Creatine Stats & Data
CVSVTCORWBXHQV-UHFFFAOYSA-NPharmacology
DrugBankDescription
An amino acid derivative that occurs in vertebrate tissues and in urine. In muscle tissue, creatine generally occurs as phosphocreatine. Creatine is excreted as creatinine in the urine.
Mechanism of Action
In the muscles, a fraction of the total creatine binds to phosphate - forming creatine phosphate. The reaction is catalysed by creatine kinase, and the result is phosphocreatine (PCr). Phosphocreatine binds with adenosine diphosphate to convert it back to ATP (adenosine triphosphate), an important cellular energy source for short term ATP needs prior to oxidative phosphorylation.
Pharmacodynamics
Creatine is a essential, non-proteinaceous amino acid derivative found in all animals. It is synthesized in the kidney, liver, and pancreas from L-arginine, glycine and L-methionine. Following its biosynthesis, creatine is transported to the skeletal muscle, heart, brain and other tissues. Most of the creatine is metabolized in these tissues to phosphocreatine (creatine phosphate). Phosphocreatine is a major energy storage form in the body. Supplemental creatine may have an energy-generating action during anaerobic exercise and may also have neuroprotective and cardioprotective actions.
Indication
For nutritional supplementation, also for treating dietary shortage or imbalance.
Elimination
Phosphocreatine is eliminated renally. The end result of creatine degredation is the product creatinine, which enters the bloodstream from its storage sites in body muscle. When creatinine enters the renal parenchyma it is filtered in the renal glomerulus to be excreted in the urine.
Receptor Profile
Receptor Actions
There are no clinically significant side-effects of creatine supplementation acutely. Numerous trials have been conducted in humans with varying dosages, and the side-effects have been limited to gastrointestinal distress (from too much creatine consumption at once) and cramping (from insufficient hydration). Studies that use a dosage range typical of creatine supplementation (in the range of 5g a day following an acute loading period) note increases to total body water of 6.2% (3.74lbs) over nine weeks, and 1.1kg (2.42 lbs) over 42 days. This effect may be responsible for creatine's capability to increase perceived body weight. Regardless, it is strongly recommended that one is familiar with harm reduction practices when using creatine.
Carcinogenicity
No indication of carcinogenicity to humans (not listed by IARC).
Effect Profile
CuratedStrong focus with moderate stimulation, low euphoria and anxiety/jitters
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Acute tolerance: develops within a single session — the reset numbers above apply after sustained heavy use, not after one binge. Within-session tachyphylaxis usually resets largely overnight.