GnRH Antagonists

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Chapter: Essential pharmacology : Anterior Pituitary Hormones

Some more extensively substituted GnRH analogues act as GnRH receptor antagonists. They inhibit Gn secretion without causing initial stimulation. The early GnRH antagonists had the limitation of producing reactions due to histamine release.


GnRH ANTAGONISTS

 

Some more extensively substituted GnRH analogues act as GnRH receptor antagonists. They inhibit Gn secretion without causing initial stimulation. The early GnRH antagonists had the limitation of producing reactions due to histamine release. Newer agents like ganirelix and cetrorelix have low histamine releasing potential and are being clinically used in specialized centres for inhibiting LH surges during controlled ovarian stimulation in women undergoing in vitro fertilization. Their advantages over longacting GnRH agonists include:

 

· They produce quick Gn suppression by competitive antagonism, need to be started only from 6th day of ovarian hyperstimulation.

· They carry a lower risk of ovarian hyperstimulation syndrome.

·       They achieve more complete suppression of endogenous Gn secretion.

·        However, pregnancy rates are similar or may even be lower.

 

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