Research Progress in Pharmacokinetics of Phosphocreatine a Cardioprotective Agent with a Dual Antiplatelet Activity - Abstract
Phosphocreatine (PCr), a natural physiological active high energy phosphate compound, plays a pivotal role in maintaining energy homeostasis via acting as a temporal and spatial buffers of bodily energy. Exogenous PCr has been developed as a cardioprotective agent with a dual antiplatelet activityand has found wide range of clinical application. Since PCr is known to have many beneficial effects , it is important to elucidate pharmacokinetic(PK) properties of PCr to get deep insight to action mechanism and clinical rational uses. Thus, here we review its PK profiles in animals and humans as well as possible transmembrane transport mechanism based on the present writer’s years of devoted research and published reports. Accruing evidence shows that PCr belongs to a twocompartment model drug. Regardless of animal species and humans, PCr exhibits rapid elimination from body. IP-HPLC and HPLC-MS/MS bioanalysis have demonstrated that most of PCr entering systemic circulation is converted to creatine (Cr). Iv administration of PCr resulted in elevated ATP level in heart and RBC. Cr as an active metabolite has proved to partially mediate PCr hemorheological improvement. PCr can be taken up by myocardiocytes, in spite of slow transcellular rate, via some special and hypothetical transport mechanisms.