A few years ago, research started coming out about the effects of common OTC painkillers effects on muscle growth. If you are new to bodybuilding in recent years, you may have missed the big news when it first came out. Many bodybuilders take them to relieve DOMS (muscle soreness) from weight training or some other ailment and don’t know about this side effect. This is also important to know because many fat burning supplements, such as hydroxycut hardcore, put willow bark ( natural form of aspirin ) in it. Acetaminophen ( Tylenol ) and the class of drugs called NSAIDS , which includes the OTC painkillers, ibuprofen (Advil, Motrin) and naproxen ( Alleve ), all have an effect on protein synthesis.

Studies on painkiller effects on protein synthesis:

One of the first studies to come out was published in
J Clin Endocrinol Metab. 2001 Oct;86(10):5067-70. It was done on 24 males to either receive ibuprofen, acetaminophen or a control after resistance excercise workout (10 – 14 sets). It showed that acetaminophen and ibuprofen had an impact on prostoglandins (in equal degree). Researchers concluded this impact on prostoglandins could have a big impact on muscle growth.

One year later, these same researchers published (Am J Physiol Endocrinol Metab. 2002 Mar;282(3):E551-6.) measuring protein synthesis after resistance workout. The study was done on 24 males who either took acetaminophen, ibuprofen, or control. Results showed that the placebo group had 75% higher protein synthesis at the skeletal muscle than the ibuprofen or acetaminophen group. These painkillers didn’t effect overall body breakdown, but did effect protein synthesis at the muscle.

Aspirin also has a effect on decreasing protein synthesis. (source: J Biol Chem. 2007 Apr;282(14):10164-71. Epub 2007 Feb 6.)

Most of the older studies discuss protein synthesis, but a more
recent study published in (Med Sci Sports Exerc. 2006 May;38(5):840-6.) compared overloading a rat muscle with or without ibuprofen on actual muscle growth. Results showed reduced muscle hypertrophy (muscle growth) by 50% in rats from ibuprofen with overload vs. overload only.

As you can see these were not minor changes in protein synthesis. Even occasional use will have a significant impact on muscle growth.

Bodybuilders have to eat thousands of calories a day in order to pack on a ton of muscle. Many bodybuilders find that the appetite itself, is what keeps them from being able to eat enough calories to gain weight. Hardgainers are the most vulnerable of all people in this regard. I decided to look around and try to find all the substances that have been used for stimulating appetite.

Cyproheptadine Hydrochloride (Periactin): This is a anti histamine drug that relieves allergy symptoms. It also has the ability to stimulate appetite, probably due to it’s serotonin blocking action on the receptors.

Sources:
- (Expert Opin Pharmacother. 2004 Nov;5(11):2287-92)
- (Nutr Clin Pract. 2005 Aug;20(4):400-10.)
- (Pediatr Pulmonol. 2005 Sep;40(3):251-6)

Periactin is sometimes prescribed clinically by doctors for underweight people who need appetite stimulation. This has led bodybuilders to wonder if other anti-histamines like benadryl will have the same effect on appetite. This doesn’t seem to be the case though. One major side effect of periactin, is it will make you groggy and tired like other histamines.

Glucocorticoids: These are drugs that work on the cortisol receptor such as Prednisone. These drugs are counterproductive to bodybuilding however, as they are inherently catabolic.

Megestrol acetate: A progestin that has been used clinically for people with cancer, to help stimulate appetite. This drug is also catabolic and of no help for bodybuilders.

Marionol & Marijuana: Marionol is a pill with THC derived from marijuana plant, to help stimulate appetite in cancer patients. Both can stimulate appetite in healthy people.

benzodiazepines: They appear to have a slight appetite increasing effect in some people, but the side effects and addiction properties outweigh the benefits.

Pro-hormones & Anabolic steroids: These will stimulate appetite, probably because of the nutrient partitioning effects on the body.

B vitamins: Vitamin B has been used clinically and by bodybuilders to stimulate appetite. Many bodybuilders inject vitamin B because they believe it absorbs better than orally. However, studies have shown Vitamin B orally to be just as effective as injections. (Clin Ther. 2003 Dec;25(12):3124-34).

