Effects of an enzymatically depolymerized heparin as compared with conventional heparin in healthy volunteers

Thromb Haemost. 1987 Feb 3;57(1):97-101.

Abstract

A low molecular weight heparin (LMW-heparin) with a mean molecular weight of 4900 dalton was prepared by controlled enzymatic depolymerization of conventional porcine mucosal heparin. The effects of 2,500, 5,000 and 10,000 U (XaI; 29, 58 and 116 mg) on factor Xa inhibition (XaI), factor IIa inhibition (IIaI), APTT, AT III and platelet count were compared to those of 5,000 U (XaI; 26 mg) of conventional heparin given s.c. to 6 healthy volunteers. 5,000 U (XaI; 58 mg) of LMW-heparin was given i.v. A dose related response with regard to the XaI and the IIa-inhibitory activities with peak values at 4 hours after the s.c. injections was obtained. An increase of the XaI/IIaI ratio over the time after injection was seen only after i.v. administration of the LMW-heparin. The APTT was only slightly prolonged and remained within normal range after s.c. injection. AT III and platelet counts were unaffected. The biological half life of the LMW-heparin was 111 minutes if assayed by Xa inhibition, 76 minutes if assayed by IIa inhibition and 40 minutes if assayed by APTT. A strong correlation between the XaI activities obtained and body weight was seen, indicating that LMW-heparin should be administered individually according to body weight.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antithrombin III / analysis
  • Body Burden
  • Factor X / antagonists & inhibitors
  • Factor Xa
  • Female
  • Heparin / metabolism
  • Heparin / pharmacology*
  • Heparin Lyase
  • Humans
  • Injections, Intravenous
  • Injections, Subcutaneous
  • Male
  • Partial Thromboplastin Time
  • Polymers
  • Polysaccharide-Lyases / pharmacology
  • Protein Conformation
  • Prothrombin / antagonists & inhibitors

Substances

  • Polymers
  • Antithrombin III
  • Prothrombin
  • Factor X
  • Factor IIa
  • Heparin
  • Factor Xa
  • Polysaccharide-Lyases
  • Heparin Lyase