Roundtable Discussion on Methyls

Longdog

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Found this on BB.com. Discussion between Will Brink, Patrick Arnold, Bruce Kneller and Par Deus.


[ Q ] What are your thoughts on methylated compounds and their impact specifically on H.R. 207, the Durbin bill, and the Bidden bill? Has the recent introduction of these substances "nailed the coffin" so to speak on a prohormone ban that is inevitable, or do you feel their widespread availability to be no less threatening--in the government's eye--than that of the earlier prohormones, 1-testosterone and the like?


Patrick Arnold: The USFA has made it clear that it represents responsible companies that sell legitimate prohormones and that market their products in ethical manners. The USFA has not hidden from the fact that our industry is riddled with inappropriate (and outright illegal) products and irresponsible, unethical advertisers. The USFA has let the government know that it agrees that the industry has its problems and needs to be cleaned up. Draconian legislation—that bans the good with the bad—is not the answer however.
So although in some manner we try to distance ourselves from these products, we still cannot stop our foes from deliberately lumping them all together. What worries me is the fact that these methylated products bring with them a whole host of potential toxicity issues, and eventually some people might fall victim to a serious illness.

For instance, let’s say that someone with compromised liver function starts taking one of these compounds and falls victim to life threatening liver dysfunction. When that happens, will the media and prohormone bashers make efforts to differentiate between these synthetic derivatives and natural prohormone products? Of course not! They will talk about how andro landed someone on the liver donation list or something. Then we are in serious trouble

Bruce Kneller: I think all of the steroidals, prohormones/prosteroids, whatever the "catch word" of the day is—“legal steroids" if you will—if they impart any direct androgenic or anabolic effect, either by themselves or by a first order metabolite, well they are all done in the next 12 months maybe 18 months tops.

So selling methylated stuff isn't going to change a damned thing. When you are doomed, you are doomed. It's not like its going to cause prohormones/prosteroids to be made C-III, they're heading that way anyhow thanks to assbags like Joe Biden who manipulate this issue solely for political gain. And frankly, I don't see how a methylated compound is any different than an ether compound or an ester compound from a legal standpoint.

I am not talking about from a chemical standpoint or the physiological effects they impart, I am talking LEGAL standpoint. If the esters and ethers are legal, so are the methyls. No difference.

I have run a lot of these scenarios, these types of questions, by a rather prominent attorney who doesn't want to be involved in this thing publicly. I was told point blank that the methyls are not controlled substances. You can argue they may or may not be unlicensed drugs but this argument would be true of the ethers and esters as well as any substance being sold as a food supplement that is somehow "modified" from its natural form and not specifically approved as a food supplement in writing by the FDA.

This would probably include phenibut and even certain esters of Vitamin C. I know I am being long winded here but the bottom line is the methyls are a very, very small part of the supplement hormonal market and an even smaller, almost trivial part of the supplement market en toto; they will never be sold in places like GNC, and maybe 50,000-100,000 bottles of ALL OF THEM will be sold worldwide before the impending ban hits. They're inconsequential. A minor bit player.

Will Brink: I think the industry passed the government’s comfort level a long time ago with the "andro" products. I think they are still trying to play catch up as to what is even out there, some of them still probably thinking androstenedione still being popular. I am sure methylated products won’t exactly help the industry defend the sale of the "andro" products, but at the same time I don't think the FDA et al care about what they use as a final excuse to pull such products versus simply looking for any excuse to pull them.

One thing you can count on in the greedy short sited supplement industry is their ability to push the envelope and give the "gubment" a reason to pull such a product. The industry being unable to show any self regulation, due to the fact that it's run primarily by greedy short sited scumbags, prevents self regulation and even common sense.

Par Deus: I think the coffin is already pretty much nailed for the anabolic prohormones. However, I think methylated androgens as supplements has the potential to take things to another level, and make it more likely that they would go after 7-keto, 6-oxo, pregnenalone, etc., if not the entire industry. It is very, very strong ammunition for them to claim how irresponsible the industry is in offering compounds this potent, with potential for hepatotoxicity, and which are so easy to obtain and administer.

Right now, THG seems to be the androgen of interest in the government and media. There was an obvious attempt by the government to tie this into the prohormone industry, both with public statements to that effect, and their planting of Patrick's name in some articles. Fortunately, the media has focused on the sports side of things much more so than the supplement industry/prohormone side of things.

Unfortunately, our foes in the government and the USADA have methylated anabolic steroid supplements just waiting to serve as poster boy for the next round of propaganda.

