Inflammation is the body's protective response to a stimulus it recognizes as offensive. While inflammation is protective for the body as a whole, the inflammatory processes can cause scarring and damage to the surrounding healthy tissue. Corticosteroids are used to preserve the normal structure of the tissues. They were developed in the 1940s, and till date remain the most potent agents for managing inflammation. Fluorometholone is one such steroid used for the management of inflammatory and allergic conditions of the eye.
Earlier fluorometholone was available as an alcohol derivative but now even the acetate derivative is available. The derivatives of steroid base (acetate, alcohol and phosphate) influence the bioavailability i.e. they determine the ability of steroid to penetrate the anterior chamber. Acetate and Alcohol derivatives are soluble in hydrophobic media whereas phosphate derivative is soluble in hydrophilic media. In the normal eye, an acetate derivative penetrates the best through the cornea, followed by alcohols, and then phosphates.
The derivatives of steroid base (acetate, alcohol and phosphate) also influence the bioactivity of that steroid so accordingly fluorometholone acetate shows superior anti-inflammatory activity in the cornea than fluorometholone alcohol.
Flosoft contains Fluorometholone acetate 0.1%. It is the World's first formulation with SOC (Stabilized Oxychlorocomplex) as the preservative. SOC is introduced as an ophthalmic preservative in 1996. Once it enters the eye, it breaks into water and salt i.e. sodium and potassium ions (NaCl), these components are already found in natural tears. Also it has no effect on mammalian cells. Hence it is more comfortable than other preservatives (Benzalkonium chloride).
Flosoft (fluorometholone acetate 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.
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.
Flosoft: Highlights
- World's first formulation of Fluorometholone acetate with SOC as a preservative
- Particle Size between 1-3 µ: Uniform Particle distribution and No agglomeration
- As effective as Prednisolone and Dexamethasone in reducing corneal inflammation
- Shows superior anti-inflammatory effect in the cornea as compared to Fluorometholone alcohol
- Fluorometholone acetate has low propensity to elevate IOP, therefore:
- Can be given to old age patients suffering from glaucoma
- Can be given to Steroid responders
- Can also be given in chronic therapy, requiring longer period of time
Composition
Fluorometholone acetate USP ....0.1 % w/v
Benzalkonium chloride IP..0.01% (As preservative)
Aqueous vehicle .... q. s.
Dosage Form
Ophthalmic suspension
Pharmacology
Pharmacodynamics
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. Corticosteroids cause a rise in intraocular pressure in susceptible individuals. In a small study, Fluorometholone acetate 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.
Indications
Fluorometholone acetate 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.
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 2 hours. If no improvement is seen after 2 weeks, consult a physician. Care should be taken not to discontinue therapy prematurely.
Contraindications
Contraindicated in acute superficial herpes simplex keratitis, vaccinia, varicella, and most other viral diseases of the 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 a known hypersensitivity to any component of this preparation.
Warnings and Precautions
General
FOR TOPICAL OPHTHALMIC USE ONLY. 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 the host response. Acute purulent infections of the eye may be masked or exacerbated by the 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.
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.
Pregnancy
Pregnancy Category C
There are no adequate and well-controlled studies of Fluorometholone in pregnant women, and it is not known whether Fluorometholone can cause foetal harm when administered to a pregnant woman. Fluorometholone should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.
Lactation
Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Because many drugs are excreted in human milk, caution should be exercised when FLOSOFT (fluorometholone acetate ophthalmic suspension), is administered to a nursing woman.
Paediatric Use
Safety and effectiveness in paediatric patients have not been established.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Undesirable Effects
Glaucoma with optic nerve damage, visual acuity and field defects, cataract formation, secondary ocular infection following suppression of the host response, and perforation of the globe may occur.
If you experience any side effects, talk to your doctor or pharmacist or write to drugsafety@cipla.com. You can also report side effects directly via the national pharmacovigilance program of India by calling on 1800 180 3024. By reporting side effects, you can help provide more information on the safety of this product
Shelf-Life
24 months
Storage and Handling Instructions
Store in a cool, dry place. Protect from light.
Packaging Information
FLOSOFT Eye drops: Vial of 5 ml
Information for Patients
Do not touch dropper tip to any surface, as this may contaminate the suspension. The preservative in FLOSOFT (fluorometholone acetate ophthalmic suspension), benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of FLOSOFT (fluorometholone acetate ophthalmic suspension) but may be reinserted 15 minutes after instillation. Patients should be advised that their vision may be temporarily blurred following dosing with FLOSOFT (fluorometholone acetate ophthalmic suspension). Care should be exercised in operating machinery or driving a motor vehicle
Last updated: April 2018
Last reviewed: April 2018