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The risk of bleeding is increased if used at the same time as other blood thinning drugs such as nonsteroidal anti-inflammatory drugs, antiplatelet drugs and heparin. [2] The blood thinning effects can be reduced if used at the same time as rifampicin and phenytoin , and increased with fluconazole .
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 ]
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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.
Thrombin time can be prolonged by heparin, fibrin degradation products, and fibrinogen deficiency or abnormality. Thrombin time is not affected by anti-Xa anticoagulants such as rivaroxaban or apixaban , but is very sensitive to direct thrombin inhibitors including dabigatran , argatroban , and bivalirudin .
Average molecular weight: heparin is about 15 kDa, and LMWH is about 4.5 kDa. [25] Less frequent subcutaneous dosing than for heparin for postoperative prophylaxis of venous thromboembolism. Once or twice daily subcutaneous injection for treatment of venous thromboembolism and in unstable angina instead of intravenous infusion of high-dose heparin.
Protamine sulfate is a medication that is used to reverse the effects of heparin. [3] It is specifically used in heparin overdose, in low molecular weight heparin overdose, and to reverse the effects of heparin during delivery and heart surgery. [3] [4] It is given by injection into a vein. [3] The onset of effects is typically within five ...
In pharmacokinetics, a loading dose is an initial higher dose of a drug that may be given at the beginning of a course of treatment before dropping down to a lower maintenance dose. [ 1 ] A loading dose is most useful for drugs that are eliminated from the body relatively slowly, i.e. have a long systemic half-life .