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Topical Spironolactone

vitamin b zinc steroid

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#1 thetruth24

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Posted 08 August 2007 - 01:02 AM

Check this out.

Spironolactone has been used by many women with great success in regards to acne and oil production.

Well what if men want to take it? Well there is now a possibility that men can obtain the same effects as women, without having to suffer the consequences of taking oral anti androgens.

There is a topical form of Spironolactone out which inhibits the DHT and equally important, ALL OTHER types of steroids and anti androgens from binding to the receptor. There has been research that shown regular testosterone/dht in the blood stream, but a higher content in the local area of the sebaceous glands. In addition these receptors may be more sensitives to DHT.

Here is the study:
http://www.freepaten...om/4543351.html

You can buy it here:
http://www.cemproducts.com/tosp5.html

The previous studies on topical anti androgens showed failure for a number of reasons
1) The topical did not have a suitable vehicle

For example:Cyproterone acetate with ethinylestradiol
Initial studies showed no improvement with CA, because the vehicle was unable to penetrate the skin effectively thus unable to deliver the medicine to the correct place. But once they used a different vehicle, significant results were noted.

2) The medicine was metabolized too fast.

Now here, I am not to sure about the effects of Spiro. Some say it is metabolized too fast in the skin or whatever. But there is a new lotion out.(link above) that should be effective in reducing sebum.

The special thing about spiro is that it can block ALL types of steroids. It also resembles a steroid so it competes for the binding but does not produce any androgenic effect.

Please let me know what you guys think about the ingredients on the 5% Spiro. Is it a suitable carrier to penetrate the skin?

SIDE NOTE:

VITAMIN B6, ZINC, AND AZELAIC acid has proven to completely eliminate the binding of DHT in the sebaceous glands when applied topically




#2 jemini

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Posted 08 August 2007 - 02:13 PM

I looked into all these studies about dht inhibitors and antiandrogens and whatnot a few weeks/months back. Here is what I've learned through research and personal experience

Topical antiandrogens (chemicals that bind to the androgen receptor but don't activate it, thus blocking the effects of naturally occuring steroids) might have their place in acne treatment. Topical spiro might help and I do remember reading some message boards where people did have some mild success with it. There are a few problems with it however. Yes, it does get metabolized by the skin very quickly. Also, as you mentioned, finding the proper carrier solution is also pretty key. It also stinks pretty bad from what I here. Topical spiro could be effective in the proper carrier, maybe with some sort of time release technology to allow it effect the skin all day, but no one has yet created one for that purpose. There was a research chemical called ru58841 which was an effective topical antiandrogen with a decent safety profile, and a company bought the rights to it and it currently doing some research with it. http://www.strakan.c...tiandrogen.html
I know there are some labs in China that will synthesize it for you, but its expensive, exact dosage is unknown, shelf life and preservation is unknown and the purity from China is also questionable. People with hairloss have been buying it, compounding their own solution and having good results so it might work for acne since they function on perhaps a similar (but not the same) mechanism.

Also, DHT (a potent form of testosterone) DOES NOT CAUSE ACNE despite the logical conclusions. For the longest time, it was believed that dht caused acne since 5 alpha reductase 1 is a predominant enzyme in the skin and that dht is the main steroid which effects the skin. So logically, it was thought a topical medicine which inhibited this enzyme would significantly reduce the effect of natural steroids on the sebaceous glands. This is not the case, there was another study that was on the net somewhere though it was very hard to find that pointed out topical 5 ar 1 inhibitors did very little for sebum output or acne. I put this to the test personally but making a topical dutasteride solution. Dutasteride (brand name Avodart) which is used for enlarged prostate, though people use it for hairloss as well, blocks all forms of the 5 alpha reductase enzyme (both 1 and 2). It also easily penetrates the skin, and on the box warns that pregnant women shouldn't even handle the pill for fear of easy absorption. I tried this solution for about a month which absolutely no change in my skin for better or worse.

