The Power behind Creatine

The Power behind Creatine
Published on Friday, May 23, 2014 by
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The average 150-pound person holds about 120-140 grams of creatine in his body and loses about 2 grams of creatine through urination per day.
Among all the bodybuilding supplements available today, none has been studied as extensively as creatine monohydrate. Furthermore, no other supplement has received as many accolades from the scientific community. In fact, there are more peer-reviewed studies supporting creatine as safe and effective than most other supplements combined.
Though creatine wasn’t introduced to North America’s commercial market until the 1990s, its ergogenic potential has been studied since the early 19th century when a French scientist named Chevreul discovered a new constituent of skeletal muscle, which he named creatine. He named it according to the source from which it was isolated, Ureas (Greek for flesh). German scientist von Liebig confirmed that creatine existed in meat and hypothesized a link between creatine and muscle performance. Nearly half a century later, scientists began extracting creatine from meat and investigating its performance-enhancing properties.
We’ve sifted through the wealth of data, research and status of creatine in its many forms to report the latest findings so that you can make educated choices with your creatine supplements. We’ll also share the current information
on timing and dosage and what benefits science tells us you should expect.


The effects of creatine are best seen in individual muscle fibers. There are numerous studies showing that creatine can start working relatively soon after supplementation begins. Creatine augments the ability’ for high-energy phosphate to diffuse between mitochondria and myosin heads, thus enhancing cross-bridge cycling and tension production. Thus, you’ll note remarkable increases in strength within weeks of starting creatine supplementation.
Creatine ingestion quickly increases phosphocreatine stores in skeletal muscle, providing support for rapid phosphorylation of ADP to ATP under repeated powerful contractions of short duration (fewer than 10 seconds). This effect provides dramatic increases in strength under shorter rest periods. In addition, the phosphorylation of ADP requires phosphocreatine and stimulates phosphofructokinase (a rate-limiting enzyme for glycolysis); this increases the rate of glycolysis, and more ATP (energy) is produced. This effect is beneficial for strength feats that last from 10 seconds to more than two minutes.
Medical studies have demonstrated that creatine is safe and well tolerated when used for long periods of time. There are also a plethora of studies illustrating that creatine supplementation is associated with skeletal muscle hypertrophy and increased protein synthesis. The postulated mechanism for creatine’s muscle-building effect is based on its ability to create an osmotic gradient whereby water is shunted into muscle cells (i.e., cell volumization), an anabolic stimulus. Furthermore, recent evidence has shown that creatine supplementation augments anabolic insulin-like growth factor-1 (IGF-1) release, thus providing another pathway for increasing lean mass.


As with most consumer products, supplement companies are constantly trying to improve the digestibility, bioavailability and potency of creatine. This focus has led to the development of several forms of this great supplement.

Creatine Monohydrate

Creatine monohydrate is aptly named because it contains one molecule of water bound to each molecule of creatine. This was the first form to start all the hype about creatine’s muscle-and strength-building properties and, as a result, it’s the most studied and scientifically supported form of creatine today. Creatine monohydrate provides great benefits for most users and is generally well tolerated as a microionized powder. Early versions of creatine were not microionized, which caused some users to feel bloated and develop cramps, and it even gave some individuals diarrhea.
Creatine monohydrate is likely the most affordable form of creatine on the market, but be aware there are substandard products out there. Buy from
reputable and well-established companies and watch for the Creapure label for assurance that you’re getting uncontaminated pharmaceutical-grade creatine.

Creatine Anhydrous

This type is the same as creatine monohydrate, except it’s been dehydrated. Thus, you get a little more creatine per gram when you buy the anhydrous form (about 5-6%) and its effects are comparable to creatine monohydrate.

Dl- and Tri-Creatine Malate

This compound is formed by bonding two (di) or three (tri) creatine molecules to malic acid. Malic acid is an organic substance that serves as an important intermediate in the citric acid (Krebs) energy cycle. This form of creatine was developed based on the hypotheses that it would boost ATP (energy) production greater than creatine monohydrate and that it would be more tolerable in the body because it’s highly dissolvable in water. There is very limited research to support creatine malate as a superior form of creatine, but anecdotal evidence suggests it’s well tolerated in those who can’t take creatine monohydrate because of the gastrointestinal side effects.

