Creatine

Creatine The Wonder Supplement Author: Andrew Langhorn 18/12/2004

Not long ago I did a large study on numerous forms of creatine and was recently reading through all of the research and found that I had forgotten much of the amazing benefits of this wonder supplement. I have decided to scoop all of my research together for you here to have a look through and become dazzled at how perfect this supplement appears to be in the laboratory and in the real world.

WHAT IS CREATINE MONOHYDRATE?
Creatine Monohydrate (methylguanidine-acetic acid) is one of the leading supplements used in athletic enhancement. Widely recognized by athletes and amateurs alike, creatine is heralded as a highly effective, natural performance enhancer (an ergogenic). Creatine has grown in popularity since the early 90's, although being studied for many years prior to this, and has become a staple supplement for many athletes regarding it almost as an essential nutrient.

WHERE DOES CREATINE COME FROM?
Creatine is a natural dietary constituent of all animal food, and is produced and stored by our own bodies. Our liver and kidneys tends to synthesize creatine from the amino acids glycine, arginine, and methionine and so is not considered an essential nutrient however many numerous studies have shown supplemental creatine of doses higher than 2 grams a day can have profound effects on various types of physical performance. The physiological effects of supplemental creatine have been so widely studied and acknowledged in terms of athletic performance research has now turned its attention to the possible beneficial use of this substance in preventing losses of muscle and neural functioning during aging or with various neuromuscular diseases.

IS CREATINE NEW?
Creatine has been acknowledged as  a food constituent for over 150 years. The substance was discovered in 1832 by a French scientist named Michel Eugene Chevreul. Even as early as the start of the 20th century creatine had been shown to increase muscle content in animals. More recently the number of human studies show time and time again that creatine supplementation has a marked effect on performance. Being non-hormonal in it's action makes this supplement equally beneficial to women as well as men. It is estimated that in the 1996 Summer Olympics in Atlanta almost 80% of the athletes, both male and female, were using creatine, with this figure surely rising to this day. Creatine, as with all supplements, is perfectly safe in normal recommended dosages. There have been a few anecdotal reports suggesting creatine misuse could lead to some possible physical ailments such as dehydration, muscle cramping or even stress to the kidneys however these findings have never been proven nor are very common. Usually the bad press about many health supplement has come from misinformation or total false accusation. 

OUR BODY NATURALLY PRODUCES CREATINE
An average man weighing 70kg stores roughly 120g creatine in total around the entire body and turns over (uses and replaces) around 2g a day. It should be noted that a large quantity of this creatine pool is stored in muscle tissue and obviously the larger the muscle becomes the higher the creatine content becomes and daily requirements to replace used creatine from training. Creatine is stored within the body as about 30 - 40% free creatine and 60 - 70% phosphocreatine (creatine bound to phosphate). Consumption of creatine in an average diet from natural food sources may also vary quite widely. A strict vegetarian may receive absolutely zero creatine  and may replenish their creatine stores purely from endogenous synthesis by their own liver. Individuals whom consume a normal omnivorous diet, whose protein intake ranges between 1 and 2g per kilogram of bodyweight daily obtain around 0.25 - 1 g of creatine from their diet. If an individual drastically increased their protein intake every single day, ingesting 1 or more pounds of red meat or fish they could achieve maybe a 3 to 4g intake of dietary creatine. Beyond this, however, it would be very difficult and unlikely to increase intake much further.

ENHANCING CREATINE ABSORPTION
Creatine is an osmotically active substance; thus an increase in intracellular creatine concentration may induce water influx into the cell. This is often a very rewarding and beneficial aspect to athletes concerned with gaining muscle mass, size or strength. Creatine may be a signal to stimulate protein synthesis, possibly by this intracellular fluid retention and increasing osmotic pressure. It is important to note that creatine absorption can actually be enhanced and the benefits increased. There is evidence that creatine uptake into tissues may be mediated by insulin (a hormone related to food consumption and it's response/action to consuming nutrients). It has been shown that ingesting large quantities of carbohydrate (upto 95g) along with a supplemental dose of say 5g of creatine facilitated greater creatine uptake by the muscles than taking creatine alone. This response was apparently mediated by the glucose-stimulated release of insulin. In fact further enhancements of creatine absorption have recently been made with the use of insulin potentiating substances such as Alpha Lipoic Acid or D-Pinnitol. Making improvements to creatine absorption is becoming common knowledge and there are many pre made creatine transport systems now available.

