Clinical Uses of Antiandrogens

Gräf, K.-J.; Brotherton, Janet; Neumann, F.

doi:10.1007/978-3-642-80859-3_7

Cited by 12 publications

(6 citation statements)

References 110 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…For methyltrienolone a high affinity to the progestin receptor has been reported (30,31) and thus the high affinity of the structurally related allyltrienolone is not surprising. CMA and MPA are used therapeutically as powerful progestogens with a 330 fold higher effect than progesterone and MPA is discussed as AR agonist and antagonist (32)(33)(34). These earlier findings are in line with our RBA values.…”

Section: Discussionsupporting

confidence: 89%

Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor

Bauer

Daxenberger

Petri³

et al. 2001

APMIS

View full text Add to dashboard Cite

Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor. APMIS 2000; 108:838+l6.For the steroidal growth promoters trenbolone acetate (TBA) and melengestrol acetate (MGA) neither the complete spectrum of biological activities nor the potential endocrine disrupting activity of their excreted metabolites in the environment is fully understood. The potency of these substances in [3H]dihydrotestosterone ([3H]-DHT) displacement from the recombinant human androgen receptor (rhAR) and from human sex-hormone binding globulin (hSHBG) was evaluated. In addition, the potency for [3H]-ORG2058 displacement from the bovine uterine progestin receptor (bPR) was tested. For comparison, different anabolics and synthetic hormones were also tested for their binding affinities. For 17ptrenbolone (1 7P-TbOH), the active compound after TBA administration, an affinity the rhAR similar to dihydrotestosterone (DHT) and a slightly higher affinity to the bPR than progesterone were demonstrated. The affinity of the two major metabolites, 17a-trenbolone and trendione, was reduced to less than 5% of the 17~-TbOH-value. The affinity of these three compounds and of MGA to the hSHBG was much lower compared with DHT. MGA showed a 5.3-fold higher affinity than progesterone to the bPR but only a weak affinity to the rhAR. The major MGA metabolites have an affinity to the bPR between 85% and 28% of the affinity of progesterone. In consequence, MGA and TBA metabolites may be hormonally active substances, which will be present in edible tissues and in manure. We conclude that detailed investigations on biodegradation, distribution and bio-efficacy of these substances are necessary.

show abstract

Section: Discussionsupporting

confidence: 89%

Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor

Bauer

Daxenberger

Petri³

et al. 2001

APMIS

View full text Add to dashboard Cite

show abstract

“…The normal gonadotrophin levels in the presence of marked reduced androgen levels often found in the past, have been interpreted as arising from a balance between the antiandrogenic and progestational actions of CPA at the hypothalamo-hypophyseal levels (Brotherton 1974;Hammerstein 1977). This consideration is based on the fact that free cyproterone is a potent antiandrogen without antigonadotrophic activity and causes, therefore, an increase in gonadotrophins and in androgens (Graf et al 1974). I n CPA, this effect is counteracted by its additional progestational/antigonadotrophic activity.…”

Section: Discussionmentioning

confidence: 99%

Effects of Cyproterone Acetate (CPA) on Pituitary Gonadotrophin Release and on Androgen Secretion Before and After LH‐RH Double Stimulation Tests in Men

et al. 1978

View full text Add to dashboard Cite

CPA administration at a medium dosage of 10 mg daily for male fertility control resulted in reduced spermiograms and in a distinct decrease in basal T (70% reduction), DHT (50%), LH (30%) and FSH (40%). The episodic fluctuations in gonadotrophin secretion were not affected, but the spiking phenomenon of androgen secretion was completely abolished. Pituitary responses to LH‐RH were reduced significantly for both LH and FSH. Also the gradual increase of T and DHT in the course of the LH‐RH double stimulation tests was reduced. It is concluded that the progestational/antigonadotrophic action of CPA predominates over the antiandrogenic action. In addition, a direct effect at the testicular level is postulated.

show abstract

“…Beginn der Pubertätsentwicklung vor dem 6. bis 8. Lebensjahr bei Mädchen wird als Frühreife bezeichnet; die Grenzen werden unterschiedlich angesetzt (1,3). Es kommt zu frühzeitiger.…”

Section: Pubertas Praecoxunclassified

“…Nach Ausschluß eines Tumors können die Symptome der Frühreife, wie Mammaentwicklung, Schambehaarung, Menstruation und Skelettreife, zum Stillstand oder zur Rückbildung gebracht werden. Als erfolgreich hat sich die Langzeit- therapie mit 20-30 mg Cyproteronacetat täglich erwiesen, aber auch Tagesdosen bis 150 mg/m2 Körperoberfläche wurden angewandt (3). Chlormadinonacetat in Dosen von 4-…”

Section: Pubertas Praecoxunclassified

See 1 more Smart Citation

Behandlung mit Antiandrogenen in der Gynäkologie

Schindler¹

1977

Dtsch med Wochenschr

View full text Add to dashboard Cite

Struktur und Wirkungsweise dieser Antiandrogene sind anderweitig dargestellt (12). Für die Behandlung kommen zwei Antiandrogene in Betracht:Cyproteronacetat, Chiormadinonacetat. Die Wirkung dieser Substanzen kommt durch mehrere Mechanismen zustande:kompetitive Wirkung an den Androgenrezeptoren der Erfolgsorgane (Talgdrüsen, Haarfollikel),Beeinflussung der LH/FSH-Sekretion und damit zum Beispiel Verminderung der ovariellen Androgenbiosynthese (antigonadotrop),Beeinflussung der ACTH-Sekretion und damit zum Beispiel Yerminderung der Androgensekretion der Nebennierenrinde (anticorticotrop), Beeinflussung der Enzyme des Steroidstoffwechsels.Die Behandlung mit Antiandrogenen ist in mehrfacher Weise möglich: alleinige Anwendung, kontinuierlich und diskontinuierlich, zusammen mit einem Östrogen, diskontinuierlich, zusammen mit Östrogen-Gestagen-Kombinationen, diskontinuierlich, zusammen mit Corticoiden, kontinuierlich und diskontinuierlich.

show abstract

Clinical Uses of Antiandrogens

Cited by 12 publications

References 110 publications

Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor

Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor

Effects of Cyproterone Acetate (CPA) on Pituitary Gonadotrophin Release and on Androgen Secretion Before and After LH‐RH Double Stimulation Tests in Men

Behandlung mit Antiandrogenen in der Gynäkologie

Contact Info

Product

Resources

About