Fluorometholone

Class: Corticosteroids
ATC Class: S01CA07
VA Class: OP300
Chemical Name: 9-fluoro-11ß,17-dihydroxy-6α-methylpregna-1,4-diene-3,20-dione
Molecular Formula: C24H31FO5
CAS Number: 426-13-1
Brands: Flarex, Fluor-Op, FML, FML-S, Tobraflex

Introduction

A synthetic fluorinated corticosteroid; structurally related to progesterone.a

Uses for Fluorometholone

Ophthalmic Inflammation

Symptomatic relief of corticosteroid-responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe. b c e g

Slideshow: Worried About Ebola? You’re More Likely to Get These 10 Serious Infections

Treatment of chronic anterior uveitisd f and corneal injury from burns or penetration of foreign bodies.d f g

Bacterial Ophthalmic Infections

Used for anti-inflammatory properties in conjunction with appropriate anti-infective therapy in some bacterial infections of the eye;d f g used in fixed combination with sulfacetamide sodium or tobramycin when such combination therapy is indicated.d f If an ophthalmic corticosteroid is used in combination with an ophthalmic anti-infective, weigh benefits against risks.g (See Infections under Cautions.)

Fluorometholone Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye(s) as an ophthalmic ointment or suspension.b c d e f g

Not for injection.b d f

Shake suspension vigorously prior to use.b d e f

Avoid contamination of the preparation container.a b c d e f

Do not administer suspensions containing benzalkonium chloride while wearing soft contact lenses.b e (See Advice to Patients.)

Dosage

Available as fluorometholone and fluorometholone acetate, alone or in fixed combination with anti-infectives; dosage of fluorometholone acetate expressed in terms of the salt.b c d e f

Pediatric Patients

Ophthalmic Inflammation
Ophthalmic

Fluorometholone 0.1% suspension: In children ≥2 years of age, instill 1 drop into the conjunctival sac of the affected eye(s) 2–4 times daily.e During initial 24–48 hours, dosage may be increased to 1 drop every 4 hours.e

Fluorometholone 0.25% suspension: In children ≥2 years of age, instill 1 drop into the conjunctival sac of the affected eye(s) 2–4 times daily.h

Fluorometholone 0.1% ointment: In children ≥2 years of age, apply ribbon of ointment (approximately 1.3 cm in length) into the conjunctival sac of the affected eye(s) 1–3 times daily.c May be applied every 4 hours during initial 24–48 hours of therapy.c

If improvement does not occur after 2 days, reevaluate the patient.c e h

Duration of therapy depends on the type and severity of the disease and response to therapy.a Do not discontinue prematurely.a c e h

In chronic conditions, gradually taper the dosage when the drug is discontinued to avoid exacerbation of the disease.a c e h

Bacterial Ophthalmic Infections
Ophthalmic

Fluorometholone and sulfacetamide sodium ophthalmic suspension: In children ≥2 years of age, instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily.d

Fluorometholone acetate and tobramycin ophthalmic suspension: In children ≥2 years of age, instill 1 or 2 drops into the conjunctival sac of the affected eye(s) every 4–6 hours.f During initial 24–48 hours, dosage may be increased to 1 or 2 drops every 2 hours.f

If improvement does not occur after 2 days, reevaluate the patient.d

Duration of therapy depends on the type and severity of the disease and response to therapy.a Do not discontinue prematurely.a d f

In chronic conditions, gradually taper the dosage when the drug is discontinued to avoid exacerbation of the disease.a d

Adults

Ophthalmic Inflammation
Ophthalmic

Fluorometholone 0.1% suspension: Instill 1 drop into the conjunctival sac of the affected eye(s) 2–4 times daily.e During initial 24–48 hours, dosage may be increased to 1 drop every 4 hours.e

Fluorometholone 0.25% suspension: Instill 1 drop into the conjunctival sac of the affected eye(s) 2–4 times daily.h

Fluorometholone 0.1% ointment: Apply ribbon of ointment (approximately 1.3 cm in length) into the conjunctival sac of the affected eye(s) 1–3 times daily.c May be applied every 4 hours during initial 24–48 hours of therapy.c

