ILUVIEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ILUVIEN (ILUVIEN).
Fluocinolone acetonide, a corticosteroid, suppresses inflammation by inhibiting phospholipase A2, reducing arachidonic acid release and subsequent prostaglandin and leukotriene synthesis. It also inhibits cytokine production and endothelial cell adhesion molecule expression.
| Metabolism | Fluocinolone acetonide is metabolized primarily by cytochrome P450 3A4 (CYP3A4) to 6α-hydroxyfluocinolone acetonide and other metabolites. |
| Excretion | Fluocinolone acetonide is primarily eliminated via hepatic metabolism and subsequent fecal/biliary excretion. Approximately 50-70% of a dose is excreted in feces as metabolites, with less than 20% recovered in urine as unchanged drug or metabolites. |
| Half-life | Intravitreal terminal half-life of fluocinolone acetonide from the Iluvien implant is approximately 30 months (range 18-36 months), providing sustained release over 36 months in the vitreous cavity. |
| Protein binding | Fluocinolone acetonide is approximately 90% bound to plasma proteins, primarily albumin and corticosteroid-binding globulin (CBG). |
| Volume of Distribution | Volume of distribution (Vd) for fluocinolone acetonide after systemic administration is approximately 0.8 L/kg, indicating extensive tissue distribution. For intravitreal delivery, Vd is limited to the vitreous cavity (~4 mL), with negligible systemic distribution. |
| Bioavailability | Intravitreal: 100% (local delivery, no first-pass metabolism). Systemic: negligible (<0.1%) after intravitreal implantation due to the slow release and low dose. |
| Onset of Action | Onset of clinical effect (reduction in diabetic macular edema) is typically observed within 2-4 weeks after intravitreal implantation, with maximal effect seen by 3-6 months. |
| Duration of Action | Duration of action is up to 36 months (3 years) from a single intravitreal implant, with sustained release of fluocinolone acetonide. Clinical effect persists for the implant's lifespan; retreatment may be needed after 3 years. |
| Molecular Weight | 452.49 |
Intravitreal implant containing 0.19 mg fluocinolone acetonide, designed to release drug over approximately 36 months. Administered as a single injection into the vitreous cavity of the eye.
| Dosage form | IMPLANT |
| Renal impairment | No dose adjustment required based on renal function; systemic exposure is negligible. |
| Liver impairment | No dose adjustment required based on hepatic function; systemic exposure is negligible. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; use not recommended. |
| Geriatric use | No specific dose adjustment for elderly; clinical studies included patients aged 65 and older with no overall differences in safety or efficacy observed. |
| 1st trimester | Fluocinolone acetonide is a corticosteroid; systemic absorption may cause fetal harm. Use only if benefit outweighs risk. No adequate studies in pregnant women. |
| 2nd trimester | Same as T1; corticosteroids may cause fetal growth restriction or adrenal suppression. Risk should be weighed. |
| 3rd trimester | Same as T1; avoid use near term due to potential adrenal suppression in the neonate. |
Clinical note
Comprehensive clinical and safety monograph for ILUVIEN (ILUVIEN).
| Placental transfer | Corticosteroids cross the placenta; fluocinolone acetonide likely crosses to some degree, but systemic exposure after intraocular administration is very low. |
| Breastfeeding | No data on presence in human milk; systemic absorption is minimal, but caution advised. Single intraocular dose likely results in negligible systemic levels, but use only if clearly needed. |
■ FDA Black Box Warning
Not applicable.
| Serious Effects |
Hypersensitivity to fluocinolone acetonide or any componentActive or suspected ocular infectionAdvanced glaucoma with uncontrolled IOPAphakic eyes with anterior chamber IOLCompromised corneal endothelium
| Precautions | Elevated intraocular pressure (IOP): Monitor IOP regularly; may require management with topical medications or surgical intervention., Cataract formation: Posterior subcapsular cataracts are common post-implantation; may require cataract surgery., Endophthalmitis: Risk with implant procedure; monitor for signs of infection., Retinal detachment: Risk during implantation or with vitreous loss., Steroid-induced glaucoma: Can lead to permanent vision loss. |
| Food/Dietary | None known. No dietary restrictions are specifically required with ILUVIEN. |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal studies, intravitreal administration of fluocinolone acetonide at doses 0.5-2 times the recommended human dose resulted in teratogenicity (cleft palate, omphalocele) and embryotoxicity. Based on mechanism, corticosteroids are associated with increased risk of cleft lip/palate in first trimester. Risk cannot be ruled out; use only if potential benefit justifies risk. |
| Fetal Monitoring | Monitor intraocular pressure (IOP) and signs of infection. In pregnant patients, consider fetal ultrasound for cleft palate if exposed in first trimester. |
| Fertility Effects | No human data. In animal studies, no effects on male or female fertility at clinically relevant doses. |
| Clinical Pearls | ILUVIEN (fluocinolone acetonide intravitreal implant) is indicated for chronic non-infectious uveitis affecting the posterior segment. Monitor for increased intraocular pressure (IOP) and cataract formation; patients may require IOP-lowering therapy or cataract surgery. The implant releases corticosteroid for up to 36 months. Do not reuse or resterilize. Use aseptic technique during administration. Contraindicated in patients with active ocular infections or glaucoma with cupping. |
| Patient Advice | ILUVIEN is an implant placed in the eye to treat inflammation from uveitis. · Do not rub or press on the eye after the procedure; protect the eye with an eye shield as directed. · You may experience temporary blurred vision after the injection; avoid driving until vision clears. · Report any eye pain, redness, light sensitivity, or vision changes immediately. · Regular eye exams are needed to check eye pressure and for cataracts. · The implant may last up to 3 years; do not attempt to remove it. · Avoid swimming or hot tubs for 1 week after implantation. |