Creatine (CR) is a naturally occurring substance, produced in our bodies in the liver from the amino acids L-Arginine, L-Glycine and L-Methionine(1).Daily turnover of creatine occurs at a rate of ~2g/day via non-enzymatic, irreversible degradation of creatine and creatinephosphate to creatinine(2). Creatinine freely diffuses out of the cell and is easily filtered by the healthy kidney(3). This loss is normally replaced by endogenous CR synthesis, as well as exogenous (dietary) sources of creatine such as meat(4). However, vegetarians typically have lower levels of creatine in serum and muscle(5), and experience a greater elevatio nin muscle CR following dietary supplementation(6).
Due in part to its relatively large mass, over 95% of the body’s store of creatine is found in skeletal muscle (~120g in a 70kg male(1)), where it participates in energetic processes to restore ATP and shuttle high energy phosphate in the form of CR phosphate from the mitochondria to the myofibrillar cross-bridges to generate muscular contractile force(7).
Because CR is a charged molecule(2) it must normally be transported across cell membranes by a CR transport protein, including that of the gut (for oral absorption) and skeletal muscle (for uptake into the cell)(8-11). Following a period of CR loading, all of a 5g daily dose of CR monohydrate is recoverable in the urine as CR or its degradative by-product creatinine(12), suggesting that in most individuals, absorption of creatine monohydrate is complete, at least at these doses.
However, anecdotal reports of gastric distress(13) suggest that some individuals may have difficulty absorbing CR in the amounts provided by a CR supplement. To aid in trans-membrane movement, ethyl esterification (akin to the acetylation of salicylic acid to make aspirin, a.k.a. acetylsalycylic acid) of drugs or other substances is commonly employed to bypass normal means of uptake, enhance bioavailability and reduce side effects(14). Although scientific investigation of the pharmacokinetics CR ethyl ester (CEE) is lacking, anecdotal reports of increased body mass without gastric discomfort are consistent with the abrupt weight gain noted innumerous research studies of CR monohydrate supplementation(15-22), suggesting the CEE does indeed make its way to skeletal muscle.
The ergogenic and anabolic effects of CR have been under investigation for more than a decade, with widely inconsistent results(23). However, taken as a whole the large body of literature suggests that supplemental CR can have ergogenic effects, especially during brief duration, high intensity exercise (such as resistance exercise) and in individuals who have low muscle CR levels, such as vegetarians, and those with abnormalities of CR metabolism(21, 24,25). Creatine may also have an anti-inflammatory action(26, 27), aid in nerve re-generation(28) have an anabolic or anti-catabolic effect on skeletal muscle(29-32), although the literature is not consistent in this regard(33,34), and/or prevent performance decrements during periods of high intensity training(35).
By aiding in muscular performance (training stimulus), affecting recovery via altering muscle protein metabolism or nerve function, CR would hypothetically enhance adaptation to exercise training, including the muscular growth adaptation to resistance training. The degree to which this occurs is likely dependent upon the degree to which supplemental CR increases muscle CR as well as body mass during the initial period of CR supplementation(36, 37).
Individuals should consult with their physician before beginning CEE supplementation, especially those with pre-existing renal disease.
Adverse medical side effects of short and long-term CR supplementation are generally absent in the scientific literature(13, 23,38-42), although individual cases of those experiencing reversable renal dysfunction in association with CR supplementation have been reported(43).
CR can be taken in doses of 2-5g / day to elevate or maintain elevated muscle creatine levels(12,44, 45). Consuming CR as CEE may even lower the amount of CR needed for this effect.
CR supplementation improves blood lipid profile by elevating HDL concentration and reducing total cholesterol, LDL, and blood triglyceride levels(46,47). CEE could be taken with with Alpha Lipoic Acid to enhance its uptake(48),as well as with carbohydrate to enhance glycogen synthesis(49). Taking CEE, along with Vitamin C, may reduce muscle soreness or inflammation(26, 27). CEE could also be used in a post-workout, weight gainer or carb-up drink along Alpha Lipoic Acid, arginine (to optimize nutrient delivery), waxy maize and/or other carbohydrate source, and a high quality protein blend .