So what does this all mean? No one knows exactly, but I have my own theories. i believe that the androgen receptors are involved in acne formation, but not directly. Over the last few years dermatological research has been aimed towards a class of receptors known as PPARs (alpha, beta/delta and gamma). By manipulating these receptors they have been able to control sebum output, skin cell proliferation and other important factors involved during acne formation. Scientists are still piecing together how exactly they work together and I do feel that down the line a few years we will see acne medications with these receptors as targets. Anyway, back to my main point. It is known that for these PPARs to express properly (or improperly in the case of acne) they form dimers with other receptors, most notably different retinoid receptors and androgen receptors, probably others as well. My theory is that antiandrogens might work by indirectly inhibiting the activation of some of the ppars (though I couldn't tell you which ones), and that proandrogens (synthetic steroids) might help ppars to "Activate." That is why people with higher amounts of male androgens might be more prone to acne, even if the androgens themselves aren't the cause per say. I believe that retinoids might do something similar in an opposite manner. High affinity retinoids (tretinoin/retin-a and other retinoid metabolites) might inhibit ppar expression by preventing the two receptors to form proper dimers. And people with extremely low amounts of vitamin a are probably more prone to acne (vitamin a deficiency is pretty rare), though I am not 100% positive on this last bit, but it would make sense.

Anyway, didn't mean to make a post this long but hopefully it offers some insight. I used to be into the b6, zinc, azelic acid and any other form of dht inhibitor in existence, but that isn't the solution. IF it was, someone would have had a cure for acne by now. Maybe in 10 or 20 years.

#3 thetruth24

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Posted 08 August 2007 - 10:24 PM

Jemini, thanks for responding!

I've read differently from a number of sites, that DHT and other androgens do in fact stimulate the sebaceous glands which results in excess sebum. So saying DHT does not cause acne is incorrect. This is why women who take anti androgens notice a huge diminish in oil and acne. Maybe the topical form doesn't work, because as stated before, it gets metabolized too quickly and/or has a problem absorbing. Taken orally, there are numerous accounts of people becoming clear on anti androgens.

These PPARs sound very interesting indeed. Question though, why is it that acne only begins to form during puberty and subsides as puberty ends? Do these PPARs become active during this time like androgens? Undoubtly, androgens surge during this period and sure enough acne follows. But it is the possibility that these PPARs are, as you stated linked to androgens. With the increase of them I really like your theory though. Is there anything out right now, that inhibits these receptors?

By the way, did you get a chance to read the study I posted? Apparently, when they used a certain kind of carrier for the spironolactone, many people achieved significant improvements in oil production and acne

#4 jemini

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Posted 11 August 2007 - 08:47 PM

Ok, let me clarify a few things for you as you are on the right track. Bear with me if my post is slightly incoherent since I took a few klonopins and had a beer. (I know I know, not the most responsibly combination). Let me try to find the study, there was a pretty one which summed up my point nicely.

http://64.233.169.10...lient=firefox-a
read page 233

Anyway i can't find the study even though I know its on google somewhere, I think I even posted it at one point on this site. Basically the study showed that sebocytes were only minorly stimulated to dht, but majorly stimulated by the addition of dht and the PPARS. Only in rare instances such as PCOS where overproduction of dht may actually in it of itself cause acne. And according to my beliefs, antiandrogens cure acne not because they inhibit dht, but that they bind up the androgen receptor so these ppars cant form dimers with them. So while dht inhibitors and antiandrogens shere many common results when applied to the body, their slight differences causes one to haave an antiacne effect while the other to have a very trivial effect on acne. I cant sum up everything on androgens, ppars, retinoids and whatnot. It is very complicated and I am by no means an expert. But I do recommend anyone who can wrap their minds around scientific texts to google ppar's, the different types and how they work with each other and other receptors. I think this type of research will bring us much closer to a "Cure."

#5 thetruth24

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Posted 12 August 2007 - 09:17 PM

Thanks Jemini!

Would you mind joining the Resveratrol discussion? We are discussing exactly whats going on with PPARs and the different receptors.

