aflibercept intravitreal

Action and Spectrum

Actions and Spectrum: 

Aflibercept is a recombinant fusion protein acting as a soluble decoy receptor, binding to and neutralizing vascular endothelial growth factor (VEGF) isoforms A and B, as well as placental growth factor (PGF). VEGF and PGF are proteins that play a key role in promoting the growth of abnormal blood vessels in the eye, leading to the development of retinal conditions. 

By inhibiting the activity of VEGF and PGF, aflibercept intravitreal reduces the growth of abnormal blood vessels, and helps to prevent further damage to the retina. This can result in improved vision and a reduced risk of blindness in patients with neovascular age-related macular degeneration, diabetic macular edema, and macular edema following retinal vein occlusion. 

Overall, aflibercept intravitreal has a broad spectrum of action, as it targets multiple isoforms of VEGF and PGF. This allows it to be effective in treating various retinal conditions that involve abnormal blood vessel growth. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Eye pain (9-13%) 

Conjunctival hemorrhage (12-31%) 

Cataract (1-13%) 

1-10% 

Corneal epithelium defect (2-7%) 

Injection site hemorrhage (1-2%) 

Vitreous floaters (6-8%) 

Retinal pigment epithelium tear (2%) 

Increased IOP (5-9%) 

Vitreous detachment (1-8%) 

Ocular hyperemia (42-5%) 

Injection site pain (1-3%) 

Blurred vision (1-4%) 

Lacrimation increased (3-4%) 

Foreign body sensation in eyes (3-4%) 

Retinal pigment epithelium detachment (3-5%) 

Eyelid edema (1-2%) 

Intraocular inflammation (1-3%) 

Corneal edema (1%) 

Conjunctival hemorrhage (5-9%) 

Retinal detachment (5-6%) 

Eyelid edema (3%) 

Increased IOP (4%) 

Corneal epithelium defect (1%) 

Lenticular opacities (1%) 

Corneal edema (1%) 

Black Box Warning

Black Box Warning: 

The black box warning is related to the risk of endophthalmitis, which is a serious eye infection that can lead to vision loss or blindness. Endophthalmitis is a rare but potentially serious complication that can occur after any injection into the eye. 

The black box warning states that there is a risk of endophthalmitis with intravitreal injections, including aflibercept. Healthcare providers should use proper aseptic injection techniques when administering the medication and should monitor patients closely for any signs of infection or inflammation following the injection. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

aflibercept intravitreal is contraindicated in patients who have a known hypersensitivity to aflibercept or any of the components in the formulation. Hypersensitivity reactions can include anaphylaxis, which is a severe allergic reaction that can be life-threatening. 

Additionally, there are some other factors that should be considered before using aflibercept intravitreal. These include: 

• Active intraocular inflammation: aflibercept intravitreal should not be used in patients who have active intraocular inflammation because it may exacerbate the inflammation. 
• Ocular or periocular infections: aflibercept intravitreal should not be used in patients who have active ocular or periocular infections because it may worsen the infection. 
• Bleeding disorders: aflibercept intravitreal may increase the risk of bleeding in patients with bleeding disorders, and caution should be exercised when administering the medication in these patients. 
• Pregnancy and breastfeeding: The safety and effectiveness of aflibercept intravitreal in pregnant and breastfeeding women have not been established. Therefore, it should only be used during pregnancy or breastfeeding if the potential benefits outweigh the potential risks to the fetus or infant. 

