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Warning About Topical Spironolactone!!  

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HitMeBack
(@hitmeback)
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Joined: 2 years ago
Posts: 82
27/08/2018 8:47 am  

Last week I ordered a bottle of Dr Richard Lee's 2% Spironolactone solution
I applied it to the thinning areas of my hairline the night before as well as the morning of a blood test which included total Testosterone and free testosterone. My blood test result came back as well below the normal range :

Total testosterone 5.4 nmol/L (normal range 9.5 - 35)
Calculated free testosterone 123 pmol/L (normal range 225 - 725)
Both my LH and FSH levels were in the normal range at 4 IU/L (range 1-10)

Exactly 3 weeks before I had the above blood test, I also had my testosterone levels tested. The results of this test were as follows :

Serum testosterone 16.1 nmol/L (normal range 12.4 - 34.1)
Free testosterone 53 pmol/L (normal range 31 - 100.0)

As you can see, I was in the low range of normal for testosterone in my first test, however, unlike the second test, I was still within the normal range.
I did not take any other medications or supplements over that 3 week period between the 1st and 2nd blood tests and I have not taken any drugs of any description for more than a year.
Since my T levels have fallen so dramatically in the space of just 3 weeks, I can't think of anything other than the 2% Spironolactone solution that could have caused this large drop. My current blood test results shows that my blood T levels are at pre-pubescent levels!

Anyone who is thinking about using topically applied Spironolactone, please don't do it. Don't believe the lies you read about topically applied Spironolactone not having any systemic effects.
I think it is imperative that anyone using topical Spironolactone be monitored closely for systemic side effects and blood hormone level alterations.


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Big Cat
(@big-cat)
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27/08/2018 10:00 am  

Actually that would have been my guess too, Spironolactone is a fairly lipophillic drug, and the normal ways in which it is applied topically would only strengthen its resolve to distribute itself systemically.

I remember I voiced these opinions once, but then some guy, its been too long so I forgot his name, last I heard he was on avantlabs a lot, that swore to me it worked only locally. Not having had much experience with hair loss in athletes, I let it go under the pretense that I didn't know enough about topically applied hair sprays, nor did I care to research it much.

Goes to show you shouldn't trust any information without verifying it yourself :s

Good things come to those who weight.

The Big Cat is a researcher and theoreticist. His advice must never be taken in the stead of proper advice from a medical professional, it is entirely intended for research purposes.


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HitMeBack
(@hitmeback)
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Posts: 82
27/08/2018 12:55 pm  

Yes. I have actually read a couple of abstracts which found no systemic effects from topically applied Spironolactone, however, regardless of these studies, I think Dr Lee should have tested systemic effects of his product before releasing it.
It appears that Dr Lee's topical Spironolactone is easily absorbed through the skin to be able to drop my T levels down so low with just two applications!

Big Cat, do you think Nizoral 2% could also be absorbed systemically? I've been using it for years now and just wonder if it may also lower T levels somewhat. I normally let it sit on my scalp for up to 5 minutes before washing it off.
As you can see above, the results of my first blood test, although still within the 'normal range' for my age, are not exactly optimal.


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HitMeBack
(@hitmeback)
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27/08/2018 1:49 pm  

Bump. Big Cat or anyone else, I'd really like to know the answer to my Nizoral question!
Thanks.


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Big Cat
(@big-cat)
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27/08/2018 2:47 pm  

Nizoral contains ketoconazole, an anti-mycotic agent. Its known to lower androgenic effects by inhibiting steroidogenisis, not by blocking the androgen receptor.

Its topical use is under some scrutiny, since there is little evidence how it works topically, since the majority if not all of its inhibition of steroidogenisis occurs in the liver. Studies have demonstrated that 2% ketoconazole can stimulate regrowth of hair 'in mice'. The mechanism of action in this regard is however not known.

To answer your question, ketoconazole is an agent that is obviously more comfortable in organic solvents than in water, but given the amount of nitrogen atoms and oxygen atoms it should be far less likely to be absorbed systemically PROVIDED THE RIGHT CARRIER IS USED.

Good things come to those who weight.

The Big Cat is a researcher and theoreticist. His advice must never be taken in the stead of proper advice from a medical professional, it is entirely intended for research purposes.


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HitMeBack
(@hitmeback)
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27/08/2018 3:33 pm  

So, I guess the cause of my recent very low test levels was the topical Spironolactone. This means that in my case it did not act as an androgen receptor blocker as it is reported to act, but rather had a direct effect on the leydig cells.
The reason I asked about the Nizoral is because ketoconazole lowers Testosterone by affecting the leydig cells.
If Spironolactone does indeed act only as an androgen receptor blocker, how could it have lowered my serum testosterone by so much?


