this study presents the influence of hydroxypropyl-β-cyclodextrin (hpbcd) on the aqueous solubility of acyl esters of cyproterone. first, a number of esters of cyproterone were synthesized. then the phase solubility analysis of the compounds in the presence of hpbcd was investigated in phosphate buffer solution at a ph of 7.4. to gain a better understanding of the complexation mechanism, the sy...

OBJECTIVE To evaluate the clinical and hormonal response of topically applied cyproterone acetate, oral cyproterone acetate, and placebo lotion in women with acne. DESIGN Placebo-controlled, randomized study. SETTING Patients were recruited from the Institute of Endocrine Cosmetics, Vienna, Austria. PATIENTS Forty women with acne. INTERVENTIONS Treatment with oral medication consisting ...

The steroid compound cyproterone acetate was identified in a high-throughput screen for glucocorticoid receptor (GR) binding compounds. Cyproterone (Schering AG) is clinically used as an antiandrogen for inoperable prostate cancer, virilizing syndromes in women, and the inhibition of sex drive in men. Despite its progestin properties, cyproterone shares a similar pharmacological profile with th...

Since the recent introduction of a drug regimen containing 2 mg of the antiandrogen cyproterone acetate and 50 micrograms ethinyl-oestradiol (Diane; oestrogen-cyproterone acetate) several uncontrolled reports have extolled the benefits of this drug. Double blind studies, however, are lacking. Sixty two patients with moderate or moderately severe acne were therefore included in a double blind tr...

A case of severe acute hepatitis caused by cyproterone acetate in a 71 year old man with prostatic carcinoma is reported with a review of the literature on hepatic reactions to this drug. The association between the use of cyproterone acetate and liver abnormalities is poorly documented. This is the fourth published report of adverse hepatic reaction to cyproterone acetate and it substantiates ...

The multiplicity of meningiomas or abrupt lesion growth in patients treated with cyproterone acetate suggests that this progestative treatment may promote lesion growth. We report the rapid regression of an incidental meningioma after discontinuation of a 10-year cyproterone acetate treatment. This unique observation suggests that conservative management of meningiomas may be the best option am...

PURPOSE Prostate specific antigen (PSA) and human glandular kallikrein (hK2) are mainly produced by the prostate and their genes are regulated by androgens through the androgen receptor. We determine whether PSA and hK2 change significantly in plasma and urine after antiandrogen treatment in male-to-female transsexuals. MATERIALS AND METHODS Plasma and urine PSA and hK2 were measured with hig...

A 70-year-old man with prostatic adenocarcinoma received cyproterone acetate 200 mg per day. Three months later, mild fatigue and anorexia with elevation of the alanine aminotransferase (ALT) level to 1311 U/L, total bilirubin level to 14 mg/dL and prothrombin time of 15/11.9 seconds developed. At that time the aspartate aminotransferase (AST) level was only 82 U/L. Viral hepatitis and autoimmu...

      This study presents the influence of hydroxypropyl-β-cyclodextrin (HPBCD) on the aqueous solubility of acyl esters of cyproterone. First, a number of esters of cyproterone were synthesized. Then the phase solubility analysis of the compounds in the presence of HPBCD was investigated in phosphate buffer solution at a pH of 7.4. To gain a better understanding of the complexation mechanism, ...

Gonadal hormones regulate the expression of alpha1-adrenoceptor subtypes in several tissues. The present study was carried out to determine whether or not cyproterone acetate, an anti-androgenic agent, regulates the alpha1-adrenoceptor subtypes that mediate contractions of the rat vas deferens in response to noradrenaline. The actions of subtype selective alpha1-antagonists were investigated in...