Caution 

• Thromboembolic events: There have been reports of thromboembolic events (such as stroke or heart attack) in patients receiving intravitreal injections of VEGF inhibitors, including aflibercept. Healthcare providers should use caution when prescribing aflibercept to patients with a history of thromboembolic events. 
• Increased intraocular pressure: aflibercept intravitreal may increase intraocular pressure (IOP) in some patients, and this can lead to glaucoma. Healthcare providers should monitor IOP in patients receiving aflibercept and treat any increase in pressure appropriately. 
• Tractional retinal detachment: There have been reports of tractional retinal detachment in some patients with proliferative diabetic retinopathy receiving aflibercept intravitreal. Healthcare providers should use caution when prescribing aflibercept to patients with this condition. 
• Immunogenicity: Some patients may develop antibodies to aflibercept, which could reduce its effectiveness. Healthcare providers should monitor patients for signs of reduced efficacy and consider alternative treatments if necessary. 
• Use in children: The safety and efficacy of aflibercept intravitreal have not been established in pediatric patients. Healthcare providers should use caution when prescribing aflibercept to children and carefully evaluate the potential benefits and risks of treatment. 

Pregnancy / Lactation

Pregnancy consideration:  

AU TGA pregnancy category: D
US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk is Not known.  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

aflibercept intravitreal is a medication used to treat various eye conditions, such as wet age-related macular degeneration, diabetic macular edema, and macular edema following retinal vein occlusion. It works by blocking the activity of certain proteins in the eye that promote the growth of abnormal blood vessels and inflammation. 

Aflibercept is a type of medication called a recombinant fusion protein. It is made up of portions of two different proteins that are naturally present in the body. These proteins are fused together to create a new protein that can bind to and neutralize the activity of other proteins that contribute to eye disease. 

Pharmacodynamics: 

The mechanism of action of this medication involves binding and preventing the activation of vascular endothelial growth factors (VEGF-A) and placental growth factor (PIGF). These growth factors can cause neovascularization and increased vascular permeability in certain conditions, such as cancer and age-related macular degeneration. By inhibiting their activation, this medication can help reduce abnormal blood vessel growth and leakage, which can improve symptoms and slow disease progression. 

Pharmacokinetics: 

Absorption 

aflibercept intravitreal is a medication that is injected into the vitreous humor which is the clear gel-like substance that fills the eye. Because it is administered directly into the eye, the absorption of aflibercept intravitreal is localized to the eye and does not result in significant systemic absorption. 

Distribution 

Volume of distribution is 6 litres. 

Metabolism 

aflibercept intravitreal is not metabolized in the body, as it is not absorbed into the systemic circulation. 

Elimination and Excretion 

The elimination half-life is 5-6 days. 

Adminstartion

Administration: 

Intravitreal administration 

aflibercept intravitreal is administered by injection into the eye, usually in a clinical setting by a healthcare professional. Here are some general guidelines for the administration of aflibercept intravitreal: 

• Preparation: A healthcare provider will prepare the medication by drawing it into a syringe and attaching a sterile needle. 
• Eye preparation: The patient’s eye will be cleaned and numbed with topical anesthesia drops. 
• Injection: The healthcare provider will use a sterile technique to inject the medication into the vitreous (the jelly-like substance in the back of the eye). The injection is usually given in the lower part of the eye. 
• Post-injection care: After the injection, the healthcare provider will monitor the patient for any immediate adverse reactions or signs of infection. The patient will be advised to use antibiotic eye drops to prevent infection and to avoid rubbing or touching the eye. 
• Follow-up: The patient will usually need to return for follow-up visits to monitor their response to treatment and assess any potential side effects. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: aflibercept intravitreal 

Pronounced: [ a-FLIB-er-sept-off-THAL-mik ] 

Why do we use aflibercept intravitreal? 

aflibercept intravitreal is a medication that is used to treat certain eye conditions that affect the retina.The primary uses of aflibercept intravitreal include: 

• Wet age-related macular degeneration (AMD): aflibercept intravitreal is FDA-approved to treat wet AMD, which leads to vision loss. 
• Diabetic macular edema: aflibercept intravitreal is also FDA-approved to treat DME, a complication of diabetes that can cause swelling in the retina and vision loss. 
• Macular edema following retinal vein occlusion (RVO): aflibercept intravitreal is also approved to treat macular edema following RVO, which is a blockage of the small veins that carry blood away from the retina.