Issue 1

By: Big Cat

Note: The views and comments in this section do not necessarily reflect those of Bodybuilding.com and its owners.

Happy New year to everyone. It's been a horrendous year for me, so I hope for everyone this may be the beginning of a new and better year. Undoubtedly it was a New year with many good resolutions, and for most of us at least one will pertain to our physique goals.

Well, with my long awaited return to the Bodybuilding.com cast of writers, I hope I can be of some assistance in furthering your knowledge on training, supplementation and nutrition in the coming months. Let's hope it will be a new year with new groundbreaking research, new successes, better techniques and, well, I guess I'll be the one to say it, less FDA involvement.

Ephedra Ban

Yes, the Ephedra ban, that seems to be the big issue right now, huh? Now I could go on a rant about how the FDA isn't the least bit consistent in what they do, what a shame it is they took away a perfectly safe and effective supplement and why on earth they don't address more important issues. But it seems the press is doing a good job of highlighting the debate. The FDA blames the supplement companies, the companies blame the FDA, they both make good points and this debate will ultimately solve absolutely nothing.

All the screaming voices in outrage at the ban, and all the under-educated over-hyped anti-supplement lobbyists doing the opposite, result in a status quo and nothing will change. Let's face it, ephedra is banned. So what is left for me to say on that?

On the ban itself, absolutely nothing. I would be preaching to the choir anyway. But let's have a look at the results of a ban, so we can all look back next year and say 'We told you so'. Because realistically what will come of it? A thriving black market for starters, no doubt. I for one am not that upset.

Results Of The Ban

Most ephedra products can't hold a candle to real ephedrine Hcl. And here in Europe where ephedra has been regulated for some time, it has been easier to inform people of benefits and dangers, and steer them toward actual ephedrine Hcl as opposed to all this ma huang crap. Prices will be a lot cheaper as well.

Every pharmacist in the world buys ephedrine Hcl in bulk at very low cost, and a lot of that will no doubt make it to the black market at next to no cost. So I don't necessarily think this ban is so bad for our community. Cheaper and more effective products.

But lets look at the people that are going to feel the effects of the ban pretty soon. The supplement companies and the public health (FDA's responsibility , isn't it?).

Supplement companies are out a major plus. Ephedra, though not really as good as actual ephedrine, was one of the few OTC supplements that by far outweighed the benefits of its illegal counterparts. There are so many regulated or illegal drugs for fat loss out there like clenbuterol, albuterol, phentermin, DNP, thyroid hormones and god knows what else. And none of them was as safe, or as effective as ephedra/ephedrine.

Sure, the lot of them were more potent, but only ephedra was suited for the long term goal of weight loss. And seriously, whoever lost weight to their satisfaction in only 2-3 weeks? No one that I know of. A good diet will easily last 12-20 weeks. Only ephedra maintained its effects over such a period of time. So the initial blow will be quite big. But the industry will rebound.

The initial blow is somewhat overcome by the drastic increase in revenue due to panicked ephedra-loyalists stocking up while they can, which could easily tide them over through the rougher end. And after that, as more people find their way to the black market with cost-effective ephedrine Hcl, the supplement companies will find there are great profits to be made, not in the manufacture of second rate, no-good fatburners, but in legal supplementation to augment ephedrine.

There is a host of legal supplements out there that make ephedrine based products so much more effective. Its not that far a fetch to bring out a product to meet the demand for that, since all these ephedra stacks are now outlawed anyway.

Public health is what I am more concerned about. With the loss of ephedra, the last decent OTC fatburner has exited the stage. And as I stated, mark my words, more and more individuals will find their way to a black market that can supply it at a lower cost. The downside to that is, once you are on the black market, its only a small step to purchasing products that aren't as safe.

It's a small step to clenbuterol, T3 and so on, but what happens when they make it to DNP? The promise of faster fat loss is an enticing one. And DNP is a potentially lethal product. I'm predicting that in future years we will see a lot more weight-loss related deaths that will by far exceed the small number of idiots who did not manage to use ephedra correctly.

And trust me, with the rising epidemics of obesity and Type II diabetes in industrialized nations, the loss of an effective and safe weight loss supplement will place an extra burden on what is already the greatest threat to our health today. It's a ticking time-bomb under our society. And most of the people around us that do not share our beliefs on health and exercise, will die from being too fat, or trying to get leaner.

