Creatine – All You Need To Know

WHAT IS CREATINE?1

Creatine is a naturally occurring compound that our body is capable of producing in the liver. It is present in diet of people who eat meat (e.g. red meat and oily fish). However, creatine is degraded during cooking because of its heat labile nature. It is stored in the major muscles including cardiac and skeletal tissues. Creatine provides quick energy to muscle as needed. It maintains high level of ATP/ADP ratio in muscle. ATP is the energy molecule in the body that is used for muscle contraction. Our muscles have a small pool of ATP that is generated during rest so that it can be used by the body during activity. Thus, a quick way to replenish ATP in the muscles is by utilizing Creatine Phosphate that is present in the cells.

Other names with which creatine is known:

alpha-methylguanidinoacetic acid

creatine monohydrate

creatine 2-oxopropanoate.

Creatine Vs Creatinine 

Creatine should not be confused with Creatinine. It is a metabolite of creatine.  Cyclocreatine or creatinol o-phosphate is analogues (only resemble in structure) of Cr.

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BENEFITS OF CREATINE

 

According to the International Society of Sport Nutrition, creatine monohydrate is currently the most effective supplement for increasing anaerobic capacity and lean body mass. It is an optimal choice for athletes and people who

  • want to improve their performance in sports, exercise and gaining lean body mass.
  • There is plethora of literature and evidence that shows that it provides advantage in intense weight workouts or high impact sports.
  • It aids in quick recovery of muscle and allows for the person to push harder.
  • It has also shown benefits in activities requiring short bursts of energy like sprinting, football, rugby and so on.
  • Furthermore, it increases the lean body mass and improves body composition in people doing resistance training.
  • It has been shown to effectively prevent the lower limb degradation and a decrease in muscle power in elite soccer players.

The most popular reasons for use of creatine are:

  • to recover from training or physical activity
  • to improve physical performance
  • to prepare for a period of training or physical activity
  • to supplement the diet
  • There has been one recent report of use of creatine even in UK-based British Army soldiers under training (SuTs) and associated staff.

The bottom line is that it increases muscle mass by providing bursts of energy when needed, especially during resistance training and sprinting. People can lift more and thus add muscle mass quickly. This in turn helps in sports like swimming, rugby, football, tennis, soccer etc. Cr does not increase endurance, however if you have enough muscle mass, you are able to train harder thus do better at sports.

BENEFITS BASED ON SPECIFIC CASES

 

Role of Creatine in muscle disorders and myopathies

In the past decade, numbers of controlled studies have been done to explore more benefits of creatine, which include:

    • Creatine has been shown to be involved in myopathies, increasing testosterone levels and improved neurological performance.
    • Role of creatine in muscle disorders: Cochran review (2007, 2009, 2011) evaluated the role of creatine treatment in muscle disorders. Evidence from randomized control trials (RCTs) showed the creatine increased muscle strength in muscular dystrophies and idiopathic inflammatory myopathy. However, high dose creatine treatment in McArdle disease impaired daily living activities and muscle pain was increased.
    • A recent study also showed that creatine regulates the formation of bone and muscle by controlling the differentiation of mesenchymal stem cells (MSCs). In addition, creatine inhibits the accumulation of fat and might have value in obesity related disorders .

Role of Creatine in Elderly

As we all know, getting older is not easy. With age our bone density and muscle strength decreases. Maintaining strength and muscle mass is very important for healthy aging. Brose et al (2003) showed that creatine monohydrate when supplemented along with resistance exercise training even in the elderly, increased the total and fat free mass, and they gained isometric muscle strength. Even results from meta analysis support the role of creatine in increasing muscle mass, strength and functionality when used along with resistance training thus leading to healthy aging.

Therefore, older people will benefit from CR supplementation provided they add resistance training to their regimen.

SHOULD WOMEN USE CREATINE?

The most asked and wondered question is should women use creatine. The shortest answer is YES. The creatine metabolism remains same in men, women and elderly. Women fear that using creatine will make them gain weight or make them big. As explained above, creatine acts by delivering water molecule to the skeletal muscle thus expanding the muscles so harder training can be done. Therefore, in the beginning as with any resistance workout or gaining muscle in the body, there is increase in weight but this kind of weight gain is not an indicator of lack of fitness. Muscle weighs more than fat. Therefore, gaining weight for a first few months when you start training and using creatine only means you are adding muscle mass to your body, which is the good weight gain.

