Estrogen metabolic effects

Raloxifene hydrochloride is a synthetic nonsteroidal drug derived from the benzothiophene and afferent to SERMs. It is known that raloxifene acts on metabolism, the skeleton, and the cardiovascular system as an estrogenic agonist (Khovidhunkit et al. 1999 Ettinger et al. 1999 Walsh et al. 1998), whereas it shows an estrogenic antagonist effect on reproductive organs such as the... 

The effect of fluconazole 150 mg on circulating ethinylestradiol concentrations has been studied on day 6 of one of two cycles in women taking oral contraceptives (343). The serum concentrations of ethinylestradiol (Cmax and AUC) were significantly increased by fluconazole, but tmax was not affected. These findings suggest that there is a potential for a clinically significant interaction between fluconazole and ethinylestradiol, by inhibition of estrogen metabolism. 

Hammond CB, Jelovsek FR, Lee KL, Creasman WT, Parker RT. Effects of long-term estrogen replacement therapy. I. Metabolic effects. Am J Obstet Gynecol 1979 133(5) 525-36. 

Although oral administration of 3,000 mg/kg/day unleaded gasoline to female mice for 3 days resulted in a three-fold increase in estrogen metabolism in isolated hepatocytes, there were no functional antiestrogenic effects as assessed by uterotrophic assays (Standeven et al. 1994b). 

Mauras N, O Brien KO, Klein KO. Estrogen suppression in males metabolic effects. J Clin Endocrinol Metab 2000 85 2370-2377. 

Lu, F., Zahid, M., Saeed, M., Cavalieri, E. L., and Rogan, E. G. (2007) Estrogen metabolism and formation of estrogen-DNA adducts in estradiol-treated MCF-10F cells. The effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin induction and catechol-O-methyltransferase inhibition. J. Steroid Biochem. Mol. Biol. 105, 150-158. 

SI. Schneider, J., Kinne, D., Fracchia, A., et al.. Abnormal oxidative metabolism of estradiol in women with breast cancer. Proc. Natl. Acad. Sci. USA 79,3047-3051 (1982). Spink, D. C., Hayes, C. L., Young, N. R., cf a/.. The effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin on estrogen metabolism in MCF-7 breast cancer cells Evidence for induction of a novel 17/3-estradiol 4-hydroxylase. J. Steroid Biochem. Mol. Biol. 51, 251-258 (1994). Spink, D. C., Spink, B. C., Cao, J. Q., et al.. Induction of cytochrome P450 IBI and catechol estrogen metabolism in ACHN human renal adenocarcinoma cells. J. Steroid Biochem. Mol. Biol. 62, 223-232 (1997). 

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