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

• Published in: Thrombosis and haemostasis Vol. 57; no. 1; p. 97
• Main Authors: Mätzsch, T, Bergqvist, D, Hedner, U, Ostergaard, P
• Format: Journal Article
• Language: English
• Published: Germany 03-02-1987
• Subjects: 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
• ISSN: 0340-6245
• DOI: 10.1055/s-0038-1651070

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.