Bioavailability and pharmacokinetics of cyproterone acetate after oral administration of 2.0 mg cyproterone acetate in combination with 50 μg ethinyloestradiol to 6 young women

Hümpel, M.; Wendt, H.; Schulze, P.; Dogs, G.; Weiss, C; Speck, Ulrich

doi:10.1016/0010-7824(77)90108-1

Cited by 26 publications

(5 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The half-life of the terminal disposition phase lies within the range of the renal elimi nation half-life of the metabolites at about 24 h. Thus, the metabolites of estradiol valer ate, which is not eliminated unchanged with the urine (own unpublished results), are elim inated at about the same rate as the metabo lites of synthetic sex steroids (levonorgestrel, ethinylestradiol) [17,18].…”

Section: Discussionmentioning

confidence: 85%

Pharmacokinetics and Biotransformation of Estradiol Valerate in Ovariectomized Women

Düsterberg¹,

Schmidt-Gollwitzer

Hümpel³

1985

Horm Res

View full text Add to dashboard Cite

Estradiol valerate is well suited for treatment of the characteristic symptoms accompanying menopause in women. The pharmacokinetics and biotransformation of estradiol valerate were studied in women following intravenous, intramuscular and oral administration. Intravenously given, estradiol valerate is split by enzymatic hydrolysis into 17β-estradiol and the fatty acid. The estrogen arising in vivo from the steroid ester is subject to intermediate metabolism. The metabolites are eliminated at a nearly constant rate mainly in urine. The biotransformation of estradiol valerate was not different following intravenous or intramuscular injection. Orally given estradiol valerate is subject to an extensive first pass metabolism. Daily repeated oral administration does not result in accumulation of 17β-estradiol and its metabolites.

show abstract

Section: Discussionmentioning

confidence: 85%

Pharmacokinetics and Biotransformation of Estradiol Valerate in Ovariectomized Women

Düsterberg¹,

Schmidt-Gollwitzer

Hümpel³

1985

Horm Res

View full text Add to dashboard Cite

show abstract

“…1969;Ismail et al, 1974;Hammerstein ef a/.. 1975;Barnes eta/., 1975;Dewhurst er al., 1977;Ekoe et a/.. 1980). Because of the long half life of cyproterone acetate (Humpel et al, 1977;Dusterberg et al, 1979), this particular combination has to be given in a complicated reversed sequential regimen to ensure regular menstrual bleeding (Hammerstein & Cupceancu, 1969). The majority of studies use subjective or at least only fairly crude objective methods to assess the effects of treatment on hair growth.…”

Section: Discussionmentioning

confidence: 99%

The Treatment of Hirsutism With a Combination of Desogestrel and Ethinyl Oestradiol

Dewis

Petsos

Newman

et al. 1985

Clinical Endocrinology

View full text Add to dashboard Cite

Some available oral contraceptive agents are unsuitable for the treatment of hirsutism since, although they suppress endogenous gonadotrophins and so ovarian androgen production, they contain a progestogen which is itself androgenic. The combination of 30 micrograms ethinyl oestradiol (EE2) and 150 micrograms desogestrel (Marvelon) does not suffer from this drawback. We have therefore assessed its value in 15 hirsute women treated for one year. Mean +/- SE androgen-dependent hair growth, assessed photographically fell from 0.31 +/- 0.01 to 0.23 +/- 0.01 mm/d at 1 year (P less than 0.001). Ten of the fifteen patients reported definite subjective improvement. Treatment was associated with a marked rise in SHBG concentration identical to that seen with 30 micrograms EE2 alone. By four months there were significant falls in serum levels of androstenedione and LH throughout the cycle, but not for testosterone, dihydrotestosterone or 5 alpha-androstane 3 alpha, beta 17 -diol. Calculated free testosterone levels were significantly suppressed. All the biochemical changes were maintained after seven months of treatment. We conclude that this preparation is a suitable oral contraceptive for the treatment of hirsute women.

show abstract

“…It binds to the receptor with about 21% of the affinity of testosterone 46. Antiandrogenic effects of cyproterone acetate are exerted by blocking AR at the pilocebaceous unit, as well as by reducing serum testosterone levels and decreasing 5α‐reductase activity 47…”

Section: Antiandrogensmentioning

confidence: 99%

“…The side effects of CPA are similar to those of medroxyprogesterone acetate and include weight gain, fluid retention, mood changes, headaches, breast tenderness, and decreased libido. Some of the side effects may be due to the glucocorticoid activity of the drug 47. CPA in combination with estrogens has mild effects on lipid profile.…”

Section: Antiandrogensmentioning

confidence: 99%

See 1 more Smart Citation

Insulin Sensitizers and Antiandrogens in the Treatment of Polycystic Ovary Syndrome

Diamanti-Kandarakis

Zapanti

2000

Annals of the New York Academy of Sciences

View full text Add to dashboard Cite

The heterogeneous origin of polycystic ovary syndrome (PCOS) has been demonstrated by several studies. Abnormalities in steroidogenesis and metabolism are present, but the exact link between these two pathologic features remains to be clarified. In clinical practice, more than one therapeutic approach for the treatment of this syndrome has been proposed over the last few decades. Because hyperandrogenism and hyperinsulinemia contribute to a different degree to the phenotype of PCOS, therapeutic efforts have focused on agents that could treat or modify the clinical manifestations of these disorders. Antiandrogens as a sole treatment or combined with oral contraceptives are considered the treatment of choice for the manifestations of hyperandrogenemia, but there is no agreement about their efficacy on the metabolic sequelae of PCOS (insulin resistance, hyperinsulinemia, dislipidemia). Furthermore, the improvement of insulin sensitivity by insulin sensitizers may be of therapeutic value directly and/or indirectly in the management of clinical manifestations of hyperinsulinemia and hyperandrogenemia.

show abstract

Bioavailability and pharmacokinetics of cyproterone acetate after oral administration of 2.0 mg cyproterone acetate in combination with 50 μg ethinyloestradiol to 6 young women

Cited by 26 publications

References 3 publications

Pharmacokinetics and Biotransformation of Estradiol Valerate in Ovariectomized Women

Pharmacokinetics and Biotransformation of Estradiol Valerate in Ovariectomized Women

The Treatment of Hirsutism With a Combination of Desogestrel and Ethinyl Oestradiol

Insulin Sensitizers and Antiandrogens in the Treatment of Polycystic Ovary Syndrome

Contact Info

Product

Resources

About