Saturday, March 5, 2011

Another one bites the dust!

It would not be an exaggeration to say that creatine is one of the most popular and effective sports supplements. Studies show that about 70% of those who use creatine supplements obtain definite ergogenic benefits, including increased body mass, strength, and upgraded muscle endurance. Most of the published studies attesting to creatine efficacy have involved creatine monohydrate, which is composed of 99% creatine and 1% water.While forms of creatine were routinely used by Russian and East German athletes in the 60s, the use of creatine as a popular sports supplement began in 1993. The ongoing popularity of creatine has led to a variety of supplemental forms of creatine. Some creatine supplements contain simple sugars, based on studies showing that promoting an insulin release boosts muscle uptake of creatine. In actuality, the efficiency of muscle creatine uptake is dependent on the creatine transporter protein found in muscle. With continued use of creatine, this muscle transporter eventually downgrades, and when that happens, most of the ingested supplemental creatine is rapidly converted into the creatine metabolic byproduct, namely creatinine. Creatinine, however, provides no ergogenic effects, although it does provide a minor antioxidant effect. In recent years, many ads for various creatine products suggest that creatine monohydrate is difficult for the body to absorb. Other ads suggest that the harsh acidic enviroment of the stomach rapidly degrades creatine into creatinine. In fact, several good studies show that creatine is completely absorbed into the gastrointestinal tract. The conversion of creatine into creatinine is negligible, contrary to some ad claims. In fact, the availability of creatine in the blood after oral ingestion approaches 100% of the dose, and you can’t get much better than that. Then why do so many products claim to be vastly superior to plain old creatine monohydrate (CM)?

Creatine is not very water soluble, and also doesn’t easily penetrate cellular membranes. Based on these known characteristics of creatine, a few creatine supplemental variants have emerged with the goal of overcoming these creatine barriers. One in particular, creatine ethyl ester (CEE) even makes the formidable claim that it bypasses the creatine transport protein limitation. It allegedly does this because the ethyl part of CEE is alcohol, which is known to easily penetrate fatty cell membranes. The theory behind CEE is that the ester protects it against premature degradation in the gut, while also speeding uptake into muscle. As such, you would need to ingest far less creatine, and the amount you do ingest would increase muscle uptake considerably. According to CEE advocates, enzymes in the gut called esterases remove creatine from its ester, thereby producing free and active creatine. But the proof for this supposed enhanced creatine uptake with CEE had little or no evidence to back up the many grandiose ad claims about CEE, such as that it provided 400% or more better uptake compared to CM. Some recent studies have tested CEE and compared it to CM. The results are not going to make those who sell CEE too happy.

For example, one study, published in Journal of the International Society of Sports Nutrition, featured 30 untrained men, divided into placebo, CM, and CEE groups. The study, which lasted for seven weeks, had the men in the creatine groups ingest 20 grams a day for 5 days, followed by 5 grams a day for 42 days. Throughout the course of the study, all the subjects trained with weights on a 4-day split routine. The results showed high blood levels of creatine in the placebo and CM groups compared to the CEE group. On the other hand, blood levels of creatinine was higher in the CEE group compared to the other groups. Both creatine groups showed higher muscle levels of creatine compared to the placebo group, but there wasn’t any significant difference between the creatine groups in this regard. While ad claims for CEE suggest that this form of creatine results in less extracellular water retention, this study showed that CEE, in fact, produced the highest level of extracellular water retention. The main conclusion of the study was that not only wasn’t CEE superior to CM, but most of ingested CEE appears to rapidly degrade into creatinine.

Another recent study, published in the International Journal of Sports Medicine tested the notion that intestinal esterase enzymes cleave the ester off of CEE, thereby liberating the creatine portion for use in muscle uptake. The study found that the esterase enzymes did not convert CEE into active creatine to any significant degree. Instead, nearly all of the creatine took a direct route into relatively useless creatinine. All of this information should not be surprising. CEE was initially formulated in the 1920s. A 1955 study found that CEE was too inherently unstable to be of any practical use. Which begs the question: Why was CEE introduced to the sports supplement market?  The answer is that the mechanism for the higher efficacy of CEE seemed initially plausible–but untested. A darker motivation for some was unabashed greed. The bottom line, however, is that all forms of supplemental CEE are considerably more expensive than CM, yet paradoxically is far less effective for its intended purpose. Perhaps it’s time to relegate CEE to the list of ineffectual  supplements that appeared promising but proved to be a bust. In that sense, CEE has plenty of company, with such notable past failures as boron to boost testosterone, HMB, and numerous others.

For more information about creatine and various other sports supplements, check out my e-book,Natural Anabolics. Information is available at:


Spillane, M, et al. The effects of creatine ethyl ester supplementation combined with heavy resistance training on body composition, muscle performance, and serum and muscle creatine levels.J Int Soc Sports Nutr 2009;6:6

Giese MW, et al. Qualitative in vitro NMR analysis of creatine ethyl ester pronutrient in human plasma.Int J Sports Med 2009: in press.

Learn the truth about anabolic supplements in my e-book, Natural Anabolics, available at