Effectiveness of oral spironolactone?

Siberian

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Am I wrong in thinking that oral spironolactone (100-200mg per day) will greatly reduce or even eliminate the male pattern balding process?

I'm assuming that reducing the overall T levels to nearly that of a genetic female will basically create the same situation - no male pattern baldness.

I'm assuming that finasteride on top of that can only help as well? Less T, and less being converted into DHT = no hair loss?

I'm aware of the side effects of oral spironolactone. It's not a concen for me.

Off topic question: are inhousepharmacy.com and inhousedrugstore.com the same store?
 

Bryan

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Siberian said:
Am I wrong in thinking that oral spironolactone (100-200mg per day) will greatly reduce or even eliminate the male pattern balding process?

I'm assuming that reducing the overall T levels to nearly that of a genetic female will basically create the same situation - no male pattern baldness.

You expect a castration-like effect from only 100-200 mg/day of spironolactone?? :)

Bryan
 

Siberian

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Bryan said:
You expect a castration-like effect from only 100-200 mg/day of spironolactone??

Well I dunno... 100-300mg is the typical dosage for pre-op transsexuals. Though they also take estrogen, so perhaps that too knocks down the T levels?

In any case, I'd hope the T levels would be reduced to a large degree.
 

Bryan

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Considering that spironolactone had been out and in use for a while before evidence for its antiandrogenic effect began to accumulate, I suspect that if such a moderate dose as that were able to produce CASTRATION-like effects, it would have been obvious to everybody right from the start! :freaked:

Bryan
 

CCS

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i thought oral spironolactone is metabolised into a much weaker anti-androgen, and has little systemic effects, compared to flutamide, which is metabolised into an androgen stronger than testosterone but much weaker than DHT. I thought topical spironolactone is the strongest, because it is not metabolised in the skin, or at least not fast.



as for the author, yes, taking finasteride with anti-androgens does improve the effect.
 

Siberian

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Well, a number of transsexuals are telling me that there's a certain dosage threshold for spironolactone where the T levels fall dramatically - and into the range of genetic females. Usually around 100mg - 200mg.

Not scientific evidence of course, and they could be wrong, but these folk take their T levels *very* seriously ;)

BUT... one huge problem I didn't consider: taking spironolactone alone will cause osteoporosis. You'd be basically a post-menopausal female. Not good for the bones.

So... I 'spose spironolactone *must* be used along with estrogen.
 

Bryan

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Siberian said:
Well, a number of transsexuals are telling me that there's a certain dosage threshold for spironolactone where the T levels fall dramatically - and into the range of genetic females. Usually around 100mg - 200mg.

Not scientific evidence of course, and they could be wrong, but these folk take their T levels *very* seriously ;)

Can you ask them if they can find any scientific evidence for that? If they can, then I'll believe it. But until then, I'll have the same objection that I stated above, which is that spironolactone was in use for a number of years before androgen-related side-effects began to be documented.

Bryan
 

Bryan

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collegechemistrystudent said:
i thought oral spironolactone is metabolised into a much weaker anti-androgen, and has little systemic effects...I thought topical spironolactone is the strongest, because it is not metabolised in the skin, or at least not fast.

See the study "Topical Canrenoic Acid -- Quantification of the Antiandrogenic Activity in the Hamster Flank Organ", Noto et al, International Journal of Dermatology, November 1991, Vol. 30, No. 11.

They got a roughly similar antiandrogenic effect from potassium canrenoate as spironolactone, when the dose was four times as high. So you can apparently make up in quantity what you lack in quality.

Bryan
 

CCS

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bryan, if we know the relative strength of the weaker metabolite to spironolactone, and we know the dose of oral spironolactone that gives the same systemic effects as the local topical spironolactone does, then we can guestimate how much spironolactone is getting into the follicles topically. If we know the concentration relative to DHT, we can calculate the equivalent blocking ability compared to propecia. I think some people would be interested in that info.
 

Bryan

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collegechemistrystudent said:
bryan, if we know the relative strength of the weaker metabolite to spironolactone, and we know the dose of oral spironolactone that gives the same systemic effects as the local topical spironolactone does, then we can guestimate how much spironolactone is getting into the follicles topically.

You might also be interested in knowing that in the hamster study that I cited above, they also measured the effect of the spironolactone and the potassium canrenoate on the hamsters' hair. And yes, they did find that the diameter of the hair was significantly reduced by them, compared to the non-treated flank-organs and the vehicle-treated ones.

