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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 ]
The European Society of Cardiology (ESC), [25] and National Institute for Health and Care Excellence (NICE) [27] guidelines recommend that if the patient has a CHA 2 DS 2-VASc score of 2 and above, oral anticoagulation therapy (OAC) with a vitamin K antagonist (VKA, e.g. warfarin with target INR of 2-3) or one of the direct oral anticoagulant ...
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]
The structure of apixaban, before adjusting the moiety's for maximum potency. Apixaban. 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.
Threshold dose is the minimum dose of drug that triggers minimal detectable biological effect in an animal. [1] At extremely low doses, biological responses are absent for some of the drugs. The increase in dose above threshold dose induces an increase in the percentage of biological responses. [2]
Antiphospholipid syndrome is known for causing arterial or venous blood clots, in any organ system, and pregnancy-related complications.While blood clots and pregnancy complications are the most common and diagnostic symptoms associated with APS, other organs and body parts may be affected like platelet levels, heart, kidneys, brain, and skin.
Irritable bowel syndrome, or IBS, is among the most common gastrointestinal conditions today.It affects some 10% to 15% of people in the U.S., per the American College of Gastroenterology.A ...
To diagnose a pulmonary embolism, a review of clinical criteria to determine the need for testing is recommended. [34] In those who have low risk, age less than 50, heart rate less than 100 beats per minute, oxygen level more than 94% on room air, and no leg swelling, coughing up of blood, surgery or trauma in the last four weeks, previous ...