Creatine Orotate

This compound also shows promise in theory but is yet to be studied extensively. Creatine orotate is a compound formed by binding creatine with orotic acid and is patented under the name CreaTate. The purported benefits of this supplement over creatine monohydrate include increased muscle phosphocreatine and free creatine levels (via augmented uridine concentration) and increased muscle carnosine levels. In theory, this supplement should increase muscular strength and endurance. In support, numerous studies illustrate orotic acid’s ability to increase muscle carnosine leading to increased muscular endurance.

Creatine Kre-Alkalyn

This is another patented form of creatine. It’s reported to be “buffered creatine” that’s produced at a higher pH, which apparently blunts the conversion of creatine to inactive creatinine, leaving more creatine to be absorbed. In addition, this form apparently doesn’t convert to creatine until it enters muscle cells, albeit there have been no clinical trials conducted to prove this suggestion. Thus, the founders claim this form of creatine can be taken in much smaller doses with the same benefits as creatine monohydrate and, because doses are smaller, it’s taken in capsule form. Although there aren’t any studies published on this supplement, numerous anecdotal reports support this form of creatine.

Creatine Citrate

Like creatine malate, creatine citrate is a compound made by binding creatine to an important Krebs cycle intermediate, with citric acid used instead of malic acid. Based on the importance of citric acid in the production of ATP, the rationale behind formulating this compound was that creatine citrate might provide greater muscular energy compared to creatine taken on its own. As well, this compound readily dissolves in water, making it easier to
digest. At present there haven’t been any peer-reviewed articles to substantiate creatine citrate as superior to creatine on its own. Also, it should be noted that because this type is formed by binding a single creatine molecule to a single citric acid molecule, less total creatine is provided per gram (about 40-50% less) as compared to creatine monohydrate or anhydrous.

Creatine Phosphate

As the name implies, this creatine is bound to phosphate, an essential step carried out in the body to make creatine active. This form of creatine was released soon after creatine monohydrate and quickly became popular, but it became obsolete when it was shown to be less effective than creatine monohydrate.

Creatine Serum

Also known as liquid creatine, this form is precisely what the name implies. The idea behind creating creatine serum was to increase digestibility and bypass the stomach’s acidic environment (known to degrade creatine). The problem is that creatine is very unsta-
ble in liquid and thus should be taken immediately after dissolving in water. Because of the unstable nature of creatine in liquid, early versions of this supplement were completely ineffective. Several companies, however, have been working on versions of liquid creatine that they claim are stable for years. There still isn’t any published data to substantiate these claims.

Creatine Tartrate

By now you’re probably starting to notice a pattern in the creatine nomenclature. This form is the result of binding a creatine molecule with a molecule of tartaric acid. You rarely see this form used as a stand-alone supplement; however, because of its stability when formed in a solid, it’s usually included in products like energy bars, capsules, tablets or chewables. An interesting and disturbing fact is that tartaric acid is a known muscle toxin in high doses.

Creatine Titrate

This is a pH-shifted form of creatine that increases the solubility of creatine
in water. The theory is that more dissolved creatine makes for easier digestion and greater bioavailability. Users report great outcomes along with less bloating, although evidence is purely anecdotal at present.

Magnesium Creatine Chelate

You guessed it — chelating creatine and magnesium together forms this compound. The rationale behind the development of this compound was based on the fact that magnesium is essential for the conversion of creatine phosphate to ATP for energy. In addition, chelation increases the stability of the compound. Scientific evidence proves that using this form of creatine is better than taking a creatine and a magnesium supplement separately. Researchers have reported greater increases in leg strength and cell volumization in those who took magnesium creatine compared to those who took the creatine and magnesium separately.


This form is created by binding the amino acids taurine and glutamine with creatine. The basis for developing this supplement was to enhance muscle cell volumization. This is a reasonable postulate because all three are cell volumizers when supplemented on their own. Furthermore, the amino acids in this combination may enhance recovery and strength gains; however, there haven’t been any peer-reviewed studies published on this compound.

