LEUPROLIDE ACETATE
(Lupron Depot-PED)Standard Prescription
Leuprolide acetate __ mg IM {frequency}
Dosages
Prevention of abnormal uterine bleeding in post-menarchal oncology patients (start 1 month prior to chemo):
3.75 mg IM every 4 weeks or
11.25 mg IM every 12 weeks
Hormone therapy for transgender females:
3.75 - 7.5 mg IM every 4 weeks, or
11.25 - 22.5 mg IM every 13 weeks
7.5 mg IM every 4 weeks or
22.5 mg IM every 13 weeks
Endometriosis or Fibroids:
Post-menarche adolescent females: 11.25 mg IM every 3 months
>= 18 years: 3.75 mg IM monthly
3.75 mg IM every 4 weeks or
11.25 mg IM every 12 weeks
Hormone therapy for transgender females:
3.75 - 7.5 mg IM every 4 weeks, or
11.25 - 22.5 mg IM every 13 weeks
Central Precocious Puberty (CPP):
(titrate by 3.75 mg every 4 weeks until clinical or lab targets achieved)
Starting dose for most children:7.5 mg IM every 4 weeks or
22.5 mg IM every 13 weeks
Endometriosis or Fibroids:
Post-menarche adolescent females: 11.25 mg IM every 3 months
>= 18 years: 3.75 mg IM monthly
Mechanism of Action
Leuprolide acetate is a gonadotropin-releasing hormone (GnRH) analogue acting as an agonist at pituitary GnRH receptors. Agonism of GnRH receptors initially results in the stimulation of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion by the anterior pituitary ultimately leading to increased serum estradiol and testosterone levels via the normal physiology of the hypothalamic-pituitary-gonadal axis (HPG axis); however, because propagation of the HPG axis is incumbent upon pulsatile hypothalamic GnRH secretion, pituitary GnRH receptors become desensitised after several weeks of continuous leuprolide therapy. This protracted downregulation of GnRH receptor activity is the targeted objective of leuprolide therapy and ultimately results in decreased LH and FSH secretion, leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels regardless of sex.
Forms Supplied
Injection:
3.75 mg and 7.5 mg (1-monthly slow release);
11.25 mg and 22.5 mg (3-monthly slow release);
30 mg (4-monthly slow release)
Comments
Amenorrhea rate: 73-96%.
Optimize calcium and vitamin D intake as may reduce bone density.
Long term use consider add-back estrogen and/or progestin therapy.
Maximum duration of treatment:
Fibroids: 3 months
Endometriosis: 6 months (if monthly injections) or 12 months if q3month injections.
Do not use a combination of syringes to achieve dose due to different drug release profiles.
Optimize calcium and vitamin D intake as may reduce bone density.
Long term use consider add-back estrogen and/or progestin therapy.
Maximum duration of treatment:
Fibroids: 3 months
Endometriosis: 6 months (if monthly injections) or 12 months if q3month injections.
Do not use a combination of syringes to achieve dose due to different drug release profiles.
References
658, 662, 663
Last Edited
2022-07-04 19:12:15