Creatine's affects are surely no secret to this audience. From increased strength to noticeable and sometimes painful pumps to enhanced recovery to increased muscle mass/volume, creatine is one of the most well-respected supplements for those that respond.
The fact that a portion of the population does not respond to creatine has been known for many years but no one took the time or energy to study it in enough detail to determine its cause or how to solve the problem. I saw this as a challenge and decided to set myself on a mission which would enable nearly all people to experience the wonderful effects of creatine.
My first challenge was to determine what made creatine work in some individuals but not in others. Through much study and effort, I determined that nonresponders where either not absorbing the creatine from the intestines efficiently or that their livers were extremely efficient at metabolizing creatine. I then started looking for a way to solve these two problems. My first thought was to find a way to modify the creatine molecule so that it was more absorbable.
I developed a patent pending compound called dicreatine malate which is a highly water soluble compound which has a much greater bioavailability than creatine monohydrate. This was definitely an improvement as our trials showed that only 15% of users didn?t respond to dicreatine malate as opposed to 25% for creatine monohydrate. I had solved part of the problem but the issue of the liver being hyper-efficient at metabolizing creatine was still a thorn to be plucked.
My thinking was to search for a totally novel compound that acted like creatine but which would not be broken down so easily in the liver. I investigated a compound called cyclocreatine. This compound worked absolutely fantastic with at least a 95% success rate. I thought I hit the jackpot. Until I realized that cyclocreatine was not a candidate for being a dietary supplement. Although very effective and safe, cyclocreatine is a purely synthetic molecule which does not occur in nature. Pressing on, I continued my search.
I decided that instead of looking for a chemical modification of creatine, I would look for precursors and metabolites of creatine in hopes of finding some golden nugget. After a little digging, I realized that the direct precursor of creatine had a high oral bioavailability and was efficiently converted in the liver to creatine. Bingo! You guessed it. The compound name is glycocyamine (pictured below) or guanidinoacetic acid. Basically, glycocyamine is creatine without a methyl group (creatine is methylguanidinoacetic acid).
The great part about glycocyamine is that while being metabolically processed by the liver it is converted into creatine. In this case, those people who have the most efficient livers would be the best responders. Finally, according to the literature, glycocyamine is an insulin sensitizer similar to Metformin. This would enhance even further its muscle volumizing effects while inhibiting additional adipose formation.
The research on glycocyamine was sound and my theory seemed perfect. I just had to prove it with real world results. Upon testing many individuals with glycocyamine, I realized that we hit pay dirt. Glycocyamine worked for nearly everyone, giving them stereotypical creatine-like effects. Furthermore, no one noticed the stomach upset and bloating that is so typical of creatine monohydrate use. To be honest, it worked better than expected. Our research wasn?t finished though as we had to test its effects in combination with other compounds as well as to study its safety profile.
The first thing that I wanted to try was to combine glycocyamine with creatine to see if there was some type of additive or synergistic effect. Obviously the creatine nonresponders did not receive any additional benefit from the creatine.
However, the creatine responders noticed a definite benefit from adding the creatine. I don?t think the effect was synergistic but was at least partially additive. From our data, it appears that glycocyamine plus creatine works about 1.5 times better than creatine alone. This was truly a breakthrough discovery that would send some shockwaves through the supplement industry.
In the beginning, I saw nothing in the literature that led me to believe that glycocyamine was not as safe as creatine. Users felt and performed well on it. At this time, I recommended about 2-3 grams per day. I then stumbled upon one critical study that made me reconsider the dosage. In a nutshell, the study discussed that creatine production in the liver from glycocyamine was the body?s greatest depleting process of valuable methyl groups.
Another critical use of these methyl groups is to metabolize and detoxify the body of homocysteine. Homocysteine is one of the bad guys in which high levels are correlated with such things as increased stroke, heart attack and dementia. Although homocysteine is not acutely toxic, it is just not healthy to have elevated levels over a long period of time.
Supplementing Betaine With Glycocyamine
The study showed that superphysiological dosages of glycocyamine, in effect, deplete the liver of methyl groups and vastly increase the blood concentration of homocysteine. Once I realized the implications of this, I set out to find a way to provide the liver with more methyl groups so that homocysteine would be adequately detoxified as well as making more efficient the glycocyamine to creatine conversion. After much research and experimentation, supplementing the diet with betaine stood out as the single best way to provide the body with an abundance of methyl groups.
Betaine is also known as trimethylglycine. Trimethylglycine is efficiently metabolized into dimethylglycine and dimethylglycine is efficiently metabolized into monomethylglycine. Each of the above demethylation reactions frees up a methyl group to be used by the body. At first, we thought a 1:1 ratio of betaine to glycocyamine would be sufficient. However, after a year of experimentation, we realized that a 4:1 ratio is optimal.
* This is where I must issue my warning. If you take glycocyamine in any dosage, it is imperative to also take at least 4 times the amount of betaine.
I must also point out that over the last several months I have read numerous articles on glycocyamine touting its many benefits. The articles went on to recommend taking 3-5 grams of glycocyamine per day. Amazingly, there was not even one mention of the use of betaine. Believe it or not, these articles were written by PhD's. How could someone that is considered an expert of experts nonchalantly recommend the usage of a compound in high dosages without even having the slightest degree of understanding of how the compound works or its safety profile? Unbelievable! There are several products currently on the market that include glycocyamine. My strong recommendation is to not take any product that does not specifically contain 4 times as much betaine as glycocyamine.
What I want everyone to take away from this article is that glycocyamine is an amazing new nutrient that can offer great benefits to both creatine responders and nonresponders alike. It is a compound that everyone should consider adding to his or her supplementation program. An optimal dosage is 1 gram per day. The only caveat: use betaine and make sure its dosage is 4 times the amount of glycocyamine.