OZURDEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OZURDEX (OZURDEX).
Dexamethasone, a potent corticosteroid, reduces inflammation by inhibiting multiple inflammatory cytokines including prostaglandins, leukotrienes, and interleukins. It suppresses the migration of polymorphonuclear leukocytes and reverses increased capillary permeability. The mechanism involves binding to the glucocorticoid receptor, leading to regulation of gene expression that reduces production of inflammatory mediators.
| Metabolism | Dexamethasone is metabolized primarily in the liver via the cytochrome P450 enzyme CYP3A4. Metabolites are inactive and excreted in urine and feces. |
| Excretion | Primarily hepatic metabolism via CYP3A4; metabolites excreted in feces (≈70%) and urine (≈30%). Less than 1% excreted as unchanged drug. |
| Half-life | In the vitreous humor, the half-life is approximately 5-7 months following intravitreal implant administration. Systemic half-life is negligible due to low systemic exposure. |
| Protein binding | Approximately 68-89% bound to albumin, with less binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Systemic Vd is approximately 0.8 L/kg, indicating distribution mainly into plasma and extracellular fluid. For intravitreal administration, local Vd is limited to the vitreous chamber, estimated at 4-5 mL. |
| Bioavailability | Intravitreal implant: 100% local bioavailability. Systemic bioavailability is negligible (<0.1% of the administered dose) due to low systemic absorption from the vitreous. |
| Onset of Action | Intravitreal implant: Reduction in macular edema and improvement in visual acuity observed within 1-2 weeks; maximal effect by 2-3 months. |
| Duration of Action | Intravitreal implant: Single implant releases dexamethasone for up to 3-6 months; clinical effect may persist for 6 months or longer in some patients. Retreatment typically considered after 3-6 months based on disease recurrence. |
| Molecular Weight | 392.46 |
| Action Class | Intravitreal corticosteriod implants |
Single intravitreal implant of 0.7 mg (dexamethasone 700 mcg) in the affected eye; repeat dosing no sooner than 3 months after the prior implant.
| Dosage form | IMPLANT |
| Renal impairment | No dose adjustment required for renal impairment; data not available for GFR-based modifications. |
| Liver impairment | No dose adjustment required for hepatic impairment; not studied in Child-Pugh categories. |
| Pediatric use | Not recommended for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; caution for increased intraocular pressure and cataract formation, monitor closely. |
| 1st trimester | Dexamethasone is known to cross the placenta. Animal studies have shown teratogenic effects including cleft palate and growth retardation. Use only if potential benefit outweighs risk. |
| 2nd trimester | Dexamethasone may cause fetal adrenal suppression and intrauterine growth restriction. Monitor fetal growth. Use only if clearly needed. |
| 3rd trimester | Dexamethasone near term may suppress fetal adrenal function and cause neonatal hypoglycemia. Caution advised. |
Clinical note
Comprehensive clinical and safety monograph for OZURDEX (OZURDEX).
| Placental transfer | Dexamethasone crosses the placenta; approximately 50% of maternal serum concentration reaches fetal circulation. It is minimally metabolized by placental enzymes. |
| Breastfeeding | Dexamethasone is excreted into human milk in small amounts. At therapeutic doses, effects on the nursing infant are unlikely, but long-term, high-dose exposure may cause growth suppression or adrenal suppression. Consider risk-benefit. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to dexamethasone or any component of the formulationActive ocular or periocular infections (including viral, fungal, or mycobacterial)Corneal epithelial defect or compromised corneal integrityIatrogenic (post-surgical) glaucoma uncontrolled by medications
| Precautions | Intravitreal injection associated risks: endophthalmitis, ocular inflammation, increased intraocular pressure, retinal detachment, and vitreous hemorrhage, Elevated intraocular pressure (IOP): May occur with treatment; monitor IOP regularly and manage appropriately, Corticosteroid-induced cataracts: Long-term use may lead to posterior subcapsular cataract formation, Delayed healing: Corticosteroids may delay wound healing, Exacerbation of infections: Use with caution in patients with active ocular infections; may mask signs of infection, Systemic effects: Prolonged use or use in susceptible patients may lead to systemic corticosteroid effects (e.g., adrenal suppression), Use with caution in patients with glaucoma: Known steroid responders should be monitored closely, Not approved for use in children |
| Food/Dietary |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category C. In animal studies, intravitreal dexamethasone caused fetal harm (cleft palate, fetal death) at systemic exposures 1.5 times the human dose. No adequate human studies. Avoid use in pregnant women unless benefit outweighs risk. First trimester: potential teratogenic effects; second/third trimesters: risk of preterm birth, low birth weight, and adrenal suppression in neonate if used systemically; however, intravitreal administration minimizes systemic exposure. |
| Fetal Monitoring | Monitor intraocular pressure (IOP) regularly; ultrasound monitoring for fetal growth if prolonged systemic exposure occurs (unlikely with single implant). In pregnant women, consider fetal assessment if signs of systemic corticosteroid effects appear. |
| Fertility Effects | In animal studies, dexamethasone decreased fertility and implantation. Human data lacking. Potential reversible suppression of hypothalamic-pituitary-adrenal axis may affect menstrual cycle. |
| No clinically significant food interactions. Avoid excessive alcohol intake as it may exacerbate potential side effects like elevated intraocular pressure or interfere with corticosteroid metabolism. |
| Clinical Pearls | OZURDEX (dexamethasone intravitreal implant) is preferred for non-infectious uveitis and macular edema due to its sustained release over 3-6 months. Monitor intraocular pressure (IOP) closely; IOP elevation occurs in up to 40% of patients, often requiring topical glaucoma therapy. Cataract progression is common in phakic patients. Do not use in eyes with active ocular infections or advanced glaucoma. The implant may migrate into the anterior chamber in patients with aphakia or posterior capsule defects, causing corneal edema. Administer using strict aseptic technique; bilateral use in same session is not recommended. Retinal detachment or endophthalmitis are rare but serious risks. In diabetic macular edema (DME), OZURDEX may be considered second-line after anti-VEGF therapy; consider the risk of IOP elevation and cataract. The implant is radiopaque; patients may see it as a black spot in vision. |
| Patient Advice | This implant releases dexamethasone slowly over several months to reduce swelling and inflammation in your eye. · Your vision may remain blurry for a while after the injection; avoid driving until vision clears. · You may see small floaters or a black spot in your vision; this is the implant itself and is harmless. · Report any sudden vision loss, eye pain, redness, or light flashes immediately—these could be signs of infection or retinal detachment. · Do not rub or press on your eye; avoid swimming or hot tubs for at least 1 week after injection. · You will need regular follow-up visits to check eye pressure and for cataract development. · If you are diabetic, this treatment may raise your eye pressure; continue your diabetes management. · Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. · Do not receive vaccines without consulting your doctor while using this drug. · Use all eye drops as prescribed; do not change or stop them without talking to your doctor. |