Introduction
Xipere (triamcinolone acetonide injectable suspension) is a corticosteroid formulation specifically developed for suprachoroidal administration. Approved by the FDA in October 2021, it represents a novel approach to treating ocular inflammatory conditions by delivering medication directly to the back of the eye while minimizing exposure to anterior segment structures.
Mechanism of Action
Xipere contains triamcinolone acetonide, a synthetic corticosteroid with potent anti-inflammatory effects. The drug exerts its therapeutic action by diffusing across cell membranes and forming complexes with cytoplasmic receptor proteins. These complexes then migrate to the cell nucleus, bind to DNA, and stimulate transcription of messenger RNA. This process leads to synthesis of various enzymes that ultimately suppress the inflammatory response by inhibiting edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scar formation.
The suprachoroidal administration route allows for targeted delivery to the posterior segment, achieving therapeutic concentrations in the choroid, retina, and retinal pigment epithelium while minimizing anterior segment exposure.
Indications
Xipere is indicated for the treatment of macular edema associated with uveitis. This includes:
- Non-infectious uveitis affecting the posterior segment
- Intermediate uveitis
- Panuveitis
- Uveitic macular edema that has been unresponsive to other treatments
Dosage and Administration
Recommended dosage: 4 mg (0.1 mL) administered as a single suprachoroidal injection into the affected eye(s) Administration:- For bilateral disease, each eye may be treated separately with at least 30 minutes between injections
- Administration must be performed by a qualified ophthalmologist trained in suprachoroidal injection technique
- Use proper aseptic technique throughout the procedure
- The injection should be administered using the specifically designed microinjector system
- Renal impairment: No dosage adjustment required
- Hepatic impairment: No specific recommendations available
- Elderly: No dosage adjustment required
- Pediatric patients: Safety and effectiveness not established
Pharmacokinetics
Absorption: Following suprachoroidal administration, triamcinolone acetonide is primarily localized to ocular tissues with limited systemic exposure. Distribution: The drug distributes primarily to posterior segment tissues with minimal anterior segment exposure. Plasma concentrations are typically below quantifiable limits (<50 pg/mL) following suprachoroidal administration. Metabolism: Primarily hepatic through conjugation and reduction to inactive metabolites. Elimination: Eliminated primarily via urine with a terminal half-life of approximately 2-5 hours in plasma. However, the ocular residence time is significantly longer due to the suspension formulation.Contraindications
- Ocular or periocular infections
- Active ocular herpes simplex, fungal, or mycobacterial infections
- Known hypersensitivity to triamcinolone acetonide or any component of the formulation
- Glaucoma that is uncontrolled despite maximal medical therapy
Warnings and Precautions
Intraocular pressure increase: Corticosteroids including Xipere may increase intraocular pressure (IOP) in susceptible individuals. Monitor IOP regularly. Cataract formation: Prolonged use of corticosteroids may result in posterior subcapsular cataract formation. Endophthalmitis: Intravitreal injections including suprachoroidal administration may be associated with endophthalmitis. Proper aseptic technique is essential. Retinal detachment: May occur following intraocular procedures. Choroidal detachment: Has been reported following suprachoroidal injection. Infection: Corticosteroids may mask signs of infection and enhance existing infection. Perforation: Globe perforation may occur with intraocular injections.Drug Interactions
Systemic interactions: Limited systemic exposure minimizes significant drug interactions, but theoretical interactions include:- Other corticosteroids (additive effects)
- CYP3A4 inhibitors/inducers (may affect metabolism)
- Vaccines (corticosteroids may diminish immune response)
Adverse Effects
Most common adverse reactions (≥2%):- Increased intraocular pressure (15%)
- Cataract (8%)
- Conjunctival hemorrhage (7%)
- Eye pain (6%)
- Vitreous floaters (3%)
- Conjunctival hyperemia (2%)
- Endophthalmitis
- Retinal detachment
- Choroidal detachment
- Ocular hypertension requiring treatment
- Perforation
Monitoring Parameters
- Intraocular pressure at baseline and follow-up visits (typically 1 week, 1 month, and quarterly post-injection)
- Visual acuity at each visit
- Slit-lamp examination for anterior segment changes
- Dilated fundus examination for posterior segment changes
- Assessment for signs of infection
- Cataract progression monitoring
- Assessment of macular edema resolution via OCT
Patient Education
- Report any eye pain, unusual sensitivity to light, vision changes, or signs of infection immediately
- Understand that multiple injections may be necessary for optimal effect
- Be aware of the risk of increased eye pressure and need for regular monitoring
- Understand that cataract development may occur with repeated treatments
- Do not rub or press on the treated eye
- Use prescribed eye drops as directed if applicable
- Attend all follow-up appointments as scheduled
- Report any systemic side effects to their healthcare provider
References
1. FDA prescribing information: Xipere (triamcinolone acetonide injectable suspension) 2. Campochiaro PA, et al. Suprachoroidal triamcinolone acetonide for retinal vein occlusion: Results of the Tanzanite study. Ophthalmol Retina. 2018;2(4):320-328. 3. Goldstein DA, et al. Suprachoroidal corticosteroid administration: A novel route for local treatment of the posterior segment. Expert Opin Drug Deliv. 2016;13(1):103-109. 4. Khanani AM, et al. Suprachoroidal injection of triamcinolone acetonide for diabetic macular edema: The Hulk study. Retina. 2018;38 Suppl 1:S79-S88. 5. ClinicalTrials.gov: PEACHTREE study (NCT02595398)