Generic
Leuprorelin Acetate
2 brands available in the market
At a glance
Leuprorelin Acetate is used for the treatment of prostate cancer, endometriosis, uterine fibroids, and breast cancer. It is a GnRH agonist that inhibits sex hormone production.
Description
Leuprorelin Acetate is a GnRH agonist that acts as a potent inhibitor of gonadotropin secretion when given on a continuous basis. Following initial stimulation, continuous administration leads to decreased LH and FSH levels and sex steroids (testosterone in males, estrogens in females) to castrate or postmenopausal levels. These hormonal changes occur within one month of initiating drug therapy at recommended doses.
Indications
- Advanced prostate cancer (palliative treatment)
- Endometriosis (up to 6 months)
- Uterine fibroids (leiomyoma uteri) - up to 6 months
- Breast cancer in pre- and peri-menopausal women
Therapeutic class
Uterine Drugs, Gonadotropin Inhibitors
Pharmacological class
GnRH Agonist
Pharmacology
Leuprorelin Acetate causes down-regulation of GnRH receptors through continuous stimulation, reducing pituitary gonadotropin secretion and inhibiting sex hormone (testosterone and estrogen) production.
Mechanism of action
Inhibits sex hormone production to reduce growth of hormone-dependent tumors.
Dosage
Prostate Cancer/Endometriosis/Uterine Fibroids/Breast Cancer:
- 11.25 mg SC or IM once every 3 months
- Endometriosis: 6 months treatment; start on first day of menstrual cycle (after ruling out pregnancy)
- Uterine fibroids: Up to 6 months treatment; preoperative therapy or symptomatic relief
Administration
- Administer under physician supervision
- Use immediately after reconstitution
- SC or IM injection; vary injection sites periodically
Missed dose
Not generally applicable (monthly/quarterly injection); consult doctor if needed.
Side effects
Common Side Effects (Men):
- Prostate tumor flare, aggravation of prostate cancer
- Decreased/increased libido, headache, muscle weakness
- Hot flushes, hypotension
- Dry skin, hyperhydrosis, rash
- Gynecomastia, erectile dysfunction
- Decreased bone density
(Women): Hot flushes, headache, vaginal bleeding, menstrual disorders, breast changes, decreased bone density
Precautions & warnings
- Initial clinical symptoms may worsen (tumor flare)
- Bone mineral density loss (hypoestrogenic state in women; long-term use in men)
- Convulsions reported (including female and pediatric populations)
- Contraindicated during pregnancy
Contraindications
- Hypersensitivity to leuprorelin acetate, similar nonapeptides, or excipients
- Not suitable for patients following orchiectomy
- Undiagnosed abnormal vaginal bleeding
- Pregnancy
Drug interactions
No pharmacokinetic-based drug interaction studies have been conducted.
Food interactions
Caution is advised when consuming alcohol with Leuprorelin acetate; consult your doctor.
Use in pregnancy
Use in Pregnancy: Leuprorelin acetate is contraindicated during pregnancy; may cause fetal harm.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: It is not known whether leuprorelin acetate is excreted in human milk; should not be used by nursing mothers.
Pediatric use
Safety and efficacy not established in children.
Geriatric use
Pharmacokinetics not determined in hepatic and renal impairment.
Renal / hepatic impairment
Pharmacokinetics not determined in hepatic and renal impairment.
Overdose effects
No specific overdose information available; symptomatic and supportive measures should be employed.
Storage conditions
Do not store above 25°C; use immediately after reconstitution; protect from freezing.
Chemical structure
Leuprorelin Acetate