7/11. Aflibercept-( Eylea)- (Nov 2011) Metabolic disorder
Drug Name:7/11. Aflibercept-( Eylea)- (Nov 2011) Metabolic disorder
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Indication:
EYLEA (aflibercept) Injection For Intravitreal Injection
Initial U.S. Approval: 2011
RECENT MAJOR CHANGES
Indications and Usage, Macular Edema Following Retinal Vein Occlusion (RVO)
(1.2) 10/2014
Indications and Usage, Diabetic Macular Edema (DME) (1.3) 7/2014
Indications and Usage, Diabetic Retinopathy (DR) in Patients with DME
(1.4) 3/2015
Dosage and Administration, Macular Edema Following Retinal Vein
Occlusion (RVO) (2.3) 10/2014´
Dosage and Administration, Diabetic Macular Edema (DME)
(2.4) 7/2014
Dosage and Administration, Diabetic Retinopathy (DR) in Patients
with DME (2.5) 3/2015
Warnings and Precautions, Thromboembolic Events (5.3) 10/2014
Drug Name- Eylea
Active Ingedient - Aflibercept
To treat patients with wet(neovascular ) age-related mascular degeneration
(AMD) , a leading cause of vision loss and blindness in Amercicans ages
60 and older
Indication-
Treat patients with wet(neovascular ) age-related mascular degeneration
(AMD) , leading to vision loss and blindness in Amercicans ages
60 and older
Approved by FDA on 18-11-2011 (Ref- FDA approved List- 2011)
Adverse Reaction:
The most common adverse reactions (.5%) reported in patients receiving EYLEA
were conjunctival hemorrhage, eye pain, cataract, vitreous floaters, intraocular
pressure increased, and vitreous detachment.
Contra-Indications:
CONTRAINDICATIONS
1 Ocular or Periocular Infections
EYLEA is contraindicated in patients with ocular or periocular infections.
2 Active Intraocular Inflammation
EYLEA is contraindicated in patients with active intraocular inflammation.
3 Hypersensitivity
EYLEA is contraindicated in patients with known hypersensitivity to aflibercept or
any of the excipients in EYLEA. Hypersensitivity reactions may manifest as
severe intraocular inflammation.
WARNINGS AND PRECAUTIONS
1 Endophthalmitis and Retinal Detachments
Intravitreal injections, including those with EYLEA, have been associated with
endophthalmitis and retinal detachments
Proper aseptic injection technique must always be used when administering EYLEA.
2.Patients should be instructed to report any symptoms suggestive of endophthalmitis
or retinal detachment without delay and should be managed appropriately
3.. Increase in Intraocular Pressure
Acute increases in intraocular pressure have been seen within 60 minutes of
intravitreal injection, including with EYLEA .
Sustained increases in intraocular pressure have also been reported after
repeated intravitreal dosing with vascular endothelial growth factor (VEGF)
inhibitors.
Intraocular pressure and the perfusion of the optic nerve head should be
monitored and managed appropriately
4.Thromboembolic Events
There is a potential risk of arterial thromboembolic events (ATEs) following
intravitreal use of VEGF inhibitors, including EYLEA.
ATEs are defined as nonfatal stroke, nonfatal myocardial infarction,
or vascular death (including deaths of unknown cause).
Dosages/ Overdosage Etc:
INDICATIONS AND USAGE
EYLEA is indicated for the treatment of patients with:
Neovascular (Wet) Age-Related Macular Degeneration (AMD)
Macular Edema Following Retinal Vein Occlusion (RVO)
Diabetic Macular Edema (DME)
Diabetic Retinopathy (DR) in Patients with DME
DOSAGE AND ADMINISTRATION
Neovascular (Wet) Age-Related Macular Degeneration (AMD)
The recommended dose for EYLEA is 2 mg (0.05 mL) administered by
intravitreal injection every 4 weeks (monthly) for the first 3 months,
followed by 2 mg (0.05 mL) via intravitreal injection once every
8 weeks (2 months).
Although EYLEA may be dosed as frequently as 2 mg every 4 weeks (monthly),
additional efficacy was not demonstrated when EYLEA was dosed every 4 weeks
compared to every 8 weeks.
Macular Edema Following Retinal Vein Occlusion (RVO)
The recommended dose for EYLEA is 2 mg (0.05 mL) administered by intravitreal
injection once every 4 weeks (monthly).
Diabetic Macular Edema (DME) and Diabetic Retinopathy (DR) in Patients
with Diabetic Macular Edema
The recommended dose for EYLEA is 2 mg (0.05 mL) administered by
intravitreal injection every 4 weeks (monthly) for the first 5 injections followed
by 2 mg (0.05 mL) via intravitreal injection once every 8 weeks (2 months).
Although EYLEA may be dosed as frequently as 2 mg every 4 weeks (monthly),
additional efficacy was not demonstrated when EYLEA was dosed every 4 weeks
compared to every 8 weeks.
DOSAGE FORMS AND STRENGTHS
40 mg/mL solution for intravitreal injection in a single-use vial
Patient Information:
PATIENT COUNSELING INFORMATION
In the days following EYLEA administration, patients are at risk of developing
endophthalmitis or retinal detachment.
If the eye becomes red, sensitive to light, painful, or develops a change in vision,
advise patients to seek immediate care from an ophthalmologist..
Patients may experience temporary visual disturbances after an intravitreal inject
ion with EYLEA and the associated eye examinations.
Advise patients not to drive or use machinery until visual function has recovered
sufficiently
Pharmacology/ Pharmacokinetics:
1 Mechanism of Action
Vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PlGF)
are members of the VEGF family of angiogenic factors that can act as mitogenic,
chemotactic, and vascular permeability factors for endothelial cells.
VEGF acts via two receptor tyrosine kinases, VEGFR-1 and VEGFR-2, present
on the surface of endothelial cells.
PlGF binds only to VEGFR-1, which is also present on the surface of leucocytes.
Activation of these receptors by VEGF-A can result in neovascularization and vascular
permeability
2. Pharmacokinetics
EYLEA is administered intravitreally to exert local effects in the eye. In patients
with wet AMD, RVO, or DME, following intravitreal administration of EYLEA,
a fraction of the administered dose is expected to bind with endogenous
VEGF in the eye to form an inactive aflibercept: VEGF complex.
Once absorbed into the systemic circulation, aflibercept presents in the plasma
as free aflibercept (unbound to VEGF) and a more predominant stable inactive
form with circulating endogenous VEGF (i.e., aflibercept: VEGF complex).
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
There are no adequate and well-controlled studies in pregnant women.
EYLEA should be used during pregnancy only if the potential benefit justifies
the potential risk to the fetus.
Females of reproductive potential should use effective contraception prior to
the initial dose, during treatment, and for at least 3 months after the last
intravitreal injection of EYLEA.
2. Nursing Mothers
It is unknown whether aflibercept is excreted in human milk. Because many drugs
are excreted in human milk, a risk to the breastfed child cannot be excluded.
EYLEA is not recommended during breastfeeding. A decision must be made
whether to discontinue nursing or to discontinue treatment with EYLEA,
taking into account the importance of the drug to the mother.
3. Pediatric Use
The safety and effectiveness of EYLEA in pediatric patients have not been
established.
4. Geriatric Use
In the clinical studies, approximately 76% (2049/2701) of patients randomized
to treatment with EYLEA were .65 years of age and approximately 46% were
75 years of age. No significant differences in efficacy or safety were seen with
increasing age in these studies.
