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Creatine in sports: use, benefits and side effects
Creatine in sports: use, benefits and side effects

Creatine in sports: use, benefits and side effects

Date: March 27, 2015

Creatine: proof and new horizons

I believe that all members of the bodybuilding community, as well as those who practice anaerobic exercise in particular, are familiar with this substance thanks to its established properties and its effectiveness. I'm talking about creatine, one of the most famous and widely taken supplements ever with proven effectiveness in various sports.
It is used as a source to obtain ATP, this interesting molecule has not had an easy run, even having been wrongly condemned as harmful, as well as a doping substance.

However, the fact is that it works well and is beneficial for a majority of people.

But do we really know everything about it and its possible administrations? Does it matter whether I take it?

It don't intend to repeat the concepts which have already been discussed thousands of times regarding activities relating to the formation of ATP and so forth. Instead, I would like to like to inform my readers about how a substance which has been classified and backed up by numerous studies for its well-known energising properties, can have multi-faceted attractive qualities.

I want to start by saying that, far from being a miracle supplement, much less definable as a "doping" substance, as many have done and the ignorantly "uninformed" continue to do, it is undeniable that its many functions are not just confined to athletic performance (as everyone knows by now), but its target extends to multiple levels, such as the brain, the bones and the immune system, where it performs a cognitive-stimulating action, and for its anti-inflammatory action.

What is creatine?

Creatine is a nitrogenous compound which is naturally produced by the body from three amino acids (glycine, arginine and methionine) in the kidneys, pancreas and mainly in the liver.

We find approximately 95% of it stored in skeletal muscle, two-thirds of which is stored in phosphocreatine form.

From here it is then released into the blood stream and is received mainly by muscle fibres by means of a sodium chloride-dependent creatine transporter, CreaT1.

The chemical formula of creatine

The chemical formula of creatine and its molecular representation

Creatine's mechanism of action

In order to rephosphorylate adenosine diphosphate (ADP) to adenosine triphosphate (ATP) during and after vigorous exercise, we depend fundamentally on the phosphocreatine stored in the muscle.

When the stocks of phosphocreatine are depleted during exercise, energy availability decreases due to the inability to resynthesise ATP in the required quantity with the resulting consequences to the performance level.

Consequently, the ability to maintain a constant level of effort decreases. That's why an oral intake in the form of a supplement is advisable, because to take the "suitable" amount, it is really "demanding" to ingest the large quantity of meat and fish (endogenous food sources) required to obtain a bioavailable gram.

Furthermore, it has been suggested that an increase in muscle creatine content, through the supplementation of creatine, can increase the availability of phosphocreatine, allowing an accelerated rate of ATP resynthesis during and after high intensity and short duration exercise.

Hence the boom in the sports supplement market which footballers, rugby players, as well as skiers can only benefit from.

More stocks, increased recovery and strong neo ATP = a ready source of explosive power.

A bodybuilder who increases his ATP levels will particularly benefit. But as I mentioned, it has a much broader set of functions.

Cerebral "Power"

This factor is intriguing! That lifting more weight can also up the ego is undeniable, but there is also scientific evidence that has demonstrated improved mental faculties.

Interestingly, a well-respected study has shown that creatine monohydrate helped the effects of antidepressant pharmaceuticals (SSRIs) by speeding up the effects on the participating women.

In Kyoon Lyoo, et al. A Randomized, Double-Blind Placebo-Controlled Trial of Oral Creatine Monohydrate Augmentation for Enhanced Response to a Selective Serotonin Reuptake Inhibitor in Women With Major Depressive Disorder. Am J Psychiatry 2012;169:937-945. Doi 10.1176/appi.ajp.2012.12010
It's no coincidence that we therefore find blends of antioxidants, B vitamins, minerals and other substances in pharmacies that may have some influence on memory, often recommended (and overrated) for students or as restorative during times of stress. You will often find creatine in these blends because it appears to provide good support for cognition and memory.

Systemic improvement of methylation

What does this mean for those of us who aren't "science buffs"?

Let's take a moment to clarify.

As I already stated, we know that the function of creatine is energy, promoting the development of strength and muscle volume. This latter factor supports it as well by helping the so-called "methylation" cycle, a complex biochemical process which, in layman's terms, manages or contributes to a wide range of essential bodily functions, including:

  • detoxification
  • regulation of immune function
  • maintaining DNA
  • energy production
  • inflammation control

Methylation is therefore a delicate process essential for life itself. SAMe (S-adenosylmethionine) is the main molecule responsible for the contribution of methyl groups in the body.

