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Spironolactone vs Cyproterone acetate

Started by Nevara, September 24, 2014, 10:33:10 PM

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Nevara

I know in the US, only Spironolactone is prescribed because Cyproterone isn't FDA approved, but from what I've read from non-Americans is that almost all of them are given Cyproterone Acetate as part of HRT.

Using Spironolactine in MtF HRT seems almost unheard outside of the US. The advantages I've found between the two seems to be that Cyproterone lacks the diuretic effect of Spiro, which really isn't that bad after after the first week or so (at least it's pretty much leveled off for me) and some studies on Cypro show it binds to and reduces androgen receptor activity slightly better than Spiro at similar doses. Seems like we need to take higher doses for the same effect.

Are we Americans getting stuck with the inferior option for HRT? For anyone that's used both, did you find one giving you more effective physical results?
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Flan

It's a trade off of potential kidney damage (spiro) and liver damage (cipro) and the FDA decided that the increased liver risk isn't worth allowing cipro to be approved in the US. They act in different ways so there will likely be different perceived results. For me spiro was more effective in controlling symptoms.
Soft kitty, warm kitty, little ball of fur. Happy kitty, sleepy kitty, purr, purr, purr.
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Cindy

I went on Spiro rather than CA. One side effect of CA is triggering quite sudden depression. I decided I would rather pee a bit more than be even more depressed :laugh:

As it happens I had no side effect from Spiro except for a beneficial lowering of BP.
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kelly_aus

Quote from: Cindy on September 24, 2014, 11:41:33 PM
I went on Spiro rather than CA. One side effect of CA is triggering quite sudden depression. I decided I would rather pee a bit more than be even more depressed :laugh:

I just went with CA.. And I got the depression.. To start with, I just stopped the CA for a while.. After which my gyno and I fiddled doses until we found a happy medium.
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Carrie Liz

Yeah... I've been on both, and CA totally kicks your butt emotionally. I've never had such extreme highs and lows before, where Spiro alone is much more slow and steady. I got faster feminization on CA, but I don't know if the extreme highs and lows are worth it.
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Nevara

Quote from: Carrie Liz on September 25, 2014, 12:09:16 AM
Yeah... I've been on both, and CA totally kicks your butt emotionally. I've never had such extreme highs and lows before, where Spiro alone is much more slow and steady. I got faster feminization on CA, but I don't know if the extreme highs and lows are worth it.

More feminization is nice and kinda what I was interested in given how long the process is already. Emotional instability doesn't sound like fun though.

I don't really have a choice now but I'll be abroad for a year in a few months so I was considering my options. My current (us) doctor had no idea about CA at all.

I really wish this process would be more doctors educating us rather than the other way around. 
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KayXo

I took CPA pre-op, I live in Canada. Felt great on it, feminization was good but if I had to redo, I would have asked for bicalutamide instead. Fewer side-effects, safer overall and VERY strong anti-androgen, also approved in the US.
I am not a medical doctor, nor a scientist - opinions expressed by me on the subject of HRT are merely based on my own review of some of the scientific literature over the last decade or so, on anecdotal evidence from women in various discussion forums that I have come across, and my personal experience

On HRT since early 2004
Post-op since late 2005
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Richenda

I came on here to comment about Spiro but need to mention about bicalutamide. It is unproven that Bicalutamide is 'safer overall.' In fact there are plenty of potentially fatal side effects, one of which I've managed to get (interstitial inflammation of the lungs) so I've been taken straight off it. On this thread there are links to the dangerous sometimes life-threatening side effects of bicalutamide which is untried and untested as a treatment for MtF's. I'm just warning forum members to exercise extreme caution: https://www.susans.org/forums/index.php?topic=210339.new;topicseen#new
Some people may be fine with it, but it doesn't help that your physician may not have heard of it, let alone as a transgender treatment.

As for Spiro, like a few other people I had an awful reaction to it. I was one of those whose blood pressure dropped through the floorboards and it very nearly killed me: when I woke up my heart was hardly beating and I couldn't stand up. It's a drug that the GiC in Britain won't administer for MtF's.

