Gonadotropin-releasing Hormone Analog

A gonadotropin-releasing hormone analog, also known as a GnRH analog or GnRH agonist, is a class of synthetic peptide drugs modeled on the human hypothalamic gonadotropin-releasing hormone and designed to mimic or antagonize the physiological effects of GnRH for therapeutic purposes. The most common drugs of this class are leuprolide, nafarelin, and buserelin. Due to the extreme sensitivity of the pituitary GnRH receptors to amount and timing of GnRH pulses, varying the dose and dosing interval of an analog can produce either stimulatory ("agonist") or suppressive ("antagonist") effects on the reproductive system. In clinical practice, these drugs are most commonly used to suppress the sex steroids produced by the reproductive system. Among the conditions in which suppression of reproductive hormones is sometimes desirable:
  1. estrogen-dependent cancers, such as breast cancer
  2. testosterone-dependent cancers, such as prostate cancer
  3. precocious puberty
  4. endometriosis
  5. severe catamenial (i.e., dependent on the menstrual cycle) disorders
There are far fewer conditions in which a GnRH analog is used as an agonist:
  1. as a substitute for GnRH (now unavailable) for endocrine diagnostic testing
  2. cryptorchidism
Of the specific drugs listed, leuprolide is by far the most commonly used in North America.

 

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