How does this medication work? What will it do for me?

Leuprolide is a medication that has been designed to mimic the actions of gonadotropin releasing hormone (GnRH or luteinizing hormone releasing hormone, LHRH), the hormone released from the hypothalamus gland in the brain. The hypothalamus uses GnRH to send messages to the pituitary gland in the brain, which then sends messages to the ovaries in women and the testicles in men, telling these organs to produce the sex hormones estrogen (in women) and testosterone (in men). Normally, GnRH comes from the hypothalamus in pulses, leading to the production of estrogen or testosterone. If GnRH came from the hypothalamus all of the time (rather than in "pulses"), it would have the opposite effect and "turn off" hormone production. This is what leuprolide does.

Leuprolide is used to treat advanced prostate cancer. For some cases of prostate cancer, testosterone causes the cancer to grow. This medication helps treat prostate cancer by reducing the amount of testosterone in the blood.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. As well, some forms of this medication may not be used for all of the conditions discussed here. If you have not discussed this with your doctor or are not sure why you are receiving this medication, speak to your doctor. Do not stop receiving this medication without consulting your doctor.

What form(s) does this medication come in?

7.5 mg vial
Eligard 7.5 mg (1-month) is supplied in two separate prefilled, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the Atrigel Delivery System, and the other contains leuprolide acetate. The Atrigel Delivery System is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable, 34% poly (DL-Lactide-co-glycolide; PLG) polymer formulation dissolved in a biocompatible solvent, 66% N-methyl-2-pyrrolidone (NMP). PLG is a copolymer with a 50:50 molar ratio of DL-lactide to glycolide containing carboxyl end groups. The second syringe contains 10.2 mg lyophilized leuprolide acetate and is designed to deliver 7.5 mg of leuprolide acetate at the time of subcutaneous injection. Eligard 7.5 mg (1-month) is available in a single use pouch packaging. The pouch packaging contains the two-syringe mixing system, a 20-gauge half-inch needle, and a silicone desiccant pouch to control moisture uptake.

22.5 mg vial
Eligard 22.5 mg (3-month) is supplied in two separate prefilled, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the Atrigel Delivery System, and the other contains leuprolide acetate. The Atrigel Delivery System is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable, 45% poly (DL-Lactide-co-glycolide; PLG) polymer formulation dissolved in a biocompatible solvent, 55% N-methyl-2-pyrrolidone (NMP). PLG is a copolymer with a 75:25 molar ratio of DL-lactide to glycolide with hexanediol. The second syringe contains 28.2 mg lyophylized leuprolide acetate and is designed to deliver 22.5 mg of leuprolide acetate at the time of SC injection. Eligard 22.5 mg (3-month) is available in a single use pouch or tray packaging. The pouch and the tray packaging contain the two-syringe mixing system, a 20-gauge half-inch needle, and a silicone desiccant pouch (two for the tray packaging) to control moisture uptake.

30 mg vial
Eligard 30 mg (4-month) is supplied in two separate prefilled, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the Atrigel Delivery System, and the other contains leuprolide acetate. The Atrigel Delivery System is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable, 45% poly (DL-Lactide-co-glycolide; PLG) polymer formulation dissolved in a biocompatible solvent, 55% N-methyl-2-pyrrolidone (NMP). PLG is a copolymer with a 75:25 molar ratio of DL-lactide to glycolide with hexanediol. The second syringe contains 35.8 mg lyophilized leuprolide acetate and is designed to deliver 30 mg of leuprolide acetate at the time of subcutaneous injection. Eligard 30 mg (4-month) is available in a single use pouch or tray packaging. The pouch and the tray packaging contain the two-syringe mixing system, a 20-gauge 5/8-inch needle, and a silicone desiccant pouch (two for the tray packaging) to control moisture uptake.

