aflibercept ophthalmic
Generic Name: aflibercept
ophthalmic (a FLIB er sept off THAL mik)
Brand Name: Eylea
Pronunciation
(a FLIB er sept)
Index Terms
AVE 0005
AVE 005
AVE-0005
VEGF Trap
VEGF Trap-Eye
Dosage Forms
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)
Brand Names: U.S.
Eylea
Pharmacologic Category
Ophthalmic Agent
Vascular Endothelial Growth Factor (VEGF) Inhibitor
Pharmacology
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.
Absorption
Low levels are detected in the
serum following intravitreal injection; levels undetectable 2 weeks after administration
.
Distribution
~6 L (IV)
Half-Life
Elimination
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 in patients with
diabetic macular edema
Macular edema: Treatment of macular edema following retinal vein
occlusion
Contraindications
Known hypersensitivity to
aflibercept or any component of the formulation; current ocular or periocular
infection; active intraocular inflammation
Dosing: Adult
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).
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)
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment
necessary.
Dosing: Hepatic Impairment
There are no dosage
adjustments provided in the manufacturer's labeling (has not been studied);
however, no adjustment expected due to minimal systemic absorption.
Reconstitution
Each vial should only be used
for the treatment of a single eye. If the contralateral eye requires treatment,
a new vial 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. Inspect vial prior to
administration; do not use if particulates, cloudiness, or discoloration are
present.
Administration
For ophthalmic intravitreal
injection only. Using aseptic technique, remove entire contents of vial using a
5 micron, 19-gauge 11/2 inch filter needle
(supplied) attached to a 1 mL syringe (supplied); keep the needle bevel
submerged to avoid introducing excess air. Draw plunger rod back to completely
empty the filter needle, then remove and discard filter needle and replace with
a sterile 30-gauge 1/2 inch needle (supplied)
for intravitreal injection procedure (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). The
intravitreal injection should be performed under controlled aseptic conditions,
which include surgical hand disinfection and the use of sterile gloves, a
sterile drape, and a sterile eyelid speculum (or equivalent). Adequate
anesthesia and a topical broad-spectrum antimicrobial agent should be
administered prior to the procedure.
Storage
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.
Drug Interactions
There are no known significant
interactions.
Adverse Reactions
>10%: Ophthalmic:
Conjunctival hemorrhage (12% to 31%), cataract (5% to 19%), eye pain (9% to
13%)
1% to 10%:
Cardiovascular: Arterial
thrombosis (2% to 6%)
Central nervous system:
Foreign body sensation of eye (3%)
Immunologic: Antibody
development (1% to 3%; most patients had immunoreactivity at baseline)
Local: Pain at injection site
(1% to 3%), bleeding at injection site (≤1%)
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%), increased lacrimation (3% to 4%), retinal pigment epithelium detachment
(3%), intraocular inflammation (2% to 3%), retinal pigment epithelium tear
(2%), blurred vision (1% to 2%), eyelid edema (1% to 2%), corneal edema (≤1%)
<1% (Limited to important
or life-threatening): Endophthalmitis, hypersensitivity, retinal detachment,
uveitis
Warnings/Precautions
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.
Special populations:
• 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.
Monitoring Parameters
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
Pregnancy Considerations
Adverse events have been
observed in animal reproduction studies. 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.
Patient Education
• 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), angina, jaw pain, vision changes, eye pain, severe eye
irritation, eye redness, eyelid edema, 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.
