A Comprehensive Exposition On Creatine Monohydrate for 2020

A Comprehensive Exposition On Creatine Monohydrate For 2020

What is Creatine?

Creatine is a naturally-occurring substance found in the human body and is essential for its everyday functions. Creatine is a popular sports supplement due to its ability to help build muscles, improve strength, and shorten recovery times.

Creatine plays a crucial role in transporting energy throughout the body, especially during intense physical activity such as heavy lifting or high-intensity training. The energy-related benefits of creatine are well researched, with scientists examining creatine’s effects on strength and power output for decades. Creatine is also believed to assist with cognitive performance, organ function, and general health, although more research is needed in these areas.

Creatine is a relatively small and simple molecule (with the chemical formula, C4H9N3O2), and it is classed as a nitrogen-containing organic acid. The average adult has between 80 – 130 grams of creatine stored in their body. The majority of people get around half of their daily creatine requirements from eating protein-rich foods such as meat and fish. The rest is produced by converting amino acids through a process called creatine biosynthesis.

creatine monohydrate
Creatine Monohdrate is probably the most effective muscle building supplement of all time.

Given meat and fish are some of the only dietary sources of creatine, people who do not eat a diet complete with protein-rich foods may have lower than normal creatine levels, such as vegetarians and vegans.

As a dietary supplement, creatine has been scientifically proven to increase physical performance and has been approved for use by regulatory bodies and sports agencies worldwide. When properly manufactured and taken at recommended doses, creatine is absorbed quickly by the body and has no harmful side effects.

How does the body make creatine?

Through creatine biosynthesis, the body converts the amino acids glycine, arginine, and methionine into creatine phosphate and phosphocreatine. Glycine, arginine, and methionine are found in food, including meat, fish, eggs, and some nuts and seeds.

The first stage of creatine biosynthesis occurs in the kidneys and pancreas. Arginine and glycine are converted by the enzyme Arginine:glycine amidinotransferase (AGAT) into guanidine acetate (GA). The liver then transforms GA into creatine using the amino acid, methionine, and the enzyme, GAMT. The synthesized creatine is then distributed to target organs, including the brain, heart, and skeletal muscles, using a plasma membrane creatine transporter (CrT).

Creatine biosynthesis in an average 70-kg man produces approximately one gram of creatine per day, with this amount gradually reducing with age. Women synthesis creatine at a slightly lower rate compared to men.

Glycine is the most plentiful of the three amino acids needed to synthesize creatine. Arginine and methionine, on the other hand, are not readily abundant. Synthesizing just one gram of creatine requires approximately 40 percent of an average person’s daily methionine intake. People whose diet is low in natural sources of methionine (i.e., eggs, fish, nuts) may have low creatine levels.

Studies have found that taking creatine monohydrate supplements can be highly effective in assisting the body’s production of creatine, especially when taken regularly and over an extended period. Daily doses of creatine monohydrate depend on one’s level of activity and training phase. Creatine monohydrate is safe to use in both the long- and short-term, and can also be taken during exercise-free periods and both with or without meals.

Bioavailability and creatine balance

An average adult has around 80 – 130 grams of creatine and phosphocreatine (PCr) in their body at any given time. This store of creatine is found mostly in the body’s muscle cells, with the vast majority of the body’s creatine stores recycled through constant conversion from phosphocreatine back to creatine.

Despite this efficient system, the body loses between two to three grams of its reserve each day through the breakdown of creatine into a substance called creatinine. The body makes up for this loss through diet (approximately one to two grams per day) and creatine synthesized by the body (about one gram per day).

Studies have found that creatine has high bioavailability, which means that it is easily absorbed into the body and available for the body to use. For example, depending on dosage, more than 95 percent of creatine monohydrate can be absorbed into the bloodstream when taken as a dietary supplement. Once ingested, creatine levels in the blood typically peak around one to two hours.

People with diets containing low levels of creatine have shown lower creatine levels on average. In comparison, people who take creatine as a supplement generally have higher creatine levels. When taking creatine supplements, body tissues eventually become fully saturated with creatine stores. As a result, it is not necessary – nor useful – to take high doses of creatine over prolonged periods.

