderly2 drops/eye every hour while awake for up to 1 week.
AdolescentsSafety and efficacy have not been established.
ChildrenSafety and efficacy have not been established.
Mechanism Of Action
Mechanism of Action: Corticosteroids suppress or prevent inflammation and immune responses when administered at pharmacological doses. Inflammation can result from mechanical injury or from chemical or immunological irritation. Corticosteroids inhibit edema, cellular infiltration, capillary dilation, fibroblast proliferation, collagen deposition, and scar formation associated with inflammation. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, collectively called lipocortins. Lipocortins, in turn, control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of the precursor molecule arachidonic acid.Ocular application of corticosteroids can reduce aqueous outflow. This increases intraocular pressure, possibly inducing or exacerbating glaucoma. A comparative study over 6 weeks showed that ophthalmic rimexolone 1% raised intraocular pressure in a similar time to that of 0.1% fluorometholone.
Pharmacokinetics
Rimexolone is administered topically. Following topical administration, rimexolone is distributed into local tissue. Some systemic absorption also takes place. It is not known whether appreciable quantities of rimexolone are distributed into human breast milk. Serum concentrations achieve a steady state after 5—7 hourly doses. Rimexolone undergoes extensive metabolism. Animal studies showed that 80% of rimexolone and metabolites were excreted in the feces. Some metabolites exhibit glucocorticoid activity, but are less active than the parent drug. Although an accurate determination of serum half-life has not been ascertained, it appears to be between 1 and 2 hours.
Pregnancy And Lactation
Rimexolone is classified in FDA pregnancy category C. Animal studies using twice the recommended ophthalmic human dose produced teratogenic and embryotoxic effects. Other corticosteroids have been shown to cause fetal resorptions and malformations. Although there have been no adequate studies conducted into the safe use of rimexolone in pregnant women, it should only be used when the potential benefits to the mother outweigh possible risk to the fetus.
According to the manufacturer, caution should be exercised when ophthalmic corticosteroids are administered to breast feeding mothers. It is not known if ophthalmic administration of rimexolone causes enough systemic absorption to produce detectable quantities in breast-milk. Pharmacokinetic studies indicate that systemic absorption after ophthalmic administration of rimexolone is limited and therefore it is unlikely that a significant amount of drug would be excreted into breast-milk. To further minimize the amount of drug that reaches the systemic circulation and breast milk, apply pressure over the tear duct by the corner of the eye for 1 minute after ophthalmic administration. When used in low doses, systemically administered corticosteroids (e.g., prednisone) are distributed into breast milk in quantities not likely to have a deleterious effect on the infant. The American Academy of Pediatrics (AAP) has not evaluated the use of rimexolone in breast-feeding mothers; however, the AAP regards the corticosteroids prednisone and prednisolone to be usually compatible with lactation. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.