Pharmacological and toxicological properties of creatinol O-phosphate. A review

N-Methyl-N-(beta-hydroxyethyl)guanidine O-phosphate (creatinol O-phosphate, COP) has proved to possess anti-ischemic and anti-arrhythmic activities associated with improved ionic balance and heart performance. These activities, which have also been shown in clinical studies, are more evident in pharmacological and clinical conditions involving a hypoxic damage of the heart muscle. Pharmacokinetic studies have shown that absorption of COP administered i.m. is complete. COP is distributed in all organs, and in particular, in the kidney, liver and myocardium. After being dephosphorylated, this drug is eliminated with urine. Dephosphorylation of COP occurs in the kidney and liver. COP crosses the membrane of the myocardial cell, concentrating in the cytosoluble fraction. The results of the toxicological studies confirm that COP has no side effects, is excellently tolerated and has a favourable therapeutic index.