Drug Detail:Xarelto (Rivaroxaban [ riv-a-rox-a-ban ])
Drug Class: Factor Xa inhibitors
1. How it works
- Xarelto is a brand (trade) name for rivaroxaban which may be used to reduce blood clotting.
- Xarelto (rivaroxaban) is a selective inhibitor of factor Xa (FXa), an enzyme that plays a key role in the formation of substances that cause blood clotting. Through its action on FXa, Xarelto makes blood less likely to clot.
- Xarelto belongs to the class of drugs known as a factor Xa inhibitor. It may also be called a direct oral anticoagulant (DOAC) (this means it stops blood from clotting).
2. Upsides
- Xarelto may be used to reduce the risk of stroke and blood clot formation in people with nonvalvular atrial fibrillation (AF) (a condition characterized by a specific heart rhythm disturbance).
- May also be used to prevent the development of deep vein thrombosis (DVT) (blood clots in the deep veins) following hip or knee replacement surgery.
- Xarelto is also used in the treatment of DVT and pulmonary embolism (PE) (where blood clots lodge in the lungs), and to lower the risk of recurrent DVT and PE.
- Xarelto may be given to reduce the risk of major cardiovascular events (such as death, a heart attack, or a stroke) in people with long-term coronary artery disease (CAD) or peripheral arterial disease (PAD).
- Xarelto is also approved as a preventive measure against venous thromboembolism (blood clots) in hospitalized acutely ill medical patients at risk for thromboembolic complications who are not at high risk of bleeding.
- Approved to prevent blood clots and blood clot-related events in children aged 2 years and older with congenital heart disease who have undergone the Fontan procedure. Currently the only DOAC with this approval.
- May also be used in children from birth onwards to treat venous thromboembolism (VTE, or blood clots) or to reduce the risk of blood clots developing after at least 5 days of initial parenteral (injected or intravenous) anticoagulant treatment.
- Available as oral tablets (2.5mg, 10mg, 15mg, and 20mg) and an oral suspension formulation (1mg/mL) for children and adults who cannot swallow tablets. Xarelto is the only DOAC to offer a suspension formulation.
- Xarelto does not need to be monitored with regular blood tests.
- It is less likely than warfarin to interact with other drugs or foods; however, it does interact with some medicines.
- Xarelto is taken as an oral tablet once or twice daily.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Serious and sometimes fatal bleeding. The risk may be increased if Xarelto is taken with other drugs (such as aspirin, NSAIDs, and SSRIs) that also increase the risk of bleeding. However, Andexxa may be used to reverse the effects of Xarelto in people with uncontrolled or life-threatening bleeding.
- Abdominal pain, dyspepsia, toothache, fatigue, back or muscle pain, sinusitis, itching, and urinary tract infection are other reported side effects.
- May increase the risk of stroke when discontinued - do not discontinue except on a doctor's advice. Consider coverage with another anticoagulant if Xarelto needs to be stopped for any reason other than significant bleeding or completion of the course of therapy because premature discontinuation has been associated with thrombotic events (the formation of a blood clot within a blood vessel).
- May need to be temporarily discontinued prior to surgery.
- Reduce the dosage of Xarelto in people with kidney disease, and people should be monitored for the development of kidney disease while taking Xarelto.
- There is an increased risk of spinal or epidural hematomas resulting in long-term or permanent paralysis forming in people taking Xarelto who are also undergoing spinal puncture or epidural or spinal anesthesia. The risk is greater in those taking other medications that affect blood clotting (such as NSAIDs, aspirin), with a history of traumatic or repeated spinal procedures or a history of spinal deformity or surgery.
- May not be suitable for people with pre-existing bleeding disorders, with artificial heart valves, or in women who are pregnant or planning to become pregnant.
- May interact with several drugs including other anticoagulants or blood thinners, medicines used to treat HIV, some antibiotics, and some anticonvulsants.
- There is currently no generic version of Xarelto.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Take the 15mg and 20mg tablets with food. The 10mg tablet can be taken with or without food. May be taken with the evening meal.
- Take exactly as directed by your doctor. If you miss a dose and you take Xarelto once daily, take it as soon as you remember, but do not double up the dose if you don't remember until the next day.
- Tablets may be crushed and mixed with applesauce immediately before use in people who have difficulty swallowing. Alternatively, a suspension formulation is available. Follow up the dose with food.
- Avoid any activities that may increase your risk of bleeding or injury. Be careful when shaving or brushing your teeth.
- Do not stop suddenly without your doctor's advice as this increases the risk of blood clots.
- Report any unusual bleeding or bruising to your doctor, such as nosebleeds, bleeding gums, heavy menstrual bleeding, urine that looks pink or brown, blood in your stools, or bleeding that will not stop. Also, tell your doctor if you feel dizzy or weak or feel like you may pass out.
- Advise all doctors and dentists that you are taking Xarelto before any invasive or dental procedure is scheduled.
- Xarelto may also increase your risk of bleeding from a minor fall or bump on the head. Contact your doctor if you experience an injury or have bleeding that will not stop. Call 911 if you experience severe or unstoppable bleeding, pink or brown urine, red or black tar-like stools, coughing, or vomiting up blood or blood clots (may look like coffee grounds). Also seek urgent medical help with any symptoms of a stroke (such as sudden dizziness, headache or loss of vision; difficulty with speech or slurring of your words, one-sided facial drooping) or signs of a blood clot (sudden, severe shortness of breath; pain, heat or swelling in a limb).
- Always check with your doctor or pharmacist that Xarelto is compatible with other medications (including herbal remedies or products bought over the counter) before taking them.
- Do not stop taking Xarelto suddenly. Your doctor will advise you on how to discontinue Xarelto when or if you no longer require it.
5. Response and effectiveness
- Xarelto starts to inhibit blood clotting within one to two hours. Peak effects are seen two to four hours after taking a tablet. Effects start to wear off after 24 hours.
6. Interactions
Medicines that interact with Xarelto may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Xarelto. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with Xarelto include:
- amiodarone
- anticonvulsants such as carbamazepine, phenytoin or valproic acid
- apixaban
- corticosteroids, such as prednisone and methylprednisone
- dabigatran
- diltiazem
- medications that inhibit or induce CYP3A4 enzymes, such as erythromycin, ketoconazole, or ritonavir
- methotrexate
- mifepristone
- NSAIDs, such as ibuprofen, diclofenac, etodolac, and naproxen
- rifampin
- St John's Wort
- tinzaparin
- warfarin.
In general, any medicine that can increase the risk of bleeding (such as clopidogrel, SSRI antidepressants [eg, citalopram, duloxetine, fluoxetine, venlafaxine], fish oils) may interact with Xarelto.
Note that this list is not all-inclusive and includes only common medications that may interact with Xarelto, You should refer to the prescribing information for Xarelto for a complete list of interactions.