Creatine is a nitrogenic compound naturally manufactured in the liver from the three amino acids Methionine, Arginine, and Glycine and is transported to the muscles via the circulatory system. Creatine is transformed into phosphocreatine and is stored in the muscle. (Also called Creatine Phosphate or CP) The conversion of Creatine to C.P. is aided by the enzyme Creatine Kinase (CK) in bonding the Creatine to a high energy phosphate group. Once C.P. is stored in a cell, it remains until it is used as a high energy source called Adenosine Triphosphate (ATP). Normally the body produces about 1-2 grams of Creatine daily, and of course, metabolizes about 2 grams daily also. The average person stores over 100 grams of Creatine in muscle tissue and in the liver. When C.P. is utilized in natural ATP regeneration, one of the by-products is called Creatinine which is then removed by the kidneys and eliminated in urine. Since Creatinine levels are checked as an indicator of proper kidney function (and as a stress indicator for the heart) one might assume supplemental Creatine would place undue stress on the kidneys. This just is not the case. In fact, a 5 year study showed no negative side effects from continuous Creatine supplementation. Pretty cool, huh? Creatine is also absorbed form animal and fish protein. In fact, I pound of red meat contains about 2 grams. Loading phases (contrary to the belief of some half-experts) are very important to bodybuilders and strength athletes when using any supplemental creatine product.
The goal is to raise muscle creatine concentrations to a supraphysiological level as quickly as possible. If the creatine product is simply ingested at a daily so-called maintenance dosage the result will be an action/reaction type response in which the body downregulates CP storage enzyme secretion thus limiting the actual possible muscle cell CP hyper-concentration (total muscle cell CP content). Since ATP is the basis of all growth, and CP is the basis of ATP regeneration, does the elimination of a loading-phase seem maximum progress goal oriented? This increases nitrogen retention and creates an osmotic effect within muscle cells. You have often read about cell volumization in every creatine ad. If a bodybuilder is using creatine stores as fast as they come in, how can a supraphysiological (above normal concentration) saturation exist? Duh! Load first. All AAS increase nitrogen retention and testosterone tends to notably create an even greater osmotic effect. Both facets increase protein synthesis and strength.
Nitrogen retention is anabolic simply because amino acids are not exiting muscle cells. They therefore are available for repair and growth instead of exiting or becoming an energy source. Osmotic reactions simply mean there is an elevated level of intracellular nutrients, including water, available. The way an osmotic response effects or induces an elevation in strength is basic physics. Try benching on a waterbed. (No, I mean weights) There is little in the way of structural integrity. Now, if you filled that waterbed with much more water, thus creating a firmer structure, the ability of it and you to support and leverage a higher weight load will improve. The osmotic effect is not simply water retention. It is an increase intracellularly (inside muscle cells) of growth nutrients, including C.P., for increased cellular repair and growth. If it were outside of the cells, you would be very smooth, but this is not the case. Strength increases from proper Creatine supplementation range from 5-10% and body weight increases (over a 2 month cycle) range from 3-10%. This means a bodybuilder that weighs 200 LBS and bench presses 200 LBS for 10 reps max can realistically expect to weigh 206-220 LBS and bench press 210-220 LBS for 10 reps by the end of a 2 month cycle. Results from any following Creatine cycles tend not to be as impressive as first time cycles. Unfortunately about 20% of Creatine users do not respond to Creatine.
This is usually due to an inability to get the Creatine into muscle cells. But there is a solution.….Read on. CREATINE SUPPLEMENTS Creatine Monohydrate (CM) This is the most common form of Creatine in the supplement industry. CM contains about 850-880 MG of free Creatine per 1000 MG of weight. When loading on C.M., daily intake will total .3 grams per kilo of bodyweight (a 220 LB bodybuilder would need 30 G per day for 5 days -100 KG x 0.3 =30 G) divided into 3-5 daily dosages, followed by a daily maintenance dosage of 5-15 GMS. C.M. dissolves much better in warn water and about 16 OZ per 5 GMS is a must. Simple fact is if it does not dissolve, it does not absorb. Undissolved C.M. crystals tend to cause intestinal irritations, and in some cases, the runs. This is due to the body’s need to flood the intestinal tract with excess water to flush out the irritant. Try that on a heavy squat day! The highest purity is a must when buying creatine products. Many brands utilize SKW Creatine (now Tracolabs), which is manufactured in Germany. When tested by HPLC (high pressure liquid chromatography) method, SKW creatine usually ranges between 99.5-99.8% pure Creatine Monohydrate. The by-product content is usually Dieyandiamide-20ppm, Creatinine-50 ppm, and Dihydrotriazine-n.d. (none detected). Ppm stands for parts per million.
