Desirudin
is the only fixed-dose subcutaneously administered DTI approved by the Federal Drug Administration (FDA) for postoperative prevention of VTE in patients undergoing elective hip replacement surgery [17]. In March 2010 it became available in the United States.
What type of clotting problem is treated with a thrombin inhibitor?
Thrombin inhibitors are used to prevent
arterial and venous thrombosis
. They can also be used to prevent and treat deep vein thrombosis or used as prophylaxis in atrial fibrillation to avoid thromboembolism.
When are direct thrombin inhibitors used?
In response to the need for new anticoagulants, direct thrombin inhibitors (DTIs) have been developed and investigated for their utility in prophylaxis and treatment of venous thromboembolism (VTE),
heparin-induced thrombocytopenia (HIT), acute coronary syndromes (ACS), secondary prevention of coronary events after ACS
…
Which anticoagulant inhibits thrombin formation?
Heparin
is an injectable anticoagulant that activates antithrombin III, which inhibits thrombin and factor Xa, factors necessary in the final stages of blood clotting cascade.
Is heparin an indirect thrombin inhibitor?
Thrombin inhibitors can be classified as either
indirect or
direct agents. Indirect thrombin inhibitors include unfractionated heparin (UFH) and low molecular weight heparins (LMWH), derived from UFH by controlled chemical or enzymatic depolymerisation [14], and vita- min K antagonists such as warfarin.
What type of drug slows blood clotting?
Anticoagulants such as heparin or warfarin (also called Coumadin)
slow down your body’s process of making clots. Antiplatelet drugs, such as aspirin, prevent blood cells called platelets from clumping together to form a clot.
How many types of anticoagulants are there?
Anticoagulants may be divided into
four main groups
: coumarins and indandiones; factor Xa inhibitors; heparins; and direct thrombin inhibitors.
Why are direct thrombin inhibitors used for HIT?
Direct thrombin inhibitors (DTIs) are a class of anticoagulants that
act by directly inhibiting thrombin to delay clotting
and are typically used during HIT and in acute coronary syndrome (see Table 1).
How does direct thrombin inhibitors work?
Direct thrombin inhibitors (DTIs) are a class of medication that act as anticoagulants (delaying blood clotting)
by directly inhibiting the enzyme thrombin (factor IIa)
. Some are in clinical use, while others are undergoing clinical development.
How are direct thrombin inhibitors reversed?
Idarucizumab is a humanized, monoclonal, antibody fragment
that reverses the direct thrombin inhibitor dabigatran. Andexanet alfa is a modified recombinant factor Xa molecule that reverses oral direct (e.g., apixaban, edoxaban, rivaroxaban) and injectable indirect (e.g., enoxaparin, fondaparinux) factor Xa inhibitors.
What are examples of anticoagulants?
- apixaban (Eliquis)
- dabigatran (Pradaxa)
- edoxaban (Lixiana)
- rivaroxaban (Xarelto)
- warfarin (Coumadin)
What is the mechanism of action for anticoagulants?
Anticoagulants achieve their effect by
suppressing the synthesis or function of various clotting factors that are normally present in the blood
. Such drugs are often used to prevent the formation of blood clots (thrombi) in the veins or arteries or the enlargement of a clot that is circulating in the bloodstream.
Which is used as antidote for heparin?
Expert opinion: Despite of the low therapeutic index,
protamine
is the only registered antidote of heparins. The toxicology of protamine depends on a complex interaction of the high molecular weight, a cationic peptide with the surfaces of the vasculature and blood cells.
Why is heparin an indirect thrombin inhibitor?
Indirect inhibitors act
via antithrombin and heparin cofactor II
. The main representatives are heparins, lowmolecular-weight heparins, fondaparinux, idraparinux and danaparoid. They bind to antithrombin and potentiate the inactivation of factor Xa and other serine proteases.
What is the difference between direct and indirect anticoagulants?
Direct FXa inhibitors may
directly bind to FXa
, whereas indirect inhibitors are dependent on antithrombin. Direct inhibitors may bind free FXa and, in contrast to indirect inhibitors, FXa within the prothrombinase complex or within clots as well.
Is Heparin a factor Xa inhibitor?
Heparin acts as an
anticoagulant
by activating antithrombin and accelerating the rate at which it inhibits thrombin, factor (f) Xa and multiple other upstream coagulation enzymes.
