piperidines and 1-1-2-2-tetramethyl-1-2-bis(4--hydroxyphenyl)ethane

In mature female and male rats sex hormone deficiency was produced by surgical castration and by antiestrogen or antiandrogen administration. For the latter purpose we used the nonsteroidal antiestrogens tamoxifen, keoxifene (LY156758) and tetramethylhexestrol, and the steroidal antiandrogen cyproterone acetate. Dosages of 0.4 mg tamoxifen/rat/day and isomolar dosages of keoxifene and tetramethylhexestrol led to a bone mass reduction which was comparable to ovariectomized rats. Cyproterone acetate showed, at 10 mg/rat/day, a similar decrease in bone mass like orchidectomy. The often discussed intrinsic estrogen activity of the antiestrogens was present only in the highest dosage tested of tamoxifen. Keoxifene and tetramethylhexestrol showed no estrogenic effects, but this may be a dosage problem. Cyproterone acetate revealed no androgenic side-effects. These results indicate that antigonadal hormone drugs reduce bone mass to a varying extent.

Topics: Androgen Antagonists; Animals; Bone Density; Bone Diseases, Metabolic; Cyproterone; Cyproterone Acetate; Estrogen Antagonists; Female; Hexestrol; Male; Orchiectomy; Ovariectomy; Piperidines; Raloxifene Hydrochloride; Rats; Tamoxifen; Testosterone