Topical AI's Superior for Gyno
- 11-15-2007, 06:58 AM
Topical AI's Superior for Gyno
Like many of you, I've had to deal with gyno. I've put a good amount of time and energy into researching methods of erradication. Along the way I've come to various conclusions, opinions and theories and have always shared them with you in order to raise awareness or bring new thoughts to the table.
The AI vs. SERM
It's quite obvious the difference. If you don't already know, an AI stands for Aromatase Inhibitor. This inhibits the enzyme aromatase from converting testosterone into estrogen, thereby depleting estrogen and starving ER (estrogen receptors). A SERM binds to the estrogen receptor itself, leaving estrogen to roam free in your body but not do damage like create gyno.
There have been arguments for both styles in erradicating gyno. Some people say Letro and AI's work better by eliminating estrogen and shrinking gyno.
Others say SERMs are better because they leave a homeostasis of test:estro (balanced), and attack the problem at the receptor specifically, instead of the whole body.
My view is that both will work, and consequently both have their place. AI's will starve the estrogen receptor and shrink your gyno, and a SERM will allow your body to rebalance itself without a 'rebound', enabling you to keep the progress you've made with an AI.
We'll be focusing on steroidal AIs.
Topical Delivery: What's so good about it?
1.) Sustained Release
Transdermal and topical AIs, such as Formestane, ATD and to a lesser extent 6-oxo haven't been popular for very long, but are showing a world of promise. Oral AI's, which by these I mean steroidal OTC aromatase inhibitors, are usually in capsule form. This ensures a fast delivery, and subsequent half-life that is shorter than a transdermal delivery. You'd be getting a burst of an anti-estrogen that would last 4-7 hours. What does this mean? It means in order to 'keep up' you would need to dose more. We all know that a higher dose of AI means less estrogen, which means more sides. With topical delivery, you'd be getting a steady flow for up to 10-12 hours with one dose. Making it 'more bang for your buck'.
2.) Local Delivery
These topical and transdermal AI's are what we call systemic. This means that no matter where you apply the gel, it will work throughout your whole body. Unlike topical fat loss creams, which target the area you apply the gel.
However! There has been anecdotal feedback that, somehow, it does work locally. Logically this makes alot of sense. I beleive if there is a OTC cure for gynecomastia out there, it has to be local. In other words, there are very few 'smart drugs' that would be target-specific. It's almost impossible to take an oral medication and have it work on a certain part of your body (IE male enhancement drugs. HAH!)
Whether it be the AI seeping into your breast tissue, the elimination of water/estrogen from the spot: logically and anectodally this is the best route. The problem lies in causing irritation from applying a topical gel to a certain area of your body everyday. This is why I recommend a EOD application to the breast, and the other days putting it on the ankles, feet, forearms, biceps. Parts of your body where there is less skin. This will prevent irritation to the area yet still have target-specific effects.
3.) More is not better
This is much like #1. I would much rather make 25mg of ATD stretch for 12 hours topically and applied locally to the breast area, rather than having to take 25mg and 25mg 6 hours later to cover myself. Higher estrogen depletion will cause side effects such as loss of libido, sore joints and lethargy. Why take more if you don't have to. For instance with Topical ATD, you can control topically how much you take. This would make lower dosing and tapering much easier.
The Future of Gyno-Related Products
Using my Tibetan black magic, crystal ball and transcendal meditation, I have seen the future of gynecomastia treatment. It lies in topical formulas.
I have heard rumors of companies creating a gyno-specific topical formula. The potential for making money in this arena, between pubertal gyno and also uneducated youngin's running over the counter steroids, is quite substantial. It only makes me wish I had the resources to make my own.
Logically, a topical formula makes the most sense. If anything is going to fix gyno, it's going to be a locally applied transdermal blend. I'm guessing including, but not limited to, Yohimbine for fat loss, Resveratrol for possible SERM properties, and a mixture of AI's such as a small dose of ATD and Formestane. It may take 6 months of daily applications, but those of you who know what it feels like to have The Nasty™ know that you are willing to take whatever measures to reduce or erradicate your gyno.