That, my fellow bodybuilders, is the legacy of the FDA and the government. They do nothing to stimulate exercise and health, but they ban safe and effective fat loss aids, allow the farces of court cases against fast food restaurants and persist in perpetuating the true cause of the epidemic : our own lazy nature.

So what has the FDA achieved realistically? It has managed to ruin the day of the few upstanding citizens that will not purchase ephedrine illegally, it has put out a mortgage on public health, has increased the revenue for people selling things illegally, and the government has lost yet another part of its tax income, from what was a very lucrative business.

The only question I have is how these people can sleep at night doing what they do? Because for the rest its no skin off my back. In the wake of this, we will look back many times on this decision, smile and say 'We told you so'. But who ever listens to the voice of reason?

Fibrates

A lot of people have written to me asking for opinions on this new hype, namely fibrate drugs. A little background for those that haven't yet heard of it, Fibrates are drugs prescribed for people with high cholesterol. They manage to reduce serum fatty acids and in the wake of that cholesterol, because they increase fatty acid oxidation.

The recent hype started with a short piece in mind and muscle magazine by spook, who pointed out that increased fatty acid oxidation makes a potent bedfellow for our current line of lipolytic supplements and drugs. Most active weight loss substances target lipolysis, or the release of fatty acids from fat deposits, leaving us largely to rely on a very strict diet to actually burn the released fatty acids.

If we could improve oxidation of fatty acids we could increase our fat loss efforts significantly. Now the article in question was rather short and unsubstantiated, but spook has admitted this and promised to write a more detailed follow-up and I trust he will do so. Since I also trust he will do so in more detail than I can here, I won't delve into that any further, but instead address some other issues related to it.

How Do They Work?

Fibrates work as agonists for the alpha form of peroxisome proliferator activated receptors. I have long felt that these receptors held a lot of promise in regulating our metabolism. But I, on the other hand, am more interested in two other pathways, namely the agonism of the delta receptor and the antagonism of the gamma receptor.

The issue of the delta receptor was raised, and the comment came that the delta receptor only assisted slightly in the activities of the alpha receptor. While this holds true in the liver, where the point was discussed and substantiated, this does not hold true in skeletal muscle fiber.

In muscle cells it was shown that the delta receptor activated preferential lipid utilization, beta-oxidation, cholesterol efflux, and energy uncoupling, whereas the alpha receptor's primary role was fructose uptake and glycogen formation, which may be slightly in contrast with our fat loss purposes.

Seeing as how muscle mass is a peripheral, metabolically active tissue that, at least in bodybuilders, can make up for well over 50% of total bodyweight, I'd say this is most definitely worth looking at, being far more promising for active people, than PPARalpha agonism. Unfortunately there are no commercially available PPARdelta agonists.

Bezafibrate

What was interesting to learn however is that at least one fibrate, bezafibrate, activates the delta receptor as well. The debates regarding fibrates have often stated that bezafibrate was by far the most potent fibrate.

But in contrast to the current theory that it is simply more potent, I will gladly state that its increased activity is most likely due to increased fatty acid oxidation in over 40% of metabolically active tissue, something no other fibrate could hold a candle too.

Meaning bezafibrate can easily give you the benefits of both PPARalpha and PPARdelta agonism. There is another product that can activate both these receptors, namely carbacyclin, a prostacyclin analogue.

As a second point, I'm currently also looking into benefits and downsides for PPARgamma antagonism. The gamma receptor seems to primarily increase Fatty acid synthase, lipid storage and glucose uptake, all parameters that would negatively affect fat loss. By somewhat downregulating the gamma receptor, we could also be adding a great plus to our dieting efforts.

Especially for those of us who believe in carb-ups and refeeds. The funny thing about this, is that many bodybuilders have been using gamma-agonists to aid them in their quest for more muscle and less fat, namely drugs like metformin and rosiglitazone.

But then bodybuilders have been known to do dumber things than that in the past, which is most likely the reason people raise there eyebrows when you say you are a bodybuilder. There are a number of gamma receptor antagonists, but benefits must first be weighed against downsides.

In short, the research of peroxisome proliferators activated receptors with regards to body composition has taken way to long to commence, and it will open a great new field of exploration for some time to come.

I would however caution against jumping on this bandwagon until we know more about long term side-effects and results. And as always, to refrain from using any type of prescription drug if you are not under medical supervision.

