Oral spironolactone - Why is it so quickly demonized here?

[Jack]

I've been reading up on oral spironolactone , and I don't understand why people go ragin' apeshit on someone whenever he considers trying it.
Over on the women's forum it's regarded as one of the weaker anti-androgens , and some of them did hormone testing and it only reduced Testosterone slightly on 200mg doses !
Flutamide and Androcur works way better in this regard.
Also in one large-scale spironolactone study for men in heart failure , gyno was only reported in about 1-2% of cases (mean dosage about 40mg).
So if Testosterone isn't affected much but androgen receptors are still blocked by spironolactone , making this a possible nice addition to 5ar inhibitors , why are people so scared by low doses of oral spironolactone?
I just want to understand WHY it is regarded as foolish in these forums.

 

[iwantperfection]

ok... you have found out its not a big deal with women taking it...add this to the fact males take it during the sex change process...do the maths. :whistle:

in simple terms taking oral spironolactone can result in turning into a woman. lol. not literally but breast tissue grows etc. :shock:

your choice :woot:

 

[Jack]

I was only bringing up the women to show that spironolactone effects testosterone only slightly but does effect the androgen receptors .
The highest gyno percentage for spironolactone I could find anywhere was 13 % in a japanese study but they were using 200mg. It's much less for 25-50mg.

 

[Cassin]

do some more research and you will see why

 

[casperz]

I was totally against it after doing a lot of research and reading reports
of transsexuals that took as little as 50mg/day to achieve their desire
to reduce testosterone to female levels. However the effect on testosterone
seems to vary from person to person. The recommended dosage for
someone changing their sex is 200mg/day. But some take less and some take
more from what I can tell. But if the recommended dosage is 200mg/day I
don't what to be anywhere near that level.

I also think most that have started oral spironolactone at any level have stopped
after a year or two or so due to side effects. I've not heard anyone come
forward that has been on longer that I recall.

With all that said I've come around a little and I've considered using up to
50mg/day with careful testing of testosterone levels before and during
treatment. But the big sticking point for me is that in reading a lot of
the info on the web about transsexuals they all say that results from the
use of spironolactone become permanent after about six months. Right now I just don't
think messing with your hormones is a good idea if the changes are
permanent after stopping the spironolactone.

Another issue I had is once I started and it actually worked very well what
happens if my T level were to crash and I had to stop. I lose all that
re-growth I assume.

 

[Bryan]

Over on the women's forum it's regarded as one of the weaker anti-androgens , and some of them did hormone testing and it only reduced Testosterone slightly on 200mg doses !

Those were _women_ who claimed that their testosterone levels were reduced slightly by 200 mg/day of oral spironolactone?

So if Testosterone isn't affected much but androgen receptors are still blocked by spironolactone , making this a possible nice addition to 5ar inhibitors , why are people so scared by low doses of oral spironolactone? I just want to understand WHY it is regarded as foolish in these forums.

My only problem with it is that ultimately, I don't see much point in taking only 25-50 mg/day. While I'm sure that such a low dose would be pretty safe, I doubt that it's going to do much at blocking androgen receptors. You can't simply reduce the dose and fool Mother Nature into giving you all the DESIRED effects you want, while reducing or eliminating the SIDE effects!

 

[Bryan]

I was totally against it after doing a lot of research and reading reports of transsexuals that took as little as 50mg/day to achieve their desire to reduce testosterone to female levels.

I'd probably laugh out loud at anybody who made such a claim.

By the way, casperz, since you're so terrified of having your testosterone reduced to female levels, I'm surprised you haven't considered using small doses of flutamide, instead of spironolactone. Flutamide definitely won't interfere with the synthesis of testosterone. In fact, it will actually INCREASE it!

 

[$tackz]

^^ Describe the mechanism in which it increases it, please.

 

[casperz]

I'd probably laugh out loud at anybody who made such a claim.

Obviously you don't believe their statements so I ask why would they have a
reason to lie? They are transsexuals, if they want to take 500mg a day and
never get an erection again they would not care. It sounds like you put
much more weight into studies than first hand accounts or you have some
other agenda.

By the way, casperz, since you're so terrified of having your testosterone
reduced to female levels,

Not terrified at all Bryan, just not gonna do anything that would.

 

[casperz]

By the way, c'mon Casperz, TS take a lot of more potent stuff than spironolactone to achieve T reduction. spironolactone is just a part of the treatment.

Nope, not really. A typical regime for a TS is spironolactone up to 200mg a day to
reduce testosterone and 17b estrogen to increase estrogen. That's it.

Also there are men (called eunuch's) that want to be chemically or
completely castrated for various reasons and to "try out the lifestyle"
all they take is spironolactone at the same doses as the transsexuals.

Oral spironolactone is not as benign even in low doses as what you guys think it is.

 

[casperz]

Read the abstract please. It's said that "In addition there were no changes in circulating serum androgen concentrations", at 100mg daily.

Um... it was a study of females that do not have testicles or much T. Do
you really think that has any application to males?

I don't trust Internet testimonials (even if they are sometimes very useful). I trust serious scientific stuff.

These are not testimonials I'm talking about, these are transsexuals
helping other transsexuals telling each other what their experience is. Just
like we do here about finasteride, minoxidil and all the other crap. I go back
to my question, why would some lie in that situation? It's not like their
selling hairloss products, they have zero to gain.

Studies are useful but everyone reacts differently. Just look at all the
people that finasteride does not work for. Oh... BTW... have you heard about
all the "fake" studies that were done just to get the cash to do them?
It happens ALL the time.

