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Leuprolide

(loo-proh-lide)

Trade/other name(s): Lupron, Lupron Depot, Eligard, leuprorelin

Why would this drug be used?

Leuprolide is used to treat advanced prostate cancer. It is also used to treat uterine fibroids, endometriosis, and other conditions.

How does this drug work?

Leuprolide is a member of the group of drugs known as hormones or hormone antagonists. It is a man-made version of the body’s luteinizing-hormone-releasing hormone (LHRH). This drug stops the release of testosterone from the testicles in men and the release of estrogen from the ovaries in women. This slows or stops the growth of cells (including cancer cells) that depend on these hormones. If the medicine is stopped, hormone levels are expected to return to normal.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any medical conditions such as kidney disease, liver disease (including hepatitis), congestive heart failure, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you have or have ever had diabetes, heart disease, high blood pressure, high cholesterol, heart attack, or stroke. Also tell your doctor if you have ever smoked. Your doctor may watch you more closely for heart and blood vessel problems while you take this drug.
  • If you have ever been diagnosed with heart problems, especially long QT syndrome, an abnormal heart rhythm, congestive heart failure, or if you have been told you have low blood levels of potassium, calcium, or magnesium (which can affect the heart). This drug can affect the rhythm of the heart, which might lead to irregular heartbeats and can even lead to death.
  • If you or others in your family have weakened bones (osteoporosis), if you have ever been a smoker or heavy user of alcohol, or if you have taken steroids or medicines to prevent seizures, which can cause bone loss. Leuprolide can speed up loss of bone strength, which can lead to bones breaking easily, even with only slight trauma. If you have any of these conditions, you may not be able to be treated with this drug. .
  • If you have trouble passing your urine due to enlarged prostate or other blockage.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug is not safe to take during pregnancy (see “Precautions”).
  • If you are breastfeeding. This drug could interfere with breastfeeding. It is also not known whether it passes into breast milk. If it does, it could harm the baby.
  • If you want to have children in the next few months or year. This drug can affect fertility while you are on it and for some time after.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

Because leuprolide can affect the rhythm of the heart, be sure your doctor is aware of any drugs you take that affect heart rhythm. Examples of these drugs include:

  • Amiodorone (Cordarone, Pacerone)
  • Disopyramide (Norpace)
  • Dofetilide (Tikosyn)
  • Flecainide (Rhythmol)
  • Ibutilide (Corvert)
  • Mexiletine (Mexitil)
  • Moricizine (Ethmozine)
  • Procainamide (Procan, Pronestyl)
  • Propafenone (Tambocor)
  • Quinidine (Quinidex, Cardioquin)
  • Tocainide (Tonocard)

Beta blocker drugs slow the heart rate and can worsen effects on the heart. This class includes drugs like acebutolol (Sectral), atenolol (Tenormin), bisoprolol (Zebeta), esmolol (Brevibloc), metoprolol (Lopressor, Lopressor LA, Toprol XL), nadolol (Corgard), propranolol (Inderal), sotalol (Betapace), and timolol (Blocadren).

Clonidine (Catapres), digoxin (Lanoxin, Cardoxin, Digitek), and the calcium channel blockers diltiazem (Cardizem) and verapamil (Covera, Calan, Verelan) can also slow the heart and might cause problems while you are on leuprolide.

These drugs affect the rhythm of the heart in the same way as leuprolide and so can also increase your risk of abnormal heart rhythm if you take them during the same times you are on leuprolide.

  • Anti-psychotic drugs such as thioridazine (Mellaril), haloperidol (Haldol), mesoridazine (Serentil)
  • Antidepressants such as venlafaxine (Effexor) and amitriptyline (Elavil)
  • Certain antibiotics (e.g., erythromycin, clarithromycin, levofloxacin, ofloxacin, moxifloxacin, sparfloxacin, pentamidine)
  • Nausea medicines such as ondansetron (Zofran), dolasetron (Anzemet), granisetron (Kytril), droperidol (Inapsine), promethazine (Phenergan), and chlorpromazine (Thorazine)

This is not a complete list. Other drugs that can slow the heart rate or prolong the QT interval of the heart can increase the increase the danger of an abnormal rhythm. Check with your doctor or pharmacist to find out if other drugs you’re taking have this effect.

Check with your doctor, nurse, or pharmacist about other medicines, vitamins, herbs, and supplements, and whether alcohol can cause problems with this medicine.

Interactions with foods

No serious interactions with food are known at this time. Check with your doctor, nurse, or pharmacist about whether foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Leuprolide is injected into a muscle (intramuscular injection) or under the skin (subcutaneous injection). Depending on the dose of the drug and what form is used, the injection can be given each month or every 3, 4, or 6 months. The actual amount given per month is the same for all patients.

