feminization at a stand still. Should I spilt spiro?

[Stephenie S]

I didn't realize there was so much debate and difference of opinion on this idea of pill splitting
My partner is a pharmacist and insists that splitting or otherwise dividing the dose is pointless.
The daily dose should be high enough to cover you for the day and it is more important to take your does at the same time each day.
Some believe that spiro doesn't really do very much other than antagonize testosterone by taking up space in T-receptors.
Estradiol does most of the feminizing.
Taking spiro is supposed to reduce the amount of E needed because some react poorly to high doses.
There is really no way to know how fast or how much secondary change occurs.
Feminization may seem to have slowed but may not have stopped, certainly not after a year or so.
I look in the mirror every day and don't think I have change but the photos I take say otherwise.
We don't see the change in ourselves as much as people who see us infrequently.

[anjaq]

Estradiol does most of the feminizing.
Taking spiro is supposed to reduce the amount of E needed because some react poorly to high doses.

Feminization may seem to have slowed but may not have stopped, certainly not after a year or so.

Feminization slows down naturally - it is not a linear thing. It will be faster after the initial start but then slow down. Patience is needed.

I do not know of a mechanism why Testosterone would slow down feminization or why Antiandrogens would help it except in thos parts of feminization that are actually de-masculinization - like slower body hair growth.
High dosages of E can be a problem, but this mainly applies for oral estrogens.
Here is the reason why: Oral estradiol is converted to Estrone up to 90%. With patches  it is 50%, with injections ist is 25%. Estrone is an estrogen, but it is not feminizing - so it gives you all the side effects but will not even show up in the usual blood tests, which only test for estradiol.
So if you have X amount of estradiol in the blood test, if you take pills, you actually have 10*X estrogens in the blood, causing more side effects. If you take transdermals you have 2*X estrogen in the blood, with Injections you have maybe up to 2*X. The conclusion is that with transdermals you can increase X more, while keeping the overal estrogen load lower than with pills. So the fear of high estradiol is basically mainly fueld because of taking oral estradiol or artificial estrogens.

[Stephenie S]

I do not know of a mechanism why Testosterone would slow down feminization or why Antiandrogens would help it except in thos parts of feminization that are actually de-masculinization - like slower body hair growth.
High dosages of E can be a problem, but this mainly applies for oral estrogens.
Here is the reason why: Oral estradiol is converted to Estrone up to 90%. With patches  it is 50%, with injections ist is 25%. Estrone is an estrogen, but it is not feminizing - so it gives you all the side effects but will not even show up in the usual blood tests, which only test for estradiol.
So if you have X amount of estradiol in the blood test, if you take pills, you actually have 10*X estrogens in the blood, causing more side effects. If you take transdermals you have 2*X estrogen in the blood, with Injections you have maybe up to 2*X. The conclusion is that with transdermals you can increase X more, while keeping the overal estrogen load lower than with pills. So the fear of high estradiol is basically mainly fueld because of taking oral estradiol or artificial estrogens.
[/quote]

Well that is good news for me then because I use patches X2 at once. The only increase I have tried is to change them every three days rather than twice per week so that I end up with two extra changes per month.
I have been on spiro for most of my transition, I take it in the morning with breakfast. My T has always been below 1 nmol/L with the female range being 0.4- 2.6 nmol/L and E has always been above 200 pmol/L




*No Dosages Please*

[V M]

Hi Stephenie 

Welcome to Susan's Place    Glad to have you here, join on in the fun

Here are some links to the site rules that we offer to all new members to help them along

Please be sure to review:

Things that you should read

• Site Terms of Service and rules to live by
  
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Hugs

V M

[Stephenie S]

Hi Stephenie 

Welcome to Susan's Place    Glad to have you here, join on in the fun

Here are some links to the site rules that we offer to all new members to help them along

Please be sure to review:

Things that you should read

• Site Terms of Service and rules to live by
  
• Standard Terms and Definitions
  
• Post Ranks (including when you can upload an avatar)
  
• Reputation rules
  
• News posting & quoting guidelines
  
• Photo, avatars, and signature images policy
  

Hugs

V M

Hey, sorry about that.
Although I don't quite understand not posting dosage.
Perhaps you could help me understand why not to do that?
Aren't we trying to inform and educate each other?

