Fareed Jawed, Hoppensteadt Debra, Walenga Jeanine, Iqbal Omer, Ma Qing, Jeske Walter, Sheikh Taqdees
Department of Pathology, Loyola University Medical Center, Maywood, Illinois, USA.
Clin Pharmacokinet. 2003;42(12):1043-57. doi: 10.2165/00003088-200342120-00003.
Enoxaparin is a low-molecular-weight heparin (LMWH) that differs substantially from unfractionated heparin (UFH) in its pharmacodynamic and pharmacokinetic properties. Some of the pharmacodynamic features of enoxaparin that distinguish it from UFH are a higher ratio of anti-Xa to anti-IIa activity, more consistent release of tissue factor pathway inhibitor, weaker interactions with platelets and less inhibition of bone formation. Enoxaparin has a higher and more consistent bioavailability after subcutaneous administration than UFH, a longer plasma half-life and is less strongly bound to plasma proteins. These properties mean that enoxaparin provides a more reliable anticoagulant effect without the need for laboratory monitoring, and also offers the convenience of once-daily administration. Clinical studies have confirmed that these pharmacological advantages translate into improved outcomes. There are important pharmacokinetic and pharmacodynamic differences between enoxaparin, other LMWHs and UFH, and therefore these molecules cannot be regarded as interchangeable.
依诺肝素是一种低分子量肝素(LMWH),其药效学和药代动力学特性与普通肝素(UFH)有很大不同。依诺肝素与普通肝素不同的一些药效学特征包括抗Xa与抗IIa活性的比例更高、组织因子途径抑制剂的释放更一致、与血小板的相互作用较弱以及对骨形成的抑制作用较小。皮下给药后,依诺肝素比普通肝素具有更高且更一致的生物利用度、更长的血浆半衰期,并且与血浆蛋白的结合力较弱。这些特性意味着依诺肝素无需实验室监测就能提供更可靠的抗凝效果,还具有每日一次给药的便利性。临床研究证实这些药理学优势转化为了更好的治疗结果。依诺肝素、其他低分子量肝素和普通肝素之间存在重要的药代动力学和药效学差异,因此这些分子不能被视为可互换的。