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JGUNS
(@jguns)
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27/08/2018 4:34 pm  

I would be interested in seeing more than anecdotal data on this topic for sure! Here is what I have always seen:

J Endocrinol Invest. 1988 Apr;11(4):273-8. Related Articles, Links

Lack of endocrine systemic side effects after topical application of Spironolactone in man.

Rey FO, Valterio C, Locatelli L, Ramelet AA, Felber JP.

Departement de Medecine, C.H.U.V., Lausanne, Switzerland.

In six healthy male volunteers, the percutaneous absorption of Spironolactone was compared with placebo in a double-blind crossover study. The subjects were randomly given either a cream containing 5% Spironolactone or placebo to be applied in a randomized sequential way to a well defined skin area equivalent to 55% of body area. During the 72 h following the application of the ointment, blood levels of canrenone, the major metabolite of Spironolactone, have been determined. In order to estimate the systemic antiandrogenic effect of Spironolactone, plasma levels of 17-alpha-Hydroxy progesterone (17 alpha-OH-P), Testosterone (pT) and non-conjugated 3 alpha-Androstanediol (3 alpha-diol, metabolite of the active androgen 5 alpha-Dihydrotestosterone or DHT) as well as salivary Testosterone (sT) which relate to the free and active plasma testosterone fraction have also been measured. Urinary levels of canrenone have been determined 48 hours after cream application. No changes in any levels of these hormones have been detected and plasma canrenone levels were undetectable during the 72 hours of topical treatment. Topically administered, Spironolactone appears to have only a local skin impregnation.


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Big Cat
(@big-cat)
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27/08/2018 5:27 pm  

That's what I was told too. But it doesn't seem to match the chemical properties of the drug and it doesn't appear to be the case at least for hitmeback if his blood levels are correct.

The discrepancy may be in the carrier that was used. If an apolar but low lipophillic carrier was used, it may have been more advantageous to permeation and eventual systemic uptake. If however thick hydrophillic or lipophillic gels were used, the retardation inside the carrier would likely have kept it from substantially absorbing to deep.

Another possible explanation is that they examined excretion of canrenone in 72 hours. With the retardation through transdermal application, possibly combined with lower absorption as described above, could have easily led to little or no appearance of canrenone in urine in that time-frame. Main site of metabolism to canrenone is the liver, but with the properties of Spironolactone, to let the drug make its way into systemic circulation and then the liver, could take considerably longer.

Like you I'd like to see more evidence and examine the difference between what was used in the study, and what was in the preparation that Hitmeback used.

Good things come to those who weight.

The Big Cat is a researcher and theoreticist. His advice must never be taken in the stead of proper advice from a medical professional, it is entirely intended for research purposes.


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needsize
(@needsize)
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27/08/2018 6:17 pm  

I'm curious... HitmeBack, were there any other substances it your solution? I know alot of people like to add finisteride to their Spironolactone solutions and that could cause a sytemic drop in testosterone.


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Big Cat
(@big-cat)
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27/08/2018 7:05 pm  

that's the curious part, both finasteride and spiro should increase test levels, or keep them the same, since the test is not bound to the AR.

Good things come to those who weight.

The Big Cat is a researcher and theoreticist. His advice must never be taken in the stead of proper advice from a medical professional, it is entirely intended for research purposes.


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HitMeBack
(@hitmeback)
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Posts: 82
27/08/2018 7:48 pm  

The product I was using was 2% Spironolactone solution from minoxidil.com
The ingredients listed are as follows : Spironolactone, alcohol, propylene glycol, BHT, sodium benzoate, water.


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Ivan D.
(@ivan-d)
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Joined: 2 years ago
Posts: 4
28/08/2018 12:27 am  

The only, but not realistic way it could have affected negative your Testosterone levels, I can right now think of, is perhaps by inhibiting the conversion of E2 to the weaker E1 (Estrogen/Estren) through inhibiting 17beta-hydroxysteroid-dehydrogenase, Spironolactone and some related derivatives seem to effect this. (1,2)
But I don't think, that a little bit of spiro would have such an effect.

(1)
Satoh T, Itoh S, Seki T, Itoh S, Nomura N, Yoshizawa I.
On the inhibitory action of 29 drugs having side effect gynecomastia on estrogen production.
J Steroid Biochem Mol Biol. 2002 Oct;82(2-3):209-16.

(2)
Tremblay MR, Luu-The V, Leblanc G, Noel P, Breton E, Labrie F,
Poirier D.
Spironolactone-related inhibitors of type II 17beta-hydroxysteroid dehydrogenase: chemical synthesis, receptor binding affinities, and proliferative/antiproliferative activities.
Bioorg Med Chem. 1999 Jun;7(6):1013-23.


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