Rimexolone

Class: Corticosteroids
ATC Class: S01BA13
VA Class: OP300
Chemical Name: 11β-Hydroxy-16α, 17α-dimethyl-17-propionylandrosta-1,4-diene-3-one
Molecular Formula: C₂₄H₃₄O₃
CAS Number: 49697-38-3
Brands: Vexol

Introduction

A synthetic nonfluorinated corticosteroid.

Uses for Rimexolone

Postoperative Ocular Inflammation

Treatment of postoperative ocular inflammation following ocular surgery (e.g., cataract extraction).^a

Anterior Uveitis

Treatment of anterior uveitis.^a

Rimexolone Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye(s) as an ophthalmic suspension.^a

Avoid contamination of preparation container.^a

Shake suspension well before using.^a

Do not administer rimexolone by injection.

Dosage

Adults

Postoperative Ocular Inflammation

Ophthalmic

Instill 1 or 2 drops of 1% suspension into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery and continuing for 2 weeks.^a

Anterior Uveitis

Ophthalmic

Instill 1 or 2 drops of 1% suspension into the conjunctival sac of the affected eye(s) every hour while awake for 7 days, then 1 drop every 2 hours while awake for an additional 7 days.^a

Duration of subsequent therapy depends on severity of the disease and response to therapy.

Gradually taper the dosage when the drug is discontinued to avoid exacerbation of the disease.

Special Populations

No special population dosage recommendations at this time.^a

Cautions for Rimexolone

Contraindications

• 
  

  Known or suspected hypersensitivity to rimexolone or any ingredient in the formulation.^{a b}

  
  


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  Viral diseases of the cornea and conjunctiva (e.g., epithelial herpes simplex keratitis [dendritic keratitis], vaccinia, varicella).^{a b}

  
  


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  Mycobacterial infection of the eye.^{a b}

  
  


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  Fungal disease of ocular structures.^{a b}

  
  


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  Acute purulent untreated infections.^{a b}

  
  

Warnings/Precautions

Warnings

Ocular Effects

Risk of ocular hypertension or glaucoma (with damage to optic nerve), defects in visual acuity and fields of vision, and posterior subcapsular cataract formation with prolonged use of corticosteroids.^{a b c d e} Use with caution in glaucoma because intraocular pressure (IOP) may increase.^{b c d e}

In conditions causing thinning of the cornea or sclera, perforations reported with use of topical corticosteroids.^{a b}

Use of high-dose corticosteroids after cataract surgery may delay wound healing.^{b c d}

If used for ≥10 days, monitor IOP routinely even though monitoring may be difficult in children and uncooperative patients.^{a b}

Infections

See Contraindications under Cautions.

Prolonged use may suppress the host response and thus increase the risk of secondary ocular infections.^a

In acute purulent conditions of the eye, corticosteroids may mask infection or enhance existing infection.^a

Herpes Simplex

Use of corticosteroids in the treatment of herpes simplex infections other than epithelial herpes simplex keratitis, in which corticosteroids are contraindicated, requires great caution; periodic slit-lamp microscopy is essential.^{a b}

General Precautions

Evaluation of Ocular Condition

Initial prescription or renewal of medication order beyond 14 days should be provided only after examination of the patient with the aid of magnification (e.g., slit lamp biomicroscopy, fluorescein staining where appropriate).^a

Reevaluate patient if improvement does not occur after 2 days.^a

Fungal Infections

Long-term local corticosteroid application associated with development of fungal infections of the cornea.^a Consider possibility of fungal infection in patients with persistent corneal ulceration who have been or are receiving corticosteroid therapy.^{a b}

Specific Populations

Pregnancy

Category C.^a

Lactation

Not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in milk.^{a b}

Caution if used in nursing women.^a Manufacturer recommends that women discontinue nursing or the drug.^a

Pediatric Use

Safety and efficacy not established in pediatric patients.^a

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.^a

Common Adverse Effects

Elevated IOP,^a blurred vision,^a discharge,^a discomfort,^a ocular pain,^a foreign body sensation,^a hyperemia,^a pruritus.^a

Adverse systemic events include headache,^{a b} rhinitis,^{a b} pharyngitis,^{a b} taste perversion,^{a b} and hypotension.^{a b}

Rimexolone Pharmacokinetics

Absorption

Bioavailability

Absorbed systemically.^a

Elimination

Metabolism

Extensively metabolized; metabolites are inactive or less active than the parent drug.^a

Elimination Route

Following IV administration in animals, 80% excreted in the feces as rimexolone and metabolites.^a

Half-life

1–2 hours.^a

Stability

Storage

Ophthalmic

Suspension

Upright at 2–25°C.^a Do not freeze.^a

ActionsActions

• 
  

  Suppresses the inflammatory response to mechanical, chemical, or immunologic agents.^{a b}

  
  


• 
  

  Corticosteroids inhibit edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.^{a b}

  
  


• 
  

  Presence of a methyl group at position C-21 may reduce the risk of increased IOP associated with topical ophthalmic corticosteroid therapy.

  
  

Advice to Patients

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  Importance of learning and adhering to proper administration techniques to avoid contamination of the tip of the suspension container.^{a b}

  
  


• 
  

  Importance of informing a clinician if an intercurrent ocular condition (e.g., trauma, surgery, infection) develops during ophthalmic therapy.^b

  
  


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  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^a

  
  


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  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^a

  
  


• 
  

  Importance of informing patients of other important precautionary information.^a (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Rimexolone

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Ophthalmic	Suspension	1%	Vexol (with benzalkonium chloride)	Alcon

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions June 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

a. Alcon Laboratories. Vexol (rimexolone) 1% ophthalmic suspension prescribing information. Fort Worth, TX; 2003 Jun.

b. AHFS drug information 2007. McEvoy GK, ed. EENT corticosteroids general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2813-5.

c. Allergan, Inc. Blephamide (sulfacetamide sodium and prednisolone acetate) ophthalmic ointment prescribing information. Irvine, CA; 2004 Sep.

d. Allergan, Inc. FML Forte (fluorometholone) ophthalmic suspension prescribing information. Irvine, CA; 2004 Jun.

e. Bausch & Lomb. Alrex (loteprednol etabonate) ophthalmic suspension prescribing information. Tampa, FL; 2006 Apr.

More Rimexolone resources

• Rimexolone Side Effects (in more detail)
• Rimexolone Dosage
• Rimexolone Use in Pregnancy & Breastfeeding
• Rimexolone Drug Interactions
• Rimexolone Support Group
• 0 Reviews for Rimexolone - Add your own review/rating

Compare Rimexolone with other medications

• Postoperative Ocular Inflammation
• Uveitis