Before you think I'm an out-and-out pansy, I've had no issues with max finasteride, a drug I've got along with very well. That's a good example of what I'm getting at here: some people have a nightmare with fin. One person's medicine may be another's poison, so just please please don't take as gospel what someone tells you is fine and safe. It might be for them. It might kill you. Always get medical guidance and be tested.

Which I guess leaves CA (by the way I believe the abbreviation 'cipro' is normally reserved in the medical community for  ciprofloxacin).

Or ... orchiectomy. Which is basically what I am going ahead with now. I'm sick and tired of almost killing myself with drugs that don't suit my system.

xx
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KayXo

Please consider doses when mentioning side-effects with this drug. Men who take it due to prostate cancer take high doses, transsexual women usually take much less.
I am not a medical doctor, nor a scientist - opinions expressed by me on the subject of HRT are merely based on my own review of some of the scientific literature over the last decade or so, on anecdotal evidence from women in various discussion forums that I have come across, and my personal experience

On HRT since early 2004
Post-op since late 2005
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kelly_aus

Quote from: Richenda on June 06, 2016, 12:20:02 AM

Which I guess leaves CA (by the way I believe the abbreviation 'cipro' is normally reserved in the medical community for  ciprofloxacin).

Funny thing is, those that can spell will shorten cyproterone acetate to cypro.

I've only ever used cyproterone acetate, I have had to make an adjustment to dose when the depressive side effects. I've also had 1-2 week periods where I didn't take it.. Even after 2 weeks without taking it, my T level didn't increase.
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Richenda

I'm on low CA / Cyproterone Acetate (;) ) now and seem to be fine with it. So that will be the first true anti androgen that has worked for me. It's only for 6 weeks prior to my orchie just to keep the T and E levels close to female, thus lessening the shock when the testicles are whipped out. Can't wait.
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kaitylynn

No kidding on the Spiro blood pressure drop...I went in to get a test done at my endo's office that was a different appointment not related to HRT.  They took my BP prior to the test and it came out 130/80.  I had an hour and a half till my Endo appointment and at my normal time to take my Spiro.  Right after leaving the first doctor's office, I took my 100mg.

A little over an hour later I was given the prelims for my Endo appointment and my BP was 117/70.

I have to be careful for a few hours after taking it when I get up, so I usually take it after I am off work.

Spiro has been plenty effective in blocking out my T, which is now in normal female ranges and I am not sure what effect beyond that suppression that an AA provides.  What feminizing effect does one provide over the other?
Katherine Lynn M.

You've got a light that always guides you.
You speak of hope and change as something good.
Live your truth and know you're not alone.

The restart - 20-Oct-2015
Legal name and gender change affirmed - 27-Sep-2016
Breast Augmentation (Dr. Gupta) - 27-Aug-2018
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Richenda

Hi Kaity,

I'm not qualified to comment on your final question except that as I'm sure you know there's the debate between T blockers (CA, Spiro, bicalutamide, flutamide) and those which block T to DHT (dutasteride and finasteride). As DHT is 9x more powerful than T I would argue that DHT blockers are the most potent form of anti androgen. Then there's those which tackle the brain first: the GnRH inhibitors. An orchiectomy removes 95% of testosterone production.

You spiro bp drop tallies with mine except mine went through the floor. I woke up one morning with my heart scarcely beating: no exaggeration. It was horrendous.
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kaitylynn

Holy moly, Richenda!  I have never gone out like that and it sounds super scary!  Passing out is bad enough.

The thought I had was exactly that on the Spiro vs. Finastride.  I have several sisters local that use Finastride and they have had good results so far.  They have mentioned feeling really moody on it though, which is something that I have not had to deal with using Spiro.
Katherine Lynn M.

You've got a light that always guides you.
You speak of hope and change as something good.
Live your truth and know you're not alone.