Creatine Ethyl Ester HCL.
This material is EXTREMELY hazardous if not dosed properly. A milligram sensitive scale must be used to ensure that the proper dosage is achieved. Please be extremely careful when dosing this material. Improper dosing may result in sickness, injury, or death. If you are currently pregnant or nursing, consult a physician prior to use. Keep out of the reach of children.
Although this product may not contain one or all of the following, this product is manufactured in a facility that handles milk, soy, egg, peanut, nut, tree, fish, crustaceans/shellfish, and wheat products.
Use the table below to approximate the gram equivalent weight for a given level measuring spoon (US Standard). Please note that accurate dosing should only be done with a recommended calibrated scale.
|Measuring Spoon (level) ||g ||mg |
|90cc Scoop ||30.6 ||30554 |
|70cc Scoop ||23.8 ||23764 |
|29.6cc Scoop ||10.0 ||10049 |
|25cc Scoop ||8.5 ||8487 |
|Tablespoon ||5.0 ||5021 |
|10cc Scoop ||3.4 ||3395 |
|½ Tablespoon ||2.5 ||2511 |
|Teaspoon ||1.7 ||1674 |
|½ Teaspoon ||0.8 ||837 |
|1.7cc Scoop ||0.6 ||577 |
|¼ Teaspoon ||0.4 ||418 |
|1/8 Teaspoon ||0.2 ||209 |
|1/16 Teaspoon ||0.1 ||105 |
|1/32 Teaspoon ||0.1 ||52 |
DISCLAIMER: The above description is provided for information only and does not constitute medical advice. Please consult your physician or the appropriately licensed professional before engaging in a program of exercise or nutritional supplementation. No information in this site has been reviewed by the FDA. No product is intended to treat, diagnose, or cure any disease.
1. Walker,J.B., Creatine:biosynthesis, regulation, and function.Adv Enzymol Relat Areas Mol Biol, 1979. 50:p. 177-242.
2. Wyss,M. and T. Wallimann, Creatinemetabolism and the consequences of creatine depletion in muscle.Mol. Cell. Biochem., 1994. 133/134:p. 51-66.
3. Hoogwerf,B.J., et al., UrineC-peptide and creatinine (Jaffe method) excretion in healthy youngadults on varied diets: sustained effects of varied carbohydrate,protein, and meat content. AmJ Clin Nutr, 1986. 43(3):p. 350-60.
4. Harris,R.C., et al., The concentration of creatine in meat, offal and commercial dog food.Research in Veterinary Science, 1997. 62(1):p. 58-62.
5. Delanghe,J., et al., Normalreference values for creatine, creatinine, and carnitine are lower invegetarians. Clin Chem, 1989.35(8):p. 1802-3.
6. Harris,R.C., et al., Elevationof creatine in resting and exercised muscle of normal subjects bycreatine supplementation.Clin. Sci.(Colch). 1992. 83:p. 367-374.
7. Bessman,S.P. and F. Savabi, Therole of the phosphcreatine energy shuttle in exercise and musclehypertrophy, in Proceedingsof the 7th International Biochemistry of Exercise Conference held onJune 1-4, 1988 in London, Ontario, Canada,A.W. Taylor, Editor. 1990, Human Kinetics Publishers: Champaign,IL.p. 167-178.
8. Sora,I., et al., Thecloning and expression of a human creatine transporter.Biochem Biophys Res Commun, 1994. 204(1):p. 419-27.
9. Guimbal,C. and M.W. Kilimans, ANa+-dependant creatine transporter in rabbit brain, muscle, heart,and kidney. J.Biol.Chem.,1998. 268:p. 8418-8421.
