Fondaparinux

Products Fondaparinux is commercially available as a solution for injection (Arixtra). It has been approved in many countries since 2002. Structure and properties Fondaparinux (C31H43N3Na10O49S8, Mr = 1728 g/mol) is a synthetic pentasaccharide belonging to the class of glycosaminoglycans. It is present in the drug as fondaparinux sodium. Effects Fondaparinux (ATC B01AX05) has antithrombotic properties. … Fondaparinux

Defibrotide

Products Defibrotide was approved in many countries in 2020 as a concentrate for the preparation of an infusion solution (Defitelio). Structure and properties Defibrotide is a mixture of single-stranded oligonucleotides derived from porcine intestinal mucosa. Effects Defibrotide (ATC B01AX01) has antithrombotic, fibrinolytic, antiadhesive, and anti-inflammatory properties. Indications For the treatment of severe hepatic veno-occlusive disease … Defibrotide

Lepirudin

Products Lepirudin was commercially available as a lyophilizate (Refludan). It was approved in many countries in 1997 and is no longer on the market. Structure and properties Lepirudin is a derivative of hirudin from the leech. Effects Lepirudin (ATC B01AX03) is anticoagulant by direct inhibition of thrombin. Indications Heparin-associated thrombocytopenia (HAT) type II.

Ginkgo Health Benefits

Products Ginkgo extract is commercially available in the form of capsules, film-coated tablets, and as drops (e.g., Symfona, Tebokan, Tebofortin, Rezirkane), among others. In addition, dried ginkgo leaves are also available. It is recommended to use standardized and refined special extracts, as these contain the relevant ingredients and are free from undesirable substances, especially the … Ginkgo Health Benefits

Dalteparin

Products Dalteparin is commercially available as an injectable (Fragmin). It has been approved in many countries since 1988. Structure and properties Dalteparin is present in drugs as dalteparin sodium, the sodium salt of a low-molecular-weight heparin obtained by depolymerization of heparin from porcine intestinal mucosa using nitrous acid. The average molecular weight is 6000 Da. … Dalteparin

Vorapaxar

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

Drotrecogin Alfa

Products Drotrecogin alfa was commercially available as a lyophilizate (Xigris). It has been approved in many countries and in the EU since 2002 and was also available in the United States and Canada. In 2011, Eli Lilly announced it was withdrawing the drug from the market worldwide. The PROWESS-SHOCK study showed insufficient efficacy. Mortality was … Drotrecogin Alfa

Streptokinase

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

Fibrinolytics

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)

Ximelagatran

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

Thrombin Inhibitors

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

Alteplase

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