FLUOROMETHOLONE
DESCRIPTION:
FML (fluorometholone acetate) is a corticosteroid prepared as a sterile
topical ophthalmic suspension. The active ingredient, fluorometholone acetate,
is a white to creamy white powder with an empirical formula of C24H31FO5 and a
molecular weight of 418.5. Its chemical name is 9-fluoro-11beta, 17-dihydrozy-
6alpha -methylpregna-1, 4-diene-3, 20-dione 17-acetate.
EACH ML CONTAINS: ACTIVE: fluorometholone acetate 1 mg (0.1%). PRESERVATIVE:
benzalkonium chloride 0.01%. INACTIVE: sodium chloride, monobasic sodium
phosphate, edetate disodium, hydroxyethyl cellulose, tyloxapol, hydrochloric
acid and/or sodium hydroxide (to adjust pH), and purified water.
ACTIONS/CLINICAL PHARMACOLOGY:
Corticosteroids suppress the inflammatory response to inciting agents of
mechanical, chemical or immunological nature. No generally accepted explanation
of this steroid property has been advanced. Clinical studies demonstrate that
Fluorometholone Acetate is significantly more efficacious than Fluorometholone
for the treatment of external ocular inflammation. (REF. 1) Corticosteroids
cause a rise in intraocular pressure in susceptible individuals. In a small
study, FML Ophthalmic Suspension demonstrated a significantly longer average
time to produce a rise in intraocular pressure than did dexamethasone phosphate;
however, the ultimate magnitude of the rise was equivalent for both drugs and in
a small percentage of individuals a significant rise in intraocular pressure
occurred within three days. (REF. 2)
INDICATIONS AND USAGE:
FML Ophthalmic Suspension is indicated for use in the treatment of steroid
responsive inflammatory conditions of the palpebral and bulbar conjunctiva,
cornea, and anterior segment of the eye.
CONTRAINDICATIONS:
Contraindicated in acute superficial herpes simplex keratitis, vaccinia,
varicella, and most other viral diseases of cornea and conjunctiva;
tuberculosis; fungal diseases; acute purulent untreated infections which, like
other diseases caused by microorganisms, may be masked or enhanced by the
presence of the steroid; and in those persons who have known hypersensitivity to
any component of this preparation.
WARNINGS:
Not for injection. Use in the treatment of herpes simplex infection requires
great caution. Prolonged use may result in glaucoma, damage to the optic nerve,
defect in visual acuity and visual field, cataract formation and/or may aid in
the establishment of secondary ocular infections from pathogens due to
suppression of host response. Acute purulent infections of the eye may be masked
or exacerbated by presence of steroid medication. In those diseases causing
thinning of the cornea or sclera, perforation has been known to occur with
chronic use of topical steroids. It is advisable that the intraocular pressure
be checked frequently.
PRECAUTIONS:
GENERAL: Fungal infections of the cornea are particularly prone to develop
coincidentally with long-term local steroid application. Fungus invasion must be
considered in any persistent corneal ulceration where a steroid has been used or
is in use.
INFORMATION FOR PATIENTS: Do not touch dropper tip to any surface, as this may
contaminate the suspension.
CARCINOGENESIS, MUTAGENESIS, IMPAIRMENT OF FERTILITY: No studies have been
conducted in animals or in humans to evaluate the possibility of these effects
with fluorometholone.
PREGNANCY: Pregnancy Category C. Fluorometholone has been shown to be
embryocidal and teratogenic in rabbits when administered at low multiples of the
human ocular dose. Fluorometholone was applied ocularly to rabbits daily on days
6-18 of gestation, and dose-related fetal loss and fetal abnormalities including
cleft palate, deformed rib cage, anomalous limbs and neural abnormalities such
as encephalocele, craniorachischisis, and spina bifida were observed. There are
no adequate and well controlled studies of fluorometholone in pregnant women,
and it is not known whether fluorometholone can cause fetal harm when
administered to a pregnant woman. Fluorometholone should be used during
pregnancy only if the potential benefit justifies the potential risk to the
fetus.
NURSING MOTHERS: It is not known whether topical administration of
corticosteroids could result in sufficient systemic absorption to produce
detectable quantities in human milk. Systemically-administered corticosteroids
appear in human milk and could suppress growth, interfere with endogenous
corticosteroid production, or cause other untoward effects. Because of the
potential for serious adverse reactions in nursing infants from fluorometholone,
a decision should be made whether to discontinue nursing or to discontinue the
drug.
PEDIATRIC USE: Safety and effectiveness in pediatric patients have not been
established.
ADVERSE REACTIONS:
Glaucoma with optic nerve damage, visual acuity and field defects, cataract
formation, secondary ocular infection following suppression of host response,
and perforation of the globe may occur.
DOSAGE AND ADMINISTRATION:
SHAKE WELL BEFORE USING. One to two drops instilled into the conjunctival sac(s)
four times daily. During the initial 24 to 48 hours the dosage may be safely
increased to two drops every two hours. If no improvement after two weeks,
consult physician. Care should be taken not to discontinue therapy prematurely.
REFERENCES:
1. Leibowitz, H. M., et. al., Annals of Ophthalmology 1984; 16:1110.
2. Stewart, R. H., et. al., Current Eye Research 1984; 3:835.
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