BTW, since you're still relatively new here, you may not be familiar with that Italian study of topical spironolactone for male pattern baldness. I know, I know, it does leave a lot to be desired in how they measured the effects, but the researchers _do_ think they got a positive result. Here's a scan of the whole study:

http://www.geocities.com/bryan50001/spiro2.htm

Bryan
 

Bryan

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Bryan said:
Siberian said:
Well, a number of transsexuals are telling me that there's a certain dosage threshold for spironolactone where the T levels fall dramatically - and into the range of genetic females. Usually around 100mg - 200mg.

Not scientific evidence of course, and they could be wrong, but these folk take their T levels *very* seriously ;)

Can you ask them if they can find any scientific evidence for that? If they can, then I'll believe it. But until then, I'll have the same objection that I stated above, which is that spironolactone was in use for a number of years before androgen-related side-effects began to be documented.

Bryan

AHA!!! It just occurred to me that there's some scientific evidence against your claim (that spironolactone causes T levels to fall dramatically to female levels), and it's in a small study oral spironolactone that I've already posted a number of times on the hairloss sites! I'd forgotten that they had measured hormone levels in that test! :wink: Here it is again:

Clinical Endocrinology (1997) 47, 759-761

Letters to the Editors

"Beneficial effect of spironolactone on androgenic alopecia"

"Sirs, Spironolactone, an established anti-hypertensive agent, has a marked anti-androgenic activity, which has been exploited for the treatment of hirsutism and acne. These are the commonest skin manifestations of mild to moderate androgen excess in women of reproductive age. Androgenic alopecia, the loss of scalp hair occurring in genetically predisposed subjects, is also related to raised androgen bioactivity. Drugs with anti-androgen action have been extensively employed for the treatment of hirsutism and acne with fairly good results although the evaluation procedures usually employed have been recently criticized. On the other hand, the usefulness of these agents in treating androgenic alopecia has never been properly assessed. We have recently had the chance to evaluate the effects of spironolactone (100 mg twice daily for six months) on the rate of scalp hair loss and the distribution of hair root phases in 4 young patients, 18-23 years of age (2 women, cases a,b and 2 men, cases c,d) with partial androgenic alopecia.

"Measurement of androgens and sex hormone binding globulin, were performed in all patients and ovarian ultrasound assessment was performed in the female patients. Furthermore, measurements of hair loss after daily washing for 10 days and hair phase evaluation with trichograms were carried out before, after 6 months on spironolactone and 3-4 months after its withdrawal. Unit area trichogram provides a proportional assessment of the 4 phases of scalp hair (anagen, catagen, telogen and dysmorphic).

"No marked changes in the endocrine parameters were observed as a result of treatment, with serum testosterone being slightly elevated in one of the female patients both of whom had polycystic ovary syndrome. A marked reduction in the rate of daily hair loss and an improvement in the trichogram score were noted during treatment, in all 4 cases, but with a partial relapse following its cessation (Table 1).

"This improvement was shown by a 50.0 to 62.9% decline in hair loss in the 4 patients, compared to their pre-treatment assessments. In terms of trichogram score changes, an increase in anagen phase was noted during treatment (from 22.0 to 84.5% over basal evaluation percentage) whereas the proportion of dysmorphic hairs during treatment was markedly lower than pre-treatment values in all 4 cases. Post-treatment evaluation showed a considerable degree of relapse in anagen hair (from 17.0 to 43.8% over treatment values), although a fair part of the improvement was retained. No adverse effects, particularly on the menstrual cycle, sperm count or sexual activity were noted. However, it should be pointed out that spironolactone may cause erectile inadequacy in other patients. A fall in blood pressure was noted in all patients, who were normotensive, and no change in renal or liver function was recorded. The beneficial effect of spironolactone on scalp hair was probably mediated through its anti-androgenic action mainly at the level of pilosebaceous unit. Recently such an effect has been also demonstrated for the 5alpha-reductase inhibitor finasteride.

"It is concluded that, in view of the beneficial effects noted in these cases, spironolactone may be a useful agent for restraining scalp hair loss in androgenic alopecia. However, a properly designed clinical trial would be necessary to prove this conclusively."