ATP - WHAT IS IT?
All cells use ATP (adenosine triphosphate) as the immediate energy source, but since ATP stores are limited they must be regenerated by other metabolic processes in the cells in order to sustain high muscle output. The classic hypothesis suggests that muscle fatigue is caused by failure of the energetic processes to generate ATP at a sufficient rate. Energy is liberated from the ATP molecule as the phosphate from ATP is removed by an ATPase enzyme leaving adenosine diphosphate (ADP) and inorganic phosphate (Pi). Collectively the ATP and Phosphocreatine (PCr) energy sources are known as the phosphagen energy system. During very high intensity exercise the phosphate from the phosphocreatine is cleaved off to provide energy for resynthesis of ATP. This allows the ATP pool to be turned over several dozen times during all-out maximal-effort exercise. From an ergogenic (performance enhancing) viewpoint, resynthesis of Phosphocreatine could be the critical factor during sustained very high intensity exercise. Further it is worth noting phosphocreatine (the primary stored form of creatine in muscle tissue) has a role in helping to buffer H+, increasing the cells capacity to attenuate the decline of pH levels during intense exercise and may help delay fatigue. This is as we know the burning sensation when lactic acid floods the muscle and causes us to cease exercise. Theoretically the phosphagen, or ATP-PCr, energy system is capable of providing energy for only a few muscle contractions before being depleted. Since PCr is the substrate for this system, it is logical to hypothesize that creatine supplementation is a possible ergogenic strategy to rapidly replenish PCr and enhance performance tasks less than or equal to 30 sec in duration.

BENEFITS FROM CREATINE SUPPLEMENTATION
Creatine may also enhance training in other ways. Increased creatine or PCr may enable athletes to reach a higher training load, improve repetitive interval sprint capacity, reduce training fatigue and possibly enhance muscle hypertrophy - all factors that may enhance competitive performance. Creatine also increases fat free body mass (muscle) which is extremely beneficial in sports requiring a high power output to resist the inertia of another body (e.g. weight training).

HOW DO I USE CREATINE?
Creatine supplementation protocols involve a loading and maintenance phase. The most commonly used research protocol for creatine loading is to ingest a daily total of 20 - 30g of creatine, usually creatine monohydrate, in four equal doses of 5-7g dissolved in about 250 ml of fluid, over the course of the day (usually early morning, noon, afternoon and evening) for a period of 5 to 7 days. When powder is used some recommend warm or hot fluids for better dissolution o creatine. Based on body weight the recommended loading dose is 0.3g/kg body mass per day for a period of 5 to 6 days. A more prolonged loading protocol of 3g/day for 28 days is just as effective as the short term loading protocol. After the creatine loading phase the recommended maintenance dosage is considerably lower, approximately 2 - 5g of creatine per day or 0.03g/kg body mass per day. After ingestion of 5g of creatine, levels in the blood peak during the first hour and then begin to dissipate during the next several hours. To help maintain peak plasma levels it is recommended to ingest 5g doses every few hours or around 4 to 5 times a day during the loading phase, however, it should be noted that several studies have shown no extra benefit from supplementing any higher than 20g a day.

Creatine has also been widely used with caffeine, which often comes as a surprise to many people. Caffeine is however a strong ergogenic aid in its own right. The adrenergenic effects of caffeine may elicit a variety of cellular responses - one being an increased sodium/potassium ATPase pump activity in the muscle cell membrane, an effect theorized to enhance creatine uptake into the muscle. Several studies have shown creatine mixed with caffeine (5mg/kg/day) has indeed increased the muscle uptake of creatine by upto 15%. However caffeine may interfere slightly with the rate of muscle PCr resynthesis during intermittent exercise. 

Creatine is excreted normally by the body by diffusion in the kidneys into the waste product creatinine. This catabolism of creatine is a fairly slow process. It is estimated that elevated muscle creatine stores will return to normal, declining slowly, over a period of around 4 weeks. This is because daily creatine turnover is only a maximum of about 2g a day. 

CREATINE INTOLERANCE
It is interesting to note that there are individuals whom have limited results with just creatine supplementation alone. Usually supplementing with creatine causes a marked 20% increase in TCr content of muscles, however, there does seem to be a few individuals, around 20 - 30% of the population, whom do not respond as well to usual creatine loading - only achieving around 8% TCr increase. It is interesting to note that this biochemical/genetic individuality is generally resolved when using a creatine/glucose combination.

CREATINE SCARES
There have, as mentioned, earlier been a few unsupported scares regarding the use of creatine monohydrate supplementation. As already mentioned most of these studies have been either totally misguided or explainable to some sensible degree. However, when purchasing your creatine supplement you want to be totally assured of the purity and quality of what you are placing in your body. It is worth noting that many suppliers of creatine do not independently test their product nor do they use a reputable source of high quality creatine such as Creapure - from SKW in Germany - the worlds leading supplier of highest quality Creapure. A product containing high quality creatine will be marked as either containing such a high quality creatine, or if you write to the company they should provide you with the information you require and whom they use as their creatine supplier. Buying cheaper creatine, or one not to high standards, may contain any or all of the following toxins:-

  • Dicyandiamide - a derivative used in the production of fertilizers, explosives, fire proofing etc. This substance breaks down into cyanide gas when exposed to strong acid such as stomach acid.

