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Supprelin LA
(histrelin acetate) Subcutaneous Implant
Supprelin LA (histrelin acetate) subcutaneous implant contains a synthetic nonapeptide analog of the naturally occurring gonadotropin releasing hormone (GnRH) that possesses a greater potency than the natural sequence hormone. The chemical name of histrelin acetate is:
L-Pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N-benzyl-D-histidyl-L-leucyl-L-arginyl-L-proline Nethylamide, 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 1.
Figure 1. Structure of histrelin
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The Supprelin LA (histrelin acetate subcutaneous implant) implant looks like a small thin flexible tube. The sterile implant consists of a 50-mg histrelin acetate drug core inside a non-biodegradable, 3.5 cm by 3 mm, cylindrical hydrogel reservoir (Figure 2).
Figure 2. Histrelin Implant diagram (not to scale)
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The drug core also contains the inactive ingredient stearic acid NF. The hydrogel reservoir is a cartridge composed of 2-hydroxyethyl methacrylate, 2-hydroxypropyl methacrylate, trimethylolpropane trimethacrylate, benzoin methyl ether, Perkadox-16, and Triton X-100. Each hydrated implant is packaged in a glass vial containing 2 mL of 1.8% sodium chloride, sterile solution, so that it is primed for immediate release of the drug upon insertion. The 3.5 mL Type I clear glass vial with the implant is closed with a pre-treated grey Teflon coated stopper and sealed with an aluminum crimp seal.
A single use sterile insertion tool (Trocar) is to be used with Supprelin LA (histrelin acetate subcutaneous implant) . The insertion tool is enclosed in a sterile bag as part of the implantation kit.
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:
Read All Potential Side Effects and See Pictures of 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...
Last reviewed on RxList: 8/5/2008
This monograph has been modified to include the generic and brand name in many instances.
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