Medications and Drugs

Pharmacy Author: Omudhome Ogbru, PharmD
Medical Editor: Jay Marks, MD

GENERIC NAME: leuprolide

BRAND NAME: Lupron

DRUG CLASS AND MECHANISM: Leuprolide is an injectable, man-made hormone that is used for treating prostate cancer, endometriosis, central precocious 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.

PRESCRIPTION: Yes.

GENERIC AVAILABLE: Yes.

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

STORAGE: Leuprolide should be stored at room temperature between 15-30 C (59-86 F).

PRESCRIBED FOR: Leuprolide is used for the treatment of advanced prostatic cancer, endometriosis, fibroids and central precocious puberty.

DOSING: 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, and the 30 mg dose every four months.

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

Fibroids are treated with either a single 11.5 mg dose of Lupron Depot or 3.75 mg doses given monthly.

The recommended starting dose of leuprolide for treating central precocious puberty is 50 mcg/kg/day. This dose can be increased by 10 mcg/kg/day depending on the response of the patient. Alternatively, Lupron Depot can be given. The dose of Lupron Depot is 0.3 mg/kg/week given as one injection. The dose can be increased by 3.75 mg every 4 weeks depending on the response of the patient.

DRUG INTERACTIONS: No drug interaction studies have been done for leuprolide.

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

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

SIDE EFFECTS: The most common side effects of leuprolide are aches and pain, headaches, hot flashes and irritation at the injection site. Leuprolide also may cause impotence, shrinking of the testes and breast enlargement in men. Depression, rare cases of suicidal behavior, low blood pressure, convulsions, joint pain and muscle aches have been reported in post-marketing surveillance.

Reference: FDA Prescribing Information

Last Editorial Review: 11/17/2003 9:15:40 AM

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