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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DUREZOL (DUREZOL).
| Breastfeeding | It is unknown if difluprednate is excreted in human breast milk. M/P ratio not established. Caution advised; potential for suppression of endogenous corticosteroid production in infant if significant exposure occurs. Recommend avoiding use during breastfeeding or using with frequent monitoring. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to difluprednate or any component.","Active viral (e.g., herpes simplex keratitis), fungal, or bacterial ocular infections.","Vaccinia or varicella infections."]
| 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."] |
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| 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. |