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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. [ 25 ]
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.
Doses of rivaroxaban under 10 mg can be taken with or without food, as it displayed high bioavailability independent of whether food was consumed or not. [38] If rivaroxaban is given at oral doses of 15 mg or 20 mg, it needs to be taken with food to aid in drug absorption and achieve appropriate bioavailability (≥ 80%).
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]
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There’s a maximum daily dose, so it’s possible to take too much metformin. Metformin overdose can include the following symptoms: Abnormally fast or slow heartbeat. Decreased appetite.
"Time to peak" refers to when maximum levels of the drug in the blood occur after a given dose. Benzodiazepines generally share the same pharmacological properties, such as anxiolytic, sedative, hypnotic, skeletal muscle relaxant, amnesic, and anticonvulsant effects. Variation in potency of certain effects may exist amongst individual ...
The median effective dose is the dose that produces a quantal effect (all or nothing) in 50% of the population that takes it (median referring to the 50% population base). [6] It is also sometimes abbreviated as the ED 50, meaning "effective dose for 50% of the population". The ED50 is commonly used as a measure of the reasonable expectancy of ...
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