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 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.

When given to boys or men, leuprolide reduces the amount of testosterone produced in the body. This medication is used to treat prostate cancer because prostate cancer cells need testosterone in order to grow and reproduce.

When given to girls or women, leuprolide reduces the amount of estrogen the body produces. It is used to treat endometriosis because reduced levels of estrogen help to relieve the symptoms of this condition.

This medication is also used to help slow down the development of the genital areas in boys (under the age of 9) and girls (under the age of 8) who are experiencing early puberty. As soon as the child stops using the medication, normal development is allowed to continue.

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 being given this medication, speak to your doctor. Do not stop using this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to use this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

5 mg vial
Each mL contain: leuprolide acetate 5 mg. Nonmedicinal ingredients: benzyl alcohol, sodium chloride, and sterile water for injection USP.

How should I use this medication?

Leuprolide is available as a daily injection (under the skin) or as a long-acting injection (into the muscle every 1, 3, or 4 months).

If you are giving yourself or your child daily injections, it is very important to follow the directions as printed on the package insert.

Be sure to check the solution for discoloration and particle matter before each use. Presterilized disposable syringes are supplied and the usual sites of injection are indicated in the package insert. To avoid damage to your skin and tissues, it is important to change the injection site on your body from time to time as recommended by your doctor.

The long-acting form of this medication (depot) is injected into your muscle by your doctor at the appropriate intervals. It is very important to receive this medication at the correct times. If you miss your appointment for an injection, make a new one as soon as possible.

It is important that this medication be administered exactly as prescribed by your doctor. If you are using the daily injections and miss a dose, administer it as soon as possible and continue with your regular schedule. If you are using the daily injections and miss a dose, administer it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not administer a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

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

Check the packaging instructions on whether to store this medication in the refrigerator or at room temperature, as different brands have different requirements. Once mixed, the suspension should be used immediately or discarded. Protect from freezing and 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 used by anyone who:

  • is sensitive or allergic to leuprolide acetate or to any of the ingredients of the medication
  • is breast-feeding
  • is pregnant
  • has undiagnosed abnormal vaginal bleeding

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.

  • headache
  • light, irregular vaginal bleeding
  • nausea or vomiting
  • stopping of menstrual periods (adult women)

Although most of these 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:

  • anxiety
  • blurred vision
  • burning, itching, redness, or swelling at site of injection
  • constipation
  • continuous vaginal bleeding (girls)
  • decreased testicle size (adult men)
  • deepening of voice (adult women)
  • depression
  • difficulty urinating
  • dizziness
  • erectile dysfunction or decreased libido (adults)
  • hot flashes
  • increased hair growth (adult women)
  • itchy skin rash
  • mood changes
  • nervousness
  • pelvic pain
  • severe bone pain
  • sleeping problems
  • swelling and increased tenderness of breasts
  • swelling of feet or legs
  • vaginal burning, dryness, itching, or discharge
  • weight gain

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

  • changes in skin colour of face
  • fainting
  • fast or irregular heartbeat
  • hives or itching
  • numbness or tingling of hands or feet
  • pain in groin or legs
  • puffiness or swelling of the eyelids or around the eyes
  • seizures
  • severe muscle or joint pain
  • shortness of breath or other breathing problems
  • 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.


September 8, 2011

Health Canada has issued new restrictions concerning the use of Lupron® (leuprolide acetate). To read the full Health Canada Advisory, visit Health Canada's web site at

Medical conditions: People with obstructive uropathy (difficulty urinating because of a block in the urinary tract), seizures, brain tumours, disorders of the blood vessels in the brain, or problems with the central nervous system (brain and spinal cord) 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 few weeks 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. A non-hormonal method of birth control (e.g., condom, diaphragm, IUD) should be used during treatment. If you become pregnant during treatment, notify your doctor as soon as possible.

Breast-feeding: It is not known if leuprolide passes into breast milk. Women should not breast-feed while receiving leuprolide treatment due to risk of harm to the infant.

What other drugs could interact with this medication?

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

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

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.