Pegaptanib Sodium

Pronunciation: peg-AP-ta-nib SO-dee-um
Class: Selective vascular endothelial growth factor (VEGF) antagonist

Trade Names

Macugen
- Injection 0.3 mg

Pharmacology

Antagonizes effects of VEGF, which are thought to contribute to the progression of neovascular form of age-related macular degeneration.

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Pharmacokinetics

Absorption

C max approximately 80 ng/mL and occurs within 1 to 4 days after 3 mg monocular dose (10 × recommended dose). AUC about 25 mcg•hr/mL.

Distribution

Radioactivity was mainly distributed in vitreous fluid, retina, and aqueous fluid 24 hr after intravitreous administration of a radiolabeled dose to both eyes of rabbits.

Metabolism

Following a 3 mg monocular dose (10 × recommended dose) plasma t ½ is about 10 days.

Indications and Usage

Treatment of neovascular (wet) age-related macular degeneration.

Contraindications

Ocular or periocular infections; standard considerations.

Dosage and Administration

Adults

Intravitreous injection 0.3 mg once every 6 wk into eye to be treated.

General Advice

  • For intravitreous injection into the eye only. Not for intradermal, subcutaneous, IM, IV, or intra-arterial administration.
  • Do not use contents in syringe if solution is cloudy, discolored, or contains particulate matter.
  • Administer adequate anesthesia and a broad-spectrum microbicide prior to injection.

Storage/Stability

Store prefilled syringes in refrigerator (36° to 46°F). Do not freeze or shake vigorously.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (10% to 40%); carotid artery occlusion, cerebrovascular accident, transient ischemic attack (1% to 5%).

CNS

Dizziness, headache (6% to 10%); vertigo (1% to 5%).

Dermatologic

Contact dermatitis (1% to 5%).

EENT

Anterior chamber inflammation, blurred vision, cataract, conjunctival hemorrhage, corneal edema, eye discharge, eye irritation, eye pain, increased IOP, ocular discomfort, punctuate keratitis, reduced visual acuity, visual disturbance, vitreous floaters, vitreous opacities (10% to 40%); blepharitis, conjunctivitis, photopsia, vitreous disorder (6% to 10%); allergic conjunctivitis, conjunctival edema, corneal abrasion, corneal deposits, corneal epithelium disorder, endophthalmitis, eye inflammation, eye swelling, eyelid irritation, hearing loss, meibomianitis, mydriasis, periorbital hematoma, retinal edema, vitreous hemorrhage (1% to 5%).

GI

Diarrhea, nausea (6% to 10%); dyspepsia, vomiting (1% to 5%).

Genitourinary

UTI (6% to 10%); urinary retention (1% to 5%).

Metabolic-Nutritional

Diabetes mellitus (1% to 5%).

Musculoskeletal

Arthritis, bone spur (1% to 5%).

Respiratory

Bronchitis (6% to 10%).

Miscellaneous

Chest pain, contusion, pleural effusion (1% to 5%); anaphylaxis/anaphylactoid reactions including angioedema (postmarketing).

Precautions

Monitor

Following injection, monitor patients for elevations in IOP and for endophthalmitis.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

IOP

Increases in IOP have been seen within 30 min of injection; therefore, monitor IOP and perfusion of the optic nerve head.

Patient Information

  • Review administration regimen and importance of returning every 6 wk for additional therapy.
  • Advise patient that medication will be prepared and administered by a health care provider in a health care setting.
  • Caution patient that there is a risk of developing endophthalmitis for several days following the injection and to immediately seek care from an ophthalmologist if any symptoms consistent with development of endophthalmitis occur (eg, eye becomes red, sensitive to light, or painful; vision changes).
  • Advise patient to contact health care provider if experiencing bothersome adverse reactions or any unusual problems.

Copyright © 2009 Wolters Kluwer Health.

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