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Clinical Pharmacology of LHRH Antagonists

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Abstract

Hypothalamic LHRH controls the pituitary synthesis and secretion of the gonadotropins that are essential for the regulation of gonadal function. Since the molecular structure of LHRH has been known, several synthetic chemical derivatives of LHRH have become available for basic and clinical studies. These analogs constitute two groups [1]. One group, LHRH agonists, are analogs up to 230 times more potent than LHRH in stimulating LH and FSH release. The other group, LHRH antagonists, are analogs that compete with endogenous LHRH at the hypophysial receptor level and directly inhibit the secretion of gonadotropins. Both groups of LHRH analogs, however, suppress pituitary and gonadal function because even LHRH agonists, when given repeatedly, lead to pituitary desensitization. This ability of LHRH analogs to selectively inhibit gonadal steroid secretion and therefore, induce a reversible medical gonadectomy has several clinical applications. These include hormone-dependent tumors, precocious puberty, cryptorchidism, in vitro fertilization, endometriosis, male and female contraception and several others. The mechanism of action of LHRH agonists and antagonists, however, is completely different.

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© 1990 Kluwer Academic Publishers

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Pavlou, S.N., Rivier, J., Vale, W., Kamilaris, T. (1990). Clinical Pharmacology of LHRH Antagonists. In: Vickery, B.H., Lunenfeld, B. (eds) GnRH Analogues in Cancer and Human Reproduction. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-0725-6_13

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  • DOI: https://doi.org/10.1007/978-94-009-0725-6_13

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-6811-6

  • Online ISBN: 978-94-009-0725-6

  • eBook Packages: Springer Book Archive

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