Facts do not cease to exist because they are ignored.

–Aldous Huxley, Novelist

nergy is the stuff which makes life possible. Every blink of our eye, every beat of our heart, and even every thought that we think are all driven fundamentally by the production of energy within the cells of our various tissues. As we age however, our cells gradually lose the ability to sustain the high energy production of youth. Outwardly, we notice that our muscles weaken, our intellectual faculties dull, and our memories falter. But, whether we realize it or not, the common biological thread running through all manifestations of aging is the cumulative impairment of cellular energy production.

Many scientists have begun to look at aging and disease fundamentally as disorders of bioenergetics, a term coined to describe energy production in living systems. As their research continues, it has become reasonable to assume that substances which improve the efficiency of energy production on a cellular level are likely to be particularly supportive of long–term health.

And fortunately, many such substances are already available to us in the form of nutritional supplements – such as creatine, for example.

Creatine (ideally supplemented in the form of creatine monohydrate) is an energy–related substance which has been used by athletes for decades to improve strength and athletic performance. But, because efficient energy production is essential to all aspects of health (and not just athletics), the far–reaching health benefits of creatine supplementation have begun to be explored as well.

And judging by the research currently available, creatine may turn out to be, not only one of the most powerful ergogenic (performance–enhancing) substances we have available to us, but also one of the most powerfully health–promoting substances as well.

Yet ironically, in the hype–riddled pages of bodybuilding and fitness magazines, creatine monohydrate is often attacked.

Creatine monohydrate – the very substance which is almost single–handedly responsible for any shred of scientific legitimacy enjoyed by the sports supplement industry; the substance with an unrivaled track record of safety and effectiveness as indicated by hundreds of controlled research studies is currently being maligned as obsolete, inefficient, and even toxic by the very same sports nutrition industry which has benefited the most from it.

The reason for this seemingly odd turn of events is simply because there’s sometimes more money to be made through lies, deception, and rampant speculation, than through adherence to the existing scientific literature. Some unscrupulous supplement sellers have taken to touting supposedly “improved” versions of creatine (products which are, of course, sold at inflated prices, and inflated profits) ranging from liquid creatine, to buffered creatine, to creatine esters, and chelates.

And, more often than not, those selling such products are not above spreading lies about creatine monohydrate to garner a share of the sizable creatine market. In advertisements, we’re told that creatine monohydrate causes “bloating,” which liquid creatine or creatine esters can prevent. We’re told that creatine monohydrate degrades into the “toxin” creatinine mere seconds after being mixed with liquid, and that buffered creatines were specifically created to prevent this.

Of course, lies of this sort have a frightening tendency to be taken as fact, not only by ill–informed and impressionable consumers, but also by the “don’t–confuse–us with–the facts” media – and by governmental agencies whose job it is to regulate your access to nutritional substances.

So the next time you see one of those ads bashing creatine monohydrate, realize that the consequences of such misinformation may be much greater than you anticipate. If we value our access to nutritional supplements, we all have a vested interest in seeing to it that supplement companies are held accountable for such deceptive practices.

As such, blatant and unfounded lies regarding creatine side–effects and “toxicity” must be combated head–on, deferring to the large body of existing scientific evidence showing the safety, stability, and effectiveness of creatine monohydrate.

And, in fact, a look at the scientific literature reveals that, unlike creatine monohydrate, many of the supposedly “improved” versions of creatine have little to no research supporting their effectiveness, or, for that matter, even their safety. Apparently, many product developers within the supplement industry don’t feel even the slightest bit of guilt in aggressively marketing completely untested compounds – in essence using your body as a chemistry set, and charging you for the privilege.

So, in this installment of the Integrated Supplements Newsletter we’ll begin to set the record straight. We’ll look to the existing research to answer some of the most common questions we receive about creatine. In the end we’ll see that that the long–term benefits of creatine supplementation may be far greater than you’ve ever imagined, and that no type of creatine can top pure creatine monohydrate for safety and effectiveness.

(Note: unless otherwise mentioned, when we refer to creatine in supplement form, we are referring to pure creatine monohydrate.)

