磷丙泊酚研究进展

Advances in research of fospropofol

该文对丙泊酚(propofol)前体药磷丙泊酚(fospropo-fol,FP)的特点及研究新进展进行综述。临床药代动力学研究表明:FP进入脑组织能迅速实现人体血药浓度平衡,没有药效滞后现象,半衰期、药时曲线下面积(AUC)明显延长或增加,中等程度镇静作用持续时间明显延长。FP的临床药效学研究指出,在大脑中,FP分解产生的丙泊酚和经典丙酚药物作用类似;持续静脉注射FP可引起剂量依赖性;可减少FP的使用剂量;可避免经典异丙酚作用持续时间短、溶解度差,注射部位疼痛、高血脂等不良反应。它的作用机制与对突触后膜的γ-氨基丁酸受体的作用、对瞬时受体电位TRPV1和TRP A1活化作用、对α-氨基羟甲基恶左丙酸(AMPA)受体等作用有关。FP是一种新型、较高效和长效、副作用较少并可使病人清醒冷静状态下接受内窥镜或小手术的检查与治疗的中等程度镇静剂。

The article reviews the characteristics and new progress of fospropofol（FP）,propofol prodrug.Clinical pharmacokinetics research indicated that FP achieved rapidly blood drug concentration balance after entering brain organization without any lag of drug action.The half-life time and medicine area under the curve（AUC） were increased or prolonged obviously.Clinical pharmacodynamics research pointed out that the effects of propofol which was metabolised and generated by FP were similar to those of classical propofol in cerebrum.FP effects were in dosage dependent manner under the condition of continual intravenous injection,and FP administration dosage could be reduced.Untowarding reactions could be avoided such as short active duration,lower solubility,the ache in injection spot,hyperlipemia induced by classical propofol.Its mechanisms were related to the activation on GABA receptor,transient receptor potential（TRP V1 and TRP A1） or α-AMPA in the post membrane of synapse.FP is a kind of effective moderate sedative with highly,prolonged effect and lower side effect,which can be used in endoscope examinations or minor surgeries to patients under conscious and calm condition.