Aflibercept (Intraocular)

Aflibercept is a fragment of a human antibody that works by altering the amount of blood flow to the retina. Below is detailed information about this drug.

Overview

The U.S. brand name for this drug is Eylea, and it is administered by injection into the treatment area. This medicine is a VEGF inhibitor that controls blood flow to the retina by preventing the development of new blood vessels. When these blood vessels are prevented from forming under the retina, blood flow is restricted to these parts. This prevents the leakage of blood and fluids from the retina.

It is a prescription-only medication that is administered by a healthcare professional and belongs to the drug class anti-angiogenic ophthalmic agents. It is available as generic drugs with aflibercept as the active ingredient. It is currently presented in solution form in glass vials.

This drug is FDA approved and got its first approval on November 18th, 2011. The drug is contraindicated for people with swellings in their eyes, bacterial, viral or fungal infections and those allergic to the medication.

Conditions Treated

  • Neovascular (wet) macular degeneration that is age-related
  • Macular edema that follows retinal vein occlusion
  • Diabetic macular edema
  • Diabetic retinopathy

Medicine Type

  • Ophthalmic agent

Side Effects

The following signs indicate an allergic reaction to aflibercept and constitute a medical emergency:

  • Hives
  • Labored or difficult breathing
  • The face, tongue, lips or throat may swell.

A doctor should also be informed immediately if the following symptoms present:

  • Vision problems that come on suddenly.
  • Blurred vision or blindness
  • An ache in the eye
  • Bloody eye
  • Sighting floaters' or sparks and flashes of light. Other issues are such as seeing a curtain or veil.
  • Swelling or redness around the eye
  • Eyes becoming more sensitive to light
  • Headaches that come on suddenly
  • Experiencing speech and balance problems or confusion
  • Weakness or numbness that may affect one side of the body and that comes on suddenly.

Others that are less seen but do warrant immediate medical attention are the following:

  • Swelling eyelid
  • Pain or bleeding at the injection site
  • Fast heartbeat
  • Headaches
  • Itching, rash, hives or skin redness
  • Hoarseness
  • Stiffness pain or swelling in joints
  • Trouble swallowing or breathing
  • Sudden severe headache
  • Pain in the legs, mainly the calves, groin, and chest
  • Shortness of breath.

Some side effects do not constitute a medical emergency. They go away in time as the body gets used to the medication. If these minor side effects do become bothersome, the advice of a healthcare professional should be sought on steps to take to prevent their occurrence or reduce their impact. These are the following:

  • Watery eyes
  • A feeling that there is something inside the eyes.

Other side effects not listed here may occur, and the healthcare professional treating the patient should be notified.

Dosage

Dosage considered here is 40mg/mL.

The dosage form is an intravitreal injectable solution.

PEDIATRIC CASES

Safety and efficacy for use in children and persons less than 18 years of age have not been established. The drug is not recommended for use for such.

ADULTS AND GERIATRIC

Dosage for Neovascular (Wet) Macular Degeneration, Age-Related. (AMD).

2mg (0.5 mL) given by intravitreal injection after every four weeks (monthly) for the first three months (twelve weeks) of treatment. This should be followed by the same dosage, 2mg (0.5mL) every two months (8 weeks).

Dosage for Macular Edema Following Retinal Vein Occlusion (RVO)

2mg (0.5mL) given monthly (every four weeks) by intravitreal injection

Dosage for Diabetic Retinopathy (DR) occurring in Patients with DME/Diabetic Macular Edema (DME)

2mg (0.5mL) given by intravitreal injection every month (4 weeks) for the first five months. This should be followed by 2mg (0.5mL) given by intravitreal injection every two months (8 weeks).

Additional comment: There was no additional efficacy when dosing was done every four weeks as compared to eight weeks.

Renal and Liver Dose Adjustments

There are no recommendations for this.

Dialysis

No recommendations are available.

