On the inhibitory action of 29 drugs having side effect gynecomastia on estrogen production

@article{Satoh2002OnTI,
  title={On the inhibitory action of 29 drugs having side effect gynecomastia on estrogen production},
  author={Takashi Satoh and Shinji Itoh and T Seki and Shungo Itoh and Itsuo Yoshizawa},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2002},
  volume={82},
  pages={209-216}
}
To examine the influence on aromatase and sulfatase pathways in estrogen pool by drugs reported to cause gynecomastia as the side effect, 29 ethical drugs were incubated with human placental microsomes as an enzyme source. The percent inhibition of drugs on aromatase pathway was obtained by sum of the velocity constants of two products, estrone (E1) and estradiol (E2) from testosterone (T) as the substrate, and that on sulfatase pathway was obtained as the velocity constant of production of E1… Expand
Studies on the interactions between drugs and estrogen. III. Inhibitory effects of 29 drugs reported to induce gynecomastia on the glucuronidation of estradiol.
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The result implies that, when the contribution of the glucuronidation to enterohepatic circulation is taken into consideration, the effect of this metabolic inhibition in the estrogen pool cannot be ignored. Expand
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A total of 14 drugs consisting of the above 13 drugs plus spironolactone were found to inhibit the 2-hydroxylation or 17-oxidation of E2 in the liver, and this is presumed to act as a trigger that causes as increase in the estradiol pool, followed by induction of gynecomastia. Expand
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References

SHOWING 1-10 OF 30 REFERENCES
Effect of flutamide on estradiol metabolism.
TLDR
This study demonstrates that flutamide produces multiple functional, reversible, cirrhosis-like disturbances of steroid metabolism, which are universal in the patients studied regardless of whether they had clinical responses toFlutamide, and doubts that the steroid metabolic changes play a role in the therapeutic effect of the drug. Expand
The effects of cimetidine on the oxidative metabolism of estradiol.
TLDR
It is demonstrated that the administration of cimetidine to men decreases the 2-hydroxylation of estradiol and results in an increase in the serumEstradiol concentration, which may help to account for the signs and symptoms of estrogen excess reported with the long-term use ofcimetidine. Expand
Studies on the interactions between drugs and estrogen: analytical method for prediction system of gynecomastia induced by drugs on the inhibitory metabolism of estradiol using Escherichia coli coexpressing human CYP3A4 with human NADPH-cytochrome P450 reductase.
TLDR
The present results suggest that IC(50) values obtained can be substituted as the prediction index for gynecomastia induced by drugs, considering the patients' individual information. Expand
Inhibition of estrone sulfatase enzyme in human placenta and human breast carcinoma
TLDR
These studies could form the basis for the design of a potent estrone sulfatase inhibitor which would have potential therapeutic activity in the management of breast cancer. Expand
Cimetidine inhibits catechol estrogen metabolism in women.
TLDR
Cimetidine was found to have little effect on selected biochemical indices of bone and calcium metabolism in both groups of women and may be helpful in hypoestrogenic states such as osteoporosis. Expand
Metabolism of the antiandrogenic drug (Flutamide) by human CYP1A2.
TLDR
These studies show the principal role of CYP1A2 in the metabolism of flutamide to 2-hydroxyflutamide, and raise the possibility that increased conversion of flUTamide to 3-hydroxylation or accumulation of 2-HydroxyFlutamide in cells may contribute to the anomalous responses to flutamia that are observed in some advanced prostate cancers. Expand
Antialdosterones: incidence and prevention of sexual side effects.
TLDR
In 182 patients with essential hypertension treated with spironolactone alone for a mean follow-up period of 23 months, daily doses of 75-100 mg were as effective on blood pressure as doses of 150-300 mg. Expand
Comparison of estrogen concentrations, estrone sulfatase and aromatase activities in normal, and in cancerous, human breast tissues
TLDR
The values of E(1)S and E(2) were significantly higher in the tumor tissue than in the area considered as normal, and the sulfatase activity was much higher than aromatase (130-200). Expand
Aromatase and Intracrinology of Estrogen in Hormone-Dependent Tumors
TLDR
All results strongly support an idea of intracrinology of estrogen, which is verified in connection with plasma levels of various steroid hormones and association constants of aromatase and estrogen receptor. Expand
Spironolactone-related inhibitors of type II 17beta-hydroxysteroid dehydrogenase: chemical synthesis, receptor binding affinities, and proliferative/antiproliferative activities.
TLDR
It was found that a para-substituted benzylthio group at the 7alpha-position enhances the inhibitory potency of spironolactone derivatives on type II 17beta-HSD, and offer an interesting tool to study the regulation of this enzyme in several biological systems. Expand
...
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3
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