General

Pronunciation:
a-fli-ber-sept

Trade Name(s)

• Eylea

Ther. Class.

ocular agents

Pharm. Class.

vascular endothelial growth factor antagonists

Indications

• Neovascular (wet) age-related macular degeneration (AMD).
• Macular edema following central retinal vein occlusion (CRVO).
• Diabetic macular edema.
• Diabetic retinopathy.
• Retinopathy of prematurity.

Action

Binds to and inactivates vascular endothelial growth factor (VEGF) receptors which normally promote neovascularization and vascular permeability.

Therapeutic Effect(s):

• Slowed progression of AMD.
• Decreased macular edema following CRVO.
• Improved visual acuity in diabetic macular edema
• Decreased severity of diabetic retinopathy
• Absence of both active retinopathy of prematurity and unfavorable structural outcomes.

Pharmacokinetics

Absorption: Action is local following intravitreal injection, minimal systemic absorption occurs.

Distribution: Distribution occurs mainly in the vitreal space.

Metabolism and Excretion: Used up in the binding process and degraded by proteolytic enzymes.

Half-life: 5–6 days (plasma).

TIME/ACTION PROFILE (improved visual acuity)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity

• Ocular/periocular infection

  Active intraocular inflammation
• Lactation: Lactation.

Use Cautiously in:

• OB:  Use during pregnancy only if potential maternal benefit justifies fetal risk;
• Rep:  Women of reproductive potential;
• Pedi:   Safety and effectiveness only established in pre-term infants with retinopathy of prematurity. Safety and effectiveness not established in children <18 yr for all other indications.

Adverse Reactions/Side Effects

CV: MI, STROKE

EENT: conjunctival hemorrhage, eye pain, blurred vision, cataract, corneal edema, corneal erosion, conjunctival hyperemia, detachment of retinal pigment epithelium, endophthalmitis (from procedure), eyelid edema, foreign body sensation, injection site hemorrhage/pain, intraocular inflammation, ↑ intraocular pressure, ↑ lacrimation, retinal detachment (from procedure), vitreous detachment, vitreous floaters

Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

None reported.

Route/Dosage

Neovascular (Wet) AMD

Intravitreal (Adults): 2 mg every 4 wk for first 12 wk, then 2 mg every 8 wk (some patients may continue to require every 4 wk dosing). After one year of therapy, may consider dosing every 12 wk.

Macular Edema Following CRVO

Intravitreal (Adults): 2 mg every 4 wk.

Diabetic Macular Edema and Diabetic Retinopathy

Intravitreal (Adults): 2 mg every 4 wk for first 5 injections, then 2 mg every 8 wk (some patients may continue to require every 4 wk dosing).

Retinopathy of Prematurity

Intravitreal (Children (Preterm Infants): 0.4 mg in affected eye(s). Dose may be repeated after 10 days, if needed.

Availability

Solution for injection (vials and prefilled syringes): 2 mg/0.05 mL

Assessment

• Monitor for elevation in intraocular pressure immediately following injection; may occur within 60 min. Check for perfusion of optic nerve head or tonometry.
• Monitor infants closely after injection until retinal vascularization has completed or until examiner is assured that reactivation of retinopathy of prematurity will not occur. In infants with retinopathy of prematurity, treatment will necessitate extended periods of monitoring and additional aflibercept injections and/or laser treatments may be necessary.

Implementation

• Administer adequate anesthesia and a broad–spectrum topical antimicrobial prior to injection.
• Intravitreal 

  Use a 5-micron sterile filter needle (19-gauge × 1½-inch) to withdraw solution from vial; do not use filter needle for injection. Each vial is for single eye use only; discard after using. Use a 1-mL sterile Luer lock syringe with marking to measure 0.05 mL for adults or 0.01 mL for pre-term infants with retinopathy of prematurity.

  • Also available in a prefilled syringe. Solution is clear, colorless to pale yellow; do not use solutions that are cloudy, discolored, or contain particulate matter. Do not use if any part of the prefilled syringe is damaged or if syringe cap is detached from Luer lock. Do not use prefilled syringe for retinopathy of prematurity. Use a sterile injection needle (30-gauge × ½-inch) for injection.

Patient/Family Teaching

• Explain purpose of aflibercept to patient.
• Advise patient to notify health care professional immediately if signs and symptoms of endophthalmitis or retinal detachment (eye pain, redness of eye, photophobia, blurring of vision) or hypersensitivity reactions (anaphylaxis, rash, pruritus, urticaria, or severe intraocular inflammation) occur.
• May cause visual disturbances. Caution patient not to drive until visual function has sufficiently recovered.
• Rep:  Advise females of reproductive potential to use effective contraceptives prior to the initial dose, during treatment, and for at least 3 mo following completion of therapy and to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

• Slowed progression of macular degeneration .
• Decreased macular edema following CRVO.
• Improved visual acuity in diabetic macular edema.
• Decreased severity of diabetic retinopathy.
• Absence of both active retinopathy of prematurity and unfavorable structural outcomes.