Eylea
Eylea
Generic Name
Eylea
Mechanism
Eylea binds and neutralizes the following ligands:
• VEGF‑A (all isoforms)
• VEGF‑B
• Placental growth factor (PlGF)
By sequestering these angiogenic mediators, the drug blocks activation of VEGF receptors on endothelial cells, inhibiting neovascularization, vascular leakage, and inflammation in the retina.
Pharmacokinetics
| Parameter | Details |
| Administration | Intravitreal injection (2 mg/0.05 mL) |
| Distribution | Primarily local to the vitreous; minimal systemic exposure |
| Absorption | Rapid intra‑vitreal distribution; peak concentration ≈1 day |
| Half‑life | Intravitreal elimination half‑life ~9 days (≈4 weeks) |
| Metabolism | Proteolytic degradation into peptides; negligible hepatic metabolism |
| Excretion | Via the retinal and choroidal circulation; systemic levels cleared by renal & hepatic pathways (minimal systemic exposure) |
| Drug–Drug Interactions | No clinically significant interactions; caution with systemic anti‑VEGF or anti‑platelet agents |
Indications
- Neovascular (wet) age‑related macular degeneration (AMD)
- Diabetic macular edema (DME)
- Macular edema secondary to central or branch retinal vein occlusion (CRVO/BRVO)
- Myopic choroidal neovascularization
- Other retinal diseases with VEGF‑mediated pathology (off‑label use)
Contraindications
- Active ocular infection (e.g., endophthalmitis)
- Severe ocular inflammation or uveitis
- Known hypersensitivity to aflibercept or any component
- Uncontrolled systemic hypertension (may exacerbate ocular hypertension)
- Recent thromboembolic event (caution in patients with recent stroke or MI)
Warnings:
• Endophthalmitis – rare but sight‑threatening; prompt recognition essential.
• Intra‑ocular pressure elevation – monitor and manage appropriately.
• Systemic cardiovascular events – rare; consider baseline cardiovascular assessment.
Dosing
- Initial loading phase: 2 mg intravitreal injection every 4 weeks for 3 consecutive doses.
- Maintenance phase: every 8 weeks (Q8W) based on disease activity.
- Alternative regimens:
- *Treat‑and‑Extend*: adjust interval by 2 weeks ± based on OCT and visual acuity.
- *Pro‑Re‑Nata (PRN)*: treat as needed after initial loading.
- Injection technique: sterile ocular prep, lid speculum, 30‑g needle, avoid reflux.
Reconstitution: Pre‑filled syringes (2 mg/0.05 mL) ready for use; no dilution required.
Adverse Effects
| Ocular | Systemic |
| *Common* | Intra‑ocular inflammation (hypopyon, anterior chamber cells) |
| Endophthalmitis (rare) | |
| Increased intra‑ocular pressure | |
| Vitreous hemorrhage | |
| Cataract progression | |
| Serious | Severe endophthalmitis |
| Acute rise in IOP leading to optic nerve damage | |
| Macular edema progression | |
| Systemic hypertension (rare) | |
| Thromboembolic events (MI, stroke) – very uncommon |
Monitoring
- Baseline: Best‑corrected visual acuity (BCVA), optical coherence tomography (OCT), intra‑ocular pressure (IOP), slit‑lamp exam.
- Follow‑up (every visit):
- BCVA and OCT to assess edema/CRT.
- IOP measurement; treat if ≥30 mmHg or >5 mmHg above baseline.
- Ophthalmic examination for signs of inflammation or infection.
- Long‑term: Document cumulative number of injections, visual outcomes, and any adverse events.
Clinical Pearls
- Pearl 1 – Early “Loading” Matters: The 3‑dose 4‑week loading schedule dramatically reduces the risk of breakthrough macular edema compared to starting on an 8‑week interval.
- Pearl 2 – Treat‑and‑Extend Yields Long‑Term Stability: Studies show that a treat‑and‑extend regimen maintains visual gains while reducing clinic visits and injections versus fixed Q8W.
- Pearl 3 – Monitor IOP Even in “Inert” Eyes: A small subset (~3–5 %) of patients develop significant IOP elevation; baseline glaucoma history warrants pre‑emptive IOP control.
- Pearl 4 – Systemic Safety Is Robust: Despite systemic VEGF inhibition, large‑scale trials report no excess cardiovascular events versus sham; still, consider cardiovascular history when initiating therapy.
- Pearl 5 – Use of Anti‑Inflammatory Adjuncts: For patients with mild ocular inflammation, a short course of topical steroids post‑injection can blunt inflammatory reactions without compromising efficacy.
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• *This drug card consolidates current evidence and is designed for quick reference by medical students and practicing clinicians.*