Q. What is Creatine?

A. Creatine is an energy–related nutrient formed in the body from the amino acids arginine, methionine, and glycine. Creatine is directly involved in a process which allows our bodies to rapidly regenerate the energy molecule known as adenosine triphosphate, or ATP. Under periods of high energy demand or physical exertion, the amount of work (both physical and mental) we are able to perform is often limited by our bodies’ ability to rapidly regenerate ATP.

As creatine plays such an important role in energy production, creatine supplements have been widely embraced by athletes (especially athletes whose sports require quick bursts of energy and muscular strength, like weightlifters, bodybuilders, sprinters, or football players). But it’s very important to realize that creatine supplementation is likely to benefit all types of individuals, including those not usually associated with creatine usage. As the research on creatine continues to accumulate, we’re seeing that diverse groups, including females, the elderly, and those simply looking to prevent the ravages of aging, can all benefit greatly from optimizing their creatine intake through supplementation.

To state fact simply, the stigma of creatine as a mere “bodybuilding” supplement must end if the larger population of health–conscious individuals are to reap the full benefits of this remarkable substance.

Along these lines, because creatine has often been deemed guilty by association with other performance–enhancing substances, it’s important to state not only what creatine is, but what it isn’t. Despite the impression which can be garnered from the mainstream media coverage of creatine, creatine is not a steroid hormone, creatine is not a hormone–percursor, and creatine use is not banned by any major athletic association or government agency in the United States.

Our body, in fact, produces creatine, and creatine is also found in our diet, in foods such as meat or fish. Our goal with supplementing creatine (as is our goal with supplementing other nutrients) is simply to maximize our intake without having to consume massive amounts of food.

Q. How does creatine work?

A. In order to grasp how creatine works, it’s helpful to think of creatine as a sort of “emergency” energy substrate – an energy substrate which the body can call upon to produce energy very quickly without having to start up the entire “assembly line” involved in producing energy from carbohydrates or fats.

Metabolically speaking, this emergency energy makes creatine a very valuable substance, but unlike carbohydrates or fats (of which we have, essentially, an inexhaustible amount), our reserves of creatine are often in relatively short supply. This is why the most demanding sort of muscular activity, like lifting heavy weights, can only be sustained for short periods of time.

Looking at the matter from an evolutionary perspective it’s not surprising that the most “valued” tissues of the body, like the brain, skeletal muscles, and heart, have a notably high ability to produce energy quickly (in the form of ATP) from a process involving creatine.

And, knowing this, it makes sense that creatine supplementation has shown promise in disorders involving the brain, heart, and musculature. Again, it’s become clear in recent years that creatine is far more than simply a muscle–builder. More than likely, it’s a substance which can benefit our overall health on a very fundamental level.

In a technical sense, creatine, which is stored in the body as creatine phosphate, [also known as phosphocreatine (CrP)] is able to donate phosphate, and rapidly recycle the energy molecule, ATP.

On a cellular level, energy is produced when ATP splits and releases one of its phosphate groups (becoming ADP, or adenosine diphosphate in the process). Phosphocreatine is able to rapidly regenerate ATP from ADP, much like the recharging of a battery. In muscles, the rapidity of this energy regeneration is responsible for maximal power output, and this helps to explain why creatine has become so popular with strength and power athletes.

Q. What can an athlete or workout–enthusiast expect to notice from taking creatine supplements?

A. Athletes almost universally notice an increase in their explosive strength and muscular endurance from taking creatine. This means that a sprinter could notice increased speed and better performance, or a weightlifter could lift heavier weights, or that a bodybuilder could increase strength, and train at a higher level throughout a workout.

Football and hockey players may notice more explosive starts and less fatigue, while baseball players may notice that they get a better jump on the ball in the field, and a more powerful swing at the plate.

Taken long–term, creatine may also help to create a better cellular environment for enhanced muscular growth and recovery, which is always an added bonus in strength and power sports.

The jury’s still out on the benefits of creatine use for endurance athletes like marathoners, and tri–athletes, however. The type of explosive energy to which creatine contributes is thought to be of lesser value in these sports. Where creatine can improve the anaerobic production of energy, endurance athletics are commonly thought to engage the aerobic sub–segment of energy production which doesn’t utilize the creatine phosphate system all that much.