The amount of creatine stored in the body reflects a balance between the average rate of creatine absorbed through one’s diet, the rate of the body’s creatine biosynthesis, and the natural rate of creatine breakdown into creatinine.  Variations in creatine stores occur gradually in response to changes in creatine intake. Therefore, creatine levels in the body may take three or four weeks to build up to their maximum levels when creatine is taken as a supplement at the recommended dose of 3 – 5 grams per day.

Metabolism, creatine, and creatinine

Creatine, the natural waste product of creatine breakdown, is expelled from the kidneys’ body, which releases it into the urine.  Scientists estimate that an average adult loses around one to two percent of his or her creatine stores via this process.

When people ingest more creatine than their body requires, most of the surplus creatine is filtered through the kidneys and excreted into the urine. Higher levels of creatine also increase the rate of breakdown of creatine into creatinine in the body, causing the concentration of creatinine in blood and urine to rise. A person with high muscle mass may show increased creatinine levels compared to someone with lower muscle mass. However, as long as creatinine levels remain within normal limits, there is no cause for concern.

Given doctors measure blood creatinine levels as a routine test for kidney disease, anyone undergoing kidney function tests should inform their doctor if they take creatine as a supplement. Elevated creatinine levels resulting from taking creatine supplements are generally not a problem. Nevertheless, anyone with kidney disease – or at risk of developing kidney disease, including diabetics or people with high blood pressure – should consult a doctor before taking creatine supplements.

How Does Creatine Affect the Body?

Increased muscle power from creatine

The vast majority – roughly 90 percent – of creatine is stored in the body’s muscle cells. Like all cells, muscle cells need energy to function, and creatine helps to provide this energy to allow muscle cells to work effectively.

Muscle cells acquire their energy from several sources. When running long distances or during other periods of prolonged exercise, the body draws first on its glycogen stores – energy stores converted from glucose – and then by burning fat. This process of creating energy is called aerobic metabolism due to the presence of oxygen in burning glycogen, amino acids, and fats.

In comparison, short bursts of intense anaerobic exercise, such as sprinting and HIIT, require immense amounts of energy that the muscles cells can immediately use. These readily assessable energy stores take the form of chemical substances known as ATP (adenosine triphosphate) and phosphocreatine (PCr). ATP and PCr work together to immediately provide the required energy, filling in until more energy can be produced through the metabolization of glucose (glycolysis), glycogen (glycogenolysis) and fat (lipolysis and fatty acid oxidation).

Creatine monohydrate helps supports strength

ATP, ADP, and creatine

Adenosine triphosphate (ATP) is the preferred energy source for most biological processes. An ATP molecule has three phosphoryl groups, which are attached to a central framework. Losing one of the phosphoryl groups converts ATP to adenosine diphosphate (ADP) and releases energy to power the cell. However, muscle cells can only store enough ATP to power a few seconds of high-intensity exercise.

While the body gradually converts ADP back into ATP using energy derived from food sources, this conversion takes time. Muscle cells, therefore, need a faster way to regenerate their ATP for more sustained exercise. This is where creatine steps in to help.

During periods of inactivity, approximately two-thirds of a muscle cell’s creatine stores exist in the energetically charged form of phosphocreatine (PCr). A PCr molecule is a creatine molecule with an added phosphoryl group. As muscle cells begin to deplete their ATP, an enzyme called creatine kinase takes a PCr molecule’s phosphoryl group and transfers it to an ADP molecule, converting ADP back into ATP. One of the fastest-acting enzymes, creatine kinase fuels the ATP regeneration process and keeps ATP levels high for an additional few seconds. ATP levels only start to drop when around 80 percent of the PCr stores are spent.

This process allows muscles to keep up the intense exercise until the supply of PCr is mostly depleted. After the muscles are no longer in use, the phosphoryl groups that were initially stripped from the PCr molecules to regenerate ATP are returned. Once returned to their initial levels, the PCr stores are ready to fuel ATP regeneration during the next bout of exercise.

Benefits of Creatine

Creatine Supplements for Sport

Given its role in transporting energy within cells, creatine is a widely used dietary supplement for athletes. Creatine supplements increase the phosphocreatine reserves in muscle cells, which in turn improves performance and shortens recovery in training and during competitions.

