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Review ArticleReview

Clinical Pharmacology of the Dietary Supplement Creatine Monohydrate

Adam M. Persky and Gayle A. Brazeau
Pharmacological Reviews June 2001, 53 (2) 161-176;
Adam M. Persky
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida
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Gayle A. Brazeau
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida
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Abstract

Creatine is a dietary supplement purported to improve exercise performance and increase fat-free mass. Recent research on creatine has demonstrated positive therapeutic results in various clinical applications. The purpose of this review is to focus on the clinical pharmacology and therapeutic application of creatine supplementation. Creatine is a naturally occurring compound obtained in humans from endogenous production and consumption through the diet. When supplemented with exogenous creatine, intramuscular and cerebral stores of creatine and its phosphorylated form, phosphocreatine, become elevated. The increase of these stores can offer therapeutic benefits by preventing ATP depletion, stimulating protein synthesis or reducing protein degradation, and stabilizing biological membranes. Evidence from the exercise literature has shown athletes benefit from supplementation by increasing muscular force and power, reducing fatigue in repeated bout activities, and increasing muscle mass. These benefits have been applied to disease models of Huntington's, Parkinson's, Duchenne muscular dystrophy, and applied clinically in patients with gyrate atrophy, various neuromuscular disorders, McArdle's disease, and congestive heart failure. This review covers the basics of creatine synthesis and transport, proposed mechanisms of action, pharmacokinetics of exogenous creatine administration, creatine use in disease models, side effects associated with use, and issues on product quality.

Footnotes

  • ↵1 Address for correspondence: Adam M. Persky, Department of Pharmaceutics, University of Florida, College of Pharmacy, 100494 J.H.M.H.C., Gainesville, FL 32610. E-mail:apersky{at}ufl.edu

  • ↵2 Present address: Department of Pharmacy Practice and Pharmaceutics, College of Pharmacy, State University of New York at Buffalo, Amherst, NY 14260-1200.

  • Published, Pharmacological Reviews Fast Forward, May 10, 2001, DOI 10.1124/pharmrev1

  • The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 53 (2)
Pharmacological Reviews
Vol. 53, Issue 2
1 Jun 2001
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Review ArticleReview

Clinical Pharmacology of the Dietary Supplement Creatine Monohydrate

Adam M. Persky and Gayle A. Brazeau
Pharmacological Reviews June 1, 2001, 53 (2) 161-176;

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Review ArticleReview

Clinical Pharmacology of the Dietary Supplement Creatine Monohydrate

Adam M. Persky and Gayle A. Brazeau
Pharmacological Reviews June 1, 2001, 53 (2) 161-176;
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  • Article
    • Abstract
    • I. Introduction
    • II. Creatine Synthesis and Transport
    • III. Mechanisms of Action
    • IV. Pharmacokinetics
    • V. Therapeutic Usage
    • VI. Side Effects
    • VII. Products
    • VIII. Conclusion
    • Acknowledgments
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