A recent double blind study showed creatine supplementation combined with resistance training improved lean mass and muscle function in women.

Again, even for women the gain of muscle mass would depend how hard they are training and of course their diet. Creatine has benefits even to women in training harder and thus gain strength for sports like tennis and swimming. In general Cr will aid in making them more fit.

Furthermore, CR supplementation has been shown to be beneficial in women with knee osteoarthritis. Literature shows creatine improves physical function and lower limb lean mass, thus improving the quality of life in postmenopausal women with knee osteoarthirits. Creatine helps them with strengthening exercises.

 

Creatine is specially recommended for postmenopausal women:

CR supplementation for 12 months in postmenopausal women along with resistance training showed an increase in bone strength. With menopause, estrogen decreases that leads to a decrease of calcium in the body thus affecting bone health. Therefore, CR supplementation along with resistance training will help gaining bone density and muscle mass. Creatinine did not present any side effects as assessed by clearance of creatine.

A recent study also showed that creatine regulates the formation of bone and muscle by controlling the differentiation of mesenchymal stem cells (MSCs). In addition, creatine inhibits the accumulation of fat and might have value in obesity related disorders.

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SIDE EFFECTS OF CREATINE SUPPLEMENTATION

 

So far there are no known side effects of creatine as long as it is taken as a supplement. As the name indicates, creatine is a supplement, so should only be added to a healthy diet and exercise regimen. A recent study on trained college athletes shows there were no detrimental effects on liver or kidney even in long-term use. Excess creatine would add stress to kidneys that could lead to health problems like kidney failure or irreversible acute and chronic renal failure.

In short, according to the International Society of Sports Nutrition and a few recent studies, the use of creatine as a supplement is safe and effective, when used within the established guidelines.

Will creatine cause bloating? According to the author’s own experience, microionized (micronized) creatine is best as it is very fine powder and the volume that needs to be ingested is very little.

Who should not take creatine and why?

  • Kids under 18yrs of age should avoid the use of creatine as they are still in growing phase and there is no telling how the use of creatine will impact the growing bones or the skeletal system in children.
  • As is self-explanatory pregnant or lactating women should not use CR supplementation at all since there have been no studies done on pregnant women and effect on fetus. And certainly there is no data to support any kind of effects on the baby as creatine will secrete through mother’s milk to the infant.
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HOW TO USE CREATINE

 

How to supplement creatine and its effect on muscle stores

There have been various methods of taking creatine to be effective in increasing creatine stores in muscle. This increase depends on the levels of creatine already present in the muscle before supplementation. People who have low muscle creatine stores (e.g. those who are vegetarian, vegan or eat little meat or fish), their muscle storage increases upto 20%-40%. However, those who already have high muscle stores of creatine, might only experience about 10%-20% increase. The degree of increase in creatine content in skeletal muscle is very important. Studies show that the performance changes are correlated to this increase .

Loading

This is the most described method in literature for supplementing creatine in the diet to gain muscle mass fast. This method involves taking approximately 0.3 grams creatine/Kg body weight/day of creatine monohydrate (CM) 4 times a day for 5-7 days. This is then reduced to 0.03 g /Kg body weight/day most commonly for 4-6 weeks.  A10-40% increase in muscle creatine and phosphocreatine (PCr) has been seen using this protocol. Alternately, a lower dose of 2-3g/day may also be utilized to increase stores slowly.

Cycling

This is another suggested supplementation protocol that does not involve ‘loading’. The protocol involves taking creatine 3g/d for 28days or 6g/ d for 12 weeks and it still leads to increase in muscle mass, size and strength. Cycling maintains and increases muscle creatine before drop to baseline values, which takes place at about 4-6 weeks. This protocol is as effective as loading though the increase is more gradual and the results are seen over a period of time.

In summary, loading is not necessary. In addition, the above doses written are based on literature where the studies were done with regular creatine monohydrate. Thus, the doses state as 3g or 5g of creatine. However, microionizedcreatine is a very fine powder and you do not need in grams. The instructions on the container are of using one scoop, which is very tiny. So those instructions need to be followed to avoid any side effects.