 

[neis]

Casperz, I guess Brian and I (I'm currently reading up quite a bit on this subjet) can show you several studies that claim that spironolactone doesn't affect androgen serum level.

Just right now I'm reading this one http://www.pubmedcentral.nih.gov/picren ... obtype=pdf

Read the abstract please. It's said that "In addition there were no changes in circulating serum androgen concentrations", at 100mg daily.

I highly doubt someone can reduce his T level with spironolactone. In my case, I didn't !
I don't trust Internet testimonials (even if they are sometimes very useful). I trust serious scientific stuff.

seaback,
You might want to consider equol as well. I have been researching this Equol avenue and I do not understand why the crew here hasn't looked more deeply into this avenue. I think it works much the same way as oral spironolactone.

Here is a study I found:
http://www.biolreprod.org/cgi/content/full/70/4/1188

 

[Petchsky]

viewtopic.php?f=23&t=52222

See Casperz thread on oral spironolactone

 

[Bryan]

^^ Describe the mechanism in which it increases it, please.

The brain's general response to antiandrogens is to send the chemical signal (LH) to the testes which tells them to start making more testosterone. It does that as a means of maintaining a homeostasis of androgenic stimulation. For example, if the brain senses too much androgen for whatever reason, it will put less LH into the bloodstream, and testosterone synthesis will decline. If it senses too little androgen (which is what would happen if you use a systemic antiandrogen), it will put more LH into the bloodstream, and testosterone synthesis will increase.

The reason that spironolactone decreases testosterone production (at least with large doses) is that spironolactone does more than just function as an antiandrogen. It also interferes chemically with the testosterone-producing machinery in the Leydig cells of the testes. If you give a large oral dose of spironolactone to a man, his testosterone will decline despite the antiandrogenic effect of the drug. But I'm unsure about what happens at much smaller doses: does the antiandrogenic effect win out, or does the testosterone-synthesis-suppressing effect win out, or is it a draw? I don't know the answer to that question.

 

[Bryan]

Of course spironolactone doesn't deal with testosterone production, so it won't decrease the T concentration in your body.

But spironolactone _does_ deal with testosterone production (although that wasn't an intended effect)! Besides being an antiandrogen, it also interferes with the chemical mechanism for synthesizing testosterone, which is why T is lowered significantly at larger doses.

But... I really would like to know the binding affinity of those antiandrogens to the AR. DHT has the highest affinity (of course), but which antiandrogen comes in second position ? From the literature I've read, results are contradictory. Skipping the new pure antiandrogens, it's between flutamide and cyproterone acetate. spironolactone would be a weak antiandrogen only.

In a study a while back which tested the RBAs (relative binding affinity) of numerous substances and drugs (about 30 or 40 altogether) in human cells, spironolactone came in with the highest RBA of all of them. It had about 2/3 the RBA of DHT, if I recall correctly. I don't think cyproterone acetate and RU58841 were included in the test, but flutamide was, and its RBA was much lower than that of spironolactone.

Of course, the RBA of an antiandrogen is just one factor that determines its relative potency and overall effectiveness. There are others, too, like the half-life and the general level of toxicity.

 

[Bryan]

I'd probably laugh out loud at anybody who made such a claim.

Obviously you don't believe their statements so I ask why would they have a reason to lie? They are transsexuals, if they want to take 500mg a day and never get an erection again they would not care. It sounds like you put much more weight into studies than first hand accounts or you have some other agenda.

I'm not necessarily saying they're LYING, I'm saying I doubt that they know what they're talking about.

We've already been over this before: almost ALL those guys were taking other powerful drugs, along with the spironolactone. There's no doubt in my mind that if their T levels were being suppressed so much, those other drugs were making major contributions to that effect. The ONLY way you're going to get me to believe that a small dose of spironolactone like only 50 mg/day can reduce testosterone to "female levels" is if you find a clinical study which actually documents that claim. THEN I will believe it.

By the way, casperz, since you're so terrified of having your testosterone reduced to female levels,

Not terrified at all Bryan, just not gonna do anything that would.

Why didn't you reply to my suggestion about flutamide?

 

[Bryan]

A typical regime for a TS is spironolactone up to 200mg a day to reduce testosterone and 17b estrogen to increase estrogen. That's it.

What makes you think that a TS takes spironolactone specifically to reduce testosterone levels? How do you know it's not just to reduce the effects of androgens by working as an antiandrogen?

 

[Bryan]

seaback,
You might want to consider equol as well. I have been researching this Equol avenue and I do not understand why the crew here hasn't looked more deeply into this avenue. I think it works much the same way as oral spironolactone.

Huh?? No, there's no similarity at all to oral spironolactone. Equol isn't an antiandrogen at all. What equol closely resembles is finasteride and dutasteride, which is why I've never been particularly interested in it (finasteride and dutasteride are cheaper, and much easier to obtain than equol).

Equol doesn't work in exactly the same way as finasteride, but the overall EFFECTS are almost exactly the same.

 

[follicle84]

But spironolactone _does_ deal with testosterone production (although that wasn't an intended effect)! Besides being an antiandrogen, it also interferes with the chemical mechanism for synthesizing testosterone, which is why T is lowered significantly at larger doses.

Brians right. Testosterone is also an androgen so it would make sense that an anti androgen such as spironolactone would effect testosterone levels.

 

[Bryan]

Not all antiandrogens have the same chemical properties as spironolactone: large doses of spironolactone LOWER testosterone, large doses of flutamide RAISE it.