D.A. Adamopoulos, M. Karamertzanis, S. Nicopoulou and A. Gregoriou
Endocrine Department, Elena Venizelou Hospital, Athens 115 21, Greece

Table 1 Mean daily hair loss and scalp hair trichograms.
---------------------------------------------------------------
.................. Hair loss ..........Trichogram phases* (%)
Treatment ... number/day .....I.........II.......III........IV
---------------------------------------------------------------
before... case a .... 156 .... 42 ...... 4 ..... 29 ...... 25
..................... b ..... 204 .... 33 ...... 7 ..... 32 ...... 28
..................... c ....... 60 .... 50 ...... 0 ..... 31 ....... 19
..................... d ..... 140 .... 41 ...... 4 ..... 29 ....... 26

during .. case a ..... 98 ....... 58 ..... 3 ...... 26 ...... 13
..................... b .... 103 ...... 61 ..... 4 ...... 27 ........ 8
..................... c ..... 30 ....... 61 ..... 1 ...... 31 ......... 7
..................... d ..... 88 ....... 55 ..... 5 ..... 25 ....... 15

after .... case a ..... 130 ..... 47 ..... 4 ...... 35 ...... 14
..................... b ..... 180 ..... 49 ..... 6 ...... 33 ...... 12
..................... c ....... 50 ...... 55 ..... 3 ...... 31 ...... 11
..................... d ...... 106 .... 48 ..... 6 ...... 29 ...... 17
-------------------------------------------------------
*I anagen, II catagen, III telogen, IV dysmorphic.
 

Siberian

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I'm getting lost. Here it affects T:

"Sirs, Spironolactone, an established anti-hypertensive agent, has a marked anti-androgenic...

Here it doesn't:

No marked changes in the endocrine parameters were observed as a result of treatment

Here one would assume it affects T again:

However, it should be pointed out that spironolactone may cause erectile inadequacy in other patients.

It sure seems to be messing with SOMETHING in the hormones.

The beneficial effect of spironolactone on scalp hair was probably mediated through its anti-androgenic action mainly at the level of pilosebaceous unit..

Ah, so maybe it doesn't affect serum T level?

Yikes, this is SO confusing. I don't have any data, I'm not claiming anything other than the fact that TSs routinely take spironolactone as part of their hormone regimen, AND that their T serum levels are very, very low. Now you have me wondering if the estrogen they take is what's actually supressing the serum T.

The *claim* is that spironolactone allows a lesser dose of E to be used, since spironolactone knocks down th T levels... leaving less competition for the E. I figured blood pressure patients simply weren't using spironolactone doses which causes significant anti-T effects.

Interesting findings you have here!
 

CCS

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I read on HLH a post from a guy who said he had seen the solubity of spironolactone in alcohol. He could not remember what it was, but he said it was "several percent", whatever that means. I'll interpret that to mean at least 3%.

Iamnaked and Bryan both said spironolactone does not stink unless you mix it with minoxidil.

i am waiting for a reply from Iamnaked for the measurements of his 25mg pills (shape, diameter, height) so i can figure out if they are 500mg like the 100mg pills Bryan has. Bryan, what are the measurements of your spironolactone tablets?
I'd prefer to buy 300 25mg tablets than 100 100mg tablets for price reasons. 300 100mg tablets is the best deal, but i don't want to fork out $109 right now. I guess the filler is not an issue if I'm the spironolactone does not dissolve it, or not enough to make hair look like icing.

I will dissolve a 100mg ground pill in 1mL of ethanol and another in 2mL of ethanol in pre-weighed vials. After good mixing, i'll let them settle, and then pipet half the volume of ethanol (0.5mL and 1mL) and evaporate the rest outside on the hot pavement. I can dischard the pipetted ethanol or put it on my head with a drop of oil. I will put the vials under a heat lamp to full dry overnight. I'll way them again, and multiply the weight difference by 2, so i don't have to waste time getting surface alcohol like Bryan, when some is probably mixed throughout the paste anyway with some spironolactone in it.

1) If they are proportional, that means the solution can hold 5% spironolactone.
2) If they the masses are equal, that means the mass is equal to 50mg, and the ethanol can hold at least 10% spironolactone.
3) If they are not proportional or equal... well you get the idea. I will continue doing them in sets of two until I know how much it can hold within about a percent. But if it can hold at least 10%, then I don't care and will stop there. If it holds at least 7%, I might see if PPG dissolves the tablet, and if not, just use that. I'll extract the spironolactone with my PPG, pipette it off, then add my ethanol to get some more, if I want to get 95% of it out and make a 1 month supply.

Add some fatty acids to make it creamy, maybe some oil if that is not creamy enough, and a few drops of vinegar to get pH 4.5, and I'm done. No white stuff. Goes on like thicker 5% minoxidil. Maybe it will look kind of like hair gel. I will go for 3% spironolactone, 25% fatty acids, 25% PPG, 25% ethanol, 20% water, and the remaining 2% will be apple vinegar or maybe a few drops of oil.

I can pull this off if the PPG and ethanol together can hold over 6% spironolactone, and the water and fatty acids don't mess that up.
 

Bryan

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Siberian said:
I'm getting lost. Here it affects T:

"Sirs, Spironolactone, an established anti-hypertensive agent, has a marked anti-androgenic...

