Xarelto
Xarelto Uses, Dosage, Side Effects, Food Interaction and all others data.
Xarelto is a highly selective direct factor Xa inhibitor. Inhibition of factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade, inhibits thrombin formation. Xarelto does not inhibit thrombin (activated factor II) and no effects on platelets have been demonstrated.
Xarelto is an anticoagulant which binds directly to factor Xa. Thereafter, it effectively blocks the amplification of the coagulation cascade, preventing the formation of thrombus. Xarelto is a unqiue anticoagulant for two reasons. First of all, it is does not involve antithrombin III (ATIII) to exert its anticoagulant effects. Secondly, it is an oral agent whereas the widely used unfractionated heparin and low molecular weight heparins are for parenteral use only. Although the activated partial thromboplastin time (aPTT) and HepTest (a test developed to assay low molecular weight heparins) are prolonged in a dose-dependant manner, neither test is recommended for the assessment of the pharmacodynamic effects of rivaroxaban. Anti-Xa activity and inhibition of anti-Xa activity monitoring is also not recommended despite being influenced by rivaroxaban.
| Trade Name | Xarelto |
| Availability | Prescription only |
| Generic | Rivaroxaban |
| Rivaroxaban Other Names | Rivaroxaban |
| Related Drugs | Xarelto, Praluent, Repatha, amlodipine, aspirin, propranolol, clopidogrel, Eliquis, warfarin, simvastatin |
| Weight | 10mg, 15mg, 20mg, , 2.5mg, 15mg + 20mg |
| Type | Tablet, (+ Free) Tablet, Bo Of (+ Free) Tablet, Film Coated, Film-coated Tablet, Oral Kit, Oral Tablet |
| Formula | C19H18ClN3O5S |
| Weight | Average: 435.881 Monoisotopic: 435.065569098 |
| Protein binding | Plasma protein binding is about 92% to 95% |
| Groups | Approved |
| Therapeutic Class | Oral Anti-coagulants |
| Manufacturer | Bayer Pharmaceuticals, Bayer Zydus Pharma, Bayer Health Care, Bayer Plc, Bayer Ag, Bayer Pharma Ag, Bayer Indonesia, Bayer Schering Pharma Ag |
| Available Country | India, Pakistan, United Kingdom, Canada, Saudi Arabia, United States, Indonesia, Germany, Nigeria, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Xarelto 2.5 mg:
- For the prevention of atherothrombotic events in adult patients after an Acute Coronary Syndrome (ACS) with elevated cardiac biomarkers (Troponin or CK-MB). It is co-administered with Aspirin alone or with Aspirin plus Clopidogrel orTidopidine.
Xarelto 10-20 mg:
- To reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation
- Deep vein thrombosis (DVT) & pulmonary embolism (PE) and reduction in the risk of recurrence of DVT and of PE
- For the prophylaxis of DVT, which may lead to PE in patients undergoing knee or hip replacement surgery
Xarelto is also used to associated treatment for these conditions: Cardiovascular Mortality, Deep Vein Thrombosis, Deep vein thrombosis recurrent, Myocardial Infarction, Pulmonary Embolism, Recurrent pulmonary embolism, Stroke, Systemic Embolism
How Xarelto works
Xarelto competitively inhibits free and clot bound factor Xa. Factor Xa is needed to activate prothrombin (factor II) to thrombin (factor IIa). Thrombin is a serine protease that is required to activate fibrinogen to fibrin, which is the loose meshwork that completes the clotting process. Since one molecule of factor Xa can generate more than 1000 molecules of thrombin, selective inhibitors of factor Xa are profoundly useful in terminating the amplification of thrombin generation. The action of rivaroxaban is irreversible.
Dosage
Xarelto dosage
Xarelto 2.5 mg:
The recommended dose is 2.5 mg twice daily. Patients should also take a daily dose of 75-100 mg Aspirin or a daily dose of 75-100 mg Aspirin in addition to either a daily dose of 75 mg clopidogrel or a standard daily dose of ticlopidine.
Xarelto 10-20 mg:
Nonvalvular Atrial Fibrillation: For patients with Creatinin Clearance >50 mL/min: 20 mg orally, once daily with the evening meal. For patients with Creatinin Clearance 15-50 ml/min: 15 mg orally, once daily with the evening meal
Treatment of DVT & PE: 15 mg orally twice daily with food for the first 21 days for the initial treatment of acute DVT or PE. After the initial treatment period, 20 mg orally once daily with food for the remaining treatment
Prevention in the risk of recurrence of DVT and of PE: 20 mg once daily with food
Prophylaxis of DVT following Hip replacement surgery: 10 mg once daily for 35 days
Prophylaxis of DVT following knee replacement surgery: 10 mg once daily for 12 days
Side Effects
The most common adverse reaction is bleeding. Increased risk of stroke after discontinuation in nonvalvular atrial fibrillation.
