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  • CLASSES

    Ophthalmological Corticosteroids

    DEA CLASS

    Rx

    DESCRIPTION

    Ophthalmic corticosteroid
    Used for postoperative ocular inflammation or anterior uveitis
    Clinically equivalent to 1% prednisolone in reducing uveitic inflammation

    COMMON BRAND NAMES

    Vexol

    DOSAGE & INDICATIONS

    For the treatment of postoperative ocular inflammation.
    Ophthalmic dosage
    Adults, including the Geriatric

    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.

    For the treatment of anterior uveitis.
    Ophthalmic dosage
    Adults, including the Geriatric

    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.

    For the treatment of vernal keratoconjunctivitis†.
    Ophthalmic dosage
    Adults, including the Geriatric

    Apply 1—2 drops into the conjunctival sac of the affected eye four times daily.

    For use as an adjunct in the treatment of rheumatoid arthritis† involving the knee joint.
    Intra-articular dosage
    Adults

    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

    MAXIMUM DOSAGE

    Adults

    2 drops/eye every hour while awake for up to 1 week.

    Elderly

    2 drops/eye every hour while awake for up to 1 week.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Injectable Administration

    Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.

    Other Injectable Administration

     
    Intra-articular Administration
    Rimexolone is not approved by the FDA for intra-articular injection.
    Inject intra-articularly into the knee joint.

    Ophthalmic Administration

    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.

    STORAGE

    Vexol:
    - Protect from freezing
    - Store between 36 to 77 degrees F
    - Store upright

    CONTRAINDICATIONS / PRECAUTIONS

    Fungal infection, herpes simplex keratitis (dendritic keratitis), infection, mycobacterial infection, varicella, viral infection

    Corticosteroid therapy may mask and/or exacerbate acute purulent infections; thus, use of rimexolone is contraindicated in the presence of all types of infection of the eye. Do not use in the presence of fungal infection, viral infection, herpes simplex keratitis (dendritic keratitis), varicella, vaccinia, mycobacterial infection, and most other viral diseases of the cornea and conjunctiva. Additionally, secondary ocular infections may develop following prolonged use of the drug. Consider the possibility of an infection in any patient who experiences persistent corneal ulceration.

    Cataracts, glaucoma, visual disturbance

    Prolonged use of ophthalmic corticosteroids can induce or exacerbate acute angle closure glaucoma, damage the optic nerve, cause visual disturbance, and result in the formation of posterior subcapsular cataracts. Rimexolone is only indicated for short-term relief of ocular inflammation. If prolonged use (>= 10 days) is required, the manufacturer recommends monitoring intraocular pressure. Administer with caution in patients with ocular hypertension.

    Pregnancy

    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.

    Breast-feeding

    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.

    Children, infants, neonates

    Safe and effective use of rimexolone in children, infants, and neonates has not been established.

    Corticosteroid hypersensitivity

    Although true corticosteroid hypersensitivity is rare, patients who have demonstrated a prior hypersensitivity reaction to rimexolone should not receive any form of rimexolone. It is possible, though also rare, that such patients will display cross-hypersensitivity to other corticosteroids. It is advisable that patients who have a hypersensitivity reaction to any corticosteroid undergo skin testing, which, although not a conclusive predictor, may help to determine if hypersensitivity to another corticosteroid exists. Such patients should be carefully monitored during and following the administration of any corticosteroid.

    ADVERSE REACTIONS

    Severe

    ocular hypertension / Delayed / 1.0-5.0
    corneal erosion / Delayed / 0-1.0
    keratitis / Delayed / 0-1.0
    visual impairment / Early / Incidence not known

    Moderate

    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

    Mild

    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

    DRUG INTERACTIONS

    There are no drug interactions associated with Rimexolone products.

    PREGNANCY AND LACTATION

    Pregnancy

    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.

    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.