Susan's Place Transgender Resources

Community Conversation => Transitioning => Hormone replacement therapy => Topic started by: Lara1969 on February 03, 2014, 02:37:13 PM

Title: Interesting Anti Androgen
Post by: Lara1969 on February 03, 2014, 02:37:13 PM
My endocrinologist suggest to Start with low dose estrogen only. She suggested to add later chlormadinone acetate as anti-androgen if needed and the testosterone level stays to high. As far as I could read in different articles it is also a strong progestine. I am currently taking Dutasteride against my hairloss and a low dose progesterone cream on my bold spots which are no longer bold.
I read that CA is also strong in stopping synthesis of the DHT. So it is maybe the perfect medications. My next appointment with my end is in two weeks. Beforehand I would like to know if any girls takes CA and how does it affect you, the mood, breast growth???

Lara
Title: Re: Interesting Anti Androgen
Post by: KayXo on February 03, 2014, 03:57:38 PM
CLIMACTERIC 2005;8(Suppl 1):3–63

Pharmacology of estrogens and progestogens: influence of different routes of administration

"In contrast to MPA and megestrol acetate, the progesterone derivative CMA has some antiandrogenic
activity which corresponds to 20–30% of that of CPA."

CMA is short for chlormadinone acetate. MPA is short for medroxyprogesterone acetate (Provera). CPA is short for cyproterone acetate (Androcur).

Also according to

J Steroid Biochem. 1987 Oct;28(4):379-84.

"It should be added that MPA, megestrol acetate and CMA are completely devoid of antiandrogenic activity".

In this context, it means that CMA (chlormadinone acetate) does not block androgen from binding to androgen receptors like Androcur (cyproterone acetate) or Spiro does. Spiro is a weaker blocker than Androcur.

Also noted in this study which is a little worrying but should be investigated further
"In agreement with glucocorticoid activity, MPA, megestrol acetate and CMA caused a marked inhibition (45-64%) of adrenal weight".

Ann N Y Acad Sci. 2003 Nov;997:292-306.
Androgens and antiandrogens

"Cyproterone acetate (CPA) is the most potent antiandrogenic progestin, followed by dienogest, drosperinone, and chlormadinone acetate."

In conclusion, CMA reduces androgen like Androcur and Spiro but does not block androgen at receptors or at least, weakly as compared to Androcur, perhaps 1/5 to 1/3 that of Androcur.
Title: Re: Interesting Anti Androgen
Post by: KayXo on February 03, 2014, 06:14:32 PM
Regarding progesterone reducing conversion of T to DHT by inhibiting 5 alpha-reductase in tissue:

Cassidenti, D. L., Paulson, R. J., Serafini, P., Stanczyk, F. Z. & Lobo, R. A.

Effects of sex steroids on skin 5 alpha-reductase activity in vitro.
Obstetrics and gynecology 78, 103-107 (1991).


http://view.ncbi.nlm.nih.gov/pubmed/1828548

"progesterone is around 97% effective at competitively blocking the conversion of testosterone to DHT by using the 5-alpha-reductase itself"

"Progesterone, levonorgestrel, and norethindrone demonstrated 97 +/- 5.3%, 47.9 +/- 6.3%, and 59 +/- 4.6% inhibition, respectively, of genital skin 5 alpha-reductase activity at 10(-4) mol/L"

If one calculates, 10(-4) mol/L comes up to 31450 ng/ml. At this level, 97% inhibition is achieved. To compare, oral progesterone (Prometrium) in doses a little higher than typically prescribed to transsexuals gives peak level (on average) of 61 ng/ml, 520 times less than what was attained in the study where 97% inhibition was observed.

In other words, one would need an extremely (unrealistic) high dose of oral and topical progesterone to obtain a marked inhibition of T to DHT. Hence, I think that applying progesterone cream to your scalp is probably not necessary, useless and a waste of time.
Title: Re: Interesting Anti Androgen
Post by: KayXo on February 03, 2014, 06:18:10 PM
Be careful that chlormadinone acetate is not prescribed as part of a birth control pill (oral contraceptive) that also contains ethinyl estradiol, a very potent estrogen which increases risk of DVT (deep vein thrombosis) and pulmonary embolism.

Few transsexuals, if ever, use this anti-androgen. I'm under the impression that it is mostly popular in Germany as many studies mentioning it are in German. And you are from Germany as well. :)

It's very much like Androcur, a progestin with very similar properties, but somewhat weaker. 
Title: Re: Interesting Anti Androgen
Post by: Lara1969 on February 04, 2014, 12:21:31 AM
I am not sure if it available alone. But the side effects are way weaker than compared to MPA and maybe Spiro. Makes it interesting for me if I will need an AA.

And yes I am from Germany. :-)

Lara
Title: Re: Interesting Anti Androgen
Post by: KayXo on February 04, 2014, 07:24:42 AM
But if you take CMA in a birth control pill with Ethinyl Estradiol, you increase significantly your risk of health complications such as DVT. There is no reason to do this. Androcur and Spiro are better than taking Ethinyl Estradiol. Bicalutamide (Casodex) is also a good option as are LhRH analogues such as Lupron or Suprefact. Please be careful and do not assume that just because a doctor prescribes it, it is safe and good. Do your own research. Do take care. :) 
Title: Re: Interesting Anti Androgen
Post by: Lara1969 on February 04, 2014, 09:45:14 AM
CMA is available stand alone. I do not want to take EE.

Thanks for sharing your thoughts :-)
Title: Re: Interesting Anti Androgen
Post by: KayXo on February 04, 2014, 09:54:15 AM
Good! :)