For gym enthusiasts, creatine is also popular as it helps people train harder, allowing for a faster increase in muscle mass. Compared to steroids and other banned substances, creatine on its own does not create muscle mass without training.  

Supported by scientific studies conducted in the past three decades, many athletes see creatine as the most effective nutritional supplement for increasing muscle strength, building lean body mass, and enhancing exercise tolerance. Creatine supplements have shown to increase both power and number of repetitions during resistance training.

In particular, creatine supplementation benefits athletes in sports that require short bursts of intense muscle power, including competitive cycling, sprinting, swimming, and football. Athletes in these disciplines have long taken creatine with excellent performance results.

Creatine, in the body’s natural form, creatine monohydrate, is proven to be effective, safe, and legal. The European Food Safety Authority (EFSA) recognizes creatine monohydrate’s general function to increase physical performance during short bouts of high-intensity exercise.

Other benefits of creatine

In addition to creatine’s energy-related benefits, research over the past two decades has found that creatine plays essential roles in not only muscles but also in other types of tissues and cells.

For example, creatine is believed to regulate the ratio of ADP to ATP by preventing high ADP levels in the cell-liquid, and low levels in the mitochondria, the cell’s “power plant.” This process is crucial for oxidative energy generation within the mitochondria and may be one of creatine’s most important functions in cellular energy metabolism. In addition, creatine plays a role in the energy transfer from the mitochondria to the intracellular fluid – a complicated process that depends on the presence of several different forms of the creatine kinase enzyme.

By reducing cell damage by oxygen radicals, creatine acts as an antioxidant and buffer against cellular pH (acidity). This function is critical during periods of intense activity when intracellular fluids tend to acidify. Creatine also contributes to balancing the various aerobic and anaerobic energy sources, including glycolysis, available to cells.

Many studies point to creatine’s role in maintaining general health – including in cognitive function and the rest of the central nervous system – especially among older people. Infants born without the ability to make or use creatine in their bodies often suffer from severe mental and physical disabilities.

New clinical studies suggest that creatine may be crucial in preventing or delaying the onset of neurodegenerative diseases such as Parkinson’s disease, Huntington’s disease, Alzheimer’s disease, and long-term memory impairments brought on by strokes.

Sources of Creatine

Creatine derived from food

Over time, creatine slowly breaks down and is flushed out of the body (for more information, refer to this paper’s section on ‘Metabolism, creatine, and creatinine’). To replenish the body’s stores, an average adult needs to replace creatine at around two to three grams per day. People eating a balanced, protein-rich diet get around half of their daily creatine requirements from food sources.

Natural creatine-rich food sources include red meat, fish, and chicken. The table below shows the average amounts of creatine found in various raw foods:

Table 1: Creatine Content of Various Raw Foods (g/kg)

Meat3 – 7
Fish3 – 7
Milk0.1
Vegetables and grains>0g

Note: The cooking process destroys some of the creatine content in meat and fish

People who do not eat a protein-rich diet may have lower creatine levels, in particular, vegetarians and vegans who may get little or no creatine directly from food sources. Supplementation, therefore, can be a great way for people with low creatine levels to increase their dietary intake of creatine. This includes people who do not regularly eat red meat or fish and those that are looking for extra creatine to build muscle, increase strength, and ensure faster recovery times.

Creatine Monohydrate

Creatine monohydrate is a natural form of creatine and is widely considered the best form for creatine supplementation. In its powder form, creatine monohydrate is effective, safe, easily absorbed by the body, and stable during storage. Creatine monohydrate has been researched extensively as one of the best exercise supplements and is recognized by regulatory authorities worldwide. The European Food Safety Authority’s estimation on creatine refers expressly to creatine monohydrate. To date, there is no peer-reviewed research to indicate there is a more effective form of creatine than creatine monohydrate.

Other Forms of Creatine

Alkalinized Creatine

‘Alkalinized’ creatine is claimed to be more stable than creatine monohydrate in stomach acid. However, as mentioned before, creatine monohydrate already enjoys high bioavailability, and alkalinized creatine may, in fact, speed up the breakdown of creatine into the waste product of creatinine. There is no peer-reviewed research that suggests that alkalinized creatine is more effective than creatine monohydrate.

