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Creatine


 General Info  

Active Forms
Creatine monohydrate, micronized creatine monohydrate, creatine phosphate, and creatine citrate.
  • Creatine monohydrate contains 88% creatine and 12% water. A 5 gram dose of creatine monohydrate provides 4.4 grams of creatine.
  • Creatine phosphate is 62.3% creatine and 37.7% water. A dose of creatine phosphate provides less creatine than an equivalent dose of creatine monohydrate, plus creatine phosphate is generally more expensive.
  • Creatine citrate is more water soluble, but contains only 40% creatine and is more expensive. Creatine monohydrate is by far the most popular form of this supplement.

    Absorption
    Creatine is readily absorbed from the stomach.

    Dietary Sources
    Animal protein is the best source of dietary creatine.

 Dosage Info
Dosage Range
2 to 20 grams daily.

Most Common Dosage
Although there is no definitive guide on how much creatine to take, many experts suggest that larger amounts should be taken as a "loading phase" during the first week of supplementation when the body is most responsive. This can reportedly create substantial gains in muscle size, strength, and performance in as little as one week. A typical loading dose is 5 grams taken four times a day for one week. After muscles are saturated with creatine, a maintenance dose of 5 to 10 grams a day can be consumed. It is generally recommended that creatine be taken 60 to 90 minutes before and/or after exercising.

Dosage Forms
Powder, capsules, tablets, liquid, gum, or effervescent powder form. Stabilization of liquid creatine is still suspect since it degrades to creatinine in this form.
Adult RDI
None established

Adult ODA
None established

RDA
None established
 
 Overview
Creatine plays an important role in the production of energy and in the process of building muscle tissue. Creatine can be produced in the body from the amino acids arginine, glycine, and methionine. However, because of the role it plays in creating energy and muscle, many athletes are using creatine as a performance-enhancing agent.(1, 2) Creatine may enhance the performance of high-intensity, short-duration exercise, but it is not useful in endurance sports.(3) Some investigators feel that high-quality research is lacking. There is roughly an even distribution between studies reporting benefits and lack of benefits.(4)

Creatine is found in the body in muscle, brain, and blood. However, most creatine in the body is stored in muscles, where it is found in two forms. About 40 percent exists as free creatine while approximately 60 percent is phosphorylated in a form known as phosphocreatine. Creatine is converted in the body to creatine phosphate, which is a storage form of high-energy phosphate used for rapid regeneration of ATP. Creatine is used by the body to recycle adenosine diphosphate (ADP) to adenosine triphosphate (ATP). ATP is stored in the mitochondria of muscle cells and produces energy when converted into ADP. Muscle fatigue occurs when the supply of ATP runs low. Creatine helps the body to convert ADP to ATP, providing more energy to the muscles. This allows the muscles to do more work and be less susceptible to fatigue.

Studies report that creatine supplementation can result in increased power and strength, improved performance times, and increased muscle mass. Creatine is currently a legal method of enhancing performance and increasing body mass. At the 19th Annual Southwest American College of Sports Medicine Meeting, two long-term creatine studies were presented by the Exercise & Sport Nutrition Lab at the University of Memphis. Both studies reported that nine months of creatine supplementation (average dose of 5 grams per day) in athletes had no negative effects on markers of renal function(5) or muscle and liver enzymes(6) in comparison to athletes not taking creatine.

Concern does exist regarding the use of creatine. French authorities are so concerned about the safety of creatine that they have made the sale of creatine supplements illegal. Furthermore, in January 2001, France's Food Safety Agency posted warning statements regarding creatine on the Agency's WEB site. Their position is that the risks associated with taking creatine are "currently insufficiently evaluated," and that, in addition to other known side effects, long-term supplementation may present "a potential carcinogenic risk."(7) However, it is noted that a Medline search did not produce studies that linked the use of creatine with cancer or increased cancer risk.

Two surveys that show substantial numbers of high school athletes are using creatine supplementation. In one survey 16% of the athletes from 11 high schools in Tennessee admitted to using creatine;(8) in another survey, 44% of the high school athletes from a single school in a suburb of New York City reported using creatine.(9) Experts strongly recommend against the use of creatine among adolescent athletes until more is known about its safety.

Topics that warrant evaluation include creatine's influence on insulin production, feedback inhibition of endogenous creatine synthesis, and contaminants that occur in products as a result of manufacturing procedures.(10)

 Toxicities & Precautions

Creatine is readily absorbed from the stomach.

General
Although creatine seems to be relatively safe, some experts feel that appropriate studies have not been conducted to evaluate the long-term safety of high-dosage consumption.

Creatine increases both the body's overall water content and its ratio between intracellular and extracellular water. Strenuous exercise causes water loss from the extracellular space. If creatine has already caused a shift or buildup of water in intracellular spaces, an imbalance may occur. Thus, strenuous exercise can make an individual dehydrate faster, which can contribute to heat stroke and cramping due to loss of water in the extracellular space.

