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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