DUREZOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DUREZOL (DUREZOL).
Corticosteroid receptor agonist; reduces inflammation by inhibiting phospholipase A2, decreasing prostaglandin and leukotriene synthesis, and suppressing immune cell migration and cytokine release.
| Metabolism | Primarily hepatic via CYP3A4; undergoes reduction and conjugation. |
| Excretion | Renal excretion of unchanged drug accounts for 30% of clearance; biliary/fecal elimination accounts for 60%, with the remainder as metabolites. |
| Half-life | Terminal elimination half-life is 12–18 hours in adults; prolonged to 24–36 hours in hepatic impairment. |
| Protein binding | ≥99% bound to albumin. |
| Volume of Distribution | 0.12–0.18 L/kg; indicates distribution primarily in plasma and extracellular fluid. |
| Bioavailability | Oral: 45–55% due to first-pass metabolism. |
| Onset of Action | Oral: 30–60 minutes; intravenous: 5–15 minutes. |
| Duration of Action | 6–12 hours; extended in hepatic impairment due to reduced clearance. |
| Molecular Weight | 392.46 |
1 drop of 0.1% ophthalmic solution in the affected eye(s) four times daily for up to 14 days.
| Dosage form | EMULSION |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No dosage adjustment required for Child-Pugh Class A or B. Not recommended for Child-Pugh Class C due to lack of data. |
| Pediatric use | Safety and efficacy not established in pediatric patients younger than 18 years. |
| Geriatric use | No specific dose adjustment needed; use with caution due to higher risk of corneal adverse events in elderly. |
| 1st trimester | Avoid use; risk of teratogenicity based on animal studies and limited human data. |
| 2nd trimester | Use only if maternal benefit outweighs fetal risk; may cause fetal hypercorticoidism. |
| 3rd trimester | Avoid prolonged use; risk of neonatal adrenal suppression and hypoglycemia. |
Clinical note
Comprehensive clinical and safety monograph for DUREZOL (DUREZOL).
| Placental transfer | Intensive placental transfer; readily crosses the placenta due to low molecular weight and lipophilicity. |
| Breastfeeding | Corticosteroids are excreted in breast milk in low amounts, but high doses may affect infant growth or cause adrenal suppression. Monitor infant for signs of hypercorticism. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Systemic fungal infectionsKnown hypersensitivity to difluprednate or any excipient
| Precautions | Increased intraocular pressure (IOP); monitor IOP regularly., Cataract formation with prolonged use., Delayed wound healing., Secondary ocular infection; fungal and viral keratitis risk., Use with caution in patients with glaucoma or corneal thinning. |
| Food/Dietary | No significant food interactions. Avoid excessive alcohol consumption as it may increase the risk of gastrointestinal adverse effects if systemic absorption occurs. |
| Clinical Pearls |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | DUREZOL (difluprednate) is a corticosteroid. In first trimester, no adequate studies; animal studies show embryocidal and teratogenic effects at high doses. Second and third trimester: associated with increased risk of intrauterine growth restriction (IUGR), adrenal suppression, and cleft palate with systemic exposure. Topical use may reduce systemic absorption but risk remains. |
| Fetal Monitoring | Monitor maternal blood pressure, blood glucose, and symptoms of Cushing's syndrome with prolonged ocular use. Assess fetal growth via ultrasound if prolonged high-dose use. Monitor infant for adrenal suppression if maternal use near term. |
| Fertility Effects | No specific human data on fertility effects. In animal studies, high doses of corticosteroids may impair male and female fertility. Local ocular use unlikely to exert significant systemic effects on fertility. |
| DUREZOL (difluprednate) is a potent corticosteroid ophthalmic emulsion for postoperative ocular inflammation. Administer one drop four times daily beginning 24 hours after surgery and continuing for 2 weeks. Shake vigorously before use. Monitor intraocular pressure closely, especially in patients with glaucoma. Do not taper; abrupt discontinuation is acceptable. Contraindicated in epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, varicella, and mycobacterial or fungal infections. Use with caution in patients with a history of herpes simplex. Prolonged use may lead to secondary ocular infections, corneal thinning, or perforation. |
| Patient Advice | Shake the bottle well before each use. · Remove contact lenses before instilling the drop and wait at least 15 minutes before reinserting. · Do not touch the dropper tip to any surface to avoid contamination. · Use exactly as prescribed; do not stop without consulting your doctor. · Report any eye pain, redness, vision changes, or discharge immediately. · Wash hands before and after administration. · If using other eye drops, wait at least 5 minutes between each medication. |