NO! That doesn't mean it's affecting T, it means it's affecting ANDROGEN RECEPTORS.

Siberian said:
Here it doesn't:

No marked changes in the endocrine parameters were observed as a result of treatment

Correct.

Siberian said:
It sure seems to be messing with SOMETHING in the hormones.

The beneficial effect of spironolactone on scalp hair was probably mediated through its anti-androgenic action mainly at the level of pilosebaceous unit..

Ah, so maybe it doesn't affect serum T level?

Now you're getting the idea! :)

Siberian said:
Yikes, this is SO confusing. I don't have any data, I'm not claiming anything other than the fact that TSs routinely take spironolactone as part of their hormone regimen, AND that their T serum levels are very, very low. Now you have me wondering if the estrogen they take is what's actually supressing the serum T.

Well, if they're castrated, they're obviously going to have much lower T levels. And yes, estrogen reduces T production in intact males.

Siberian said:
The *claim* is that spironolactone allows a lesser dose of E to be used, since spironolactone knocks down th T levels... leaving less competition for the E. I figured blood pressure patients simply weren't using spironolactone doses which causes significant anti-T effects.

Well, spironolactone probably actually has sort of a "biphasic" effect on testosterone levels. Any antiandrogen (spironolactone is an antiandrogen, as we all know) will tend to RAISE testosterone production, as a result of its effect on the hypothalamic-pituitary-gonadal axis. On the other hand, spironolactone also happens to have the property of being able to interfere with the synthesis of testosterone, which would obviously lower it. So there are two different actions of spironolactone which have conflicting effects on T production. My own guess is that the first one tends to predominate at lower doses, and the second one predominates at much higher doses.

Bryan
 

Siberian

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Bryan said:
You expect a castration-like effect from only 100-200 mg/day of spironolactone?? :)

Sorry to resurrect an old thread of mine, but I finally got my blood tested after 4.5 months of:

200mg oral spironolactone
6-8mg estriadol B17

My levels are:

Serum Testosterone = 24 ng/dl (241 - 827 normal for males, 20 - 80 for females)
Estriadol = 449 pg/ml (10 - 60 normal for males, 20 - 400 for females)

My pre-HRT testosterone was almost 800.

Obviously, taking estriadol contaminates the results, but from what I've read, estriadol alone can't push T down very far unless used in massive doses - which is dangerous and why an anti-androgen is used.
 

JDW

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Are you not at all worried that your levels are at the low end for women let alone men?
Have you had any sides as a result of thus?
 

Siberian

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JDW said:
Are you not at all worried that your levels are at the low end for women let alone men?
Have you had any sides as a result of thus?

Oh yes, there are sides alright. But I'm changing my sex. The sides are actually the point ;)

Do NOT try this regimen at home.

I just thought it was interesting that the serum T level could be knocked down so far via drugs. In theory, the T is even less effective than the numbers show since spironolactone apparently inhibits T receptors as well.
 

Bryan

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Siberian said:
Sorry to resurrect an old thread of mine, but I finally got my blood tested after 4.5 months of:

200mg oral spironolactone
6-8mg estriadol B17

My levels are:

Serum Testosterone = 24 ng/dl (241 - 827 normal for males, 20 - 80 for females)
Estriadol = 449 pg/ml (10 - 60 normal for males, 20 - 400 for females)

My pre-HRT testosterone was almost 800.

HUH?? You're claiming that your testosterone was reduced by 97% just from taking spironolactone and estradiol at those stated doses?? Sorry, but I don't buy it. Are you taking any other drugs? Have you had those tests repeated to verify their accuracy? There's something else going on here...

Bryan
 

Siberian

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Bryan said:
Siberian said:
Sorry to resurrect an old thread of HUH?? You're claiming that your testosterone was reduced by 97% just from taking spironolactone and estradiol at those stated doses?? Sorry, but I don't buy it. Are you taking any other drugs? Have you had those tests repeated to verify their accuracy? There's something else going on here...

labs.jpg


THAT sure raised a few red flags, lol... since the computer thinks I'm male ;)

Believe what you want. I'm just reporting what happened, and what happens constantly with thousands of transsexuals every day. My regimen is very typical, as are these results.

Verified? Why? This is what I expected. Quest isn't in the habit of screwing up blood tests since people's lives are at stake. Besides, the breasts, skin changes, fattening thighs and rear, zero erections and facial changes are darn good verification ;)

Yes, I'm also taking Propecia. Not sure why anymore... kinda redundant now, lol.
 

hellohello

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Sorry to steal light from your post, but I was wondering what you have noticed is different with your skin?

Im just wondering what affect lowering test. has on your skin...
 
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