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Anticoagulants: Xarelto, a new oral direct factor Xa inhibitor


Xarelto is a medicine that contains the active substance Rivaroxaban; it is used for the following in adults : to prevent venous thromboembolism ( VTE ) in patients who are undergoing surgery to replace a hip or knee; to prevent stroke caused by a blood clot in the brain and systemic embolism in patients with non-valvular atrial fibrillation; to treat deep vein thrombosis ( DVT ) and pulmonary embolism, and to prevent DVT and pulmonary embolism from re-occuring; to prevent atherothrombotic events after an acute coronary syndrome.
Acute coronary syndrome is a group of conditions that includes unstable angina and myocardial infarction. It is used together with antiplatelet medicines, which prevent the blood from clotting.

Xarelto is available as tablets ( 2.5, 10, 15 and 20 mg ).

When Xarelto is used to prevent venous thromboembolism in patients undergoing hip or knee replacement surgery, the recommended dose is 10 mg once daily. Treatment with Xarelto should start six to 10 hours after surgery, provided that the patient is no longer bleeding from the site of surgery. Treatment should continue for five weeks in patients who have had hip replacement surgery, and for two weeks in patients who have had knee replacement surgery. The tablets can be taken with or without food.
When Xarelto is used to prevent stroke or systemic embolism in patients with non-valvular atrial fibrillation, the recommended dose is 20 mg once daily. Treatment with Xarelto should be continued provided the benefit outweighs the risk of bleeding. The tablets are taken with food.
When Xarelto is used to to treat deep vein thrombosis and pulmonary embolism or to prevent DVT and pulmonary embolism from re-occuring, the recommended dose for the initial treatment of acute deep vein thrombosis is 15 mg twice daily for the first three weeks followed by 20 mg once daily. The tablets are taken with food.
When Xarelto is used to prevent atherothrombotic events in patients who have had acute coronary syndrome, the recommended dose is 2.5 mg taken twice a day. It should be taken either in combination with Acetylsalicylic acid ( Aspirin ) or together with Acetylsalicylic acid and Clopidogrel ( Plavix ) or Acetylsalicylic acid and Ticlopidine ( Tiklid ). Treatment should start as soon as possible after the acute coronary syndrome has stabilised. The benefits of ongoing treatment should be regularly evaluated by the phisicians against the risk of bleeding.
In patients with reduced kidney function the dose of Xarelto may need to be adjusted.

Patients undergoing hip or knee replacement surgery and patients with atrial fibrillation, deep vein thrombosis, pulmonary embolism or who have had acute coronary syndrome are at a risk of blood clots forming or re-occuring and moving to another part of the body. The active substance in Xarelto, Rivaroxaban, is a factor Xa inhibitor. This means that it blocks factor Xa, an enzyme that is involved in the production of thrombin. Thrombin is central to the process of blood clotting. By blocking factor Xa, the levels of thrombin decrease, which reduces the risk of blood clots forming in the veins and arteries, and also treats existing clots.

For the prevention of venous thromboembolism after surgery, Rivaroxaban was compared with Enoxaparin ( Clexane, Lovenox ) in three main studies, two in patients undergoing hip replacement surgery and one in patients undergoing knee replacement surgery. In hip replacement surgery, the first study compared five weeks of Rivaroxaban with five weeks of Enoxaparin in around 4,500 patients, and the second study compared five weeks of Rivaroxaban with two weeks of Enoxaparin in around 2,500 patients. The third study compared two weeks of Rivaroxaban with two weeks of Enoxaparin in around 2,500 patients undergoing knee replacement surgery. In all of the studies, the effectiveness was measured by looking at the number of patients who either had blood clots in the veins or in the lungs, or who died of any cause during the treatment period.
For the prevention of stroke and systemic embolism, Rivaroxaban was compared with Warfarin ( Coumadin ) in one main study in 14,264 patients with non-valvular atrial fibrillation. The main measure of effectiveness was the number of patients who had either a stroke or a blood clot in a blood vessel.

For deep vein thrombosis and pulmonary embolism, Rivaroxaban was compared with Enoxaparin given in combination with a vitamin K antagonist ( VKA ) in two main studies in 3,449 patients with acute deep vein thrombosis and 4,833 patients with pulmonary embolism, respectively. The main measure of effectiveness was the number of patients who had either a DVT recurrence or pulmonary embolism.
For the prevention of atherothrombotic events in patients who have had acute coronary syndrome, Rivaroxaban was compared with placebo in one main study involving over 15,000 patients who had recently had an acute coronary syndrome. All patients also received standard antiplatelet medicines. The main measure of effectiveness was the number of patients who had an event such as a myocardial infarction or stroke or who died due to heart problems during the study.

In the three studies in patients undergoing surgery, Rivaroxaban was more effective than Enoxaparin in preventing the formation of blood clots or death. In the first study in hip replacement surgery, 1% of the patients who completed treatment with Rivaroxaban either had blood clots or died ( 18 out of 1,595 ), compared with 4% of the patients receiving Enoxaparin ( 58 out of 1,558 ). In the second study, 2% of the patients taking Rivaroxaban had blood clots or died ( 17 out of 864 ), compared with 9% of the patients receiving Enoxaparin ( 81 out of 869 ). After knee replacement surgery, 10% of the patients receiving Rivaroxaban had blood clots or died ( 79 out of 824 ), compared with 19% of the patients receiving Enoxaparin ( 166 out of 878 ).
In the study in patients with non-valvular atrial fibrillation, 2.7% ( 188 out of 6958 ) of patients treated with Rivaroxaban had either a stroke or a blood clot in a blood vessel, compared with 3.4% ( 241 out of 7004 ) of patients receiving Warfarin.
In the study in patients with acute deep vein thrombosis, 2.1% ( 36 out of 1,731 ) of patients treated with Rivaroxaban had either DVT recurrence or pulmonary embolism, compared with 3.0% ( 51 out of 1,718 ) of patients receiving Enoxaparin / vitamin K antagonist.
In the study in patients with pulmonary embolism, 2.1% ( 50 out of 2,419 ) of patients treated with Rivaroxaban had a recurrence of either deep vein thrombosis or pulmonary embolism, compared with 1.8% ( 44 out of 2,413 ) of patients receiving Enoxaparin / vitamin K antagonist.
In the study in patients who have had acute coronary syndrome, 6.1% ( 313 out of 5,114 ) of patients treated with Rivaroxaban had an event such as a myocardial infarction, stroke or death due to heart problems during the study, compared with 7.4% ( 376 out of 5,113 ) of patients receiving placebo.

The most common side effects with Xarelto ( seen in between 1 and 10 patients in 100 ) are anaemia, dizziness, headache, bleeding in various parts of the body, hypotension, haematoma, pain in the stomach and belly, dyspepsia, nausea, constipation, diarrhoea, vomiting, pruritus, rash, ecchymosis, pain in the extremities, decreased kidney function, fever, peripheral oedema, decreased general strength and energy, increased levels of some liver enzymes in the blood and oozing of blood or fluid from the surgical wound in patients undergoing surgery.

Xarelto must not be used in people who are hypersensitive ( allergic ) to Rivaroxaban or any of the other ingredients. It must not be used in patients who are bleeding or in patients who have a liver disease or a condition that is associated with an increased risk of bleeding. Xarelto must not be used together with any other medicines called anticoagulants that prevent the blood from clotting, except in specific conditions. Xarelto must not be used in women who are pregnant or breast-feeding. ( Xagena )

Source : European Medicines Agency ( EMA ), 2013

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