Zoplide
Leuprolide Acetate Injection
Strength
✓11.25 mg✓22.50 mg
Pack Size
1 Vial
Drug Class
Gonadotropin-Releasing Hormone (GnRH) Agonists
Specification
USP/BP/IH Specs offered for exports
Storage
Store at 25°C to 30°C.
Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH or LH-RH).
The analog possesses greater potency than the natural hormone.
The chemical name is
5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate.
Leuprolide acetate is indicated in the palliative treatment of advanced prostatic cancer.
In a clinical study comparing leuprolide acetate injection with DES in patients with metastatic prostate cancer, adverse reactions were assessed.
Common adverse events included
- Hot flashes (55% with injection vs. 12% with DES)
- Gynecomastia (63% vs. 7%)
- Decreased libido (11% vs. 7%)
Bone pain occurred in
- 5% of injection patients
compared to
- 2% with DES
Other reported adverse reactions included
- Cardiovascular issues like ECG changes/ischemia
- Gastrointestinal symptoms such as nausea/vomiting
- Urinary tract issues like hematuria
Overall, injection was associated with a higher incidence of hot flashes and gynecomastia but showed comparable rates of bone pain and other systemic effects compared to DES in this trial.
Pregnancy
It can cause fetal harm when administered to pregnant women and it should not be used during pregnancy.
Breastfeeding
It is not known whether leuprolide acetate is excreted in human milk.
Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, breastfeeding should be discontinued during treatment with leuprolide acetate.
Fertility
Leuprolide acetate may cause reversible suppression of reproductive function.
In females
- Amenorrhoea
- Suppression of ovarian function
have been reported.
Regular menstrual cycles may not resume immediately after discontinuation of therapy.
In males
- Suppression of spermatogenesis
leading to
- Azoospermia
- Oligospermia
has been observed.
Teratogenicity
Leuprolide acetate has the potential to cause fetal harm and is contraindicated during pregnancy.
Women of childbearing potential should use effective contraception during treatment with leuprolide acetate to prevent potential fetal exposure and related risks.
The recommended dose is 1 mg (0.2 mL or 20 units on the mark) administered as a single daily subcutaneous injection.
As with other drugs administered chronically by subcutaneous injection, the injection site should be varied periodically.
Each 0.2 mL contains
- 1 mg of leuprolide acetate
- Sodium chloride for tonicity adjustment
- 1.8 mg of benzyl alcohol as preservative
- Water for injection
The pH may have been adjusted with sodium hydroxide and/or acetic acid.