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Original Article

J App Pharm Sci. 2020; 10(8): 105-110


THROMBOELASTOGRAPHY AS AN INSTRUMENT OF PRECLINICAL STUDIES OF THE POTENTIAL DRUG

Aleksandr Livievich Urakov, Ilshat Ganeevich Mustafin, Rosa Mullayanovna Nabiullina, Linara Irekovna Bashirova, Konstantin Sergeevich Mochalov, Aleksandr Vladimirovich Samorodov, Ferkat Adelsyanovich Khaliullin, Danila Olegovich Lipatov, Vladislav Igorevich Korunas, Lina Nailevna Ismagilova, Almaz Radicovich Khalimov.


Abstract

There are no recommendations for assessing the effect of potential drugs on the haemostatic system irrespective of the anticipated application area, which leads to long-term financial losses. The examples of papaverine hydrochloride, pentoxifylline and acetylsalicylic acid demonstrated the potential of thromboelastography (TEG) as a screening method for products that affect haemostatic system, safety assessment method for hypercoagulability/hypocoagulability and thrombosis model, using tissue factor or thrombin. The blood of male donors (n=60) and patients with acute de novo thrombosis (n=90) were used. Using activated TEG, in vitro haemostatic system hyperactivity modelling was performed with the blood of healthy male donors (n=20); 0.2 М CaCl2, recombinant tissue factor and thrombin were used as TEG activators. General coagulation tendency (R), functional activity of thrombocytes and fibrinogen (МА, Angle), fibrinolysis activity and physical–mechanical properties of the formed clots were determined from thromboelastograms. Effect of anti-aggregants was characterised by significant decrease in МА. The potential of TEG as a screening method for assessing the effect of new pharmacological agents on haemostatic system at preclinical stage was demonstrated, possibility of safety assessment for hypercoagulability/hypocoagulability was shown and the comparability of haemostatic parameters of the patients with thrombosis and TEG, activated by tissue factor and/or thrombin, was demonstrated.

Key words: Thromboelastography, haemostatic system, thrombosis, anti-aggregants, coagulation






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