The pharmacology of antiandrogen

    • 7 posts
    August 15, 2010 6:42 AM BST
    As I know, antiandrogen blocks the target organs to receive testosterone secreted by testes,
    according to my recent blood test report, my testosterone level is 0.5 (normally 27.x - 34.7 for genetic male)

    But I have a question, will the activity of testes reduce since no any reception of testosterone? (i.e. testes secrete less testosterone)
    (beacuse I propose to reduce the dosage of antiandrogen......)
    • 1912 posts
    August 15, 2010 1:29 PM BST
    Yes and no. First off it depends on which antiandrogen you are using, along with the dosage you may be taking.

    I use bicalutamide (Casodex) which blocks androgen receptors in the brain which will eliminate the negative feedback loop of testosterone on the release of luteinizing hormone (LH). This in turn will lead to a dramatic increase in testosterone and estrogen levels Bicalutamide treatment will block the effects of rising testosterone levels but the effect of rising estrogen levels will remain unopposed and lead to feminizing effects. So in effect, the testosterone is still produced but travels through the body with no where to be received, the body then converts some of the excess testosterone into estrogen E1, and the remainder is flushed from the body. Testosterone level tests are useless because T is still being produced, just that it has no where to go. There is minimal effect on the scrotal area tissue allowing ample tissue availability for most SRS procedures.

    On the otherhand, spironolactone competes for receptors and effectiveness is based on dosage. So the more you use, the more blockage is achieved. I don't know enough to go into too much detail, but from what I have read and heard others describe, testosterone production is decreased and the testes become smaller. Depending on length of time of using the drug, recovery to the original state may be possible. So testosterone levels should be checked on a routine basis. If too much shrinkage in the scrotal tissue surrounding the testes occurs, this can potentially effect which SRS procedures are available and the maximum depth that can be achieved with surgery.

    There are other antiandrogens that have different modes of action and you cannot discount estrogen on its own can suppress testosterone if taken at sufficient levels. The drawback on each is there are side-effects which you need to be aware of.

    Maybe others here will describe their experiences with spironolactone or other antiandrogens. I have been extremely satisfied with Casodex. As always I recommend seeing a doctor while using any HRT medication. Casodex is deadly at higher dosages. Casodex 150mg was withdrawn from Canadian and UK markets because of the increased death rate. I hope that helps make my point on drug safety.

    Hugs,
    Marsha
    • 7 posts
    August 17, 2010 9:17 AM BST
    Thank you very much, Sue James.

    I think the antiandrogen that I have ben taking is the second type (i.e. blocking the receptors).
    However, will "reducing in production of testosterone" result in "testes shrinkage"?
    • 746 posts
    August 17, 2010 1:24 PM BST
    It takes a natal female 3-7 years to achieve full breast growth, and actually it can continue on and off for years after....so for us, the task is complicated by the need to eliminate or reduce or block testosterone as well as getting estrogens into our system, so immediate changes are not real. Could be just a repositioning of fat, but not true growth...
    Correct me if I'm wrong! Anyone?
    Traci
    • 1912 posts
    August 17, 2010 2:03 PM BST
    I have probably had some shrinkage in genital size but I would call it minimal, not that I had a lot to shrink in the first place and I have been using bicalutamide (casodex) for several years now along with what is considered a high dosage of estradiol cypionate. I have been on HRT for about 5 1/2 years now.

    As for breast development, this morning I had my third mammogram which was performed by the same tech I had the prior years. Her first comment was how amazing it is what hormones can do because my breasts look so natural. And for those who take expensive progesterone believing you need it for better development, I only tried it for a very short period and don't credit it with having any effect on my breast development. I am somewheres between a B and C cup, depending on the bra style.

    Hugs,
    Marsha
    • 871 posts
    August 18, 2010 1:20 AM BST
    I am not on any AAs. As Sue stated, the oestrogen should naturally cause the testosterone to reduce production. I think the less drugs one takes the better.
    • 1912 posts
    August 18, 2010 2:24 AM BST
    The whole principle of using an antiandrogen is to increase the effectiveness of the estradiol medication that is being taken. You cannot write-off the benefit of antiandrogens when they may reduce the need for higher doses of estrogen. I have known gals who take 50mg of spironolactone and others that take 400mg to control testosterone levels. Likewise, a given dose of estradiol will not offer the same testosterone suppression for everyone. So just because any of these options works for a gal here, the only way you will know what works for you is if you have lab tests done to verify results. It would be a pity to be a year or so into transition and find out your development is not only slow, but actually non existent because your hormone levels have not been changed due to improper HRT dosages.

    Penny and Sue noted that "the oestrogen should naturally cause the testosterone to reduce production." The question you should be asking is "Will it reduce testosterone production enough?" A reduction from 350 to 300 is a reduction, but it is meaningless in the big scheme of things when you should get down below 50 if not 15. No wonder so many gals want breast augmentation because hormones don't appear to be giving them the development they hoped for. But, but, but it worked for so and so. You are not so and so. See a doctor, find the lowest dosage that gives you the greatest results.

    Hugs,
    Marsha
    • 530 posts
    August 15, 2010 11:51 PM BST
    There are two types of anti-androgen, one blocks production, one blocks the receptors. I believe but might be corrected that the latter is now the preferred method.
    As with most forms of drugs, after a period of time the body itself decides what it is going to do. So if and when it realises that testosterone is 'no longer required', it will begin to shut down production of it's own accord. This will also start to happen if comparatively large doses of oestrogen are introduced.
    This is why medical supervision should always be in place, and unless one is thinking of taking things further, such as eventually to GRS, one should be very careful and have regualr tests to ensure nothing permanent occurs.

    I was on oestrogen with a blocker, which definitely increased the effects, which pleased me greatly. However, after a couple of years, I could almost do without, for the reasons stated above.

    So yes, continued use is likely to reduce the natural production of testosterone.
    • 530 posts
    August 17, 2010 1:13 PM BST
    From personal experience, I experienced a definite reduction in size of all 'parts', not just the testes, and have spoken to many others who confirmed they had as well.
    There are obviously exceptions to most things, so there will be some who do not experience any changes at all, but my money would be on you will.
    Bear in mind we are not talking weeks but on average about two years before there are noticeable effects.
    If you are including oestrogen in the mix, the same sort of timescale applies to any changes in the breast area. Though once again, there are those who will claim they have breasts after a couple of doses - this is unusual and rare.