Pegaptanib Sodium

Name: Pegaptanib Sodium

Indications

Macugen is indicated for the treatment of neovascular (wet) age-related macular degeneration.

What is pegaptanib ophthalmic (macugen)?

Pegaptanib is made from a human antibody fragment. It works by keeping new blood vessels from forming under the retina (a sensory membrane that lines the inside of the eye). In people with a certain type of eye disease, new blood vessels grow under the retina where they leak blood and fluid. This is known as the "wet form" of macular degeneration.

Pegaptanib ophthalmic (for the eyes) is used to treat wet age-related macular degeneration.

Pegaptanib ophthalmic may also be used for purposes not listed in this medication guide.

What is the most important information i should know about pegaptanib ophthalmic (macugen)?

You should not receive pegaptanib if you are allergic to it, or if you have cataracts or glaucoma, or any type of bacterial, fungal, or viral infection in or around your eyes.

Call your doctor at once if you have eye pain or redness, swelling or puffiness around your eyes, or sudden vision problems at any time during treatment.

What should i avoid while taking pegaptanib ophthalmic (macugen)?

This medication may cause blurred vision. Be careful if you drive or do anything that requires you to be able to see clearly.

Introduction

Polyethylene glycol (PEG)-conjugated, modified synthetic RNA oligonucleotide and aptamer; selective vascular endothelial growth factor (VEGF) antagonist.1 3 13 14 15 16

Interactions for Pegaptanib Sodium

No formal drug interaction studies to date.1

Metabolized by nucleases; generally not affected by CYP isoenzymes.1

Photodynamic Therapy with Verteporfin

No apparent difference in the pharmacokinetic profile of pegaptanib involving patients treated with pegaptanib alone or in combination with photodynamic therapy and verteporfin.1 9 14 No adverse effects attributed directly to concomitant use of pegaptanib with verteporfin.2 4

Pegaptanib Sodium Pharmacokinetics

Absorption

Bioavailability

Slowly absorbed into systemic circulation from the eye with mean peak plasma concentration usually attained within 1–4 days.1

Distribution

Extent

Distributed into vitreous fluid, retina, aqueous fluid, and kidneys.1

Crosses the placenta in mice; not known whether crosses the placenta in humans.1

Not known whether distributed into human milk.1

Elimination

Metabolism

Appears to be metabolized by endo- and exonucleases.1

Elimination Route

In animals, excreted principally in urine as unchanged drug and metabolites.1

Half-life

Average: 10 days.1

Special Populations

No dosage adjustment required in those with renal impairment.1

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Pegaptanib Sodium

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Injection, for intravitreal use only

0.3 mg/0.09 mL (of the free acid of the oligonucleotide without polyethylene glycol)

Macugen (preservative-free; available as single-dose prefilled syringe with needle)

Eyetech (also promoted by Pfizer)

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