Progestagenic and Antigonadotrophic Activities of STS 557<sup>1</sup>)

Stölzner, W; Kurischko, A.; Freund, H.‐J.; Freund, Ronald K.; Meyer, Martine De; Oettel, M

doi:10.1055/s-0029-1210217

Cited by 9 publications

(3 citation statements)

References 3 publications

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“…The rabbit endometrium is a preferred target for the bioassay of synthetic progestins in rodents. In this animal model the transformation-inducing activity of Dienogest was found to be considerably higher than that of levonorgestrel for both oral and sub- fraction, o---0 metabolite fraction cutaneous administration (Stölzner et al, 1983). On the other hand, the ovulation-inhibiting effect of Dienogest in rabbits was shown to exceed that of levonorgestrel only after oral administration but was inferior to the latter when the drugs were given by s.c. route (ibid.).…”

Section: Discussionmentioning

confidence: 67%

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Pharmacokinetics of the Progestin Dienogest (STS 557) in Rabbits^*)

Hillesheim¹,

Ritter²,

Valentin³

et al. 2009

Exp Clin Endocrinol Diabetes

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Disposition and excretion of the progestin Dienogest (17 alpha-cyanomethyl-17 beta-hydroxy-estra-4,9-dien-3-one, STS 557) were investigated in female rabbits. Following single and repeated administration of the tritium-labelled compound the plasma concentration courses of total radioactivity (Dienogest + metabolites) and of the parent drug alone were estimated and also the urinary and fecal excretion of total radioactivity. From these data basic pharmacokinetic parameters were calculated. Additionally, the enterohepatic recirculation of biliary excreted metabolites was studied using bile of donors for oral administration to recipients. Following oral administration the high bioavailability of Dienogest which was already found in other animal species and in man could also be confirmed with rabbits. The parameters of Dienogest disposition do not differ significantly from those of the progestin levonorgestrel. Thus, the different effects of the both progestins in the McPhail-Clauberg assay in the rabbit cannot be attributed to differences in pharmacokinetics.

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Section: Discussionmentioning

confidence: 67%

“…Dienogest (1 7c-cyanomethy1-1 7ß-hydroxy-4, 9-estradien-3-one, STS 557) is characterized by a high progestagenic effect in the McPhail-Clauberg test in the rabbit being stronger than that of levonorgestrel (Stölzner et al, 1983). In women, however, the high progestagenic activity could not be confirmed.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of the Progestin Dienogest (STS 557) in Rabbits^*)

Hillesheim¹,

Ritter²,

Valentin³

et al. 2009

Exp Clin Endocrinol Diabetes

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“…Progestagenic activity. The progestagenic activity was evaluated using the McPhail test (see Stölzner et al, 1983). Infantile female rabbits received at total priming dose of 30 zg/animal estradiol-17ß-benzoate, divided to 6 s.c. injections, once on days 1-4 and twice on day 5.…”

Section: Introductionmentioning

confidence: 99%

Further Report on the Endocrinological Profile of Two Synthetic Estrogens with Antifertility Properties, STS 456 and STS 593

Koch¹,

Ivanenko²,

Kurischko³

et al. 2009

Exp Clin Endocrinol Diabetes

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Two synthetic estrogens, STS 456 and STS 593, with noteworthy post-coital antifertility properties in the rat were studied for their estrogenic, antiestrogenic, progestagenic, antiprogestagenic, antigonadotrophic, androgenic and antiandrogenic effects in laboratory animals. Beside their weak estrogenic activity which corresponds to their slight affinity to the uterine estrogen receptor in the rat, both steroids show remarkable antiestrogenic effects. No progestagenic, androgenic and antiandrogenic effects were found but STS 593 showed some antiprogestagenic activity. The antigonadotrophic efficacy of STS 456 was relatively high while STS 593 was scarcely active. The results are discussed with respect to possible application of these drugs for interceptive purposes.

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