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  2. Direct factor Xa inhibitors - Wikipedia

    en.wikipedia.org/wiki/Direct_factor_Xa_inhibitors

    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]

  3. Discovery and development of direct Xa inhibitors - Wikipedia

    en.wikipedia.org/wiki/Discovery_and_development...

    The p-methoxy group of apixaban connects to S1 pocket of FXa but does not appear to have any interaction with any residues in this region of FXa. The pyrazole N-2 nitrogen atom of apixaban interacts with Gln-192 and the carbonyl oxygen interacts with Gly-216. The phenyl lactam group of apixaban is positioned between Tyr-99 and Phe-174 and due ...

  4. Apixaban - Wikipedia

    en.wikipedia.org/wiki/Apixaban

    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. [ 25 ]

  5. Discovery and development of direct thrombin inhibitors

    en.wikipedia.org/wiki/Discovery_and_development...

    Unlike the hirudins, bivalirudin is only partially (about 20%) excreted by the kidneys, other sites such as hepatic metabolism and proteolysis also contribute to its metabolism, making it safer to use in patients with renal impairment; however, dose adjustments are needed in severe renal impairment. [8] [16]

  6. Hepatotoxicity - Wikipedia

    en.wikipedia.org/wiki/Hepatotoxicity

    Hepatotoxicity (from hepatic toxicity) implies chemical-driven liver damage. Drug-induced liver injury (DILI) is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn from the market after approval.

  7. Vorapaxar - Wikipedia

    en.wikipedia.org/wiki/Vorapaxar

    Vorapaxar is contraindicated for people with a history of stroke, transient ischemic attack, or intracerebral hemorrhage. [2] In studies of vorapaxar on persons with prior ischemic stroke, there was an increased risk of intracranial hemorrhage without an improvement in major vascular events.

  8. Adenosine diphosphate receptor inhibitor - Wikipedia

    en.wikipedia.org/wiki/Adenosine_diphosphate...

    The neutral sidechain R1=CONH 2 and R1=CH 2 OH were accepted with slight loss of affinity and the metabolism had shifted from biliary to hepatic metabolism. Because of this, in vitro hepatic microsomal assays could be used which simplified the optimization of pharmacokinetic properties. Addition of phenyl cyclopropylamine substituent in the 5 ...

  9. Adverse drug reaction - Wikipedia

    en.wikipedia.org/wiki/Adverse_drug_reaction

    Type A: augmented pharmacological effects, which are dose-dependent and predictable [5]; Type A reactions, which constitute approximately 80% of adverse drug reactions, are usually a consequence of the drug's primary pharmacological effect (e.g., bleeding when using the anticoagulant warfarin) or a low therapeutic index of the drug (e.g., nausea from digoxin), and they are therefore predictable.