A Human Pharmacological Study Comparing Conventional Heparin and a Low Molecular Weight Heparin Fragment

Abstract

SummaryThe pharmacokinetics of a heparin fragment of low molecular weight (LMWH) of 4000-5000 D and unfractioned standard heparin (UFH) have been studied after i. v. injections of different doses and infusions in 8 humans.The heparin activity was significantly higher and the effect on APTT lower after LMWH fragment as compared to UFH in the same doses.The half-life of heparin activity was about 1 hr for UFH and about 2 hr for LMWH. LMWH was found to be eliminated according to first order kinetics and there were no signs of dose dependency.

Heparin and Its Low Molecular Weight Derivatives: Anticoagulant and Antithrombotic Properties

“…Further, the duration of the activity of Fragmin was significantly longer than that of heparin, indicating that 1 injection dailycompared to 2-3 injections in current usagewould be sufficient to provide adequate thrombosis prophylaxis. On intravenous in jection, the half-life of Fragmin was twice that of standard heparin [21], In summary, certain preparations of low molecular weight heparin have a good doserelated prophylactic effect against thrombo sis in the rabbit at doses which do not ad versely affect hemostasis in vivo. Other properties such as the relatively minor effects on platelets [8,22] and on lipolysis [18,23] and the favorable pharmacokinetics make these preparations highly interesting from the clinical point of view.…”

Laboratory Studies on the Intravenous and Subcutaneous Administration of PK 10169 in Man

“…Due to better bioavailability, less toxic effects (bleeding, osteoporosis, hep arin-induced thrombocytopenia) and pre dictable clinical effects, these agents have been favored over conventional heparin. Many controlled clinical trials and human studies have also reported on the efficacy of these fractions as therapeutic and prophylac tic agents [11][12][13][14][15][16][17][18]. These agents have been reported to produce their antithrombotic ac tions for periods of up to 24 h after a single dose; however, the relationship between the available laboratory parameters and their clinical effects has not been established up to this time [1,17,18].…”

Randomized Trial of a Low-Molecular-Weight Heparin (Kabi 2165) versus Adjusted-Dose Subcutaneous Standard Heparin in the Prophylaxis of Deep-Vein Thrombosis after Elective Hip Surgery

“…LMWHs are characterized by better phar macokinetic properties than standard hepa rin, mainly a longer half-life and better bio availability [22][23][24]. Recently, several wellconducted, randomized, clinical trials have clearly established that LMWHs adminis tered once daily are as effective as standard heparin given twice daily in preventing post operative thrombosis in general surgery [14][15][16][17].…”