Susan's Place Transgender Resources

Hi, it seems there are evidences that long-term use of antiandrogens, such as cyproterone or spironolactone can cause after few years a hypersensitivity of the androgen's receptors, and this will turn back again the androgen's effectson body, also if there are very low circulating T and DHT.
On the MTF hormones forum on facebook many users assert this, so many of them encourage to avoid the use of antiandrogens, exactly for this reason.

I would ask those of you who are taking cyproterone or spironolactone from many years if you experienced this effect (to have hypersensitivity to androgens, and have androgen's effects on the body even with very low circulating T and/or DHT), and after how many years did you start to feel it.

Sorry for my english, i hope the question is clear :)

Thanks

I have been on a typical transition level Spironolactone dosage for almost nine years and have had absolutely no problems on the medication. 

I thought about cutting back/eliminating it altogether because at this point estrogen alone is likely sufficient to maintain my hormones levels. The cost is so low, with the  benefits to my complexion and controlling my blood pressure, my doctor doesn't see any point to stopping.

I switched to zoladex (t inhibitor implant) as its far more effective and has very few side effects I have felt.

I am not sure what is the exact question you are asking.

As for the effectiveness of any anti-androgen, there have been no reports of loss of effectiveness with long term use. There may be some side effects that become a problem later on. Any long term use of a drug must be evaluated as to the benefits and risks for that specific drug.

If long term use of an anti-androgen is considered, you should also consider orchiectomy as a more permanent solution. Orchiectomy is not for everyone but many of us are happy with this.

I started with spiro for heart failure in 1993. Low dose for use as diuretic. The one thing it did was kill my sexual desires after a few years. Not that i had many to begin with. Now I am on a much higher dose and my T level is at 23 and my E level is at 362. Some opt for orchiectomy because who wants to take more pills and it is the only sure way to reduce t levels. Frankly I take about 14 medications a day so I can't attribute my poor feelings on any one drug. For example yesterday I almost passed out in the market. Today I feel perfectly fine.

thanks for your answer.. my question was a little different: did you experience any increasing of androgen's effects after some years of anti-androgens?
I ask this because it seems that long term use of anti-androgens causes increasing of androgen receptors sensitivity, so even if you have very low T and DHT, you will feel their even so their effects.

Quote from: Kendra on September 27, 2018, 08:31:03 AM
I disagree. 

Dr. Facebook didn't complete medical school for a decade or even a few days.  Couldn't be bothered with a medical internship.  Failed to qualify for a career in any clinic.  And isn't qualified to guide any of my health care decisions.

By the same token, doctors and the pharmaceutical industry have a terrible track record when it comes to women's HRT. They quickly settled on bioidentical testosterone for men's hormone replacement (a comparatively small market), but when it came to women's hormone replacement (a much larger market), the pharmaceutical industry has been pushing synthetics for decades.

The pharmaceutical industry business model revolves around patents, and having a period of patent protection during which they can sell a drug for high prices without fear of being undercut by competitors. If a drug can't be patented, it's of no interest to them, even if it works much better than their patented products. Bioidentical hormones (bioidentical means chemically identical to the hormones that occur naturally in the human body) were already there in nature and weren't invented by man, so can't be patented. Although they've had the ability since at least the 1950s to produce hormones that are completely chemically indistinguishable to our own hormones, this issue of patentability meant that the pharmaceutical industry instead opted to promote "synthetic" hormones, which are manmade substances designed to target the same receptors as our naturally occurring hormones do, and produce similar effects.

As a result, most of the hormones used in medicine, and virtually all the hormone replacement given to women, has until very recently either been synthetics, or an extract of horse estrogens called Premarin. Although the estrogens in premarin are naturally occurring and therefore can't be patented, the means of production (extraction from the urine of pregnant mares) could be protected by patents, giving a single pharmaceutical company (Ayerst, later Wyeth, and now Pfizer) the monopoly on production. Even though it's an inferior estrogen, slick marketing means that premarin grew to become the main women's hormone replacement (a position I think it still holds in the US even now).

The way synthetics (and Premarin) have been marketed, is that their effects are essentially the same as the human body's own naturally occurring hormones. In fact, nothing could be further from the truth, and they all seem to have harmful side effects associated with them that aren't seen with bioidentical hormones. The orally active synthetic estrogens are particularly bad in that regard (e.g. DES and ethinylestradiol). They have a very high risk of causing DVTs, pulmonary embolisms, and cardiovascular events (strokes and heart attacks).

DES also turned out to be quite a potent carcinogen, and was eventually withdrawn (not until after millions of women and their unborn babies had been exposed though). Another side effect of DES, one the pharmaceutical industry have so far managed to keep quiet, is that, when administered during pregnancy, it crosses the placenta, and can trigger female brain development in male babies (see the DES thread on this site).