Administration

  • Reference should be made to the product information from the manufacturer for preparation guidelines.
  • The vial with the medicine should be inspected before using it. If the contents of the vial appear cloudy, discolored or have particulates, the medication should be discarded as it is unsafe to use.
  • Aflibercept should be given under controlled aseptic conditions. The doctor giving the intravitreal injection should do appropriate surgical hand disinfection, and wear sterile drape, gloves and eyelid speculum or any equivalent. A broad spectrum topical microbicide and proper anesthesia should be administered before giving the injection.
  • The patient should be appropriately monitored following the injection, and required apparatus readied in case of an emergency situation.
  • The patient should be directed to inform their healthcare provider of symptoms that may indicate retinal detachment or endophthalmitis. The signs to look out for include redness in the eye, eye pain, blurred vision, and photophobia.
  • Each vial of aflibercept is for use for treatment of one eye. Any unused medicine should be discarded and a new vial used if the other eye requires treatment.

Interactions

DRUG AND FOOD INTERACTIONS

There are no known Eylea drug interactions. However, this should not imply that a medical practitioner should not be informed of what a patient is taking while on treatment. The medical practitioner must be notified of all other drugs, vitamins, minerals and other natural products that a patient is taking before and while they receive treatment with Eylea (aflibercept ophthalmic).

Natural and organic products should not be considered safe and must be listed for a medical practitioner to determine safety.

DISEASE INTERACTIONS

Eylea has one known disease interaction. It interacts with ocular infections.

Warnings

PREGNANCY

Animal studies done showed evidence of embryofetal toxicity when aflibercept is administered during gestation. There are no controlled studies done for pregnant women. It is an AU TGA pregnancy category D drug. These are drugs that are very likely to be unsafe in pregnancy and may increase the incidence of irreversible damage or fetal malformations in humans. The pharmacological effects of these drugs are also adverse.

It is a U.S. FDA category C drug. Animal studies show this drug harms the fetus when administered during gestation. There are no well-controlled, adequate studies done on humans to determine the safety of aflibercept during pregnancy conclusively. Pregnant women may receive this drug, however, if the benefits of using it outweigh the risks. For the most part, however, it is to be avoided during pregnancy.

Women of childbearing age should use an effective contraceptive if they are to receive aflibercept treatment. They should continue taking the contraceptives three months after the last injection to ensure they do not conceive at this time.

BREASTFEEDING WARNINGS

This drug should not be used by a mother who has a breastfeeding child as there are no studies to determine if it passes into breast milk, and what effect it would have on the child if it does. If a mother must use this drug, it is recommended that she discontinue breastfeeding.

OTHER WARNINGS

  • Aflibercept may cause blurred vision a few days after receiving the injection. A patient should be advised to avoid driving or operating machinery for some time until they can see clearly again.
  • Renal detachments and endophthalmitis have been observed where intravitreal injections had been administered. The injection techniques used to administer aflibercept must be proper and aseptic. Patients must be advised on what to look out for in case of these complications and report any issues as soon as they occur.
  • Intraocular pressure may increase. Intraocular pressure has been seen to increase acutely within 60 minutes of a patient receiving an intravitreal injection. Intraocular pressure should be monitored and managed appropriately so that subsequent dosages of aflibercept do not worsen the situation.
  • There is a likely risk of arterial thromboembolic events (ATE) with the administration of aflibercept.

Storage

Aflibercept should be refrigerated at 2 to 8 degrees centigrade, but not frozen. Additionally, it should be well protected from light and stored in its original carton until the day of use. It should not be used after the use by date which is usually stamped on the container.

Summary

Eylea (Aflibercept ophthalmic) is a safe intervention for the medical conditions it is meant to treat. However, this does not imply that a patient can start or stop this medication anytime, or mix it with any other without proper consultation with a healthcare provider. No medicine is too safe that the advice of a trained professional is not required.

A patient receiving aflibercept should also not try to add other medications to their eyes without consulting a medical practitioner. Even though aflibercept has no known interactions, it would still be unsafe for a patient to prescribe themselves some medication. It is particularly dangerous to use someone else's medicine. Patients receiving this drug are not advised to medicate on their own even when faced with the not so serious side effects. Only a doctor should offer solutions in response to any side effects.

A drug only works well if it is used correctly and at the right dosages, which should just be prescribed by a medical practitioner. The information contained herein on aflibercept is in no way conclusive. It is not meant to endorse aflibercept for treatment of any disease or medical condition. Only a doctor can determine what is best in a given situation.

The information should be used as a general guide but should never replace getting the advice of a healthcare professional.

Resources
Last Reviewed:
December 10, 2017
Last Updated:
April 27, 2018