Fluorometholone (EENT)

AHFS Class: Corticosteroids (52:08.08)

VA Class: OP300
ATC Class: S01CA07
Chemical Name: 9-fluoro-11ß,17-dihydroxy-6α-methylpregna-1,4-diene-3,20-dione
Molecular Formula: C₂₄H₃₁FO₅

View the associated AHFS monograph.

Brands: Flarex^® , Fluor-Op^® , FML^® , FML-S^® , Tobraflex ^®; also available generically.

Introduction

A synthetic fluorinated corticosteroid; structurally related to progesterone.^a

Uses

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}

Treatment of chronic anterior uveitis^{d 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.)

Dosage and Administration

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}

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}

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

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

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}

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}

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}

Pharmacokinetics

Absorption

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

Stability

Storage

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

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 chloride^{b 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

Fluorometholone

Routes	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	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	Forms	Strengths	Brand Names	Manufacturer
Ophthalmic	Suspension	0.1%	Flarex® (with benzalkonium chloride)	Alcon

Fluorometholone Acetate Combinations

Routes	Forms	Strengths	Brand Names	Manufacturer
Ophthalmic	Suspension	0.1% with Tobramycin 0.3%	Tobraflex® (with benzalkonium chloride)	Alcon

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit www.drugstore.com.

Flarex 0.1% Suspension (ALCON VISION): 5/$40.99 or 15/$109.13

Fluor-Op 0.1% Suspension (NOVARTIS OPTHALMICS): 10/$25.99 or 30/$71.97

Fluor-Op 0.1% Suspension (NOVARTIS OPTHALMICS): 15/$30.99 or 45/$86.97

FML Forte 0.25% Suspension (ALLERGAN): 5/$25.99 or 15/$69.97

FML Forte 0.25% Suspension (ALLERGAN): 10/$41.99 or 30/$117.97

FML Forte 0.25% Suspension (ALLERGAN): 15/$56.99 or 45/$162.97

FML Liquifilm 0.1% Suspension (ALLERGAN): 5/$35.99 or 15/$85.97

FML Liquifilm 0.1% Suspension (ALLERGAN): 15/$70.99 or 45/$203.96

FML Liquifilm 0.1% Suspension (ALLERGAN): 10/$51.99 or 30/$147.97

FML S.O.P. 0.1% Ointment (ALLERGAN): 3/$39.99 or 10/$105.98

FML-S Liquifilm 0.1-10% Suspension (ALLERGAN): 10/$35.99 or 30/$102.98

© Copyright, September 2007, American Society of Health-System Pharmacists, Inc. 7272 Wisconsin Avenue, Bethesda, MD 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.