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What is Creatine?

Creatine has been one of the most popular and effective supplements since it's introduction as creatine monohydrate back in 1993, with the first product coming from EAS, called PhosPhagen (named after one of the body's energy systems). This was a milestone product to be sure.

Let's define exactly what creatine is: it's a nitrogenous compound that occurs naturally in meats and fish and is synthesized by the liver, pancreas and kidney. It's produced from three amino acids: methionine, arginine and glycine.

Creatine is not really new as it was first discovered in 1835 by a French scientist named Chevreul, who named it after the Greek word for flesh “Kreas”. It was first linked to muscle tissue in 1847. In 1922, human studies dating back to 1910 were reviewed by a scientist named Hunter(1), in these studies, subjects were loading with creatine up to 20 grams per day for 6 days. In 1926, Chanutin (2) detailed case studies where human subjects loaded 4 times a day for 10 days. In the 70's, researchers thought insulin might be involved in the uptake of creatine, this was determined yet again in 1992 by Harris(3). By the way, the 1992 Harris study was one of the pioneering steps to creatine hitting the marketplace. In 1993 creatine monohydrate was actually introduced as a supplement, as mentioned above, by EAS. Ed Byrd, known as “Mr. Creatine”, an EAS co-founder and the man that gave us NO2 in 2002, was largely responsible for it's introduction. It caught on pretty quickly and caused most every supplement manufacturer to scramble for their own version. It's interesting to note that many major manufacturers of the day turned down the chance to be the first to market it because they didn't understand it. This was the days of the mega calorie weight gainer and to come along with a product that has no calories? No way will that ever fly! Well, as we now know, it has proven extremely successful, re-defining what a natural supplement can do!

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Benefits of Creatine:

  • Increases muscular endurance.
  • Increases muscle size and strength through cell expansion.
  • May be involved in protein synthesis.

To better understand the benefits, we need to take a look at how creatine works:

Muscles store creatine as creatine phosphate, which functions as part of the ATP-CP energy system, also called the Phosphagen system. Muscle cells contain 4 to 6 times as much creatine phosphate as ATP. ATP is the immediate energy source for muscle cells at both high and low intensities, however, it can take less than a second to burn your bodies reserve of ATP. This is where creatine phosphate (also called phosphocreatine) comes in. Your body has a small reserve of creatine that your muscles can quickly convert to ATP. However, this will only power an all out effort for 3 to 15 seconds. As exercise intensity decreases and the duration increases, as in a marathon type race, your body turns to other systems of energy production. The Phosphagen system is used primarily for shorter duration exercise, as in bodybuilding training. Creatine use as a product that can enhance muscle cell energy production becomes obvious when you look at the re synthesis of creatine. There's a regulating enzyme known as creatine kinase that breaks down creatine, separating the phosphate molecule from the creatine molecule. Phosphate then binds with ADP, which lacks just one phosphate from becoming ATP. So basically your body can manufacture fresh ATP through this process, which can take up to 4-5 minutes.

So, the more creatine available, the more that can ultimately be used for energy, allowing you to train harder and longer which can lead to better results, whether it's improved performance or more muscle and strength.

It also acts as a voluminizer or cell expansion product by pulling water into the muscle cell, causing it to expand, resulting in a increase in muscle size and strength. This is also referred to as sarcoplasmic hypertrophy and is one of the current theories of muscle growth. As well, this is a very big product category right now, covering pre workout drinks, intra workout drinks and numerous stand alone products but creatine was really the first product to cause this effect. In fact, when it was first introduced you heard more about this benefit and not as much about the endurance aspects.

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Evidence Behind Creatine

There are numerous reports of quite a few tests being done on creatine, here is an example of a recent one:

Dr Martin Engelhardt from the Orthopoadische Universitatsklinik in Frankfurt formulated a cycle ergometer experiment comparing endurance/ power endurance exercise in athletes without creatine supplementation against those with low-dose supplementation.

