Studies on the Anti-Oestrogenic and Oestrogen-Like Action of Clomiphene Citrate. Animal experiments

Schulz, K.-D.; August, S.; Gasde, K.; Kramer, Gerald L.

doi:10.1159/000301750

Cited by 13 publications

(4 citation statements)

References 6 publications

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“…Our present data seem to indicate that this suppressive effect might be attributed to the inherent oestrogenic properties of clomiphene. This is consistent with data derived from studies in rats as recently reviewed by Schulz et al (1972) suggesting that the extent of the biological anti-oestrogenic or oestrogenic activity of clomiphene on the female hypothalamo-pituitary-ovarian axis is regulated by the absolute concentration of the compound in the different organs, and by the clomiphene :oestrogen ratio in the central nervous system and other oestrogen dependent tissues.…”

Section: Discussionsupporting

confidence: 91%

Gonadotrophin Release in Ovariectomized Patients

Ravid

Jedwab

Persitz

et al. 1977

Clinical Endocrinology

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Administration of clomiphene citrate (150 mg/day) for 5 days to twenty-four ovariectomized patients and seven normal female patients evoked a significant release of FSH and LH in the normal control group and suppressed the gonadotrophin secretion in the castrated patients. A similar suppressive effect on gonadotrophin secretion was noted in eight ovariectomized patients treated for 10 days with low doses (50 microgram/day) of ethinyl oestradiol. It is suggested that in the ovariectomized hypoestrogenic patients, clomiphene acted as an oestrogen, suppressing by a negative feedback action gonadotrophin release in a way similar to ethinyl oestradiol. In the normal control group with an adequate steroid environment, clomiphene acted (probably at the hypothalamic level) as an oestrogen antagonist and stimulated gonadotrophin secretion. In view of our findings, it seems as if the ability of anovulatory patients to respond to clomiphene treatment by increased gonadotrophin secretion depends upon the absolute concentration of the compound in the different organs and by the quantitative relation of clomiphene to the endogenous oestrogens.

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Section: Discussionsupporting

confidence: 91%

Gonadotrophin Release in Ovariectomized Patients

Ravid

Jedwab

Persitz

et al. 1977

Clinical Endocrinology

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“…Overall the appearance of the cells is similar to that seen at dioestrus when the epithelium is under the influence of progesterone [9,11]. At this dose CC may block the effect of or inhibit the production of endogenous oestrogen [12].…”

Section: Resultsmentioning

confidence: 58%

Clomiphene Citrate Alters Vaginal Surface Morphology in Cycling Rats

Terry

Murphy²,

Shorey³

1992

Cells Tissues Organs

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Cycling virgin female rats were treated with clomiphene citrate (CC) during dioestrus of the reproductive cycle. Animals were sacrificed 2 days after the initial injection and their vaginal tissue was examined by scanning electron microscopy. Animals treated with one dose of CC had an epithelium consistent with a prolonged dioestrus. Treatment with CC for 2 days induced changes in the epithelium that had no resemblance to any normal hormonally controlled event in the vagina. It was found that CC had effects consistent with progesterone alone as well as effects unique to this superovulatory drug.

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“…These effects have been demonstrated using such para meters as uterine weight gain [7], vaginal comification [2,7], glycogen uptake in uterine cells [16], inhibition of tritiated estradiol-17y? entry into uterine cells [13][14][15], effect on protein synthesizing activity of uterine cells [14,15], effect on RNA synthesis in uterine cells [14,15], and gonadotro pin stimulation or inhibition [1,7]. Since the mechanism of action of clomi phene in its clinical role as an inducer of ovulation is possibly a result of these estrogenic and antiestrogenic characteristics, a more precise quan-…”

mentioning

confidence: 99%

Effect of Cis- and Trans-Clomiphene on the Uterine Blood Flow of Oophorectomized Ewes

Jg¹,

Fc²

1976

Gynecol Obstet Invest

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Changes in the left uterine artery blood flow (UBF) after intraarterial administration of estradiol-17β and cis- and trans-clomiphene citrate to conscious, oophorectomized ewes were monitored by chronically implanted electromagnetic flow probes. Cis-clomiphene produced UBF increases comparable to or greater than those produced by estradiol-17β but at dose levels 20 times greater. Comparison of UBF response curves for cis-clomiphene with those for estradiol-17β showed a delayed onset of initial vasodilation and a delayed peak response. The duration of uterine vasodilation produced by cis-clomiphene was dose-dependent and exceeded that produced by estradiol-17β. Similar responses were observed with trans-clomiphene but at dose levels at least 1,000 times those of estradiol-17β. The characteristics of clomiphene-induced UBF responses that differed from those after estradiol-17β may reflect differences in estrogen receptor activation between the compounds.

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Studies on the Anti-Oestrogenic and Oestrogen-Like Action of Clomiphene Citrate. Animal experiments

Cited by 13 publications

References 6 publications

Gonadotrophin Release in Ovariectomized Patients

Gonadotrophin Release in Ovariectomized Patients

Clomiphene Citrate Alters Vaginal Surface Morphology in Cycling Rats

Effect of Cis- and Trans-Clomiphene on the Uterine Blood Flow of Oophorectomized Ewes

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