Years ago, anti-estrogens were only available for bodybuilders by prescription. Their purpose was for during and after a cycle. Since then, with pro-hormones hitting the supplement industry, various supplement companies have put anti-estrogens on the market.

About Anti-estrogens:

Anti-estrogens are compounds taken by bodybuilders, for the purpose of controlling estrogen levels in the body. There is two major ways they can act. The first type acts as a weaker estrogen, competing with real estrogen on the receptors. It therefore acts as a damper and mimics low estrogen levels in the body, without actually lowering it. Nolvadex and clomid fall under this group. Depending on other tissues in the body, these anti-estrogens can act like a estrogen or an anti-estrogen, giving different side effects.

The other type is aromatase inhibitors. Aromatase is the enzyme that converts testosterone to estrogen. Aromatase inhibitors block the enzyme from converting to estrogen, resulting in lower body estrogen levels. Arimidex and the first legitimate anti-estrogen supplement available over the counter 6-OXO, are just a couple from this group. Because aromatase inhibitors actually kill off the enzymes and lower the estrogen levels, there is usually a rebound effect on estrogen, after stopping use.

Use of Anti-Estrogens for bodybuilders:

Anti-estrogens have been used by bodybuilders after a steroid cycle to bring back natural testosterone, called PCT (post cycle therapy). At one time, bodybuilders never used to use PCT. Contrary to common bodybuilding belief, anti-estrogens are not necessary to get natural testosterone production back in most people. However, taking anti-estrogens speed up the pace making recovery and retention of muscle better. They also help prevent Gyno, which you are susceptible to post-cycle from the low testosterone high estrogen ratio post cycle. Certain individuals may not be able to restore testosterone to pre-cycle levels, without anti-estrogens. Some are so slow to recover, that they may have to resort to longer cycles at higher doses of anti-estrogens.

Anti-estrogens have also been used by themselves as testosterone booster cycles, for the purpose of enhancing muscle gains or cutting. Taking anti-estrogens even when your testosterone levels are normal, will automatically boost your testosterone levels. Your body measures it’s estrogen levels and when it declines through use of anti-estrogens, it makes more testosterone. This has made some bodybuilders think that taking anti-estrogens by themselves, could give muscle gains or fat loss.

While anti-estrogen use looks good on paper, with the higher tesosterone and lower estrogen, it doesn’t work that way. Estrogen works in conjunction with testosterone to burn fat and gain muscle. It is a bodybuilding myth that estrogen hurts your gains and eliminating it will help. Excessive estrogen does, but not when you have healthy testosterone levels and the ratio of testosterone to estrogen is balanced. For further reading on estrogen, please read our previous articles:
-Fat loss effects of estrogen
-Anabolic effects of estrogen

While studies show anti-estrogens give significant boosts in testosterone and decline in estrogen, they have never shown success for body recompositioning purposes. Those with low testosterone who never have done steroids have also considered taking anti-estrogens. While anti-estrogens would help these people, when they come off them they will begin to drop again. The only way it would work is if they stayed on them indefinitely. However, the long term use of anti-estrogens is not healthy. Estrogen has beneficial effects on the body. Anti-estrogens should only be used when necessary, that is bringing back testosterone levels after a cycle.

Sometimes bodybuilding supplement science comes from the most unusual places. A few days ago, someone wrote me asking about Imodium (an over the counter anti-diarrhea drug) as a potential cortisol blocker. At first I thought it was a joke, but I actually started searching around and was surprised at what I found.

What is Loperamide?

Loperamide is the active ingredient in the over the counter product Imodium(and a few other brand names). Loperamide is part of the class of opioid receptor agonists. There is no potential for drug dependance or CNS overdose as it only acts on the intestines. However, it can cause dependance and even euphoria at high doses, so caution should be taken.

Why would loperamide be applicable to bodybuilding?