Perhaps there is a compound out there waiting to be stuck in some Penetrate formula and sold to the starving masses. But until then it looks like a Topical AI would be a very good bet.
Last edited by RenegadeRows; 11-15-2007 at 07:25 AM.
- 11-15-2007, 07:30 AM
Great read man.......now go pitch to Glaxo or someone and get it done!
- 11-15-2007, 10:14 AM
I concur, topical will likely resurface as a key player despite the boom in orals.
Site specificity however, remains somewhat elusive for the average consumer.
A site specific patch delivery system may be an avenue...but putting bandaids on your nipples is more a fetish thing. lol
11-15-2007, 10:32 AM
11-15-2007, 12:32 PM
does anyone have any opinions on AIFM? i have heard some good reviews on it, but id like to hear from the AM guys on this.
11-15-2007, 01:02 PM
11-15-2007, 02:37 PM
11-15-2007, 04:27 PM
11-15-2007, 05:22 PM
11-15-2007, 05:38 PM
While I agree with your sustained release, and "more is not better" part I am not so sure you can say anecdotally that a transdermal AI is site specific. Most of the Formestane feedback you here about "destroying my gyno..." is really not guys with gyno imho. Most people are just paranoid and have chest fat they need to deal with.
Do you know of any studies show site specificity with these compounds. How do the site patches Bio stated work exactly (not too familiar with them)?
Either way its a good discussion. Should see if you can get Primoridalperf to comment as I am guessing his trans knowledge is pretty good.
Good write up/post though bro . Something like this has been on my mind for a while. Just dont understand the mechanism to provide site specific application to the breast area.
11-15-2007, 06:14 PM
I admit that AIs are systemic in their delivery, however its hard to ignore a topical application as not having SOME sort of effect locally.
I'd like to hear others input as well, I think it could be a good discussion.
11-15-2007, 08:32 PM
11-15-2007, 09:38 PM
Just some random info I thought I would throw in this thread:
Letro powder = Molecular Weight: 285.30274 g/mol (so throwing letro in a transdermal carrier is possible)
Add to say abliderate?
Then found this study, interesting:
ScienceDirect - The Journal of Steroid Biochemistry and Molecular Biology : Hormonal effects of aromatase inhibitors: focus on premenopausal effects and interaction with tamoxifen*1Hormonal effects of aromatase inhibitors: focus on premenopausal effects and interaction with tamoxifen*1
M. DowsettCorresponding Author Contact Information, E-mail The Corresponding Author and B. P. Haynes
Academic Department of Biochemistry, Royal Marsden Hospital, Fulham Road, London SW3 6JJ, UK
Available online 16 September 2003.
Third generation aromatase inhibitors have excellent specificity. Some reports indicate that letrozole may have a minor effect on cortisol synthesis but these were not confirmed: valid comparisons with other aromatase inhibitors requires randomised study.
The putative use of a third generation inhibitor as a single agent in premenopausal women has been investigated using YM511. It was hypothesised that in this situation site-specific suppression of estrogens in breast carcinomas, without systemic effects, may lead to a down-regulation of tumour proliferation. Plasma levels of androstenedione and testosterone were significantly increased by 2 weeks treatment with YM511. Mean plasma estrone levels were suppressed, but some plasma estradiol levels were abnormally high and others abnormally low. These differential effects of YM511 on circulating estrogens supported the concept that peripheral synthesis of estrogens might be suppressed while ovarian production remained high. However, YM511 did not demonstrate anti-proliferative effects in hormone sensitive breast carcinomas.
Consideration of the pharmacology of the estrogen receptor during tamoxifen therapy indicates that tamoxifen effectively saturates the receptor (>99.94% occupancy) in postmenopausal women. The addition of an aromatase inhibitor in this situation would be very unlikely to affect the biological activity of the estrogen receptor. This provides a possible explanation why the clinical efficacy of tamoxifen combined with an aromatase inhibitor appears to be equivalent to that of tamoxifen alone.
Author Keywords: Hormonal effects; Aromatase inhibitors; Tamoxifen; Breast cancer; Estradiol; YM511; Premenopausal
Last edited by Travis; 11-15-2007 at 09:39 PM. Reason: Edit: added link to abstract...
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