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Direct factor Xa inhibitors (xabans) are anticoagulants (blood thinning drugs), used to both treat and prevent blood clots in veins, and prevent stroke and embolism in people with atrial fibrillation (AF).
Still, the blood values are approximately equal between the arterial and venous sides for most substances, with the exception of acid–base, blood gases and drugs (used in therapeutic drug monitoring (TDM) assays). [6] Arterial levels for drugs are generally higher than venous levels because of extraction while passing through tissues. [6]
Results are given in units/mL of anti-factor Xa, such that high values indicate high levels of anticoagulation and low values indicate low levels of anticoagulation in the plasma sample. [ 17 ] LMWHs have a targeted therapeutic window of approximately 0.6–1.2 IU/ml. LMWH has a potency of 70 units/mg of anti-factor Xa activity and a ratio of ...
The first crystal structure of human factor Xa was deposited in May 1993. To date, 191 crystal structures of factor Xa with various inhibitors have been deposited in the protein data bank. The active site of factor Xa is divided into four subpockets as S1, S2, S3 and S4. The S1 subpocket determines the major component of selectivity and binding.
Factor Xa was identified as a promising target for the development of new anticoagulants in the early 1980s. In 1987 the first factor Xa inhibitor, the naturally occurring compound antistasin, was isolated from the salivary glands of the Mexican leech Haementeria officinalis. Antistasin is a polypeptide and a potent Xa inhibitor.
Rivaroxaban inhibits both free and bound Factor Xa in the prothrombinase complex. [33] It is a selective direct factor Xa inhibitor with an onset of action of 2.5 to 4 hours. [34] Inhibition of Factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade, inhibiting both thrombin formation
It is a direct factor Xa inhibitor. [8] In 2007, Pfizer and Bristol-Myers Squibb began the development of apixaban as an anticoagulant. [13] Apixaban was approved for medical use in the European Union in May 2011, and in the United States in December 2012. [7] [8] [14] It is on the World Health Organization's List of Essential Medicines. [15]
Cardiovascular agents are drugs that affect the rate and intensity of cardiac contraction, blood vessel diameters, blood volume, blood clotting and blood cholesterol levels. [1] They are indicated to treat diseases related to the heart or the vascular system (blood vessels), such as hypertension , hyperlipidemia , coagulation disorders , heart ...