Although only a couple of cases have been reported, large doses of creatine coupled with intense exercise can lead to kidney dysfunction.(11, 12) Excess creatine is excreted through the kidneys. To reduce kidney burden, suggest increased fluid intake in order to dilute the contents and facilitate elimination.

Another potential problem associated with creatine use is related to possible contaminants that are produced during the manufacture of the product. Creatine is produced from sarcosine and cyanamide. This process results in the generation of variable amounts of contaminants such as dicyandiamide, dihydrotriazine, and creatinine.(12) Consumers should be advised of this and realize that consumption of large doses of creatine also increases the level of ingested contaminants. However, some companies state on their labels that their creatine products are guaranteed to be free of these contaminants. Until further toxicological studies are conducted, the effects of these contaminants are not fully understood. Also, an additional concern in Europe about creatine products has to do with the fact that the amino acid sarcosine, which is used in the production of creatine, could originate from bovine sources.

Health Conditions
Since excess creatine is excreted through the kidneys, hypertensive individuals should use caution due to fluid retention and potential increased stress on kidney function.

Side Effects
Reports have linked creatine to weight gain, cramping,(13) dehydration, diarrhea, dizziness, and on rare occasions, kidney problems. To avoid diarrhea, limit doses to no more than 5 grams per serving.

 Functions in the Body
Uses
Clinical Applications

ALS

Congestive Heart Failure

Enhancement Of Sports Performance

McArdle Disease

Neuromuscular Disease

Phosphocreatine
Creatine combines readily with phosphate to form phosphocreatine, which serves as a source of high-energy phosphate for use in anaerobic muscle activity. When muscles use ATP for energy, the ATP is broken down into ADP (adenosine diphosphate), inorganic phosphate, and energy is released. Phosphocreatine is able to react with the ADP in the body and turn inactive ADP back into the "super fuel" energy source (ATP), which means more strength and stamina for muscles.(14)

Prevent Muscle Breakdown
Studies suggest that creatine supplementation may help prevent muscle breakdown or protein catabolism.(15, 16)


