Leuprolide is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH). It acts as a potent GnRH agonist. Following initial stimulation, continuous administration leads to a profound suppression of pituitary gonadotropins (LH and FSH), resulting in a marked decrease in estrogen and testosterone levels. This makes it a cornerstone therapy for hormone-dependent conditions like prostate cancer, endometriosis, and central precocious puberty.
Adult: 1 mg (0.5 ml) administered subcutaneously once daily. For prostate cancer/endometriosis/fibroids, treatment duration is typically limited (e.g., 3-6 months for fibroids) due to bone density concerns.
Note: For subcutaneous use only. Administer daily, rotating injection sites (abdomen, thigh, upper arm). The vial is for single use only; discard any unused portion. Allow the solution to reach room temperature before injection to minimize discomfort. Use aseptic technique.
Leuprolide is a potent agonist of the GnRH receptor in the anterior pituitary. Initial administration causes a transient surge in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a temporary increase in gonadal steroidogenesis (testosterone or estradiol). This is the 'flare' effect. With continuous daily administration, the pituitary GnRH receptors become desensitized and downregulated. This results in a profound and sustained suppression of LH and FSH secretion, leading to a hypogonadal state with markedly reduced levels of testosterone in men and estradiol in women.
Pregnancy: CONTRANDICATED - Pregnancy Category X. Can cause fetal harm based on mechanism and animal data. May cause fetal loss or teratogenicity. Exclude pregnancy before starting therapy. Women of childbearing potential must use non-hormonal contraception during and for some time after treatment.
Driving: May cause fatigue, dizziness, or visual disturbances. Patients should be cautioned about operating machinery or driving until they know how the drug affects them.
| Androgens (e.g., Testosterone) or Estrogens | Antagonizes the therapeutic effect of leuprolide. | Major |
| Drugs that prolong QT interval (e.g., Class IA/III antiarrhythmics, certain antipsychotics, antibiotics) | Additive risk of QT prolongation and cardiac arrhythmias. | Moderate |
| Corticosteroids (e.g., Prednisone) | May exacerbate bone mineral density loss. | Moderate |
| Other drugs metabolized by CYP450 enzymes | No significant interaction expected as leuprolide is not a CYP inhibitor/inducer. | None |
Same composition (Leuprolide (1mg/0.5ml)), different brands: