youngbaldie
Established Member
- Reaction score
- 3
Would this help prevent the upregulation of testosterone seen with Avodart or Propecia?
"Cyproterone acetate (Androcur®, Cyprostat®, Cyproteron®, Procur®, Cyprone®, Cyprohexal®, Ciproterona®, Cyproteronum®, Neoproxil®, Siterone®) is an antiandrogen, i.e. it suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). Its main indications are prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions in which androgen action maintains the disease process. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female transgendered people.
Until the development of leuprolide, cyproterone was one of the few drugs used to treat precocious puberty. It was also used in animal experimentation to investigate the actions of androgens in fetal sexual differentiation.
In addition, cyproterone acetate has weak progestational activity (e.g., it acts like progesterone) and can be used to treat hot flushes. As part of some contraceptive pills (Diane®) it decreases acne and hirsutism (male-pattern hair growth)."
http://en.wikipedia.org/wiki/Cyproterone
This section confuses me:
"Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist with weak progestational and glucocorticoid activity. Some portion is metabolized by hydrolysis to cyproterone and acetic acid.[1] However, unlike many other steroid esters, cyproterone acetate is not extensively hydrolyzed, and much of its pharmacological activity is attributed to its acetate form.[2] Cyproterone acetate has approximately three times the anti-androgenic activity of cyproterone.[3]
Cyproterone acetate inhibits the steroidogenic enzyme 21-hydroxylase and to a lesser extent 3beta-hydroxysteroid dehydrogenase, both of which are needed to synthesize cortisol.[4] The blockade of 21-hydroxylase can also result in reduced production of aldosterone, the primary mineralcorticoid hormone. Mutations in the gene encoding 21-hydroxylase are fairly common in the human population, therefore some patients may be affected more than others. Although cyproterone has some glucocorticoid activity,[5] this is offset by the fact that cyproterone acetate inhibits cortisol production and can act as a competitive inhibitor of cortisol at the glucocorticoid receptor,[6] thus its adrenosuppressive effects are usually fairly minor.[7] However, since the glucocorticoid effects appear to be due to metabolites, rather than cyproterone acetate itself, the net effect may vary depending on the rate at which cyproterone acetate is metabolized.[8] The progestational and glucocorticoid effects reduce production of gonadotropins, which usually results in lower testosterone levels, however the blockade of adrenal 21-hydroxylase results in the accumulation of androgen precursors which may be converted to testosterone, reducing the efficacy of the antiandrogen treatment. Due to the possibility of increased adrenal androgens, cyproterone acetate is sometimes combined with the 5-alpha-reductase inhibitor finasteride, and studies of hirsutism treatment show increased efficacy of this combination over cyproterone acetate alone.[9] Some in vitro studies have suggested that cyproterone or cyproterone acetate may have a slight inhibitory effect on 5-alpha-reductase, however no significant reduction in DHT production has been observed in vivo"
Can someone explain this for me? Why is androcur effective at lowering testosterone but not DHT?
"Cyproterone acetate (Androcur®, Cyprostat®, Cyproteron®, Procur®, Cyprone®, Cyprohexal®, Ciproterona®, Cyproteronum®, Neoproxil®, Siterone®) is an antiandrogen, i.e. it suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). Its main indications are prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions in which androgen action maintains the disease process. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female transgendered people.
Until the development of leuprolide, cyproterone was one of the few drugs used to treat precocious puberty. It was also used in animal experimentation to investigate the actions of androgens in fetal sexual differentiation.
In addition, cyproterone acetate has weak progestational activity (e.g., it acts like progesterone) and can be used to treat hot flushes. As part of some contraceptive pills (Diane®) it decreases acne and hirsutism (male-pattern hair growth)."
http://en.wikipedia.org/wiki/Cyproterone
This section confuses me:
"Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist with weak progestational and glucocorticoid activity. Some portion is metabolized by hydrolysis to cyproterone and acetic acid.[1] However, unlike many other steroid esters, cyproterone acetate is not extensively hydrolyzed, and much of its pharmacological activity is attributed to its acetate form.[2] Cyproterone acetate has approximately three times the anti-androgenic activity of cyproterone.[3]
Cyproterone acetate inhibits the steroidogenic enzyme 21-hydroxylase and to a lesser extent 3beta-hydroxysteroid dehydrogenase, both of which are needed to synthesize cortisol.[4] The blockade of 21-hydroxylase can also result in reduced production of aldosterone, the primary mineralcorticoid hormone. Mutations in the gene encoding 21-hydroxylase are fairly common in the human population, therefore some patients may be affected more than others. Although cyproterone has some glucocorticoid activity,[5] this is offset by the fact that cyproterone acetate inhibits cortisol production and can act as a competitive inhibitor of cortisol at the glucocorticoid receptor,[6] thus its adrenosuppressive effects are usually fairly minor.[7] However, since the glucocorticoid effects appear to be due to metabolites, rather than cyproterone acetate itself, the net effect may vary depending on the rate at which cyproterone acetate is metabolized.[8] The progestational and glucocorticoid effects reduce production of gonadotropins, which usually results in lower testosterone levels, however the blockade of adrenal 21-hydroxylase results in the accumulation of androgen precursors which may be converted to testosterone, reducing the efficacy of the antiandrogen treatment. Due to the possibility of increased adrenal androgens, cyproterone acetate is sometimes combined with the 5-alpha-reductase inhibitor finasteride, and studies of hirsutism treatment show increased efficacy of this combination over cyproterone acetate alone.[9] Some in vitro studies have suggested that cyproterone or cyproterone acetate may have a slight inhibitory effect on 5-alpha-reductase, however no significant reduction in DHT production has been observed in vivo"
Can someone explain this for me? Why is androcur effective at lowering testosterone but not DHT?
