Susan's Place Transgender Resources

In natal men excess testosterone gets converted to estrogen by enzymes (though I haven't been able to find what they're called).  Does anyone know which enzymes these are?  My other question is that do you think it would be possible to increase the amount of conversion enzymes to more readily convert testosterone into estrogen? 

Well, after scanning the interweb, I came up with this... which may answer your first question.

From: http://www.vrp.com/articles.aspx?ProdID=art2341&zTYPE=2

Testosterone is subject to enzyme-induced transformation, a contributor to overall lowering of available testosterone.  One of the most commonly discussed enzymes involved in this conversion is 5 alpha-reductase. This enzyme is responsible for converting testosterone into dihydrotestosterone (DHT). DHT is thought to be responsible for the signature male health problems of prostatic hyperplasia and male pattern hair loss (in men that are genetically susceptible).4 DHT binds to androgen receptors with greater affinity than does testosterone. In fact, DHT binding is thought to be four times more potent (in terms of receptor activation) than testosterone in this regard.

Testosterone not transformed to DHT may then be converted by yet another enzyme known as aromatase. Also known as estrogen synthetase, it converts the testosterone molecule into the closely related, but vastly different estradiol molecule—an active estrogen metabolite. Aromatase is a cytochrome P-450 enzyme that catalyzes the rate-limiting step in estrogen synthesis, which is the conversion of androgens (androstenedione and testosterone) into estrogens. A significant amount of estrogen in men is produced via the aforementioned enzymatic conversions that most often occur in the adipose tissue, liver, and brain.

As for your second question, I've only been able to find patents for aromatase activators (like this (http://www.freepatentsonline.com/y2006/0127412.html) one). So I don't know whether anything like that is available or not.

it does sound like a good idea though....
Estrogen and anti-androgen all in one  :D

Thank you so much! That aromatase activator looks like a pretty cool idea.

Bicalutamide, bay-bee!

Lia

There is a sort of way to increase T to E transformation
since fats contain plenty of aromatase enzymes.
But, the problem is that if T levels are high, fat accumulations
will mostly be around the abdomen, which wont help your
curves. There is a reason why fat men have man boob,
fat goes there and on their legs because of the increased E in their system.

If you look at fat men and fat women, they look remarkably similar.

Higher levels of middle fat in women has an impact on insulin which
interfeers with E normal mechanism for fat storage and fat is
stored in the manly pattern.

In women losing weight, they'll
lose tons from the mid section if they eat foods that don't raise insulin
levels (proteins, vegetables, eating often) and exercise.

Quote from: Keira on July 16, 2008, 12:30:28 AM

There is a sort of way to increase T to E transformation
since fats contain plenty of aromatase enzymes.
But, the problem is that if T levels are high, fat accumulations
will mostly be around the abdomen, which wont help your
curves. There is a reason why fat men have man boob,
fat goes there and on their legs because of the increased E in their system.

If you look at fat men and fat women, they look remarkably similar.

Higher levels of middle fat in women has an impact on insulin which
interfeers with E normal mechanism for fat storage and fat is
stored in the manly pattern.

In women losing weight, they'll
lose tons from the mid section if they eat foods that don't raise insulin
levels (proteins, vegetables, eating often) and exercise.

God Keira I love it when you weigh in on this kind of stuff!!! I'm just starting HRT (estradiol & spiro) and still have weight to lose, great info...and great post Maddie :-*

Quote from: Kiera on July 16, 2008, 05:55:40 AM
Tres cher Lia!

Well, yes, it can be.  Since we're not allowed to discuss dosages here, I'm not able to defend my position, but I will just say that at the effective dose it can be quite affordable.

Lia

The only drawback seems to be the price. At $6.66/tablet it's pretty pricey!! And that was a Canadian company that would fill the script. Possibly because of its use in oncology. Just a guess but USA proces would be steeper still.

Spiro, oth, is about $ 0.99/tablet.

I'd imagine that for some the difference would be a reason not to use Bicalutamide.

As usual w/ androgen-blockers one would also need to be aware of osteoporosis and heart problems developing. The Wiki article Kiera quoted also suggests an LHRH would help reduce that. But an LHRH is also gonna reduce the effects that MTFs want to see.

