Pegaptanib

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intraocular [preservative free]:

Macugen: 0.3 mg (0.09 mL)

Pharmacology

Mechanism of Action

Pegaptanib is an apatamer, an oligonucleotide covalently bound to polyethylene glycol, which can adopt a three-dimensional shape and bind to vascular endothelial growth factor (VEGF). Pegaptanib binds to extracellular VEGF, selectively inhibiting VEGF from binding to its receptors and thereby suppressing neovascularization and slowing vision loss.

Pharmacokinetics/Pharmacodynamics

Absorption

Slow systemic absorption following intravitreous injection

Metabolism

Metabolized by endo- and exonucleases

Half-Life Elimination

Plasma: 10 ± 4 days

Use: Labeled Indications

Macular degeneration (neovascular age-related): Treatment of neovascular (wet) age-related macular degeneration (AMD)

Contraindications

Known hypersensitivity to pegaptanib or any component of the formulation; ocular or periocular infections

Dosage and Administration

Dosing: Adult

Macular degeneration (neovascular age-related): Intravitreous injection: 0.3 mg into affected eye once every 6 weeks

Dosing: Geriatric

Refer to adult dosing.

Administration

For ophthalmic intravitreal injection only. Attach a 30 gauge ¹/₂ inch needle to the medication syringe. Slowly depress plunger to expel excess air and medication (refer to product labeling for detailed instructions). Injection should be performed under aseptic conditions. Adequate anesthesia and a topical broad spectrum antibiotic should be administered prior to the procedure.

Storage

Store at 2°C to 8°C (36°F to 46°F); do not freeze. Do not shake vigorously.

Drug Interactions

Pegloticase: May diminish the therapeutic effect of PEGylated Drug Products. Monitor therapy

Pegvaliase: PEGylated Drug Products may enhance the adverse/toxic effect of Pegvaliase. Specifically, the risk of anaphylaxis or hypersensitivity reactions may be increased. Monitor therapy

Adverse Reactions

>10%:

Cardiovascular: Hypertension

Ophthalmic: Anterior chamber inflammation, blurred vision, cataract, conjunctival hemorrhage, corneal edema, decreased visual acuity, eye discharge, eye discomfort, eye irritation, eye pain, increased intraocular pressure, punctate keratitis, visual disturbance, vitreous opacity

1% to 10%:

Cardiovascular: Cerebrovascular accident (1% to 5%), chest pain (1% to 5%), occlusive arterial disease (carotid artery: 1% to 5%), transient ischemic attacks (1% to 5%)

Central nervous system: Dizziness (6% to 10%), headache (6% to 10%), vertigo (1% to 5%)

Dermatologic: Contact dermatitis (1% to 5%)

Endocrine & metabolic: Diabetes mellitus (1% to 5%)

Gastrointestinal: Diarrhea (6% to 10%), nausea (6% to 10%), dyspepsia (1% to 5%), vomiting (1% to 5%)

Genitourinary: Urinary tract infection (6% to 10%), urinary retention (1% to 5%)

Hematologic & oncologic: Bruise (1% to 5%), periorbital hematoma (1% to 5%), vitreous hemorrhage (1% to 5%)

Local: Local inflammation (eye: 1% to 5%), local irritation (eyelid: 1% to 5%)

Neuromuscular & skeletal: Arthritis (1% to 5%), bone spur (1% to 5%)

Ophthalmic: Blepharitis (6% to 10%), conjunctivitis (6% to 10%), photopsia (6% to 10%), vitreous disorder (6% to 10%; includes inflammation), allergic conjunctivitis (1% to 5%), conjunctival edema (1% to 5%), corneal abrasion (1% to 5%), corneal deposits (1% to 5%), epithelial keratopathy (1% to 5%), endophthalmitis (1% to 5%), meibomianitis (1% to 5%), mydriasis (1% to 5%), retinal edema (1% to 5%), swelling of eye (1% to 5%)

Otic: Auditory impairment (1% to 5%)

Respiratory: Bronchitis (6% to 10%), pleural effusion (1% to 5%)

<1%, postmarketing, and/or case reports: Accidental injury, anaphylactoid reaction, anaphylaxis, angioedema, arthropathy, blindness, choroidal detachment, colonic polyps, decreased white blood cell count, dysphagia, feeling abnormal, foreign body sensation of eye, giant-cell arteritis, hematochezia, hemoptysis, hemorrhage, iatrogenic traumatic cataracts, immune thrombocytopenia, increased heart rate, inflammation, intracranial hemorrhage, iridocyclitis, iritis, loss of consciousness, mass (pulmonary), musculoskeletal chest pain, myalgia, neuritis, non-small-cell lung carcinoma (adenocarcinoma), obstructive pulmonary disease, ocular hyperemia, pain, pain at injection site, prolonged partial thromboplastin time, pulmonary disease, pulmonary hemorrhage, retinal detachment, retinal hole without detachment, sclera disease, skin rash, sprue-like symptoms, subretinal neovascularization, syncope, tremor, urticaria, uveitis (intermediate)

Warnings/Precautions

Concerns related to adverse effects:

• Endophthalmitis/retinal detachment: Intravitreous injections are associated with endophthalmitis. Proper aseptic injection techniques should be used and patients should be instructed to report any signs of infection (eg, eye pain or redness, photophobia, blurred vision) immediately. Retinal detachment and iatrogenic traumatic cataract have been reported.
• Hypersensitivity: Rare hypersensitivity reactions (including anaphylaxis/anaphylactoid reactions and angioedema) have been associated with use, occurring within several hours of use; monitor closely. Equipment and appropriate personnel should be available for monitoring and treatment of anaphylaxis.
• Increased intraocular pressure: Intraocular pressure may increase within 30 minutes following intravitreal injection. Monitor intraocular pressure and optic nerve perfusion.
• Thromboembolic events: Thromboembolic events (eg, nonfatal stroke/MI, vascular death) have been reported following intravitreal administration of other VEGF inhibitors.

Other warnings/precautions:

• Concurrent administration in both eyes: Safety and efficacy for administration into both eyes concurrently have not been studied.

Monitoring Parameters

Optic nerve head perfusion (immediately after injection), intraocular pressure (within 30 minutes and during the week after injection); signs of infection/inflammation (for first week following injection) or hypersensitivity; retinal perfusion, endophthalmitis, visual acuity

Pregnancy

Pregnancy Risk Factor

B

Pregnancy Considerations

Pegaptanib is a vascular endothelial growth factor (VEGF) inhibitor; VEGF is required to achieve and maintain normal pregnancies. Reports of intravitreal VEGF inhibitor use in pregnancy are limited and information specific to use of pegaptanib has not been located (Peracha 2016). Based on studies in nonpregnant adults, VEGF inhibitors can alter systemic concentrations of VEGF and placental growth factor following intravitreal administration (Peracha 2016; Zehtner 2015). Until additional information is available, intravitreal use during the first trimester should be avoided and use later in pregnancy should be based on patient specific risks versus benefits (Peracha 2016; Polizzi 2015).

Evaluate pregnancy status prior to use in females of reproductive potential. Based on information from other VEGF inhibitors, women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for at least 3 months after the last intravitreal injection (Peracha 2016).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience floaters, dizziness, diarrhea, or nausea. Have patient report immediately to prescriber severe headache, vision changes, eye pain, severe eye irritation, difficult urination, dysuria, eyelid swelling, eye redness, eye discharge, bleeding in eye, or sensitivity to light (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.