in therivaroxaban group died.Apixaban is an oral active Aspect Xa inhibitor derivedfrom razaxaban, Celecoxib with superiorpharmacological proprieties. It is a small molecule ableto inhibit inside a selective and reversible manner the activesite of both totally free and prothrombinase-bound Aspect Xa.Preclinical studies demonstrate that apixaban has an oralbioavailability of more than 50%: its plasma peak is achievedin about 3 h and its half-life is about 12 h. The drugis absorbed within the gastrointestinal tract, is metabolised inthe liver by cythocrome-dependent and -independent mechanismsand it is eliminated by means of both the renal and thefaecal routes.Apixaban has been assessed for the treatment of DVTin a dose locating study. Patientswere randomised to obtain apixaban 5 mg bid, 10 mg bid,20 mg od or LMWH vitamin K antagonists.
The primaryefficacy outcome, defined as the composite of symptomaticrecurrent VTE and asymptomatic deterioration within the thromboticburden as assessed by repeat bilateral compression ultrasonographyand perfusion lung scan, occurred in 4.7% ofpatients treated with apixaban and in 4.2% of LMWH/vitaminK antagonists treated patients. No dose effect was observedacross apixaban Celecoxib doses. The principal safety outcome,defined as the composite of main and clinically relevantnon-major bleeding, occurred in 7.3% of the apixaban treatedpatients and in 7.9% of LMWH/vitamin K antagonists treatedpatients. On the basis of this study, phase III studies, testing apixaban atthe doses of 10 mg and 5 mg twice every day, are now undergoing.Studies assessing the efficacy and safety of other element Xainhibitors, like edoxaban, are also underway.
CONCLUSIONSThe present management of VTE is largely depending on theuse of anticoagulant drugs, both parenteral drugs such asUFH, LMWH or fondaparinux for the treatment of the acutephase and oral drugs like the vitamin K antagonists forthe long term secondary prevention. All these drugs havebeen proven to be highly efficient in preventing thrombuspropagation, embolization, Alogliptin and recurrence. For the managementof the acute phase of the disease, LMWH has largelyreplaced UFH hence contributing to simplify the managementof VTE, and now a large proportion of patients with DVTdo not need to be hospitalized and can be completely treatedas outpatients.
For the long term secondary prevention, vitaminK antagonists remain the only choice for clinicians,and their clear rewards when it comes to efficacy need to be periodicallybalanced in every patient against their risks in termsof safety and their inconvenient HSP management. Inside a verynear future, the armamentarium of clinicians involved inthe prevention and treatment of thromboembolic disorderscould Alogliptin become considerably larger. Right after the good outcomes of thefirst clinical trials, new direct thrombin inhibitors and directFactor Xa inhibitors that are administered orally are closelyapproaching the marketplace. With predictable anticoagulant responsesand low possible for food-drug and drug-drug interactions,these new agents is often offered in fixed doses withoutcoagulation monitoring. These properties and also the oral administrationrender these compounds a lot more convenient than bothvitamin K antagonists and LMWH.
According to design of thephase III clinical trials, we can speculate that some of thesecompounds will challenge the vitamin K antagonists for thelong term secondary prevention of VTE, and that other willalso challenge the parenteral drugs for the acute phase management,as they are tested as a stand-alone treatment forboth DVT and PE. Therefore, patients Celecoxib with VTE could possibly be treatedwith a single oral agent right immediately after the objective diagnosisof the disease. Specific places of particular interest for thesenew agents consist of the treatment of patients with cancerand VTE, for whom long term treatment with LMWH iscurrently advisable and for whom an oral agent witha low propensity for drug-drug interactions could representthe ideal therapy, and of course the long term treatmentof patients with unprovoked VTE, where the complex balancebetween rewards and risks of the currently availabledrugs could possibly be simplified with the use of a lot more practicalIn what discussant Dr.
Arnesen termed a landmark study,the AVERROES trialshowed that the anticoagulant apixabanlowered the incidence of strokeby more than 50%, compared with aspirinin patients withatrial fibrillationwho were not candidates for therapy witha vitamin K antagonist.Apixaban is an oral, selective direct element Xa inhibitor witha 12-hour half-life and multiple excretion pathways.No routine Alogliptin coagulation monitoring is necessary. In earlierresearch, it was shown to be secure and efficient for preventingvenous thromboembolism in orthopedic surgery, stated AVERROESlead investigator Dr. Connolly. He also noted that strokerisk is high in AF patients and that although vitamin K agonisttherapy is efficient against stroke, it is unsuitable for up to 50%of patients due to the difficulty in controlling the Inter -national Normalized Ratioand bleeding.AVERROES, a double
Saturday, April 20, 2013
Undiscovered Information About Alogliptin Celecoxib Uncovered By The Experts
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