The endogenous formation of creatine (which mainly occurs in the liver and kidneys) empties the reserves of SAMe, adversely affecting methylation. This is why supplementation is sure to be a positive support, ensuring that the body seeks amino acids for the formation of creatine.


Mitochondria, site of ATP synthase

Reducing inflammation and improving recovery

Each workout, in order to be effective, must be followed up by a more than adequate recovery.

We know that creatine improves performance and muscle growth at the cellular level, but it also promotes recovery between training sessions, playing a key role by modulating inflammation.

It has been noted that, by measuring inflammatory markers (therefore related to muscle pain) such as creatine-kinase, lactate dehydrogenase, prostaglandin E2 and tumour necrosis factor-Alfa, in runners after a thirty kilometre race, researchers have shown that by supplementing creatine with fifteen to twenty grams of maltodextrin per day, for five days before the event. These values ??were significantly different from the study group that did not take the supplement, which instead showed an increase of creatine-kinase which was four times higher when compared to the initial level, as well as an observed increase of six times the prostaglandin E2 and lactate dehydrogenase by 43%.

The group assisted by taking creatine did not show any significant increase in lactate dehydrogenase and a reduction of creatine-kinase by 19%, prostaglandin E2 by 61% and the tumour necrosis factor-Alfa by 34% in comparison to the control group. Thus concluding that creatine supplementation would reduce cell damage induced by exercise and the relative inflammation.

Santos, R. V. et al. (2004) The effect of creatine supplementation upon inflammatory and muscle soreness markers after a 30km race. Life Sciences, Volume 75(16), pages 1917-1924.

Increased IGF-1 deactiviation of satellite cells

Even the average bodybuilder knows how important the production of IGF-1 is as an essential growth factor on the activation of satellite cells. While taking creatine, the IGF-1 levels were significantly higher, but the interesting factor is that it could also directly activate satellite cells and their differentiation.

These are responsible for the repair and healing of the muscle cells.

Rapid weight gain

Not to diminish the importance of the previous points, but a bodybuilder is primarily interested in what he sees in front of the mirror. When muscles are saturated with creatine, being an osmotically active substance, they can retain more water internally, giving a fuller and rounder appearance. This osmosis ensures that there will be an increase in cell volume, giving value to the basic biochemical concept that "a hydrated cell is cell anabolism", which in turn will cause a stretch effect of the cell membrane and biochemical consequences which further promote muscle growth.

Side effects of creatine

Is creatine bad for you? In addition to abdominal bloating, users notice a little water retention (extracellular), however, it is defined as a safe product overall.

The "tall tale" regarding the potential to cause kidney or liver damage by a bigoted and often too closed scientific community has finally been proven to be totally unfounded, with several studies confirming this (creatine is the supplement that boasts the largest number of studies overall).

Muscle cramps, contractures, dehydration and diarrhoea are side effects which have been highlighted by some users. In fact what I noticed in athletes were (although in only a few cases) episodes of diarrhoea and slight dehydration.

In any case, Chad Kerksick, Ph.D., assistant professor of exercise physiology at the University of Oklahoma, a leading authority in sports supplementation asserts that "creatine is one of the most sought after and studied supplements on the market and no studies in published literature define it as unsafe. "

Then we have Jose Antonio Ph.D., a professor at Nova Southeastern University, CEO of the International Society of Sports Nutrition, a great supporter of cyclised creatine, who states that "it has been proven that users experience less cramping and dehydration issues, muscle strain and in any case, it does not cause any damage in its routine consumption. "

An important part of the scientific literature which proves the safety of its consumption:

Creatine loading phase: is it really necessary?

Big question!

I remember years ago when it came out on the market, considering the limited knowledge back then, users were advised to employ a kind of loading strategy in order to saturate the muscle stores and then to follow that up with a maintenance dose.

Users were always advised to pair this with simple sugars because it was said that they facilitated the "transport" of the creatine.

There were companies that built successful commercial success stories on the strength of this concept.

But what does the real science tell us?

On average, a 70kg man has about 120g of Creatine stocks, 95% of which resides in the skeletal muscles.

That's why we tried (and some still do) a loading phase. It is, without a doubt, a quick way to fill the muscle stores and gain weight, with favourable effects on performance.