Of course, the aerobic/anaerobic distinction is somewhat over–simplified – it’s not really a black–or–white phenomenon. No activity engages solely one type of energy production at the expense of others, and as such, creatine has been found to offer some unique benefits to endurance athletes.

Creatine may potentially be able to spare muscle glycogen, the carbohydrate fuel source of working muscles, thus making more glycogen available in the latter stages of training.

Researchers have also noted that short bursts of explosive energy (the kind creatine does help with) are of increasing importance in competitive endurance sports. An athlete who has the ability to intersperse short bursts of explosive speed into his or her race has a distinct edge on the competition, and this is another area where creatine delivers for endurance athletes:

Study Link – Creatine supplementation in endurance sports.

Quote from the above study:

We conclude that creatine supplementation at doses of 6 g daily has positive effects on short–term exercise included into aerobic endurance exercise.

Creatine could also indirectly benefit endurance athletes because of its remarkable effects on reducing exercise–induced inflammatory damage, and improving muscular recovery.

Researchers have found that creatine supplementation (5 grams taken 4 times per day) for 5 days prior to a 30 kilometer run significantly reduced several markers of tissue damage and inflammation in experienced distance runners:

Study Link – The effect of creatine supplementation upon inflammatory and muscle soreness markers after a 30km race.

Quote from the above study:

Pre–race blood samples were collected immediately before running the 30km, and 24h after the end of the test (the post–race samples). After the test, athletes from the control group presented an increase in plasma CK (4.4–fold), LDH (43%), PGE2 6.6–fold) and TNF– α ( 2.34–fold) concentrations, indicating a high level of cell injury and inflammation. Creatine supplementation attenuated the changes observed for CK (by 19%), PGE2 and TNF– α ( by 60.9% and 33.7%, respectively, p<0.05) and abolished the increase in LDH plasma concentration observed after running 30km.

The runners in the above study reported no side–effects from creatine use (even at what could be considered a relatively substantial dose), and their race completion times were unaffected.

Because it’s so important for athletes to find safe ways to keep inflammation and tissue damage to a minimum, creatine use certainly deserves some serious consideration by all types of athletes and fitness enthusiasts. Even if it doesn’t immediately improve performance, moderate doses of creatine have the potential to significantly shorten recovery time after races and between workouts which, in the long–run is certain to be of significant benefit.

Q. Can creatine supplementation benefit non–athletes and sedentary individuals?

A. It seems likely that it can – and by several different mechanisms, at that. The anti–inflammatory effect exhibited in the above study is a clue that creatine may have beneficial effects in reducing oxidative stress (which we’ve written about in previous newsletters). We also saw in our nitric oxide newsletters, how creatine may be able to reduce levels of the suspected cardiovascular toxin, known as homocysteine. In fact, knowing how creatine works, and how important proper energy production is to the health of the bodies most valued tissues, creatine is likely to be one of the most effective anti–aging supplements we have at our disposal.

As a potential anti–aging compound, creatine supplementation has begun to be studied in aging adults. While the research isn’t conclusive at this point, even creatine’s “mere” ability to increase muscular strength and recovery appears to be of unique benefit to older individuals.

For young people, building muscle mass is often viewed merely as a means to improve athletic performance, or, to improve the aesthetic appeal of ones physique. But the gradual loss of muscle mass and function which often accompanies old age is, in fact, a life–threatening medical problem.

As such, researchers wondered if creatine’s benefits, which are now very well–documented in younger athletes, would translate to improving muscle mass and strength in older individuals as well.

Increasingly, research is beginning to show that it may. Studies conducted with both eldery men and elderly women have found strength, and the ability to perform functional living tasks to improve with creatine supplementation.

Study Link – Creatine supplementation improves muscular performance in older men.

Quote from the above study:

These data indicate that 7 d of creatine supplementation is effective at increasing several indices of muscle performance, including functional tests in older men without adverse side effects. Creatine supplementation may be a useful therapeutic strategy for older adults to attenuate loss in muscle strength and performance of functional living tasks.

Study Link – Creatine supplementation improves muscular performance in older women.

Quote from the above study:

Short–term creatine supplementation resulted in an increase in strength, power, and lower–body motor functional performance in older women without any adverse side effects.