References

Dressel U, Allen TL, Pippal JB, Rohde PR, Lau P, Muscat GE.
The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells.
Mol Endocrinol. 2003 Dec;17(12):2477-93. Epub 2003 Oct 02.

Peters JM, Aoyama T, Burns AM, Gonzalez FJ.
Bezafibrate is a dual ligand for PPARalpha and PPARbeta: studies using null mice. Biochim Biophys Acta. 2003 Jun 10;1632(1-3):80-9.

Kim MJ, Deplewski D, Ciletti N, Michel S, Reichert U, Rosenfield RL.
Limited cooperation between peroxisome proliferator-activated receptors and retinoid X receptor agonists in sebocyte growth and development.
Mol Genet Metab. 2001 Nov;74(3):362-9.

Do You Really Need Estrogen Control?

This is a controversial topic, and I will no doubt get a lot of heat for bringing it up, but I feel it is a point that needs to be addressed. In users of aromatizable steroids, estrogen levels will rise and we all know this can lead to complications if estrogen levels are high enough, the most known example being gynocomastia, or the growth of breast tissue in men.

For a long time now the debate has raged on about whether or not, however, these excess levels of estrogen contribute to the anabolic potency of these anabolic androgenic steroids. My personal belief is they do. As with androgens, a great number of benefits are seen when comparing normal levels of estrogen to low levels, or no estrogen at all.

This is to be expected, and as such you will not hear an educated man suggest that you need to block estrogen entirely. In either case, the maintenance of a normal level of estrogen is wishful to say the least. Therefore its not advisable to use only non-estrogenic steroids, or massive amounts of anti-estrogens. There is however little to no data on the effects of excess estrogen compared to physiologically normal levels.

As with androgens one might expect that some of these benefits will be expressed more, while others will become irrelevant. There is however no data on this, so this debate will no doubt rage on for some time to come.

Anti-Estrogens

The issue I wanted to raise however is another entirely, not directed at the benefits of estrogen, but rather the downside to using anti-estrogens, especially aromatase inhibitors. First of all, the immediate estrogenic risk is exaggerated to a great extent. A normal person will not experience gyno in doses of 750 mg of testosterone per week or less.

So in most cases, people start taking aromatase inhibitors simply as a matter of precaution, not because they need them. This is a behavioural pattern I want to warn against. It has come to my attention that people using aromatase inhibitors often experience MORE problems after use then before. People coming off a cycle, and at a time when estrogen levels are extremely low even, they begin developing gyno.

Or people who did not get gyno before, suddenly developing gyno when using a lower dose of product. Something I found quite odd. In the first case, I simply attributed it to there not being as much androgen, but that would hardly be the case in the second event. So I did some digging, and it appears that you are, in most cases, shooting yourself in the foot with the use of aromatase inhibitors.

First of all, estrogen increases are not linear. Its not because you have a given amount of estrogen with the use of 500 mg of testosterone, that that means you will automatically have 50% more estrogen if you use 750 mg. Studies show that high estrogen levels will downregulate aromatase so less estrogen is formed. And secondly, it appears that low estrogen levels may upregulate the estrogen receptor, making you more sensitive to estrogenic effects when estrogen levels increase again.

So whilst not needing estrogen control (except in very high doses) you are paying for an expensive and unneeded product, that only perpetuates the need of this same product, as it makes you more prone to estrogen related problems.

Mind you, that does not mean there is no need for estrogen control at all. But I would advise against the use of aromatase inhibitors and in favour of selective estrogen receptor modulators (like Clomid and Nolvadex). There is no way around these anyway, as they play a key role in post-cycle recovery, but also they do not lower estrogen levels and they still exhibit some activity at a number of receptors so they will not affect aromatase or the estrogen receptor to the same extent.

On the contrary. I would also caution against unneeded estrogen control without the care of a physician who can check if your estrogen levels are still high enough to be within physiological range at least.

References

Nakamura J, Lu Q, Aberdeen G, Albrecht E, Brodie A.
The effect of estrogen on aromatase and vascular endothelial growth factor messenger ribonucleic acid in the normal nonhuman primate mammary gland.
J Clin Endocrinol Metab. 1999 Apr;84(4):1432-7.

Agarwal VR, Sinton CM, Liang C, Fisher C, German DC, Simpson ER.
Upregulation of estrogen receptors in the forebrain of aromatase knockout (ArKO) mice.
Mol Cell Endocrinol. 2000 Apr 25;162(1-2):9-16

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