Toxicity
Excessive bleeding. Overdosages should be treated using activated charcoal and supportive measures such as mechanical compression and hemodynamic support. If bleeding is not controlled, the following procoagulants can be administered: activated prothrombin complex concentrate, prothrombin complex concentrate and recombinant factor VIIa. There is also a higher chance of post procedural hemorrhage compared to enoxaparin (1.55% vs. 1.39% respectively).
Precaution
Xarelto can cause bleeding. Promptly evaluate signs and symptoms of blood loss. Xarelto use not recommended in case of Prosthetic heart valves.
Interaction
CYP3A4, P-GP inhibitors and NSAIDs.
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
- Avoid St. John's Wort. Co-administration will decrease levels of this medication.
- Take with food. Xarelto 15-20mg dose should be taken with food as food significantly impacts the bioavailability at that dose.
- Take with or without food. Xarelto 10mg dose can be taken with or without food as it does not significantly impact the bioavailability at that dose.
Xarelto Drug Interaction
Major: aspirin, aspirin, aspirinModerate: omega-3 polyunsaturated fatty acidsUnknown: tadalafil, rosuvastatin, furosemide, atorvastatin, pregabalin, metoprolol, metoprolol, polyethylene glycol 3350, acetaminophen / hydrocodone, acetaminophen, tiotropium, budesonide / formoterol, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
Xarelto Disease Interaction
Major: bleeding, hepatic impairment, renal disease, valvular heart disease, unstable blood pressure
Volume of Distribution
The steady state Vd is 50 L
Elimination Route
Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. However, the 15-20 mg dose have a lower bioavailability if taken in the fasted state and consequently should be taken with food.
Half Life
The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly.
Clearance
Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h.
Elimination Route
Approximately two-thirds of rivaroxaban is excreted into urine (via active tubular secretion in which approximately 36% as unchanged drug and 30% as inactive metabolism). The remaining third of the administered dose is excreted via feces in which 7% is in the form of unchanged drug and 21% as inactive metabolites.
Pregnancy & Breastfeeding use
There are no adequate or well-controlled studies of Xarelto in pregnant women, and dosing for pregnant women has not been established.
Safety and efficacy of Xarelto have not been established in breast-feeding women
Contraindication
Active pathological bleeding & severe hypersensitivity reaction to Xarelto
Storage Condition
Protect from light, store below 30° C. Keep out of reach of children.
Innovators Monograph
You find simplified version here Xarelto
Xarelto contains Rivaroxaban see full prescribing information from innovator Xarelto Monograph, Xarelto MSDS, Xarelto FDA label
FAQ
What is Xarelto used for?
Xarelto is used to treat and prevent deep venous thrombosis , a condition in which harmful blood clots form in the blood vessels of the legs.
How safe is Xarelto?
Xarelto is safe to take for a long time. There do not seem to be any lasting harmful effects from taking it for many months and years.
How does Xarelto work?
Xarelto works by stopping a clotting factor called factor Xa from working. This thins your blood so it takes longer to clot.Xarelto works within a few hours of taking it.
What are the common side effects of Xarelto?
The common side effect of Xarelto is bleeding more easily than normal, such as having nosebleeds, heavier periods, bleeding gums and bruising. It tends to happen in the first few weeks of treatment or if you're unwell. Always carry your anticoagulant alert card with you.
Is Xarelto safe during pregnancy?
There are no controlled data in human pregnancy. This drug should be used during pregnancy only if the benefit outweighs the risk. Some authorities consider it contraindicated.
Is Xarelto safe during breastfeeding?
exposure of Xarelto via breastfed is seldom clinically relevant for the infant. A pediatric assessment of the infant found no detectable drug-related adverse effects.
Can I drink alcohol with Xarelto?
The alcohol can increase Xarelto effect and make you more likely to bleed.
When should I take Xarelto?
It's usual to take Xarelto once or twice a day. Take Xarelto just after you have eaten a meal or snack. It's important to take it with food to help your body absorb the whole dose.
Should I take Xarelto in morning or at night?
Once a day with your evening meal. Take your next dose at your regularly scheduled time.
Does Xarelto cause insomnia?
It's possible to have insomnia while you're taking Xarelto.
Can Xarelto cause kidney problems?
One of the severe side effects of Xarelto is that it can cause acute kidney injuries. In the past few years, medical researchers have recognized a new type of acute kidney injury: Anticoagulant-related nephropathy.
How long does Xarelto stay in my system?
Xarelto takes 2–4 hours for it to reach its full blood-thinning effect, and it leaves your system more quickly than warfarin—typically in about 24 hours.
Can I just stop taking Xarelto?
Do not stop taking Xarelto without talking to your doctor. If you stop taking Xarelto, the rate at which your blood clots will return to what it was before you started taking it, usually within a day or two of stopping.
Can I take Xarelto every other day?
You can take your dose at any time of day.
Who should not take Xarelto?
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Can Xarelto cause liver problems?
Xarelto has been shown to cause liver damage, particularly in men over 60 who have been on the medication for six months or more. Anyone who has taken Xarelto for any period of time is urged to get their liver function tested.
What happens if I overdose on Xarelto?
Seek emergency medical attention.Overdose may cause excessive bleeding.