So, even though creatine is commonly thought of as a supplement to improve power for athletic performance, the fact that creatine improves energy production at a very fundamental level makes it apt to benefit people at every stage of life. Of course, in the elderly, an increase in muscular strength and power output may manifest in something as simple as being able to get out of a chair without assistance, or being able to climb a flight of stairs; but maintaining or regaining the ability to perform such simple tasks can have truly life–altering implications. If creatine delivers in this regard, as research indicates it may, the days of creatine’s stigma as a mere bodybuilding supplement should be numbered.

Q. If creatine improves energy production at a fundamental level, can creatine offer benefits outside of the muscular system?

A. Yes. Where creatine is a nutrient utilized by various tissues, it’s no surprise that the benefits noticed from creatine aren’t just limited to our muscles. For example, in recent years, creatine’s role in improving mental function has begun to be explored as well.

One of the most compelling studies in this regard was conducted by researchers from the University of Tokyo, and was published in the journal, Neuroscience Research, in 2002.

The researchers found that creatine supplementation (8 grams per day for 5 days) significantly reduced the mental fatigue associated with performing repeated mathematical calculations.

Participants in the study were asked to perform a test of mental functioning known as the Uchida–Kraepelin test; in which subjects are asked to calculate the addition of random numbers over a 15–minute period, take a five minute rest, then perform the test for another 15 minutes.

In the Uchida–Kraeplin test, it’s commonly found that after the 5–minute rest period, test scores initially increase slightly relative to the end of the first 15–minute period, only to rapidly decline soon thereafter as a result of mental fatigue.

The researchers who conducted the following study, however, found that creatine consumption was able to increase test scores relative to the placebo group in both the first and second 15–minute intervals of the test. Creatine appeared to be particularly effective in preventing the drop–off in test performance during the second interval, and thus appears to significantly delay mental fatigue.

The researchers also noted a reduction of oxygenated hemoglobin in the brains of the subjects taking creatine which could imply improved oxygenation of the brain, or possibly a reduced requirement for oxygen in the presence of creatine:

Study Link – Effects of creatine on mental fatigue and cerebral hemoglobin oxygenation.

Quote from the above study:

Using double–blind placebo–controlled paradigm, we demonstrated that dietary supplement of creatine (8 g/day for 5 days) reduces mental fatigue when subjects repeatedly perform a simple mathematical calculation. After taking the creatine supplement, task–evoked increase of cerebral oxygenated hemoglobin in the brains of subjects measured by near infrared spectroscopy was significantly reduced, which is compatible with increased oxygen utilization in the brain.

Another notable study on creatine and brain function found an improvement in working memory and intelligence in vegetarians taking 5 grams of creatine daily for six weeks (vegetarians consume less creatine than meat–eaters, therefore, the effects of creatine supplementation are often more pronounced in vegetarians).

Study Link – Oral creatine monohydrate supplementation improves brain performance: a double–blind, placebo–controlled, cross–over trial.

Quote from the above study:

Creatine supplementation had a significant positive effect (p < 0.0001) on both working memory (backward digit span) and intelligence (Raven's Advanced Progressive Matrices), both tasks that require speed of processing. These findings underline a dynamic and significant role of brain energy capacity in influencing brain performance.

Recent research has also found that creatine may be able to slow the neurological decline associated with aging. And because overall aging and neurodegeneration are so closely related, it has been proposed that creatine supplementation may even extend healthy lifespan.

In a very recent study conducted with mice, researchers from the University of Munich found that creatine supplementation led to a 9% increase in average healthy lifespan, and significantly improved performance on neurobehavioral tests. In the study, creatine was found to reduce markers of oxidative stress and interestingly, creatine significantly reuduced the formation of the age pigment, lipofucsin (lipofuscin can be noticed on the skin in the form of unsightly “age spots” or “liver spots,” but its presence in all tissues, including the brain, is a clear marker of the degeneration of aging).

