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What is leuprolide, and how does it work (mechanism of action)?
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.
What are the side effects of leuprolide?
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.
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What is the dosage for leuprolide?
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.
Which drugs or supplements interact with leuprolide?
No drug interaction studies have been done for
leuprolide.
Is leuprolide safe to take if I’m pregnant or breastfeeding?
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 else should I know about leuprolide?
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).