I have heard about a lot of loading and dosing systems, from one or two days, up to two weeks, with doses ranging from four to six doses a day from 5 grams at a time.

With reasonable moderation, to acquire a loading effect, a two or three day phase is advisable, in which a ratio of 0.071 g/kg body weight (about 6g for a 90kg athlete) is taken four times a day, possibly combined with meals which are high in carbohydrates in order to create a significant insulin response which favours the transfer.

Following this phase, you should reduce your intake to a single daily dose of approximately 0.029 g/kg (about 2.5 g/3 for a person weighing 90kg) which often becomes a standardised 5g per day dose to create a better effect, counting on the fact that the bodybuilder trains intensively and often with a substantial workout volume.

That said, I wish to clarify that no rule is law, just like the same load phase is unnecessary for many. Often you may want to reduce or eliminate it for one or two months and then start taking it again, however no study supports this theory.

It is claimed that it is better to use it for two or even three months, with a suspension of one month because it would increase the effectiveness of the transport modes to the muscle cells and thus elicit a better response (it is no coincidence that after a certain period of use it is easy to notice a decrease in effectiveness).

Many users have had excellent results simply taking it with water (a generous amount) and consuming a meal high in carbohydrates or by adding (as they did long ago) grape juice to maximise the absorption.

We know that absorption is improved when insulin levels are high and for those who follow a low-carb or carb backloading diet, you can opt for insulin agonists such as whey, bcaa or GDA (glucose disposal agents) such as lipoic acid or cinnamon.

What is the best type of creatine?

In recent years, different forms of creatine have been released; citrate, ethyl ester, nitrate, malate, pyruvate, alkaline, liquid and hydrochloride, the latest.

Many forms are modified to have, or rather try to have better forms of transport and absorption, but the best is the classic creatine monohydrate.

While all of these forms had moments of piqued interest to then vanish, the only innovation that is producing interesting results is hydrochloride, which is very effectively absorbed, therefore causing less water retention and swelling of the monohydrate.

However, the effervescent version does not possess any absorption benefits in comparison to the monohydrate as some have claimed, which, like the liquid and ethyl ester, is "unstable", in the sense that it is difficult for them to arrive at the " destination", whereas the "micronised" monohydrate version has benefits for those who are unable to tolerate it in the intestine.

Creatine and coffee

Once it was believed that caffeine interfered with the absorption of creatine and therefore annuls its effect. This belief stemmed from a Belgian study published in 1996 which demonstrated the cancellation of the ergogenic effect of creatine when taken together with caffeine.

Subsequent studies have greatly put the Belgian study into perspective and now it is commonly believed that the normal consumption of caffeine has no effect on the properties of creatine, some even going so far as to praise the performance effects on sprints.

However, it must be borne in mind that for creatine to be assimilated as it should be it requires a basic gastric pH and caffeine, understood as a supplement (anhydrous), does not alter the pH, so for this reason they can also be assumed together.

Note how many new pre-workout supplements combine creatine and caffeine as a stimulant.

Coffee, understood as a beverage, which is often consumed before training, behaves differently because it makes the gastric environment acidic and is therefore not entirely suitable to maximise the absorption of creatine.

Therefore coffee and caffeine are not the same thing.

Is creatine effective for everyone?

It is important to consider that some variability exists in the response to creatine supplementation.

In order to differentiate the subjects, the terms "responders" and "non-responders" were defined, i.e., those who respond or do not respond positively to the effect of creatine.

It is assumed that the majority of this variability is to be found in the regulation and activity of creatine transporters. The increase in muscle stores depends on the levels present in the muscle before the supplementation.

In fact, the loading phase advice stems from here.

Those with naturally lower muscle creatine stocks, such as those who eat little meat or fish, or do not eat animal protein altogether (a vegetarian diet), are more likely to see their muscle storage increase by 20-40%, while those with relatively high muscle stocks can increase storage by only 10-20%.

It is curious how there is controversial scientific evidence on the effectiveness of creatine in women.

For those who want in-depth information:

In conclusion: it is not only a muscle supplement

My whole lengthy article has made it clear that creatine may be useful for both bodybuilders, as well as for the "average man", young or old.

It is a fact that it is a proven first-rate supplement for bodybuilders to keep in their arsenal in consideration of the established aid it can offer in complete safety.

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