USA produced Creatine normally ranges in purity from 80-95% pure Creatine with by-product contents of Dicyandianmide 300-400-ppm, Creatinine 190-2500-ppm, and Dihydroltriazinde 90-410-ppm. Don’t even think about China’s Nanjing or Jeangsu produced Creatine. Purity ranges from 50-70% pure Creatine with other interesting things. Look for the Creapure R registered trade mark on Creatine Products. It means SKW manufactured Creatine. There are other forms of Creatine. Creatine Citrate is very water soluble but requires twice the amount to equal the same amount of Creatine Monohydrate. Creatine Phosphate is another option but cost to effectiveness makes the product less effective than Creatine Monohydrate. Many people have tried the second generation creatine products. These are products containing other nutrients to increase muscle cell absorption of C.P. There is a direct correlation between the amount of Creatine absorbed (not merely ingested) and results. At one time, the market was flooded with products containing Dextrose (glucose) and Creatine. They did improve cellular absorption to some extent. The reason is Insulin. (Yes, go back and read the whole section on Insulin again) Okay, Insulin is a storage hormone.
When the body senses excess blood sugar (Glucose), the pancreas releases Insulin to force it into cells including muscle tissue. So by utilizing a high glycemic carb such as Dextrose, an Insulin spike is created and more carbs and amino acids enter cells. Oh, did I mention Creatine is an amino acid? The idea helped, but the problem is timing. After ingesting Creatine, blood circulatory levels peak at about 90 minutes. So what? After ingesting Dextrose, circulatory levels peak and cause an Insulin spike after about 30 minutes, and is on the down side when the peak levels of Creatine arrive. The third generation of Creatine products employed natural Insulin optimizers (they make Insulin receptors more sensitive in muscle tissue) and mimickers. The first real break through was the Insulin mimicker… ALFA LIPOIC ACID. Alfa Lipoic Acid? Without writing an ad for anybody, let me simply say that Lipoic Acid increases receptor site sensitivity while also mimicking Insulin’s actions. Though my choice for micro-nutrient of the year award for maximum creatine transport without an increase in bodyfat synthesis would be 4-hydroxy- Isoleucine. Major potential here! For Creatine supplementation to result in an increase in strength and protein synthesis, the cellular concentration level must reach 20 MMOL/KG DM. During a 5 day loading periods with a high glycemic carbohydrate such as Dextrose and Creatine, the level reaches MMOL/KG DM.
When Creatine levels increase in muscle cells, the active Creatine transporters are down-regulated, so less Creatine is transported. This could be avoided if the Creatine is fortified with the Creatine substrate 3-guanidinopropionate. Second, Creatine cannot be diffused across the muscle cell membrane without the cotransports of sodium and chloride ions to cause enough electrical charge to transport the Creatine. (Table salt) Other up-regulators of Creatine transport are Clenbuterol and Ephedrine as well as T-3 thyroid hormone. These are quite potent transporters to say the least. Of course, Insulin (Humulin) and IGF-1 are very effective Creatine transporters. Though Dextrose is an excellent trigger for Insulin release there is a higher glycemic carbohydrate. Malt extracts contain a mixture of maltodextrins, glucose, and dextrose which are made of glucose chains of 3-7 gycosyl units. And guess what? The small intestines absorb glucose chains containing 3-7 gycosyl units much faster than dextrose. This means a higher and stronger Insulin spike. So barley malt extract or maltodextrin is a better carb choice and can be utilized in lower levels than 75 GMs per dose. Whey protein also creates an Insulin spike which can prolong the spike from high glycemic carbs. By the way, caffeine intake over 400 MG daily, as well as the isoflavone genistein in soy protein inhibit creatine transport. Genistein inhibits tyrosine kinases which is necessary for nutrient transport. The body has 3 periods when creatine uptake is highest: After a nights sleep, the body is in a fasted stated due to a period of natural GH pulses (about half of your daily total GH production is released during the first 4 hours of sleep) and a prolonged period without nutrients. This results in an up-regulation of nutrient transporters and enzymes which favor intramuscular uptake of nutrients, including Creatine.
When Creatine is ingested 45-90 minutes before a work-out, an athlete can take advantage of the training induced increases in blood flow to muscle tissue to transport essential nutrients across muscle cell membranes. (This also acts as a buffer to lactic acid) Since high intensity work-outs trigger the release of adrenal hormones such as Epinephrine and Norepinephrine, the cellular uptake of nutrients is improved. Remember, Ephedrine increases cellular uptake? Well Ephedrine is an Epinephrine Mimicker. Within the first 45-90 minutes following an intense work-out, the body is in a very nutrient receptive state. Heavy training reduces muscle glycogen stores (glycogen comes from blood sugars such as carbs) and receptor-sites for nutrients become sensitive. This means the body is in a catabolic state requiring nutrient supply. Several storage enzymes are up- regulated and creatine (CP) levels are lower which of course means intramuscular nutrient storage ability is at a high level. It also means the muscle cells need ATP regeneration.