When should creatine be used: pre or post work out?

Looking at the creatine metabolism the best time to take creatine is an hour before workout. As explained, creatine provides burst of energy when needed by the muscles. Therefore, having adequate stores of creatine phosphate before resistance training will yield optimal results by making you lift more weights or train harder than you normally can. However, after workout it is recommended to rescue muscle with whey protein with added BCAAs. Creatine does not help in muscle recovery, it prevents muscle from breaking down by supplying energy molecule ATP.

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WHAT IS THE BEST CREATINE SUPPLEMENT TO TAKE

 

Creatine monohydrate remains the best possible creatine preparation with best absorption in the body, which is easy to take, and produces very little side effects like bloating and cramping.

Micronized (microionized) creatine has been passed through a mechanical process, which decreases the particle size of creatine and increases its water solubility. In regards to supplementation, it is the same as creatine monohydrate except it remains suspended in water longer and is easier to dissolve.

So in comparison to creatine monohydrate and micronized creatine monohydrate, micronized form is the best. It is cheap, easy to take, barely any side effects like bloating and is effective in the body.

All other forms in the market, do not offer any superior rewards over the basic creatine. They have been produced in an effort to get more benefit of creatine in the body like better absorption. However, in the end they are more expensive and not better than the basic creatine monohydrate.

There are different formulations of creatine available. It could be very confusing for the consumers to decide which one is best for them. Some of these creatines include

phosphocreatine

ß-hydroxy-ß-methylbutyrate (HMB) creatine

creatine + glutamine

creatine ethyl ester

Most of these formulations have been reported to be no better than the traditional creatine monohydrate (CM) in terms of benefits like performance and endurance. It has been shown that different creatine formulations might work differently in terms of kinetics but there were no differences in bioavailability since absorption of CM is close to 100% already. Thus, in terms of absorption or effects, CM seems to be the best option so far.

Three creatine formulations show promise but there is lack of evidence in their support in comparison to CM:

Creatine Phosphate

This has been shown to be as effective as CM alone in terms of strength and lean muscle mass,however, there is only one published study. In addition, this formulation is very expensive in contrast to CM.

Creatine/HMB:

showed promise but has conflicting data in regards to its efficacy than the CM alone.

Creatine+glycerol combination:

one study has shown this combination to increase the water retention in the body, a method that can be used for hyperhydration prior to exercise. Again, this is only one study and first of its kind, thus nothing can be confirmed at this point.

However, some recent studies show that the addition of ß-alanine to CM might produce better results (like higher lean mass, strength, and a greater delay in neuromuscular fatigue) than CM alone. It has been shown that addition of 93g of carbohydrate to 5g of CM significantly increased the muscle retention. On the other hand, 47g carbohydrate used in conjunction with 50g of protein with 5g CM produced the same results as with 96g of carbohydrate and 5g CM mix. This increase in muscle mass could be due to improved ability to accomplish high intensity training because of increase in phosphocreatine and ATP synthesis .

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RECOMMEENDED CREATINE MONOHYDRATE PRODUCTS

 

Following four products all use micronized creatine monohydrate, thus we recommend you to check their prices and quantity and choose the least expensive, or according to your own brand preference.

Creapure creatine monohydrate

Creapure Creatine Monohydrate is produced using a unique patented process (U.S. patent 5,719,319). Each batch is produced using Good Manufacturing Practices (GMPs) in an FDA-registered plant in Trostberg, Germany and is rigorously tested using state-of-the art techniques like high-pressure liquid chromatography (HPLC). It is unique since it has been purified to eliminate harmful impurities that are usually found in other creatines.

Note: Any creatine that is made from CreapureCreatine means that that creatine is microionized, which is superior to basic monohydrate form.

Optimum Nutrition Creatine Powder

Optimum Nutrition creatine is the most popular creatine on amazon and uses the same Creapure Creatine Monohydrate (micronized)

 

All Max Creatine

According to the manufacturer, All Max Creatine is pure Micronized Creatine Monohydrate (99.99%). The producers use the sole CreaMax technology to microparticulate this Creatine that leads to high absorption in the body. It is devoid on any fillers and is laboratory tested for verification.

 

Six star creatine

Again, the Six Star Creatine is pure Micronized Creatine Monohydrate powder without any fillers and should work the same.

