Durezol

Ophthalmological Corticosteroids

 
NOTE: Care should be taken not to discontinue therapy prematurely. If ocular signs and symptoms fail to improve after 2 days, the patient should be re-evaluated. Intraocular pressure should be monitored after 10 days of therapy, and an ophthalmologic exam should occur after 14 days of therapy.

Difluprednate is administered topically to the eye. Shake well before use.
Do not to touch the tip of the dropper to the eye, fingertips, or other surface.
Instruct patient on proper instillation of eye solution.
When using difluprednate, the patient should not wear contact lenses.

uveitis / Delayed / 0-10.0
ocular hypertension / Delayed / 1.0-10.0
keratitis / Delayed / 1.0-10.0
visual impairment / Early / 1.0-5.0
macular edema / Delayed / 0-1.0

conjunctival hyperemia / Early / 5.0-15.0
blepharitis / Early / 5.0-15.0
hyperemia / Delayed / 0-15.0
corneal edema / Early / 2.0-15.0
photophobia / Early / 2.0-15.0
blurred vision / Early / 5.0-10.0
iritis / Delayed / 1.0-10.0
ocular inflammation / Early / 1.0-5.0
cataracts / Delayed / Incidence not known
impaired wound healing / Delayed / Incidence not known
superinfection / Delayed / Incidence not known
ocular infection / Delayed / Incidence not known

ocular pain / Early / 5.0-15.0
ocular irritation / Rapid / 0-10.0
xerophthalmia / Early / 2.0-5.0
lacrimation / Early / 0-1.0
foreign body sensation / Rapid / 0-1.0
striae / Delayed / 0-1.0
ocular pruritus / Rapid / 0-1.0

Durezol

Rx

Ophthalmic corticosteroid
Used for postoperative ocular pain and inflammation and endogenous anterior uveitis
Safety and efficacy comparable to betamethasone 0.1% ophthalmic solution

Instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery; continue giving 4 times/day for the first 2 weeks of the postoperative period, then administer 2 times daily for 1 week. At the end of the third week, taper dose based on response.

Instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery; continue giving 4 times/day for the first 2 weeks of the postoperative period, then administer 2 times daily for 1 week. At the end of the third week, taper dose based on response. In a double-blind trial in pediatric patients (aged 0 to 3 years) who underwent cataract surgery, a similar safety profile was observed in patients who received difluprednate 0.05% (n = 39) compared to those who received prednisolone acetate ophthalmic suspension 1% (n = 40).

Instill 1 drop into the conjunctival sac of the affected eye(s) 4 times daily for 14 days followed by tapering as clinically indicated.

No dosage guidelines are available; it appears no dosage adjustment is needed.

No dosage guidelines are available; it appears no dosage adjustment is needed.

There are no drug interactions associated with Difluprednate products.

Difluprednate/Durezol Ophthalmic Emulsion: 0.05%

4 drops/day in each affected eye.

4 drops/day in each affected eye.

4 drops/day in each affected eye.

4 drops/day in each affected eye.

4 drops/day in each affected eye.

Safety and efficacy have not been established.

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the exact mechanism of action for ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. Lipocortins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of the precursor molecule arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
 
Corticosteroids can increase intraocular pressure. The mechanism by which ophthalmic corticosteroids increase intraocular pressure is not clear. Corticosteroids are associated with the presence of extracellular glycosaminoglycans in ocular trabecular cells, which have been hypothesized to increase the resistance of aqueous outflow.

Difluprednate is administered topically to the eye. Difluprednate undergoes deacetylation in vivo to the active metabolite 6 alpha, 9-difluoroprednisolone 17-butyrate (DFB).

Limited systemic absorption of difluprednate occurs following daily administration. In clinical pharmacokinetic studies, DFB levels in blood were below the quantification limit (50 ng/mL) at all time points for all subjects after repeat ocular instillation of 2 drops of difluprednate (0.01% or 0.05%) four times daily for 7 days.

Difluprednate is classified as pregnancy category C. Animal studies using subcutaneous doses produced teratogenic and embryotoxic effects. Other corticosteroids have been shown to cause fetal resorptions and malformations. The systemic absorption of difluprednate following ophthalmic administration is minimal; however, according to the manufacturer, because there have been no adequate studies conducted into the safe use of difluprednate in pregnant women, it should only be used when the potential benefits to the mother outweigh possible risks to the fetus.

Difluprednate has not been studied during breast feeding. While the American Academy of Pediatrics does not comment on the use of ophthalmic difluprednate during breast-feeding, it does consider some systemic corticosteroids (prednisone and prednisolone) to be usually compatible with breast-feeding. It is not known whether ophthalmic difluprednate results in sufficient systemic absorption to produce detectable quantities in breast milk; but pharmacokinetic studies indicate that systemic absorption after ophthalmic administration of difluprednate is limited and therefore unlikely that a significant amount of drug would be excreted into breast-milk. To further minimize the amount of drug that reaches the systemic circulation and breast milk, apply pressure over the tear duct by the corner of the eye for 1 minute after ophthalmic administration. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.