aflibercept

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.

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

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: Discontinue aflibercept or discontinue breastfeeding.

Use Cautiously in:

• OB:  Use during pregnancy only if potential maternal benefit justifies risk to fetus
• Rep:  Women of reproductive potential;
• Pedi:   Safety and effectiveness not established.

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 noted.

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).

Availability

Solution for injection: 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.

Potential Diagnoses

• Deficient knowledge, related to medication regimen (Patient/Family/Teaching) 

Implementation

• Administer adequate anesthesia and a broad–spectrum topical antimicrobial prior to injection.
• Intravitreal Each vial is for single eye use only; discard after using.

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 female patient 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 breast feeding.

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.