 

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VIABLE ALTERNATIVES

Cell Tech Performance Series Hardgainer Creatine Formula for gaining muscle mass faster

This product is a scientifically engineered creatine formula designed for people who have trouble putting on size and strength. This product delivers faster muscle growth. It contains both the basic monohydrate form of creatine as well as the newer formulations like creatineHCl. 

According to the label, each two scoops of Cell-Tech delivers 7 grams of GPLC-certified creatine monohydrate and 3 grams of creatineHCl. It also contains 200mg of alpha lipoic acid (ALA). Theoretically, lipoic acid (a fatty acid) should make the formulation pass easily through the membranes to muscle.

According to the manufacturer, Hardgainer formula produces an insulin-spiked post-workout, as this creatine delivers multi-stage combination of carbohydrates. Theoretically, this is what makes creatine shuttled to muscle quickly, and the glycogen stores are replenished that allow supercompensation of glycogen thus producing a strong muscle-expanding effect. However, other than one abstract, there are no case studies supporting these facts, only customer reviews.Tarnopolskyet. al. 2001, have shown one study on the effect of this creatine on bench press, leg press and bicep curl. According to this study there was an increase on all these parameters by 17%, 29% and 28% respectively.

One clinical study (again an abstract) shows that no cycling might be required with this formulation as it did not down regulate the creatine transporters that will allow the athletes to use creatine without cycling on and off. However, theoretically it seems impossible because once transporters are loaded, they do get down regulated unless some additional transporters are being used. It is possible that presence of simple sugars and lipoic acid lead to the use of other transporters in addition to the usual creatine transporters. Real research studies need to be carried out to support these claims.

However, there might be one drawback of this form of Creatine due to the presence of large amounts of Vitamin C in this formula (more than 1000mg) Close et. al. 2006 have shown that 1000mg or more of vitamin C consumption leads to delayed recovery of muscle.

In short, this is a good supplement for people who have trouble gaining muscle mass. When using this particular creatine, try not to consume more than 1000mg Vitamin C 1h before and until 2h after workout.

 

Creacore Creatine for reduced bloating

CreaCore® is a very concentrated and creatineHCl powder. According to the manufacturer, it contains 1750mg of creatineHCl per scoop (2x more than other concentrated creatines). The super-concentrated formula requires no loading or cycling off, and does not cause bloating. This is the first formulation containing fenugreek extract that is believed to improve creatine transport to the muscle in a similar fashion to d-glucose (dextrose). Thus, CreacoreCreatine might be an effective creatine, which does not require ingestion of enormous amounts of carbohydrates.

 

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OTHER FORMULATIONS CURRENTLY NOT RECOMMENDED

 

based on lack of available evidence or conflicting data

Magnesium chelated creatine

What does chelation mean? Chelation is formation of multiple bonds between a central atom (in ionic form) and a ligand (in this case creatine). Chelation prevents the compound from being bonded with insoluble salts in the stomach, which can make the metal ineffective for absorption.

In this case, chelation of CRwith magnesium is again an attempt to have a product with better absorption of creatine and less breakdown into creatinine before reaching muscle. Theoretically, magnesium chelated creatine should be better than creatine monohydrate because of two reasons: (a) magnesium has an alkaline pH thus it could neutralize the stomach acids and prevent CR to be degraded in the stomach as in the case of creatine monohydrate (b) Magnesium plays an important role in a number of physiologic functions,especially in ATP synthesis in the body. As explained above, creatine does not provide the energy on its own. It’s the replenishing creatine that leads to regeneration of ATP that leads to the performance benefit.

The literature is conflicting in regards to whether Magnesium chelated creatine is superior than creatine monohydrate.

A couple of studies show that Magnesium chelated creatine leads to increase in muscle similar to creatine monohydrate without the water weight gain. Once again these studies are statistically insignificant. Thus, more research needs to be done for confirmation one way or the other.

However, magnesium chelated creatine is a good alternative for people who don’t see benefit with creatine monohydrate or have problems while dosing with it.

Available Products with Magnesium Chelated Cr:

 

Optimal Creatine by “Seeking Health”

Creatine ethyl ester (Creatine CEE)

Once again this is an attempt to produce a creatine that is better absorbed in the body and increases the muscle mass with few side effects.  The original idea was to bypass the creatine transporter by bonding ethyl ester to creatine. Yet again there is conflicting evidence as to its superiority. Another report suggests that it increased the muscle mass in comparison to monohydrate form, without increasing the water weight.

