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Current recommendations for the prevention of deep venous thrombosis
Published in Peter Gloviczki, Michael C. Dalsing, Bo Eklöf, Fedor Lurie, Thomas W. Wakefield, Monika L. Gloviczki, Handbook of Venous and Lymphatic Disorders, 2017
Rivaroxaban (Xarelto) is an oral direct factor Xa inhibitor which impairs coagulation by inhibiting the conversion of prothrombin to thrombin.62 Upon oral ingestion, rivaroxaban is 80% bioavailable, with a time to peak concentration of 2–4 hours. Its elimination half-life is between 7 and 11 hours. A significant portion of rivaroxaban is metabolized through the liver’s CYP450 system, primarily through CYP3A4 and CYP2J2. Potential drug interactions include medications which inhibit or promote the CYP3A4 or P-glycoprotein pathways. Rivaroxaban is contraindicated in patients with moderate to severe hepatic impairment (Child–Pugh B and C) or in patients with any degree of hepatic disease with coagulopathy. A total of 66% is also excreted via the kidney and, as a result, cautious use is warranted in patients with creatinine clearances of 30–50 mL/minute, and it should not be used in patients with creatinine clearances of less than 30 mL/minute. This drug is not dialyzable due to its high plasma protein binding (92%– 95%). Use of rivaroxaban is not appropriate for all patient populations, and the risks and benefits need to be considered carefully.
Briefing Therapeutic Approaches in Anticoagulant, Thrombolytic, and Antiplatelet Therapy
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Currently available direct factor Xa inhibitors are rivaroxaban, apixaban, and edoxaban (Figure 7.7). Rivaroxaban is given orally. It can inhibit both free factor Xa and factor Xa bound in the prothrombinase complex. Inhibition of Factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade by inhibiting both thrombin formation and development of thrombi [48]. Apixaban is a highly selective; orally bioavailable and reversible direct inhibitor of free and clot-bound factor Xa. It was approved in Europe in 2012. Subsequently, it was approved in the U.S. in 2014 for treatment and secondary prophylaxis of deep vein thrombosis (DVT) and pulmonary embolism (PE) [49].
Epidural and Intrathecal Analgesia
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Rivaroxaban is an oral antithrombotic agent recommended for thromboprophylaxis after total hip and knee joint replacement. It also has a long half-life (nine hours), which increases with declining renal function, but its effect can be monitored by measuring PT and APTT levels. Guidelines recommend about a three-day interval between the last dose of rivaroxaban and neuraxial blockade in patients with normal renal function, with this interval to be extended in patients with renal impairment. Administration to patients with an epidural catheter in situ is not recommended, but it can be started at least six hours after removal of an epidural catheter.
Experimental design, formulation, and in-vivo evaluation of novel anticoagulant Rivaroxaban loaded cubosomes in rats model
Published in Journal of Liposome Research, 2023
Hadeer A. El-Hashemy, Abeer Salama, Amira Rashad
A novel oral anticoagulant drug named Rivaroxaban ‘RX’ will be studied in this research work (Machado et al.2021). It is used to prevent blood clots from forming following hip or knee replacement surgery, or because of a specific irregular heartbeat (atrial fibrillation), or after hip or knee replacement surgery (Anwer et al.2020). It eliminates blood clots and prevents their recurrence in cases like deep vein thrombosis (DVT) and pulmonary embolism (PE) (Piyush Patel et al.2017). Rivaroxaban is a crystalline, non-hygroscopic, white to a yellowish white substance that is immiscible in water but soluble in DMSO (European Medicines Agency 2020). A direct factor Xa inhibitor, rivaroxaban inhibits the synthesis of thrombin and the development of thrombi by obstructing the intrinsic and extrinsic pathways of the blood coagulation surge (Abouhussein et al.2019, Duna et al.2019).
Clinical implications and cost-effectiveness analysis of rivaroxaban in patients with coronary artery disease or peripheral arterial disease in the Netherlands
Published in Journal of Medical Economics, 2021
J. A. Spoorendonk, J.-B. Briere, K. Bowrin, A. Millier, M. Coppens, S. Tempelaar, B. Verheggen
Rivaroxaban is a direct factor Xa inhibitor that decreases thrombin production. When a plaque rupture occurs, it prevents clotting and generation of a thrombus and subsequent atherothrombotic events. Data from the randomized phase III Cardiovascular OutcoMes for People using Anticoagulation Strategies (COMPASS; ClinicalTrials.gov number, NCT01776424) trial, the main pivotal trial comparing rivaroxaban in combination with acetylsalicylic acid (ASA) versus ASA in a head-to-head comparison, showed that rivaroxaban in combination with ASA significantly reduced the composite of cardiovascular (CV) death, non-fatal stroke or non-fatal MI compared with ASA monotherapy in patients suffering from stable cardiovascular disease or PAD (hazard ratio [HR] 0.76; 95% confidence interval [CI] 0.66–0.86; p < .001). In addition, the net clinical benefit by which CV death, stroke, MI, fatal bleeding, or symptomatic bleeding into a critical organ are measured favored rivaroxaban plus ASA over ASA monotherapy (HR 0.80; 95% CI 0.70–0.91; p < .001), indicating that although more bleeds were observed, rivaroxaban combination therapy led to significant benefits. Furthermore, no significant differences were observed in terms of intracranial and fatal bleeding compared with ASA monotherapy11.
The use of direct oral anticoagulants in the treatment of acute venous thromboembolism in cancer patients
Published in Expert Review of Hematology, 2018
Hikmat Abdel-Razeq, Antoine Finianos, Ali T. Taher
Several other ongoing studies are testing rivaroxaban in various clinical conditions. The PRIORTY study is an open-label, multi-center, and randomized phase II trial designed to compare the safety and efficacy of rivaroxaban against subcutaneous dalteparin in patients with acute VTE and upper gastrointestinal, hepatobiliary, or pancreatic cancers. Rivaroxaban will be given at 15 mg orally twice daily for 3 weeks followed by 20 mg once daily for 21 weeks [40]. The CASTA-DIVA study is another ongoing non-inferiority open-label randomized multicenter trial designed to compare rivaroxaban and dalteparin in patients with active cancer and acute symptomatic VTE. Both the experimental and control treatments will be given for 3 months [41].