Which medications in the drug class Gonadotropin-Releasing Hormone Analogs are used in the treatment of Endometriosis?

Updated: May 10, 2021
  • Author: G Willy Davila, MD; Chief Editor: Michel E Rivlin, MD  more...
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Answer

Gonadotropin-Releasing Hormone Analogs

Gonadotropin-releasing hormone (GnRH) analogues produce a hypogonadotrophic-hypogonadic state by downregulation of the pituitary gland. Goserelin and leuprolide acetate are commonly used agonists.

Normal menstrual cycles rely on pulsatile delivery of GnRH to the pituitary. The GnRH analogues (agonists) supply constant stimulation of the pituitary receptors, leading to downregulation and eventual suspension of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) secretion. This suspension results in a profound hypoestrogenic state, similar to menopause. Because endometrial implants are dependent on estrogen stimulation, they subsequently regress. Owing to hypoestrogenic adverse effects, the use of these drugs is limited to 6-months duration.

The use of so-called add-back therapy, addition of low-dose estrogen with or without a progestin, for prolonged therapy has been investigated. The results are mixed, and, thus, a sound recommendation cannot be made currently.

The expense of GnRH analogues is a significant limitation to their long-term use. GnRH agonists should be used with caution in adolescents younger than 16 years because of adverse effects on bone density.

Goserelin (Zoladex)

Goserelin suppresses ovarian and testicular steroidogenesis by decreasing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels. This agent is administered monthly as a subcutaneous (SC) implant in the upper abdominal wall; it is otherwise similar to the drugs in this class.

Leuprolide (Lupron Depot, Eligard)

Leuprolide suppresses ovarian and testicular steroidogenesis by decreasing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels. This agent is available in a daily subcutaneous (SC) dosing regimen and the much more convenient monthly intramuscular (IM) depo formulation. A 3-month depo dosing formulation is also available, but experience with its use is limited for endometriosis.

Nafarelin (Synarel)

Nafarelin is an analogue of gonadotropin-releasing hormone (GnRH) that is approximately 200 times more potent than natural endogenous GnRH. Upon long-term administration, this agent suppresses gonadotrope responsiveness to endogenous GnRH, thereby reducing secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn reduces ovarian and testicular steroid production.

Nafarelin is available as a nasal solution (2 mg/mL). Administration of this agent is delivered via a nasal spray, which requires twice daily (bid) dosing; it is otherwise similar to the other drugs in this category.


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