[V M]

Hey, sorry about that.
Although I don't quite understand not posting dosage.
Perhaps you could help me understand why not to do that?
Aren't we trying to inform and educate each other?

Sure, glad to help you

It is part of the rules that were presented to you in the Site Terms of Service and rules to live by

8. The discussion of hormone replacement therapy(HRT) and it's medications are permitted, with the following limitations:
A. You may not advocate for or against a specific medication or combinations of medication for personal gain. This is strictly prohibited.
B. You may not discuss the means to acquire HRT medications without a prescription. The discussion of self medication without a doctor's supervision is prohibited.
C. The posting of recommended, or actual dosages, is strongly discouraged to prevent information obtained on this site from being used to self medicate.

We cannot in good conscience condone the self administering of these medications. Not only may self medication be illegal, but HRT medications can cause serious health problems, and many have the potential for life-threatening side effects that can only be detected and prevented with proper medical supervision.

Thank you

V M

[anjaq]

I have been on spiro for most of my transition, I take it in the morning with breakfast. My T has always been below 1 nmol/L with the female range being 0.4- 2.6 nmol/L and E has always been above 200 pmol/L

Well. My guess is, if you would slowly reduce Spiro over the course of about 4 weeks, and then test Testosterone, it most likely is still in the female range. Did you ever get LH and FSH checked? If they are very low, chances you can just phase out Spiro are even higher.

[Stephenie S]

Well. My guess is, if you would slowly reduce Spiro over the course of about 4 weeks, and then test Testosterone, it most likely is still in the female range. Did you ever get LH and FSH checked? If they are very low, chances you can just phase out Spiro are even higher.

No I have never been tested for those.
I follow a protocol that was developed by a health center in Toronto.
I just do what the doctor and the protocol say.
Chances are I won't have to worry much longer anyway as I may hear in a month about a surgery date in the spring or summer next year.
And anyway why worry about taking spiro when my potassium has always been fine and in fact all the things tested for are just fine.
I only feel a little light headed sometimes because of the lower blood pressure and that is manageable.
Since T did go up just a little and then down again I was concerned and so I don't want to fiddle with anything when surgery may not be that far off.
I have loved the lower T and how much it has helped me feel settled down and the lowered libido is a blessing.

[transnztal]

Update I've been splitting spiro everything is the same

[kelly_aus]

Update I've been splitting spiro everything is the same

Which is pretty much what is expected.

[KayXo]

I didn't realize there was so much debate and difference of opinion on this idea of pill splitting
My partner is a pharmacist and insists that splitting or otherwise dividing the dose is pointless.

Half-life of the substance determines how frequently one should take it. Spiro's half life is around 12-16 hours, if I'm not mistaken.

Some believe that spiro doesn't really do very much other than antagonize testosterone by taking up space in T-receptors.

Also reduces testosterone by inhibiting its production at the stage of 17-hydroxylation

J Urol (Paris). 1981;87(9):635-8.

"The authors examined the influence of spironolactone on the concentration of testosterone, 5 alpha - dihydrotestosterone (DHT), progesterone, oestradiol (E2), LH, and FSH in 47 patients with prostatic hypertrophy, aged from 60 to 80 years. The control group consisted of 58 men of the same age."

"There was a considerable fall in the concentration of testosterone and of DHT and, at the same time, an increase in the concentration of progesterone, E2 and LH."

Arch Sex Behav. 1989 Feb;18(1):49-57.

"Following the initial visit, all 50 were begun on spironolactone and low-dose female hormone therapy. Despite high-dose estrogen treatment for more than 2 years, the mean testosterone (T) level for the CT group was not in the female range (169 +/- 193 ng/dl; normal 20-80). Spironolactone, in doses of 200-600 mg/day, lowered T to the female range in both groups after 12 months (CT 87 +/- 111 and SPS 49 +/- 41 ng/dl). This was achieved in the CT group despite decreases in estrogen dose and discontinuation of parenteral therapy."