During my research, I discovered study after study where loperamide reduced cortisol levels. Blocking cortisol has become a new fad in the bodybuilding and supplement industry. Cortisol is a nasty hormone and excessive levels cause muscle loss, fat gain(visceral fat), overtraining, and health problems.

Here is the summary of just one study of loperamide on cortisol levels from the Journal of Clinical Endocrinology & Metabolism in 1992.

Final thoughts on loperamide:

Loperamide seems to give the impression of being a potential miracle supplement for bodybuilders. But there are some serious things that will stop it from ever catching on for widespread use. The biggest problem with imodium AD is it can cause dependance and slowing down waste removal in the colon. Slowing the flow of the colon long term, by using something like imodium, would lead to increased risk of colon cancer(a very fast spreading deadly cancer) and other diseases. Not to mention it would be a very uncomfortable experience being more susceptible to constipation.

I don’t see imodium AD(loperamide) as a useful cortisol blocker for bodybuilders, at least not for consistent long term use. If it is to be used, it should only be done in recommended dosages for very short periods of time, once in a great while. Of course, also make sure you take plenty of fiber supplements during it’s use.

Site enhancement oil (also known for short SEO) has become more common use among the hardcore group of bodybuilders. Many pro-bodybuilders are now also using it in limited quantites. How do SEOs cause muscle gain and is it dangerous?

What is site enhancement oil?

Site enhancement oil are oils used by bodybuilders to be injected into muscle parts. The goal is to emphasize certain muscles or bring up lagging parts for symmetry. Synthol (brand name) was the first product to come out and is often used as the generic name for site enhancement oils. Since then other companies have come out with site enhancement oils. SEOs will gradually leave the muscle, taking years to leave it completely.

Who uses site enhancement oils?

Some pro-bodybuilders are suspected of using SEOs, but since it is still frowned upon even in pro-bodybuilding, it is not publically admitted. Greg valentino an amateur bodybuilder, is an example of someone who overabused SEOs and now looks ridiculous.

How does site enhancement oil cause muscle gains?

There is a few theories out there. There is no actual research on the issue, so we are only left to decide which theory is the most probable. The first theory is that the oil exclusively causes the size. They then assume that once the oil is gone, that the muscle gains are lost too. This is probably not true, based on the reports of bodybuilders who have used it. There seems to be a more permanent component that causes the muscle gains.

The other theory is that it causes muscle growth due to scar tissue. I found this on wikipedia, which isn’t a reliable source anyways(since its all volunteer by many average people’s input). While scar tissue may be a side effect, I highly doubt it contributes to most of the muscle gains.

The most reasonable theory out there is, SEOs cause muscle growth due to muscle fascia tissue stretching. The injected oil causes the muscle fascia tissue to stretch significantly, that we know from basic anatomy. The question is, does this stretching of the muscle fascia actually facilitate muscle growth? You can read more about muscle fascia stretching and how to stimulate it in workouts in a previous article of mine: Muscle Fascia Stretching

Side effects of using Site enhancement oils:

Using SEOs is very dangerous. If it accidentally gets into a major blood vessel it can cause many serious problems, including stroke. The long term leakage into the body is also a concern of health. While not as effective, it would be safer to naturally stimulate the muscle fascia in your workouts. To see what happens to someone who grossly abuses SEO, see a previous article of ours on Greg Valentino.

This is a very common question among bodybuilders thinking of doing steroids. It also is a concern for middle aged men thinking of trying testosterone supplementation (Hormone replacement therapy). You may have read about some links between prostate cancer and steroids/HRT therapy. Is it really fact or is it just based on far reaching assumptions?

Steroids and prostate growth (BPH)

Before we discuss steroids and it’s role on prostate cancer, first we must discuss steroids’ possible actions on prostate growth (BPH). The prostate first grows during puberty. Then around 25, the prostate starts to grow again in a 2nd phase. The 2nd phase eventually may lead to prostate enlargement years down the road. Half the men in their 60’s will have significant prostate enlargement.

