For palliative treatment of prostate cancer.

Trade names Lupron, Eligard, Lucrin

A luteinizing hormone release agonist, LH-RH.

Routes of administration implant, subcutaneous, intramuscular

Drug class GnRH analogue; GnRH agonist; Antigonadotropin

pregnancy category D.

Elimination half-life 3 hours

Excretion Kidney

Suppresses testosterone.

Leuprorelin, also known as leuprolide, is a manufactured version of a hormone used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, as part of transgender hormone therapy, for early puberty, or to perform chemical castration of violent sex offenders.

It is given by injection into a muscle or under the skin.

Leuprorelin is in the gonadotropin-releasing hormone (GnRH) analogue family of medications.

It works by decreasing gonadotropin and therefore decreasing testosterone and estradiol.

Common side effects include hot flashes, unstable mood, trouble sleeping, headaches, and pain at the site of injection.

Other side effects may include high blood sugar, allergic reactions, and problems with the pituitary gland.

Use during pregnancy may harm the fetus.

A transient increase in testosterone will occur in the first few weeks of therapy.

May cause a temporary increase in urinary symptoms and pain.

One, 3 and 4 month doses are available.

Leuprorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer and breast cancer. 

It may also be used for estrogen-dependent conditions such as endometriosis or uterine fibroids.

It may be used for precocious puberty in both males and females.

It can prevent premature ovulation in cycles of controlled ovarian stimulation for in vitro fertilization (IVF). 

It may be used to reduce the risk of premature ovarian failure in women receiving cyclophosphamide for chemotherapy.

Along with triptorelin and goserelin, it has been used to delay puberty in transgender youth until they are old enough to begin hormone replacement therapy.

It also sometimes used as alternatives to antiandrogens like spironolactone and cyproterone acetate for suppressing testosterone production in transgender women, and for suppressing estrogen production in transgender men.

It is considered a possible treatment for paraphilias.

Common side effects of leuprorelin injection include redness/burning/stinging/pain/bruising at the injection site, hot flashes, increased sweating, night sweats, tiredness, headache, upset stomach, nausea, diarrhea, impotence, testicular shrinkage, constipation, stomach pain, breast swelling or tenderness, acne, joint/muscle aches or pain, insomnia, reduced sexual interest, vaginal discomfort/dryness/itching/discharge, vaginal bleeding, swelling of the ankles/feet, increased urination at night, dizziness, breakthrough bleeding in a female child during the first two months of leuprorelin treatment, weakness, chills, clammy skin, skin redness, itching, or scaling, testicle pain, impotence, depression, or memory problems.

The rates of gynecomastia with leuprorelin have been found to range from 3 to 16%.

Leuprorelin is a gonadotropin-releasing hormone (GnRH) analogue acting as an agonist at pituitary GnRH receptors. 

Agonism of GnRH receptors initially results in the stimulation of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion by the anterior pituitary ultimately leading to increased serum estradiol and testosterone levels

This occurs by the normal physiology of the hypothalamic–pituitary–gonadal axis (HPG axis).

The HPG axis is incumbent upon pulsatile hypothalamic GnRH secretion, pituitary GnRH receptors become desensitised after several weeks of continuous leuprorelin therapy. 

The protracted downregulation of GnRH receptor activity is the targeted objective of leuprorelin therapy and ultimately results in decreased LH and FSH secretion, leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels regardless of sex.

The initial increase in testosterone levels associated with the initiation of leuprorelin therapy for prostate cancer is counterproductive to treatment goals. 

This effect is avoided with concurrent utilization of 5α-reductase inhibitors, such as finasteride, or flutamide which function to block the downstream effects of testosterone.

Leuprorelin is available in the following forms:

Short-acting daily intramuscular injection 

Long-acting depot intramuscular injection 

Long-acting depot subcutaneous injection 

Long-acting subcutaneous injection

Long-acting subcutaneous implant 

Long-acting leuprolide mesylate (Camcevi) for the treatment of advanced prostate cancer.

Leuprolide acetate and norethindrone acetate combination pack.




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