Leuprolide
Lupron Depot · Eligard
Half-life
30 days
Time to Peak
4 hr
Steady State
~150 days
Bioavailability
100%
Dose Range
3.75–45 mg
Frequency
Monthly
Overview
GnRH agonist depot injection ("puberty blocker"). Continuous GnRH receptor stimulation causes downregulation, suppressing LH/FSH and gonadal sex hormone production to castrate levels. Available in 1-month (3.75/7.5 mg), 3-month (11.25/22.5 mg), 4-month (30 mg), and 6-month (45 mg) depot formulations. Initial "flare" effect (1-2 weeks of INCREASED hormones) before suppression occurs. Free peptide half-life is ~3h, but depot provides sustained release over the formulation period.
Mechanism of Action
Synthetic GnRH analogue. Continuous administration desensitizes the GnRH receptor, suppressing pituitary LH and FSH secretion. Results in castrate levels of testosterone and estradiol after 2-4 weeks.
Dosing Information
| Route | Dose Range | Half-life | Tmax | Frequency |
|---|---|---|---|---|
| Intramuscular (IM) | 3.75–45 mg | 30 days | 4 hr | Monthly, Every 3 months, every 4 months, Every 6 months |
| Subcutaneous (SubQ) | 7.5–45 mg | 30 days | 4 hr | Monthly, Every 3 months, every 4 months, Every 6 months |
Used in Regimens
Leuprolide is not currently part of any catalog regimen.
Data Sources
- FDA Label Lupron Depot (leuprolide acetate) FDA Prescribing Information
- FDA Label Eligard (leuprolide acetate) FDA Prescribing Information
Related Tools
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