  • Creatinine - as mentioned earlier a byproduct of creatine metabolism with absolutely no ergogenic value. Also linked to increased colon cancer incidence.

  • Dihydrotriazine - not enough research provided on the toxic effects of this substance.

  • Sodium - aside from the obvious health implications, people surely don't want to be spending the amount of money they are on creatine to find such a high level of sodium in poor quality creatine products.

Obviously when you are loading on a creatine product you surely don't want to be dumping high levels of these toxins into your system and so it is always worth spending that little bit extra on a reputable brand clearly labeling their creatine.

 

Enhancing Creatine Absorption Further

Creatine supplementation is a successful supplement for most individuals in its monohydrate form or one of the transport systems. Expect gains in energy, strength and muscle size from creatine use. These benefits will continue for as long as creatine is used and around four weeks after cessation of use. Gains in lean body weight from enhanced strength and possibly enhanced protein synthesis can be retained when coming off creatine. Useful mainly in sports related to short bursts of high intensity exercise such as weight training and sprinting. Beneficial to endurance athletes also, so long as the body weight gain does not hinder increased performance. Variation with dosage normally reveals a beneficial optimum.

Creatine transport systems have been developed and improved upon over the years as a system to force feed maximal amounts of creatine into the muscle cell and minimize wastage. Using creatine monohydrate alone can sometimes only result in maximum of 50% absorption of the product. Using a transport system as either a full cycle tool for improved benefits or even just as a loader for the first 5 - 6 days of creatine use generally results in enhanced results and further benefits. Also useful for the small percentage of the population whom appear unable to reap benefits from creatine used on it's own.

There are quite a few various formulas out on the market today with various added ingredients. The basic aim of these ingredients are to firstly improve the action of the anabolic hormone insulin. For detailed information about this hormone and it's action see the section Insulin. Simply put this hormone is the key to taking nutrients places in the body and storing them. The better and more efficient your insulin and the stability of it will shuttle much more nutrient into the muscle cell including creatine thus the transport systems are concerned initially with getting more of the substance into the cell where it can do it's work. For this reason transport systems often, but not always, contain high amounts of carbohydrates, especially in a simple form such as dextrose. It is important to note that these products should be avoided when trying to diet or concerns where high sugar diets may be a high risk to performance, e.g. diabetes or Ketogenic Diets (Lipolytic-Ketosis). Very shortly we will be seeing the increasing popularity of transport systems with much lower, if not zero carbohydrates in them. Next a transport system may be involved with including ingredients of a synergistic nature. It is well known that creatine has a energy increasing potential and a cell volumising potential. Both factors involved in and vital to the process of muscle growth and repair from exercise. In this instance other cell volumising nutrients may be added or energy producing nutrients to back up the function of creatine further. Finally the transport system is an aid to good intestinal absorption - another area where creatine monohydrate alone may come into trouble. It is vital that the correct environment is provided in the stomach to enhance uptake and fast assimilation by the body.

As each product varies here is a list of what ingredients may actually be included in many formulas.


As mentioned earlier there are a number of various techniques now employed to enhance the uptake of creatine by the muscle. Primarily these techniques involve enhancing the action of the highly anabolic hormone insulin. Many companies now see the added benefits of these techniques and so have brought to the market pre-mixed creatine transport systems (see creatine transport systems).

Creating your own transport system can sometimes prove expensive but still favoured by many. Here are a few things that you can do to increase you creatine absorption especially during the loading phase.

  • Add your creatine to around 75 - 100g of carbohydrate. A mixture of dextrose primarily for high insulin output, maltodextrin, second, for sustained energy. A little fructose for liver glycogen.

  • Add taurine to the mix. Around 1 gram has an added cell volumising effect much the same as creatine has in drawing fluid into the muscle.

  • Add phosphate to the formula to enhance the lactate buffering creating a more favourable pH balance decreasing the onset of muscular fatigue. This can also help lower the acidity of the stomach, improving absorption and causing less waste of creatine being converted into creatinine before even being used.

  • A number of antioxidants such as Vitamin C and E would be of benefit to help deal with the waste byproducts of intense training which could adversely affect performance.

  • Glutamine could also be added in a dose of between 5 - 10g as a secondary cell volumiser, again enhancing the size gains caused by creatine. Glutamine is also the primary amino acid which makes up around 70% of human skeletal muscle tissue and is vital to muscle repair and growth. Adding glutamine in this way can seriously improve recovery rate and reduce muscle soreness dramatically.

  • Several insulin priming nutrients would be of benefit. Chromium Picolinate (around 200 mcg) enhances the action of insulin making it much more stable and better at its job. Vanadyl Sulphate (around 15 mg) has also had plenty of research showing it's insulin mimicking properties and ability to literally force feed muscles with nutrients including creatine. Alpha Lipoic Acid, a strong anti oxidant also with insulin improving properties, would be an excellent choice at a dose of around 200 - 300 mg. Finally new research is showing D-Pinnitol would be a worthy addition. 

