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Anticoagulant and fibrinolytic pharmacokinetics of sulodexide in man
THURSDAY
252 Anticoagulant and flbrinolytic pharmacokinetics of sulodexide in man MILANI MR, BARBANTI M, CALANNI RINDINA F, MARCHI E Research Department Alfa Wassermann, Bologna, Italy
Sulodexide (SDX) (VESSEL-2F@, Alfa Wassermann) is a well-known antiatherosclerotic and antithrombotic drug. The purpose of our study was to evaluate the pharmacokinetic properties of the anticoagulant activity and then the behavior of the little known profibrinolytic activity in man. Six heathy subjects received a single I.V. administration of 50 mg of SDX. Multiple blood samples were collected for measurement of the anticoagulant activity by APlT, thrombin time (IT), anti-Xa (a-Xa) and Heptest assays; to test the fibrinolytic activity fibrin plate lysis diameter (FPLD), plasminogen activator inhibitor activity (PAIORTHO) and PAI-I antigen (ORTHO) assays were used.
JUNE 28 1990
99
SDX induced a prolongation of the ‘IT and Heptest 15 minutes after I.V. treatment, but TT activity rapidly decreased whereas the significant increases in Heptest were observed up to 4 hours after I.V. administration. SDX produced a significant elevation on APTT’and a similar effect on a-Xa. The drug induced a very important profibrinolytic activity immediately after the I.V. treatment; in fact FPLD significantly increased and at the same time the PAI level and activity decreased very rapidly for up to 2 hours. The results of this study indicate that the antithrombotic activity of SDX could be attributed to its anticoagulant and fibrinolytic activities. This multifactorial mechanism of SDX action may play on important role in the prevention as well as in the treatment of thrombotic disease.
252 Anticoagulant and flbrinolytic pharmacokinetics of sulodexide in man MILANI MR, BARBANTI M, CALANNI RINDINA F, MARCHI E Research Department Alfa Wassermann, Bologna, Italy
Sulodexide (SDX) (VESSEL-2F@, Alfa Wassermann) is a well-known antiatherosclerotic and antithrombotic drug. The purpose of our study was to evaluate the pharmacokinetic properties of the anticoagulant activity and then the behavior of the little known profibrinolytic activity in man. Six heathy subjects received a single I.V. administration of 50 mg of SDX. Multiple blood samples were collected for measurement of the anticoagulant activity by APlT, thrombin time (IT), anti-Xa (a-Xa) and Heptest assays; to test the fibrinolytic activity fibrin plate lysis diameter (FPLD), plasminogen activator inhibitor activity (PAIORTHO) and PAI-I antigen (ORTHO) assays were used.
JUNE 28 1990
99
SDX induced a prolongation of the ‘IT and Heptest 15 minutes after I.V. treatment, but TT activity rapidly decreased whereas the significant increases in Heptest were observed up to 4 hours after I.V. administration. SDX produced a significant elevation on APTT’and a similar effect on a-Xa. The drug induced a very important profibrinolytic activity immediately after the I.V. treatment; in fact FPLD significantly increased and at the same time the PAI level and activity decreased very rapidly for up to 2 hours. The results of this study indicate that the antithrombotic activity of SDX could be attributed to its anticoagulant and fibrinolytic activities. This multifactorial mechanism of SDX action may play on important role in the prevention as well as in the treatment of thrombotic disease.