So what was the best Creatine mixture currently available?
16-32 OZ of water 300 MG of Lipoic Acid and/or 50 MG of D-Pinitol
5-10 G of Creatine A source of 3-guanidinopropionate
250-500 MG of salt 4-25 G of Glutamine
50 G of Malt Extract 30 G-50 G of whey protein
25 MG of Ephedrine 1 MG of Triacana
CREATINE AND MUSCLE HYPERPLASIA How many times have you heard some gym supplement expert say that the weight gained from creatine is just water? Well, researchers wrote an interesting paper concerning creatine called: Dangott, B. Schulz, E. Mozdziak, P.E. “Dietary Creatine Monohydrate supplementation increases satellite cell mitotic activity during compensatory hypertrophy” in International Journal of Sports Medicine 21:13-16,2000. What the heck is that, huh? Satellite-cells are the “stem cells” of skeletal muscle which the body utilizes to produce or add new cells and fibers to existing cells. This means satellite-cells are used to: (1) Repair damaged muscle fibers from training (2) To add cells to existing fibers to make them larger (3) To form new muscle fibers through an action called muscle fiber hyperplasia. These researchers cut off the soleus and gastrocnemius (calve) muscle on a bunch of rats, then split them into two groups. One group received a creatine/glucose/water mixture and the other did not.
Then they exercised the poor rodents in a manner that the plantaris leg muscles had to compensate for the missing calve muscles. In both groups, the plantaris showed significant hypertrophy (growth). But the creatine/dextrose supplemental group showed much higher satellite-cell activity. In simple terms, the creatine appears to have increased hyperplasia and total muscle cell numbers. So what? Okay, go read “Growth Hormone” and come back. So, this supports idea that Creatine Supplementation increased the actual muscle mass on a very important level. More cells, more fibers, bigger muscles. If you have been reading so far with a close eye upon anabolism (muscle growth) you will already realize the connection between CP, ATP, Anabolic/Androgenic steroids, Growth Hormone, Insulin, thyroid hormones, IGF-1, prohormones, and Creatine.
Each is tied to the other by the actions of ATP and cellular CP levels. When a bodybuilder does a heavy set, intracellular ATP levels decrease. (Remember, muscle contractions depend on available ATP) As the work-out continues, ATP is further depleted. Another adaptive response to training is the up-regulation of androgen receptors. Simply stated, for several hours after training, your muscle cells have more androgen receptors than they did before training. This allows a greater amount of androgens, (whether naturally produced endogenously, or provided from exogenous sources such as steroids and prohormones) to enter the cell and signal anabolism. Unfortunately due to depleted ATP levels, the cell lacks the “energy” to do its thing. This results in low anabolism, or at least much less than would occur with higher ATP stores.
This in part explains why Methyltestosterone and Oxandrolone made any reported AAS cycle much more effective. Methyltestosterone increases 3-guanidinopropionate and Oxandrolone increases CP synthesis. Another example is GH and IGF-1. When GH finds a GH receptor-site on a muscle cell, it triggers IGF-1 release within the cell (or from the liver if the GH activates IGF-1 production there) and a high level of anabolism results. But not if ATP/CP levels are low. This is one of the reasons why, during dieting, it is difficult to increase muscle anabolism. GH works anabolically, only with high calories because high calories increase ATP production, and anabolism depends on ATP for an energy source. Anabolism is hard work.
Again, this is why most anabolic/androgenic steroids work only in an environment of high calories. Every muscle fiber contains satellite-cells just waiting to join the fibers so the fibers can grow thicker and stronger. More cells, more fibers and thicker fibers, means more cell/fibers to grow. Creatine Monohydrate is an exogenous source of CP which increases ATP production. I have noted that dieting bodybuilders not using Creatine lose bodyweight more quickly. Yet they also lose much more lean muscle mass as well. Those who used a T-3 thyroid hormone also had higher creatine stores, and those using Creatine supplementation with T-3 had the highest creatine stores. I have also noted that those using a fast acting glycemic carb, whey protein, creatine drink only after training and during diet phases lost more bodyfat yet actually gained lean muscle mass. Those who used the mixture of whey, Creatine, D-Pinitol, Triacana, Ephedrine, and Maltodextrin, looked much harder and fuller. So what do you think of Creatine now? There are several good creatine forms such as effervescent and those providing transporters and Insulin mimickers. But this is a book about hormones.