 Clinical Applications
ALS
In an animal model, researchers report that oral creatine may provide benefits to patients with amyotrophic lateral sclerosis (ALS). Creatine helped to stabilize mitochondrial enzymes and provided improvement in motor performance and extended survival times.(17)
Congestive Heart Failure
In a double-blind, placebo-controlled trial, patients receiving creatine (20 gm daily for 10 days) exhibited improvements in both strength and endurance.(18) In another study, patients with congestive heart failure were tested with a device that allowed researchers to measure skeletal muscle metabolism. Patients supplemented with creatine (20 gm daily for 5 days) exhibited greater muscle endurance and improved skeletal muscle metabolism as determined by decreases in ammonia and lactate in the muscles upon exertion.(19)
Enhancement Of Sports Performance
Studies report that creatine can help improve exercise performance in high-intensity, short duration forms of exertion or competition. In one study, men ingesting creatine exhibited significant improvements in exercise performance during 80 minutes of repeated bike-sprint exercise compared to no improvement in the placebo group.(20) In a double-blind study, trained weight lifters were given either creatine or placebo capsules for 12 weeks. The amount of creatine consumed was 25 grams/day for the first week, and then 5 grams/day for the remainder of the training program. After 12 weeks, the men taking creatine reported the following significant gains compared to the placebo group: increases in body mass (6.3 percent vs 3.6 percent), increased fat-free mass (6.3 percent vs 3.1 percent), increased bench press (24 percent vs 16 percent), increased squat (32 percent vs 24 percent). No negative side effects to the supplementation were reported.(21) Another study reported that women supplementing with creatine registered similar gains.(22) A double-blind study with athletes who were trained jumpers and sprinters produced the following results. Jumpers taking creatine out-performed placebo controls by 7 percent during the first segment of the continuous jumping test, and this improvement increased to 12 percent during the second segment of the test. Runners taking creatine improved by 13 percent compared to controls on the all-out treadmill run-to-exhaustion test.(23)
McArdle Disease
In this double-blind, placebo-controlled crossover trial, 5 of 9 patients (55%) with McArdle disease responded well to creatine supplementation with a reduction of muscle complaints and improved skeletal muscle function.(24) The condition is characterized by a myophosphorylase deficiency, which causes an abnormal accumulation of glycogen in muscle tissue resulting in pain, fatigue and muscle stiffness after prolonged exertion.
Neuromuscular Disease
Based on evidence that creatine increases strength in young healthy subjects. Researchers gave creatine to 81 patients with the following neuromuscular diseases: mitochondrial cytopathies (n = 17), neuropathic disorders (n = 18), dystrophies/congenital myopathies (n = 15), inflammatory myopathies (n = 14), and miscellaneous conditions (n = 17). Two studies were conducted, using doses of 5 grams/day and 10 grams/day for five days. Body weight, handgrip, dorsiflexion, and knee extensor strength were measured before and after treatment. Creatine administration increased all measured indices in both studies, prompting the researchers to state, "short-term creatine monohydrate increased high-intensity strength significantly in patients with neuromuscular disease."(25)
 Symptoms & Causes of Deficiency
Creatine deficiency can be caused by inadequate protein intake. Symptoms of creatine deficiency include muscle fatigue and lack of energy and stamina.
 Footnotes
1 Selsby JT, DiSilvestro RA, Devor ST. Mg2+-creatine chelate and a low-dose creatine supplementation regimen improve exercise performance. J Strength Cond Res. May2004;18(2):311-5.
View Abstract
2 Lehmkuhl M, Malone M, Justice B, et al. The effects of 8 weeks of creatine monohydrate and glutamine supplementation on body composition and performance measures. J Strength Cond Res. Aug2003;17(3):425-38.
View Abstract
3 Ostojic SM. Creatine supplementation in young soccer players. Int J Sport Nutr Exerc Metab. Feb2004;14(1):95-103.
View Abstract
4 Graham AS, Hatton RC. Creatine: a review of efficacy and safety. J Am Pharm Assoc (Wash). Nov1999;39(6):803-10.
View Abstract
5 Kreider RC, et al. Long-term creatine supplementation does not affect markers of renal stress in athletes. Sports Medicine, Training and Rehabilitation. In press; 2000.
6 Almada A, et al. Long-term creatine supplementation does not affect muscle or liver enzyme efflux in athletes. Sports Medicine, Training and Rehabilitation. In press; 2000.
7 McDonough M. Associated Press wire report (Paris AP). Jan2001.
8 Ray TR, Eck JC, Covington LA, et al. Use of oral creatine as an ergogenic aid for increased sports performance: perceptions of adolescent athletes. South Med J. Jun2001;94(6):608-12.
View Abstract
9 Metzl JD, Small E, Levine SR, Gershel JC. Creatine use among young athletes. Pediatrics. Aug2001;108(2):421-5.
View Abstract
10 Benzi G. Is there a rationale for the use of creatine either as nutritional supplementation or drug administration in humans participating in a sport? Pharmacol Res. Mar2000;41(3):255-64.
View Abstract
11 Graham AS, Hatton RC. Creatine: a review of efficacy and safety. J Am Pharm Assoc (Wash). Nov1999;39(6):803-10.
View Abstract
12 Benzi G, Ceci A. Creatine as nutritional supplementation and medicinal product. J Sports Med Phys Fitness. Mar2001;41(1):1-10.
View Abstract
13 Benzi G, Ceci A. Creatine as nutritional supplementation and medicinal product. J Sports Med Phys Fitness. Mar2001;41(1):1-10.
View Abstract
14 Benzi G, Ceci A. Creatine as nutritional supplementation and medicinal product. J Sports Med Phys Fitness. Mar2001;41(1):1-10.
View Abstract
15 Persky AM, Brazeau GA. Clinical pharmacology of the dietary supplement creatine monohydrate. Pharmacol Rev. Jun2001;53(2):161-76.
View Abstract
16 Parise G, Mihic S, MacLennan D, et al. Effects of acute creatine monohydrate supplementation on leucine kinetics and mixed-muscle protein synthesis. J Appl Physiol. Sep2001;91(3):1041-7.
View Abstract
17 Klivenyi P, et al. Neuroprotective effects of creatine in a transgenic animal model of amyotrophic lateral sclerosis. Nat Med. Mar1999;5(3):347-50.
View Abstract
18 Gordon A, Hultman E, Kaijser L, et al. Creatine supplementation in chronic heart failure increases skeletal muscle creatine phosphate and muscle performance. Cardiovasc Res. Sep1995;30(3):413-8.
View Abstract
19 Andrews R, Greenhaff P, Curtis S, et al. The effect of dietary creatine supplementation on skeletal muscle metabolism in congestive heart failure. Eur Heart J. Apr1998;19(4):617-22.
View Abstract
20 Preen D, Dawson B, Goodman C, et al. Effect of creatine loading on long-term sprint exercise performance and metabolism. Med Sci Sports Exerc. May2001;33(5):814-21.
View Abstract
21 Volek JS, et al. Performance and muscle fiber adaptations to creatine supplementation and heavy resistance training. Med Sci Sports Exerc. Aug1999;31(8):1147-56.
View Abstract
22 Vandenberghe K, et al. Long-term creatine intake is beneficial to muscle performance during resistance training. J Appl Physiol. Dec1997;83(6):2055-63.
View Abstract
23 Bosco C, et al. Effect of oral creatine supplementation on jumping and running performance. Int J Sports Med. Jul1997;18(5):369-72.
View Abstract
24 Vorgerd M, Grehl T, Jager M, et al. Creatine therapy in myophosphorylase deficiency (McArdle disease): a placebo-controlled crossover trial. Arch Neurol. Jul2000;57(7):956-63.
View Abstract
25 Tarnopolsky M, Martin J. Creatine monohydrate increases strength in patients with neuromuscular disease. Neurology. Mar1999;52(4):854-7.
View Abstract
 
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