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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.
The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
[28] [29] In August 2014, the FDA approved apixaban for the additional indication of the treatment of recurring deep vein thrombosis and pulmonary embolism. [28] [30] During its development the drug was known as BMS-562247-01. [31] By late 2019, sales of the product by BMS accounted for thirty percent of their quarterly revenue. [32]
ELIQUIS ® (apixaban) Demonstrated Superiority In Reducing A Composite Of Recurrent Venous Thromboembolism And All-Cause Death Without Increasing The Rate Of Major Bleeding Versus Placebo During ...
Heparin targets multiple factors in the blood coagulation cascade, one of them being FXa. At first, it had many side effects but for the next twenty years, investigators worked on heparin to make it better and safer. It entered clinical trials in 1935 and the first drug was launched in 1936. Chains of natural heparin can vary from 5.000 to 40. ...
Andexanet alfa, sold under the brand name Andexxa among others, is an antidote for the medications rivaroxaban and apixaban, when reversal of anticoagulation is needed due to uncontrolled bleeding. [8] It has not been found to be useful for other factor Xa inhibitors. [9] It is given by injection into a vein. [9]
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.
The clinically approved dose of prasugrel is a 60-mg loading dose PO and a 10-mg a day maintenance dose PO. [28] Ticagrelor is a much more potent inhibitor of platelet aggregation than clopidogrel, however, it is associated with increase of dyspnoea episodes in patients. These episodes can range from mild to moderate severity.
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