45 mg vial
Eligard 45 mg (6-month) is supplied in two separate prefilled, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the Atrigel Delivery System, and the other contains leuprolide acetate. The Atrigel Delivery System is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable, 50% poly (DL-Lactide-co-glycolide; PLG) polymer formulation dissolved in a biocompatible solvent, 50% N-methyl-2-pyrrolidone (NMP). PLG is a copolymer with a 85:15 molar ratio of DL-lactide to glycolide with hexanediol. The second syringe contains 58.2 mg lyophilized leuprolide acetate and is designed to deliver 45 mg of leuprolide acetate at the time of subcutaneous injection. Eligard 45 mg (6-month) is available in a single use tray packaging. The tray packaging contains the two-syringe mixing system, a 18-gauge 5/8-inch needle, and two silicone desiccant pouches to control moisture uptake.

How should I use this medication?

Leuprolide is given as an injection under the skin by your doctor. Depending on the dosage form used, it may be given once every 1, 3, 4, or 6 months.

Many things can affect the dose of a medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are receiving the medication without consulting your doctor.

It is very important to receive this medication exactly as recommended by your doctor. If you miss an appointment to receive leuprolide, contact your doctor as soon as possible to reschedule your appointment.

Leuprolide vials or kits should be stored in the refrigerator (between 2°C and 8°C) and protected from light. Leuprolide may be stored at room temperature in the original packaging for up to 8 weeks before it is used. Keep out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Leuprolide should not be given to anyone who:

  • is allergic to leuprolide or to any of the ingredients of this medication
  • is allergic to medications called GnRH agonists or LHRH agonists (e.g., buserelin, goserelin)
  • is breast-feeding
  • is pregnant or may become pregnant while receiving the medication

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent. The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • blurred vision
  • bone pain
  • constipation
  • decreased sex drive
  • decreased testicle size
  • difficulty getting or maintaining an erection
  • dizziness
  • headache
  • hot flashes (sudden sweating and feeling of warmth)
  • nausea or vomiting
  • sleeping problems
  • swelling and increased tenderness of breasts
  • swelling of feet or legs
  • weight gain

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • difficult or painful urination
  • heavy sweating
  • nervousness
  • severe hot flashes
  • severe swelling, itching, burning, or redness at the place of injection

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • breathing problems
  • changes in skin colour of face
  • chest pains
  • fainting
  • fast or irregular breathing
  • fast or irregular heartbeat
  • numbness or tingling of hands or feet
  • pain in groin or legs
  • puffiness or swelling of the eyelids or around the eyes
  • severe bone, muscle, or joint pain
  • shortness of breath
  • skin rash, hives, or itching
  • sudden, severe decrease in blood pressure and collapse
  • tightness in chest or wheezing

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

HEALTH CANADA ADVISORY

September 8, 2011

Health Canada has issued new restrictions concerning the use of Eligard® (leuprolide acetate). To read the full Health Canada Advisory, visit Health Canada's web site at www.hc-sc.gc.ca.

Medical conditions: People with urinary tract obstruction (a blockage in the urinary tract), reduced kidney or liver function, spinal cord compression, or cancer that has spread to the bones of the spine should discuss with their doctor how this medication may affect their medical condition, how their medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Men and the heart: There may be an increased risk of heart-related events (e.g., heart attacks, stroke, heart-related death) in men being treated for prostate cancer with GnRH medications. Before you start treatment, tell your doctor if you have diabetes, heart disease, had a previous heart attack or stroke, or have cardiovascular risk factors (e.g., high blood pressure, smoking, or cholesterol). If you have any of these conditions, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Osteoporosis: Leuprolide can cause the bones to lose thickness. People who are at risk for osteoporosis or who are taking other medications that tend to thin bones should be monitored by their doctor while taking this medication.

Starting treatment: During the first week of treatment with leuprolide, you may notice that your signs and symptoms temporarily get worse. This is due to a sudden increase in hormones that will normalize once the right dose for you has been found.

Pregnancy: Leuprolide should not be used during pregnancy. Leuprolide is not recommended for use by women.

Breast-feeding: It is not known if leuprolide passes into breast milk. Leuprolide is not recommended for use by women.

Children: The safety and effectiveness of using this medication have not been established for children under 12 years of age.

What other drugs could interact with this medication?

There may be an interaction between leuprolide and any of the following:

  • bupropion
  • medications that promote loss of bone density (e.g., prednisone)
  • selective serotonin reuptake inhibitors (SSRIs, e.g., citalopram, fluoxetine, paroxetine, sertraline)
  • testosterone and androgens

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.