PMID- 10470990
OWN - NLM
STAT- MEDLINE
DCOM- 19991022
LR  - 20190724
IS  - 0160-2446 (Print)
IS  - 0160-2446 (Linking)
VI  - 34
IP  - 3
DP  - 1999 Sep
TI  - Comparative study on the in vitro and in vivo activities of heparinoids 
      derivative investigated on the animal model.
PG  - 340-5
AB  - In this study we compared the antithrombotic and anticoagulant properties of 
      sodium and calcium derivatives of pentosan polysulfate (Na-PPS, Ca-PPS), 
      unfractionated heparin (UFH), and low-molecular-weight heparin (Fraxiparin). The 
      antithrombotic effects of these agents have been investigated in an experimental 
      thrombosis model in which rat mesenteric venules with a diameter of 20-30 microm 
      were injured by well-defined argon laser lesions. Furthermore, the in vivo and in 
      vitro anticoagulant activities [activated partial thromboplastin time (aPTT), 
      Heptest] of these agents have been studied. Thrombus formation was significantly 
      inhibited after s.c. injection of Na-PPS and Ca-PPS in doses >10 mg/kg. The 
      duration of the antithrombotic effect lasted 8 h for Na-PPS and 12 h for Ca-PPS. 
      After oral administration of Na-PPS, an antithrombotic effect was not observed. 
      Oral application of Ca-PPS in doses >20 mg/kg significantly inhibited thrombus 
      formation. Na-PPS and Ca-PPS markedly prolonged clotting time in aPTT and Heptest 
      in concentrations ranging from 0.01 to 0.2 mg/ml rat PTT. Two h after s.c. 
      administration of these agents in a dose of 10 mg/kg, the aPTT increased 
      threefold and the Heptest 2.5-fold compared with controls. After oral application 
      of 50 mg/kg Na-PPS and Ca-PPS, no effect on the coagulation test could be 
      measured. Intravenous injection of UFH prolonged the Heptest after 1 min and the 
      aPTT after 30 min. In ex vivo studies of aPTT and Heptest performed in rat plasma 
      between 2 and 24 h after s.c. injection of 0.2 mg/kg Fraxiparin, no inhibition of 
      any coagulation test was measured. The antithrombotic effect of 0.2 mg/kg 
      Fraxiparin after s.c. injection was significant. Intravenous injection of 20 U/kg 
      UFH significantly inhibited thrombus formation. The smallest antithrombotic 
      effect was after i.v. injection of UFH.
FAU - Giedrojc, J
AU  - Giedrojc J
AD  - Department of Haematology, University Medical School, Bialstok, Poland.
FAU - Klimiuk, M
AU  - Klimiuk M
FAU - Radziwon, P
AU  - Radziwon P
FAU - Kloczko, J
AU  - Kloczko J
FAU - Bielawiec, M
AU  - Bielawiec M
FAU - Breddin, H K
AU  - Breddin HK
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - United States
TA  - J Cardiovasc Pharmacol
JT  - Journal of cardiovascular pharmacology
JID - 7902492
RN  - 0 (Blood Coagulation Factors)
RN  - 0 (Fibrinolytic Agents)
RN  - 0 (Heparinoids)
RN  - 0 (Nadroparin)
RN  - 37300-21-3 (Pentosan Sulfuric Polyester)
RN  - 9005-49-6 (Heparin)
SB  - IM
MH  - Animals
MH  - Blood Coagulation Factors/antagonists & inhibitors
MH  - Disease Models, Animal
MH  - Fibrinolytic Agents/*therapeutic use
MH  - Heparin/therapeutic use
MH  - Heparinoids/chemistry/*therapeutic use
MH  - Lasers
MH  - Male
MH  - Nadroparin/therapeutic use
MH  - Pentosan Sulfuric Polyester/therapeutic use
MH  - Rats
MH  - Rats, Wistar
MH  - Thrombosis/metabolism
MH  - Venous Thrombosis/*drug therapy
EDAT- 1999/09/02 00:00
MHDA- 1999/09/02 00:01
CRDT- 1999/09/02 00:00
PHST- 1999/09/02 00:00 [pubmed]
PHST- 1999/09/02 00:01 [medline]
PHST- 1999/09/02 00:00 [entrez]
AID - 10.1097/00005344-199909000-00004 [doi]
PST - ppublish
SO  - J Cardiovasc Pharmacol. 1999 Sep;34(3):340-5. doi: 
      10.1097/00005344-199909000-00004.