[ Q ] Further, what impact—if any—do you feel the recent abundance of these compounds has or will have on the public's perception of the sports supplement industry as a whole?


Bruce Kneller: I don't think the general public will ever even know about them for the most part, or know specifically that they are somehow "different" from any other hormonal supplement. Most of the "GNC'ers" blindly think "andro" and what they remember from some pseudo-scientific piece they saw on pulp television when you talk about these substances. Go into GNC and start talking about the difference between a 3,17 diol and a 3,17 dione with anyone, even the guy working behind the counter and I bet you will get a blank stare back at you. Clueless.
To the public at large, they are all the same thing, same compound, there might as well be zero difference between them to most of America. So I don't think that the addition of 17-aa'ed hormonals to the market is going to alter the public’s perception of us one iota in either direction. Now if some dickhead reporter with a hard-on for the supplement industry does some slanted, yellow journalism type piece targeting methylated hormonals, that might be a different story.

Will Brink: Being the public is as dumb as dirt, I don't think they have any impact beyond what androstenedione has had already. To the public, they are all andro products, evil steroids that will kill you faster then Joe six tooth public can reach for another drink or cigarette.

Par Deus: I think it has the potential to be very damaging. Not only are these anabolic steroids, but they could contribute to liver damage, and they are very easy to administer in that you do not have to rub on a gel or inject yourself. You just have to swallow them like... Vitamins.

Patrick Arnold: I don't think the general public will ever really know what is going on. I DO think that congress will however, and they will see how people are taking advantage of the lack of legislation (more accurately, the lack of ENFORCEMENT of existing legislation but that's not how they will view it) in regards to nutritional supplement products.

They will see that a serious public health issue is arising. This may lead them to lend knee jerk support to some of the ill founded and dangerous legislation out there such as the Biden bill and the Durbin Bill.

[ Q ] What about the relationship between methylated compounds and liver toxicity? How significant is the threat they pose; is it overrated, or not emphasized enough??


Will Brink: I have not personally heard of increased liver values, but it would not surprise me. Of course increased liver values from oral steroids are as a rule overrated anyway, and usually go back to normal post cycle. This does not mean people should ignore increased liver values from the use of any steroid, or other medication, but as a rule, increased liver values are not an indication of liver damage when it comes to oral steroid use, whether it be andros or illegal steroids.
Par Deus: I think the dangers are overstated, as with about anything, but the potential for them to contribute to problems definitely seems to be there. If you do not have other predisposing factors, it probably would not be a problem, especially if appropriate caution were taken with dosing, adjunctive supplements such as NAC, silymarin, etc. are used, and enzyme levels are monitored, but most people do not do this.

A large % of people treat these potent drugs like they were little more than creatine or vitamin C. As long as the companies are not misleading (which of course many are), I think that it should be the consumer’s responsibility if he or she wants to be a dumbshit. But obviously our paternalistic government does not view it this way, not with the infantile masses, crying to be taken care of.

Patrick Arnold: The medical literature makes it very clear that the liver toxicity from methylated steroids is significant. Cases of benign and malignant tumors, and more commonly peliosis hepatitis (formation of blood filled cysts in the liver), related to use of these compounds has been widely reported.

One must understand of course that the development of these ailments is very rare in individuals with healthy livers. However, a substantial amount of people have compromised liver function, or pre-existing liver disease, and are totally unaware of it because individuals with such conditions are often asymptomatic. When one of these people starts abusing a methylated AAS they put themselves at risk for the development of one of the aforementioned serious liver disorders.

In addition to these potentially life threatening liver diseases, there is also the issue of adverse effects upon blood lipids. The usage of 17alpha-alkylated steroids is strongly linked to elevated total cholesterol, and decreased HDL cholesterol. Users should be aware of this, and if one has pre-existing blood lipid problems (high cholesterol) they probably should avoid these compounds.

Bruce Kneller: What liver toxicity? Has it been proven? Show me a study that shows methyldienolone or methyl-1-testosterone is liver toxic. Is it anywhere in any peer reviewed, referred journal? Yeah, hormones that are 17-aa'ed have been sometimes linked to transient rises in liver transaminase levels. So what? Tylenol and Jack Daniels have been linked to the same f***ing thing. This liver toxicity issue is way overblown. It is like an urban legend.
Many pro bodybuilders use upwards of a gram of methylated steroidals per week. Are any of them dying of fulminant hepatic failure? Are any of them needing liver allografts? Are there hundreds of write-ups in journals about bodybuilders showing up in emergency rooms with clinical signs of yellow jaundice? The answer of course is "no". Used in moderation, methylated hormones are probably no more dangerous than Tylenol or a shot of Stolichnaya.

