Impact of different GnRH analogs in benign gynecological disorders related to their chemical structure, delivery systems and dose.
This review addresses the question of whether the different gonadotropin releasing hormone (GnRH) agonists in clinical use might have different impacts, related to their chemical structure, delivery system and dose. Impact was investigated in benign gynecological disorders, i.e. endometriosis and leiomyoma. Arguments are presented indicating that a difference in impact of different analogs can be expected. All currently used intranasal, daily subcutaneous and depot preparations finally give rise to low levels of serum estradiol. The number of days before the first ovulatory menstruation after discontinuation of GnRH agonist treatment is remarkably constant. Four weeks after the last impact of the agonist, there is resumption of follicle growth. This phenomenon is independent of chemical structure, delivery system and dose. One should realize, however, that it generally takes about 30 days before the impact of a depot preparation disappears. Consequently, the impact of a depot preparation lasts 4 weeks longer than that of an otherwise applied agonist. Thus resumption of pituitary activity after discontinuation of a depot formulation takes 4 weeks longer than after discontinuation of non-depot formulations. All agonists have an impressive effect on endometriosis, independent of their chemical structure and delivery system. However, there are no studies comparing different agonists with the same delivery system in comparable endometriosis groups. Similarly, all agonists considerably reduce myoma volume, independently of their chemical structure and delivery system.(ABSTRACT TRUNCATED AT 250 WORDS)
Department of Obstetrics and Gynaecology, Rijnstate-EG Hospital, Arnhem, The Netherlands.
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Van Leusden
D002064:Buserelin / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D004715:Endometriosis / Q000188:drug therapy*; D004958:Estradiol / Q000097:blood; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000819:agonists* / Q000493:pharmacokinetics; D017273:Goserelin / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D006801:Humans; D007889:Leiomyoma / Q000188:drug therapy*; D016729:Leuprolide / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D008597:Menstrual Cycle / Q000187:drug effects; D017274:Nafarelin / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D017329:Triptorelin Pamoate / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use
D017329:Triptorelin Pamoate; D017273:Goserelin; D017274:Nafarelin; D007987:Gonadotropin-Releasing Hormone; D004958:Estradiol; D016729:Leuprolide; D002064:Buserelin