in therivaroxaban group died.Apixaban is an oral active Factor Xa inhibitor derivedfrom razaxaban, Celecoxib with superiorpharmacological proprieties. It is a little molecule ableto inhibit in a selective and reversible manner the activesite of both cost-free and prothrombinase-bound Factor 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 in 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 obtaining 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 in 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% with 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 factor Xainhibitors, for instance edoxaban, are also underway.
CONCLUSIONSThe current management of VTE is largely according to theuse of anticoagulant drugs, both parenteral drugs such asUFH, LMWH or fondaparinux for the treatment with the acutephase and oral drugs for instance the vitamin K antagonists forthe long term secondary prevention. All these drugs havebeen proven to be extremely successful in preventing thrombuspropagation, embolization, Alogliptin and recurrence. For the managementof the acute phase with the disease, LMWH has largelyreplaced UFH hence contributing to simplify the managementof VTE, and now a large proportion of patients with DVTdo not ought to be hospitalized and can be completely treatedas outpatients.
For the long term secondary prevention, vitaminK antagonists remain the only selection for clinicians,and their clear positive aspects in terms of efficacy ought to be periodicallybalanced in each 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 turn out to be much larger. Immediately after the good results of thefirst clinical trials, new direct thrombin inhibitors and directFactor Xa inhibitors which are administered orally are closelyapproaching the marketplace. With predictable anticoagulant responsesand low possible for food-drug and drug-drug interactions,these new agents may be offered in fixed doses withoutcoagulation monitoring. These properties as well as the oral administrationrender these compounds a lot more convenient than bothvitamin K antagonists and LMWH.
According to style 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. Thus, patients Celecoxib with VTE might be treatedwith a single oral agent appropriate soon after the objective diagnosisof the disease. Particular places of particular interest for thesenew agents include things like the treatment of patients with cancerand VTE, for whom long term treatment with LMWH iscurrently advised and for whom an oral agent witha low propensity for drug-drug interactions could representthe best therapy, and not surprisingly the long term treatmentof patients with unprovoked VTE, where the complex balancebetween positive aspects and risks with the presently availabledrugs might be simplified with all 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 factor 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 successful for preventingvenous thromboembolism in orthopedic surgery, stated AVERROESlead investigator Dr. Connolly. He also noted that strokerisk is high in AF patients and that even though vitamin K agonisttherapy is successful 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
Unknown Info About Alogliptin Celecoxib Shared By The Industry Professionals
Subscribe to:
Post Comments (Atom)
No comments:
Post a Comment