Buffered Creatine

Buffered creatine (Kre-Alkalyn) and creatine hydrochloride (Con-Cret) are negated by stomach acid and, therefore, return to a typical creatine molecule. A 2012 study published in the Journal of the International Society of Sports Nutrition found no differences in efficacy between buffered creatine and creatine monohydrate. This included no remarkable differences in muscle creatine content, body composition, or training adaptations compared to creatine monohydrate

Creatine Ethyl Ester

The esterification of creatine is intended to increase creatine’s bioavailability; however, numerous studies have found no evidence to support the claim that creatine ethyl ester (CEE) increases the bioavailability of the substance. In fact, while creatine monohydrate is almost completely absorbed into the body, some studies demonstrate that CEE rapidly decomposes into an ineffective form of creatinine and is not as effective in improving muscle strength and power.

How to Use

How should I take creatine?

As a sports supplement, creatine monohydrate can be dissolved into a liquid (i.e., water, tea, juice, or milk) or taken as capsules, tablets, or bars. Creatine dissolved quickly in the stomach, so loose suspension is not an issue. While you do not need to dissolve the powder entirely before drinking it, creatine should always be taken with plenty of liquid when mixed into a drink to ensure proper hydration.

Some studies show that taking creatine with carbohydrates and/or other protein sources yields synergistic effects, thus increasing the amount of creatine available to muscle cells.

How much should I take?

The recommended daily dose of creatine monohydrate is between three to five grams. The European Food Safety Authority indicates that three grams of creatine are safe on a daily basis, while an expert panel in the U.S. recommends five grams. Creatine monohydrate supplements can be taken as a capsule, powder, or a chewable tablet, depending on individual preference. As a creatine supplement’s purity is critical (impurities such as DHT-related compounds have been linked with cancer), you should only take creatine products from established sources and manufactured using the highest quality standards.

When should I take it?

Creatine supplements can be taken at any time of the day, either with or without meals. Most athletes take creatine supplements less than 60 minutes before working out or immediately after training. Nevertheless, there is no conclusive research to support whether ‘timing’ your creatine intact is more or less beneficial for performance outcomes.

Should I take creatine on my rest days?

Taking creatine monohydrate supplements has been found to be most effective when taken on a regular basis. If you do not exceed the daily recommended dose of three-five grams per day, you should continue taking your creatine monohydrate supplements on your rest days and during extended exercise-free periods.

Side Effects

Creatine monohydrate supplements have proven to be safe when manufactured according to high-quality standards and taken at the recommended dose. Anecdotal evidence describes cases of stomach pain, dehydration, and convulsions when some people take creatine supplements. However, the International Society of Sports Nutrition concluded in 2017 that, “there is no compelling scientific evidence that the short- or long-term use of creatine monohydrate has any detrimental effects.”[1] One non-detrimental side effect noted by some studies is a small amount of weight gain. This is primarily due to an increase in water accumulation in the muscle cells and the gradual increase in muscle mass desired by athletes taking creatine supplements. If an individual consumes more creatine than needed – either through food sources or dietary supplements – the excess creatine is broken down into creatinine and expelled in the urine.

Creatine Myths

Myth: You need to ‘load’ creatine to see the most benefits

You do not need to engage in ‘creatine loading’ to benefit from creatine supplementation. Many Internet ‘fitness gurus’ suggest loading creatine – taking significantly higher doses of creatine than the daily-recommended amount of three to five grams and then reducing the dosage after a few days. However, studies have shown that creatine loading is unnecessary. Research demonstrates that, after three to four weeks of taking the recommended three to five grams of creatine daily, the body’s creatine levels are the same as when high doses are taken at the beginning of the ‘loading phase.’ There also may be health risks when taking higher doses of creatine. While the daily intake of three to five grams of creatine is considered safe, higher dosages can lead to health complications and damage the kidneys, liver, and/or heart.

Myth: You should cycle creatine supplementation

You do not have to pause your creatine supplement schedule or regularly change dosages. If you are not overdosing, you can take three to five grams of creatine per day year-round, including during training and rest periods.

