Supprelin LA

DRUG DESCRIPTION

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

Supprelin LA (histrelin acetate)   Structural Formula Illustration

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)

Histrelin Implant diagram - Illustration

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.

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,...

Read All Potential Side Effects and See Pictures of Supprelin LA

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...

Read All Potential Precautions of Supprelin LA


Supprelin LA Consumer (continued)

SIDE EFFECTS: Irritation at the implant site (such as bruising, pain, redness), mood swings, or headache may occur. In men using this medication for prostate cancer, hot flashes (flushing), increased sweating, night sweats, tiredness, swelling of the ankles/feet, or constipation may occur. In girls using this medication for early puberty, breast tenderness or abnormal vaginal bleeding may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Infrequently, breast tenderness/swelling may occur in men and boys as a result of lowered testosterone levels. Shrinking of the testicles and reduced sexual interest/ability may also occur in men. Talk to your doctor if these effects occur.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

If you are a man using this medication for prostate cancer, tell your doctor immediately if any of these unlikely but serious side effects occur: new/worsening bone pain, easily broken bones, increased thirst/urination.

Get medical help right away if any of these rare but serious side effects occur: chest discomfort/pain, irregular heartbeat, weakness on one side of the body, slurred speech.

Rarely, a very serious problem with the pituitary gland (pituitary apoplexy) has been reported with similar drugs, usually in the first 2 weeks after starting treatment. Seek immediate medical attention if any of these very serious side effects occur: sudden severe headache, sudden severe mental/mood changes (e.g., severe confusion, difficulty concentrating), vision changes, severe vomiting, fainting.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: 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 following risk factors for osteoporosis: long-term alcohol use, smoking, family history of osteoporosis and broken bones, use of certain medications (e.g., corticosteroids such as prednisone, certain anti-seizure drugs such as phenytoin).

This product is not approved for use in women. Histrelin must not be used during pregnancy. It may harm an unborn baby. Consult your doctor for details.


Supprelin LA Patient Information Including Side Effects

Brand Names: Supprelin LA, Vantas

Generic Name: histrelin (implant) (Pronunciation: his TREL in)

  • What is histrelin (Supprelin LA)?
  • What are the possible side effects of histrelin (Supprelin LA)?
  • What is the most important information I should know about histrelin (Supprelin LA)?
  • What should I discuss with my health care provider before I receive histrelin (Supprelin LA)?
  • How is histrelin given (Supprelin LA)?
  • What happens if I miss a dose (Supprelin LA)?
  • What happens if I overdose (Supprelin LA)?
  • What should I avoid after receiving a histrelin implant (Supprelin LA)?
  • What other drugs will affect histrelin (Supprelin LA)?
  • Where can I get more information?

What is histrelin (Supprelin LA)?

Histrelin is a man-made form of a hormone that regulates many processes in the body. Histrelin overstimulates the body's own production of certain hormones, which causes that production to shut down temporarily.

The Supprelin LA brand of histrelin is used to treat precocious puberty in both male and female children.

The Vantas brand of histrelin is used to treat symptoms of prostate cancer in men and should not be used in women or children. Histrelin treats only the symptoms of prostate cancer but does not treat the cancer itself. Use any other medications your doctor has prescribed to best treat your condition.

Histrelin may also be used for other purposes not listed in this medication guide.

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

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, easy bruising or bleeding;
  • feeling short of breath, even with mild exertion;
  • swelling in your hands or feet; or
  • nausea, vomiting, loss or appetite, or jaundice (yellowing of your skin or eyes).

Less serious side effects may include:

  • tired feeling;
  • weight gain or loss;
  • pain or swelling in your testicles;
  • impotence, loss of interest in sex, trouble having an orgasm;
  • breast swelling or tenderness;
  • night sweats, feeling hot or cold;
  • warmth, redness, or tingly feeling under your skin;
  • sleep problems (insomnia);
  • headache, dizziness, depressed mood;
  • stomach pain, constipation; or
  • joint or muscle pain.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about histrelin (Supprelin LA)?

You should not receive this medication if you are allergic to histrelin or other medications that affect gonadotropin hormones. The Supprelin LA brand of histrelin is used to treat precocious puberty in children. The Vantas brand of histrelin is used to treat symptoms of prostate cancer in men and should not be used in women or children.

Before you receive histrelin, tell your doctor if you have painful or difficult urination, osteoporosis, or a condition affecting your spine.

Histrelin can cause a miscarriage or birth defects. Do not use if you are pregnant. Use effective birth control, and tell your doctor if you become pregnant during treatment.

You may have a temporary increase in symptoms of your condition for a week or so after you have received the histrelin implant. Call your doctor if any of these symptoms become severe.

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, fast or pounding heartbeats, pale skin, easy bruising or bleeding, feeling short of breath, swelling in your hands or feet, or jaundice (yellowing of your skin or eyes).

To be sure this medication is helping your condition, your blood will need to be tested often. Do not miss any scheduled appointments.

A histrelin implant is usually left in place for 12 months and then removed. Your doctor will determine at that time whether you need to receive another implant for treatment of your symptoms.

If you are using histrelin to treat prostate cancer, use any other medications your doctor has prescribed to best treat your condition. Histrelin treats only the symptoms of prostate cancer but does not treat the cancer itself.

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