A synthetic progesterone mimic called medroxyprogesterone acetate (brand name Provera) has also seen extensive use in women's hormone replacement, and has since been shown to increase the risks (DVTs etc) associated with synthetic estrogens, as well as leading to an increased cancer risk in its own right.

All this has led to HRT gaining an undeserved reputation for being dangerous. In actual fact, it's not hormones per se that are the problem, but the type of hormone. All the hormones used for women's HRT that led to increased rates of disability and death are non-bioidentical, either synthetics (DES, ethinylestradiol and medroxyprogesterone) or premarin (whose main hormonally active ingredients are estrogens unique to horses, and for which we don't have the enzymes and other systems in place to deal with). There's no evidence of comparable harm associated with bioidentical hormones (other than estradiol taken by mouth increases clotting risk, a risk that can be avoided by using transdermal or injected forms).

Since hormones are prescription medicines, doctors have the legal monopoly on dispensing them. Even so, that doesn't alter the fact that they have a terrible track record in needlessly harming and killing women with bad HRT! IMO, if you're going to be taking hormones, it's important to understand at least the basics of what constitutes good and bad HRT, and not just blindly assume your doctor knows what they're doing. All too often they don't, and are just following stuff some pharma industry sales rep told them. That's why groups such as the trans HRT group on Facebook are important (and also so that trans women who don't have access to medical care, and are forced to use black market hormones, can at least minimise the risks to themselves).

Quote from: PurplePelican on September 27, 2018, 12:11:10 PM
If it's the group I'm thinking of, there are several doctors in it, all of whom are experienced in trans medicine.

As a group, they do take some of their claims way too far, but the science they base them all on is sound - and there are more than a few other doctors around that agree with them.

If it's the one I'm thinking of then don't take what they preach as gospel. They remove any posts that run counter to their version of hormone therapy. I left the group after just a couple of months because I tried to share my research into the effects of different medications and they didn't like what it showed. I have shared it here before. Lists of known side effects, primary metabolites, activation of receptor sites, ect. They didn't like real science being put up there.


That whole, "spit and rinse your mouth after the estrace dissolves because you don't want to let any tiny bit get swallowed", is bull.

Pharmaceutical companies are only interested in profits. No more no less.

It is common for people to develop resistance and/or side effects from current medications. The good thing about being MtF is that their is a fix. An orchiectomy would be the next step whether wanted or not and makes sense.

Personally, I only want to take spiro long enough to get my orchiectomy. I don't want to take more meds than needed.

Been on Cypoterone for 12 years, when I run out the estrogen maintains just fine until I get more. No sensitivities or crashes, I do hate any slight resurgence in sebaceous activity when not using androcur.

Quote from: cdtv4life on October 09, 2018, 08:24:42 AM
Been on Cypoterone for 12 years, when I run out the estrogen maintains just fine until I get more. No sensitivities or crashes, I do hate any slight resurgence in sebaceous activity when not using androcur.

How long do you find you can go without it?

Quote from: cdtv4life on October 09, 2018, 08:24:42 AM
Been on Cypoterone for 12 years, when I run out the estrogen maintains just fine until I get more. No sensitivities or crashes, I do hate any slight resurgence in sebaceous activity when not using androcur.

Then you've been lucky, CPA is well known for causing a number of issues. It's also known for causing issues due to very low T levels due to it's efficacy. Frankly, it's crap and has no place in trans hormone protocols.

Quote from: PurplePelican on October 09, 2018, 07:20:56 PM
Then you've been lucky, CPA is well known for causing a number of issues. It's also known for causing issues due to very low T levels due to it's efficacy. Frankly, it's crap and has no place in trans hormone protocols.

Just because you had a bad experience with it doesn't mean everyone does. I couldn't get on with Spiro, it brought my blood pressure dangerously low. It doesn't mean I think it's "crap and has no place in trans hormone protocols." Now I take cypro and I'm very happy.

Quote from: Ellement_of_Freedom on October 10, 2018, 01:44:19 AM
Just because you had a bad experience with it doesn't mean everyone does. I couldn't get on with Spiro, it brought my blood pressure dangerously low. It doesn't mean I think it's "crap and has no place in trans hormone protocols." Now I take cypro and I'm very happy.

A recent study on Cypro: https://www.lexpress.fr/actualite/societe/sante/androcur-dernier-medicament-sur-la-sellette_2033489.html It's in French.

And that's just one of several I can show showing the issues with it. Depression is a known issue, one that antidepressants don't remedy - Bayer actually have to admit to this one..

This is a rare moment I wish we could talk dose, but I'll say what I can.. Androcur come in 2 'strengths' and the smallest of them is still a 4x bigger dose than most need - if they really require an antiandrogen at all. In consultation with my docs, I ceased taking all AA's about 2 years ago, T level is fine, as is my E level. Sublingual E is all I take.

By coincidence, I was DX'ed as having a meningioma about 4 weeks ago. Benign, but it is causing issues with the hearing in my left ear.

