The dynamics of gonadotropin inhibition in women induced by an antagonistic analog of gonadotropin-releasing hormone

The Journal of Clinical Endocrinology and Metabolism
N S CetelS S Yen

Abstract

The inhibitory effect of a GnRH antagonist, [AC-delta 2-Pro1, p-F-D-Phe 2, D-Trp3,6]GnRH (4F-Antag), on gonadotropin secretion was determined by four sequential studies in five hypergonadotropic postmenopausal women. In response to an iv (80 micrograms/kg) dose of 4F-Antag, a progressive decline in basal gonadotropin levels with a marked attenuation of pulse amplitude was observed. Mean serum LH and FSH concentrations were maximally reduced by 46% and 26%, respectively, 4 and 9 h after the iv bolus. A similar pattern of suppression was found with sc and im routes of administration, with maximal effects occurring at 6.0 h for LH and 8.5 h for FSH. This was followed by the resumption of pulsatile release and a return to basal levels between 10 and 24 h for both gonadotropins. When 4F-Antag was superimposed during an iv infusion of GnRH (0.2 micrograms/min) at the time (2 h) of maximal LH release (231% above basal values), a 47.1% decrease in GnRH-stimulated LH levels and a 15.8% decrease in FSH values occurred at 1.75 h. A positive linear correlation was found between basal and exogenous GnRH-stimulated LH and FSH concentrations and the inhibitory effect of the 4F-antagonist. The dynamics of the antagonistic effect demonstrated b...Continue Reading

Citations

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