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Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [ 28 ]
Side effects may include bleeding, most commonly from the nose, gastrointestinal tract (GI) or genitourinary system. [2] Compared to the risk of bleeding with warfarin use, direct factor Xa inhibitors have a higher risk of GI bleeding, but lower risk of bleeding in the brain. [2]
A range of test have been developed including smartphone based platforms, and tests targeting blood, saliva, faecal matter, urine, and tears have been proposed. [16] Saliva in particular may offer sufficiently high detection rates in tandem with a non-invasive and user friendly procedure, although reliability requires improvement. [17]
Therapeutic drug monitoring (TDM) is a branch of clinical chemistry and clinical pharmacology that specializes in the measurement of medication levels in blood. Its main focus is on drugs with a narrow therapeutic range , i.e. drugs that can easily be under- or overdosed. [ 1 ]
It can be performed by continuously measuring certain parameters by using a medical monitor (for example, by continuously measuring vital signs by a bedside monitor), and/or by repeatedly performing medical tests (such as blood glucose monitoring with a glucose meter in people with diabetes mellitus).
The 13F moiety intermediate before apixaban was fully developed. During the SAR development of apixaban there were three groups that needed to be tested to attain maximum potency and bioavailability. The first group to be tested was the non-active site as it needs to be stabilized before SAR testing on the p-methoxyphenyl group (S1 binding moiety).
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [ 8 ] Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [ 11 ]
An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. [1] Some occur naturally in blood-eating animals, such as leeches and mosquitoes, which help keep the bite area unclotted long enough for the animal to obtain blood.