Many transwomen can attest to T levels dropping under Spironolactone, when taken alone.

September 2012, Vol. 11, No. 5 , Pages 779-795

"Spironolactone acts as an anti-androgen by binding to the androgen receptors; lowers circulating testosterone by increasing its metabolic clearance and preventing a compensatory rise in testicular androgen synthesis; displaces estrogen from sex hormone-binding globulin (SHBG) and increases the peripheral conversion of testosterone to estrogen leading to elevated estradiol [12]. Estradiol levels decrease and testosterone increase significantly 3 – 6 months after stopping spironolactone [12]."

Ann Intern Med. 1977 Oct;87(4):398-403.

"blood estradiol levels in the spironolactone group (30 +/- 4 pg/ml) were significantly greater (P less than 0.01) than in the control group (13 +/- 2 pg/ml). These changes were primarily due to significant increases in the metabolic clearance rate of testosterone (P less than 0.02) and in the rate of peripheral conversion of testosterone into estradiol (P less than 0.001) in the spironolactone-treated group."

To be fair, other studies found no change in E2 or T following Spironolactone usage. So, it may depend on dose and individual.

Estradiol does most of the feminizing.

Androgen is a strong inhibitor of feminization (i.e. breast growth). In women with complete androgen insensitivity, their breasts grow significantly, even sometimes more than typical females despite low estrogen levels (around 50 pg/ml). This confirms androgen's role in suppressing female sexual secondary characteristics. Androgen will reduce estrogen sensitivity by reducing number of estrogen receptors.

Sobrinho LG, Kase N, Grunt JA (1971). Yale J Biol Med. 44 (2): 225–9.

"The serum concentration of estradiol in this patient, though far less than that found in normal males (around 30 pcg/ml.),15 was still enough to induce breast growth in the presence of androgen insensitivity. This phenomenon emphasizes the anti-estrogenic effect of androgens in mammary growth."

In men taking only anti-androgens, gynecomastia can be quite common despite no estrogen taken.

Clin Endocrinol (Oxf). 1994 Oct;41(4):525-30.

"Despite an increase in testosterone levels, excellent androgen blockade was obtained, as shown by a decrease in prostate specific antigen levels in 22/23 patients."

"mild gynaecomastia and/or breast tenderness were seen in 48 and 30% of cases respectively."

Taking spiro is supposed to reduce the amount of E needed because some react poorly to high doses.

This notion of "poor response to high doses" of E comes from a time when non bio-identical estrogens were used. Today, many studies have shown high doses of bio-identical E to be relatively safe, safer when taken non-orally. Times have changed. 

Oral estradiol is converted to Estrone up to 90%. With patches  it is 50%, with injections ist is 25%. Estrone is an estrogen, but it is not feminizing - so it gives you all the side effects but will not even show up in the usual blood tests, which only test for estradiol.

"It is often assumed that the high oestrone levels seen after oral intake of oestradiol
are disadvantageous as compared with the relatively low oestrone/oestradiol ratio
during transdermal treatment with oestradiol. It should be borne in mind that the
intrinsic hormonal activity of oestradiol is much greater than that of oestrone
and both can be interconverted in the target cells and hepatocytes according to
the equilibrium conditions. Oestrone and oestrone sulphate therefore represent
oestradiol metabolites and precursors at the same time and the oestrone/oestra-
diol ratio is of no real clinical importance."

Also,

British Journal of Obstetrics
October 1984. Vol. 91 . pp. 1031-1036

"during oral treatment, high concentrations of oestrone by competition and displacement may increase the amounts of free oestradiol."

But estrone may compete with estradiol at receptors, as well. Not so good.

So the fear of high estradiol is basically mainly fueld because of taking oral estradiol or artificial estrogens.

More specifically, because of the high doses of non bio-identical estrogens as these are metabolized very slowly by the body, namely equine estrogens (found in Premarin) and ethinyl estradiol, which end up recirculating many times through the portal vein where coagulation factors are negatively impacted. Bio-identical estrogen is quickly metabolized and non-orally, there is less impact in the liver.

