[The antithrombotic activity of para-aminobenzoic acid in experimental thrombosis]

Izv Akad Nauk Ser Biol. 1999 May-Jun:(3):329-36.
[Article in Russian]

Abstract

It was shown for the first time that p-aminobenzoic acid (PABA), in addition to the previously described fibrinolytic activity, exerts the properties of a direct anticoagulant both in vitro and in vivo. PABA not only displays antithrombin activity, but also inhibits activated factor X and, upon intravenous injection to rats and rabbits, shows the antithrombotic effect. The most pronounced antithrombotic affect was observed at a dose of 1.5 mg/kg. PABA at 0.5 mg/kg has insignificant efficacy and at 3 mg/kg, a high efficacy, but induces hemolysis of erythrocytes in about a half of cases. Equally efficient antithrombotic activity of blood plasma of rats was noted after intravenous injection of low molecular weight heparin "Fraxiparin" at 40 anti-Xa U/kg and PABA at 25 anti-Xa U/kg (1.5 mg/kg). Unlike "Fraxiparin", which exerts an immediate effect, the effect of PABA was expressed within 1.5 to 5 h after injection with a peak of antithrombotic activity at 3 h (which correlates with anti-IIa and anti-Xa activities of plasma) and terminated by 5 h after injection. For PABA, the ratio of anti-Xa to anti-IIa activities (an important parameter, which determines the antithrombotic potential of drugs) equals 2.4. PABA at 0.5 or 1.5 mg/kg did not affect the number of thrombocytes, while at 3 mg/kg, it decreased the number of thrombocytes by 20%. Thus PABA at 1.5 mg/kg, which has a high anticoagulant activity and does not cause side effects, is most interesting for further studies.

Publication types

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

MeSH terms

  • 4-Aminobenzoic Acid / pharmacology
  • 4-Aminobenzoic Acid / therapeutic use*
  • Animals
  • Blood Coagulation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Female
  • Fibrinolytic Agents / pharmacology
  • Fibrinolytic Agents / therapeutic use*
  • In Vitro Techniques
  • Male
  • Nadroparin / pharmacology
  • Rabbits
  • Rats
  • Thrombosis / blood
  • Thrombosis / drug therapy*
  • Time Factors

Substances

  • Fibrinolytic Agents
  • Nadroparin
  • 4-Aminobenzoic Acid