pegaptanib (Discontinued)

>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

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 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.

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