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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]
Apixaban is recommended by the National Institute for Health and Clinical Excellence for the prevention of stroke and systemic embolism in people with non-valvular atrial fibrillation and at least one of the following risk factors: prior stroke or transient ischemic attack, age 75 years or older, diabetes, or symptomatic heart failure. [17]
Antiplatelet medications are one of the primary recommendations for treatment of both stable [4] and unstable [5] ischemic heart disease.Most commonly, aspirin is used as a single medication in cases of uncomplicated stable angina, and in some cases of unstable angina.
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 .
After the following elimination of HCl and morpholine, the iodine is substituted by 2-piperidinone by copper-catalization and the ethyl esther is converted to an amide . This reaction was registered as a patent in 2009. [31] Synthesis of apixaban, as published by Pinto, et al. in 2007. [30]
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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.