The restart - 20-Oct-2015
Legal name and gender change affirmed - 27-Sep-2016
Breast Augmentation (Dr. Gupta) - 27-Aug-2018
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Richenda

Yeah it was really awful Kaity. So frightening. My pulse went below 30  :(

The one consistent anti androgen medicine I have taken right through is finasteride. I'll tread carefully here but I've been similar to my brother's prostate intake level if that makes sense. I've not noticed any bad side effects apart from some sinus-type headaches. This is where one person's medicine can be another girl's poison because I know lots of people have depression from finasteride (my brother does).

In terms of the effect I have almost no body hair now and significant breast enlargement, though that's presumably been helped by oestrogen.

My journey with other anti androgens has been a nightmare. In addition to the spiro issue, dutasteride spun me out badly and bicalutamide caused a dangerous reaction. I'm currently on low dose Androcur (CA) which seems okay so far.
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KayXo

Quote from: Richenda on June 17, 2016, 10:57:37 PMAs DHT is 9x more powerful than T

https://en.wikipedia.org/wiki/Dihydrotestosterone

"DHT has two to three times greater androgen receptor affinity than testosterone"

"The dissociation rate of testosterone from the receptor is five-fold faster than DHT.[5]"

QuoteDHT blockers are the most potent form of anti androgen

They are called androgen blockers and block all androgens to a certain degree. Some also reduce androgen production such as Spiro and cyproterone acetate.

QuoteAn orchiectomy removes 95% of testosterone production.

Prog Brain Res. 2010;182:321-41.

"after castration, the 95-97% fall in serum testosterone does not reflect the 40-50% testosterone (testo) and dihydrotestosterone (DHT) made locally in the prostate from DHEA of adrenal origin."

Despite this, we still have less than pre-menopausal women because their ovaries are another source from which androgen is produced.
I am not a medical doctor, nor a scientist - opinions expressed by me on the subject of HRT are merely based on my own review of some of the scientific literature over the last decade or so, on anecdotal evidence from women in various discussion forums that I have come across, and my personal experience

On HRT since early 2004
Post-op since late 2005
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anjaq

I have to add something to this discussion.
If you give two options, I give you a third: No antiandrogens! There are countless patient reports and even a few minor studies that show that Testosterone can be supressed in 50-99% of the cases with estrogen and progesterone alone. The hypothalamus has a feedback mechanism that is activated either by testosterone or by estrogen+progesterone and will thus reduce the amount of requested hormones if there are sufficient hormones in the blood. So if your estrogen levels are high enough, testosterone will drop anyways. Those who got estradiol injections as I did in the late 1990ies almost never need antiandrogens as T was very low with that sort of estradiol in the blood. Of course, nowadays its not injections anymore but pills and transdermals and with pills taking adequate dosages is hard - with patches or gel however, an increased estradiol dosage that is high enough for the body to shut down its own hormone production is easily reached and not dangerous since transdermals do not increase liver issues and are not known to increase cancer risk or DVT risk significantly either.

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Richenda

That's very interesting Anjaq. It ties in anecdotally with conversations I've had out here in Thailand with MtF transsexuals. I've lost count the number of times I've been told that after a few years they no longer take Androcur (Cypreterone Acetate). This is invariably from girls who look totally female. I can well believe that estrogen can act as a powerful anti androgen. It's a shame that there aren't long term studies on this. I have a hunch that a short period of so-called anti-androgens followed by continuous estrogen might be sufficient for our needs.

Re my earlier post I also think in blood tests we possibly get fixated on T levels when it's DHT that is 9x more powerful. Drugs like Dutasteride, Finasteride and Bicalutamide effectively block the latter not the former. (Bic elevates endogenous estrogen due to inhibiting androgen feedback on GnRH secretion by the pituitary gland which actually elevates serum testosterone, but it stops having masculizing effects because the receptors are blocked: mind you I think it's a potentially dangerous drug.)

The other thing is that perhaps we also sometimes focus on those tests without looking at the other obvious body signs? After 18 months on finasteride and estrogen and only inter-mittent anti-androgens I have virtually no body hair and significant breasts. I lactate daily.

