Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravitreal [preservative free]:
Eylea: 2 mg/0.05 mL (0.05 mL)
Solution Prefilled Syringe, Intravitreal [preservative free]:
Eylea: 2 mg/0.05 mL (0.05 mL)
Mechanism of Action
Aflibercept is a recombinant fusion protein that acts as a decoy receptor for vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PLGF). Aflibercept binds to VEGF-A and PLGF and inhibits binding and activating of endothelial cell receptors, thereby suppressing neovascularization and slowing vision loss.
Low levels are detected in the serum following intravitreal injection; levels undetectable 2 weeks after administration .
~6 L (IV)
Plasma: ~5 to 6 days (IV)
Use: Labeled Indications
Age-related macular degeneration: Treatment of neovascular (wet) age-related macular degeneration.
Diabetic macular edema: Treatment of diabetic macular edema.
Diabetic retinopathy: Treatment of diabetic retinopathy.
Macular edema: Treatment of macular edema following retinal vein occlusion.
Known hypersensitivity to aflibercept or any component of the formulation; current ocular or periocular infection; active intraocular inflammation
Dosage and Administration
Age-related macular degeneration: Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 12 weeks (3 months), followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months). Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 12 weeks of therapy (first 3 injections). Some patients may also be treated every 12 weeks (3 months) after one year of effective treatment (not as effective as every 8 week administration).
Diabetic macular edema: Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 5 injections, followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months). Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 20 weeks of therapy (first 5 injections).
Diabetic retinopathy: Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 5 injections, followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months). Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 20 weeks of therapy (first 5 injections).
Macular edema following retinal vein occlusion: Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly)
Refer to adult dosing.
Prefilled syringe: Each prefilled syringe should only be used for the treatment of a single eye. Syringe tray should be opened under sterile conditions. Twist off syringe cap, then attach a 30-gauge 1/2-inch needle (not supplied) onto the prefilled syringe. Expel air bubbles and slowly depress plunger to expel excess medication (plunger tip should align with the black dosing line on syringe). Refer to manufacturer's labeling for additional information.
Vial: Each vial should only be used for the treatment of a single eye. Remove contents from vial using the supplied 5 micron (19-gauge 11/2-inch) filter needle and 1 mL syringe. Discard filter needle and replace with the supplied 30-gauge 1/2-inch needle (do not use filter needle for intravitreal injection). Expel air bubbles and slowly depress plunger to expel excess medication (plunger tip should align with the 0.05 mL marking on syringe). Refer to manufacturer's labeling for additional information.
For ophthalmic intravitreal injection under controlled aseptic conditions. Each vial or prefilled syringe should only be used for the treatment of a single eye. If the contralateral eye requires treatment, a new vial or prefilled syringe should be used and the sterile field, syringe, gloves, drapes, eyelid speculum, filter, and injection needles should be changed before aflibercept is administered to the other eye. Should be administered using a 30-gauge 1/2-inch sterile needle. Adequate anesthesia and a topical broad-spectrum antimicrobial agent should be administered prior to the procedure.
Store refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. Protect from light. Store in original container prior to use. Discard unused product.
There are no known significant interactions.
>10%: Ophthalmic: Conjunctival hemorrhage (12% to 31%), cataract (≤19%), eye pain (9% to 13%)
1% to 10%:
Cardiovascular: Arterial thrombosis (2% to 6%)
Central nervous system: Foreign body sensation of eye (3% to 4%)
Immunologic: Antibody development (1% to 3%)
Local: Pain at injection site (1% to 3%), bleeding at injection site (≤2%)
Ophthalmic: Increased intraocular pressure (2% to 9%), vitreous detachment (2% to 8%), vitreous opacity (1% to 8%), epithelial keratopathy (2% to 7%), ocular hyperemia (4% to 5%), retinal pigment epithelium detachment (3% to 5%), increased lacrimation (3% to 4%), blurred vision (1% to 4%), intraocular inflammation (1% to 3%), retinal pigment epithelium tear (2%), eyelid edema (≤2%), corneal edema (≤1%), retinal detachment (<1%)
<1%, postmarketing, and/or case reports: Endophthalmitis, hypersensitivity reaction
Concerns related to adverse effects:
- Endophthalmitis/retinal detachment: Intravitreous injections are associated with endophthalmitis, retinal detachments, retinal tear, retinal pigment epithelium tear, and cataract, including traumatic cataract. Use proper aseptic injection techniques. Instruct patients to report any signs of infection (eg, eye pain or redness, photophobia, blurred vision) immediately; manage appropriately.
- Hypersensitivity reactions: Hypersensitivity may present as rash, pruritus, urticaria, severe anaphylactic/anaphylactoid reactions, or severe intraocular inflammation.
- Increased intraocular pressure: Following intravitreal injection, intraocular pressure may increase (acute). Onset is seen within 60 minutes. Sustained increases in intraocular pressure have also been reported (with repeated dosing of intravitreal VEGF inhibitors). Monitor intraocular pressure and optic nerve head perfusion.
- Thromboembolic events: Risk of thromboembolic events (eg, nonfatal stroke/MI, vascular death) may be increased following intravitreal administration of VEGF inhibitors, including aflibercept.
- Women: Women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for at least 3 months after the last dose.
Intraocular pressure immediately following injection; signs of infection/inflammation (for first week following injection); optic nerve head perfusion; signs/symptoms of endophthalmitis or retinal detachment; visual acuity; signs/symptoms of hypersensitivity reaction
Aflibercept (ophthalmic) is a vascular endothelial growth factor (VEGF) inhibitor; VEGF is required to achieve and maintain normal pregnancies. Reports of intravitreal VEGF inhibitor use in pregnancy are limited and information specific to use of aflibercept (ophthalmic) has not been located (Peracha 2016). Based on studies in nonpregnant adults, VEGF inhibitors can alter systemic concentrations of VEGF and placental growth factor following intravitreal administration (Peracha 2016; Zehtner 2015). Until additional information is available, intravitreal use during the first trimester should be avoided and use later in pregnancy should be based on patient specific risks versus benefits (Peracha 2016; Polizzi 2015).
Evaluate pregnancy status prior to use in females of reproductive potential. Women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for at least 3 months after the last intravitreal injection.
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience floater in the eye. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), chest pain, jaw pain, vision changes, eye pain, severe eye irritation, eye redness, eyelid swelling, or sensitivity to light (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.