It’s really amazing to think that a simple, safe, and economical supplement like creatine, in addition to its effects on muscular function, may also be able to improve mental function, intelligence, and neurological health as well. But as we at Integrated Supplements have been saying for some time, when we improve the ability of the cells to produce energy efficiently, the result is a remarkable improvement in every conceivable bodily function and aspect of health. The far–reaching benefits of creatine are yet another testament to the validity of this approach, and we’ll have more to say about the anti–aging effects of creatine in upcoming Integrated Supplements Newsletters.

Q. Creatine detractors say that creatine simply causes the cells of the body to hold more water, and that it’s this effect which is responsible for creatine’s effect on muscles. Some people are concerned that any effects they notice from taking creatine will be short–lived, and will disappear soon after creatine use is discontinued. Is there any validity to this line of thinking?

A. Not really. As we’ve seen, creatine is primarily an energy molecule, and creatine primarily works by allowing the cells (of various tissues) to produce energy more efficiently. For athletes undergoing weight training this means increases in muscle strength, and ultimately, muscle size.

It is true that creatine can add to the water–volume inside muscle cells – and this phenomenon may have much to do with the initial weight gain some people notice when taking creatine. But to say that creatine “just” causes the cells to hold more water, or to imply that creatine’s benefits are short–lived or superficial is downright ridiculous.

But unfortunately, this is precisely the type of misinformation that is often heard from the ill–informed, self–proclaimed experts who take it upon themselves to (knowingly or not) disseminate falsehoods and lies about creatine.

The fact is that no single nutritional substance has been shown, in more peer–reveiwed, double–blind studies, to be more effective than creatine for increasing muscle power, strength and recovery. And some studies have shown, despite the pervasive myth to the contrary, that lean tissue mass and strength are maintained in exercising individuals, months after creatine supplementation is ceased:

Study Link – Effect of ceasing creatine supplementation while maintaining resistance training in older men.

Quote from the above study:

Strength (1–repetition maximum [1–RM]), endurance (maximum number of repetitions over 3 sets at 70–80% 1–RM), and [lean tissue mass] (dual–energy X–ray absorptiometry) were assessed before and after 12 weeks of [creatine] cessation combined with reduced–volume training. No changes in strength or [lean tissue mass] occurred.

Anyone who even implies that creatine “just causes the cells to hold more water” simply looks foolish in the eyes of those who have studied the existing research.

It’s possible, too, that, far from being an unwanted side–effect, creatine’s effect on cellular hydration may be one of the factors responsible for the growth–promoting actions of creatine. It’s important to remember that a hydrated cell is integral for the process of growth, repair, and recovery to take place optimally.

It’s important to note as well that the real benefits of creatine occur in the long–term, not the short–term. As creatine allows a person to consistently train with greater power and intensity, creatine can be a major factor in fostering long–term gains in muscle size and function. The long–term gain in muscle mass experienced while taking creatine will manifest as actual muscle tissue – not simply water–weight.

As evidence, several lines of research indicate that creatine monohydrate supplementation is able to trigger the activation of satellite cells (satellite cell activation is considered to be a primary event in the growth and regeneration of muscle tissue):

Study Link – Dietary creatine monohydrate supplementation increases satellite cell mitotic activity during compensatory hypertrophy.

Quote from the above study:

[C]reatine supplementation in combination with an increased functional load results in increased satellite cell mitotic activity.

Study Link – The Effects of Ergogenic Compounds on Myogenic Satellite Cells.

Quote from the above study:

Creatine in the monohydrate form induced differentiation of myogenic satellite cells...These results provide initial evidence for a mechanistic understanding of observed effects in vivo of increased muscular size and strength from creatine supplementation.

In a practical sense, if a person finds that the athletic gains they noticed from taking creatine disappear soon after creatine supplementation is stopped, it’s usually an implicit admission that either they didn’t take it for long enough to notice the longer–term gains, or their training and/or diet are insufficient to support meaningful gains in the first place. Rather than blaming creatine, such people would be well–served to shore up their diet and training regimens in order to then reap the full athletic and muscle–building benefits of creatine.

Q. It has been said that some new types of creatine don’t cause bloating. Is this true?

A. We’ll have more to say about these supposedly “new” types of creatine in the next installment of the Integrated Supplements Newsletter, but briefly, many of these “new” types of creatine (creatine ethyl ester, buffered creatines, liquid creatines, and several others) are being marketed as if they somehow lack the cell volumizing ability of creatine monohydrate (of course, in marketing lingo, we’re told that these creatines don’t cause “bloating” – a term with clearly negative connotations which is probably used purposefully to mislead the consumer).