10. Nash,S.R., et al., Cloning,pharmacological characterization, and genomic localization of thehuman creatine transporter.Receptors Channels, 1994. 2(2):p. 165-74.http://www.ncbi.nlm.nih.gov/cgi-bin/Entrez/referer?http://www.ncbi.nlm.nih.gov/htbin-post/Omim/getmim%3ffield=medline_uid&search=7953292
11. Proujansky,R., et al., Cloning and characterization of a human intestinal creatine transporter.Gastroenterology, 1995. 108(4):p. A314.
12. Vandenberghe,K., et al., Long-termcreatine intake is beneficial to muscle performance during resistancetraining. J. Appl. Physiol.,1997. 83:p. 2055-2063.
13. Bizzarini,E. and L. De Angelis, Isthe use of oral creatine supplementation safe?J Sports Med Phys Fitness, 2004. 44(4):p. 411-6.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15758854
14. Beaumont,K., et al., Designof ester prodrugs to enhance oral absorption of poorly permeablecompounds: challenges to the discovery scientist.Curr Drug Metab, 2003. 4(6):p. 461-85.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14683475
15. Balsom,P.D., et al., Creatinesupplementation per se does not enhance endurance exerciseperformance. Acta PhysiolScand, 1993. 149:p. 521-523.
16. Balsom,P.D., et al., Creatinesupplementation and dynamic high-intensity intermittent exercise.Scand J Med Sci.Sports, 1993. 3:p. 143-149.
17. Greenhaff,P.L., et al., Effectof oral creatine supplementation on skeletal muscle phosphocreatineresynthesis. Am J Physiol,1994. 266:p. E725-E730.
18. Söderlund,K., et al., Creatinesupplementation and high-intensity exercise: Influence on performanceand muscle metabolism. Clin.Sci.(Colch). 1994. 87:p. 120.
19. Stroud,M.A., et al., Effectof oral creatine supplementation on respiratory gas exchange andblood lactate accumulation during steady-state incremental treadmillexercise and recovery in man.Clin. Sci.(Colch). 1994. 87:p. 707-710.
20. McNaughton,L.R., et al., Theeffects of creatine supplementation on high-intensity exerciseperformance in elite performers.Eur. J. Appl. Physiol. Occup. Physiol., 1998. 78(3):p. 236-40.
21. Tarnopolsky,M.A., et al., Arandomized, controlled trial of creatine monohydrate in patients withmitochondrial cytopathies.Muscle Nerve, 1997. 20:p. 1502-1509.
22. Ziegenfuss,T.N., et al., Acutefluid volume changes in men during three days of creatinesupplementation. JEPonline,1998. 1:p. Issue 3. http://www.css.edu/users/tboone2/asep/jan13d.htm
23. Lemon,P.W., Dietarycreatine supplementation and exercise performance: why inconsistentresults? Can J Appl Physiol,2002. 27(6):p. 663-81.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=12501003
24. Tarnopolsky,M. and J. Martin, Creatinemonohydrate increases strength in patients with neuromusculardisease. Neurology, 1999.52(4):p. 854-857.
25. Sipilä,I., et al., Supplementarycreatine as a treatment for gyrate atrophy of the choroid and retina.N Engl J Med, 1981. 304(15):p. 867-70.
26. Santos,R.V., et al., Theeffect of creatine supplementation upon inflammatory and musclesoreness markers after a 30km race.Life Sci, 2004. 75(16):p. 1917-24.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15306159
27. Khanna,N.K. and B.R. Madan, Studieson the anti-inflammatory activity of creatine.Arch Int.Pharmacodyn.Ther., 1978. 231:p. 340-350.
28. Ozkan,O., et al., Effectof systemic creatine monohydrate supplementation on denervated muscleduring reinnervation: experimental study in the rat.J Reconstr Microsurg, 2005. 21(8):p. 573-9.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16292735
29. Ingwall,J.S., et al., Creatine:a possible stimulus for skeletal and cardiac muscle hypertrophy.Recent.Adv.Stud.Cardiac.Struct.Metab., 1975. 8:p. 467-481.