Fluorometholone acetate 0.1% suspension: Instill 1 or 2 drops into the conjunctival sac of the affected eye(s) 4 times daily.b During initial 24–48 hours, dosage may be increased to 2 drops every 2 hours.b

If improvement does not occur after 2 days, reevaluate the patient.c e h

Duration of therapy depends on the type and severity of the disease and response to therapy.a Do not discontinue prematurely.a c e h

In chronic conditions, gradually taper the dosage when the drug is discontinued to avoid exacerbation of the disease.a c e h

Bacterial Ophthalmic Infections
Ophthalmic

Fluorometholone and sulfacetamide sodium ophthalmic suspension: Instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily.d

Fluorometholone acetate and tobramycin ophthalmic suspension: Instill 1 or 2 drops into the conjunctival sac of the affected eye(s) every 4–6 hours.f During initial 24–48 hours, dosage may be increased to 1 or 2 drops every 2 hours.f

If improvement does not occur after 2 days, reevaluate the patient.d

Duration of therapy depends on the type and severity of the disease and response to therapy.a Do not discontinue prematurely.a d f

In chronic conditions, gradually taper the dosage when the drug is discontinued to avoid exacerbation of the disease.a d

Special Populations

No special population dosage recommendations at this time.a b c d e f h

Cautions for Fluorometholone

Contraindications

  • Viral diseases of the cornea and conjunctiva (e.g., epithelial herpes simplex keratitis [dendritic keratitis], vaccinia, varicella).b c d e f g h

  • Mycobacterial infection of the eye.b c d e f g h

  • Fungal disease of ocular structures.b c d e f g h

  • Acute, purulent, untreated infections of the eye.b g

  • Known hypersensitivity to fluorometholone, other corticosteroids, or any ingredient in the formulation.b c d e f g h

Warnings/Precautions

Warnings

Ocular Effects

Risk of glaucoma (with damage to optic nerve), defects in visual acuity and fields of vision, and posterior subcapsular cataract formation with prolonged use of corticosteroids.b c d e f g h Use with caution in glaucoma because IOP may increase.b c d e f g h

Average time until IOP increase occurs is longer with fluorometholone than with ophthalmic dexamethasone.b c d e f h

If used for ≥10 days, monitor IOP routinely even though monitoring may be difficult in children and uncooperative patients.c d e f g h

In conditions causing thinning of the cornea or sclera, perforations reported with use of topical corticosteroids.b c d e f g h

Use of high-dose corticosteroids may delay healing.b c e g Use after cataract surgery may delay healing and increase incidence of bleb formation.c d e g h

Infections

See Contraindications under Cautions.

Prolonged use may suppress the host response and thus increase the risk of secondary ocular infections.b c d e f g h

In acute purulent conditions of the eye, corticosteroids may mask infection or enhance existing infection.b c d e f g h

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.b d c g h

General Precautions

Evaluation of Ocular Condition

Initial prescription or renewal of medication order beyond 8 g of 0.1% ointment or 20 mL of 0.1 or 0.25% suspension should be provided only after examination of the patient with the aid of magnification (e.g., slit lamp biomicroscopy, fluorescein staining where appropriate).c d e h

Reevaluate patient if improvement does not occur after 2 days.c d e h

Fungal Infections

Long-term local corticosteroid application associated with development of fungal infections of the cornea.b c d e f g Consider possibility of fungal infection in patients with persistent corneal ulceration who have been or are receiving corticosteroid therapy.b c d e f g

Use of Fixed Combinations

When fluorometholone or fluorometholone acetate is used in fixed combination with sulfacetamide sodium or tobramycin, consider the cautions, precautions, and contraindications associated with the concomitant agent.d f

Ophthalmic Ointments

Use of ophthalmic ointments may decrease rate of corneal reepithelialization.c g

Specific Populations

Pregnancy

Category C.b c d e f h

Lactation

Not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in milk.b c d e f h

Caution if used in nursing women.b f Most manufacturers recommend that women discontinue nursing or the drug.c d e h