Precautions

In men

Leuprolide may briefly increase testosterone levels when the drug is first started. This causes the symptoms of prostate cancer to get worse for about a week and is called a disease or tumor “flare”. To help prevent this, doctors can give drugs that block testosterone for the first week or so of treatment. These symptoms usually improve after a week or two, but sometimes extra treatment is needed:

  • The prostate gland may enlarge, and you might have blood in your urine, painful urination, or trouble passing urine. Call your doctor if you have these symptoms. If the flow of urine is blocked completely, this can lead to kidney failure.
  • If prostate cancer has spread to the bones, bone pain may worsen. Call your doctor or nurse right away if your pain medicine is not stopping the pain. They will help you get the right dose or drug for the increased pain.
  • If prostate cancer has spread to the bones of the spine, the flare can cause the cancer to press on the spinal cord and cause spinal cord compression. Early symptoms include numbness in the legs or feet, trouble urinating or moving your bowels, back pain, and weakness in the legs. If left untreated it can lead to paralysis (loss of movement). Call your doctor right away if you have any of these symptoms.
  • Tell your doctor right away if you have any of the above flare symptoms lasting longer than 2 weeks.

Your doctor will check your blood during treatment to see the drugs effect on your cancer and look for side effects. It’s important to keep all your appointments, even those just for blood tests.

This drug may raise your blood sugar (glucose) levels or even lead to diabetes. Tell your doctor if you have ever had diabetes or high blood sugar, or if you have symptoms that can be caused by high blood sugar, such as feeling thirsty all the time or having to urinate more often than normal. Your doctor may check your blood sugar levels while you are taking this drug.

Patients on triptorelin have an increased risk of heart attack and stroke. Call your doctor right away if you have pain in the chest, neck, pain, jaw or arm, shortness of breath, headache, numbness or weakness on one side of your body, or trouble talking,

Androgen deprivation therapy (such as leuprolide) can cause a change in heart rhythm called prolonged QT interval. Tell your doctor if you have ever been diagnosed with any type of heart disease, especially an abnormal heart rhythm or long QT syndrome. Your doctor may need to test your heart rhythm with an EKG and test your blood levels of certain minerals that could affect heart rhythm during treatment. Tell your doctor or nurse right away if you notice a fast or irregular heartbeat, very slow heartbeat, lightheadedness, dizziness, fainting, or shortness of breath to your doctor right away. Tell your doctor if you start to take or have any changes in heart or blood pressure medicines.

This drug can rarely cause a severe allergic reaction. Call your doctor right away if you develop skin welts (hives), itching, swelling in your face, mouth, or throat.

In women

Leuprolide could briefly increase estrogen levels when the drug is first started. This can cause breast tenderness, vaginal spotting, and worsening of cancer symptoms that usually get better without treatment after a week or two.

Menstrual periods usually stop while you are on this drug. If you keep having periods, there may be a problem, and so you should talk to your doctor.

Although menstrual periods usually stop, it does not mean you cannot get pregnant. Taking this drug at the time of conception or during pregnancy can increase the risk of miscarriage or other harm to the fetus. Women who are taking this drug should use effective birth control during treatment. Ask your doctor what kinds of birth control can be used with this medicine. If you get pregnant while taking this drug, tell your doctor right away so that the drug can be stopped.

By lowering estrogen levels, this drug can affect emotions and worsen problems with depression. Let your doctor know if you have a depressed mood, crying spells, trouble sleeping, loss of appetite, or suicidal thoughts.

This drug can rarely cause a severe allergic reaction. Call your doctor right away if you develop skin welts (hives), itching, swelling in your face, mouth, or throat.

Possible side effects

You will probably not have most of the following side effects, but if you do have any, talk to your doctor or nurse. They can help you understand the side effects and cope with them. This drug can have different side effects in men and women.

Common

  • Hot flashes and sweats
  • Headache (more common in women)
  • Testicles getting smaller (in men)
  • Menstrual periods stopping or becoming much lighter.* In most women, periods resume within a few months after the drug is stopped. (in women)
  • Depression or feeling emotional (in women)*
  • Vaginal dryness or irritation (in women)
  • Pain, including muscle and joint pain

Less common

  • “Flare” reaction at the start of treatment for prostate cancer (in men)*
  • Dizziness (in men)
  • Breast tenderness or swelling (in men)
  • Decreased sexual desire
  • Decreased sexual ability in men (impotence or erectile dysfunction)
  • Low energy (seen less often in women)
  • Nausea and vomiting (rarely seen in men)
  • Abnormal lab tests, including increased cholesterol or triglyceride levels and liver function tests
  • Bruising or irritation at the injection site
  • Problems passing urine, including feeling the urgent need to pass urine, burning when passing urine, and blood in the urine
  • Severe bone thinning or weakness (osteoporosis), which increases the risk of having a bone break

Rare

  • Swelling of the hands and feet
  • Reduction in breast size (in women)
  • Loss of appetite
  • High blood sugar or diabetes (in men)
  • Seizures (convulsions) (in men)
  • Serious liver injury
  • Kidney problems
  • Pressure or bleeding in the pituitary gland, causing vomiting, headache, changes in vision, confusion, collapse, or other serious symptoms (this can occur in people who had a tumor in the pituitary, but didn’t know it before treatment)
  • Problems with heart rhythm, which may be serious*
  • Blood vessel disease, which can cause heart attacks and strokes (in men)*
  • Birth defects and other fetal harm if used during pregnancy*
  • Allergic reaction*
  • Death due to diabetes, heart problems, stroke, or some other cause

*See “Precautions” section for more detailed information.

Other side effects not listed above can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 1985.

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.


Last Medical Review: 09/17/2014
Last Revised: 09/17/2014