[ Q ] How do you come to a conclusion on safety, or lack thereof, given the fact that there are few studies on humans that explore the relationship between dose and/or duration and liver toxicity?


Par Deus: For this very reason, it is pretty difficult to come to absolute conclusions and recommendations, but there is enough to suggest that they probably are quite capable of contributing to problems, if other variables line up.
Patrick Arnold: There is no way to come to any conclusion without any such studies.

Bruce Kneller: Why are you singling out methylated legal steroids here? I mean, there are a ton of other supplements that are being sold that we have no clue whether they have toxic side effects or not. Remember Usnic Acid? How about Guanidinopropionic Acid? Or Glycocyamine? How about Sclarea Extract? I can think of a list a mile long of "supplements" that are perfectly legal that might cause serious hepatic, renal, cardiac and/or other organ system damage.

The only way to determine this is through study. This takes money. And if you want studies on methylated legal steroids, why should you stop there? Why not examine each and every other supplement being sold for safety or toxicity? You can't be prejudicial based on urban legends of toxicity.


"I think crack should be available to adults, if they choose to use it."
We either fundamentally change the way the ENTIRE supplement industry is allowed to bring stuff to market by making companies conduct all sorts of studies, or we leave it alone like it is now. And if you change it, you have essentially really just created a secondary or "junior league" pharmaceutical industry. And if you change it, who will pay for all these studies? Who wants to pay $500/kg for creatine or whey protein isolate? So there really is no way to come to a "conclusion". It's either safe or it isn't. You have to wait and see. This is how we have always done it in the supplement industry. Why **** up a good thing like we have now?

Will Brink: The best you can do at this point is extrapolate from other oral steroids more or less. Each, having different properties, such as androgenic/anabolic ratio, ability to convert to estrogen or DHT, etc., has to be looked at individually, so blanket generalized statements are difficult to make.

[ Q ] We hear a great amount of feedback pointing to users experiencing a considerable array of side effects, some of which are more severe than others. How safe are these substances, how much do we know about them, and should they be readily available over the counter for anyone to use?


Patrick Arnold: We know about 17alpha-alkylated compounds and the risks associated with them IN GENERAL (qualitatively). We do NOT know the DEGREE of toxicity associated with each of these designer compounds however. Nor do we know if any of these compounds have unique toxic effects above and beyond that which is common to the class of 17-AA androgens as a whole.
It is my opinion that the possibility for toxicity with these compounds is high and that not enough is known about these compounds to predict how safe or unsafe they are. I therefore think that they should not be readily available over the counter. It’s all a moot point however since these compounds are not legal for sale anyway—as they fall into the classification of "unapproved drugs"

Bruce Kneller: What side effects are you talking about? That they get big and strong and lose fat? Yeah, there are a lot of people "complaining" about that. I know a number of people using methylated legal steroidals and none of them are manifesting any real side effects that would be unique to the methyls.

Sure, acne, oily skin, libido changes and some hair loss have occurred, but these side effects happen with non-methylated legal steroidals too.

Adding a methyl functional group to a steroid at C-17 doesn't magically make it some monster side effect inducer.

Will Brink: Of course the safety of these compounds is more or less unknown in that data is lacking. We can extrapolate from data and experience from steroids in general however. The side effects I keep hearing, in particular with 1-MT, are extreme lethargy, drops in libido, and increases in blood pressure.

One of the oddest, but pretty consistent, is reports of severe muscle spasms. Being I have never seen or heard about that effect from other steroids, assuming it's a real effect from 1-MT, it would be a steroid specific effect, which I personally can't explain. Someone like Pat Arnold, who spends a great deal of time researching such things, might be able to come up with a plausible mechanism.

Par Deus: I think crack should be available to adults, if they choose to use it. It comes down to the person—some will tolerate a lesser ratio of benefit to harm if it means significant benefit and, of course, the actual real world ratio will differ among individuals.

[ Q ] Considering the safety concerns, whether overemphasized or not, should these compounds be sold with no concern for the industry? Should irresponsible free enterprise be allowed to destroy the availability of all prohormone-related compounds?