It may also result in higher serum creatinine levels due to creatine ethyl ester being converted into creatinine via non-enzymatic means in an environment similar to the digestive tract. Creatine ethyl ester rapidly degrades to creatinine in stomach acid.

Regardless of the contradictions, it seems CEE is the ineffective version of Creatine because it breakdowns rapidly in to creatinine in the intestine, despite its ability to diffuse passively through cell membranes. It is a pronutrientfor creatinine and not creatine. CEE is converted to CM by modifying an acid moiety through ester bond attachment. CEE is claimed to have a better solubility in lipids leading to higher absorption rates. However, in contrast to CM, CEE can be converted to creatinine in the gastrointestinal tract. Spillane et. al. (2009) have shown in a case study that serum creatine increased 1.5 fold in six days after ingestion of CM, barely with CEE. Nevertheless, after ingestion of CEE, creatinine leves in the plasma were tripled.

Creatine alpha ketoglutarate (Creatine AKG)

Theoretically, this formulation should be the highly superior form of Creatine, where CR is bound to AKG. Once again, there is no literature supporting an increased rate of absorption with Creatine AKG.

The major reason for binding creatine to AKG has been that AKG is an intermediate in Krebs Cycle or Citric Acid Cycle (TCA cycle). Krebs Cycle takes place in the mitochondria, and serves as the main source of cellular energy by generating high-energy phosphate compounds. An increase in mitochondria is found in cells that spend large amount of energy, e.g. muscle cells. Thus, AKG can act as a transporter of creatine to the targeted muscle cells.

Creatine Ethyl Ester AKG (CEE AKG)

Therefore, instead of using Creatine ethyl ester or creatine alpha ketoglutarate (AKG) alone, a next generation product is highly recommended that uses a combination of both ethyl ester and AKG. Again, there is no scientific studies/study supporting the claim of superior effect. From all the different formulations described above, it seems monohydrate is the basic form that does produce more muscle. However, other formulations are being made so the same effect or more is achieved faster with less degraded creatine to creatinine before being transported to muscle.

Ethyl Ester makes creatine “lipophilic” that means something that has affinity to fat (lipos). This CR theoretically should easily cross the membranes to reach muscle. However, as explained in the section 6 (CEE), the ethyl ester form breaks down easily into creatinine despite its superior absorption potential. At the same time as explained above, AKG can easily transport CR to muscle being an important member of Krebs Cycle. Therefore, it is possible that the presence of both ethyl ester and AKG does transport CR to muscle faster in its intact form.

Thus a super creatine formula ‘CEEAKG’ has been created in the hope of achieving superior results in short period of time and the recommened product is:

Available Products with CEE AKG:

 

Body Fortress Super Creatine CEE AKG

Creatine Nitrate

Cr Nitrate is a form of creatine where a Nitrate (NO3) group is bound to the creatine molecule. It has been shown that attaching nitrate to creatine significantly increases its solubility (˜ 10 fold) in water. Theoretically there is a possiblity that creatine nitrate would have faster increase in muscle because of the presence of creatine and nitrate which is present in some amino acids that lead to increase in muscle mass. However, there is no literature or experimental data supporting this. The only studies on this supplement are on its increased solubility in water.

Available Products with CEE AKG:

 

Cellucor C4 Extreme Workout Supplement

Buffered Creatine (Kre-Alkylyn as brand name)

To produce a buffered substance means playing with its pH to make it more soluble or better absorbed in the body. Buffered creatine has a higher pH than the monohydrate form. Thus, theoretically it should lead to a significant increase in translocation across the cytoplasmic membrane and thus more buildup in the muscle tissue. In addition, due to buffering, the creatine should have increased absorption. At the same time, this formulation is rapidly neutralized in the stomach. Therefore, the buffered creatine needs to have enteric coating for protection against quick neutralization from the digestive acids.

Neverthless, the research shows that even an enteric coating does not make it more efficient than creatine monohydrate. It has been shown that buffered creatine is not significantly different than the basic creatine monohydrate.