Twelve regional class triathletes aged between 22 and 27 were selected to take part in the test. Each athlete underwent a preliminary incremental cycle ergometer test to determine their 3 mmol.L-1 blood lactate intensity. Once established, this intensity was used as the aerobic exercise intensity for the experiment.

The testing began with each athlete performing their aerobic exercise on the cycle for 30 minutes, followed by two bouts of high-intensity interval training, which involved cycling hard for 15 secs and then 45 secs at their aerobic exercise intensity,10 times before two minutes rest and systematically repeating the interval session. After this, the subjects were 'rewarded' with another 30 minutes of cycling at their specific aerobic exercise intensity (a total of one hour and 20 minutes cycling!).The test results were then kept from the athletes, and the following day they were administered 6 grams of creatine daily (to be taken in two 3g doses) for a period of five days before returning to repeat the test. You've probably noticed that the creatine loading dose only amounted to 30g over the five days, whereas in many other studies of creatine supplementation the normal dose is 100g (four doses of 5g daily for five days).

Blood samples were taken throughout the testing to monitor creatine, creatinine (the degradation product of creatine), glucose and lactate levels, whereas urine samples(for measurement of creatine and creatinine urine levels) heart rate and oxygen uptake were measured both before and after the aerobic exercises.

The results: after creatine supplementation analysis of the blood and urine samples showed significant increases in the serum creatine concentration in the blood and serum creatinine levels in the urine. Fifty percent of the athletes in the first test couldn't complete the entire second 30 min bout of endurance exercise,whereas after taking creatine each of the athletes who had struggled in the first test managed to increase their ride time by four minutes. However, after creatine supplementation, the researchers report that the total number of interval reps increased significantly and that 75 percent of the athletes improved their performance (nobody did the reverse).

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Creatine Safety

Amazingly there is still a lot of misconception about creatine. Some people, including members of Congress and some sport federations, think creatine is a steroid. In fact, many college level sport federations have banned creatine and Congress would like to see it banned from retail sale. The truth is, creatine is not a steroid, it will not kill you or ruin your kidneys. As should be the case anyway, you should be drinking a lot of water as part of your daily program as this does help flush out creatinine, the waste by-product of creatine. As well, and as is the case with any supplement, spend some time doing research, including reading user reviews. This will help you to make an informed choice and choose a quality brand.

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Creatine Supplements, Timing and Dosage

Creatine comes in tablets capsules, powder versions and chewables, with less popular versions as liquid and even effervescent packets. There are numerous types that have hit the market since the early 90's:

Monohydrate - again, this is the original, you have to take sugar with it in order for it to be properly absorbed (any sugary drink will do but when it first hit the market, apple or grape juice was recommended). It requires a loading phase of 4-5 doses (typically 5 grams per dose timed to be on an empty stomach) per day for up to 5 days and once a day thereafter. Some side effects reported in some users are bloating, gas and diarrhea. For this reason, companies began to explore other versions that did not require sugar, loading or 5 grams per dose and did not cause the side effects associated with monohydrate.

Ethyl Ester – one of the first products requiring a smaller dose, typically 2-3 grams per serving. No sugar is needed for absorption and no loading is required. This version, as is the case with most newer versions, eliminates the monohydrate effects. Available as a pill or powder, you usually take one serving (usually 2-3 grams) twice a day separated by at least 6 hours.

Tri creatine Malate - Tri-creatine malate is a compound made from three creatine monohydrate molecules that are attached to one molecule of malic acid. Malic acid is involved in the Krebs energy cycle as an intermediate substance, and helps to provide energy to the body. When malic acid and creatine monohydrate form Tri-creatine malate, it becomes more water-soluble than regular creatine monohydrate, deals with the side effect of gastric discomfort, and is more efficient at impacting the ATP cycle. Tri-creatine malate is also believed to offer greater bio-availability over regular creatine monohydrate. What is the Kreb's energy cycle? It is defined as a cycle of enzyme-catalyzed reactions in living cells that is the final series of reactions of aerobic metabolism of carbohydrates, proteins, and fatty acids, and by which carbon dioxide is produced, oxygen is reduced, and ATP is formed. Also called citric acid cycle, tricarboxylic acid cycle. It's important to note that there are actually several energy systems that the body uses.

