thrombin inhibitors

Antithrombotics

Effects Antithrombotic Anticoagulant Fibrinolytic Active ingredients Salicylates: Acetylsalicylic acid 100 mg (Aspirin Cardio). P2Y12 antagonists: Clopidogrel (Plavix, generics). Prasugrel (Efient) Ticagrelor (Brilique) GP IIb/IIIa antagonists: Abciximab (ReoPro) Eptifibatide (Integrilin) Tirofiban (Aggrastat) PAR-1 antagonists: Vorapaxar (Zontivity) Vitamin K antagonists (coumarins): Phenprocoumon (Marcoumar). Acenocoumarol (Sintrom) Not on sale in many countries: dicoumarol, warfarin. Heparins: Heparin sodium Heparin-Calcium … Antithrombotics

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.

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

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Products Ximelagatran (Exanta, film-coated tablets) was withdrawn from the market or not approved in some countries in 2006 because liver-toxic properties had been observed in clinical trials.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

Bivalirudin

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

DOAK

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

Dabigatran

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

Deep Vein Thrombosis

Symptoms The possible symptoms and signs of deep vein thrombosis include: Pain or cramping in the legs Swelling (edema), feeling of tension Warmth sensation, overheating Reddish to blue-purple discoloration of the skin Increased visibility of the superficial veins The symptoms are rather nonspecific. Deep vein thrombosis may also be asymptomatic and discovered by chance. A … Deep Vein Thrombosis

Factor Xa Inhibitors

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

Argatroban

Products Argatroban is commercially available as a concentrate for the preparation of an infusion solution (Argatra). It was approved in many countries in 2014. Structure and properties Argatroban (C23H36N6O5S, Mr = 508.6 g/mol) is a derivative of the amino acid arginine. Effects Argatroban (ATC B01AE03) has antithrombotic properties. It inhibits fibrin formation, coagulation factor activation, … Argatroban

Pulmonary Embolism Causes and Treatment

Symptoms Possible symptoms of pulmonary embolism include: Shortness of breath (dyspnea), rapid breathing, cyanosis. Chest pain Cough with blood or sputum Rapid heartbeat Fever, sweating Loss of consciousness (syncope) Low blood pressure, shock Symptoms of deep vein thrombosis, such as a swollen, warm leg The severity varies and depends, among other things, on how large … Pulmonary Embolism Causes and Treatment