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All about: Leuprolide acetate

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Generic name: Leuprolide acetate
Brand names: Lupron Depot

Why is Leuprolide acetate prescribed?

Lupron is a synthetic version of the naturally occurring gonadotropin releasing hormone (GnRH). Lupron suppresses shedding of the endometrium (lining of the uterus) during menstruation and is used to treat endometriosis, a condition in which cells from the endometrium grow outside of the uterus. Endometriosis causes painful growths to form around the outside of the uterus, fallopian tubes, and ovaries.

Two forms of Lupron--Lupron Depot 3.75 and Lupron Depot 11.25--are prescribed to relieve the pain of endometriosis and shrink the growths. (The hormonal medication norethindrone acetate is often added to the regimen.) Three other forms of Lupron--Lupron Depot 7.5, Lupron Depot 22.5, and Lupron Depot 30--are prescribed to relieve the symptoms of advanced prostate cancer.

The first two forms of Lupron are also used before surgery, along with iron, to treat anemia caused by fibroids (tumors) in the uterus when iron alone is not effective. Some doctors also prescribe Lupron for infertility and for early puberty.

Most important fact about Leuprolide acetate

Lupron lowers estrogen levels, which can lead to a decrease in bone density in both men and women. Decreased bone density could increase your risk of osteoporosis, or brittle bone disease, later in life. Consequently, the drug is not usually given for longer than 6 months at a time.

How should you take Leuprolide acetate?

Lupron must be given under the supervision of a physician. It is given by injection once a month, every 3 months, or every 4 months, depending on the form you've been prescribed.

--If you miss a dose...

Women who miss their monthly injections of Lupron Depot 3.75 may experience resumption of menstrual bleeding.

--Storage instructions...

Lupron does not need to be refrigerated. Protect from freezing.

What side effects may occur?

Side effects cannot be anticipated. If any develop or change in intensity, inform your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking Lupron.


Lupron stops menstruation and reduces estrogen levels in your body. Reduced estrogen may cause side effects such as acne, decreased sex drive, headaches, hot flashes, mood swings, muscle pain, a reduction in breast size, and vaginal inflammation and dryness. Your menstrual periods and estrogen levels will return to normal when you stop taking Lupron.

  • More common side effects may include:
    Anxiety, appetite changes, breast tenderness or pain, depression, fluid retention, development of male characteristics, dizziness, general pain, inflammation of the vagina (vaginitis), insomnia or other sleep disorders, joint pain, memory problems, nausea and vomiting, nervousness, skin reactions, stomach or intestinal disorders, unusual burning or prickling sensation of the skin, weakness, weight gain or loss
  • Additional side effects you may experience if you are taking Lupron for anemia include:
    Body odor, flu symptoms, nail problems, nasal irritation, pinkeye, taste disorders


Lupron increases male hormone levels.

  • More common side effects may include:
    Breathing problems, dizziness/vertigo, fluid retention, headache, hot flashes, impotence, sleep disorders, joint disorders, nausea, pain, skin reaction, stomach and intestinal disorder, sweats, testicle shrinking, urinary problems, vomiting, weakness

A few other side effects are possible with the Lupron Depot 30 formulation.

Why should Leuprolide acetate not be prescribed?

Lupron should not be used if you are known to be hypersensitive to it, or to any drug containing a form of GnRH.

If you have undiagnosed abnormal vaginal bleeding, you should not take Lupron.

If you are pregnant or might become pregnant, you should not take Lupron. The drug could harm a developing baby. Also avoid Lupron if you are breastfeeding.

Lupron Depot 30 is for use by men only.

Special warnings about Leuprolide acetate


Your doctor will want to make sure you are not pregnant before giving you Lupron. If you become pregnant while taking the drug, stop taking it and notify your doctor immediately.

Even though your menstrual periods stop while you are taking Lupron, there is still a chance you could become pregnant and you should take birth control measures. Use condoms or diaphragms rather than hormonal methods such as birth control pills or Norplant, because hormones will interfere with Lupron treatment.

Notify your doctor if you continue to have a menstrual period. If you miss successive doses of Lupron you may have some bleeding.

Treatment with Lupron can cause an irreversible weakening of the bones (osteoporosis). No more than one course of therapy is recommended for women who develop this problem or who are at risk of bone loss. Adding norethindrone to the treatment regimen reduces bone loss, but increases the risk of other side effects such as clotting problems and fluid retention. If norethindrone is part of your regimen, your doctor will be on the alert for inflamed veins (thrombophlebitis) and other signs of clotting disorders. Norethindrone should be used with caution if you have heart-disease risk factors such as high cholesterol or cigarette smoking. The doctor should also monitor you carefully if you have kidney disease, asthma, epilepsy, or other conditions that might be aggravated by fluid retention. Norethindrone may cause depression, and should be discontinued if severe depression occurs. The drug should also be discontinued if you develop vision problems or migraine headaches.

Lupron therapy for endometriosis has not been studied in women under 18 years of age, nor is the product recommended for women over 65.


Men taking Lupron for prostate cancer may find that their symptoms get worse, or that new symptoms appear, during the first few weeks of treatment. If this happens, let your doctor know immediately. Bone pain may increase temporarily, and in rare cases a blockage in the urinary tract or pressure on the spinal cord may appear. If you already have problems in the spine or urinary tract, the doctor will start Lupron therapy with caution.

Possible food and drug interactions when taking Leuprolide acetate

If Lupron is taken with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with your doctor before combining Lupron with any type of hormones, such as birth control pills.

No interactions are likely in men.

Special information if you are pregnant or breastfeeding

Do not take Lupron if you are pregnant or breastfeeding.

Recommended dosage


For endometriosis, a single intramuscular injection is given once a month. Norethindrone may be included in the treatment regimen. Treatment lasts 6 months. One additional 6-month course of treatment may be given, provided norethindrone is included in the second regimen.

For anemia due to uterine fibroids, the same dose is given once a month for up to 3 months.


For prostate cancer, a single injection is given once a month.


For endometriosis, a single injection is given every 3 months. Norethindrone may be included in the treatment regimen. Treatment lasts 6 months. One additional 6-month course of treatment may be given, provided norethindrone is included in the second regimen.

For anemia due to fibroids, the usual treatment is a single injection.


For prostate cancer, a single injection is given every 3 months.


For prostate cancer, a single injection is given every 4 months.


An overdose is extremely unlikely. However, if you suspect overdosage, call your doctor immediately.

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