Overview of low molecular weight heparins and heparinoids: basic and clinical aspects.

J Hirsh
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Abstract

Low molecular weight heparins (LMWHs) are fragments derived by enzymatic or chemical depolymerization of standard heparin (SH). They are approximately one-third the size of SH, with a mean molecular weight of 4,000 to 6,000. LMWHs produce less bleeding for equivalent antithrombotic effects than SH in experimental animals. Clinically LMWHs exhibit different pharmacokinetics than SH; they have much better bioavailability at low doses, a longer half life than SH and clearance pattern which is dose independent. In addition, LMWHs have a more predictable dose response than SH. These differences in pharmacokinetic properties occur because in contrast to SH, LMWHs show minimal binding to endothelium and plasma proteins. Clinical trials have demonstrated that LMWHs are effective and safe for the prevention and treatment of venous thromboembolism. In patients having orthopaedic surgery, LMWHs are more effective than low dose SH, more effective than dextran or warfarin. They are also more effective than SH in preventing venous thrombosis in stroke patients and those suffering spinal injury. In addition, recent studies suggest that LMWHs administered by subcutaneous injection in fixed weight-adjusted doses are at least as effective and safe as adjusted dose SH given by continuous intravenous infusion for the treatment of venous thrombosis.

低分子肝素和类肝素综述:基础和临床方面。
低分子量肝素(LMWHs)是标准肝素(SH)通过酶解或化学解聚得到的片段。它们的大小约为SH的三分之一,平均分子量为4,000至6,000。在实验动物中,LMWHs产生的出血比SH少,具有同等的抗血栓作用。临床低分子肝素表现出与SH不同的药代动力学;它们在低剂量下具有更好的生物利用度,比SH有更长的半衰期和与剂量无关的清除模式。此外,低分子腰油比SH具有更可预测的剂量反应。这些药代动力学特性的差异是因为与SH相比,低分子腰油与内皮和血浆蛋白的结合最小。临床试验表明,低分子肝素对预防和治疗静脉血栓栓塞是有效和安全的。在接受骨科手术的患者中,lmwh比低剂量SH更有效,比右旋糖酐或华法林更有效。它们在预防脑卒中患者和脊髓损伤患者静脉血栓形成方面也比SH更有效。此外,最近的研究表明,在治疗静脉血栓形成方面,皮下注射固定体重调整剂量的低分子肝素至少与持续静脉输注调整剂量的SH一样有效和安全。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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