Kre-Alkayn is one of the buffered forms of CR supposed to be more effective and safe than creatine monohydrate (All American Pharmaceutical, Billings, MT, USA). According to the manufacturer, this form of CR is very stable in the stomach and not converted to creatinine thus available for utilization in the body.

The manufacturer has made quite a few claims like this CR does not completely stable (100%) until delivered to the muscle; that it does not cause cramping and bloating because very little is needed (1.5 g of Kre-Alkalyn is equivalent to 10-15g of creatine monohydrate) and so forth. The studies cited by the manufacturerthat took place in Bulgaria, are not referenced anywhere in literature like pubmed or the authors themselves. One study that was presented at the International Society of Sports Nutrition annual meeting in 2007 showed opposite results than what manufacturer of KA is claiming. The study reported that CrM was degraded less than 1% to creatinine upto 120minutes while KA was converted 35% more than CrM.

Jagimet. al. (2012) showed that KA is not better than creatine monohydrate. Of course taking supplemental CR in any form might provide health benefits as long as extra amounts of creatine are delivered to muscle.

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CREATINE PRODUCTS OF CURRENTLY NOT RECOMMENDED CR FORMULATIONS

 

based on lack of available evidence or conflicting data

GNC AMP Amplified Creatine 189

As the name suggests, this is an amplified or concentrated form of creatine. The product label states that it leads to significant muscle creatine absorption, provides creatine equivalent to 5g in two tablets and a major increase in dosage efficiency to enhance strength and athletic performance.

Potential Side Effects: According to MayoClinic.com, GNC AMP Amplified Creatine 189 should be taken exactly as described on the label, Otherwise it could cause

(a) Digestive side effects as muscle and abdominal cramps, bloating, diarrhea.

(b) Muscle Strain: Increased CR consumption can lead to muscle cramps that prevent the proper blood flow, which hinders the transfer of nutrients to muscles. This leads to even lower muscle mass than what is desired.

(c) Kidney and liver damage: Taking more than the recommended dosage or long term use of this creatine can lead to an increase in creatine concentrations in kidney that strains both of these organs and causes toxicity (MayoClinic.com).

Con-cret Concentrated Creatine (Creatine Hydrochloride)

CON-CRET is a patented highly pure creatine hydrochloride. Creatine hydrochloride (CreatineHCl) is a form of creatine where the creatine molecule is bound to a hydrochloric acid moiety. Biochemically, it means it will dissolve better in water and thus more CR will get absorbed in the body, and less will remain at the bottom of the cup.

According to the manufacturer, it is unique in comparison to other creatines available. This is because of the phenomenon of MICRO-DOSING which means need to take very little (750 mg per 100 lbs. of body weight). It dissolves very well, that leads to improved creatine uptake in to the muscle. Since very little amounts of this creatine are used, there is no water retention, bloating, or cramping. Due to micro-dosing, it does not require loading or cycling off.

However, these claims have not been confirmed by FDA nor any scientific studies are available to support these assertions.

Optimal Creatine by “Seeking Health”

It is in powder form and has chelated magnesium with creatine for optimal absorption.

As explained above, magnesium is crucial for quite a few biochemical mechanisms in the body. It is one of the most copious mineral in the body and thus is vital for good health. Theoretically, using creatine chelated with magnesium should make S-adenosyl methionine (SAMe) more accessible in the body to maintain various methyltransferase enzymes.

According to the manufacturer’s website, this creatine leads to increased absorption of creatine. The manufacturer also claims that ‘optimal creatine’ enables the transport of oxygen to the muscle tissue and enhances energy.

However, these claims have not been confirmed by FDA nor any scientific studies are available to support these assertions.

Body Fortress Super Creatine CEE AKG Nutritional Supplement

This is a next generation creatine that should require no loading and contains both ethyl ester and AKG. Once again, there is no literature supporting the superiority of this creatine. As the attached groups suggest, and as explained above, this should be the most superior formula out there. However, due to lack of any actual case studies, it seems the use boils down to personal choice.

Cellucor C4 Extreme Workout Supplement

This product contains creatine with nitrate and is highly recommended based on the customer reviews and the results they got (enhanced stamina and workout).  The manufacturer claims this supplement to be superior to all other marketed creatines.

However, there are no actual studies to support the above facts either way.

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