Pediatric Use

Safety and efficacy of fluorometholone alone or in fixed combination with sulfacetamide sodium or fluorometholone acetate in fixed combination with tobramycin not established in children <2 years of age.a c d e f h

Manufacturer states that safety and efficacy of fluorometholone acetate alone have not been established in children of any age.a b

Geriatric Use

No substantial differences in safety or efficacy relative to younger patients.c d e f h

Common Adverse Effects

Elevated IOP,c d e h transient stinging or burning,e g h blurred vision,e g h ocular irritation,e g h taste perversion.e h

Fluorometholone Pharmacokinetics

Absorption

Bioavailability

Corticosteroids are absorbed through the aqueous humor; because only low doses are given, little if any systemic absorption occurs.g

Stability

Storage

Ophthalmic

Ointment

<25°C. c Avoid exposure to temperatures >40°C. c

Suspension

Fluorometholone or fluorometholone acetate suspension: 2–27°C.a b Do not freeze. a b

Fluorometholone and sulfacetamide sodium suspension: Light-protected container at 15–30°C.d Do not freeze.d Do not use suspension if dark brown. d

Fluorometholone acetate and tobramycin suspension: Upright at 2–25°C.f

Compatibility

Ophthalmic

Suspension

Fluorometholone and sulfacetamide sodium suspension: Incompatible with preparations containing silver.d

Actions

  • Corticosteroids suppress the inflammatory response to mechanical, chemical, or immunologic agents.b c d e f g h

  • Corticosteroids inhibit edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.c d e g h

Advice to Patients

  • Importance of discontinuing therapy and consulting a clinician if inflammation or pain persists for >48 hours or worsens.c d e h

  • Importance of removing soft contact lenses prior to administering preparations containing benzalkonium chlorideb e and of delaying reinsertion of the lenses for ≥15 minutes after administration.e

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the tip of the container.b c d e f h

  • Importance of warning the patient not to share the drug.c d e h

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

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.c d e f h

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.c d e f h

  • Importance of informing patients of other important precautionary information.b c d e f g h (See Cautions.)

Preparations

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

Fluorometholone

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Ointment

0.1%

FML (with phenylmercuric acetate)

Allergan

Suspension

0.1%

Fluor-Op (with benzalkonium chloride)

Novartis

Fluorometholone Ophthalmic Suspension

Bausch & Lomb, Falcon

FML (with benzalkonium chloride)

Allergan

0.25%

FML Forte (with benzalkonium chloride)

Allergan

Fluorometholone Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Suspension

0.1% with Sulfacetamide Sodium 10%

FML-S Liquifilm (with benzalkonium chloride and povidone)

Allergan

Fluorometholone Acetate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Suspension

0.1%

Flarex (with benzalkonium chloride)

Alcon

Fluorometholone Acetate Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Suspension

0.1% with Tobramycin 0.3%

Tobraflex (with benzalkonium chloride)

Alcon

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions September 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

a. AHFS drug information 2007. McEvoy GK, ed. Fluorometholone. Bethesda, MD: American Society of Health-Systems Pharmacists; 2007: 2825.

b. Alcon Laboratories, Inc. Flarex (fluorometholone acetate) suspension prescribing information. Fort Worth , TX; 1999 Jun.

c. Allergan, Inc. FML (fluorometholone) ointment prescribing information. Irvine, CA; 2001 Nov.

d. Allergan, Inc. FML-S (fluorometholone and sulfacetamide sodium) suspension prescribing information. Irvine, CA; 2005 Feb.

e. Allergan, Inc. FML (fluorometholone) ophthalmic suspension, 0.1% prescribing information. Irvine, CA; 2003 Jun.

f. Alcon Pharmaceuticals. Tobraflex (tobramycin and fluorometholone acetate) suspension prescribing information. Fort Worth, TX; 2001 May.

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

h. Allergan, Inc. FMLForte(fluorometholone) suspension prescribing information. Irvine, CA; 2004 Jun.

Hide
(web2)