  • Adding the primary amino acids of creatine synthesis may be beneficial, especially to cell hydration, methionine, arginine and glycine.

  • It is possible that albion chelated magnesium may also enhance the absorption of creatine by around 100% and uptake by the muscle cells of around 200%.

  • Taking your creatine mixed formula in a warm (preferably not hot, nor cold) liquid would be ideal. Stomach emptying is much better at body temperature, when taking a drink cold, 1st your body must increase the liquids temperature while the creatine does not dissolve properly. Taking a liquid too hot could easily damage the creatine and force the stomach to first cool the temperature of the beverage down. 

  • As noted earlier caffeine may exert a beneficial addition to the creatine mix, as apposed to common belief, so long as daily you keep well hydrated. It would therefore be an idea to add 200mg caffeine tablets to your intake of creatine or simply a good cup of regular hot coffee either before or straight after your creatine. Some people even mix their powder straight into the coffee once it has begun to cool.

  •  
    • Ribose - see the section dedicated primarily to this nutrient. Suffice to say this adds a lot to a hard trainers recovery rate and is involved extensively in the manufacture of ATP.

    • HMB - Hydroxy Methyl Butyrate another very popular supplement with a very different action to creatine. Used highly successfully on it's own HMB does not actually need to be added to creatine but can have a double punch effect, so to speak, when combined together.

    • TMG - Tri Methyl Glycine usually added to a transport system with a lot of glutamine added but is also becoming much more popular in it's own right. Used as a nutrient to cleanse the blood of toxic ammonia this nutrient has also been shown to have growth enhancing properties all of it's own.

    • Ginseng - and other energy providing adaptogens. Added mainly to enhance the energy boosting properties of the creatine formula.

    • L - Carnitine is often added as an energy booster. Also an aid to fat loss as this nutrient causes stored body fat to be broken down and used to fuel the mitochondria of every cell to provide energy.

    • Effervescent formulas are also gaining popularity. All as a possible aid to further enhance stomach absorption and surface of the stomach lining for greater uptake.

    • 2 - Hydroxy - 1,2,3 - Propanetricarboxylic Acid assists the breakdown of carbohydrates to the molecular level for immediate cellular absorption and also bonds with creatine allowing it to transport in liquid form.

    • Sodium Hydrogen Carbonate - essential for maintaining osmotic equilibrium (cellular fluid levels)

     Tri-Creatine Malate
    While we know that things such as creatine and other items help with weight and muscle gain when combined with a smart lifting and eating program, the combination of Kreb cycle and metabolic intermediates citrulline and malate may have been overlooked by many in the sport supplement world.

    A recent study found that supplementing citrulline and malate (six grams total per day) over a 15-day period reduced muscle fatigue, increased energy production (ATP) by 34%, and caused a 20% increase in phosphocreatine recovery after exercise. Simply put, this means that at least in this one study, the citrulline-malate supplement improved aerobic metabolism, enhanced cellular energy production, and induced an enhanced state of muscular recovery.

    More studies are needed, but this citrulline/malate combination just might be the next generation in effective, natural sports supplements.

    "The New and Improved Creatine" goes over all the newest forms of creatine and creatine delivery systems on the market, such as creatine citrate, phosphate, malate, tartrate, and anhydrous. Of course, though they are all pricier than basic creatine monohydrate, there’s not a lick of evidence to prove they are any more effective.

    The ultimate creatine molecule that is water soluble. Tri-Creatine Malate comprises of molecular bonded Creatine and Malic acid. The bond is broken in stomach acid to release pure Creatine(not creatine monohydrate) and Malic acid. Both of which are then immediately absorbed through the intestine. The beauty of this stunning new Creatine salt is the fact that it contains Malic acid. Malic acid supports energy production. Furthermore, Malic acid acts as a catalyst to the Krebs cycle where fats and glucose are converted into energy. All of this makes for a far more powerful energy supplement to your diet in a superior stable format.

In Summary
Creatine supplementation is a successful supplement for most individuals in its monohydrate form or one of the transport systems.

Expect gains in energy, strength and muscle size from creatine use. These benefits will continue for as long as creatine is used and around four weeks after cessation of use.

Gains in lean body weight from enhanced strength and possibly enhanced protein synthesis can be retained when coming off creatine.

Useful mainly in sports related to short bursts of high intensity exercise such as weight training and sprinting. Beneficial to endurance athletes also, so long as the body weight gain does not hinder increased performance. Variation with dosage normally reveals a beneficial optimum.

Possible side effects to note are dehydration and muscle cramping. Resolve by increasing water intake daily.

 



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