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LHRH Agonists/GnRH Analogs

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Pharmacology

Summary

The lesson revolves around Gonadotropin Releasing Hormone (GnRH) Analogs, more commonly known as LHRH Agonists. These substances are produced by the hypothalamus and released by the pituitary gland. A normal, pulsatile release of GnRH leads to the release of Luteinising hormone (LH) and follicle stimulating hormone (FSH) which stimulate the production of testosterone and estrogen respectively. However, the continuous administration of exogenous GnRH analogs, such as leuprolide, goserelin, and triptorelin, results in a hyperstimulation of the pituitary, causing a brief hormone surge followed by pituitary desensitization, lowering hormone levels and decreasing the release of estrogen and testosterone. These analogs are useful in a variety of scenarios. They are used in the treatment of conditions like advanced prostate cancer, hormone receptor positive breast cancer, and uterine leiomyomas. Additionally, GnRH analogs are also employed in the process of gender transition, where they aid in lowering endogenous hormone levels when used with gender-affirming hormones. Other uses include treatment for endometriosis, management of precocious puberty to allow normal skeletal growth, and as part of in-vitro fertilization procedures. Despite the benefits, potential side effects range from structural changes like osteoporosis, reduced muscle mass and increased fat stores to sexual side effects such as loss of libido, erectile dysfunction, hot flashes and diarrhea. In rare cases, they can lead to pituitary apoplexy.

Lesson Outline

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