Slightly different topic,  but I've been unable to find any quality research on the use and outcomes of GNRH blockers  (gosrelin, lupron, Decapeptyl etc.. ).

Just one of my considerations for getting GRS is that I don't want to be taking these drugs for the next 40 years...

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Quote from: PurplePelican on October 10, 2018, 12:57:26 PM
A recent study on Cypro: https://www.lexpress.fr/actualite/societe/sante/androcur-dernier-medicament-sur-la-sellette_2033489.html It's in French.

And that's just one of several I can show showing the issues with it. Depression is a known issue, one that antidepressants don't remedy - Bayer actually have to admit to this one..

This is a rare moment I wish we could talk dose, but I'll say what I can.. Androcur come in 2 'strengths' and the smallest of them is still a 4x bigger dose than most need - if they really require an antiandrogen at all. In consultation with my docs, I ceased taking all AA's about 2 years ago, T level is fine, as is my E level. Sublingual E is all I take.

By coincidence, I was DX'ed as having a meningioma about 4 weeks ago. Benign, but it is causing issues with the hearing in my left ear.

One of the brain scans in that link was of a woman who was on it for 20 years. I am in my final 3 months of using Cypro (SRS in January), so I'll be on it for a total of 2 years and 4 months. In another journal article I read, the risk was substantial in women who have been on the drug in excess of 10 years. Well I'm nowhere close to 10 years so I feel okay about it.

I wouldn't recommend anyone being on it indefinitely.. or for any period greater than 5 years. Not that I'm a doctor, that's my unqualified opinion.

Quote from: Ellement_of_Freedom on October 10, 2018, 06:02:56 PM
One of the brain scans in that link was of a woman who was on it for 20 years. I am in my final 3 months of using Cypro (SRS in January), so I'll be on it for a total of 2 years and 4 months. In another journal article I read, the risk was substantial in women who have been on the drug in excess of 10 years. Well I'm nowhere close to 10 years so I feel okay about it.

I wouldn't recommend anyone being on it indefinitely.. or for any period greater than 5 years. Not that I'm a doctor, that's my unqualified opinion.

I was on it for less than 5 years. And it's not the only issue.. A 7x increase in 6 months of use is not to be sneezed at.

But as usual, because it goes against the grain of "accepted" trans health, my comments are held to some kind of higher standard. Many oncologists no longer use cypro, mainly due to the side effects. In fact, many oncologists follow a protocol that is most beneficial to trans women, one which I'm on, but seems to cause other trans women to freak out.. Sublingual E only, no antiandrogen of any kind. My doc says my levels are fine and I've had further development over the last 2 years on the protocol - I previously stalled in development at about 18 months in.

Quote from: PurplePelican on October 11, 2018, 03:23:30 AM
I was on it for less than 5 years. And it's not the only issue.. A 7x increase in 6 months of use is not to be sneezed at.

But as usual, because it goes against the grain of "accepted" trans health, my comments are held to some kind of higher standard. Many oncologists no longer use cypro, mainly due to the side effects. In fact, many oncologists follow a protocol that is most beneficial to trans women, one which I'm on, but seems to cause other trans women to freak out.. Sublingual E only, no antiandrogen of any kind. My doc says my levels are fine and I've had further development over the last 2 years on the protocol - I previously stalled in development at about 18 months in.

Not everyone is going to have the exact same baseline T levels as you. Some people need an anti-androgen at least to begin with. Everyone responds a certain way to different drugs because we all have different genetics and lifestyles. Your experience is not applicable to every single other trans woman out there.

Quote from: Ellement_of_Freedom on October 11, 2018, 05:25:37 PM
Not everyone is going to have the exact same baseline T levels as you. Some people need an anti-androgen at least to begin with. Everyone responds a certain way to different drugs because we all have different genetics and lifestyles. Your experience is not applicable to every single other trans woman out there.

This is a protocol used with great success in prostate cancer patients, where T suppression is very important. It uses a biofeedback loop within the endocrine system.. My personal levels were immaterial. And I'm far from the only trans woman using this protocol or similar - just most of them don't talk about it. (Or do so in such a sensationalised way, no one takes them seriously.)

I'll bow out of this convo now, this is going the way these convo's usually do.

Quote from: PurplePelican on October 11, 2018, 06:15:37 PM
This is a protocol used with great success in prostate cancer patients, where T suppression is very important. It uses a biofeedback loop within the endocrine system.. My personal levels were immaterial. And I'm far from the only trans woman using this protocol or similar - just most of them don't talk about it. (Or do so in such a sensationalised way, no one takes them seriously.)

I'll bow out of this convo now, this is going the way these convo's usually do.

Sorry that your conversations tend to end this way. Perhaps there's a common denominator.

I haven't seen any mention here of dutasteride (Avodart).  Some of us here are on it for BPH.  It's sometimes used with with estrogen for MtF HRT.  I've been on it for over 1.5 years.