Buffered Creatine - also known as Kre-Alkalyn. This version actually has a patent on it, #6,399,631. The research on this ties into creatine's conversion to creatinine, a waste byproduct of creatine usually produced at a reasonably constant rate, which gets filtered through the kidneys and passes out in the urine. The advertising behind this product talks about creatine converting quickly to creatinine when mixed in liquid (many creatine products encourage drinking their powder within 10 minutes of mixing for this reason). The research behind this product indicates that as the ph of creatine rises, conversion to creatinine slows. At a ph of 12, it stops altogether. So, this version solves that problem, requires less total creatine per serving, removes any potential gastric discomfort. With this product, you use 1-2 grams in the morning and again before training.

Micronized Creatine - this is a version of monohydrate comprised of smaller particles than regular monohydrate powder – as much as 20 times smaller! The primary purpose is improved absorption , better mixing and no stomach bloat or upset. The serving size is 5 grams, you mix one heaping teaspoon into 8oz of juice or water and drink right away. For best results, you should drink 8 to 10 glasses (8 oz) of water a day. There is a loading phase similar to the standard monohydrate version: Loading Phase: Day 1 through 5- Take 1 heaping teaspoon 4 to 6 times daily.

Maintenance Phase: Day 6 through 21- Take 1 heaping teaspoon twice daily. Then go off for 3 days, and repeat the cycle.

Liquid Creatine - this is not as popular as it once was, the biggest complaint being the lack of stability which leads to poor results.

Conjugated - This is one of the hot versions on the market, the primary product being Con-Cret by Promera. This product is a concentrated creatine, requiring a micro-dose of one teaspoon. As with the other versions competing with monohydrate, you have superior absorption, no side effects, and the need for less total creatine.

Creatine anhydrous – This is creatine monohydrate without the water molecule, providing about 6% more pure creatine per serving compared to creatine monohydrate.

Creatine citrate - Creatine citrate first appeared on the market not long after monohydrate. Creatine citrate is a creatine molecule bonded to a citric acid molecule. Remember that citric acid is important in providing aerobic energy in the muscles. For this reason it's speculated that creatine citrate will provide an athlete with more energy.

Creatine phosphate - This is another early form of creatine. This is a creatine molecule bonded to a phosphate molecule. This is actually a process that naturally occurs within muscle cells. This version seems to be less effective then mnonhydrate and as such, is not that popular.

Magnesium creatine - Magnesium creatine is creatine chemically bonded to magnesium. Magnesium assists in the digestion of creatine, primarily helping it pass through the stomach. Magnesium is also involved in the process of turning creatine phosphate into ATP.

Creatine glutamine taurine - This version of creatine is bonded with glutamine and taurine. Both glutamine and taurine act to volumize cells, with a side benefit - taurine has been shown to improve strength.

Creatine is also found in numerous formula products, such as pre workout, intra workout and post workout supplements as well as some protein and weight gain powders. You can even find it in some protein bars.

Timing, then, becomes a little cloudy but primarily, it's best to use it before/during a workout and depending on the product, one other time of the day, typically several hours before or after training. However, if you are using a pre or intra workout product, you may need to buy a separate, stand alone version to use on your off days and non training time frames. Dosage, as we have seen, is product and version specific, so label reading is a must. Additionally, many people cycle creatine. The main reason for this is to simply give your body and wallet a break. Cycling is not required but like most things, you adjust to it after a while and results slow, going off for 6-8 weeks allows for fresh results when you go back on. Finally, as mentioned above, maintain a high water intake, which is important anyway as we are primarily made of water and so many of the chemical processes happen in our bodies in the presence of water.


by creatine supplementation. Clinical Science 83:367-374,1992
Also used was the college textbook Discovering Nutrition, by Paul Insel, R.Elaine Turner and Don Ross,
Published by the American Dietetic Association

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