Steroids(including normal testosterone in the body) stimulate the androgen receptors in the prostate. Excessive levels of androgenic steroids (such as through steroid use) causes prostate growth/enlargement called BPH (Benign prostate hyperplasia) in a short period of time. Once excessive system levels of androgenic steroids drops, than the prostate will start to shrink back again. It may not shrink completely back to it’s former size however.

In non-steroid users, testosterone mainly causes it once it converts to DHT. DHT is much more androgenic(binds to the receptors stronger) than testosterone. The drug finasteride is prescribed to help alleviate prostate growth. It works by blocking the conversion of testosterone to DHT. Steroid users will often use finasteride, in order to block the effects of hair loss and prostate growth while on cycle.

BPH caused by Testosterone or Estrogen?

In non-steroid users, older men are afflicted with BPH. This seems backwards, since BPH is supposed to be correlated with high androgens right? We know that older men have lower testosterone(and DHT) levels, so how is this possible?

Well there is 3 basic theories on what causes BPH for non-steroid users. No one yet seems to know for certain which theory is correct.

Theory 1 - Excessive estrogen levels. Older men have a higher estrogen and lower testosterone levels. According to research, the use of anti-estrogens are well documented to help shrink the prostate. The famous steroid research chemist Patrick Arnold, has claimed that there is more evidence pointing to a high estrogen to low testosterone being the cause of BPH.

Theory 2 - Despite the lowering testosterone levels( and hence DHT) levels in older men, research suggests men still probably accumulate high levels of DHT in the prostate. This would explain why people why older men can still get BPH despite declining levels of testosterone and DHT in the body. Another fact to help support this theory, is that Men who don’t produce DHT naturally due to genetic defect, also don’t develop BPH.

Theory 3 – Genetic Programmed growth. The fact that prostate cells awaken again in the mid 20’s to re-grow suggests that maybe BPH growth is programmed genetically. By the time men are in their 90’s, 90% will suffer from BPH.

Other interesting study results: In one study, when estrogen and dht were both reduced with hormonal blockers, the prostate gland actually increased in size. This is startling since if one of these hormones is to play a role in BPH, why when reducing both, did it cause prostate growth?

What causes prostate cancer?

First we must realize BPH and prostate cancer are not the same thing. BPH is a condition of excessive growth of the prostate. They do not know currently, if BPH is a pre-cursor condition to prostate cancer. Prostate cancer is actually a very common occurence in men, much more than the public is aware. It is said that most men would die of prostate cancer, if they didn’t die of something before that. Prostate cancer is usually very slow growing. Many elderly men live decades with prostate cancer and may not even know they have it.

The truth is, no one really knows what leads exactly to prostate cancer. There is a lot of conflicting data. In fact, if you look at many studies out there, most don’t even show a link between prostate cancer and higher testosterone levels. Yet, many doctors seem to believe it does. Some recent studies have shown that there was no increased risk of prostate cancer based on testosterone levels. Many doctors who put middle aged men on testosterone replacement therapy, have not seen a higher incidence of prostate cancer developing. Doctors are also usually worried about BPH from testosterone, but men have actually had a reduction in their BPH from using testosterone hormone replacement therapy to treat low testosterone.

The fear of prostate cancer by doctors, is one reason why doctors are often hesitant to do HRT(hormone replacement therapy). HRT therapy is for older men and others deficient in testosterone, to bring them up to healthy levels. The January 2004 New England Journal of Medicine (NEJM) wrote that testosterone does not cause prostate cancer, but they need to be monitored, since it may stimulate hidden prostate cancer. What do they mean by hidden prostate cancers? Apparently in about half the men over age 50, they may have prostate cancer, but it is asymptomatic. In other words, it is not growing and causing harm. If they were to supplement with testosterone, according to them, it may possibly stimulate these harbored cancer cells into a aggressive form of prostate cancer. That is why doctors will check for PSA(prostae specific antigen), BPH, and have more frequent prostate exams when starting HRT therapy. PSA is a very accurate marker of existing cancer and when it goes back to zero it means the person has been cured. Testosterone therapy could “awaken” these sleeper cancer cells. This is what they theorize, yet there is no scientific research to show that this is really what happens.

