Generic
Leuprolide acetate
2 brands available in the market
At a glance
Leuprolide acetate is used in the treatment of prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. It is a GnRH agonist that reduces sex hormone (testosterone and estrogen) production.
Description
Leuprolide acetate is a gonadotropin-releasing hormone (GnRH) agonist. Following initial stimulation, continuous administration leads to down-regulation of GnRH receptors and subsequently reduces pituitary gonadotropin secretion. Reduced gonadotropin levels inhibit sex hormone (testosterone and estrogen) production. Within 2-4 weeks after treatment initiation, testosterone levels in males may be reduced to below castrate threshold.
Indications
- Advanced prostate cancer (palliative treatment)
- Endometriosis (up to 6 months treatment)
- Uterine fibroids (leiomyoma uteri) - up to 6 months treatment
- Central precocious puberty (girls <8 years, boys <9 years)
- Breast cancer in pre- and peri-menopausal women
Therapeutic class
Uterine Drugs, Gonadotropin Inhibitors
Pharmacological class
GnRH Agonist
Pharmacology
Leuprolide 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: 1 mg (0.2 mL) SC daily OR 3.75 mg IM monthly OR 11.25 mg IM every 3 months
Endometriosis: 3.75 mg IM monthly (up to 6 months) OR 11.25 mg IM every 3 months (2 doses, total 6 months)
Uterine Fibroids: 3.75 mg IM monthly (up to 3 months) OR 11.25 mg IM once
Precocious Puberty (Children): 50 mcg/kg/day SC; may titrate up by 10 mcg/kg/day; <2 years: Safety not established
Administration
- Your doctor or nurse will give this medicine; do not self-administer
- Subcutaneous (SC) or intramuscular (IM) injection
- Injection sites should be varied periodically
Missed dose
If you miss a dose, please consult your doctor.
Side effects
Common Side Effects:
- Decreased libido
- Testicular atrophy
- Increased sweating
- Fatigue
- Muscle weakness
- Erectile dysfunction
- Bone pain
- Injection site reaction
- Hot flashes
Precautions & warnings
- Caution when driving or operating machinery (may cause drowsiness, dizziness, or visual disturbances)
- Long-term use may lead to bone loss and fracture risk
- Take vitamin D and calcium supplements
- Use non-hormonal contraception to prevent pregnancy during treatment
- Menstrual periods stop during treatment and resume 7-12 weeks after final injection
Contraindications
- Pregnancy and lactation
- Hypersensitivity to GnRH, GnRH agonist analogs, or product excipients
- Undiagnosed abnormal vaginal bleeding
Drug interactions
No significant drug interactions known (peptide; not metabolized by CYP450; 46% plasma protein bound).
Food interactions
Caution is advised when consuming alcohol with Leuprolide acetate; consult your doctor.
Use in pregnancy
Use in Pregnancy: Leuprolide acetate is highly unsafe during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Completely contraindicated.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Information regarding the use of Leuprolide acetate during breastfeeding is not available; consult your doctor.
Pediatric use
Precocious puberty: Dose established for children over 2 years; safety not established in children under 2 years.
Geriatric use
No special dose adjustment needed.
Renal / hepatic impairment
Renal Impairment: Limited information available; consult your doctor.
Hepatic Impairment: Limited information available; consult your doctor.
Overdose effects
No specific overdose information available; symptomatic and supportive measures should be employed.
Storage conditions
Store below 25°C; use immediately after reconstitution; protect from freezing.
Chemical structure
Leuprolide Acetate