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Briefing Therapeutic Approaches in Anticoagulant, Thrombolytic, and Antiplatelet Therapy
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
The molecular weight (MW) of LMWHs is lesser than the MW of UFHs. To inactivate thrombin, heparin molecule must form a ternary complex as a bridge between antithrombin and thrombin, which requires minimum 18 saccharide units and thus smaller heparin molecules, cannot facilitate the interaction between antithrombin and thrombin. The implication of the minimum size requirement is that there must be at least 13 saccharides next to the pentasaccharide for thrombin binding. Therefore, LMWHs have greater affinity towards factor Xa, but lesser to thrombin as shown in Figure 7.3. If the MW of LMWHs is greater than 5000 Da, the anti-IIa specific activity of LMWH is drastically reduced and selectivity increased towards the inhibition of factor X. Enoxaparin, dalteparin, tinzaparin, parnaparin, nadroparin, certoparin, bemiparin, reviparin are the approved LMWHs. Tinzaparin is withdrawn from the market. These agents have improved subcutaneous bioavailability; dose-independence clearance; longer biological half-life; lower incidence of thrombocytopenia; and a reduced need for routine laboratory monitoring in comparison to UFH [38–41].
Antithrombotics
Published in Ann Richards, Nursing & Health Survival Guide, 2014
Bemiparin sodium (Zibor®), dalteparin sodium (Fragmin®), enoxaparin sodium (Clexane®), reviparin sodium (Clivarine®), tinzaparin sodium (Innohep®) Longer duration of action than standard or unfractionated heparin.May be given once daily by subcutaneous injection.More predictable response.Do not need to monitor using blood tests.
Fibrinolytic Enzymes for Thrombolytic Therapy
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Swaroop S. Kumar, Sabu Abdulhameed
Murray et al. (1937) showed that heparin could prevent thrombus formation in traumatized veins of dogs. Later it was used as anticoagulant in humans in the year 1937. It enhanced the clotting time during 2 h infusion (Murray et al., 1937). Several reports expressed successful use of heparin (McLean and Johnson, 1946; Lange et al., 1945), but clinical practice of the molecule reflected certain shortcomings such as heparin induced thrombocytopenia (HIT), bleeding complications, etc. which have to be constantly monitored as well as multiple and regular administration of heparin on a daily basis is essential (Cohen, 1999). Despite these limitations, heparin still remains as one of the widely used cardiovascular drugs, though it is the oldest therapeutic used as anticoagulant. Apart from heparin, low-molecular-weight heparins (LMWHs) derived from heparin by its depolymerization also find their application as anticoagulants. They unveil better therapeutic index with lower frequency of HIT in comparison with heparin. But, LMWHs are not appropriate for management of already established HIT, since the antibodies produced against heparin react with them. Each LMWH is distinct in its molecular weight and therapeutic properties (Bick and Fareed, 1999; Cohen, 1999). On the other hand, LMWHs also need to be injected and the major route of clearance is renal. Hence, the half-life of the molecule is higher in patients with renal failure leading to its accumulation (Hirsh et al., 2001). A few of these LMWHs include enoxaparin, dalteparin, nadroparin, tinzaparin, certoparin, reviparin, ardeparin, parnaparin, and bemiparin.
A journey through anticoagulant therapies in the treatment of left ventricular thrombus in post-COVID-19 heparin-induced thrombocytopenia: a case report
Published in Hematology, 2022
Alberto Lázaro-García, Inés Martínez-Alfonzo, Rosa Vidal-Laso, Diego Velasco-Rodríguez, Marta Tomás-Mallebrera, Marta González-Rodríguez, Pilar Llamas-Sillero
The patient required non-invasive mechanical ventilation. The acenocoumarol treatment was discontinued, and a therapeutic dose of bemiparin was initiated (10,000 IU/24 h, considering the patient’s weight [81 kg] and a normal renal and hepatic function). The patient’s progress was favourable, and he was discharged 10 days later and prescribed at-home subcutaneous injections of bemiparin. No other drugs were added to his usual medications.