Glerelin, containing the active ingredient Leuprolide, is a synthetic gonadotropin-releasing hormone (GnRH) agonist. It is used in various hormone-dependent conditions, particularly in the treatment of prostate cancer, breast cancer, endometriosis, and central precocious puberty.

Uses

• Prostate Cancer: Advanced and metastatic prostate cancer.

• Breast Cancer: Hormone-dependent breast cancer in premenopausal women.

• Endometriosis: Management of endometriosis symptoms and to reduce endometrial lesions.

• Central Precocious Puberty (CPP): Treatment of early-onset puberty in children.

Mechanism of Action

Leuprolide acts as a GnRH agonist. It initially stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a temporary increase in sex hormone levels. However, continued administration causes downregulation of GnRH receptors, resulting in decreased production of testosterone and estrogen.

Dosage and Administration

• Prostate Cancer: Typically administered as a depot injection (7.5 mg monthly or 22.5 mg every 3 months) based on clinical need.

• Endometriosis: 3.75 mg intramuscularly every month or 11.25 mg every 3 months.

• Central Precocious Puberty: Dosage depends on body weight and is typically 0.2 to 0.3 mg/kg subcutaneously daily or depot formulations monthly.

Administration should always be under the supervision of a healthcare professional.

Side Effects

Common side effects include:

• Hot flashes

• Injection site reactions

• Mood swings

• Decreased libido

Serious side effects:

• Bone density loss

• Cardiovascular issues

• Severe allergic reactions

Precautions

• Regular monitoring of hormone levels, bone density, and cardiovascular function is essential.

• Use with caution in patients with a history of cardiovascular disease.

• Women of childbearing potential should use nonhormonal contraception.

Onset and Duration of Action

• Onset: Initial flare effect within 1 week, followed by suppression in 2-4 weeks.

• Duration: Depends on the depot formulation used (1, 3, or 6 months).

Storage

Store in a refrigerator (2°C to 8°C). Protect from light and keep in original packaging until use.