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Prior to 1993, the dietary supplement industry was hard-pressed to produce a discount product that actually built muscle. There was protein, various amino acid pills, brewer’s yeast, fat burners, multi-vitamins, and liver tabs. There was also a plethora of useless discount products that merely drained the wallet. Even the above named supplements, while helpful, didn’t produce noticeable, rapid gains in size and strength. Little did the dietary supplement industry know, that in 1920, scientists discovered ingestion of large quantities of creatine phosphate, a component in skeletal muscle first discovered in 1832, led to an increase in intra-muscular creatine levels (1). Why is this important? To explain that question, a brief biology lesson is in order: After being transported into the muscles (more on transport agents later), creatine bonds with phosphate to form creatine phosphate, which reacts with acatalyst enzyme, to form phosphocreatine (PCr). Creatine monohydrate increases PCr levels up to 20%. This increase in PCr is important because it binds with ADP to form ATP. More ATP in muscles means more anaerobic strength, an increase in muscle size, and quicker recovery (1). Finally, creatine supplements are now available.

While competitive athletes from Eastern-Bloc counties may have been using creatine supplements as far back as the 1970's, it wasn't until a few years after the 1993 release of Phosphagen by EAS, that creatine supplements caught on. Recreational athletes, bodybuilders and power-lifters in particular were seeing gains of up to two lbs. in as little as one week (1). In 1998, MuscleTech one-upped EAS by including carbohydrates and alpha-lipoic-acid (ALA) in its discount creatine product, which became extremely popular, especially among hard-gainers due to its calorie content and addition of ALA.  ALA is a potent anti-oxidant that has been clinically proven to enhance PCr levels, improve insulin sensitivity, and increase glucose uptake into skeletal muscle (2,3,). 

However not everyone wants a massive dose of carbohydrates with their creatine supplements.  In addition, many people experienced stomach-cramping and/or diarrhea from creatine monohydrate, which led to the advent of creatine-transport products These products incorporate different salts of creatine, such as creatine-titrate, citrate, and malate to name a few. In addition to replacing the monohydrate salt, other ingredients intended to increase the transport of creatine into muscle cells without the extra calories were discovered. A few examples of such ingredients are: Cinnulin-PF, a water-soluble extract of cinnamon, various phosphates, other amino acids such as taurine, glutamine, and arginine, as well as herbal extracts such as 4-hydroxy-isoleucine from the fenugreek herb, and d-pinitol from the leaves of the soybean plant. Yet another creatine innovation came in 2004, with the release of creatine ethyl ester (CEE), or estrified creatine. CEE products claim to provide all the benefits of regular creatine supplements, without the need for added carbohydrate or transport agents to get the creatine into muscles, as the addition of an ester theoretically, would allow the creatine to reach muscle cells through diffusion.

In terms of dosing, the initial protocol for creatine monohydrate has two options: a loading period of 20 grams per day for 5-7 days, followed by 5-10 grams per day for a given period thereafter, or 2-5 grams a day, which produces slower results, but doesn't tax the kidney's as much, and is safer if one decides to use creatine for an indeterminate time. Dosing for different creatine products such as CEE and the various cell-volumizers available vary greatly depending on the product.  Following the directions on the label is the best option.  In addition, many researchers now believe that the loading period for regular creatine is not necessary. One very important note regarding creatine is product purity.  Impure creatine can contain creatinine, a metabolic byproduct of creatine that is toxic to the kidneys.  Also, creatine begins to convert to creatinine within 24 hours of being added to liquid, so never pre-make your creatine supplement drinks. Micronized-creatine is also a more convenient option, as it has a higher solubility in water, and doesn't have to be constantly shaken during consumption. 

When creatine first started gaining popularity, media scrutiny followed. Some athletes complained of muscle cramps, and during the late 1990's news stories concerning the safety of creatine supplements would pop up frequently. It was later determined that muscle cramping during creatine supplementation is caused from dehydration, and a loss of as little as 2% of body weight can cause an athlete to be dehydrated. It is recommended to consume at least a gallon to a gallon and a half of extra water a day while on creatine for this reason.  Despite the negative publicity that came with its meteoric rise to fame (supporting the idea that no publicity is bad publicity), creatine is still one of the safest, and widely used dietary supplements to this day. Even the original Phosphagen and Cell-Tech formulas remain top sellers, despite their being close to a hundred other discount creatine products available. In addition, the original, tried and true creatine monohydrate remains the most popular form of creatine, with annual US sales reaching $400 million in 2005 (1).

References:
1. Creatine. Wikipedia. Available: http://en.wikipedia.org/wiki/Creatine
2. V. Therunavukkarusu, Et. al. Lipoic acid attenuates hypertension and improves insulin sensitivity, kallikrein activity and nitrite levels in high fructose-fed rats. Journal of Comparative Physiology. 2004 Nov;174(8):587-92. Epub 2004 Sep 29. Available: PubMed.
3. Burke, D.G. Effect of alpha-lipoic acid combined with creatine monohydrate on human skeletal muscle creatine and phosphagen concentration.” International Journal of Sport Nutrition and Exercise Metabolism.

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