What we do know, is that there is many factors that might increase the risk of prostate cancer.

1) Increased ejaculation in your 20’s. This may sound awkward, but there were some studies that recently came out with this result. They found that those who ejaculated a lot more frequently in their 20’s, had less likely occurence of prostate cancer. The prostate gland is known to hold a much higher concentration of the bodies’ toxins. The researchers believed that ejaculation may lead to “cleansing” the prostate from carcinogens (cancer causing toxins).

2) Genetics & Heredity – Prostate cancer also seems to run at a higher rate in families with a pre-disposition to it. There is currently research looking at various enzymes and prostate genes, that may be involved in developing the cancer. African americans also have a higher incidence of prostate cancer.

3) Diet/Environment – Diets high in animal fat increase incidence of prostate cancer. Men who moved from Japan where prostate cancer incidence is lower, had increased risk in their sons and grandsons when living in the U.S. Therefore, diet and other environmental factors seem to increase risk of prostate cancer.

Summary

Prostate cancer is caused by a variety of risk factors. Experts seem to continue to try and make this link between high testosterone levels (or other steroids) and prostate cancer, yet there is no real solid research proof that testosterone levels is the direct cause. There is a growing body of research showing there is no link and that it may be caused by other factors. If Testosterone and steroids caused prostate cancer, a lot of men at a young age would probably be getting prostate cancer.

Bodybuilders today are now starting to inject growth hormone at an increased rate. The media also is reporting sports athletes using it as a way to get beyond steroid tests. Most bodybuilders know that growth hormone, isn’t so much of a mass builder as it is for burning fat. But they do believe it has some performance and muscle gaining benefit or else they wouldn’t be spending thousands of dollars for it. But Does growth hormone really help gain muscle and strength for bodybuilders? And is it really the holy grail for middle aged people looking for the fountain of youth?

Growth Hormone increase skeletal muscle or organ weight?

The most recent study was done in March of 2008, where they analyzed 27 studies previous studies together. When they analyzed them, there was a increase in lean muscle mass, but usually no increase in strength in the legs and arms. There was even an increase in fatigue. This is contradiction to the commony belief that HGH not only builds lean muscle, but it increases performance.

In many past studies where growth hormone shows a positive benefit on lean muscle in older individuals, what the researchers don’t tell you is that lean muscle can be anything other than fat, such as bones, water, and organs. Everyone is aware that growth hormone causes organ growth (GH gut for example). Is it possible that this growth is purely organ growth and not actual muscle growth? I think the research points to that idea.

Two studies published by fitforlife not only showed no performance benefit, but no gains in muscle. Two seperate studies done on HIV patients(note: not AIDS) took 9 and 12mgs of growth hormone per day for 12 weeks. They had no gain in skeletal muscle. If it can’t help HIV individuals, who could growth hormone help?

Another study was done on a younger group of healthy experienced athletes only aged 22-23. They took 2.87 mgs of Growth hormone a day. They actually did gain about a 4% in lean muscle weight. So is this proof it works? Of course not, 4% could easily be explained as organ growth, especially considering all the studies showing there is no positive effect on performance or muscle increase.

Does Growth Hormone work for anti-aging?

There is no scientific evidence that growth hormone injections cause a longer life. In fact there are studies that show that people with higher levels of HGH in the body tend to live shorter lives.

Growth hormone may increase the quality of your life however, in making you look and feel younger. Growth hormone replacement therapy doesn’t seem to have a beneficial effect on increasing actual skeletal muscle or strength either in older individuals. There have been many studies, where there was no noticeable strength increase in older individuals supplementing with GH.

Does growth hormone help lose fat?

There seems to be more evidence that growth hormone promotes fat loss than there is for it increasing muscle or athletic performance. Research results vary and some studies find no fat burning effects. The fat loss results are often within the scope of statistical significance and may even be explained(my theory), as a result of organ growth increasing the metabolism of the body. No scientific authority has yet to say as a result of all the studies done over the years, whether growth hormone in fact does definitely help lose significant amounts of fat.

Growth hormone injections a waste of money?

