Supprelin LA (Histrelin Acetate Subcutaneous Implant) Drug Information: Description, User Reviews, Drug Side Effects, Interactions

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May 26, 2012

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Supprelin LA User Reviews >>

Supprelin LA

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SUPPRELIN LA
(histrelin acetate)

DRUG DESCRIPTION

SUPPRELIN LA is a sterile, non-biodegradable, diffusion-controlled, MedLaunch™ polymer reservoir containing histrelin acetate, a synthetic nonapeptide analog of the naturally occurring gonadotropin releasing hormone (GnRH) possessing a greater potency than the natural sequence hormone. SUPPRELIN LA is designed to deliver approximately 65 mcg histrelin acetate per day over 12 months.

The SUPPRELIN LA implant looks like a small thin flexible tube and consists of a 50-mg histrelin acetate drug core inside a 3.5 cm by 3 mm, cylindrical, MedLaunch™ polymer reservoir (Figure 1).

Figure 1: SUPPRELIN LA Implant Diagram (not to scale)

The chemical name of histrelin acetate is: L-Pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N-benzylD-histidyl-L-leucyl-L-arginyl-L-proline N-ethylamide, acetate salt.

The molecular formula for histrelin acetate is C₆₆H₈₆N₁₈O₁₂ x 2 CH₃COOH and its molecular weight is 1443.70 (or 1323.52 as free base). Histrelin is also chemically described as 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-Lseryl-L-tyrosyl-Nt-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide diacetate. The chemical structure of the free base (histrelin) is represented below in Figure 2.

Figure 2: Structure of Histrelin

SUPPRELIN LA (histrelin acetate) Structural Formula Illustration

The drug core also contains the inactive ingredient stearic acid NF. The MedLaunch™ polymer reservoir is a hydrophilic cartridge composed of 2-hydroxyethyl methacrylate, 2-hydroxypropyl methacrylate, trimethylolpropane trimethacrylate, benzoin methyl ether, Perkadox-16, and Triton X-100. Each implant is packaged hydrated in a glass vial containing 2 mL of sterile 1.8% sodium chloride solution, so that it is primed for immediate release of the drug upon insertion.

A single use, sterile, Insertion Tool is provided along with the implant that can be used for the placement of the SUPPRELIN LA implant into the subcutaneous tissue of the inner aspect of the upper arm. The Insertion Tool is enclosed in a sterile bag and is provided separately from the implant in the Implantation Kit [see Recommended Procedure for Implant Insertion and Removal].

What are the possible side effects of histrelin (Supprelin LA, Vantas)?

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 a serious side effect such as:

severe numbness or tingling in your legs or feet;
muscle weakness, problems with balance or coordination;
loss of bladder or bowel control;
urinating more or less than usual, or not at all;
fast or pounding heartbeats;
pale skin,...

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What are the precautions when taking histrelin acetate subcutaneous implant (Supprelin LA)?

Before using histrelin, tell your doctor or pharmacist if you are allergic to it; or to similar drugs (e.g., leuprolide); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart disease (such as heart attack), stroke, family history of sudden cardiac death.

If you are a man using this medication for prostate cancer, histrelin may weaken your bones and increase your risk for bone loss (osteoporosis) if used for a long time. Before using this medication, tell your doctor or pharmacist if you have osteoporosis or if you have any of the...

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Last reviewed on RxList: 4/17/2012
This monograph has been modified to include the generic and brand name in many instances.