Difluprednate

Difluprednate is an Anti-inflammatory belonging to the Corticosteroid class.

Difluprednate is a topical corticosteroid used for the symptomatic treatment of inflammation and pain associated with ocular surgery.

Difluprednate penetrates the corneal epithelium rapidly and effectively. Low systemic absorption. Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the drug’s active metabolite. Endogenous tissue esterases then metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), which limits systemic exposure to the active compound.

Difluprednate shows side effects like Blurred vision, decrease in vision, and seeing glare from lights or sun.

Difluprednate is available in the form of Ophthalmic emulsion.

Difluprednate is available in India, US, Canada, Mexico, UK, China, Brazil, Germany, Japan, Australia, and Malaysia.

Difluprednate is a Corticosteroid belonging to the class Anti-inflammatory.

Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

Difluprednate is available in the form of Ophthalmic emulsion.

Difluprednate is for ophthalmic use only. Wash hands before use and avoid contact with bottle tip with skin or eye.

Difluprednate is an Ophthalmic corticosteroid used for the treatment of inflammation and pain associated with eye surgeries. It is also used for the treatment of inflammation of the middle layer of the eye, uvea (uveitis).

Difluprednate is an Anti-inflammatory belonging to the Corticosteroid class.

Difluprednate corticosteroids inhibit the inflammatory response including edema, capillary dilation, leukocyte migration, and scar formation. Difluprednate penetrates cells readily to induce the production of lipocortins. These proteins modulate the activity of prostaglandins and leukotrienes.

Difluprednate is approved for use in the following clinical indications

• Endogenous anterior uveitis
• Inflammation/pain associated with ocular surgery

• Endogenous anterior uveitis

Ophthalmic: Instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily for 14 days, then taper as clinically indicated.

• Inflammation/pain associated with ocular surgery

Ophthalmic: Instill 1 drop in the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery, continue for 2 weeks, then decrease to 2 times daily for 1 week, then taper based on response.

Difluprednate is available in various strengths at 0.05%.

Difluprednate is available in the form of Ophthalmic emulsion.

1. Dosage Adjustment in Kidney Patient

There are no dosage adjustments provided.

2. Dosage Adjustment in Hepatic Impairment Patient

There are no dosage adjustments provided.

Difluprednate is contraindicated in patients with

• other ophthalmic corticosteroids are contraindicated in most active viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and in mycobacterial infection of the eye and fungal disease of ocular structures.

• IOP Increase

Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity, and fields of vision. Steroids should be used with caution in the presence of glaucoma. If this product is used for 10 days or longer, intraocular pressure should be monitored.

• Cataracts

The use of corticosteroids may result in posterior subcapsular cataract formation.

• Delayed healing

The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. The initial prescription and renewal of the medication order beyond 28 days should be made by a physician only after examination of the patient with the aid of magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.

• Bacterial infections

Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infections. In acute purulent conditions, steroids may mask infection or enhance existing infection. If signs and symptoms fail to improve after 2 days, the patient should be re-evaluated.

• Viral infections

Employment of corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution. The use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex).

• Fungal infections

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. Fungal culture should be taken when appropriate.

• Topical ophthalmic

Difluprednateis not indicated for intraocular administration.

It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Caution should be exercised when Difluprednate is administered to a nursing woman.

Pregnancy category C

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant the use of the drug in pregnant women despite potential risks.

Common

· Reduced visual acuity, posterior subcapsular cataract formation, increased intraocular pressure, corneal perforation, delayed healing, immunosuppression (e.g. increased risk for bacterial, viral and fungal infection), exacerbation of infections, Cortico-induced and paradoxically cortico-sensitive dermatitis, and cushingoid syndrome (prolonged use), slowing of growth in children, Ciliary, conjunctival and limbal hyperemia; eye pain, photophobia, posterior capsule opacification, anterior chamber cells, anterior chamber flare, corneal and conjunctival edema, blepharitis, punctate keratitis, eye inflammation, iritis, blurred vision, eye irritation, uveitis, dry eye, iridocyclitis, Headache, Skin atrophy, stretch marks, secondary ecchymotic purpura, cutaneous fragility, acneiform or pustular eruptions, hypertrichosis, depigmentation, allergic contact dermatoses, Telangiectasia.

Common

· Reduced visual acuity, posterior subcapsular cataract formation, increased intraocular pressure, corneal perforation, delayed healing, immunosuppression (e.g. increased risk for bacterial, viral and fungal infection), exacerbation of infections, Cortico-induced and paradoxically cortico-sensitive dermatitis, and cushingoid syndrome (prolonged use), slowing of growth in children, Ciliary, conjunctival and limbal hyperemia; eye pain, photophobia, posterior capsule opacification, anterior chamber cells, anterior chamber flare, corneal and conjunctival edema, blepharitis, punctate keratitis, eye inflammation, iritis, blurred vision, eye irritation, uveitis, dry eye, iridocyclitis, Headache, Skin atrophy, stretch marks, secondary ecchymotic purpura, cutaneous fragility, acneiform or pustular eruptions, hypertrichosis, depigmentation, allergic contact dermatoses, Telangiectasia.

The common side effects of Difluprednate include the following

Common side effects

· Blurred vision, decrease in vision, seeing glare from lights or sun.

• Pregnancy

Pregnancy Category C

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but having potential benefits may warrant the use of the drug in pregnant women despite potential risks.

• Nursing Mothers

It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Caution should be exercised when Difluprednate is administered to a nursing woman.

• Pediatric Use

In pediatric patients, safety and effectiveness have not been established.

• Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

• Pharmacodynamic

Difluprednate is a corticosteroid used as an anti-inflammatory steroidal drug used primarily in ocular surgery.

• Pharmacokinetics

Absorption

Difluprednate penetrates the corneal epithelium rapidly and effectively. Low systemic absorption.

Metabolism and Excretion

Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the drug’s active metabolite. Endogenous tissue esterases then metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), which limits systemic exposure to the active compound.

1. Korenfeld MS, Silverstein SM, Cooke DL, Vogel R, Crockett RS. Difluprednate ophthalmic emulsion 0.05% for postoperative inflammation and pain. Journal of Cataract & Refractive Surgery. 2009 Jan 1;35(1):26-34.
2. Mochizuki M, Ohno S, Usui M, Masuda K, Sekiya T, Ogawa T, DFBA Study Group. A phase III, open-label, clinical study of difluprednate ophthalmic emulsion (DFBA), 0.05% in the treatment of severe refractory anterior uveitis. Investigative Ophthalmology & Visual Science. 2007 May 10;48(13):3905-.
3. Birnbaum AD, Jiang Y, Tessler HH, Goldstein DA. Elevation of intraocular pressure in patients with uveitis treated with topical difluprednate. Archives of ophthalmology. 2011 May 9;129(5):664-76.

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022212lbl.pdf
• https://www.uptodate.com/contents/difluprednate-drug-information?search=difluprednate&selectedTitle=1~3&usage_type=panel&display_rank=1&kp_tab=drug_general&source=panel_search_result
• https://www.drugs.com/cdi/difluprednate.html
• https://medlineplus.gov/druginfo/meds/a609025.html#:~:text=Difluprednate ophthalmic is used to,that cause swelling and pain.
• https://go.drugbank.com/drugs/DB06781