30. Ingwall,J.S., Creatineand the control of muscle-specific protein synthesis in cardiac andskeletal muscle. Circ.Res.,1976. 38:p. I115-I123.
31. Rogozkin,V.A., Therole of low molecular weight compounds in the regulation of skeletalmuscle genome activity during exercise.Med Sci.Sports, 1976. 8:p. 1-4.
32. Ziegenfuss,T.N., et al., Acutecreatine ingestion: Effects on muscle volume, anaerobic power, fluidvolumes and protein turnover.Med.Sci.Sports Exerc., 1997. 29(5Supp.): p. S127.
33. Fry,D.M. and M.F. Morales, Areexamination of the effects of creatine on muscle protein synthesisin tissue culture. J CellBiol, 1980. 84:p. 294-297.
34. Parise,G., et al., Effectsof acute creatine monohydrate supplementation on leucine kinetics andmixed-muscle protein synthesis.J Appl Physiol, 2001. 91(3):p. 1041-7.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=11509496
35. Volek,J.S., et al., Theeffects of creatine supplementation on muscular performance and bodycomposition responses to short-term resistance training overreaching.Eur J Appl Physiol, 2004. 91(5-6):p. 628-37.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14685870
36. Kilduff,L.P., et al., Effectsof creatine on body composition and strength gains after 4 weeks ofresistance training in previously nonresistance-trained humans.Int J Sport Nutr Exerc Metab, 2003. 13(4):p. 504-20.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14967873
37. Burke,D.G., et al., Effectof creatine and weight training on muscle creatine and performance invegetarians. Med Sci SportsExerc, 2003. 35(11):p. 1946-55.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14600563
38. Poortmans,J.R., et al., Effectof short-term creatine supplementation on renal responses in men.Eur J. Appl. Physiol., 1997. 76(6):p. 566-7.
39. Poortmans,J.R. and M. Francaux, Renaldysfunction accompanying oral creatine supplements [letter].Lancet, 1998. 352(9123):p. 234.
40. Poortmans,J.R. and M. Francaux,Long-term oral creatinesupplementation does not impair renal function in healthy athletes[see comments]. Med Sci SportsExerc, 1999. 31(8):p. 1108-10.
41. Graham,A.S. and R.C. Hatton,Creatine: a review of efficacyand safety. J Am Pharm Assoc(Wash), 1999. 39(6):p. 803-10; quiz 875-7.
42. Mayhew,D.L., et al., Effectsof long-term creatine supplementation on liver and kidney functionsin American college football players.Int J Sport Nutr Exerc Metab, 2002. 12(4):p. 453-60.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=12500988
43. Koshy,K.M., et al., Interstitialnephritis in a patient taking creatine [letter].N Engl J Med, 1999. 340(10):p. 814-5.http://www.ncbi.nlm.nih.gov/cgi-bin/Entrez/referer?http://www.nejm.org/content/scripts/search/page.asp%3fvolume=340&page=814
44. Balsom,P.D., et al., Creatinein humans with special reference to creatine supplementation.Sports Med, 1994. 18:p. 268-280.
45. Hultman,E., et al., Musclecreatine loading in men. J.Appl. Physiol., 1996. 81:p. 232-237.
46. Earnest,C.P., et al., High-performancecapillary electrophoresis-pure creatine monohydrate reduces bloodlipids in men and women. Clin.Sci.(Colch). 1996. 91:p. 113-118.
47. Kreider,R.B., et al., Effectsof creatine supplementation on body composition, strength, and sprintperformance. Med Sci SportsExerc, 1998. 30(1):p. 73-82.
48. Burke,D.G., et al., Effectof alpha-lipoic acid combined with creatine monohydrate on humanskeletal muscle creatine and phosphagen concentration.Int J Sport Nutr Exerc Metab, 2003. 13(3):p. 294-302.http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14669930
49. Green,A.L., et al., Creatineingestion augments muscle creatine uptake and glycogen synthesisduring carbohydrate feeding in man.J.Physiol.Lond., 1996. 491:p. 63P-64P.