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All About Creatine: The Definitive Guide (Part I)

Part I explains what creatine is, how the ATP–PCr system works, common loading and maintenance protocols, and potential gastrointestinal issues.

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All About Creatine: The Definitive Guide (Part I)

PART I

 1. WHAT IS CREATINE AND WHERE IS IT FOUND?

 

At a historical level, creatine from the Greek κρέας = kreas, meaning meat (Williams et al. 1999) is an amine discovered more than 170 years ago by the French researcher Michel Eugene Chevreul (1832). Although it is actually considered a non-protein amino acid synthesized from arginine, glycine and methionine in the kidney, liver and pancreas.

Endogenous and exogenous creatine synthesis and metabolism
Fig 1. A. Endogenous creatine synthesis and its metabolism B. Metabolism of exogenous creatine supplementation.

In addition to not being considered an essential amino acid since its synthesis can also be endogenous, Cr can also be obtained through diet, mainly in products of animal origin.

Although currently almost everything we know today about Cr and performance comes from the English scientist Roger Harris. The use of creatine in sports stems from the studies of this researcher in 1992, leading to different English athletes using it during the Barcelona Olympics. Later, the Atlanta Games were known as the "Creatine Games."

Creatine (Cr or methylguanidinoacetic acid) is a biochemical compound that is found mainly in skeletal muscle with much smaller quantities in cardiac muscle (∼94–97%), the rest can be found in both testicles and brain.

Phosphocreatine (PCr) represents a 60% (2/3) of that reserve, while a 40% (1/3) is found in the form of free creatine. Total creatine (PCr + Cr) in muscle averages is 120 mmol/kg dry muscle mass for a 70 kg individual. However, the upper limit of creatine storage appears to be approximately 160 mmol/kg dry muscle mass in most individuals.

Amount of creatine stored in muscle
Fig 2. Amount of creatine at muscle level

Approximately 1-2% of intramuscular creatine is degraded to creatinine (metabolic byproduct) and excreted in the urine. Therefore, the body needs to replenish around 1-3 g of creatine per day to maintain normal (unsupplemented) creatine stores depending on the amount of muscle mass.

 2. HOW DOES IT WORK AND WHAT ARE ITS MAIN ACTION MECHANISMS?

There are many functions that creatine is currently recognized for, not only at the level of sports performance but also in the clinical field. From a performance point of view.

Cr is an important physiological compound as part of the ATP/PCr energy system. Cr and inorganic phosphate combine to form PCr and a greater muscle Cr pool will allow for higher concentrations and/or rates of PCr biosynthesis in the muscle. Therefore, PCr is an immediate fuel reserve for ATP replenishment in the ATP-PCr energy system and Cr is an important substrate supporting this system.

 

Creatine action in the cytosol and mitochondria
Fig 3. Exchange and mechanism of action of creatine at the cytosolic and mitochondrial level.

 

That is, its main function is to act as a donor of phosphate groups to ADP to regenerate ATP. This will generate a positive effect on performance resulting in a greater generation of ATP (energy currency used by the human body) between sets of strength exercise, which allows athletes to maintain greater training intensity and improve the quality of training.

3. WHAT IS THE APPROPRIATE SUPPLEMENTATION PROTOCOL? DO I HAVE TO TAKE IT WITH CARBOHYDRATES? WHEN?

The goal of creatine supplementation is to saturate muscle creatine storage, and there are two common methods to achieve said saturation. These increases can vary depending on the initial concentration between 20-40% of Cr/PCr reserves at the muscle level, depending on the initial concentration.

Loading is a popular method, which involves taking very high doses of creatine (20-25 grams per day, divided by 4-5 doses) for 4-7 days in a row. After this loading phase, muscle creatine storage is maximized and a maintenance dose of 2-5 grams per day is taken thereafter.

While loading is certainly effective, it is not strictly necessary. Research has shown that moderate daily doses of 3 grams per day can saturate muscle creatine storage after approximately 3-4 weeks of supplementation. When deciding whether to load or not, the main factors to consider are time and gastrointestinal comfort. If you really need your results to be maximized within seven days of supplementation, loading would be the most reliable option. However, mild gastrointestinal discomfort is often seen with creatine supplements; If you have difficulty taking 20-25 grams of creatine in a single day, then loading would not be your best option, and a more patient approach would be preferable.

Regarding the time or “timing” of consumption (time of day), some studies conclude that its effectiveness increases after training, others confirm that before it is much better. My recommendation is that the time of day does not matter as long as it is consumed, so I would try to associate it with a time of day that is easy for me to supplement or that I have the possibility of doing without forgetting. Since, as we have read previously, it works by accumulation.

Regarding the intake of carbohydrates/protein, it is true that insulin can play an important role in helping creatine transport into the muscle cell, but in the long term the magnitude of the effect fades and no significant differences are found when it comes to consuming it dissolved in water, for example.

 

Muscle creatine saturation across supplementation protocols
Fig 4. Effectiveness of muscle creatine saturation in different protocols

4. WHAT IS ENOUGH AMOUNT TO PRODUCE IMPROVEMENTS IN PERFORMANCE?

 According to the different studies between 0´05 – 0´07 chronically it would be more than enough to increase creatine deposits in the muscle and thus maximize the ergogenic effects of this substance.

  5. CAN IT CAUSE GASTROINTESTINAL PROBLEMS? BAD INTERACTION WITH CAFFEINE?

Several studies highlight some of the gastrointestinal problems caused by the consumption of creatine, in fact, this usually occurs especially in two cases.

  • High doses of creatine monohydrate.
  • Consumption with high amounts of caffeine (in fact, this may be the widespread “myth” that these two substances should not be consumed together, there is controversy in all of this. But the latest studies indicate the non-existence of all these adverse effects, even so as a principle of prudence, I would try to avoid the co-ingestion of these two substances as much as possible due to the possible effects at the gastrointestinal level if we use the loading protocol in terms of creatine monohydrate or high amounts of caffeine (> 5 mg/kg).

 

Potential interactions between creatine and caffeine
Fig 5. Possible negative interactions between Creatine and caffeine

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COMPLETE BIBLIOGRAPHY

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