Nichole

At the price you quote, Nichole, I agree.  Too expensive.  There are, however, generics, which one could take which would cost even less than the tablet of Spiro you mention.  My apologies if that's vague; I'm trying to be good and not break any rules.

Lia

And you are. I understand that as I am trying not to as well! :laugh:

But the swift hustle I did showed me that the lowest price I found (checked 6) for a generic was $3/tablet. That's still about $2 above the going rate for Spiro. There may be others, like I said it was a quick hustle.

N~

Wow, this is all great stuff for when I get to start HRT.  I have to wait til I can get them prescribed to me and I don't want to do a DIY.  I noticed.  As far as mixing things to gain the effect of a more expensive pill, do endocrinologists do that sort of thing?

Its not low androgen that causes bone loss but LOW ESTROGEN (even in men).
Shhs, I just wish this myth would be soundly defeated once and for alll.

In men, part of the free T (unbinded to T receptors) is aromatised into E, which helps
ward against bone loss. Since T levels decline very slowly, E remains usually high enough
to prevent bone loss until the late 60's.

In women, crashing E levels in the mid 40's lead to increase mid fat accumulation and
increased risk of osteoporosis. The conversion of unbinded free T from the adrenals
by fats is not enough to help the bones. Ironically, in a women, an anti-androgen
would actually help the bones by increasing the level of T available for conversion
to T (since T could not bind to T receptors) and the adrenal level of T is not
controlled by the free blood level of T.

I men, using an anti-androgen increases free T (unbinded T) and thus the pituitary
gland instructs the testes to reduce T output. If the anti-androgen level is high
enough, there will always be too much unbinded T produced by the testes and
through a retroactive loop, the testes output will be
eventually reduced towards zero.

Eventually, the unbinded T levels become too low for a proper conversion to E
(this is particularly true if someone is thin and thus have a low level of aromatased
activity). So a man taking anti-androgen and nothing else will soon be
in the same situation as a post menauposal women taking an anti-androgen.

Quote from: Keira on July 16, 2008, 04:29:04 PM


Eventually, the unbinded T levels become too low for a proper conversion to E
(this is particularly true if someone is thin and thus have a low level of aromatased
activity). So a man taking anti-androgen and nothing else will soon be
in the same situation as a post menauposal women taking an anti-androgen.

So, that's why I ended up getting Osteoporosis at 50 y/o. Always have been thin and I've have never taken anti-androgens.



Dawn

Quote from: Kiera on November 02, 2008, 10:49:04 AM

Quote from: Purple Pimp on July 15, 2008, 08:08:11 PM
Bicalutamide, bay-bee!

Lia, after a recent change of med routine due primarily to risks associated with *achm* age I am now using Casodex (you too?) & estradiol valerate IM and according to some follow up reading which I always do whenever a change is implemented is it true that bicalutamide blocks DHT binding (if not "conversion") thus dutasteride is no longer required as well?

Quote from: wikipeadiaOther anti-androgens include bicalutamide, flutamide, and nilutamide. Unlike the two medications above[Spironolactone & Cyproterone acetate], these do not lower testosterone levels but rather prevent testosterone and dihydrotestosterone from binding to androgen receptors.

While I find it incredible that I feel so great for once and am actually ready to stop taking pills every day cost wise as well (over time) this appears to be the best therapy I've experienced so far . . .

Yes i would like to also know that if you switched to Bicalutamide or Casodex would that mean no need to also take dutasteride. I used to take genuine Avodart but now take either Duprost or Duta's depending on who's doing the best price that month but if i didnt need to also take this is would put it back into the spiro price bracket and im sure i could get either of those scripted.

As far as I know, casodex does indeed invalidate the need for other DHT blockers.  I can't really say any more than that, since it's been forever since I did the research on it and no longer take casodex since I'm post-op now (I switched to fincar instead to take care of the DHT since I didn't need to block testosterone anymore).

Maybe Keira is still around and can comment further?

Lia

 I have always believed that anti-androgens were sufficient DHT blockers because they compete for the same androgen receptor.
and as stated previously in this thread the Blocked T that has not converted to DHT can be converted to E. But the unbound
DHT cannot be converted to E, and until the T production is shut down, a little DHT is alot IMO. That is why I take Avodart yep yep yep! to reduce the amount of unbound DHT, I certainly don't want that stuff lingering around.

Nicole