Myth: Creatine supplementation can lead to kidney failure

As long as you are healthy and have no history of kidney disease, you should not be concerned if you take the appropriate dose of creatine. There has been no evidence to indicate that the recommended creatine dosage of three to five grams causes lasting damage to the kidneys. However, if you have preexisting kidney conditions or have a condition that increases the risk of kidney disease (i.e., diabetes), you should consult with your physician before taking creatine supplements.

Myth: Taking creatine supplements causes hair loss

There is no research to support the myth that creatine supplementation leads to hair loss. Hair loss has not been found as a side effect of taking creatine supplements across numerous studies conducted on creatine.

Creapure®

What is Creapure®?

Creapure® is the trademark name for pure creatine monohydrate manufactured by AlzChem Trostberg GmbH in Germany. Creapure® is one of the most widely researched forms of creatine and is proven to be effective and safe as a dietary creatine supplement. When buying Creapure® supplements, you can trust that you are using one of the best and most reliable products on the market. Creapure® is vegan and produced exclusively through chemical synthesis. Given that its raw materials and intermediates are not derived from animal or herbal products, you can rest assured that there are no traces of animal or herbal byproducts in Creapure®. The production of Creapure® is IFS FOOD certified, a quality standard recognized by the “Global Food Safety Initiative,” and is produced in compliance with Jewish and Muslim food regulations (both Kosher and Halal certified).

creapure
High Quality Creatine Monohydrate made of Creapure brand.

Production Process

Creapure® is manufactured according to the strictest guidelines used in the pharmaceutical and food industry. Good Manufacturing Practice (GMP) quality standards ensure high-quality production throughout the entire manufacturing process. To ensure any sources of contamination or processing disturbances are identified and eliminated, manufacturing processes operate according to the principles of the HACCP concept (Hazard Analysis and Critical Control Points). The custom-built Creapure® manufacturing plant eliminates almost all risk of cross-contamination or contamination by other products. Creapure® is produced on a completely closed production line, beginning with the delivery of raw materials to the final packaging process. Each production batch is quality tested with high-performance liquid chromatography (HPLC) and other analytical techniques before being released for shipment.

Creapure® vs. Generic Creatine

Creatine is only manufactured in two countries in the world: Germany (Creapure®) and China (generic creatine). Test results have repeatedly demonstrated that Creapure® is the purest source of creatine.

In recent years, regulators have increased their oversight of nutrition ingredients, particularly impurities. In regards to creatine supplements, the EFSA (European Food Safety Authority) recommends that a creatine product should not exceed:

  • Dicyandiamide (DCD) levels of 50 mg/kg
  • Dihydro-1,3,5-triazine (DHT) levels of 3 mg/kg

These impurities, such as DHT-related compounds, are suspected of causing cancer. The graph below compares the average results from 9 different Creapure® creatine monohydrate products and 20 other generic creatine monohydrate products. In generic creatine products, the average amounts of DCD and DHT significantly exceeded the levels recommended by the EFSA. Creapure® creatine monohydrate products, on the other hand, remain well below the EFSA’s recommended limits.


creapure creatine

[1] Kreider, Richard B et al. “International Society of Sports Nutrition position stand: safety and efficacy of creatine supplementation in exercise, sport, and medicine.” Journal of the International Society of Sports Nutrition vol. 14 18. 13 Jun. 2017, doi:10.1186/s12970-017-0173-z

Creatine Tips and Tricks

These tip and tricks are not necessarily backed by science. Some are and some are not. However, these tips and tricks come from years of experience by the author, who is an expert in supplementation.

Use creatine with carbohydrates.

Use creatine with hydrolyzed protein. Hydrolyzed protein is insulinotropic thus that will help with creatine effectiveness.

Don’t use creatine with caffeine

Typical Creatine Drink For Sports Nutrition and Bodybuilding

1 tsp of Creapure

2 tbs of Peptopro

20 oz of Pomegranate Juice

Mass Building

1 tsp of Creapure

2 tbs of Raw Honey

1/4 of Oat Muscle

1/4 Cup of Muscle Shake

Blueberries and bananas

Mix in almond milk, regular milk, or water. I personally like banana milk, and other nut milk.