Anyway, I've pretty much decided I'm having an orchiectomy next month. That will take care of the T issue as it wipes out 95% of testosterone. In theory I might continue on a much reduced dose of finasteride but it's going to be important to watch for osteoporosis.

p.s. and androgen comes from the Greek andras for man so anything countering male hormones is an anti androgen including estrogen :)
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anjaq

Androgen is a wrong word because all the so called androgens are also existing in women. Did you know that a woman has usually more Testosterone than Estrogen in her body? And younger women have more than older men? Its really fascinating once you look into it. The distinction of Testosterone = Man and Estrogen = Woman is a fairytale, both hormones exist in both and are needed in both.

The people I spoke with used estrogen only from the beginning - no antiandrogens ever, not even for some months. Although for some this was the standard therapy so they had CPA for a while and then stopped. I cannot describe details here because of the rules (no dosages etc...), but it does work with slightly higher estradiol than recommended by many endocs - although many other endocs are totally fine with those dosages as they are far from crazy high. Just the maximum dosage of patches usually works fine with most.

the mechanism , as you mention GNRH , is this:


As you can see, the hypothalamus (GNRH) and pituary gland (LH and FSH) do regulate the bodys hormones. If there is not enough Tesosterone in the body, it will ramp up production until it registers enough testosterone again. This is regulating testosterone production and blood levels in males. However the glands do not care if it is testosterone or estrogen. For women it is more complex but essentially  also there more estrogen and progesterone in the blood means less LH and FSH and thus a downregulation of internal hormone production. Now the neat thing is - since the glands do not distinguish that much between testosterone and estrogen, they give the signal "I am full" when one of the two is high enough - and reduce LH and FSH and GNRH and thus the bodys own hormone production. This is why estrogen (maybe in combination with progesterone) alone almost always wil suppress T.
[this is a VERY simplified version of what is happening, so please do not be thrown off if you read about some details being different elsewhere, especially regaring the female hormone system which obviously is cyclical]

Now what many trans women seem to seek however is demaskulinization - no libido and erections anymore, reduced body hair etc. This often is reached only if you drop testosterone levels below that which is normal for females. So then, antiandrogens are loved because they can do that, but beware of the price - remember also women have a libido and life without it is not that great and that testosterone is also important for muscle growth (including growing new muscles in a more feminine shape) and many other body functions. When yout pubic hair starts to become very thin, its a warning sign, since only old and very young women have little pubic hair (unless you remove it of course ;) )

Richenda - your description was warning signs placed over it in my eyes. Please let a doctor do your blood tests soon - and be sure to measure prolactin! Lactating may be somewhat fun and a nice affirmation of being female, but it is also a sign of elevated prolactin levels usually and this is not healthy. Antiandrogens are known to increase the prolactin, especially Androcur which can cause Prolactinoma, a tumor of the pituary gland that produces prolactin.

Last but not least - be very careful with long term use of DHT blockers. There are massive reports about ill side effects of this. Google it. It can even cause some slight forms of dementia. Again, blocking out all and every "androgen" in the body is counterproductive as the female body also needs some of those hormones. Also be aware that progesterone is a soft DHT inhibitor. I and some others I know use Progesterone Gel on the temples and top of the head and it regeneratesd hair growth as it also reduces DHT production. (it is a 5 alpha reductase inhibitor).

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Richenda

Very wise words Anjaq about the tests. Thank you too for such a fabulous explanation of the mechanisms.

Let me just allay your fears a little about my lactation. I only have it when I'm breast pumping, which I do once a day for ten minutes to stimulate them. It has increased breast and areola size. The pumping always produces a small lactation.

My last test was 4 weeks ago and I will have another soon in Bangkok. My prolactin result was 14.7 ng/mL which is top end for a male but midrange for a non pregnant female (4.79 - 23.3)

I love what you have written which was so helpful. However, I do confess to being slightly anxious over the idea of high dosage anything, including estrogen. Part of the reason I'm having an orchiectomy in six weeks is so that I can cut out entirely all anti-androgens (I believe this is correct: I will literally be taking none of them) and just keep a lose dose of estradiol valerate. Removal of testicles makes one the same as a GRS post-op MtF. As you rightly point out, there are side effects and consequences for most all of the meds we take and that concerns me.
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