Ramsay R E, DeToledo J
Department of Neurology, University of Miami, FL, USA.
Neurology. 1996 Jun;46(6 Suppl 1):S17-9. doi: 10.1212/wnl.46.6_suppl_1.17s.
Fosphenytoin is a water-soluble disodium phosphate ester of phenytoin that is converted in plasma to phenytoin. Fosphenytoin is compatible with most common i.v. solutions and can be administered safely through the i.m.route. An additional safety factor is the absence of propylene glycol in the fosphenytoin formulation. Propylene glycol is used as a vehicle in the i.v. phenytoin preparation and by itself may produce serious cardiovascular complications. Studies of the pharmacokinetics, safety, and tolerance of i.v. fosphenytoin have demonstrated that fosphenytoin produces phenytoin plasma concentrations similar to those achieved with oral and i.v. phenytoin, but without significant cardiovascular effects and only minimal discomfort at the injection site. Aside from local reactions, the most common adverse events associated with fosphenytoin have been pruritus and reactions typical of phenytoin (e.g., dizziness, somnolence, and ataxia). Fosphenytoin represents a significant advance in the treatment of patients with seizures who require parenteral therapy.
磷苯妥英是苯妥英的水溶性磷酸二钠酯，在血浆中可转化为苯妥英。磷苯妥英与大多数常用静脉输液相容，可通过肌内途径安全给药。另一个安全因素是磷苯妥英制剂中不含丙二醇。丙二醇用作静脉注射苯妥英制剂的溶媒，其本身可能会产生严重的心血管并发症。对静脉注射磷苯妥英的药代动力学、安全性和耐受性研究表明，磷苯妥英产生的苯妥英血浆浓度与口服和静脉注射苯妥英所达到的浓度相似，但无明显心血管效应，且注射部位仅有轻微不适。除局部反应外，与磷苯妥英相关的最常见不良事件为瘙痒和苯妥英典型的反应（如头晕、嗜睡和共济失调）。对于需要肠外治疗的癫痫患者，磷苯妥英是治疗方面的一项重大进展。