Bruce Kneller: I don't really understand what you're getting at here. I don't see how selling methylated legal steroids is irresponsible free enterprise and I don't see how it is destroying the availability of these compounds one bit.
Will Brink: They are already being sold with no concern for the industry as the industry is full of people who care not at all about the industry as a whole, but how they can make a quick buck and get out.

I can count on one hand the "white hats" in the industry. The rest are out for themselves and generally don't care about the industry as a whole or see the bigger picture regarding what they are selling, or what effects their marketing strategies have, on the industry.

Par Deus: In a perfect world, the government would do its job in protecting people from fraud and misleading claims, and let adults make their own decisions and take their own responsibility, but that is not the world we live in. I do not think companies should sacrifice the industry for their own gain, but again, in the world we live in, that is what almost everyone will do without a second thought. I would rather the government go after only the offenders than go after everyone, but I certainly do not trust them to exercise such discretion.

I would certainly like to see supplement consumers display the ability to think beyond the current moment, take note of the long-term ramifications that could result from the sale of these products, and treat the companies accordingly.

Patrick Arnold: Our industry is not regulated, and unfortunately there is no way to stop people from selling whatever they want, no matter how dangerous or inappropriate the products may be. Many people just see that there is a quick buck to be made and whether they hasten the demise of our industry in the long run is of little concern to them.


About The Authors

Will Brink:
Will Brink is the author of the best selling e-books Diet Supplements Revealed and Muscle Building Nutrition, each of which can be purchased through our affiliate program, or by going to www.musclebuildingnutrition.com. Will is also the author of the best selling print book Priming The Anabolic Environment. He writes a monthly column for MuscleMag International and is considered by many as one of the top (if not THE top) gurus on supplements and training in the US and globally.

Patrick Arnold:
Patrick Arnold is a renowned chemist who is responsible for the introduction of androstenedione to the market as well as other second and third generation prohormone products. Patrick currently is president of LPJ Research Inc., an Illinois company that manufactures bulk prohormone products as well as other dietary supplement ingredients. He also heads a private label supplement company called Ergopharm that specializes in prohormones. Patrick can regularly be found on the Avant Labs Forums, or by visiting www.ergopharm.com

Bruce Kneller:
Bruce Kneller has been "hanging around" the magazine and supplement industry in one form or another since 1994 when he first met Dan Duchaine and became Dan's "eyes and ears" while Dan was incarcerated in the federal penitentiary system. Bruce was the medical editor for what is considered Duchaine's grandest work, the diet handbook Bodyopus. Bruce has also written under his own name for Muscle Media, MuscleMag International, and most recently, he has been made a staff columnist for Muscular Development Magazine.

Bruce (along with Bill Roberts) was the first person to come up with the idea of using a prohormone in a topical application (Androsol by Biotest) and although the formula was crude by today's standards, it was an effective supplement that set the stage for an entirely new direction in sports performance supplementation. Currently, Bruce is working on an aromatase inhibitor called 3b-hydroxyandrost-4-ene-6,17-dione (3-OHAT) and a more effective version of 7-keto-DHEA, both of which he has patents pending on.

Caleb Stone:
Caleb Stone, President and Lead Developer of Avant Labs (aka Par Deus), can be largely be credited with making leptin, "refeeds” and the "fed state" common topics of discussion in bodybuilding circles. Caleb Stone has recently translated his theories on the matter into the groundbreaking Cellular Metabolic Optimizer LeptiGen, which was released for test marketing in mid-July 2003.

In addition to numerous articles for Mind and Muscle, Mr. Stone has recently ventured into the print magazine world, with translations appearing in the Italian "BIG" magazine, and Japanese BodyPower, as well as articles for IronMan and Muscle and Fitness in fall 2003 and Early 2004. Par Deus and Avant Labs have also been favorably mentioned several times in Bruce Kneller's column in Muscular Development.
 
bioman

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You can really see who the various stake holders are in that column even without direct knowledge of who's who.

Kneller-sells methyls and wants to sell more-though I agree with most of his statements, he'll fan the fire of the PH ban with his rhetoric

Pat- choses not to sell methyls but is also trying to salvage anything he can of the PH market. His conservative approach in trying to sway the legislation is realistically the only way to go.

Will Brink- simply knows the supp industry. Doesn't sell or use PHs
 
Sir Foxx

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Interesting read. I don't think Bruce(at the end of the article, bio info) was the first to bring topical delivery to PH's on the consumer market. I think that award goes to the Dr.(can't remember his name off hand) who owns Medlean.
 

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