I cannot say definitely that HGH doesn’t work because most of the studies use smaller doses than many bodybuilders would use. However, there is no real evidence that HGH helps increase real muscle or strength at this time. Some bodybuilders believe that supplementing testosterone with growth hormone, will have a synergistic effect that increases growth hormones anabolic and performance benefit. However, there is no research at this time studies this combination. I’m sure it is something that will be researched soon, since HGH is now getting under more scrutiny in congress.

In older individuals looking for the fountain of youth, growth hormone may have positive effects on your appearance and mood. Users of growth hormone often appear younger also, due to it’s effect on tissue growth. However, there may be long term health effects to growth hormone replacement therapy, so I don’t recommend it for that purpose.

You may want to read a older article I wrote on the Effects of HGH on the Body

Bodybuilders have been using spironolactone as a topical to help prevent hair loss for a few years now. I decided to do some more research to find out more about spironolactone.

What is Spironolactone?

Spironolactone (also known as Aldactone) is in fact a steroid. So how can a steroid actually help prevent hair loss? Well it is a steroid in the sense of being a testosterone derivative, but is not a anabolic androgenic steroid like testosterone.

How does Spironolactone work?

Spiro’s main use orally for bodybuilders has been for it’s diuretic effects during contest time. It has an effect on of aldosterone, which is the body hormone that regulates sodium retention(and hence water retention). Spiro doesn’t seem to work in the same mechanisms as for example propecia. Propecia works by blocking the conversion of testosterone to DHT which is the main contributor to hair loss. There is research that points to the idea that spiro competes with DHT in the hair follicle androgen receptor. In other words, it replaces a stronger androgen(DHT), with Spironolactone.

Spironolactone topicals:

As an anti-androgen it obviously would cause serious problems for bodybuilders to take it orally. Some have developed topicals to use spiro so it goes to where it is only needed, on the top of your head. There will be some leakage into the body, but most of it will stay in the scalp only.

Most people know that testosterone is responsible for muscle gains and for sexual health. Testosterone is also a potent fat burner (anti-lipolytic). This is the reason why women and men with low testosterone levels have an easy time gaining fat.

How does testosterone reduce fat gain?

Testosterone, like all androgens, leads to higher density of adrenoreceptors in the fat cells causing fat loss. Testosterone like all steroids, also helps block the cortiscosteroid receptors for the hormone cortisol. Cortisol is a hormone which promotes muscle wasting. Testosterone has many other complex actions on the body on the cellular level. It also works synergistically with other hormones in the body, such as growth hormone, to help promote fat loss. Testosterone also converts to estrogen and DHT, both of which also have anti-lipolytic properties to them.

Testosterone causes fat loss or just prevent fat gain?

We have used the term “fat loss” liberally. Testosterone doesn’t inherently cause fat burning, nor does any steroid for that matter. What really happens is it helps protect against fat synthesis( fat gain). Either way of looking at it, they both give the same ultimate result in the end, which is loss of fat.

In a previous post I wrote about the anabolic effects of estrogen. You can read that post here Not only does estrogen have muscle gaining abilities, but it also can help in reducing fat. This may sound far reaching since estrogen is known for causing a bloated puffy look. One must remember that is because of increased water retention due to it increasing aldosterone, a hormone that controls sodium retention.

Estrogens according to research could help fat loss in a few major ways. Estrogens have the ability to not only reduce insulin receptor count, but also increase their insulin sensitivity at high doses. Insulin sensitivy and response is an important way to reducing fat. Estrogen also raises growth hormone levels. Growth hormone is a very potent fat burning hormone. Estrogen also can help reduce hunger during dieting due to it’s role on melanin-concentrating hormone (MCH). During dieting MCH levels increase, causing increased appetite. Estrogens will block this increase in MCH.

One must keep in mind that too high of estrogen, will have the opposite effect for fat loss and muscle gain. A healthy balance of estrogen and testosterone is key to maximum muscle gains and fat loss. This is one reason why people with higher bodyfat percent usually gain more of their weight as fat. The fat cells will convert testosterone to estrogen in the body.