Dosing and uses of Macugen (pegaptanib)
Adult dosage forms and strengths
intravitreous injection
- 0.3mg/90mcL (prefilled syringe)
Neovascular (Wet) Age-Related Macular Degeneration
0.3 mg intravitreous q6Weeks
Pediatric dosage forms and strengths
Indication not applicable to children
Macugen (pegaptanib) adverse (side) effects
>10%
Anterior chamber inflammation
Blurred vision
Cataract
Conjunctival hemorrhage
Corneal edema
Eye discharge, irritation, pain
Hypertension
Inceased IOp
Ocular discomfort
Punctate keratitis
Reduced visual acuity
Visual disturbance
Vitreous floaters
Vitreous opacities
1-10%
Allergic conjunctivitis
Blepharitis
Conjunctival edema
Conjuctivitis
Corneal abrasion, corneal deposits, corneal epithelial d/o
Contact dermatitis
Endophthalmitis
Eye inflammation/swelling, eyelid irritation
Mydriasis
Periorbital hematoma
Photopsia
Retinal edema
Vitreous d/o, vitreous hemorrhage
Arthritis
Bone spur
Bronchitis
Carotid artery occlusion
Chest pain, contusion
CVA/TIA
Dizziness
Headache
Hearing loss
Meibomianitis
Pleural effusion
Urinary retention
UTI
Diabetes mellitus
Diarrhea
Dyspepsia
Nausea
Vomiting
<1%
Iatrogenic traumatic cataract
Retinal detachment
Angioedema hypersensitivity
Warnings
Contraindications
Hypersensitivity
Ocular/periocular infections
Cautions
Use proper aseptic techniques to minimize risk of endophthalmitis
Risk of increased IOP; monitor IOP and perfusion of the optic nerve
In clinical studies, less effective in the second year than during the first
Efficacy decreased at doses >1 mg
Thromboembolic events reported following intravitreal administration of other VEGF inhibitors
Safety and efficacy of concurrent administration on both eyes not studied
Pregnancy and lactation
Pregnancy category: B
No adequate human data; in mice, produced no maternal toxicity and no evidence of teratogenicity or fetal mortality at IV doses up to 40 mg/kg/day (about 7,000 times the recommended human monocular ophthalmic dose of 0.3 mg/eye)
Lactation: Ecretion in breast milk unknown; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Macugen (pegaptanib)
Mechanism of action
Aptamer that binds to and inhibits binding of the angiogenic cytokine VEGF to the receptor, which in turn suppresses neovascularization and slows vision loss
Metabolism
Endo- and exonucleases (based on preclinical data)
Elimination
Excretion: Primarily urine
Half-life: 6-14 days