There are several factors to consider:

First off, even assuming these new creatines are viable forms of creatine at all (which is not the case for many of them, as we shall see), on a cellular level, there’s no reason to believe that some types of creatine would work differently than others. Again, no matter what molecule creatine is attached to when you consume it, creatine will be stored in the cells as phosphocreatine (as the body attaches a phosphate to creatine intracellularly). There’s simply no reason to believe that some types of creatine will “magically” work differently once creatine is taken up by the cell.

Empirically though, some people do report less bloating when taking types of creatine other than creatine monohydrate. But this doesn’t mean that these products are, in any way, better than creatine monohydrate.

The reason is that these product often contain very little creatine – thus, logically, the user won’t experience the cellular hydration associated with creatine. Of course, such products often contain various stimulants such as caffeine, so a performance enhancing effect is often noticeable, but these effects are not due to creatine. A few years back, a certain popular brand of liquid creatine, which claimed to offer benefits above and beyond creatine monohydrate, was independently tested, and was found to contain almost no creatine whatsoever.

Study Link – The creatine content of Creatine Serum and the change in the plasma concentration with ingestion of a single dose.

Quote from the above study:

Analysis showed 5 ml of Creatine Serum to contain <10 mg [creatine monohydrate] and approximately 90 mg creatinine. Phosphorylcreatine was not detectable and only a trace amount of phosphorous was present. Total nitrogen analysis ruled out significant amounts of other. forms of creatine. We conclude that the trace amounts of creatine in the product would be too little to affect the muscle content even with multiple dosing.

Other types of creatine (such as esters and chelates) may offer some slight benefits, but often, the stability and efficacy of these products is questionable as well. It’s highly unlikely that these products offer any benefits over creatine monohydrate, but people may notice less water retention simply because they are consuming significantly lower doses of creatine when they take esters and chelates (the recommended dose of these products contains far less actual creatine than the recommended dose of many creatine monohydrate products).

When we compare apples to apples, the same reduction in water–weight gain could be achieved using similarly low doses of creatine monohydrate (which may be all that is necessary to reap creatine’s benefits as an athletic or anti–aging substance in the first place). So, low doses of creatine from any source are unlikely to cause noticeable water–weight gain. It’s usually only relatively high doses of creatine which have a visibly noticeable effect on cellular hydration.

But, it shouldn’t be forgotten that creatine monohydrate is the only type of creatine which has been shown in countless studies to be stable, safe, and effective. In fact, preliminary research on some of the newfangled types of creatine currently being marketed indicates that they are likely to be quite unstable under physiologic conditions. If such products don’t cause cellular hydration in the same way as creatine monohydrate, this is likely to be because these compounds degrade into useless creatine metabolites upon ingestion. As such, these products offer not a benefit, but an added risk when compared to creatine monohydrate.

Along the same lines, when the word “bloating” is used, the term may be referring to the stomach upset some people notice when taking large doses of creatine monohydrate. But, this effect too is simply a function of dose and not of creatine monohydrate per se. Stomach upset, if it occurs when taking creatine monohydrate, can be easily rectified by lowering the dose taken.

Q. Speaking of creatine dosage, is taking a loading dose of creatine necessary?

A. Probably not. Many studies using creatine monohydrate have employed a loading dose of creatine (where creatine is initially taken in high doses to saturate the muscle cells) of approximately 20 grams per day for 5 days. The loading dose is often followed by a maintenance dose of 3 to 5 grams per day thereafter.

But, although there is evidence to suggest that a loading dose is beneficial for quickly saturating muscles with creatine, other studies suggest that smaller doses of creatine, taken consistently, are able to saturate the muscle cells with creatine equally (though, logically, reaching muscle saturation will take longer).

One of the most often–cited studies in this regard, showed that muscle creatine concentrations were increased by 20% when 20 grams of creatine was taken over a six–day period – yet a similar increase was found when 3 grams of creatine was taken over a 28–day period.

