Durezol Information
Durezol () Indications And Usage
Durezol () (difluprednate ophthalmic emulsion) 0.05%, a topical corticosteroid, is indicated for the treatment of inflammation and pain associated with ocular surgery.
Durezol () Dosage And Administration
Instill one drop into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period, followed by 2 times daily for a week and then a taper based on the response.
Durezol () Dosage Strengths
Durezol () contains 0.05% difluprednate as a sterile preserved emulsion for topical ophthalmic administration.
Durezol () Contraindications
The use of Durezol () , as with other ophthalmic corticosteroids, is contraindicated in most active viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal disease of ocular structures.
Durezol () Adverse Reactions
Adverse reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.
Ocular adverse reactions occurring in 5-15% of subjects in clinical studies with Durezol () included corneal edema, ciliary and conjunctival hyperemia, eye pain, photophobia, posterior capsule opacification, anterior chamber cells, anterior chamber _are, conjunctival edema, and blepharitis. Other ocular adverse reactions occurring in 1-5% of subjects included reduced visual acuity, punctate keratitis, eye inflammation, and iritis. Ocular adverse events occurring in
Durezol () Use In Specific Populations
Teratogenic Effects
Pregnancy Category C. Difluprednate has been shown to be embryotoxic (decrease in embryonic body weight and a delay in embryonic ossification) and teratogenic (cleft palate and skeletal) anomalies when administered subcutaneously to rabbits during organogenesis at a dose of 1-10 μg/kg/day. The no-observed-effect-level (NOEL) for these effects was 1 μg/kg/day, and 10 μg/kg/day was considered to be a teratogenic dose that was concurrently found in the toxic dose range for fetuses and pregnant females. Treatment of rats with 10 μg/kg/day subcutaneously during organogenesis did not result in any reproductive toxicity, nor was it maternally toxic. At 100 μg/kg/day after subcutaneous administration in rats, there was a decrease in fetal weights and delay in ossification, and effects on weight gain in the pregnant females. It is difficult to extrapolate these doses of difluprednate to maximum daily human doses of Durezol () , since Durezol () is administered topically with minimal systemic absorption, and difluprednate blood levels were not measured in the reproductive animal studies. However, since use of difluprednate during human pregnancy has not been evaluated and cannot rule out the possibility of harm, Durezol () should be used during pregnancy only if the potential benefit justifies the potential risk to the embryo or fetus.
Durezol () Description
Durezol () (difluprednate ophthalmic emulsion) 0.05% is a sterile, topical anti-inflammatory corticosteroid for ophthalmic use. The chemical name is 6α,9difluoro-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate 17-butyrate (CAS number 23674-86-4). Difluprednate is represented by the following structural formula:
Difluprednate has a molecular weight of 508.56, and the empirical formula is CHFO.
Each mL contains: ACTIVE: difluprednate 0.5 mg (0.05%); INACTIVE: boric acid, castor oil, glycerin, polysorbate 80, water for injection, sodium acetate, sodium EDTA, sodium hydroxide (to adjust the pH to 5.2 to 5.8). The emulsion is essentially isotonic with a tonicity of 304 to 411 mOsm/kg. PRESERVATIVE: sorbic acid 0.1%.
Durezol () Clinical Pharmacology
Corticosteroids inhibit the inflammatory response to a variety of inciting agents that may delay or slow healing. They inhibit edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of in_ammation such as prostaglandins and leukotreines by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A.
Difluprednate is structurally similar to other corticosteroids.
Difluprednate undergoes deacetylation in vivo to 6α, 9-difluoroprednisolone 17-butyrate (DFB), an active metabolite of difluprednate.
Clinical pharmacokinetic studies of difluprednate after repeat ocular instillation of 2 drops of difluprednate (0.01% or 0.05%) QID for 7 days showed that DFB levels in blood were below the quantification limit (50 ng/mL) at all time points for all subjects, indicating the systemic absorption of difluprednate after ocular instillation of Durezol () is limited.
Durezol () How Supplied/storage And Handling
Durezol () (difluprednate ophthalmic emulsion) 0.05% is a sterile, aqueous topical ophthalmic emulsion supplied in an opaque plastic bottle with a controlled drop tip and a pink cap in the following size: 5 mL in a 5 mL bottle (NDC 0065-9240-05).
Store at 15-25°C (59-77°F). Do not freeze. Protect from light. When not in use keep the bottles in the protective carton.
Durezol () Patient Counseling Information
This product is sterile when packaged. Patients should be advised not to allow the dropper tip to touch any surface, as this may contaminate the emulsion. If pain develops or if redness, itching, or inflammation becomes aggravated, the patient should be advised to consult a physician. As with all ophthalmic preparations containing a preservative, patients should be advised not to wear contact lenses when using Durezol () .
U.S. Patent: 6,114,319
©2010 Alcon , Inc.
Manufactured for:
Alcon Laboratories, Inc.
6201 South Freeway
Fort Worth, Texas 76134 USA
1-800-757-9195
[email protected]
Manufactured By:
Catalent Pharma Solutions
Woodstock, IL 60098
