Products Vorapaxar was approved in the form of film-coated tablets in the United States in 2014, in the EU in 2015, and in many countries in 2016 (Zontivity, MSD). Structure and properties Vorapaxar (C29H33FN2O4, Mr = 492.6 g/mol) is present as a white powder. It is a tricyclic 3-phenylpyridine derivative of himbacin, a natural alkaloid … Vorapaxar
Products Streptokinase was commercially available as an injectable in many countries (Streptase, off label). It is still available in other countries. Structure and properties Streptokinase is a protein derived from group C hemolytic streptococci. Effects Streptokinase (ATC B01AD01) has fibrinolytic and thrombolytic properties. It combines with plasminogen to form a streptokinase-plasminogen complex. This complex converts … Streptokinase
Effects Fibrinolytic: dissolve fibrin Thrombolytic: dissolve thrombi Indications For the treatment of thrombosis and embolism: Myocardial infarction Ischemic stroke Deep vein thrombosis Pulmonary embolism Acute and subacute thrombosis Arterial occlusive diseases Agents Alteplase (Actilyse) Urokinase (Urokinase HS medac) Reteplase (Rapilysin, out of trade) Streptokinase (streptase, out of trade) Tenecteplase (metalysis)
Products Ximelagatran (Exanta, film-coated tablets) was withdrawn from the market or not approved in some countries in 2006 because liver-toxic properties had been observed in clinical trials. Structure and properties Ximelagatran (C24H35N5O5, Mr = 473.6 g/mol) is a prodrug that is biotransformed in the organism to the active metabolite melagatran. Melagatran was itself also commercially … Ximelagatran
Products Thrombin inhibitors are commercially available in many countries in the form of infusion preparations and as capsules. The first oral thrombin inhibitor to be launched was ximelagatran (Exanta) in 2003. Due to its liver toxicity, sales had to be discontinued. Currently, the most widely used oral and direct thrombin inhibitor, dabigatran (Pradaxa), was approved … Thrombin Inhibitors
Products Alteplase is commercially available as an injectable (Actilyse). The drug has been approved in many countries since 1988. Structure and properties Alteplase is a recombinant tissue plasminogen activator (rt-PA) produced by biotechnological methods. It is a serine protease composed of 527 amino acids. Effects Alteplase (ATC B01AD02) has fibrinolytic and thrombolytic properties. The enzyme … Alteplase
Products Bivalirudin was commercially available as a powder for preparation of a concentrate for solution for injection or infusion (Angiox). It was approved in many countries as of 2007. It has since become unavailable. Structure and properties Bivalirudin originated from hirudin, an anticoagulant substance found in leeches. Effects Bivalirudin (ATC B01AE06) has antithrombotic properties. Indications … Bivalirudin
Products Direct oral anticoagulants (abbreviation: DOAKs) are commercially available in the form of film-coated tablets and capsules. By definition, they are oral drugs. Some representatives of the corresponding drug groups are also available as infusion preparations. Rivaroxaban (Xarelto) and dabigatran (Pradaxa) were the first active ingredients to be approved in 2008. The DOAKs were developed … DOAK
Products Dabigatran is commercially available in capsule form (Pradaxa). It has been approved in many countries since 2012. It was first approved in 2008. Structure and properties Dabigatran (C25H25N7O3, Mr = 471.5 g/mol) is present in drugs as mesilate and in the form of the prodrug dabigatran etexilate, which is metabolized in the organism by … Dabigatran
Products Direct factor Xa inhibitors are commercially available in the form of film-coated tablets and capsules. In 2008, rivaroxaban (Xarelto) was the first agent in this group to be approved in many countries and in the EU. Today, there are other drugs on the market, which are listed below. Like thrombin inhibitors, these active ingredients … Factor Xa Inhibitors
Products Dipyridamole was commercially available in many countries in the form of capsules in combination with acetylsalicylic acid (Asasantin). It had been approved in many countries since 1997. The drug is no longer marketed in many countries. Structure and properties Dipyridamole (C24H40N8O4, Mr = 504.6 g/mol) Effects Dipyridamole (ATC B01AC30) has antithrombotic properties. Indications Secondary … Dipyridamole
Products Urokinase is commercially available as a powder for the preparation of a solution for injection or infusion (Urokinase HS medac). The drug has been approved in many countries since 1988. Structure and properties Urokinase is a serine protease, which is extracted from human urine in China. It is also possible to produce it using … Urokinase
