Fosphenytoin:临床药物动力学和比较优势在急性发作的治疗。

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费舍尔JH, Patel电视,费舍尔PA

Fosphenytoin:临床药物动力学和比较优势在急性发作的治疗。

Pharmacokinet。2003; 42(1):长篇论文。doi: 10.2165 / 00003088-200342010-00002。

PubMed ID
12489978 (在PubMed
]
文摘

Fosphenytoin磷酸是一种酯前体药物开发替代静脉注射苯妥英的急性发作的治疗。优势包括更方便和快速静脉注射管理、可用性肌内注射,低电位在注射部位局部不良反应。缺点包括瞬时感觉异常和瘙痒的发生快速注入率,和成本。Fosphenytoin高度绑定(93 - 98%),血浆蛋白。饱和绑定在更高的血浆浓度占其体积分布和间隙的增加与增加剂量和输注速率。Fosphenytoin完全消除通过血液和组织新陈代谢苯妥英磷酸酶。派生苯妥英的生物利用度相对于静脉注射苯妥英后静脉注射或肌内管理大约是100%。转换的半衰期fosphenytoin苯妥英范围从7 - 15分钟。更快的静脉输液率和竞争取代苯妥英来自血浆蛋白结合位点推迟fosphenytoin补偿预期的转化苯妥英的等离子体。游离苯妥英等离子体浓度通过静脉fosphenytoin加载剂量的100 - 150年苯妥英钠或50 - 100毫克当量/分钟相媲美,并取得相似的时候,那些克分子数相等的剂量静脉注射苯妥英的50(最大推荐率)或20 - 40毫克/分钟,分别。 The rapid achievement of effective concentrations permits the use of fosphenytoin in emergency situations, such as status epilepticus. Following intramuscular administration, therapeutic phenytoin plasma concentrations are observed within 30 minutes and maximum plasma concentrations occur at approximately 30 minutes for fosphenytoin and at 2-4 hours for derived phenytoin. Plasma concentration profiles for fosphenytoin and total and unbound phenytoin in infants and children closely approximate those in adults following intravenous or intramuscular fosphenytoin at comparable doses and infusion rates. Earlier and higher unbound phenytoin plasma concentrations, and thus an increase in systemic adverse effects, may occur following intravenous fosphenytoin loading doses in patients with a decreased ability to bind fosphenytoin and phenytoin (renal or hepatic disease, hypoalbuminaemia, the elderly). Close monitoring and reduction in the infusion rate by 25-50% are recommended when intravenous loading doses of fosphenytoin are administered in these patients. The potential exists for clinically significant interactions when fosphenytoin is coadministered with other highly protein bound drugs. The pharmacokinetic properties of fosphenytoin permit the drug to serve as a well tolerated and effective alternative to parenteral phenytoin in the emergency and non-emergency management of acute seizures in children and adults.

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