[Deborah]

Spiro has reduced my blood concentration of testosterone to less than 3 ng/dl.  That's the lowest it can be measured.  Since the blood concentration is so low it indicates that testosterone is no longer being produced.  This is a lowering of blood concentration of T by 823 ng/dl over the period of a year and a half.


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[Stephenie S]

The major feminization occurs using estradiol not spiro. Some people take only estradiol but it has to then be high doses. The antiandrogenic effect of spiro allows people to take lower doses of E. This is clearly stated in the protocol I follow as do most m2f trans patients in Ontario.
The OP was concerned with feminization being at a stand still, in their opinion. Is there actually any way to know that is the case when it is based on subjective assessment?
I don't understand why the admins for this sight are ok with people advocating going against doctors orders concerning prescriptions.
The bottom line is you should take your meds as prescribed.
Hormone therapy is based on research developed protocols not the pseudo science that people expound. I say pseudo science because people look things up online and think they know all they need to know.
Doctors prescribe based on what is understood about a drug therapy and feel obliged to do so because that is part of their professionalism.
On the subject of half life, i will bet most people don't know that it takes several half life cycles to clear a drug from ones body. My understanding is that its about 5 cycles.
There will always be some drug in your system if you take spiro once daily.
Spiro is considered a 24 hour drug which is why it is prescribed to be taken once a day.
All the mumbo jumbo about half life etc. is just that.
Follow your doctors orders, they need to know what you are doing in case you run into trouble. They expect that you are following their orders not the advice of people based on anecdotal reporting.
Admins! please have a proper policy about giving advice that goes against doctors orders. Show some real concern for peoples health instead of worrying about people stating what their prescribed doses are which anyone can find in the multitude of protocols published online. A concern that is based on needing to cover your butts.

[Deborah]

Spiro is considered a 24 hour drug which is why it is prescribed to be taken once a day.
All the mumbo jumbo about half life etc. is just that.

Except that some Doctors prescribe it for twice a day.  Mine does and treats lots of trans patients. 

I agree though that in the greater scheme of feminization it probably doesn't make much, if any difference one way or the other.


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[LShipley]

Then it's a question for the doctor, but none of you should change how you take your meds based on anything said here. You can even ask a doctor or pharmacist online these questions about half life but either way clear it with your doctor before you change HOW you take a prescription. Same for oral/sublingual/rectal. No need to take desperate measures for minimal results

[KayXo]

I am NOT a doctor. I convey information that is published in studies and studies is how medical knowledge is gathered and updated. This is science, not pseudoscience. I believe it is useful to read such articles which doctors sometimes don't have the time to read as they are so busy. I will share the information I gather with my doctors and sometimes, they agree with me and will change their position on a certain matter, based on the findings of several studies. As I have learned, time and time again, doctors are not infallible. They are human, can make mistakes and cannot know everything. Sometimes, working together with them can prove to be useful and they might appreciate this.

I'm not advocating going against doctor's order. I'm simply providing information, sharing my opinion so that others may get another perspective on the matter, get to think more critically about the matter and perhaps relate what they learnt to their doctors...and who knows, their doctors might see things differently. I see this sharing of information as only positive if interpreted in this manner.

I know many doctors who tell their patients to take their spironolactone twice daily while others advise once daily suffices. Who is right, who is wrong? In the end, if the patient and doctor feel comfortable with the regimen, then that's all that really matters. Splitting Spiro, for instance, for some is better as taking the full dose can bring on too many side-effects all at once, like having to go the bathroom constantly or headaches/dizziness where splitting makes things easier, effects become milder. It depends. The doctor with the patient's feedback should determine how the substance is taken.

I choose to be proactive in my health. To each their own. Not everyone can, I also understand. I also think blindly following orders may not be in one's interest. To question without doing it excessively can be constructive. Following orders, yes but trying to be as informed as possible as well is also important, in my opinion.

Final words: do as your doctor says, I AM NOT A DOCTOR, and everything expressed in this forum or any forum should be taken with a grain of salt, questioned, I agree. Doing your own research may prove to be useful.

Take care.