It is suggested that the alpha receptor is in control lipid metabolism. There was a study with individuals with and without acne. THe ones with acne had significantly lower apolipoprotein A1, which is responsible for

Quote from autonomous:
"so what does it mean to have lower apolipoprotein a1? this lipoprotein is a part of hdl cholesterol and is manufactured by the liver to collect excess blood cholesterol and shuttle it back to the liver to be excreted through the bowels, otherwise it just hangs around in the body. Its a very interesting correlation but what it means exactly i dont know.
its interesting to see that ppar alpha can enhance lipid clearance and that ppar alpha is also seen to have a major role in sebaceous gland lipogenesis supposedly suppressing it, this information in a way seems to point to ppar alpha as still playing a major role in acne for its dual ability to influence both abnormal lipid metabolism and sebaceaous gland lipogenesis."

So maybe by activating the alpha receptor, there will be more "control" on oil production since the lipids will be metabolized better.

#6 nikkigirl

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Posted 13 August 2007 - 10:55 AM

i was a male with severe acne until i gave up and changed my sex.heres what i can tell you from my research.when i used spiro and estrogen(premarin)sepatately my skin would still break out but together my skin was perfect.i was on 100 to 200 mgs og spiro and 2.5 mgs of premarin daily.since this is putting a great risk with my health due to risks of heart atacks and cancer i decided to finally go to thialand this spring and under go srs.now my skin will break out once in awhile but not that often and i dont have to use meds to keep it clear.not suggesting guys do this but its was a very last resort for me.

#7 Listener

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Posted 14 August 2007 - 01:29 PM

Just out of interest..... are you saying you changed your sex to get rid of your acne? I'm guessing that's not what you meant.
No offence meant at all.


#8 reviresco

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Posted 17 August 2007 - 09:11 AM

so has anyone purchased this, i am tempted by either this or the vitamin cure stuff.

#9 Cal07

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Posted 14 February 2013 - 05:50 PM

Check this out.

Spironolactone has been used by many women with great success in regards to acne and oil production.

Well what if men want to take it? Well there is now a possibility that men can obtain the same effects as women, without having to suffer the consequences of taking oral anti androgens.

There is a topical form of Spironolactone out which inhibits the DHT and equally important, ALL OTHER types of steroids and anti androgens from binding to the receptor. There has been research that shown regular testosterone/dht in the blood stream, but a higher content in the local area of the sebaceous glands. In addition these receptors may be more sensitives to DHT.

Here is the study:
http://www.freepaten...om/4543351.html

You can buy it here:
http://www.cemproducts.com/tosp5.html

The previous studies on topical anti androgens showed failure for a number of reasons
1) The topical did not have a suitable vehicle

For example:Cyproterone acetate with ethinylestradiol
Initial studies showed no improvement with CA, because the vehicle was unable to penetrate the skin effectively thus unable to deliver the medicine to the correct place. But once they used a different vehicle, significant results were noted.

2) The medicine was metabolized too fast.

Now here, I am not to sure about the effects of Spiro. Some say it is metabolized too fast in the skin or whatever. But there is a new lotion out.(link above) that should be effective in reducing sebum.

The special thing about spiro is that it can block ALL types of steroids. It also resembles a steroid so it competes for the binding but does not produce any androgenic effect.

Please let me know what you guys think about the ingredients on the 5% Spiro. Is it a suitable carrier to penetrate the skin?

SIDE NOTE:

VITAMIN B6, ZINC, AND AZELAIC acid has proven to completely eliminate the binding of DHT in the sebaceous glands when applied topically

Has anyone tried this yet???



#10 mikito

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Posted 12 March 2013 - 05:29 AM

When thetruth24 says vitamin b6, zinc, azelaic has proven to completely eliminate the binding of DHT in the sebaceous glands when applied topically, has anyone tried this cream and had success?

 

Because I think its difficult to get a solution with this mix. I have read in an article that says it`s easy to get a cream with vitamina 6 and zinc, but the difficult thing is to add azelaic acid.