Study Link – Muscle creatine loading in men.

Quote from the above study:

Muscle total creatine concentration increased by approximately 20% after 6 days of creatine supplementation at a rate of 20 g/day… A similar, but more gradual, 20% increase in muscle total creatine concentration was observed over a period of 28 days when supplementation was undertaken at a rate of 3 g/day… The ingestion of 3 g creatine/day is in the long term likely to be as effective at raising tissue levels as this higher dose.

So, it seems that creatine loading is not entirely necessary to reap benefits from creatine supplementation.

But the question then arises: are there performance benefits to be gained from loading creatine which wouldn’t be gained by taking maintenance doses on a regular basis? Some researchers suspect there may be. It’s possible that a dramatic rise in muscle creatine stores may, in and of itself, trigger growth–promoting mechanisms in the muscle cell. If this is true, we may want to devise strategies to load creatine as safely and efficiently as possible.

As nearly every creatine user can attest, creatine isn’t the most soluble of compounds when mixed in water. The advent of micronized creatine (creatine with a very small particle size) several years ago helped creatine suspend in water more efficiently (which serves to reduce creatine’s gritty texture considerably), but particle size doesn’t significantly affect a compounds solubility, and the relatively low solubility of creatine monohydrate can be problematic when large doses are taken.

In general, 5 grams of creatine will require somewhere in the neighborhood of 16 ounces of water to be dissolved. And, of course, the more creatine is dissolved in liquid, the more can be absorbed into the bloodstream. If creatine is taken without sufficient liquids, its relatively poor solubility may draw water into the gastrointestinal tract, causing stomach upset or diarrhea.

Also, when large doses of creatine are taken, the breakdown products of creatine which are formed may be able to provide a nitrogen (protein) source for various intestinal bacteria. Much of the gas and intestinal upset associated with creatine use may be attributable to the metabolism of creatine–related compounds by intestinal bacteria.

A certain researcher in the nutritional supplement field has written that the creatine metabolite creatinine may be of benefit to intestinal health. This researcher has apparently confused the effects of beneficial intestinal bacteria with those of pathogenic intestinal bacteria. The existing research makes it very clear that intestinal bacteria is likely to produce toxic metabolites from creatinine. These metabolites are probably of relatively little significance in healthy individuals, but the formation of nitrogen–based toxins by intestinal bacteria could is certainly not beneficial, and could easily account for much of the stomach upset some creatine users notice. This is yet another reason why finding the right dose is so important with creatine.

Study Link – Implication of creatinine and gut flora in the uremic syndrome: induction of "creatininase" in colon contents of the rat by dietary creatinine.

Quote from the above study:

…microbial action could lead to the formation of toxic products from creatinine that, in the presence of decreased renal function, would be retained.

And the fact is that many people unknowingly consume much larger amounts of creatine than their body can efficiently absorb at any one time – creating a surefire formula for stomach upset.

Most people taking creatine may even be taking far higher amounts than they think they are. For example, the standard serving size of creatine listed on most straight–creatine monohydrate products is 5 grams – a reasonable dose by most standards. But, this serving size is often listed rather nebulously as a “heaping teaspoon.” Of course, in actual practice, few people measure their creatine dose precisely, and a heaping teaspoon of creatine usually ends up being six, seven, or eight grams of creatine (depending upon how generously we interpret the term “heaping,” and whether an actual measuring teaspoon is used). And let us not forget that most bodybuilders aren’t known for their sense of precision or moderation when it comes to substances which can improve performance.

So a “heaping teaspoon” of creatine taken 4 times a day could easily amount to 28–32 grams of creatine at the very least – a pretty far cry from the 20 grams we’d be shooting for in most creatine–loading protocols.

The take home message is that it may be worthwhile to give creatine loading a try, assuming proper doses are taken, spaced out over the course of the day, and taken with sufficient water for best absorption. Excessive doses of creatine (especially large doses taken all at once) are quite likely to cause stomach upset, and this can give users a bad first impression of creatine. But it’s very important to remember, again, that, it’s the dose of creatine responsible for this effect, not creatine per se.

We’ll continue with our creatine Q & A in the next Integrated Supplements Newsletter.