[TonyaW]

Hi

Also a pharmacist here. 

Once or twice daily dosing of spironolactone should make no difference in effectiveness.

Never make changes to any of your meds without your doctors knowledge, they need to know what you're doing especially if it differs from what they prescribe.  If you don't trust your doctor, get a new one that you do.  I know that is not always easy or possible, especially for HRT. That doesn't mean you should never question them or ask about other meds etc.  They should be open to suggestions but I hope they are not influenced by "I read it on the Internet".

Also, off the top of my head I think that finasteride would be a better option than spironolactone. My guess is it is not used more because it can take a while for newer treatments to filter out to the mainstream (especially for a drug that's already off patent) and/or potential side effects from the finasteride.

I have not looked into this, but I plan to soon as my plan is to start HRT in January.



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[Stephenie S]

Except that some Doctors prescribe it for twice a day.  Mine does and treats lots of trans patients. 

I agree though that in the greater scheme of feminization it probably doesn't make much, if any difference one way or the other.


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Okay fine your doctor prescribes twice daily and is probably following a protocol that they know are have reasons to trust.
The OP said they were splitting their dose, they didn't say how many times though.
I know a person who obsesses over her dosage and splits hers 8x thinking this is better for her keeping it in her system.
I just don't like seeing people get stressed about this which possibly is more detrimental.
I know doctors don't know everything and that they are open to advice and changing things based on the patients wellbeing. But doctors also get some rather far out suggestions from their patients too.
Everyone should know that the hormone therapy is not an exact science and is based mostly on observed effects and a general understanding of what the meds do.
Again, the OP's concern was to do with feminization apparently at a standstill and wondered about splitting spiro which isn't the main feminization component.
Why wouldn't people suggest asking the doctor to increase the estradiol or change the form used?
Also not mentioned are any test results about E and T levels.
Most doctors will say that if your levels are in the female range then you are going to experience effects from this.

[Stephenie S]

Hi

Also a pharmacist here. 

Once or twice daily dosing of spironolactone should make no difference in effectiveness.

Never make changes to any of your meds without your doctors knowledge, they need to know what you're doing especially if it differs from what they prescribe.  If you don't trust your doctor, get a new one that you do.  I know that is not always easy or possible, especially for HRT. That doesn't mean you should never question them or ask about other meds etc.  They should be open to suggestions but I hope they are not influenced by "I read it on the Internet".

Also, off the top of my head I think that finasteride would be a better option than spironolactone. My guess is it is not used more because it can take a while for newer treatments to filter out to the mainstream (especially for a drug that's already off patent) and/or potential side effects from the finasteride.

I have not looked into this, but I plan to soon as my plan is to start HRT in January.



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My understanding is that finasteride is to control a form of testosterone that contributes to hair loss, not as a spiro substitute.
I have been on finasteride for a year and in that year my T went up and down but thankfully always still below 1.0
My understanding also is that the effects of finasteride will be felt after taking it for six months.
Six months in was when my T started to rise from the rock bottom reading of 0.1 which is where it was from 3rd month until about 12 months on hormone therapy.
I don't know what to make of it and now I have added progesterone about three months ago.
It's all a crap shoot in the end or if you prefer the Forest Gump perspective then it's a box of chocolates. You really don't know what you will get.

[TonyaW]

My understanding is that finasteride is to control a form of testosterone that contributes to hair loss, not as a spiro substitute.
I have been on finasteride for a year and in that year my T went up and down but thankfully always still below 1.0
My understanding also is that the effects of finasteride will be felt after taking it for six months.
Six months in was when my T started to rise from the rock bottom reading of 0.1 which is where it was from 3rd month until about 12 months on hormone therapy.
I don't know what to make of it and now I have added progesterone about three months ago.
It's all a crap shoot in the end or if you prefer the Forest Gump perspective then it's a box of chocolates. You really don't know what you will get.

Well finasteride is used for hair loss (Propecia)  and to shrink prostate in BPH (Proscar).  Different dosages for those, the hair loss being lower dose. The goal for us is testosterone suppression and there is no official indication for that so no "approved" dosage.

Thanks for a start to my research

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