Macugen (Pegaptanib Sodium) Drug Information: Description, User Reviews, Drug Side Effects, Interactions

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February 9, 2012

Macugen

Macular Degeneration »

Macular degeneration facts

The macula is in the center of the retina, the light-sensitive layer of tissue at the back of the eye. The macula is responsible for central vision (straight-ahead vision). Degeneration of the macula occurs most often after the age of 60 years and is termed age-related macular generation (AMD).
AMD is a painless condition.
There are two types of AMD: dry AMD and wet AMD.
Smoking, high blood pressure, obesity, a diet high in unsaturated fats and simple carbohydrates and lack of exercise all increase the risk of AMD.
Early symptoms of dry AMD include slightly blurred vision, the need for more light for reading, and difficulty recognizing faces until very close to the person. A symptom of more advanced dry AMD is the presence of a blurred spot in the center of vision. An early symptom of wet AMD is the wavy appearance of straight lines.
Dry AMD cannot be treated...

Read the Macular Degeneration article »

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Macugen

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MACUGEN®
(pegaptanib sodium) Injection

DRUG DESCRIPTION

Macugen (pegaptanib sodium injection) is a sterile, aqueous solution containing pegaptanib sodium for intravitreous injection. Macugen is supplied in a single-dose, pre-filled syringe and is formulated as a 3.47 mg/mL solution, measured as the free acid form of the oligonucleotide. The active ingredient is 0.3 mg of the free acid form of the oligonucleotide without polyethylene glycol, in a nominal volume of 90 μL. This dose is equivalent to 1.6 mg of pegaptanib sodium (pegylated oligonucleotide) or 0.32 mg when expressed as the sodium salt form of the oligonucleotide moiety. The product is a sterile, clear, preservative-free solution containing sodium chloride, monobasic sodium phosphate monohydrate, dibasic sodium phosphate heptahydrate, hydrochloric acid, and/or sodium hydroxide to adjust the pH and water for injection.

Pegaptanib sodium is a covalent conjugate of an oligonucleotide of twenty-eight nucleotides in length that terminates in a pentylamino linker, to which two 20-kilodalton monomethoxy polyethylene glycol (PEG) units are covalently attached via the two amino groups on a lysine residue.

Pegaptanib sodium is represented by the following structural formula:

MACUGEN® (pegaptanib sodium) Structural Formula Illustration

Where R is

MACUGEN® (pegaptanib sodium injection) Structural Formula Illustration

and n is approximately 450.

The chemical name for pegaptanib sodium is as follows: RNA, ((2'-deoxy-2'-fluoro)C-G_m-G_m-A-A-(2'-deoxy-2'-fluoro)U-(2'-deoxy-2'-fluoro)C-A_m-G_m-(2'-deoxy-2'-fluoro)U-G_m-A_m-A_m-(2'-deoxy-2'-fluoro)U-G_m-(2'-deoxy-2'-fluoro)C-(2'-deoxy-2'-fluoro)U-(2'-deoxy-2'fluoro)U-A_m-(2'-deoxy-2'-fluoro)U-A_m-(2'-deoxy-2'-fluoro)C-A_m-(2'-deoxy-2'-fluoro)U-(2'deoxy-2'-fluoro)C-(2'-deoxy-2'-fluoro)C-G_m-(3'→3')-dT), 5'-ester with α,α'-[4,12-dioxo-6[[[5-(phosphoonoxy)pentyl]amino] carbonyl]-3,13-dioxa-5,11-diaza-1,15pentadecanediyl]bis[ω-methoxypoly(oxy-1,2-ethanediyl)], sodium salt.

The molecular formula for pegaptanib sodium is C₂₉₄H₃₄₂F₁₃N₁₀₇Na₂₈O₁₈₈P₂₈[C₂H₄O]_n (where n is approximately 900) and the molecular weight is approximately 50 kilodaltons.

Macugen is formulated to have an osmolality of 280-360 mOsm/Kg, and a pH of 6–7.

What are the possible side effects of pegaptanib (Macugen)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects: