leuprolide (Lupron, Eligard)

Leuprolide is an injectable, man-made hormone that is used for treating prostate cancer, endometriosis, central precocious puberty (early onset of puberty), and fibroids. It is similar to but stronger than human gonadotropin releasing hormone (GnRH).

GnRH is made in the hypothalamus (a part of the brain) and travels to the pituitary gland where it causes the production of luteinizing hormone (LH) and follicle stimulating hormone (FSH). LH and FSH are released by the pituitary into the blood and stimulate the production of testosterone by the testes in men and estrogens by the ovaries in women. The release of GnRH, LH and FSH is governed by negative feedback which means that when there is too much testosterone or estrogen being produced, the body sends a signal to the pituitary gland to reduce the production of GnRH which, in turn reduces the production of LH and FSH. This results in reduced production of testosterone and estrogen. When given continuously, leuprolide initially increases the production of LH and FSH as well as testosterone and estrogen; however, after a few weeks of continuous leuprolide, the levels of LH and FSH drop because the pituitary gland stops responding to GnRH and leuprolide. This leads to a decrease in the production of estrogen and testosterone.

Testosterone promotes the growth of prostate cancer. Therefore, leuprolide is used in treating prostate cancer to slow the growth of the cancer. In children with central precocious puberty (puberty caused at an early age because of too much LH and FSH) leuprolide, by suppressing LH and FSH, reduces the levels of estrogen and testosterone and allows for more normal timing of puberty. Estrogens promote the growth of fibroids (benign tumors of the uterus) and areas of endometriosis (abnormal uterine tissue that exists outside of the uterus). Leuprolide is used to reduce the production of estrogen and treat both fibroids and endometriosis. The FDA approved leuprolide in April 1985.

What brand names are available for leuprolide?

Lupron, Lupron Depot, Lupron Depot-Ped, Eligard

Is leuprolide available as a generic drug?

Yes.

Do I need a prescription for leuprolide?

Yes.

The most common side effects of leuprolide are:

• aches and pain,
• fatigue,
• edema,
• headaches,
• hot flashes,
• chest pain, and
• irritation at the injection site.

Other important side effects of leuprolide include:

• impotence,
• shrinking of the testes, and
• breast enlargement in men (gynecomastia).

Depression, rare cases of suicidal behavior, low blood pressure, convulsions, joint pain and muscle aches have been reported in post-marketing surveillance.

Leuprolide is injected under the skin (subcutaneously). Lupron Depot is injected into muscle (intramuscularly).

For prostate cancer, leuprolide can be given daily or Lupron Depot can be given monthly or at 3 to 4 month intervals. The daily dose of leuprolide is 1 mg. The 3.5 and 7.5 mg doses of Lupron Depot are injected monthly, the 11.25 and 22.5 mg doses every three months, the 30 mg dose every four months, and the 45 mg dose every 6 months.

For endometriosis, the recommended dose of Lupron Depot is 3.75 mg monthly or 11.5 mg every 3 months. The recommended duration of treatment is 6 months.

No drug interaction studies have been done for leuprolide.

Leuprolide should not be administered to pregnant women because there is a high chance of harm to the fetus.

The effects of leuprolide on the infant have not been studied in women who are breastfeeding.

What preparations of leuprolide are available?

Leuprolide injection: 5 mg/ml and 3.75 mg . Lupron Depot microspheres for injection: 3.75, 7.5, 15, 11.25, 22.5, 30, and 45 mg/vial.

How should I keep leuprolide stored?

Leuprolide should be stored at room temperature, between 15 C to 30 C (59 F to 86 F).