Creatine HMB

This form is what you get when beta-hydroxy beta-methylbutyrate (HMB) is bound to creatine. It’s well documented that HMB speeds recovery, is antieatabolic and aids in fat loss, especially in those who’ve just started heavy weight training. By binding HMB with creatine, the compound is more soluble and apparently less prone to degradation in the stomach. As a result, creatine HMB is speculated to be a more bioavailable form that gives you all the benefits of creatine and HMB supplementation. Studies that have used this compound are lacking, hut users generally report good results.

Creatine Ethyl Ester (CEE)

Also known as creatine ester or CEE, this is one of the newest creatine forms, made by adding an alcohol and an acid to form creatine ester ethyl hydrochloride. The patent on CEE is in the hands of UNeMed at the University of Nebraska Medical Center. The motivation for developing CEE was in an effort to provide a more bioavailable form of creatine. The addition of an ester to creatine theoretically increases the lipophilicity (fat dissolvability) of creatine, making it very easy for it to cross cell membranes driving more creatine into muscle cells. Unfortunately, recent scientific evidence has shown that the addition of an ethyl group to creatine reduces its acid stability and is inactivated to creatinine in the physiological environment.

Effervescent Creatine

This is an older form of creatine made by combining creatine monohydrate (or citrate) with citric acid and bicarbonate. When water dissolves the powder, the acid (citric acid) reacts with bicarbonate (an acid buffer) to release a highly soluble form of creatine into the buffered aqueous environment. Scientists hypothesize this form of creatine is more easily digested and remains stable in solution for hours. Unfortunately, there aren’t any studies to back these claims, but users report good results from this form of creatine.

Timed-Release Creatine

This format is a relatively new approach to maximizing creatine delivery. The idea behind timed-release creatine is that the body can take on more creatine if it’s delivered in precise amounts throughout the day. Several companies have their own version of this product on the market, and their “delivery systems” are pro-
prietary or kept secret. As such, there aren’t any published studies to show that this form of creatine is superior to others.


In total, that’s 16 different forms of creatine. At this point you should be aware that some forms are better than others and most aren’t backed by any scientific studies. Of all the forms available, however, one still stands out as the gold standard: micro-ionized creatine monohydrate. After all, it’s the most affordable and most studied form, with an abundance of data backing it as the most successful supplement to date.
Based on scientific data, the best way to supplement creatine monohydrate is by including a one-week loading phase at approximately 0.3 grams/ kilogram (bodyweight) per day followed by maintenance at approximately 0.1 grams/kilogram (bodyweight) per day . To calculate your weight in kilograms, divide your weight in pounds by 2.2 (e.g., A 200-pound bodybuilder is 90.9 kilograms; 200/2.2 = 90.9). During the loading phase, split the daily dose into approximately 5-gram servings to be ingested throughout the day, making certain that one dose is ingested 30 minutes before your workout and another is taken 4-6 hours post-workout. During the maintenance phase, ingest one serving prior to and another post-
workout. On your rest days take one dose in the morning with breakfast and one dose with dinner.
Some argue that creatine monohydrate should be cycled for best results. A typical creatine cycle could be carried out in three phases: 1) Loading: one week; 2) Maintenance: four weeks; 3) Recovery: three weeks, no creatine. Repeat cycle as many times as desired.
Always mix creatine monohydrate in 6-8 ounces of a high-glycemic index sugar-based drink and avoid mixing with acidic juices like orange or grapefruit juice, as the acid will degrade the creatine. Sugar-based drinks are the best way to consume your creatine (especially post-workout) because the sugar helps boost insulin response, which research shows can boost creatine absorption by as much as 60%!
While you may have thought that fruit juice is the No. 1 option when mixing creatine, that’s a mistake. Most fruit juices contain fructose, which isn’t a fast sugar. Furthermore, the acid in citrus juices may render the creatine inactive by converting it to creatinine. Stick with high-glycemic index (fast) sugar-based drinks that contain maltose, glucose or dextrose.

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