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- What is leuprolide, and how does it work (mechanism of action)?
- What brand names are available for leuprolide?
- Is leuprolide available as a generic drug?
- Do I need a prescription for leuprolide?
- What are the side effects of leuprolide?
- What is the dosage for leuprolide?
- Which drugs or supplements interact with leuprolide?
- Is leuprolide safe to take if I'm pregnant or breastfeeding?
- What else should I know about leuprolide?
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 are the side effects of leuprolide?
The most common side effects of leuprolide are:
- aches and pain,
- hot flashes,
- chest pain, and
- irritation at the injection site.
Other important side effects of leuprolide include:
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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.
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).
Reference: FDA Prescribing Information
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EndometriosisEndometriosis implants are most commonly found on the ovaries, the Fallopian tubes, outer surfaces of the uterus or intestines, and on the surface lining of the pelvic cavity. They also can be found in the vagina, cervix, and bladder. Endometriosis may not produce any symptoms, but when it does the most common symptom is pelvic pain that worsens just prior to menstruation and improves at the end of the menstrual period. Other symptoms of endometriosis include:
- Pain during sex
- Pain with pelvic examinations
- Cramping or pain during bowel movements or urination
Treatment of endometriosis can be with medication or surgery.
Endometriosis QuizEndometriosis is a common gynecological condition. Take this quiz to learn what happens when a woman has endometriosis as well as causes, treatments, and risks.
Premenstrual Dysphoric Disorder (PMDD)Premenstrual dysphoric disorder (PMDD) is considered a severe form of premenstrual syndrome (PMS). PMDD has also been referred to as late luteal phase dysphoric disorder. The cause of PMDD is unknown. Some of the common symptoms of PMDD (not an inclusive list) include:
- mood swings,
- breast tenderness,
- hot flashes
- and more.
Prostate CancerProstate cancer is the most common cancer in men after skin cancer. Risk factors include age, family history, ethnicity, and diet. Prostate cancer is diagnosed by digital rectal exam, prostate specific antigen (PSA) test, and prostate biopsy. Symptoms may include frequent need to urinate, incontinence, pain, blood in the urine, fatigue, and more. Prognosis and treatment depend on cancer staging. Watchful waiting, surgery, radiation, cryotherapy, and other management strategies are available. Research and clinical trials strive to find new and better treatments for prostate cancer.
PubertyThe time when boys and girls begin the process of sexual maturation is called puberty. During this time, both sexes undergo a series of biological changes that include a rapid increase in height, bone growth, weight increase, the growth of pubic hair, breast development and the onset of menstruation in girls, and testicle, penis, and muscle enlargement in boys.
TeenagersTeenagers recognize that they are developmentally between child and adult. Teen health prevention includes maintaining a healthy diet, exercising regularly, preventing injuries and screening annually for potential health conditions that could adversely affect teenage health.
Uterine FibroidsUterine fibroids are benign tumors that originate in the uterus and are usually round or semi-round in shape. The most common symptom of a uterine fibroid is abnormal vaginal bleeding. Other symptoms include pressure, pelvic pain, pressure on the bladder, or pain during a bowel movement. Treatment options vary from surgery to medication.
Benign uterine growths are tissue enlargements of the female womb (uterus). Three types of benign uterine growths are uterine fibroids, adenomyosis, and uterine polyps. Symptoms include:
- Abdominal pressure and pain
- Pelvic pain
- Pain during intercourse
- Pain during bowel movements
Diagnosis and treatment of benign uterine growths depends upon the type of growth.